The drug acyclovir from the herpes virus. Aciclovir - uses, side effects and drug interactions How fast do aciclovir tablets work

Acyclovir is a popular antiviral drug with selective activity against herpes simplex viruses (Herpes simplex) types 1 and 2, Varicella zoster and Epstein-Barr viruses, as well as cytomegalovirus. The antiviral activity of acyclovir is achieved by suppressing the multiplication of viral particles.

It is most often used for the treatment of herpes and is highly effective when used before the vesicular stage of rashes. With later use, it accelerates the healing and resolution of the elements. The instructions for use of acyclovir indicate that the drug has an immunostimulating effect.

Pharmacological group: Antiviral drugs

Composition, physico-chemical properties, cost

Acyclovir is available in four dosage forms: lyophilisate, cream, ointment, tablets.

Lyophilisate

Cream 5%

Ointment 3%

Tablets Acyclovir

Base substance Acyclovir 250 mg or 500, 1000 mg in 1 vial Acyclovir 50 mg in 1 g of cream Acyclovir 30 mg in 1 g of ointment Aciclovir 200 mg or 400 mg
Excipients Sodium hydroxide Medical vaseline oil, vaseline, cetostearyl alcohol, propylene glycol, poloxamer 407, purified water, dimethicone Emulsifier, lipocomp "C", polyethylene oxide 400, nipazol, nipagin, purified water Milk sugar, potato starch, aerosil, medium molecular weight polyvinylpyrrolidone, calcium stearate
Physiochemical properties Powder of white or white-cream color Cream almost white Ointment white-yellow Tablets are flat, white
Package Glass bottles packed in cardboard boxes Aluminum tube, 5 g, in a cardboard box 10 tablets in a contour blister pack, in cardboard packs
Price 130-410 rub.
40-70 rub.
20-30 rub. 30-150 rub.

pharmachologic effect

The antiviral activity of acyclovir is explained by its ability to inhibit the synthesis of viral DNA, i.e. due to the suppression of the replication of viral particles sensitive to the drug. The genetic apparatus - nucleic acids DNA and RNA, are complex compounds with nitrogenous bases included in them. Each individual has its own sequence of nitrogenous bases.

Nitrogenous bases, when combined with carbohydrates (deoxyribose and ribose), form nucleosides. One of them, called thymidine, is activated to deoxythymidine by the enzyme thymidine kinase. Deoxythymidine is included in the chain of replicated DNA. Acyclovir, being a synthetic substance, is similar in structure to thymidine. As a result, it interacts with the enzyme thymidine kinase, turning into mono-, di- and triphosphate. It is acyclovir triphosphate that is able to integrate into the chain of replicated DNA and cause its damage. In parallel, inhibition of the viral DNA polymerase occurs, the synthesis of viral DNA is disrupted, and the viral particle does not multiply.

Clinically, the effect of acyclovir is manifested by stopping the spread of skin herpetic rash and healing of existing vesicles, reducing pain and itching, and eliminating the effects of general intoxication, if any. Treatment with acyclovir helps prevent complications of herpes infection on the internal organs.

Acyclovir, in addition to antiviral action, strengthens the immune system. The drug manifests its qualities both locally and throughout the body when taken internally or intravenously, without damaging human cells, i.e. purposefully affects only the genetic material of viruses.

Pharmacokinetics

Lyophilisate and tablets

When taken internally, the bioavailability of the drug is about 15-30%. It is actively distributed in the fluids and tissues of the human body. It binds to plasma proteins by 9-33%. Metabolism of acyclovir is carried out in the liver. The elimination half-life for oral administration is about 3 hours, for intravenous administration it is about 2.5 hours. It is excreted in the urine and in small quantities through the intestines with feces.

Ointment and cream

The drug quickly penetrates the corneal epithelium, creating the necessary therapeutic concentration of acyclovir in the intraocular fluid, and is rapidly absorbed into the affected skin when applied externally. With these methods of application, the created concentration of the drug in the blood has not been studied. A small part of acyclovir is found in the urine.

Indications for use

Cream - skin infections caused by Varicella zoster and Herpes simplex viruses (lichen, skin herpes, chicken pox).
Ointment - herpetic keratitis and other eye lesions caused by Herpes simplex 1 or 2 tons.

Tablets :

  • Viral infections of mucous membranes and skin (Herpes simplex viruses 1 and 2 tons), primary and secondary, including genital herpes;
  • Prevention of exacerbations of recurrent viral infections (Herpes simplex 1 and 2 tons) in a normal state of immunity and in people with immunodeficiency;
  • As a complex treatment drug in groups of patients with severe immunodeficiency and people after bone marrow transplantation;
  • Therapy of acute and recurrent diseases caused by the virus Varicella zoster and Herpes zoster).

