Spectrum of activity and adverse drug reactions of antifungal drugs: fluconazole, terbinafine, ketoconazole. Application in children. Laser therapy for fungus

Itraconazole and terbinafine are the most popular antifungal drugs. They are best suited for the treatment of onychomycosis. Onychomycosis general fungal infection nails. Itraconazole and terbinafine are also associated with a number of potentially dangerous drug interactions.

Itraconazole capsules need an acidic gastric environment, so it is recommended to take it with meals for better assimilation, as the products stimulate the production of hydrochloric acid it is responsible for the acidity of the environment in the stomach. If you are taking other drugs such as inhibitors proton pump, H-2 antagonists, antacids, etc., which can reduce the acidity in the stomach, then itraconazole should be taken one to two hours apart. Unlike Itraconazole capsules, Itraconazole does not need acidity in the mixture. gastric juice for absorption, so it does not need to be taken with food. Itraconazole remains in the nails for six to nine months after cessation of therapy. Drugs that can increase the concentration of itraconazole: macrolides (clarithromycin), antibiotics (erythromycin) and inhibitors such as ritonavir. Itraconazole should not be used with the following drugs:

Antiarrhythmic drugs such as digoxin, quinidine

Anticonvulsants such as carbamazepine

Rifabutin

Anticancers like busulfan, docetaxel, vinca alkaloids

Antipsychotics (pimozide)

Benzodiazepines such as alprazolam, diazepam, midazolam, triazolam

Blockers calcium channels: dihydropyridines, verapamil

Gastrointestinal motility agents (cisapride) and HMG-CoA reductases such as atorvastatin, lovastatin, simvastatin.

Complications such as bidirectional ventricular tachycardia, ventricular fibrillation, cardiac arrest, and/or sudden death can occur if you take the above drugs and itraconazole at the same time. Researches show increased risk acute necrosis skeletal muscles with the simultaneous use of itraconazole and HMG-CoA reductases. Itraconazole increases plasma concentrations of benzodiazepines and causes sedative and hypnotic effects.

On the other hand, Terbinafine is well absorbed after oral administration in 70% of cases, the acidity of gastric juice does not affect digestibility.
Rbinafine is lipophilic, meaning that it has a high affinity of reactive species to combine with lipids. After oral administration, the drug is found in adipose tissue, stratum corneum, skin, epidermis and nails, terbinafine is 99% protein bound. It is not metabolized in the cytochrome P450 system, unlike itraconazole. Terbinafine remains in the nails for up to nine months after cessation of therapy. Medicines that can reduce the concentration of Terbinafine: anticonvulsants(carbamazepine, phenobarbital, phenytoin), antimicrobials (isoniazid, rifabutin, rifampicin), gastric acid suppressors/neutralizers and nevirapine. Terbinafine should be taken with caution if you are taking warfarin because studies show that terbinafine interacts with warfarin. There are studies showing the interaction of the drug with contraceptives and hormonal drugs, theophylline, phenytoin, thiazide drugs, diuretics, beta-blockers and calcium channel blockers.

Basic information:

1. Itraconazole and terbinafine antifungal drugs. Best suited for the treatment of onychomycosis.

2. Itraconazole capsules require an acidic gastric environment and are recommended to be taken with food for better absorption.

3. Drugs such as proton pump inhibitors, H-2 antagonists, antacids, etc., which can reduce stomach acid should not be taken with Itraconazole. Mekstura Itraconazole does not need gastric acidity.

4. The acidity of gastric juice does not affect the absorption of Terbinafine.

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Systemic therapy is the most effective and reliable treatment onychomycosis. To systemic therapy resort when treatment local funds turns out to be ineffective.

INDICATIONS FOR SYSTEMIC THERAPY

Clinical characteristics of onychomycosis:

clinical form:

distal-lateral (late stages),

proximal,

total;

damage to more than half of the nail;

involvement in the matrix process;

pronounced changes in the nail (hyperkeratosis, onycholysis);

damage to more than 2-3 nails

Failure of local therapy

The combination of onychomycosis with a widespread lesion of the skin or hair

Although systemic therapy most often provides a cure for onychomycosis, its use is associated with a number of difficulties. With systemic administration, the drug does not enter the nails immediately, but first overcomes numerous obstacles. Its concentration in the nails is much less than with topical application. For this concentration to become effective, i.e. destroyed fungi or inhibited their growth, you can, firstly, increase the concentration as a result of increasing the dose of the drug. However, increasing the dose will increase the risk of side and toxic effects. To overcome these difficulties, new drugs are used that accumulate in the nail with repeated administration. Secondly, you can choose a drug that is effective in a small concentration. Modern drugs with very low MICs for onychomycosis pathogens meet this requirement.

Systemic antifungals

There are only 8 systemic antimycotics. Of these, griseofulvin, terbinafine, ketoconazole and itraconazole are widely used in the treatment of onychomycosis, and fluconazole is currently being introduced into therapy. All these drugs are administered orally.

The main criteria that determine the effectiveness of a systemic antifungal drug in onychomycosis:

- antifungal activity and spectrum of action;

- pharmacokinetics (the ability to quickly penetrate the nails, accumulate and linger in them);

- safety.

Not all systemic therapies meet each of these criteria. When prescribing them, one should take into account the characteristics of each case of onychomycosis, the patient's condition, concomitant diseases and their therapy. Below we present the main characteristics of each drug.

Griseofulvin

The antifungal antibiotic griseofulvin is the first systemic drug for the treatment of dermatophyte infections. Griseofulvin has been used in the treatment of onychomycosis for over 30 years.

Griseofulvin acts only on dermatophytes, the IPC for them is in the range of 0.1-5 mg / l.

Griseofulvin is not completely absorbed from the gastrointestinal tract, absorption improves when taken with food. In order to improve absorption, micronized (finely dispersed) and ultramicronized forms have been developed. Taking 500 mg of griseofulvin provides maximum concentrations of 0.5-2.0 mg / l, which does not always exceed the MIC. Treatment of onychomycosis is usually carried out with griseofulvin at a dose of 1000 mg / day.

In the blood, griseofulvin partially binds to plasma proteins. Metabolism is carried out in the liver, more than a third of the drug is excreted in the feces.

Although griseofulvin is a lipophilic substance that can accumulate in tissues, its affinity for keratin is rather low. 48-72 hours after discontinuation of the drug, it is no longer found in the stratum corneum, so the treatment of onychomycosis with griseofulvin is carried out constantly, until a healthy nail plate grows back. In general, the kinetics of griseofulvin in the nail has been little studied.

Griseofulvin for oral administration is available in 1 tablets and in the form of an oral suspension. Tablets contain 125 or 500 mg of griseofulvin, in a package of 25 or 1000 tablets of 125 mg, 25 or 250 tablets of 500 mg. 1 ml of suspension contains 0.1 g of griseofulvin.

Enhanced absorption forms include micronized griseofulvin (griseofulvin-forte) available in 125, 250, or 500 mg tablets and ultramicronized griseofulvin in 125 mg tablets. In recent decades, micronized forms have been most widely used.

The dose of griseofulvin is set in accordance with the age and body weight of the patient. The daily dose for adults of the micronized form of griseofulvin for onychomycosis is from 500 to 1000 mg (in 2-4 doses), but not less than 10 mg / kg. The duration of treatment is about 4-6 months for nails on the hands, from 9 to 12, sometimes up to 18 months on the legs.

For children weighing less than 25 kg, the daily dose is prescribed at the rate of 10 mg / kg (or in 2 doses of 5 mg / kg), children weighing more than 25 kg are given 250-500 mg / day. In general, it is not recommended to prescribe griseofulvin for the treatment of onychomycosis in children.

When treating with ultramicronized griseofulvin, the dose is reduced by a third or even half.

When prescribing griseofulvin with other drugs, their possible interaction. Barbiturates reduce the absorption of griseofulvin. Griseofulvin weakens the action indirect anticoagulants, reduces the concentration of cyclosporine. It should be remembered that griseofulvin can significantly weaken the effect of hormonal contraceptives.

Most common side effects when taking griseofulvin - nausea, sometimes vomiting, a feeling of discomfort in the epigastrium, headache and dizziness. In addition, griseofulvin has a photosensitizing property. Toxic effects include an effect on the liver, as well as rare cases of agranulocytosis. Griseofulvin is not prescribed to pregnant and lactating mothers.

Terbinafine (Lamisil)

Terbinafine is a synthetic allylamine drug that has been used in the treatment of onychomycosis since the early 1990s.

The average MIC of terbinafine for dermatophytes does not exceed 0.06 mg/L. In addition, in vitro terbinafine acts on many other molds. The efficacy of terbinafine in non-dermatophytic mold infections is unknown. Many yeast mushrooms, in particular Candida albicans, are resistant to terbinafine in MICs up to 128 mg/l.

Terbinafine is well absorbed in the gastrointestinal tract, food intake does not affect absorption. Peak plasma concentrations at doses of 250 and 500 mg are about 0.9 and 1.7-2 mg/l, respectively. This far exceeds the MIC for susceptible fungi. Concentrations are directly dependent on the dose and increase with its increase and with repeated administration of the drug. In the blood, terbinafine binds to proteins of all plasma fractions and to formed elements.

Terbinafine is metabolized in the liver. 15 of its metabolites are known, all of them are inactive. About 80% of the drug is excreted in the urine. Lack of liver or kidney function slows down excretion.

At the distal edges of the nails, terbinafine appears on average at the 8th week from the start of treatment. Terbinafine penetrates the nail plate primarily through the matrix, but also through nail bed. After discontinuation of treatment, terbinafine in effective concentrations is retained in the nails for 4-6 weeks.

Terbinafine hydrochloride for oral administration is available in tablets of 125 and 250 mg, in a package of 14 or 28 tablets.

In the treatment of onychomycosis caused by dermatophytes, terbinafine is used at a dose of 250 mg / day. AT last years terbinafine is prescribed in short courses: for nail infections on the hands for a period of 6 weeks (1.5 months), for infections of the toenails for a period of 12 weeks (3 months). The effectiveness of terbinafine at a dose of 500 mg per day for 3 months in nail candidiasis was studied. Possible pulse therapy with terbinafine at a dose of 500 mg / day in one-week courses for 3-4 months.

Doses for children are 62.25 mg (half a tablet of 125 mg) with a body weight of up to 20 kg, 125 mg for up to 40 kg, children weighing over 40 kg are given a full dose. Experience in treating children with terbinafine is limited.

When prescribing terbinafine, one should take into account its possible interaction with drugs metabolized by the liver. Rifampicin decreases and cimetidine and terfenadine increase terbinafine concentrations.

The most common side effects of terbinafine treatment include nausea, a feeling of fullness or abdominal pain, and sometimes decreased appetite. Loss or change in taste during treatment has been described. In addition to dyspeptic symptoms, urticaria may develop during treatment with terbinafine. Toxic effects - hepatotoxicity, agranulocytosis, damage to the organ of vision, and some others are very rare. Terbinafine should not be given to persons with liver disease. In renal insufficiency, the dose of terbinafine should be reduced by half if creatinine clearance exceeds 50 ml/min. Terbinafine is not prescribed to pregnant and lactating mothers.

Ketoconazole (nizoral, oronazole)

This synthetic drug from the azole class has been used in the treatment of mycoses since the late 70s.

Ketoconazole has a wide range actions. The average MIC for dermatophytes is about 0.1-0.2 mg / l, for Candida albicans - about 0.5 mg / l. Many molds that cause non-dermatophytic onychomycosis are resistant to ketoconazole.

Ketoconazole is not completely absorbed from the gastrointestinal tract. Absorption is worse with reduced acidity and improves when taken with food. Taking 200 mg of ketoconazole leads to a peak plasma concentration of about 3 mg / l, taking 400 mg - 5-6 mg / l. These concentrations exceed the MIC for susceptible pathogens.

In the blood, ketoconazole is almost completely bound to plasma proteins and is extensively metabolized in the liver. Metabolites are inactive, most of them are excreted in the feces.

Ketoconazole has a high affinity for keratin. The drug enters the nails through the matrix and the nail bed, it can be detected on the 11th day from the start of treatment. Although ketoconazole appears to be retained in the nail for some time after discontinuation of treatment, the kinetics of the drug in the nail has not been well studied.

Ketoconazole for oral administration is available in 200 mg tablets, in a package of 10, 20 or 30 tablets.

With onychomycosis, ketoconazole is prescribed at a dose of 200 mg / day. The drug is best taken with food. Treatment takes 4-6 months for onychomycosis of the hands and 8-12 months for onychomycosis of the feet.

For children weighing 15 to 30 kg, ketoconazole is prescribed 100 mg (half a tablet). Children with greater body weight are given the full dose. In general, ketoconazole should not be used to treat onychomycosis in children.

When prescribing ketoconazole, it is necessary to take into account its possible interaction with many drugs. Antacids and drugs that reduce gastric secretion interfere with the absorption of ketoconazole. Ketoconazole increases half-life antihistamines terfenadine, astemizole, and cisapride; the combined use of these drugs can lead to the development of arrhythmia. Ketoconazole increases the half-life of midazolam, triazolam, cyclosporine and potentiates the effect of indirect anticoagulants. Ketoconazole concentrations decrease when administered with rifampicin and isoniazid, and change when administered with phenytoin.

Common side effects of ketoconazole include nausea, less often vomiting, decreased appetite. Taking the drug with meals or at night, you can avoid these phenomena.

The main toxic effect of ketoconazole is its effect on the liver. An increase in the concentration of hepatic transaminases during treatment is observed in 5-10% of patients taking ketoconazole. If these phenomena become constant or intensify, the drug should be discontinued. Severe liver injury is rare, but long-term treatment onychomycosis their likelihood increases. The effect of ketoconazole on steroid metabolism in the human body may cause changes in cholesterol levels and steroid hormones in the blood, but these changes are not clinically manifested. Do not prescribe ketoconazole to pregnant and lactating mothers.

Itraconazole (orungal)

This synthetic drug from the azole class has been used in the treatment of onychomycosis since the early 90s.

The spectrum of action of itraconazole is the widest among all antifungal agents for oral administration. Itraconazole acts on dermatophytes (with an average MIC of about 0.1 mg / l), different types Candida (with an MIC in the range of 0.1-1 mg / l) and many molds found in onychomycosis.