Lyophilisate :

  • Viral infections, the etiological factor of which are Herpes simplex viruses 1 and 2 tons and Varicella zoster;
  • Prevention of diseases caused by these viruses;
  • Severe immunodeficiency (as a complex treatment drug);
  • Treatment of patients after bone marrow transplantation (prevention of cytomegalovirus infection).

Contraindications

  • lactation period;
  • Hypersensitivity to the components of acyclovir or valaciclovir;
  • Children's age up to 3 years (tablets).

With caution, tablets and lyophilisate are prescribed:

  • during pregnancy;
  • for the treatment of the elderly;
  • with kidney dysfunction;
  • with a history of various neurological reactions in response to taking cytotoxic drugs.

Dosage

Before use Dosage A course of treatment

Cream

Before applying the cream and after processing, wash your hands with soap and water. Do not rub damaged areas of the skin.

Adults and children:

Applying the cream to the affected parts five times a day after 4 hours, except at night.

Course - 5 days, maximum - 10 days. The greatest effect is achieved at the beginning of treatment in the prodromal period (before rashes).

Ointment

Wash hands thoroughly with soap before and after the procedure. Adults and children: a 1 cm strip of ophthalmic ointment is placed in the lower conjunctival sac every 4 hours, five times a day. The course of treatment is until complete healing, plus another 3 days after healing.

Lyophilisate

After preparing the solution, the drug is administered intravenously, drip. Adults and children from 12 liters: 5-10 mg per 1 kg of weight, with an interval between injections - 8 hours. Children 2 months-12 liters: 250-500 mg / m2 of body surface, with an interval between injections - 8 hours.
Dei 0-3 months: 10 mg per 1 kg of weight, with an interval between injections - 8 hours.
The duration of treatment is set individually.

Tablets

Take during or immediately after a meal with water.

Treatment of diseases of the mucous membranes and skin(Herpes simplex 1 and 2 t): Adults: 200 mg five times a day for 5 consecutive days, observing a 4-hour break between doses (night break - 8 hours). In severe cases, the course is extended up to 10 days.
Severe immunodeficiency, condition after BM transplantation: Adults: 400 mg five times a day.
Prevention of recurrent infections, Herpes simplex 1 and 2 tons in people with a normal state of immunity: 200 mg four times a day or 400 mg twice a day.
Infection prevention that cause Herpes simplex 1 and 2 tons in immunocompromised patients: 200 mg four times a day or 400 mg five times a day (in severe condition).
The preventive course is set on an individual basis, taking into account the risk of developing infections.
Treatment of Varicella zoster virus infections:
  • Adults: 800 mg five times a day every 4 hours with an 8-hour break at night, a course of 7-10 days.
  • Children: 20 mg per 1 kg of weight four times a day. within 5 days.
Treatment of Herpes zoster virus infections: Adults and children over 3 years: 800 mg four times a day every six hours for 5 days.
Treatment and prevention of infections caused by Herpessimplex 1 and 2 tons in children with normal immunity and immunodeficiency:
  • Children 3-6 years: 400 mg four times a day;
  • Children from 6 years: 800 mg four times a day. Course 5 days.

special instructions

  • With oral and intravenous use of the drug in elderly patients, it is necessary to organize sufficient fluid intake;
  • When treating patients with end-stage renal failure, the dose is reduced to 200-800 mg of acyclovir twice a day (depending on the pathology);
  • The use of acyclovir in pregnant women is possible if the real benefit to the mother exceeds the possible risks to the fetus.
  • Contact with external forms of acyclovir on mucous membranes should be avoided;
  • When treating the eyes, you can not use lenses during the entire period of treatment.

Side effect

  • Allergic reactions local: in extremely rare cases, hypersensitivity reactions develop (urticaria, Quincke's edema). More often there is itching, redness, peeling.
  • From the side of the eyes when applied: rarely - superficial punctate keratopathy, conjunctivitis, blepharitis. More often there is a slight burning sensation.
  • When taken orally: nausea, diarrhea, abdominal pain, vomiting, fatigue, skin rash, headaches, dizziness, hallucinations, insomnia or drowsiness, fever. Hair loss and changes in the blood picture are rarely observed.
  • With / in the introduction: crystalluria, acute renal failure, encephalopathy, inflammation of the veins at the injection site, vomiting and nausea.

Overdose

It is possible with parenteral and internal administration of dosage forms and accidental ingestion of cream and ointment. Symptoms: neurological disorders, headache, shortness of breath, vomiting, diarrhea, nausea, kidney dysfunction, convulsions, coma. Treatment is inpatient.