Itraconazole is not completely absorbed from the gastrointestinal tract. Absorption of the drug is worse at low acidity, but improves significantly when taken with food. After taking 100 mg of the drug, the maximum plasma concentrations are 0.1-0.2 mg / l, rising to 1 mg / l when taking 200 mg and up to 2 mg / l when taking 400 mg. This exceeds the MIC for most pathogenic fungi.

In the blood, Itraconazole is almost completely bound to plasma proteins and is extensively metabolized in the liver. The main metabolite is hydroxyitraconazole, which is not inferior in activity to itraconazole. Most of metabolites are excreted in the feces.

The keratophilicity of itraconazole provides it high concentrations in the skin and nails, 4 times higher than plasma. At the distal ends of the nail plates, itraconazole can be detected after 1 week of treatment. Itraconazole penetrates into the nail plate both through the matrix and immediately through the nail bed. The drug accumulates in the matrix and is excreted only when a new nail plate grows, therefore, the effective concentration of the drug after its withdrawal is maintained in the nails on the hands for another 3 months, and on the legs - for 6-9 months with a 3-month course of treatment.

Itraconazole for oral administration is available in capsules containing 100 mg of the drug, in a package of 4 or 15 capsules.

It is possible to treat onychomycosis with short courses of 200 mg of itraconazole every day for 3 months. In recent years, the technique of pulse therapy has received more recognition, when itraconazole is prescribed at 400 mg / day (for 2 doses) for 1 week. In the treatment of infections on the hands, 2 courses of pulse therapy are prescribed at a one-week course every month. In the treatment of infections on the legs, 3 or 4 courses are prescribed, depending on the form and severity of the lesion. Itraconazole should be taken with meals, for 1 dose no more than 200 mg (2 capsules). Because experience with itraconazole in pediatrics is limited, dosing recommendations for the drug in children have not been developed.

When prescribing itraconazole, the risk of interaction with other drugs is taken into account. Antacids and agents that reduce gastric secretion interfere with the absorption of itraconazole. Do not prescribe itraconazole together with astemizole, terfenadine or cisapride due to the possibility of developing arrhythmias. Itraconazole also increases the half-life of midazolam and triazolam, digoxin, cyclosporine, and potentiates the action of indirect anticoagulants. Rifampicin and phenytoin reduce itraconazole concentrations.

The most common side effects are nausea, epigastric discomfort and abdominal pain, and constipation. A small proportion of patients have a transient increase in the concentration of hepatic transaminases. If it does not decrease or symptoms of hepatitis appear, then treatment is stopped. Itraconazole should not be used in patients with liver disease. At these doses, itraconazole has no effect on the metabolism of steroid hormones. Pregnant and lactating mothers are not treated with itraconazole for onychomycosis.

fluconazole (diflucan)

Fluconazole, a drug from the azole class, was obtained in 1982. It has been used in onychomycosis in recent years.

The spectrum of action of fluconazole is wide. MIC for dermatophytes is up to 1 mg/l, for Candida albicans - 0.25 mg/l. The activity of fluconazole against various molds seems to be less than against yeasts.

Fluconazole is almost completely absorbed from the gastrointestinal tract. When administered orally 50 mg of the drug, the maximum plasma concentration is about 1 mg / l, with repeated administration it reaches 2-3 mg / l. This exceeds the MIC for many sensitive fungi.

In plasma, no more than 12% of the drug binds to proteins, the main amount is in free form. Fluconazole is very poorly metabolized by the liver, excreted by the kidneys mainly unchanged. Elimination of the drug depends on the rate glomerular filtration.

High concentrations of fluconazole are created in the skin and nails. The hydrophilicity of fluconazole, which is in free form, allows it to quickly penetrate into the nail plate through the nail bed. In the nail plate, fluconazole can be detected already a few hours after ingestion. Fluconazole has some keratinophilicity and is excreted from the stratum corneum more slowly than from plasma.

For oral administration, the drug is available in the form of gelatin-coated capsules of 50, 100, 150 or 200 mg, in a package of 1, 7 or 10 capsules.

In the treatment of onychomycosis, fluconazole is used according to the pulse therapy regimen, prescribing 150 mg (once) per week. The duration of such therapy depends on the form and localization of onychomycosis: about 6 months with damage to the nails on the hands, up to 12 months - on the legs. Abroad, a pulse therapy regimen is used with the appointment of 300 mg per week (2 capsules of 150 mg) for 9 months. Doses for children should not exceed 3-5 mg/kg per week.

The possible interaction of fluconazole with other drugs should be taken into account. Fluconazole should not be co-administered with cisapride. Fluconazole increases the half-life of hypoglycemic agents - glibenclamide, chlorpropamide, tolbutamide, potentiates the action of indirect anticoagulants, increases the concentration of phenytoin and cyclosporine. Rifampicin reduces fluconazole concentrations.

When prescribing fluconazole for long courses in large doses take into account the state of kidney function.

Side effects include nausea and abdominal discomfort. Treatment of onychomycosis with small doses of fluconazole once a week is usually not accompanied by any side and toxic effects.

Choice of drug

When choosing a remedy for the systemic treatment of onychomycosis, one must remember that each drug can provide a cure with a reasonable and reasonable prescription.

We consider the spectrum of its action to be the main criterion determining the choice of a systemic drug. The spectrum should include fungi isolated from affected nails. In this regard, the etiology of onychomycosis, according to the cultural study, should be known to the doctor. If the etiology is unknown or several fungi are isolated, a broad-spectrum drug is prescribed, including both dermatophytes and fungi. genus Candida, and mold non-dermatophyte fungi (Table 4.2.1).

Table 4.2.1

With a known etiology, the choice of the drug is determined by the type of fungus isolated in the culture. For onychomycosis caused only by dermatophytes, terbinafine or griseofulvin is prescribed. With onychomycosis caused by Candida mushrooms, and for candidal paronychia, itraconazole, ketoconazole, or fluconazole are indicated. For onychomycosis caused by non-dermatophyte molds, itraconazole is used.

We consider the second criterion clinical form onychomycosis, severity and localization of the lesion. In the treatment of fungal infections, affecting the nails on the legs, with severe hyperkeratosis and matrix involvement, requires long-term treatment. In these cases, griseofulvin or ketoconazole are often ineffective and unsafe in terms of side effects and toxic effects. For onychomycosis of the toes, itraconazole and terbinafine are the drugs of choice.

If you still have to prescribe griseofulvin and ketoconazole, then systemic treatment they are best combined with local therapy with antifungal agents, removal of the affected nail plate. This increases the effectiveness of the treatment and helps to reduce its duration.

The third criterion is the safety of treatment, the risk of side and toxic effects. Security issues are discussed below.

Duration of treatment

The duration of treatment for onychomycosis depends on the growth rate of the nail. The growth rate is determined by localization (toenails grow more slowly), the age of the patient and comorbidities- in elderly and debilitated patients, persons with chronic systemic diseases or previous pathology of the nails, they grow more slowly.

On average, healthy nails on the hands grow back in 4-6 months, on the legs - in 12-18 months. These terms determine the duration of treatment with griseofulvin and ketoconazole, as well as fluconazole.

Terbinafine and, to a greater extent, itraconazole are able to accumulate in the nail and linger in it for a long time after discontinuation of treatment. This allows you to reduce the duration of treatment by using short courses, intermittent therapy regimens and pulse therapy. However, the duration of treatment recommended for such schemes is only indicative; in some cases, if the toenails are affected with severe hyperkeratosis or dystrophic phenomena, the treatment has to be extended.

Methods of prescribing drugs

There are 4 destination schemes systemic drugs with onychomycosis.

1. Standard regimen, providing for daily intake usual dose drug during the entire period of treatment. The duration of treatment corresponds to the time of regrowth of the nail plate. According to this scheme, you can prescribe any systemic drug.

2. A shortened regimen, in which the treatment period is shorter than the nail regrowth time. Treatment is carried out with usual or increased doses. According to this scheme, itraconazole and terbinafine can be used, capable of for a long time linger in the nails after stopping treatment.

3. An intermittent, or intermittent, regimen provides for the appointment of a regular or increased dose of the drug in several short courses. The intervals between these courses are equal to the duration of the courses themselves, for example, a weekly course with a weekly interval. According to this scheme, itraconazole and terbinafine can be used, which accumulate and linger for a long time in the nails, and, in principle, all lipophilic drugs. The discontinuous scheme has not yet received wide acceptance.

4. Scheme of pulse therapy. According to this scheme, an increased dose of the drug is prescribed in short courses at intervals exceeding the duration of the courses themselves. Treatment may be short, as with itraconazole, or timed to nail regrowth, as with fluconazole.

The most common prescribing regimens used worldwide are given in Table. 4.2.2.

Table 4.2.2

* In the practice of domestic dermatologists, it is customary to change the regimen during treatment with griseofulvin: in the 1st month, 1000 mg of the drug is prescribed every day, in the 2nd month - every other day, in the 3rd and the rest - 1 time in 3 days.

The advantage of short, intermittent therapy and pulse therapy regimens is their safety in terms of side and toxic effects and convenience for the patient while maintaining high efficiency. However, the standard regimen of treatment with any drug gives statistically best performance cured.

Treatment safety

Security, i.e. the absence of serious side and toxic effects of the drug is one of the main requirements for any systemic therapy. First of all, it should be said that none of the antifungal agents used is devoid of side effects and toxic action. In general, with a reasonable prescription of drugs, all these side effects are transient, do not pose a threat to the life and health of the patient, and are almost always easily tolerated. Severe disorders that complicate treatment with systemic drugs are very rare and refer to either anaphylaxis or idiosyncrasy.

According to the pharmacokinetic properties that determine the distribution and metabolism of the drug in the patient's body, and hence the possibility of certain side effects, all presented in Table. 4.2.2 drugs can be divided into 2 groups. One group includes lipophilic drugs: griseofulvin, terbinafine, ketoconazole and itraconazole. They are not completely absorbed in the intestine, they are found in the blood mainly in the form associated with plasma proteins, accumulate in tissues, undergo intensive metabolism in the liver and are excreted in an altered form. The only representative of the other group is the hydrophilic drug fluconazole.

General pharmacokinetic properties cause some side effects common to all listed drugs.

So, suction digestive tract of all 4 lipophilic drugs can be complicated by dyspeptic symptoms: nausea, discomfort in the abdomen, sometimes pain, vomiting. Intensive metabolism in the liver predetermines the possibility of hepatotoxic effects, manifested by an increase in the concentration of hepatic transaminases, alkaline phosphatase. All of these effects can be prevented by prescribing therapeutic doses drugs strictly according to the indications in compliance with the recommended method of application.

Fluconazole - relatively safe drug, as evidenced by the extensive experience of its application in deep mycoses. Side effects of fluconazole are also similar to those of other drugs - dyspepsia and very rare cases. toxic hepatitis. Features of the side and toxic effects of each of those included in the table. 4.2.2 antifungals are shown above in the description of these drugs.

It should be recognized that the risk of toxic effects depends on the effectiveness of the drug. The lower the effectiveness of the drug, the larger its doses have to be prescribed. Probability toxic influences also depends on the pharmacokinetics. Drugs with a high affinity for keratin that accumulate in the nails can be given in shorter courses. The shorter the treatment period, the less likely unwanted effects.

the least dangerous are pulse therapy regimens, intermittent and shortened regimens;

the appointment of the drug must be etiologically justified. If the spectrum of action of the drug does not include the isolated pathogen, it should not be prescribed even in large doses;

duration of treatment traditional means can be reduced by using combination therapy or intermittent regimen;

interactions with other drugs should be taken into account; no systemic drug should be given to patients with liver disease;

no systemic drug should be prescribed during pregnancy and lactation.

The low efficiency and relatively low ability to accumulate in the nails cause a greater risk of using traditional systemic agents griseofulvin and ketoconazole. These drugs are prescribed for standard scheme for up to 1 year, sometimes longer. The frequency of side and toxic effects is highest when using griseofulvin and ketoconazole. With the advent of modern antifungal agents, neither griseofulvin nor ketoconazole is recommended for use as monotherapy for onychomycosis.

If a doctor has no other drugs in his arsenal, except for griseofulvin or ketoconazole, he should think about how to make treatment with these drugs safe while maintaining effectiveness. There are two solutions to the problem. Firstly, it is possible to shorten the duration of treatment, and at the same time increase its effectiveness by combination therapy using local antifungal drugs and aids. Secondly, an intermittent regimen can be applied, periodically (no longer than 1 week) allowing the patient's body to rest and also combining systemic therapy with active local treatment.

The possibility of interaction of antifungal agents with other systemic drugs should always be considered. When prescribing the drug, you need to carefully read the annotation or refer to this section of our book.

The main contraindications to systemic therapy of onychomycosis are liver disease and pregnancy. None of the systemic antifungal drugs should be given to patients with a history of liver disease or hepatotoxic reactions. If persistent clinical or laboratory signs abnormal liver function, treatment is stopped.

When prescribing any drug daily for a period of more than 1 month, it is necessary to regularly determine the indicators of liver function - the content of aminotransferases and alkaline phosphatase (Table 4.2.3), starting from the control study to the start of therapy.

With impaired renal function, a decrease in glomerular filtration rate, dose adjustment of terbinafine may be required, since this drug is excreted mainly by the kidneys. Dose adjustment of fluconazole is not required, because it is prescribed in a relatively small dose only 1 time per week.

drug allergies, such as penicillin antibiotics many authors consider griseofulvin to be a contraindication.

Table 4.2.3

* When prescribing any drug, one should take into account the individual characteristics of the patient, in particular his attitude to alcohol. Individuals who regularly use alcoholic drinks, the level of liver aminotransferases is recommended to be determined after 1 week of treatment with any drug.

None of the 5 systemic drugs is recommended for pregnant women. In onychomycosis, the therapeutic benefit does not outweigh the risk to the fetus. Since everything system tools excreted or can be excreted in milk, they should not be administered during lactation.

Drugs from the azole group can affect the metabolism of steroids in the human body. However clinical manifestations such interactions are not observed at therapeutic doses. Doses, regimens and terms of treatment used in the treatment of onychomycosis are much less than the maximum safe doses and terms recommended for azole preparations. Treatment of onychomycosis with azole preparations does not pose any risk of disturbing the patient's steroid hormone metabolism.

Causes of Systemic Therapy Failure

Considering cases of unsuccessful treatment of onychomycosis with systemic antifungal drugs, it is worth paying attention to both the shortcomings of the drugs themselves and their incorrect prescription by the doctor and the patient's non-compliance with the prescribed regimen.

The least effective and most common side effects are treatment with griseofulvin and ketoconazole. Even with a treatment period of 1 year, the clinical and mycological efficacy of treatment barely reaches 50%, and the recurrence rate is 30-40%. Failed treatment only griseofulvin or ketoconazole without the use of local therapy can be considered a common occurrence.

The doctor's mistakes include the appointment of potentially highly effective antifungal drugs without taking into account the clinic and etiology of onychomycosis, the use of inadequate doses and terms of treatment, ignorance individual features patient (Table 4.2.4).

Non-compliance with the prescribed regimen for taking the drug by the patient is partly a mistake of the doctor, who did not explain the meaning to the patient. strict observance this scheme and not following up on its recommendations.

There are cases when, even with a comprehensively justified appointment, if the doctor and the patient follow all the rules and recommendations, it is not possible to cure onychomycosis, to achieve the removal of the fungus from the affected nails. In these cases, the duration of treatment is extended, the drug is replaced (for example, terbinafine is replaced by itraconazole and vice versa), treatment with local antifungal agents is added to systemic therapy. In addition to the appointment of antifungal agents, in the treatment of onychomycosis, it is necessary to remove the affected parts of the nail. different ways(removal of the nail plate, keratolytics, cleaning of the nail bed).

Table 4.2.4

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Terbinafine is a broad-spectrum fungicidal antifungal drug from the allylamine class, effective against dermatophytes, yeasts and molds. Available in tablets of 250 mᴦ. The daily dose for adults is 250 mᴦ. For kids daily dose is calculated depending on the body weight of the child and amounts to 62.5 mg / day for body weight up to 20 kg, 125 mg / day from 20 to 40 kg, 250 mg / day for more than 40 kg. Terbinafine is prescribed 1 time per day, food intake and acidity of gastric juice do not affect its absorption. The duration of treatment on average is 6 weeks for nails on the fingers of the hands, and 12 weeks for the feet. Patients young age with a normal nail growth rate, it is possible to reduce the duration of therapy and vice versa, with poor growth nail therapy with terbinafine is indicated for more than 3 months. Terbinafine has the highest activity among systemic antimycotics against dermatophytes, which cause the majority (up to 94%) of cases of dermatomycosis. Fungicidal concentrations of the drug remain in the skin and nail plates for 30-36 weeks after the end of treatment, ᴛ.ᴇ. the effect of the drug in the nail persists for up to 9 months, which significantly increases the percentage complete cure. Side effects in the form of discomfort in the epigastrium, nausea, loss of taste, itching of the skin are short-term and do not require discontinuation of treatment. In general, terbinafine is well tolerated.

Terbinafine, unlike other systemic antimycotics, does not affect the cytochrome P 450 system and, therefore, does not interact with other drugs (antihistamines, oral hypoglycemic drugs, oral contraceptives). Due to this, terbinafine can be used in the treatment of onychomycosis in the elderly, in the presence of concomitant pathology and taking other drugs, with chronic compensated diseases of the liver and kidneys. Terbinafine can be used in the treatment of onychomycosis in children (officially approved for use in pediatric practice).

Itraconazole is an antifungal drug from the class of azoles with a wide spectrum of action. It is prescribed for patients with onychomycosis caused by dermatophytes, yeasts and molds. Itraconazole is most effective when administered by the method of pulse therapy, ᴛ.ᴇ. take 2 capsules of 100 mg in the morning and evening (400 mg / day) for 7 days, then after a three-week break, the course is repeated. When the nails on the fingers are affected, patients receive two courses of therapy, on the toes - 3-4 courses, depending on the type, shape, area of ​​the lesion, and the rate of nail growth. After stopping treatment, the effective concentration of the drug in the nails on the hands remains for 3 months, on the feet after 3 courses - 6-9 months, after 4 courses - up to 1 year. Tolerability of the drug is satisfactory. Side effects in the form of dysfunction gastrointestinal tract͵ headache, skin itching short-term and do not require a break in treatment.

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What are the treatments for nail fungus?

A severe lesion of the nail plate, when it is completely deformed, is called the hypercarotic form. In this case, self-medication is unacceptable. In other cases, you can get by with ointments, creams and sprays based on some kind of multi-fungal active substance.

Most often, therapy includes:

• Oral antifungal medication plus application similar drug to the site of injury.
• Removal of the affected part of the nail plate using keratolic patches Ureaplast, Microspore, Onychoplast, followed by treatment with antifungal drugs. Removing part or all of the plate speeds up the process of treatment and restoration of the nail.
• Application of antifungal varnishes. Helps in complex treatment, as prophylactic or on the initial stage illness. Trade names varnishes: Amorolfine (Amorolfine), Lotseril ( active substance amorolfine), Cyclopirox, Batrafen (on ciclopirox), Omorolfine.
• Application of creams, ointments, solutions and sprays based on terbinafine.
• Appointment of oral systemic antifungal drugs - Griseofulvin, Grimelan, Ketoconazole, Itraconazole, Irunin, Terbinafine, Fluconazole and others. Simultaneously with the tablets, external agents are prescribed, depending on the nature of the disease.
• With a severe course of the disease, drugs are prescribed, which include not only antifungal substances, but also antibacterial or corticosteroid components. For example, travocort includes isoconazole from fungi and diflucortolone valerate (a corticosteroid), which relieves itching and allergies. The drug Pimafucort is also good, which contains a broad-spectrum antibiotic, an antifungal drug and a corticosteroid.
• As maintenance therapy, lotions with Dimexide are prescribed - it removes inflammatory processes, drops and ointments with zinc, copper - accelerate the restoration of the skin and nails.

One of the most affordable means for oral, that is, external, administration for nail fungus is Terbinafine. The name of the drug and the active substance are the same. Also suitable for the treatment of skin, hair, mucous membranes. It is available in the form of ointments, creams, tablets, sprays, solutions. It is rarely prescribed systemically, in most cases it is indicated topical application. Belongs to the group of allylamines.

Terbinafine has a strong fungicidal effect on different kinds dermatophytes and other fungi and yeasts. It destroys the intercellular membranes, and over time, the fungi die. This drug is prescribed for a number of diseases: nail fungus, microsporia, mycoses caused by the rubrum fungus, trichophytosis, candidal lesions of the mucous membranes and skin.

For local treatment fungus Terbinafine cream, ointment or spray is prescribed 1 time per day. The approximate duration of the course is 1 week. It is impossible to interrupt the course, despite the fact that the improvement will occur after the second or third use of the drug. The main contraindications for use medicines with this active ingredient are hepatic and kidney failure as well as tumors different nature, psoriasis, endocrine diseases.

It is most convenient to use sprays from various manufacturers. Alcohol solutions terbinafine are rapidly absorbed into the nail plate, practically do not enter the bloodstream (less than 5%), and dry out instantly. So you can wear socks and shoes almost immediately after application.

Preparations for the treatment of mycoses with this active substance:

• Lamisil.
• Binafin.
• Thermicon.
• Terbasil.
• Fungoterbin.
• Exifin.
• Atifin and others.

All of them have the same active ingredient, the same concentration for specific forms. Only auxiliary substances differ, which are responsible for softening the plate and transporting active substances to the nail. It is worth choosing according to individual portability and price.

This is another drug for the treatment of fungus with a wide spectrum of action. Belongs to the group of triazoles. Itraconazole has also been used successfully to treat lesions of the nail plate, as has Terbinafine. However, it is prescribed with caution to patients with a diseased liver, kidneys.

Names of drugs based on Itraconazole:

• Irunin.
• Orungal.
• Teknazol.
• Orungamine.
• Orunit.
• Rumikoz and others.

The most affordable capsules are Irunin. The duration and course of treatment (with intervals in admission) are prescribed by the doctor strictly individually.

It also refers to the drugs of the triazole series, that is, it acts similarly to Itraconazole. Its advantage over related drugs is that it has virtually no effect on pathogenic microflora human, that is, on beneficial fungi in our body.

It is a relatively expensive drug that is prescribed in rare cases when the patient has difficulty with immune system. So, he can be discharged if there are tumors, immune depression, if the patient has to undergo surgery in the near future, radiation therapy. In banal cases of fungal infection of the nail, Fluconazole is not recommended. It is worth noting that this drug has a number of unpleasant adverse reactions, which are not characteristic of other antifungal agents.

Analogues:

• Diflucan.
• Mycosist.
• Flucostat.

All these capsule preparations are mainly focused on the systemic treatment of fungal diseases associated with genitourinary system person.

A fairly active antifungal drug that is most effective in the treatment of systemic lesions. It has practically no contraindications - only intolerance, pregnancy, lactation, serious illness liver, however, can give a number of side effects.

Preparations containing Ketoconazole:

• Mycozoral.
• Fungikok.
• Oronazole.
• Dermazol.

Also, this active ingredient is often used in the production of medical and cosmetic shampoos, ointments. For example, it is in Nizoral shampoo and Perhotal.

Video: Antifungal drugs

Let's summarize the main drugs for nail fungus

Modern pharmacology can offer a number of antifungal drugs that act on many types of microfungi. Some of the drugs can be classified as specialized for the treatment of certain groups of diseases. So, for example, they work medications based on Ketoconazole or Fluconazole.

Most often, mycologists prescribe drugs based on Terbinafine or Itraconazole for the treatment of nail fungus. Some of the drugs based on them are widely advertised and are quite expensive. At the same time, the effect of such popular drugs is well studied, which allows doctors to recommend these particular drugs.

If the problem has not gone too far, you can try to self-medicate. To do this, soften the damaged part of the plate using special patches, and remove it. Then choose an ointment, cream or spray for local application based on Terbinafine or Itraconazole and use according to the instructions.

For elimination discomfort ointments with corticosteroids are suitable. Zinc and copper ointments will contribute to the restoration of the skin. If therapy does not work, a visit to the doctor is necessary. It is possible not only to lose the nail, but systemic lesion organisms with fungi.

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For systemic therapy of onychomycosis, terbinafine (Lamisil) from the group of allylamines, which has a fungicidal effect, and itraconazole (Orungal), which belongs to triazoles and has a fungistatic effect, are currently used. Treatment with terbinafine is usually carried out continuously for 12 weeks, itraconazole is used continuously (at the same time) or for 1 week of each month for 3-4 months (pulse therapy), and a number of authors consider pulse therapy to be as effective as and continuous treatment with itraconazole or terbinafine. In a prospective, multicenter, double-blind, randomized study, the efficacy and safety of continuous treatment with terbinafine was compared with pulse therapy with itraconazole in patients with onychomycosis of the feet. The study, which was conducted for 72 weeks, involved 35 centers in 6 European countries. The study group consisted of 496 patients aged 18 to 75 years with clinically and mycologically confirmed foot onychomycosis caused by dermatophytes. Patients were randomized into 4 parallel groups and received treatment with terbinafine 250 mg/day for 12 (group T12) or 16 weeks (T16) or itraconazole 400 mg/day (4 x 100 mg capsules) for 1 week each month for 3 or 4 months (groups I3 and I4).

The primary end point was the mycological cure rate, as determined by negative microscopic and culture findings from target diseased nails (nail thumb feet). Mycological cure rate was assessed after 72 weeks of follow-up. Secondary efficacy endpoints were clinical cure rate (100% nail clearance), complete cure rate (mycological and clinical), clinical efficacy (mycological cure, regrowth of at least 5 mm of a new nail free of fungal infections), and overall score given by the doctor and the patient.

The triggers were: Trychophyton rubrum (89,3%), T.mentagrophytes (8,5%), T. rubrum+ non-dermatophyte molds (1.6%), T.rubrum + T.mentagrophytes (0,6%).

The frequency of mycological cure after 72 weeks was: 75.7% and 80.8% in groups T12 and T16, 38.3% and 49.1% in groups I3 and I4 (see Fig.). The clinical cure rate with any of the terbinafine regimens was significantly higher compared with itraconazole pulse therapy (p<0,0022). На протяжении всего исследования (вплоть до 72-й недели) частота микологического и клинического излечения в обеих группах тербинафина продолжала повышаться, тогда как в группах итраконазола она не менялась.

Rice. Mycological cure rate (in %)

Complete cure rates and clinical efficacy were significantly higher in the terbinafine groups than in the itraconazole groups (p<0,005). Общая оценка результатов лечения выявила достоверное преимущество непрерывного лечения тербинафином по сравнению с пульс-терапией итраконазолом (р<0,0001).

Reported adverse events 236 patients (55, 61, 60 and 60 in groups T16, T12, I3, I4, respectively). The characteristics of adverse events for all 4 groups did not differ significantly and did not go beyond the known safety profiles of both drugs.

The results of treatment were rated as good or very good by 79-85% of doctors and patients in the terbinafine groups and only 44-55% in the itraconazole groups.

The study showed that treatment with terbinafine 250 mg/day for 12 or 16 weeks provides a greater rate of mycological and clinical cure compared with itraconazole pulse therapy after 72 weeks of follow-up.

One possible explanation for the higher efficacy of terbinafine in this study is the differences in fungicidal and fungistatic concentrations of both drugs described in the literature. Terbinafine has a fungicidal effect against dermatophytes, and its minimum fungicidal concentration (MFC) is approximately 0.004 μg / ml. Itraconazole, on the other hand, has a fungistatic effect, and its average MPA in relation to dermatophytes is approximately 0.6 μg / ml. When treating with terbinafine, drug concentrations in the nail are created that are 100 times higher than its MPA, while when using itraconazole, the concentration of the drug in the nail is only on the border between the fungistatic and fungicidal concentration. Fluctuations in the concentrations of itraconazole observed in different patients can worsen the results of treatment, while the use of terbinafine, despite significant fluctuations in concentrations, ensures the destruction of the pathogen. The therapeutic advantage of terbinafine was more clearly manifested in this study, since it included patients who had severe onychomycosis with a relatively large prevalence of lesions and a long course of the disease.

Literature:
Source: E.G.V. Evans, B. Sigurgeirsson. Double blind, randomized study of continuous terbinafine compared with intermittent itraconazole in treatment of toenail onychomycosis. // British Medical Journal, 1999; 318:1031-1035.