The drug under this name is better known as an external remedy for the treatment of herpes. However, there is also a tablet form of the drug intended for systemic therapy of viral infections. The drug should be used strictly for medical purposes, since there are a number of contraindications and restrictions on use.

Is acyclovir ® an antibiotic or not?

Pharmacological group

The tablet preparation is classified as an antiviral agent intended for the treatment of herpes infections.

Composition of the tablet Acyclovir ®

Like any tablet dosage form, this drug consists of the main and auxiliary components. The sodium salt active ingredient has the chemical name 2-Amino-1,9-dihydro-9-[(2-hydroxyethoxy)methyl]-6H-purine-6-OH. To put it simply, the active substance of Acyclovir ® is acyclovir, a synthetic analogue of DNA structural elements (purine nucleosides).

Once in the body, it undergoes a series of certain transformations. After entering a virus-infected cell, aciclovir is phosphorylated by thymidine kinase to form monophosphate, then diphosphate, and finally to triphosphate. It is the final compound that has antiviral activity: it integrates into the DNA of the pathogen and stops the replication process.

Reception of Acyclovir ® in tablets is indicated for the defeat of the body by the following viruses:

  • Herpes simplex - causes herpes, has several varieties; the spectrum of activity of the drug includes two of them - HSV types 1 and 2.
  • Varicella zoster is the causative agent of the well-known chicken pox, which most people get sick in childhood and receive lifelong immunity.
  • The Epstein-Barr virus is the cause of many pathologies, which include various cancers, hepatitis and other dangerous diseases.
  • Cytomegalovirus is a common subspecies of herpetic viruses that is extremely dangerous for people with immunodeficiency conditions and newborns.

In children, Epstein-Barr viruses and cytomegalovirus often cause

Release form Acyclovir ®

Based on the active substance, several dosage forms are produced that are applied externally, used for intravenous administration, as well as for oral administration. In the latter case, these are tablets, regular and prolonged action, containing 200 and 400 mg of the active ingredient, respectively.

Photo of the packaging of Acyclovir ® in the form of tablets of 400 mg

Under the original name Acyclovir ® , the antiviral agent is produced by the Belmedpreparaty ® manufacturer from Belarus and the domestic company OZON. The tablets contain 200 mg of the active ingredient, as well as calcium, milk sugar, potato starch, polyvinylpyrrolidone and aerosil. They are packed in 20 pieces in blisters and packs of cardboard, sold at a price of about 32 rubles, Acyclovir ® has a shelf life of 3 years from the date of manufacture.

In addition, the drug for oral use is produced by many Russian and foreign pharmaceutical enterprises with the addition of branded postfixes to the main name: Acyclovir-Akrikhin ® , Acyclovir-sandoz ® , Acyclovir-akos ®, etc. Tablets prolonged in a dosage of 400 mg are called Acyclovir-forte ® .

What do Acyclovir ® tablets help with?

The drug in tablet form is intended for systemic treatment of diseases caused by several types of herpeviruses. For example, tablets, especially in combination with an external ointment, are good for rashes on the lips and genital herpes. They are also prescribed for shingles and chickenpox. The treatment of chicken pox with acyclovir ® is especially important for adults: children tolerate it relatively easily, and at an older age the disease is severe and can cause complications.

Recipe Acyclovir ® in Latin

You can take pills only as directed by a doctor, since there are certain contraindications for the systemic treatment of viral infections. When filling out a prescription form, the specialist indicates in a short form the basic information about the patient (age and full name) and makes a note intended for the pharmacist in Latin with a prescription in Russian:

Rep.: Tab. Aciclovir 0.2

D.t. d. No. 20

S. 1 tablet 5 times a day.

Acyclovir ® - indications for use

Tablets are prescribed for the purpose of systemic therapy of infections of the skin and mucous membranes caused by susceptible viruses:

  • Herpes simplex, both primary and in case of relapses.
  • Genital herpes affecting the genitals.
  • Severe infection.
  • Chickenpox in adults and children, starting from the first day after the onset of a characteristic vesicular rash.
  • Shingles (this disease is a consequence of a previous chickenpox and the presence of a virus in the body).

The drug is also shown to patients with immunodeficiency (who underwent organ transplantation, undergoing chemotherapy) for the prevention and treatment of herpes sores.

Contraindications to the use of Acyclovir ®

The only strict contraindication is individual hypersensitivity to acyclovir ® itself and its predecessor valaciclovir ® . However, there are cases when caution should be exercised when using tablets. These include conditions associated with kidney failure and dehydration. The possibility of using the drug for the treatment of pregnant and lactating women is considered in the appropriate section.

Dosage and method of administration Acyclovir ® tablets

When ingested, the active substance is partially absorbed, its bioavailability does not exceed 30%. The presence of food in the stomach and intestines does not affect the rate of absorption, so you can drink tablets at any time.

Herpes simplex

For the treatment of primary and recurrent herpes provoked by Herpes simplex, it is recommended to observe a 4-hour interval during the day and an 8-hour interval at night:

  • Children from 2 years of age and adults with normal immune status are shown a 5-day course, during which you need to take 200 mg of the drug 5 times daily. For prophylactic purposes - the same single dose, but every 6 hours.
  • In the presence of HIV infection, after transplantation and during chemotherapy, a single dose is 400 mg, and the treatment and prevention regimens are similar.
  • For the treatment of children under two roses, the dosages are halved (that is, 100 m for each of 5 doses).

Chicken pox

The period of treatment of chickenpox is from 7 to 10 days, while adults and children whose body weight is above 40 kg are shown to take 800 mg of the drug 5 times a day. For a younger child, the amount of the active substance must be calculated by weight. Recommended treatment regimen: 5-day course, 20 mg of acyclovir per kilogram of body weight every 6 hours.

Shingles

The drug is prescribed according to age:

  • children under 2 years old - 200 mg per dose;
  • from two to 6 - 400 milligrams each;
  • over 6 and adults - 800 each.

Tablets should be taken four times a day at regular intervals, the full course of treatment is 5 days.

Acyclovir ® - side effects, effects and overdose

Any negative reactions of the body to taking the drug are noted quite rarely.

On the part of the digestive system, dyspeptic disorders and diarrhea are most likely. In isolated cases, there is an increased transient activity of ALaT and ASAT - liver enzymes.

On the use of Acyclovir ® in tablets, side effects from the nervous system are as follows:

  • general weakness,
  • drowsiness or agitation
  • dizziness or headache.

More severe conditions are possible only with intravenous administration or overdose. Oral medication usually does not affect the hematopoietic system. Allergy to Acyclovir as a side effect is manifested by urticaria, skin itching.

More serious body reactions occur when the recommended dose is exceeded, especially when the drug is administered parenterally. When ingested, the following overdose symptoms are mentioned: headache, shortness of breath, fever, neurological disorders, diarrhea and vomiting. In especially severe cases - convulsive syndrome, coma and lethargy (observed after a single intake of 20 grams of the active substance).

Acyclovir ® during pregnancy and breastfeeding

Large-scale clinical studies on the effect of the drug on the fetus have not been conducted. Based on the available information on women and their children who took the drug during pregnancy, it can be concluded that there is no teratogenic effect. That is, it is possible to prescribe Acyclovir during pregnancy from the 1st to the 3rd trimester, however, taking into account the possible risks, it still penetrates through the placenta.

The active substance is also excreted into breast milk in sufficiently large quantities. Therefore, the use of Acyclovir ® during breastfeeding is not recommended. It is advisable to refuse breastfeeding for the period of treatment of a viral infection, replacing feeding with a special mixture.

Acyclovir ® and alcohol - compatibility

It is known about the potential nephrotoxic effect of the antiviral agent on the kidneys due to its accumulation in the tubules. That is why it is recommended to drink more fluids during treatment and avoid taking other drugs that are dangerous to the kidneys. Can I drink alcohol while taking acyclovir ® ?

There is no direct prohibition on the joint use of alcohol with these tablets in the instructions from the manufacturers, however, it is necessary to take into account the general negative effect of ethanol on the body weakened by the disease. In addition, alcohol always increases the likelihood of side effects, especially from the nervous and digestive systems.

Acyclovir ® analogues in tablets

As already mentioned at the beginning of the article, there are quite a lot of acyclovir-based antiviral drugs. Pharmacy chains offer the following structural substitutes for the original:

  • Acyclovir-AKOS ®
  • Zovirax ®
  • Acyclovir-Acri ®
  • Acyclovir-Belupo ®
  • Virolex ®
  • Cyclovir ®
  • Acyclovir-Sandoz ®
  • Acyclovir-Akrikhin ®
  • Cyclovax ®
  • Acyclostad ®
  • Vivorax ®
  • Supraviran ®
  • Herperax ®
  • Provirsan ®
  • Lizavir ®
  • Cycloviral-SEDICO ®
  • Citivir ®

In the case of Acyclovir ®, it is simply not advisable to look for cheaper analogues. It is the original domestic drug that is the most affordable in pharmacies, while imported substitutes can cost several times more.

Zovirax ® or Acyclovir ® , which is better?