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Terbinafine is a broad-spectrum fungicidal antifungal drug from the allylamine class, effective against dermatophytes, yeasts and molds. Available in tablets of 250 mg. The daily dose for adults is 250 mg. For children, the daily dose is calculated depending on the body weight of the child and is 62.5 mg / day for body weight up to 20 kg, 125 mg / day from 20 to 40 kg, 250 mg / day for more than 40 kg. Terbinafine is prescribed 1 time per day, food intake and acidity of gastric juice do not affect its absorption. The duration of treatment on average is 6 weeks for nails on the fingers of the hands, and 12 weeks for the feet. In young patients with a normal nail growth rate, the duration of therapy may be reduced, and vice versa, with poor nail growth, terbinafine therapy is indicated for more than 3 months. Terbinafine has the highest activity among systemic antimycotics against dermatophytes, which cause the majority (up to 94%) of cases of dermatomycosis. Fungicidal concentrations of the drug remain in the skin and nail plates for 30-36 weeks after the end of treatment, i.e. the effect of the drug in the nail persists for up to 9 months, which significantly increases the percentage of complete cure. Side effects in the form of a feeling of discomfort in the epigastrium, nausea, loss of taste, itching of the skin are of a short-term nature and do not require discontinuation of treatment. In general, terbinafine is well tolerated.

Terbinafine, unlike other systemic antimycotics, does not affect the cytochrome P 450 system and therefore does not interact with other drugs (antihistamines, oral hypoglycemic drugs, oral contraceptives). Due to this, terbinafine can be used in the treatment of onychomycosis in the elderly, in the presence of comorbidities and other medications, in chronic compensated diseases of the liver and kidneys. Terbinafine can be used in the treatment of onychomycosis in children (officially approved for use in pediatric practice).

Due to the fungicidal effect, short course of treatment and high percentage of complete cure (93-96%), terbinafine is considered the drug of choice for the treatment of onychomycosis.

Itraconazole is an antifungal drug from the class of azoles with a wide spectrum of action. It is prescribed for patients with onychomycosis caused by dermatophytes, yeasts and molds. Itraconazole is most effective when prescribed by the method of pulse therapy, i.e. take 2 capsules of 100 mg in the morning and evening (400 mg / day) for 7 days, then after a three-week break, the course is repeated. When the nails on the fingers are affected, patients receive two courses of therapy, on the toes - 3-4 courses, depending on the type, shape, area of ​​the lesion, and the rate of nail growth. After stopping treatment, the effective concentration of the drug in the nails on the hands remains for 3 months, on the feet after 3 courses - 6-9 months, after 4 courses - up to 1 year. Tolerability of the drug is satisfactory. Side effects in the form of dysfunction of the gastrointestinal tract, headache, skin itching are short-term and do not require a break in treatment.

studopedia.su

Terbinafine and clotrimazole - what's the difference

After analyzing the instructions of the medicines, we revealed the advantage of Clotrimazole over Terbinafine. If Terbinafine ointment can be used for children only from the age of 12, then Clotrimazole can be used from the age of two.

After conducting a full comparison of them, we came to the conclusion that medicines are equally good in their intended use. Another thing is when you need an answer to the question of how effectively this or that drug treats, specifically your disease. With this question, we recommend that you contact your Dermatologist.

A specialist with extensive experience in professional activities will prescribe you the best treatment option for a particular ailment. This will be the best solution for your situation.

Video: Everything you need to know about Terbinafine

24.10.2018

Fungal diseases occupy the first place among dermatological problems. You can get infected anywhere. Diseases of a fungal nature can be asymptomatic or declare themselves more eloquently - with spots on the body, itching, deep skin lesions. To cure the fungus, doctors often prescribe Lamisil. This is a whole line of drugs, the main advantage of which is a quick effect.

Release forms

The name Lamisil was given to several dosage forms with a single active substance - terbinafine. Most often, Lamisil is prescribed in the form of a cream. It is produced in two packages - 15 g and 30 g each. Lamisil spray is popular. This is a liquid solution for external use. Produced in various volumes - 15 and 30 ml. An alternative to the cream is dermgel. This dosage form is produced only in 15 g. For a quick cure for the fungus, there is a special drug - Lamisil Uno. It is a skin solution packaged in a miniature metal tube. For serious dermatomycosis, doctors prescribe Lamisil tablets. They are sold in packs of 14 per carton.

Active substance

The active component of all drugs from the Lamisil line is terbinafine. The substance differs significantly from other compounds with antifungal properties. It is characterized by a wide spectrum of action (active against yeast, mold, some dimorphic fungi). Terbinafine kills the most common causative agents of lichen on the body and dermatomycosis on the feet - trichophytons and microsporums. It is a compound with lipophilic properties (soluble in fats). It has a high bioavailability rate, binds well to blood proteins, spreads to all tissues and organs. Terbinafine accumulates in the skin, sebaceous glands, hair follicles. Due to this, the substance kills the fungus in those places where drugs for external use cannot always penetrate.

Pharmacological properties

Lamisil topical products kill fungi on the surface, inside the epidermal (outer) and deep layers. To increase the penetrating ability of terbinafine, all preparations contain special conductors - organic alcohols.

Lamisil solution (in the form of a spray) and deramgel have approximately equal properties. They are well distributed on the surface of the skin, suitable for the treatment of extensive skin mycoses. Substances do not make its surface greasy, dry quickly, which is optimal for a fungus accompanied by weeping or diaper rash (in the folds of the skin). In addition, these products do not stain clothes, do not require rubbing, which significantly speeds up their application.

Creamy Lamisil is prescribed for mycoses accompanied by dryness, as well as for lesions of the mucous membranes (genitals, external ear). This drug has light moisturizing properties, eliminates the discomfort associated with hyperkeratosis and dryness. The cream requires rubbing, it penetrates less deeply into the dermis. The courses of treatment with its use are somewhat longer than with solutions.

Lamisil UNO is a unique antifungal drug. The special composition of the solution, when exposed to the skin and air, forms a thin polymer film on the skin. It is resistant to water, but dissolves with soap and organic solvents. After application, the solution polymerizes immediately. This ensures prolonged skin contact with the preparation. The active component passes from the film into the stratum corneum of the dermis in high concentrations. It kills the fungus and remains active for a long time. This property provides a preventive effect for 3 months.

Lamisil tablets are prescribed for the treatment of skin mycoses and nail fungus (onychomycosis). Other forms of Lamisil cannot have a therapeutic effect in case of damage to the nail plates. With onychomycosis, it is important that the drug penetrates into all layers of the nail. External agents Lamisil are not capable of this. But the tablets are excellent at fighting ringworm, accompanied by inflammation.

Indications

Indications for use for external preparations Lamisil are the same. They are prescribed for dermatomycosis of smooth skin and hairy parts of the body, feet. Among the indications are the most common fungal diseases of the dermis - inguinal and interdigital epidermophytosis, "athlete's foot", ringworm and pityriasis, seborrheic dermatitis. The doctor selects the dosage form based on the intensity of manifestations and concomitant symptoms.

Tablets are prescribed for fungal infections of the nails and skin under the hair, as well as for all complicated or extensive mycoses on the body (dermatomycosis of the feet, legs, trunk, in the groin, skin candidiasis).

Lamisil tablets are not used for multi-colored (pityriasis) versicolor.

Mode of application

Instructions for use Lamisil spray: Using the built-in dispenser, the affected areas of the skin are abundantly irrigated with a solution. There is no need to rub the product by hand. The solution is well distributed by itself and dries quickly. In diseases of the skin of the feet, torso, in the groin, the solution is applied 1 time per day (2 times - with pronounced symptoms) for 7 days. With pityriasis versicolor, the drug is used for 2 weeks.

Lamisil dermagel is applied to the areas of dermatomycosis with the palm of your hand. A small amount of the product is squeezed out of the tube onto the fingers, the gel is evenly distributed with soft stroking movements. The multiplicity and duration of application are similar to those for the spray.

Instructions for use Lamisil ointment: a small amount of the product is squeezed onto the fingers, rubbed into the affected areas of the skin for 3-5 minutes. With ringworm on the feet, pityriasis versicolor and skin candidiasis, the drug is used 1-2 times a day (depending on the symptoms), for 2 weeks. In diseases of the smooth skin of the trunk, it is enough to apply the cream for 7 days in a row, once a day.

Lamisil Uno is applied to washed, well-dried feet. The palms must also be completely dry. Approximately half of the contents of the tube are squeezed onto the hand, distributed over the foot, starting from the interdigital space and fingers. The arches of the foot (lateral surfaces) are treated to a height of 1.5 cm. Even if the symptoms of the fungus are only on one limb, both legs should be lubricated. After dispensing the product, the feet are dried in the air. After the solution has completely dried, you can put on socks. Feet should not be washed for 24 hours. In the future, the feet are taken care of in the usual way, excluding friction with a pumice stone, washcloth or towel.

The advantage of external agents Lamisil is a shorter (compared to other drugs) course of treatment.

Instructions for the use of tablets should be given by a doctor. Often the drug is prescribed 1 tablet per day. With skin lesions on the head, feet, torso, the course of treatment lasts 2-4 weeks. With onychomycosis, Lamisil is prescribed for 1.5-3 months.

Overdose

With external use of Lamisil, an overdose is unlikely. The intake of high doses of the drug into the body is possible by swallowing the solution or the contents of the tubes, since a meager amount of the active substance penetrates the skin. Tablets can be overdosed if you drink more than 3 tablets at a time.

Intoxication with Lamisil is manifested by nausea, vomiting, abdominal pain. Treatment involves washing the stomach and taking sorbents (activated charcoal).

Side effects

When using Lamisil cream or solutions, local sensitivity reactions are possible - irritation in the area of ​​\u200b\u200bregular application, dryness, burning, urticaria. When taking tablets orally, dyspeptic disorders (stool disorders, nausea, bloating), dysfunction of the hematopoietic organs are possible. Lamisil can disrupt the functioning of the liver and kidneys, up to the development of insufficiency of these organs (with prolonged treatment at high doses).

Contraindications

Preparations from the Lamisil line are contraindicated only in case of individual sensitivity of the patient to terbinafine and auxiliary components of the funds. In children's practice, only cream is used (from the age of 12). All other drugs are prescribed to persons over 18 years of age. Tablets should be recommended by a doctor. Before use, it is desirable to assess the condition of the internal organs (using a biochemical blood test). In case of violations in the functioning of the heart, liver, kidneys, Lamisil is prescribed with caution, for the shortest possible time.

Pregnancy and lactation

All forms of Lamisil are undesirable for lactation. The agent enters the systemic circulation in small quantities, but even they pass into breast milk. The drug can adversely affect the growth and development of the newborn. With an urgent need for treatment with tablets, breastfeeding is stopped.

Pregnant women are prescribed antifungal agents only in extreme cases (for health reasons). Expectant mothers did not participate in the trials of Lamisil. Animal studies have not confirmed the ability of the substance to cause mutations or abnormalities in the development of the fetus. However, there is no objective evidence to confirm the safety of Lamisil for pregnant women.

Analogues

There are quite a few drugs based on terbinafine on the pharmaceutical market. All of them act in the same way as Lamisil. Funds are issued by various companies, which affects their price. Lamisil is one of the most expensive antifungal drugs. Cheaper analogues:

• sprays with terbinafine - Termikon (240-260 rubles for 15 ml, 440-460 rubles for 30 ml), Fungoterbin (420-460 rubles for 30 ml);
• creams- Terbizil cream (270-310 rubles), Binafin (170-200 rubles), Fungoterbin (320-340 rubles);
• tablets- Terbizil (950-1000 rubles), Binafin (620-680 rubles); Thermikon (500-550 rubles).

Cost by release form

A large Lamisil spray (30 ml) costs 750-790 rubles, a small one (15 ml) costs 590-620 rubles. Cream in a large tube can be bought for 880-920 rubles, in a small one - 550-610 rubles. Dermgel Lamisil costs 560-600 rubles. 14 tablets of Lamisil are also sold in pharmacies for 2100-2270 rubles.

With the development of a disease of fungal etiology, the problem of choice is acute - there are a lot of drugs in the pharmacy, but you need to choose the one that will help in the shortest possible time, and also leave as few side effects as possible.

Antifungal drugs include several groups - azole, polyene and allylamine drugs. In addition, there are drugs outside this classification.

For this reason, the question of the rational choice of a drug for treatment with such a variety of drugs is not surprising. The most popular and advertised drugs are azoles, which include drugs such as Fluconazole and Itraconazole (Irunin). Patients often face the choice of which is better - Fluconazole or Itraconazole.

What is this article about?

Should I choose Fluconazole or Intraconazole?

Since both drugs belong to the same pharmaceutical group of antimycotic agents, the question arises as to which of the drugs is better and whether these drugs can be combined during complex antifungal therapy. Most doctors agree that these drugs should not be taken together, as such therapy can increase the risk of side effects and adversely affect the overall health of a patient suffering from mycotic infection.

When comparing these two medications, you can initially notice a significant difference in cost. Itraconazole has a price in Russia in the range of 390-460 rubles, and Fluconazole is only 35-60 rubles.

Both products have a wide spectrum of action and have pronounced fungicidal properties. Both drugs are not recommended for use during pregnancy and lactation.

Each of these agents causes a small number of side effects, but they should not be combined.

Brief description of Itroconazole - its properties and composition

The composition of Itraconazole includes the active substance of the same name, which fights many types of fungal pathogens. Its action is based on the fact that itraconazole, a derivative of triazole, inhibits the cell wall of the fungus, thereby the pathogen loses its protective layer and dies. Effective against fungi such as Candida, Aspergillus, Histoplasma, Trichophytum and Epidermophytum. The spectrum of its action is extremely wide, which allows it to be prescribed in the most severe and combined cases.

The drug is taken orally, while its largest amount in biological fluids is reached after 4-5 hours. The half-life is 15-17 hours. In order for the concentration to remain stable for a long time and the pathogenic flora to be affected, it is necessary to drink the drug regularly, not skipping and increasing the dose. In the blood, the concentration increases gradually, reaching a maximum after 6 hours. The drug is transformed in the liver, while being carried by special proteins. A feature of the drug is its deposition in cells that are rich in keratin, such as the skin, hair and nails. Gradually, the drug leaves the tissues, it depends on the speed of skin regeneration in a person.

In the cells of the mucous membranes, the period is no more than three days.

Features of the use of Itraconazole

The main indication for the appointment of Itraconazole (Irunin) is a fungal infection of the skin, hair, nails and mucous membranes. It is also used for thrush, in particular for diseases of the vagina and intestines. The drug is used in dermatology, ophthalmology and otorhinolaryngology.

Itraconazole is used for systemic fungal pathologies, for example, for mycoses of internal organs. With mycotic meningitis, the drug is prescribed as a reserve drug.