The cost of 25 tablets manufactured by GlaxoSmithKline Pharmaceuticals S.A. ® today is almost 15 times higher than the price of a domestic drug. At the same time, there is no fundamental difference in the composition of medicines, since the dose of the active substance is the same. Therefore, there are no differences in the list of indications, contraindications, as well as possible side effects.

Thus, the difference between Zovirax ® and Acyclovir ® is only in cost, manufacturer and external design. No differences in the therapeutic effect were clinically identified and confirmed.

Which is better, Acyclovir ® or Famvir ® ?

The active ingredient in Swiss-made tablets is another antiviral compound, famciclovir.


Photo famvira ® 250 mg 21 coated tablets

It is active against the same viruses, but is characterized by higher bioavailability. In addition, strains of Herpes simplex resistant to acyclovir ® are susceptible to it. Due to the longer half-life, Famvir ® is also more convenient to use (not more than 3 times a day). The only negative is the cost of 1500 rubles for a pack of 3 tablets.

What is the difference between Valacyclovir ® and Acyclovir ®

Valacyclovir ® , on the basis of which various antiviral drugs are also produced, is the precursor of acyclovir ® - the hydrochloride salt of its L-valyl ester. In infected cells, it undergoes the same transformations and acts similarly.

However, there is a difference between acyclovir ® and valaciclovir ®, which determines the higher efficiency of drugs based on the latter (for example, Valtrex ®, popular in America). In the form of a prodrug, the antiviral agent is much better and absorbed to the fullest extent.

The antiviral drug Acyclovir has proven itself against herpes. It is used in various forms, most often in the form of tablets or ointments. And in both cases it is very effective. How to take acyclovir, in what form and in what cases, will be described below.

acyclovir for herpes


With three types of herpes simplex pathogens, the drug effectively copes, the creation of which brought the US pharmacologist Gertrude Elion the Nobel Prize. Acyclovir is similar to the nucleoside, a component of DNA. It prevents the reproduction of herpes viruses at the genetic level, although the body cannot completely get rid of them. However, it perfectly fights relapses and symptoms of all three types of infections.

It is necessary to start taking Acyclovir for herpes as early as possible, at the first manifestations of the disease. This will ensure the timely distribution of the drug throughout the body. And do not neglect the advice of a doctor. Reception of Acyclovir has a serious impact on all systems and organs and should not occur uncontrollably.

Usually, to achieve the best effect, it is advised to use Acyclovir in the form of an ointment for herpes and take tablets at the same time. This has an effect on the state of the body as a whole and on local manifestations of the disease.

Acyclovir tablets


How to drink Acyclovir tablets? As a rule, in the very first case of the manifestation of herpes, while the body has not yet developed antibodies, the doctor prescribes a large dosage of the drug. With subsequent relapses, the dose is reduced.

Here are the basic rules to follow when taking Acyclovir:

  • Take Acyclovir tablets with plenty of water, at least a full glass. Pure water during treatment must be consumed a lot. This will help the kidneys deal with the effects of the infection.
  • Acyclovir should not be taken on an empty stomach. It is taken with or after food.
  • It is necessary to strictly follow the treatment regimen prescribed by the doctor and not stop taking Acyclovir even if the symptoms disappear. If herpes is not cured in time, it can cause serious complications.
  • If it was not possible to drink the medicine on time, you should not drink two tablets at once. It is better to take one, and the next according to the scheme after the required period of time.

Acyclovir has side effects and contraindications, like other active substances. Therefore, the physician prescribing treatment must be aware of the patient's health status, the presence of current and chronic diseases or allergic reactions. This is especially true for kidney problems.

If the taken Acyclovir negatively affects the body, this will become clear by the presence of such symptoms:

  • headache;
  • nausea, vomiting, bowel dysfunction;
  • painful, difficult urination;
  • lower back pain;
  • general weakness and drowsiness;
  • nosebleeds and the formation of hematomas under the skin.

Ointment Acyclovir

Usually, Acyclovir ointment is used to enhance the effect of taking pills and to get rid of the symptoms of a herpes infection as soon as possible. It works very well at the first manifestations of relapse and helps to relieve itching and swelling in the affected area. Sometimes this avoids the appearance of blistering rashes and associated painful skin injuries.

An ointment against herpes is applied several times a day. How long it takes to heal depends on the severity of the recurrence of the disease. Usually 5-7 days are enough, but often the course is extended. Acyclovir should be applied with a cotton swab to avoid the spread of infection. Preliminarily, the skin is carefully moistened with a cotton swab. Sores inside the mouth are not treated with ointment, but if it accidentally gets into the mouth, nothing needs to be done, it will not do harm. But getting the ointment in the eyes should be avoided.