Method of application of the drug - oral. It is necessary to drink it after a meal, preferably rich in vitamins and trace elements. This is necessary so that the medicine penetrates the skin better and has a therapeutic effect. The most optimal are foods containing fats - meat, fish, nuts. It is necessary to take the medication 2 capsules twice a day, for a month. After this, it is imperative to take a break in the intake so that the liver restores its functionality and there is no overdose. If the patient has severe concomitant immune system diseases, the dose should be increased to prevent relapse.

Despite the good effect on the body, Irunin can affect different body systems, such as:

1. Central nervous system. In many patients, taking the drug may be accompanied by discomfort in the forehead or neck, migraine-like conditions.
2. Allergy to any component of the drug, which increases depending on the dose. So, with an overdose of the drug, a reaction similar to Quincke's edema may develop. Also, the phenomena of urticaria and unbearable skin itching are not uncommon.
3. Damage to the organs of the digestive system can manifest itself with signs such as pain in the epigastric region, nausea, urge to vomit or belching. There are frequent manifestations such as stool disorder by the type of diarrhea or constipation, and flatulence is also observed in some patients.
4. Changes in the blood, anemia or leukocytopenia may occur.

Patients with liver damage should not take this drug, as this may be fraught with the development of toxic hepatitis and, as a result, cirrhosis and liver failure.

In addition, passing damage to the organs of hearing and vision is possible - after stopping the use of the drug, these symptoms disappear.

Brief description of Fluconazole - pharmacological properties and composition

Fluconazole is an antifungal drug that, like Itraconazole, has a broad spectrum of activity against fungal pathogens.

The mechanism of action of the active substance is the inhibition of the cell wall and enzymes of the microorganism, which leads to the death of the pathogen. In addition, a high concentration of the drug in the skin and its appendages can inhibit the reproduction of pathogenic flora.

It acts more selectively on fungal cells, unlike Itraconazole, which has more negative effects on the body, in particular on the cytochromes of human cells.

It is used as an antifungal reserve agent. This means that fluconazole is used in the most serious and life-threatening conditions, such as massive transplantation and subsequent fungal infection of internal organs. The drug is also extremely effective in carrying out chemotherapy and radiation therapy in patients with malignant processes. It goes well with antibiotics and cytostatics. It gives the best effect in combination with, the active substance is terbinafin.

When taking Fluconazole, the quality and calorie content of the food that is consumed does not matter. You can drink it both after meals and on an empty stomach. Unlike Itraconazole, it is not as actively bound to plasma proteins, but, despite this, it is also transformed in the liver. The highest concentration of the drug is achieved by the third day of administration due to the fact that the patient is given a double dose at the first dose. This allows you to eliminate a large number of the pathogen at a time.

In blood and other fluids, the concentration of the drug is the same. This must be taken into account in cases where treatment occurs during pregnancy and lactation. It is necessary to take into account the risks for the mother and fetus, and only then prescribe therapy.

The highest concentration of the drug is in the skin and its appendages - hair and nails. The drug accumulates in them gradually, as well as it is excreted. From the skin, the medicine comes out a week after stopping the intake, from the nails - within six months.

Excretion of the drug through the kidneys provides a half-life of 25 hours.

In people with impaired kidney and urinary function, this process is disrupted and lengthened.

Features of the use of the drug Fluconazole

The main indication for the appointment of this drug is a massive or deep fungal infection of the skin, its appendages or internal organs. The drug works even in such difficult cases as fungal meningitis. With mycotic sepsis, this drug is widely used as the main method of treatment. In patients with acquired immunodeficiency syndrome, this medication is used as a permanent prophylactic that prevents the massive reproduction of fungal microorganisms.

Fluconazole is used when wearing prostheses, in particular dental prostheses, when there is a risk of developing a persistent fungal infection.

This drug is contraindicated in people who have an allergic predisposition to one or more of the components of the drug. In this case, it is better to replace the drug with another, with a composition similar in action, but different in structure.

Do not take Fluconazole together with drugs such as Erythromycin and Amiodarone - this can potentiate their effect on the body, and lead to the development of many side effects.

Those people who have renal or hepatic insufficiency should take the drug with extreme caution so as not to provoke the development of the terminal stage of the disease. During pregnancy, it is better to refrain from the drug or replace it with a safer analogue.

Side effects that the medication can cause:

1. On the part of the digestive system - sharp pains in the abdomen, not associated with eating, vomiting without nausea, retention of stool and gases is also possible.
2. Frequent symptoms from the central nervous system are headache and dizziness.
3. An allergy to the drug is considered a very dangerous side effect - it can be either swelling of the larynx or a massive skin reaction with rejection of the epidermis.
4. In the presence of heart disease, such as coronary artery disease or hypertension, the drug can cause rhythm disturbances and voltage changes. This is felt by chest pain, a feeling of lack of air, tachycardia, palpitations.
5. Hair loss may develop after prolonged use of the drug.

Additionally, on the part of the psyche, inappropriate behavior, the development of psychoses, depression and hallucinations are possible.

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According to doctors, it is impossible to completely protect yourself from fungal infections. Infection of nails with mycosis (onychomycosis) does not pose a great health hazard, but creates discomfort, makes the nail plates and fingers unattractive. In advanced cases, the pathology causes pain. From nail fungus, both expensive remedies and inexpensive, but effective pills are used.

Antimycotic drugs in tablets, depending on the main active substance, act on the fungus in one of the following ways:

Composition of tablets from nail fungus

Each tablet contains an antimycotic active substance and a number of auxiliary components.

The active substance can be:

• itroconazole;
• terbinafine hydrochloride;
• fluconazole;
• ketoconazole.

Auxiliary elements in the composition of capsules or tablets are represented by gelatin, sucrose, titanium dioxide and other substances.

Indications for use

Antimycotic drugs are prescribed for fungal infections of the nail plates (onychomycosis), the skin of the feet and hands.

There are several types of onychomycosis:

With the normotrophic manifestation of onychomycosis, the color of the nail changes, white or yellowish stripes, spots appear, which over time can cover the entire surface. But their appearance does not affect the thickness and luster of the nail plate.

The atrophic form causes a discoloration - the nail may acquire a gray tint, become dull. The destruction of the plate begins to complete atrophy. With hypertrophic fungal infection, not only the color of the nail changes, but also its thickness. The nail plates fade, crumble, deform, the usual shine disappears.

To achieve positive results and finally destroy the fungus, doctors prescribe complex therapy - not only drugs in tablets, but also external agents that act locally.

Contraindications

Antifungal drugs, getting into a weakened patient's body, can do more harm than good. Therefore, in certain diseases, the use of antimycotic agents is prohibited.

The prohibition applies to patients suffering from:

Treatment for chronic alcohol dependence and tumors is allowed under the supervision of a specialist.

During pregnancy and during breastfeeding, taking drugs is allowed only in cases where the disease causes significant harm to the health of the mother.

Breast-feeding is stopped until the end of therapy. There is a separate ban on the simultaneous intake of tablets from the fungus and certain drugs.

Adverse reactions

Tablets from nail fungus are not always safe for health. Their use can provoke the occurrence of adverse reactions.

The most common of them are:

• nausea;
• depression and loss of strength;
• headaches and dizziness;
• diarrhea and other malfunctions of the digestive system;
• pain in muscle tissues;
• rash and itching.

Types of pharmaceutical preparations against nail fungus

In pharmacies, a large number of medicines for internal and external use are presented, created to destroy fungal infections.

In addition to tablets, antimycotic drugs are presented in the form of:

The composition of external preparations differs from each other in the main substance.

Well cope with onychomycosis ointments, creams, gels based on:

• terbinafine;
• ciclopiroxolamine;
• bifonazole.

The actions of terbinafine, ciclopiroxolamine, bifonazole are to disrupt the normal functioning of the cell membrane of fungi, which leads to the death of pathogenic microorganisms.

Names of effective inexpensive drugs, prices

Tablets from nail fungus, inexpensive, but effective, are presented in the table.

Irunin: instructions for use

The main active ingredient of the antimycotic agent is itraconazole. It interferes with the synthesis of ergosterol, which causes the death of fungal cells.

With a fungus of the nail plates, Irunin is taken for 3 months at 200 mg per day (once 2 capsules).

Or they use pulse therapy: several weekly courses of therapy are carried out. After each course there is a break - 3 weeks.

To combat mycotic lesions on the toenails, 3 courses will be needed.

Treatment with breaks will take 9 weeks. Daily dose: 4 capsules (2 pcs in the morning and evening). The same course is carried out if the lesions affected the toenails and fingernails at the same time.

For fungal diseases of the nails on the fingers, it is recommended to conduct 2 week courses with a 3-week break between them. Treatment will take 5 weeks. The daily dose is the same: 4 capsules. Small package "Irunina" contains 6 capsules, large - 14 pcs.

"Irunin" can give side effects:

• allergic skin rashes;
• nausea;
• loss of appetite;
• state of nervousness;
• dizziness and headache;
• discomfort in the gastrointestinal tract (constipation, pain, digestive disorders);
• fast fatigue.

Contraindications:

• heart failure;
• allergic reactions;
• pathology of the liver, kidneys;
• pregnancy, lactation;
• obstructive bronchitis.

If the dosage has been exceeded, you should wash the stomach, drink activated charcoal or another sorbent, and observe the condition of the body for several days.

Terbinafine

Inexpensive, but effective pills for nail fungus are represented by Terbinafine. The drug has the name of the active substance that destroys the fungus.

Tablets are taken after meals. The duration of the course for each patient is individual - it is determined by the doctor depending on the stage and extent of the disease. Most often, the duration of treatment is 3 months. The daily norm is 250 mg.

Possible side effects:

• disorders of the nervous system;
• digestive problems;
• decrease in the number of leukocytes and platelets;
• allergic manifestations, including skin rashes;
• pain in joints, muscles.

Contraindications are the same as for other antifungal tablets. Children should not use the drug if their weight is less than 20 kg.

Fungavis

Another antifungal agent that effectively eliminates not only fungal infections, but also fights some bacteria. The active substance is ketoconazole (in 1 tablet - 200 mg). The package contains 20 tablets.

To cure onychomycosis, it is recommended to drink it once a day, during meals - from 200 to 400 mg (the dosage is determined by the doctor). The minimum course duration is 3 months. "Fungavis" is taken until complete recovery. Contraindications and side effects are similar to previous drugs.

Orungal

An antimycotic agent with the active substance itraconazole is available in liquid form and in the form of capsules. Depending on the duration of the course of treatment, you can choose a package with the required number of capsules. The smallest contains 4 pcs.

The drug is taken after meals, washed down with water. The dosage is prescribed based on the stage of the disease and the degree of damage. To get rid of nail fungus, pulse therapy is performed, as with the use of irunin.

You can also follow the usual treatment schedule: take the drug every day, once, 2 capsules at a time. In this case, therapy can last 3 months. The results are judged by observing the gradual replacement of the nail.

Fluconazole

Tablets from nail fungus, inexpensive, but effective, are released under the name "Fluconazole". The name of the drug is the same as the name of the active substance. Its content in one capsule is 50 mg or 150 mg (depending on the dosage).

Contraindications are:

• early childhood - up to 4 years;
• simultaneous use of drugs responsible for the normalization of cholesterol levels - statins; astemizole and terfinadine - antihistamines.

Use with caution when:

• renal failure;
• liver diseases;
• arrhythmias and other cardiovascular pathologies;
• alcoholism;
• pregnancy and during breastfeeding.

For the treatment of nail fungus, Fluconazole is taken 150 mg once a week. Reception is stopped when the nail is completely renewed. It is allowed to repeat the course.

The drug is also suitable for fighting fungal infections in children.

Lamisil

The basis of the drug is terbinafine (250 mg), packs of 7 or 14 tablets. "Lamisil" is drunk on a tablet 1 time per day, after a meal. In mild forms of the disease, the duration of therapy is about 2 months. In more serious cases - up to 4 months.

Contraindications and side effects are the same as for similar pharmaceuticals.

Exifin

The active substance of Exifin is terbinafine (250 mg). Take 1 tablet per day. The maximum duration of treatment with Exifin can be up to 4 months. Treatment of children up to 12 years is allowed. With a weight of over 20 kg, the child is given 1 time per day ½ tablet. If the weight does not exceed 20 kg, the daily dose is reduced to ¼ tablet.

Contraindications:

• children's age up to 3 years;
• pregnancy, lactation;
• pathology of the kidneys, liver;
• component intolerance.

With caution and under the constant supervision of a physician, taking "Exifin" is allowed with:

• alcoholism;
• oncological diseases;
• diseases of the circulatory system and heart;
• psoriasis.

Side effects are the same as those of the above antimycotic agents.

Pimafucin

Tablets for nail fungus, inexpensive, but effective, are relatively safe. "Pimafucin" favorably stands out against the background of other antifungal agents. This is a drug based on natamycin (100 mg).

Average course duration: 2 months. Daily dose: 4 times 1 tablet. With the help of "Pimafucin" fungal infections are treated during lactation (feeding during this period is stopped), pregnancy. You can use it to treat children. Daily dose for them: one tablet in the morning and evening.

Possible side effects: nausea and indigestion. Despite this, therapy is recommended to continue, side effects should disappear over time.

The main contraindication is individual intolerance to substances in the composition of the product. Overdose is unlikely because the drug has low absorption.

Ketoconazole

To cope with nail fungus, tablets with the active substance ketoconazole are taken 1 pc. in the morning and in the evening. The minimum course of treatment takes six months. Overdose may cause side effects. In such cases, the stomach is washed and symptomatic therapy is carried out.

Contraindications:

• intolerance to components;
• pregnancy, lactation;
• pathology of the kidneys and liver;
• children's age up to 3 years.

Side effects:

• nausea;
• headache;
• digestive disorders;
• reduction in the number of platelets;
• vomit;
• skin rashes;
• temperature rise;
• nervous states.

Griseofulvin

The active substance of the drug is griseofulvin (125 mg). It inhibits fungal cell division and prevents them from developing. The package contains 20 tablets. The duration of the course can be up to 8 months. In the 1st month, the tablets are drunk daily, in the 2nd - every other day, from the 3rd month the drug is taken twice a week.

The recommended dose for adults is 500 mg per day. For children (over 2 years old), the dosage is calculated individually. Tablets are best taken after meals or during meals - along with foods rich in fats. Side effects are the same as most of the previously listed antifungal agents.

Contraindications:

• kidney failure;
• individual intolerance;
• liver pathology;
• lupus erythematosus;
• pregnancy, lactation;
• oncological diseases;
• uterine bleeding;
• diseases of the circulatory system.