It is important to remember that mixing Acyclovir with any other cream or cosmetic is by no means permissible.

With herpes on the lips

With this type of infection, the following treatment with Acyclovir in both forms is advisable:

  • in tablets - 0.2 g 5 times a day with meals for 7 days;
  • ointment is applied per day up to 6 times.

With genital herpes


With the defeat of herpes simplex of the second type, the genitals and their mucous membranes most often suffer. It manifests itself in the same way as on the lips, with itching, rashes and sores, but in the intimate area they cause much more trouble. This is also due to the fact that the ointment for genital herpes is not effective. Instead, some "home" remedies are used that have a drying, soothing and healing effect. But they can only alleviate the symptoms. Treat this type of infection with antiviral drugs in the form of tablets.

The usual dosage of taking Acyclovir in this case is as follows:

  • 10 days - a course for rectal infection - take 0.4 g 5 times a day during or after meals;
  • 7-10 days - a course for genital infections - 5 times a day, 0.2 g;
  • 5 days - prophylactic course for genital herpes - 0.2 g 2-5 times a day.

Prevention measures


When it comes to the prevention of herpes, most often refers to the prevention of recurrence of this disease. In total, 90% of people suffer from herpes. And given its extreme contagiousness, there is hardly much chance of not getting sick with it. But you can reduce the frequency of relapses to a minimum by fulfilling simple conditions:

  • Taking a prophylactic course of antiviral drugs.
  • Do not use other people's hygiene items.
  • Do not touch the affected areas with your fingers or use products to treat them more than once, so as not to transfer the infection to other vulnerable parts of the body.
  • Compliance with hygiene standards during sexual contact.
  • People who show visible signs of herpes should not be directly contacted, but genital herpes can also be contracted during a calm period, so do not neglect the means of protection, even when it seems that everything is in order.
  • Strengthening the immune system not only by taking vitamin complexes and immunomodulators, but also by proper nutrition, hardening and maintaining a healthy lifestyle.

Should be remembered

  • Alcohol while taking Acyclovir should not be taken. This can lead to temporary blurred vision, drowsiness and slow reaction time.
  • The sun's rays and solarium are also contraindicated. This substance affects the susceptibility to ultraviolet light. Therefore, during treatment with Acyclovir, it is advisable to wear clothing that protects as much as possible from the sun.
  • During pregnancy, Acyclovir is prescribed only when absolutely necessary. And expectant mothers should never self-medicate in case of a recurrence of herpes. This can lead to miscarriage.
  • If a recurrence of a herpes infection occurred during the period of breastfeeding and Acyclovir was prescribed as treatment, a pause should be made in feeding. This drug accumulates in milk.

It should be said about the availability and democracy of drugs, which include Acyclovir as an active ingredient. Here are some of the trade names for medicines containing Acyclovir: Acyclovir, Acivir, Acic, Geviran, Gerpevir, Medovir, Zovirax. All of these are drugs based on acyclovir, and they all help well with herpes. They can always be found in pharmacies in the right forms and at affordable prices.

Acyclovir belongs to the group antiviral drugs. The effectiveness of this medication has been repeatedly proven in large medical studies, along with the study of its mechanism of action and the determination of side effects. Despite the fact that the drug was invented more than 20 years ago, it remains a relevant and effective tool for combating both herpes simplex and herpes zoster viruses, chicken pox ( chickenpox), Epstein-Barr and cytomegalovirus.

A wide range of forms of release of this drug allows you to use it both systemically and locally. In addition, the therapeutic window ( range of acceptable therapeutic doses that do not cause side effects) of acyclovir is large enough to safely use it on an outpatient basis ( at home).

With a sufficiently high degree of confidence, it can be assumed that acyclovir does not have a carcinogenic effect when used systemically, that is, it does not cause the appearance of malignant tumors, which cannot be said about a number of other antiviral drugs. However, the effect of external forms of acyclovir on the skin and mucous membranes has not been thoroughly studied.

Teratogenic effect ( influence on the appearance of developmental anomalies) of this drug was also not observed in animal studies, even when using excessively high doses. There was no decrease in testicular function and sperm activity after the use of acyclovir in men.

For pregnant women, this drug is indicated only in cases where the benefits of its use outweigh the potential harm to the fetus. According to studies, women who took acyclovir during pregnancy did not show an increase in the frequency of having children with developmental anomalies, which indicates its relative safety.

However, despite all the advantages of this drug, it also has significant disadvantages. One of them is the need for frequent administration due to low bioavailability ( the amount of the drug that is completely distributed throughout the body in relation to the amount of the drug absorbed by the patient) and short half-life ( the time it takes for half of the administered dose of the drug to be eliminated from the body).