Recommendations and reviews of doctors about the treatment of fungus with tablets

Tablets from nail fungus, inexpensive, but effective, deservedly receive positive feedback not only from buyers, but also from doctors.

In order for the desired effect to be achieved, experts advise adhering to the following rules:

• do not interrupt treatment in the middle of the course, all prescribed manipulations should be completed;
• along with tablets, use topical preparations (ointments, gels, sprays) - so the result will manifest itself faster;
• monitor the hygiene of the affected areas;
• additionally carry out measures to increase immunity;
• after recovery, do not forget about preventive measures so as not to get infected again.

Both expensive pharmaceutical products and inexpensive, but effective pills for nail fungus can prevent deformation, destruction of the nail plates and the loss of their aesthetics. Exact implementation of all recommendations is a guarantee of successful treatment.

Article formatting: Vladimir the Great

Video about pills for nail fungus

Pills for nail fungus are inexpensive and effective:

The present invention relates to medicine, namely to topical pharmaceutical compositions containing fluconazole and/or ketoconazole and/or terbinafine and liposomes.

Recently, liposomes are most often used as carriers for various biologically active substances, such as vitamins, antibiotics, fruit acids, and others, in medicine. The range of liposomal medicines includes ointments, creams and gels for the treatment of various diseases.

Fluconazole (2-(2,4-difluorophenyl)-1,3-bis(1H-1,2,4-triazol-1-yl)-2-propanol is an antifungal drug of the chemical group - triazole derivatives. Active against a number of yeast fungi, dermatophytes and pathogens of opportunistic and endemic mycoses.It is used for various fungal infections: for cryptococcosis, including cryptococcal meningitis; for systemic candidiasis, candidiasis of the mucous membranes, vaginal candidiasis; for the prevention of fungal infections in patients with malignant neoplasms in the treatment of their cytostatics or radiation therapy, in patients with AIDS, during organ transplantation and in other cases when immunity is suppressed and there is a risk of developing a fungal infection.Assign orally and intravenously.Medications containing fluconazole for topical use are not described.

Ketoconazole (1-cis-1-acetyl-4-para- - methoxyphenyl-piperazine - an antifungal drug of the chemical group - imidazole derivatives. It is active against dermatophytes, yeast-like and mold fungi, pathogens of systemic mycoses, as well as leishmanias. It is prescribed for superficial and systemic mycoses: dermatomycosis and onychomycosis caused by blastomycetes, mycosis of the scalp, vaginal mycosis, blastomycosis of the oral cavity and gastrointestinal tract, genitourinary organs, histoplasmosis and other mycoses of internal organs, as well as purulent leishmaniasis. % shampoo in vials of 25 and 60 ml; 2% cream in tubes of 15 g; 2% ointment in tubes of 20, 30, 40 and 50 g; vaginal suppositories of 0.4 g.

Terbinafine (E) - N-(6,6-dimethyl-2-hepten-4-ynyl) -N-methyl-1-naphthylmethylamine - an antifungal drug of the chemical group - derivatives of N-methylnaphthalene. When applied topically (in the form of a cream or solution), it is little absorbed and has a slight systemic effect; quickly diffuses through the skin and accumulates in the sebaceous glands; excreted in sebum, creating relatively high concentrations in the hair follicles and hair. Within a few weeks after the start of treatment, it also penetrates into the nail plates. It is prescribed for onychomycosis, dermatomycosis, mycosis of the scalp, candidiasis of the skin and mucous membranes. Apply inside and out. Described for external use: 1% solution and spray in vials of 15 and 30 ml; 1% cream in tubes of 10, 15 and 30 g.

The disadvantage of the above means is that they do not penetrate the skin well and, therefore, when applied topically, are effective only in its surface layers.

Known gel Essaven, which includes: escin, "essential" phospholipids and heparin sodium salt and used for phlebitis, thrombophlebitis and hemorrhoids (Mashkovsky M.D. Medicines. - 15th ed., revised, corrected and added . - M .: New Wave, 2006. - pp. 461-462).

Pharmaceutical compositions containing fluconazole and/or ketoconazole and/or terbinafine and liposomes are not described for topical use.

Thus, the object of the present invention is to provide a topical pharmaceutical composition containing fluconazole and/or ketoconazole and/or terbinafine and liposomes with rapid penetration through the skin.

The present invention provides a topical pharmaceutical composition comprising fluconazole and/or ketoconazole and/or terbinafine and pharmaceutically acceptable carriers or excipients, characterized in that it further comprises liposomes.

As a preferred embodiment of the claimed invention, a pharmaceutical composition is proposed, which has the following composition, wt.%:

As another of the preferred embodiments of the claimed invention, a pharmaceutical composition is proposed, which has the following composition, wt.%:

The technical result of the present invention is to obtain a pharmaceutical composition based on fluconazole and/or ketoconazole and/or terbinafine and liposomes, which has the ability to quickly penetrate the skin and, accordingly, rapid absorption. Additional advantages are also ease of use and ease of dosing.

The pharmaceutical composition of the present invention is usually prepared by conventional methods using solid or liquid pharmaceutically acceptable carriers or excipients selected from emulsifiers, dispersing agents, preservatives, flavoring agents, pH adjusters, polymeric carriers, and other excipients that are suitable for preparing topical compositions. The pharmaceutical composition of the present invention may be prepared in the form of a gel, cream, ointment and the like.

The rapid penetration through the skin is due to the binding of fluconazole and / or ketoconazole and / or terbinafine with liposomes containing hydrogenated lecithins in combination with cholesterol.

In preferred embodiments, the compositions are oriented: in the first case, for the treatment of candidiasis, in the second, for the treatment of dermatomycosis and onychomycosis, in the third, for dermatomycosis, the binding of active substances to liposomes ensures their stability and duration of action, as well as penetration into the deep layers of tissues affected by the fungal flora .

The present invention is illustrated by the following examples.

The pharmaceutical composition in the form of a cream based on fluconazole and liposomes has the following composition:

The specified composition is prepared according to the following method. In demineralized water, when heated to 80°C, the following are mixed: fluconazole, carbomer, emulsifier, then cooled to 30°C and liposomes and a preservative are added. The resulting cream is homogenized and evacuated.

The pharmaceutical composition in the form of a cream based on ketoconazole and liposomes has the following composition:

This composition is prepared as in EXAMPLE 1, it differs in that ketoconazole is used instead of fluconazole.

The pharmaceutical composition in the form of a cream based on terbinafine and liposomes has the following composition:

This composition is prepared as in EXAMPLE 1, it differs in that terbinafine is used instead of fluconazole.

Study of a pharmaceutical composition with fluconazole and liposomes for the ability to quickly penetrate the skin.

To this end, the ability of the rapid penetration into the skin of the composition of the present invention based on fluconazole and a control composition containing fluconazole without liposomes was compared. The tests were carried out on rabbits. These compositions were applied to the inner surface of the ear of a rabbit. Absorption was determined by the amount of fluconazole remaining on the skin of the rabbit 10 minutes after application of the compositions, and expressed as a percentage of the initial amount of fluconazole in the composition.

Results of the study: control composition - 50% of the remaining fluconazole; the composition of the present invention is 10% of the remaining fluconazole. Similar results were obtained in the study of the compositions of examples 2 and 3.

Thus, the pharmaceutical composition according to the present invention has the ability to quickly penetrate the skin, providing a more rapid manifestation of the therapeutic effect of the active substances of the composition.

1. Pharmaceutical composition for topical application, characterized in that it contains fluconazole, liposomes, emulsifier, preservative, demineralized water in the following ratio, wt.%:

2. Pharmaceutical composition for topical application, characterized in that it contains ketoconazole, liposomes, emulsifier, preservative, demineralized water in the following ratio, wt.%:

3. Pharmaceutical composition for topical application, characterized in that it contains terbinafine, liposomes, emulsifier, preservative, demineralized water in the following ratio, wt.%:

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Classification of antifungal (antimycotic) drugs

In order to treat diseases caused by a fungus of the genus Candida, drugs of the following pharmacological groups can be used:

• antibiotics of the polyene group: levorin, nystatin, natamycin, amphotericin-B;
• imidazole derivatives: clotrimazole, isoconazole, voriconazole, ketoconazole, fenticonazole, butoconazole and others;
• thiazole derivatives: fluconazole;
• bis-quaternary ammonium salts: dequalinium chloride;
• derivatives of N-methylnaphthalene: terbinafine.

Let's consider each group in more detail.

Antibiotics of the polyene group

They are natural antifungals. The mechanism of their action has been studied quite well and it consists in binding the drugs of this group with the ergosterol of the membrane of fungal cells, as a result, the integrity of this membrane is violated, which leads to the dissolution (lysis) of the cell.

The spectrum of activity of polyenes, in addition to Candida, also includes some protozoa: Trichomonas, Amoebas and Leishmania.

When ingested in the organs of the digestive tract, as well as from the surface of healthy, intact skin, these drugs are practically not absorbed. They are low toxic.

Most drugs are applied topically and orally, amphotericin B - intravenously.

Against the background of taking polyenes, undesirable effects such as allergic reactions, nausea, vomiting, abdominal pain, and diarrhea may develop.

Currently, drugs of this group for the treatment of thrush are used quite rarely, since other, more modern and effective drugs for this purpose have already been developed. The most common antifungal antibiotic is nystatin.

Nystatin

Produced in the form of tablets for oral administration and vaginal tablets, ointments, rectal suppositories (candles).

It is used to treat candidiasis of the mucous membranes of the mouth, skin and internal organs, as well as to prevent these diseases in case of long-term antibiotic therapy.

Adults are recommended to take the drug 250 thousand units 6-8 times a day or 500 thousand units 3-4 times a day. The average daily dose is 1.5-3 million units, and the maximum is 4-6 million units. You can use 2 dosage forms of nystatin - tablets and ointment - at the same time. The course of treatment is usually 10-14 days. With recurrent candidiasis, repeated courses of treatment are recommended - after 2-3 weeks from the previous one.

Vaginal tablets are administered 1-2 pieces (100-200 thousand units) deep into the vagina for 1.5-3 weeks.

Rectal suppositories are injected into the rectum 1-2 pieces (250-500 thousand units) twice a day for 10-14 days.

Nystatin preparations are contraindicated in case of increased individual sensitivity to this substance.

Side effects are nausea, vomiting, chills, fever, allergic reactions. In the event of these symptoms, it is recommended to reduce the dose of the drug. When using vaginal tablets, local irritation and soreness in the vagina may occur.

Nystatin is also part of combined antibacterial and antifungal drugs, such as Polygynax, Terzhinan.

Derivatives of imidazole and thiazole

The mechanism of action of drugs in this group is due to their effect on the synthesis of ergosterol, which is a structural component of the fungal cell membrane. Due to a violation of the production of this substance, the integrity of the cell membrane of the pathogen (the fungus that caused the disease) is violated, the cell dissolves, the fungus dies.

Different representatives of imidazole derivatives have their own spectrum of activity, that is, they affect a different number of fungal species.

They are applied systemically - inside - and locally.

Systemic drugs are ketoconazole, fluconazole, voriconazole and itraconazole.

For the purpose of local treatment, isoconazole, miconazole, clotrimazole, econazole, ketoconazole and others can be used.

Resistance (resistance, immunity) of the fungus to the action of these drugs develops quite rarely, but in certain clinical situations, for example, in the treatment of HIV-infected patients for a long time, resistance may develop.

When taken orally, imidazole and thiazole derivatives (azoles) are well absorbed by the organs of the gastrointestinal tract. They are distributed in most organs and tissues, creating high concentrations in them. Some drugs, in particular, itraconazole, penetrate into saliva, cerebrospinal fluid and intraocular fluid in extremely small quantities. The half-life of different drugs is different and varies between 8-30 hours. Reaching the liver, they undergo a number of biochemical changes in it. They are excreted mainly with feces. Fluconazole is excreted mainly through the kidneys.

Azoles for topical use when taken orally are absorbed poorly, and are effective only when applied topically. In the skin, they create high concentrations. The maximum half-life is noted for bifonazole and it is 19-32 hours. Absorbed into the bloodstream in a minimal amount.

Side effects of systemic azoles are as follows:

• nausea, vomiting, constipation or diarrhea, pain in the abdomen, cholestatic jaundice (one that is associated with stagnation of bile in the biliary tract), increased activity of liver enzymes;
• dizziness, headache, drowsiness, irritability, tremor (involuntary trembling), paresthesia (numbness), convulsions, visual disturbances;
• a decrease in the level of platelets in the blood (agranulocytosis);
• allergic reactions in the form of a skin rash, accompanied or not accompanied by itching, burning;
• peeling of the skin, contact dermatitis.

When taken intravaginally (locally - in the vagina), there may be burning, itching, swelling and redness of the vaginal mucosa, increased discharge from it, pain during intercourse, increased urination.

Clotrimazole (Canesten, Candibene, Candide, Candid-B6, Clotrimazole)

Available in the form of vaginal tablets, gels and ointments for vaginal use.

When applied intravaginally, only 5-10% of the drug is absorbed, therefore it acts only locally, and does not affect the body as a whole. The concentration necessary for the implementation of the therapeutic effect is stored in the vagina for another 3 days after the use of the drug. The part of the active substance that has been absorbed into the blood is modified in the liver and excreted in the bile.

In case of skin candidiasis, it is used in the form of gels or ointments: the drug is applied 1-3 times a day to the affected areas and rubbed into the skin for some time. The duration of treatment is from 1 week to 1 month. In the case of a fungal infection of the feet, in order to reduce the likelihood of a recurrence of the disease, treatment is extended to 3 weeks.

With urogenital candidiasis, 1 tablet per day is injected into the vagina for 7 days, plus the skin of the perineum and external genital organs are lubricated with clotrimazole cream. Alternative tablet regimens are 200 mg three days in a row or 500 mg once.

The vaginal gel is administered at bedtime deep into the vagina, 1 full applicator (which is 5 g) for 6 days.

Vaginal suppositories are administered 1 time per day at bedtime for 6 days.

Treatment of urogenital candidiasis (fungal infection of the genitourinary system) should be carried out outside of menstruation.

Clotrimazole is contraindicated in case of individual intolerance to it, as well as in the first 12-16 weeks of pregnancy.

When used simultaneously with polyenes, it reduces their effectiveness. Cannot be used with nystatin.