Another disadvantage is the potential nephrotoxic ( kidney damaging) the action of acyclovir. Passing through the renal tubules, the drug can cause inflammation and blockage. However, this happens only when the concentration of the drug in the primary urine reaches a high level. High concentrations may result from an excessive initial dose, rapid entry of the active substance into the body, or dehydration. Thus, to prevent acute renal failure, it is necessary to take the drug only according to the instructions and drink plenty of fluids during the entire period of treatment.

The last, but not the least, disadvantage of acyclovir is the frequent development of tolerance to it. In other words, the viruses targeted by the effect of the drug develop certain defense mechanisms against it ( To date, at least three mechanisms are known by which the herpes simplex virus is protected from the action of acyclovir.). As a result, with repeated use, the effectiveness of the drug decreases from time to time, forcing the patient and his doctor to resort to second- and third-line drugs.

Types of medication, commercial names of analogues, release forms

Acyclovir is available in the following dosage forms:
  • tablets;
  • lyophilizate for preparation of solution for intravenous drip injection;
  • ointment and cream for external use;
  • eye ointment.
The use of acyclovir does not imply any age restrictions. The choice of dosage form is based on the severity of a particular case. For outpatient treatment, you can use the tablet form of the drug, as well as a cream for external use and an eye ointment. The use of a lyophilisate for the preparation of perfusion solutions imposes some precautions, so it is preferable to use this dosage form exclusively in a hospital under the supervision of medical personnel.

Acyclovir is found in pharmacies under the following commercial names:

  • Cycloviral;
  • Cyclovir;
  • Cyclovax;
  • Supraviran;
  • Provirsan;
  • Medovir;
  • Lizavir;
  • Zovirax;
  • Herpes;
  • Herperax;
  • Gerpevir;
  • Gervirax;
  • Virolex;
  • Vivorax;
  • Acyclostad;
  • Acigerpin and others.

Manufacturers of acyclovir

Firm
manufacturer
Commercial name
drug
Producing country Release form Dosage
Stada Arzneimittel AG Acyclostad Germany Tablets
(800 mg).
The dosage of the drug depends on the type of disease, associated complications and the age of the patient.

With the herpes simplex virus, 200 mg is prescribed 5 times a day, except at night.

With chicken pox and shingles - 800 mg 5 times a day.

Children older than 2 years are prescribed the same doses as adult patients.

Children under 2 years of age are given half the dose with the same frequency of administration ( 5 times a day).

The last tablet should be taken at least 2 to 3 hours before going to bed.

The duration of treatment on average takes from 5 to 10 days.

Ozone LLC
Acyclovir Russia Tablets
(400 mg).
Obolenskoye - pharmaceutical company Acyclovir forte Russia
BELUPO d.d. Aciclovir Belupo Republic of Croatia
NIZHFARM Acyclovir Russia Tablets
(200 mg).
Salutas Pharma Aciclovir Sandoz Germany
Stada Arzneimittel AG Acyclostad Germany
KRKA Virolex Slovenia
Glaxo Wellcome Zovirax Spain
Belmedpreparaty RUE Acyclovir Republic of Belarus
Cadila Pharmaceuticals Vivorax India
PRO.MED.CS Praha a.s. Provirsan Czech Republic
GlaxoSmithKline Manufacturing S.p.A. Zovirax Italy
(250 mg).
The lyophilizate is used in severe cases of herpes simplex and genital herpes, with severe pain caused by herpes zoster, etc. The perfusion solution is made immediately before use by mixing the powder from the vial with the amount of saline indicated in the instructions ( different salts of acyclovir have different solubility in saline).

On average, adults are prescribed 5 mg of the drug per 1 kg of the patient's body weight 3 times a day. In severe complications of the disease, such as meningoencephalitis and viral pneumonia, 10 mg / kg is prescribed 3 times a day.

The maximum dose for intravenous administration is 30 mg / kg / day, and for children under 2 years old, half as much.

The introduction of the drug should be carried out exclusively drip and slowly ( at least 1 - 2 hours) to avoid acute renal failure.

KRKA Virolex Slovenia
North China Pharmaceutical Corporation Acyclovir China
Anfarm Hellas Medovir Greece
Belmedpreparaty RUE Acyclovir Republic of Belarus Lyophilisate for preparation of perfusion solution
(250 mg, 500 mg, 1 g).
VERTEX Acyclovir Russia
(5% - 2, 5, 10 mg).
A cream or ointment is applied to the affected areas of the skin at the first signs of the disease, on average 4-5 times a day.

The duration of treatment varies from 5 to 10 days.