Econazole (Santequin, Gino-pevaril, Econazole)

Release form - pessaries, vaginal suppositories, gel and cream for external use.

When applied topically for 3 days causes the death of the fungus.

When applied to the skin creates therapeutic concentrations in the dermis and epidermis. Absorbed into the blood in a minimal amount; that part of the drug that has been absorbed is excreted in the urine and feces.

Outwardly: apply a small amount of cream or gel to the affected area of ​​the skin, rub it until completely absorbed; the multiplicity of application is 2 times a day. Duration of treatment - 14 days, in the treatment of mycosis of the feet - up to 6 weeks.

Intravaginally injected 1 time per day (before going to bed) deep into the vagina. The course of treatment is 3 days. If this is not enough, the course is continued for another 3 days and repeated after 10 days. Can be used during menstruation.

Pessaries are inserted into the posterior fornix of the vagina, 1 piece 1 time per day, in the supine position, at bedtime.

Econazole is contraindicated in case of hypersensitivity of the patient's body to it.

Use with caution in the first 12-16 weeks of pregnancy, as well as during lactation. With vulvovaginal candidiasis, simultaneous treatment of the sexual partner is mandatory.

Isoconazole (Gyno-Travogen)

Used locally. From the surface of the skin is absorbed in small quantities.

The cream is applied once a day to the affected areas of the skin for at least 4 weeks. With the localization of mycoses in the interdigital spaces after applying the cream, a gauze bandage should be applied between them.

Side effects occur quite rarely and are manifested by the occurrence of burning and itching in the first 12-24 hours after the administration of the suppository. When using the cream, allergic reactions are extremely rare, as well as skin irritation and a slight burning sensation.

Within 1 week after the introduction of the suppository, douching should not be performed.

Ketoconazole (Ketodine, Livarol, Ketoconazole)

Available in the form of vaginal suppositories, pessaries.

Applied locally.

Suppositories are injected 1 piece deep into the vagina in a squatting position or lying on your back with legs bent at the knees, before going to bed. The course of treatment is 3-5 days, but if necessary, it can be extended until the patient recovers completely. In chronic candidiasis, the course of treatment is 10 days.

Side effects are extremely rare, standard.

In the first 12-16 weeks of pregnancy, the drug is not used, in the 2nd and 3rd trimester and during lactation, it is used only after assessing the benefit for the mother-risk for the child.

Fenticonazole (Lomexin)

Release form - vaginal capsules and cream, cream for external use.

The absorption of the drug through the skin is minimal, a small amount of it is absorbed by the vaginal mucosa. Not phototoxic. Does not affect the function of the female and male gonads.

Vaginal cream is administered in the amount of 1 applicator deep into the vagina, applied before bedtime, if necessary - in the morning.

In order to prevent reinfection (re-infection), the sexual partner should also be treated with an antifungal drug.

The cream is applied to the skin 1-2 times a day, gently rubbing.

It is usually well tolerated, side effects occur only in a small proportion of patients.

Fenticonazole is not recommended during pregnancy and lactation.

Butoconazole (Ginofort)

Available in the form of a vaginal gel.

5 g of the drug (contains 100 mg of the active ingredient) is injected deep into the vagina once, preferably at bedtime.

Side effects are standard.

During pregnancy and lactation, use only on the advice of a doctor.

Release form - vaginal suppositories, cream.

Candles are administered 1 time per day, preferably at bedtime, deep into the vagina. Suppositories containing 150 mg of the active substance are administered for 6 days, 300 - 3 days, 900 mg - once. It is advisable to start the course of treatment after menstruation. During treatment and for 7 days after its completion, it is not recommended to douche.

The cream is applied in a thin layer to the affected area of ​​the skin and gently rubbed. Multiplicity of application - 1-2 times a day. The course of treatment is from 14 days to one and a half months. The drug should be used for another 7 days after the disappearance of the symptoms of the disease.

Use with caution during pregnancy and lactation.

Sertaconazole (Zalain, Zalain Ovuli)

Available in the form of a cream for external use and in the form of vaginal suppositories.

Enter 1 suppository deep into the vagina at bedtime 1 time per day once. If signs of the disease persist, you can enter again after 1 week.

The cream is applied evenly to the affected area of ​​the skin 1-2 times a day for 1 month.

Side effects are standard, rarely observed.

During the period of treatment with the drug, you should refrain from sexual intercourse, use cotton underwear, do not douche. You can carry out therapy during menstruation.

During pregnancy and lactation, the drug should be used with caution.

There are a number of combined topical preparations containing 2 or 3 antimicrobial / antifungal components at once. It:

• Klion-D 100 (vaginal tablets; contains 100 mg of miconazole and metronidazole);
• Klevazol (vaginal cream, 1 g of which contains 20 mg of clindamycin and miconazole);
• Metromicon-neo (vaginal suppositories containing 500 mg of metronidazole and 100 mg of miconazole);
• Neo-penotran (vaginal suppositories containing 750 mg of metronidazole and 200 mg of miconazole).

Fluconazole (Difluzol, Diflucan, Mikosist, Fluzamed, Fluzak, Futsis, Diflazon, Difluzol, Mikomax and others)

Release form: capsules, tablets, solution for infusions and injections, powder for suspensions, gel.

Well absorbed in the digestive tract after oral administration. Eating does not affect absorption. The maximum concentration in the blood is determined after 0.5-1.5 hours. The half-life is 30 hours.

When injected into a vein, the pharmacokinetics are similar to those when administered orally. It penetrates well into all body fluids. Excreted with urine.

It is used for candidiasis of any localization. In case of a severe course of the disease, it is administered parenterally (into the muscle) or intravenously (drip).

With disseminated (common) candidiasis, 400 mg per day are taken orally, then 200 mg per day. The duration of treatment is determined individually. The dose of the drug administered parenterally varies depending on the severity and characteristics of the course of the disease.

For vaginal candidiasis, take 150 mg of fluconazole once. In order to reduce the frequency of relapses, the drug should be taken at 150 mg every month. The duration of therapy in this case is from 4 to 12 months.

Fluconazole is contraindicated in case of hypersensitivity to it or compounds similar in chemical structure, as well as in the case of treatment with terfenadine.

Side effects are similar to those of other triazole derivatives.

If the patient shows signs of liver damage, treatment with this drug should be discontinued. Pregnant women and women during lactation should not use the drug.

Itraconazole (Funit, Eszol, Itracon, Itrungar, Mikokur, Orungal, Sporagal)

Release form: capsules, tablets, vaginal suppositories.

When taken orally, it is well absorbed. The maximum concentration in the blood is determined 3-4 hours after ingestion. Distributed in many organs and tissues of the body. Excreted with bile.

For vaginal candidiasis, 200 mg twice a day for 1 day or 200 mg 1 time per day for three days are used.

With oral candidiasis - 100 mg 1 time per day for 15 days.

With systemic candidiasis (damage by fungi of the genus Candida) - 100-200 mg 1 time per day, the course of treatment ranges from 3 weeks to 7 months.

The drug is contraindicated in case of hypersensitivity to itraconazole.

During treatment with the drug, the following side effects may occur:

• nausea, vomiting, abdominal pain, constipation, increased activity of liver enzymes, in some cases - hepatitis;
• dizziness, headache, peripheral neuropathy;
• allergic reactions.

During pregnancy and lactation, the drug is prescribed only in case of systemic mycoses.

Voriconazole (Vfend, Voritab)

Release form: tablets, powder for solution for infusion.

After oral administration, it is absorbed quickly and almost completely. The maximum concentration in the blood is determined 1-2 hours after administration. Absorption of the drug does not depend on the acidity of gastric juice. It penetrates the blood-brain barrier (the physiological barrier between the circulatory system and the brain) and is found in the cerebrospinal fluid. The elimination half-life depends on the dose and averages 6 hours.

It is used in case of severe candidal infections, with candidiasis of the esophagus.

The dosage of the drug varies widely depending on the course of the disease, age and body weight of the patient.

Contraindicated while taking certain drugs, such as terfenadine, astemizole, quinidine, rifampicin, carbamazepine, ritonavir, ergot alkaloids, as well as in case of individual intolerance to voriconazole.

Use this drug with caution in people suffering from severely impaired liver and kidney function. Treatment should be carried out under the control of indicators of liver function.

During pregnancy and lactation, the drug is not used. During the period of treatment, a woman should be reliably protected.

Posaconazole (Noxafil)

Powerful antifungal agent.

With oropharyngeal candidiasis (fungal infection of the oral cavity and pharynx), it is used in patients with reduced immunity or low efficacy of topical preparations.

On the first day of therapy, take 200 mg of the drug 1 time per day with meals, then 100 ml 1 time per day for 13 days.

Contraindications for Noxafil are similar to those for voriconazole.

During pregnancy and lactation is not used.

Dequalinium chloride (Fluomizin)

Release form - vaginal tablets.

It has a wide spectrum of antimicrobial activity, in particular, it has a negative effect on fungi of the genus Candida. The mechanism of action of this drug is to increase the permeability of the cell membrane, which leads to cell death.

When administered intravaginally, it is absorbed into the blood in a small amount.

It is used in case of vaginal candidiasis.

It is recommended that in the supine position, with legs slightly bent, insert 1 tablet deep into the vagina. The frequency of administration is 1 time per day, the duration of treatment is 6 days. Treatment with a shorter course may lead to relapse.

The drug is contraindicated in case of individual hypersensitivity to its components, in case of ulcers in the vagina and cervix, as well as in girls before reaching puberty.

Side effects are rare. In some cases, patients note burning, itching, hyperemia of the vaginal mucosa. Allergic reactions are possible.

The drug is approved for use during pregnancy and lactation. However, care should be taken when prescribing it in the 1st trimester of pregnancy.

Terbinafine (Lamisil, Mycofin, Terbizil, Terbinorm, Fungotek, Exifin and others)

Release form: tablets, cream, gel, skin spray.

In relation to Candida, it has both fungicidal (causes the death of fungi) and fungistatic (inhibits their growth) activity (depending on the type of fungus).

The drug inhibits the synthesis of ergosterol in the fungal cell, which ultimately leads to the death of its cell.

When administered orally, it accumulates in the skin, nails, hair in the concentration necessary to achieve a fungicidal effect.

Terbinafine is used for various fungal infections, in particular for candidiasis.

Cream or gel 1-2 times a day is applied to cleansed dry skin at the site of the lesion, capturing and adjacent healthy areas, lightly rubbed. The duration of treatment is approximately 7 days.

The drug is contraindicated in case of hypersensitivity to its components.

Against the background of the use of terbinafine, the following side effects may develop:

• nausea, vomiting, loss of appetite, abdominal pain, diarrhea;
• allergic reactions - skin rashes with or without itching, extremely rarely - Stevens-Johnson syndrome;
• violations of taste sensations in some cases;
• when applied topically - redness, itching or burning at the site of application.

Patients with severe liver and / or kidney disorders are recommended to prescribe a half dose of the drug.

Terbinafine should not be taken during pregnancy and lactation.

Above, you were able to get acquainted with the majority of drugs used to treat candidiasis (thrush) of various localizations. We draw your attention to the fact that you should not self-medicate, choosing a drug based on data taken on the Internet - if you have symptoms characteristic of a fungal disease, you should seek qualified medical help as soon as possible.

Which doctor to contact

For fungal infections of the skin or nails, it is best to consult a dermatologist. Candidiasis of the oral mucosa will be cured by a dentist, and vaginal - by a gynecologist. With recurrent candidiasis, consultation with an immunologist is necessary, since this disease is a frequent companion of immunodeficiencies. In case of systemic candidiasis with damage to internal organs, an infectious disease specialist or mycologist, as well as a specialized doctor, is involved in the treatment of the patient.

myfamilydoctor.ru

Classification:

Polyenes - nystatin

Azoles - flucosanol, ketoconazole

Allylamines - terbinafine

Azoles:

Activity spectrum: The main pathogens of candidiasis (albicans, tropicales), dermatomycetes.

NLR: Dyspepsia, CNS (headache, dizziness, paresthesia, tremor, convulsions), allergic reactions (rash, itching), hepatotoxicity (increased ALT, AST, jaundice)

Allylamines:

Dermatomycetes, Candida, Aspergillus.

NLR: same as azoles

Basic anti-inflammatory drugs. Classification, effects, NLR, indications for use.

(in question 25 more)

The basis of the treatment of RA and SLE is NSAIDs + basic drug. Basic drugs, compared with NSAIDs, suppress the inflammatory process more deeply, but the therapeutic effect develops more slowly (weeks, months).

Methotrexate

Gold standard for RA. Folic acid antagonist. Has a pronounced immunosuppressive effect even in small doses

Gold compounds

Violate the activation of T-lymphocytes and the development of an autoimmune reaction

NLR: pruritus, dermatitis, proteinuria, diarrhea. In case of significant complications, dimercaprol (a drug that binds gold)

Penicillamine:

Significantly inferior to gold in terms of efficacy and tolerability

NLR: Nephrotic syndrome, jaundice, myasthenia gravis.

Sulfasalazine

Better than penicillamine

NLR: nausea, vomiting, rash

Chloroquine:

Portability is good, but much inferior in effectiveness to the rest

NLR: rarely - dermatitis, myopathy

Principles of choice of antimicrobial drug, route of administration and dosing regimen.

Antimicrobial therapy is of two types - etiotropic and empirical. Etiotropic - when the pathogen is known, empirical - when it is not known. Often you have to resort to empirical therapy, because. identification of the pathogen requires several days, and sometimes is not possible at all. To increase the effectiveness of empirical therapy, certain principles should be followed:

1. The choice of the drug should be based on an accurate diagnosis, this allows you to determine at least the alleged pathogen. 2. Preference is given to drugs with a narrower spectrum of action. 3. Do not prescribe antibacterial drugs for a viral infection.

Routes of administration

It is necessary to take into account:

1. If orally, whether it is absorbed from the intestines into the blood.

2. If into soft tissues, whether they are released from the muscles and enter the bloodstream or whether they cause destruction of soft tissues.

3. Is it possible to inject the drug into the bloodstream.

4. Or it is better to use the drug locally inhalation.

Dosing regimen

When choosing doses, one must take into account the ability of antimicrobial drugs to penetrate one or another barrier. For example, bezylpenicillin. It can damage the cerebral cortex, but it is unable to cross the blood-brain barrier. Therefore, it belongs to the broad-dosing AB. The dose of, for example, cephalosporins can also vary, but not more than 5 times. They belong to limited-dose ABs. Well, for example, macrolides, aminoglycosides, their doses can differ by no more than 2 times. They refer to AB strictly dosing. They are the most dangerous, because the difference between the concentration to achieve a therapeutic effect and the maximum allowable is not large.

Principles of rational antibiotic therapy, antibiotic resistance.

- AB should be prescribed in accordance with the sensitivity of a particular pathogen to it

- AB should be prescribed in such a dose and administered in such a way as to provide a therapeutic concentration in the focus of inflammation

- AB should be prescribed in such a dose and administered in such a way that its damaging effect is limited as much as possible

Antibiotic resistance

Primary resistance - associated with the genetic characteristics of the species

Secondary - occurs during the treatment of AB

Criteria for evaluating the effectiveness and safety of antibiotic therapy. Examples.

Efficiency:

Normalization of t, disappearance of symptoms. Decrease in the number of leukocytes, ESR, CRP.

Security:

To assess the safety of antibiotics, it is necessary to detect possible ADRs clinically and in the laboratory. For example, when taking drugs with a nephrotoxic effect, monitor kidney function (blood creatinine).

cyberpedia.su

Release form and composition

Terbinafine is available in several dosage forms:

• tablets: pack of 250 mg (14 or 28 pcs.);
• spray for external use: bottle with microspray 10 g or 20 g;
• cream: 10 and 15 g (polymer or aluminum tubes), 30 g (dark glass jar);
• terbinafine ointment 1%: 15 g;
• solution 1%.

The active substance of all forms of release is terbinafine. However, in tablets, its content is higher.

Composition of the ointment: polysorbate, methylaparaben, vaseline oil, purified water. The components of the tablets are cellulose and silicon dioxide, as well as lactose monohydrate.

The cream, in addition to polysorbate and purified water, contains benzyl and cetyl alcohols, sodium hydroxide. The composition of the spray and solution includes only terbinafine hydrochloride.

All forms of the drug, except for tablets, are available without a prescription.

Price and analogues of Terbinafine

You can buy Terbinafine in a pharmacy at the following prices:

• tablets: 14 pcs. - 270 rubles, 28 pcs. - 390 rubles.
• spray: 10 g - 135 rubles, 20 g - 180 rubles.
• cream: 10 g - up to 100 rubles, 15 g - 140 rubles, 30 g (jar) - up to 300 rubles.
• ointment: 15 g - 87 rubles.
• solution: up to 200 rubles.

There are analogues of Terbinafine, similar in components and active substance. Many choose them, because often the price differs in a favorable direction - this is especially true for domestic drugs. But remember that such a change in medication must always be coordinated with a specialist.

Analogues include:

• Thermikon - 348 rubles;
• Fungoterbin - 326 rubles;
• Exifin - 849 rubles;
• Lamisil dermgel - 567 rubles;
• Ativin - 228 rubles;
• Exiter - 724 rubles;
• Terbiks - from 182 to 929 rubles;
• Mikonorm - about 100 rubles;
• Terbinox - 128 rubles;
• Tefalin - from 87 rubles;
• Atifin - from 228 rubles;
• Terbinor - from 200 rubles;
• Erbinol - from 150 rubles.

The right choice of a treatment agent is a guarantee of the absence of unpleasant health-related consequences, relapses, and allergic reactions. It is impossible to answer which is better - Terbinafine or Lamisil, if there is no access to the patient's diagnosis. The drug is prescribed individually.

The action of the remedy

The main pharmacological action is antifungal, fungicidal.

Therefore, Terbinafine is the right choice for those who decide not only to get rid of annoying symptoms, but to completely destroy microorganisms.

The agent is rapidly absorbed from the gastrointestinal tract. For treatment with this drug, the proper functioning of the liver is necessary, since Terbinafine is partially metabolized in it. Repeated application does not reduce effectiveness.

Indications

Among the indications for the use of the drug inside, the prevention and treatment of the following diseases are distinguished:

For external use (anti-fungal ointment, cream, spray), the drug is used as a prophylaxis and therapy for the following diseases:

Consult with a specialist first, undergo special examinations to exclude an incorrect diagnosis. Be extremely honest when talking about your illness - when it was caused, whether any of your relatives have a similar problem.

Instructions for use Terbinafine

Remember that the duration of treatment depends not only on the form of the drug, but also on the individual characteristics of the patient - the severity of the disease, the affected area, the localization of infection. The age of the patient and his state of health also play a significant role.

In older patients, there may be changes in the functioning of the liver and/or kidneys, so it is important to monitor the overall health until complete recovery.

Tablets

For children, the drug is prescribed once a day, after meals. Due to age, a single dose is calculated solely on the basis of the weight of the child.

In this way:

• 20-40 kg - 125 mg tablet;
• from 40 kg - 250 mg of the product.

Adults should take 250 mg/day in the evening or 125 mg twice daily. Keep track of the quantity, because the recovery process largely depends on the patient himself - whether he forgets about the timely intake, whether he observes additional preventive measures. It is important to independently control your condition, periodically seeking advice from a specialist. This is the only way to avoid relapse.

Remember that the duration below is calculated as an average:

• fungal infections of the feet - up to 6 weeks;
• mycosis of other parts of the body (trunk, limbs) - up to 4 weeks;
• cutaneous candidiasis - from 2 to 4 weeks.

With mycosis of the scalp (the disease is inherent mainly in children), the treatment period is about 4 weeks.

Onychomycosis is treated until a healthy nail grows instead of an infected nail. This is calculated on a case-by-case basis, but a 12-week course for toenail fungus and a 6-week course for plate mycosis on the hands are commonly used.

The characteristics of the body play an important role: in some patients, the nails will grow longer, so the duration of therapy should also be increased if your doctor indicates this.

Cream, ointment, solution

It is first necessary to thoroughly clean and dry the infected areas on which it is planned to apply the emulsion. This is done 1-2 times a day, depending on the instructions of the specialist. The substance is gently rubbed into the affected area and neighboring places with a thin layer.

Average duration of therapy:

• ringworm of the feet, trunk, candidiasis - from 2 to 4 weeks;
• multi-colored lichen - up to 2 weeks;
• onychomycosis - about 6 months.

Results are already observed in the first few days of treatment, unlike tablets. If you do not complete the course of therapy to the end, complications, relapse are possible.

Spray, solution

Spray is used orally, 250 mg/day, may be taken in several doses. The duration of therapy depends on the severity of the disease and the localization of infection, the average period for skin mycoses is up to 4 weeks, for onychomycosis - from 6 weeks to 6 months or more, if the nail plates grow slowly.

Application for children:

• less than 20 kg - ½ tablet 125 mg;
• 20-40 kg - 125 mg tablet;
• from 40 kg - 250 mg of the product.

External spray is used up to 2 times a day for about 2 weeks.

Indications and contraindications

The main contraindication, in which it is really worth refusing to use the drug, is hypersensitivity to its components, main or auxiliary.

Restrictions on ingestion (tablets, spray):

• renal and / or liver failure. For this reason, it is necessary to monitor the condition of elderly patients during therapy with Terbinafine;
• lupus erythematosus, psoriasis. Probably exacerbation of diseases or their recurrence when using this remedy.

Restrictions for external use (ointment, cream, spray):

• hepatic and / or renal failure;
• alcoholism;
• vascular pathology.

During pregnancy, the drug is allowed in the case when the expected benefit far outweighs the possible harm. Make sure that the baby's skin does not come into contact with the treated surface.

During lactation, the use is prohibited, since Terbinafine is excreted in milk.

Side effects include:

• exacerbation of lupus;
• depression, apathy, mental disorders, irritability;
• headache, dizziness (often), partial loss of taste;
• tinnitus;
• nausea followed by vomiting, bloating;
• arthralgia;
• increased fatigue, in rare cases - insomnia;
• probably an increase in body temperature;
• allergic reactions (itching, burning, redness, irritation of the skin, urticaria, swelling).

In rare cases, side effects from the circulatory system, such as anemia, are possible.

Real Patient Testimonials

“There is no point in spending money on expensive drugs, even if their photos are posted everywhere, constantly advertised! Terbinafine coped well with the fungus on the big toe. I used pills, additionally applied ointment - it's better, because the infection touched the skin too. It’s her own fault - she didn’t start treating right away! ”

Protein FF

“I could not decide - cream or ointment. I took the pills. I lost my sense of taste for a while, but then, after some time after recovery, everything returned. Satisfied with the result. I no longer go to the pool where, most likely, I caught a fungus - Terbinafine, of course, will also help a second time, but I don’t want to risk my health. ”

napalce.ru

What are the treatments for nail fungus?

A severe lesion of the nail plate, when it is completely deformed, is called the hypercarotic form. In this case, self-medication is unacceptable. In other cases, you can get by with ointments, creams and sprays based on some kind of multi-fungal active substance.

Most often, therapy includes:

• Oral administration of antifungal drugs plus application of a similar drug to the site of the lesion.
• Removal of the affected part of the nail plate using keratolic patches Ureaplast, Microspore, Onychoplast, followed by treatment with antifungal drugs. Removing part or all of the plate speeds up the process of treatment and restoration of the nail.
• Application of antifungal varnishes. Helps in complex treatment, as a prophylactic or at the very initial stage of the disease. Trade names of varnishes: Amorolfine (Amorolfine), Loceryl (active ingredient amorolfine), Cyclopirox, Batrafen (on cyclopirox), Omorolfine.
• Application of creams, ointments, solutions and sprays based on terbinafine.
• Appointment of oral systemic antifungal drugs - Griseofulvin, Grimelan, Ketoconazole, Itraconazole, Irunin, Terbinafine, Fluconazole and others. Simultaneously with the tablets, external agents are prescribed, depending on the nature of the disease.
• With a severe course of the disease, drugs are prescribed, which include not only antifungal substances, but also antibacterial or corticosteroid components. For example, travocort includes isoconazole from fungi and diflucortolone valerate (a corticosteroid), which relieves itching and allergies. The drug Pimafucort is also good, which contains a broad-spectrum antibiotic, an antifungal drug and a corticosteroid.
• As maintenance therapy, lotions with Dimexide are prescribed - it relieves inflammation, drops and ointments with zinc, copper - accelerate the restoration of the skin and nails.

One of the most affordable means for oral, that is, external, administration for nail fungus is Terbinafine. The name of the drug and the active substance are the same. Also suitable for the treatment of skin, hair, mucous membranes. It is available in the form of ointments, creams, tablets, sprays, solutions. It is rarely prescribed systemically, in most cases local application is indicated. Belongs to the group of allylamines.

Terbinafine has a strong fungicidal effect on various types of dermatophytes and other fungi and yeasts. It destroys the intercellular membranes, and over time, the fungi die. This drug is prescribed for a number of diseases: nail fungus, microsporia, mycoses caused by the rubrum fungus, trichophytosis, candidal lesions of the mucous membranes and skin.

For local treatment of the fungus Terbinafine cream, ointment or spray is prescribed 1 time per day. The approximate duration of the course is 1 week. It is impossible to interrupt the course, despite the fact that the improvement will occur after the second or third use of the drug. The main contraindications to the use of drugs with this active substance are liver and kidney failure, as well as tumors of various nature, psoriasis, endocrine diseases.

It is most convenient to use sprays from various manufacturers. Alcoholic solutions of terbinafine are quickly absorbed into the nail plate, practically do not enter the bloodstream (less than 5%), and dry out instantly. So you can wear socks and shoes almost immediately after application.

Preparations for the treatment of mycoses with this active substance:

• Lamisil.
• Binafin.
• Thermicon.
• Terbasil.
• Fungoterbin.
• Exifin.
• Atifin and others.

All of them have the same active ingredient, the same concentration for specific forms. Only auxiliary substances differ, which are responsible for softening the plate and transporting active substances to the nail. It is worth choosing according to individual portability and price.

This is another drug for the treatment of fungus with a wide spectrum of action. Belongs to the group of triazoles. Itraconazole has also been used successfully to treat lesions of the nail plate, as has Terbinafine. However, it is prescribed with caution to patients with a diseased liver, kidneys.

Names of drugs based on Itraconazole:

• Irunin.
• Orungal.
• Teknazol.
• Orungamine.
• Orunit.
• Rumikoz and others.

The most affordable capsules are Irunin. The duration and course of treatment (with intervals in admission) are prescribed by the doctor strictly individually.

It also refers to the drugs of the triazole series, that is, it acts similarly to Itraconazole. Its advantage over related drugs is that it has practically no effect on human pathogenic microflora, that is, beneficial fungi in our body.

This is a relatively expensive drug that is prescribed in rare cases when the patient has problems with the immune system. So, he can be discharged if there are tumors, immune depression, if in the near future the patient will have to undergo surgery, radiation therapy. In banal cases of fungal infection of the nail, Fluconazole is not recommended. It is worth noting that this drug has a number of unpleasant side reactions that are not characteristic of other antifungal agents.

Analogues:

• Diflucan.
• Mycosist.
• Flucostat.

All these capsule preparations are focused mainly on the systemic treatment of fungal diseases associated with the human genitourinary system.

A fairly active antifungal drug that is most effective in the treatment of systemic lesions. It has practically no contraindications - only intolerance, pregnancy, lactation, serious liver diseases, but it can give a number of side effects.

Preparations containing Ketoconazole:

• Mycozoral.
• Fungikok.
• Oronazole.
• Dermazol.

Also, this active ingredient is often used in the production of medical and cosmetic shampoos, ointments. For example, it is in Nizoral shampoo and Perhotal.

Video: Antifungal drugs

Let's summarize the main drugs for nail fungus

Modern pharmacology can offer a number of antifungal drugs that act on many types of microfungi. Some of the drugs can be classified as specialized for the treatment of certain groups of diseases. For example, drugs based on Ketoconazole or Fluconazole act.

Most often, mycologists prescribe drugs based on Terbinafine or Itraconazole for the treatment of nail fungus. Some of the drugs based on them are widely advertised and are quite expensive. At the same time, the effect of such popular drugs is well studied, which allows doctors to recommend these particular drugs.

If the problem has not gone too far, you can try to self-medicate. To do this, soften the damaged part of the plate using special patches and remove it. Then choose an ointment, cream or spray for topical use based on Terbinafine or Itraconazole and use according to the instructions.

To eliminate discomfort, ointments with corticosteroids are suitable. Zinc and copper ointments will contribute to the restoration of the skin. If therapy does not work, a visit to the doctor is necessary. It is possible not only the loss of the nail, but the systemic damage to the body by fungi.