Salutas Pharma Aciclovir GEKSAL Germany
BELUPO d.d. Aciclovir Belupo Republic of Croatia
Glaxo Wellcome Operations Zovirax Great Britain
KRKA Virolex Slovenia
Agio Pharmaceuticals Acigerpin India
Synthesis JSC Acyclovir Russia Eye ointment
(3% - 4.5, 5 mg).
A strip of ointment 0.5 - 1 cm long is placed behind the lower eyelid. Next, the eye is closed for a few minutes in order for the substance to spread through the cornea and be absorbed into it.

Apply the ointment 5 times a day for 5 to 10 days.

KRKA Virolex Slovenia
Draxis Pharma Inc. Zovirax Canada

Mechanism of therapeutic action of acyclovir

Once in the gastrointestinal tract, this medicine is absorbed into the blood only in a small amount ( approximately one fifth). With an increase in the dose that enters the body, an increase in the concentration of the drug in the blood does not occur, no matter how paradoxical it may sound. The explanation lies in the fact that acyclovir is able to penetrate the mucous membrane of the initial sections of the digestive system with a limited speed. Moreover, with an increase in the dose, there is a slight decrease in the absorption of the drug due to overload of the transport systems of the cells of the mucous membrane of the stomach and duodenum. Eating food together with taking acyclovir does not change the rate of its absorption in any way.

Once in the blood, the drug only partially binds to plasma proteins ( 9 - 33% ). For this reason, the bulk of the active substance circulates freely in the blood and is rapidly metabolized and excreted from the body. Nevertheless, with the timely intake of the next dose of the drug in the blood, its constant concentration is maintained, which ensures its penetration into all tissues of the body without exception. Thus, acyclovir freely penetrates the blood-brain and hematoplacental barrier, is found in high concentrations in the tissues of the kidneys, liver, lungs, eyes, in the secretions of the lacrimal, salivary and sex glands. In the cerebrospinal fluid, the concentration of the drug is equal to half of its concentration in the blood plasma. Absorption of the drug from the surface of the skin is moderate, and from the surface of the mucous membranes - pronounced.

It is important to note that acyclovir has a selective effect on the target virus and does not damage healthy body cells. Once in a healthy cell, it does not produce any changes in the metabolism of its substances, it is excreted unchanged and neutralized in the liver. However, when the drug enters an infected cell, it is first converted from the original acyclovir molecule to acyclovir monophosphate by a viral enzyme called thymidine kinase. Further, with the help of some enzymes of the cell itself, the drug is converted into acyclovir triphosphate, the most active form of this drug substance. Acyclovir triphosphate acts on the virus in two ways. The first way involves interaction with the DNA polymerase of the virus ( an enzyme that makes copies of the virus) and slowing down the pace of its work. This leads to the isolation of the virus and the impossibility of its spread along the nerve fibers. The second route involves the insertion of acyclovir into the DNA chain ( deoxyribonucleic acid - a carrier of genetic information) of the virus instead of purine bases ( building blocks that make up DNA). In this case, the genome of the virus becomes unstable and disintegrates.

The neutralization of this drug occurs in the liver with the help of two enzymes - alcohol dehydrogenase and aldehyde dehydrogenase. These enzymes, as you can easily guess from the name, inactivate alcohol consumed from the outside. Accordingly, the use of alcohol in parallel with treatment with acyclovir is fraught with a slowdown in the neutralization of alcohol and an excessive accumulation of the medicinal substance itself. This, in turn, leads to severe intoxication even from a small dose of alcohol and a pronounced hangover syndrome, as well as to an overdose of the drug, the outcome of which is often acute renal failure.

Excretion of the drug is carried out mainly by the kidneys. At the same time, its main part is excreted in the form of inactive metabolites and only a small part ( no more than 14% when taken orally) is active. With intravenous administration, the proportion of the active substance in the urine can reach 79%. With a low glomerular filtration rate and tubular secretion occurring during dehydration and at night, acyclovir and its metabolites tend to settle in the renal tubules and cause acute renal failure. The same side effect can develop with rapid intravenous administration of the drug, when one single dose is poured in less than one hour.

For what pathologies is it prescribed?

Acyclovir has the most pronounced directed action in relation to the herpes simplex virus of the first and second types. In addition, this drug is used to combat herpes zoster, cytomegalovirus, varicella-zoster virus, and Epstein-Barr virus, but its therapeutic effect in these cases is somewhat less pronounced.

The use of acyclovir

Name of the disease Mechanism of therapeutic action Dosage of the drug
Herpes simplex virus 1 and 2 (genital)type The drug penetrates into the infected cell and turns into an active form - acyclovir triphosphate with the help of a number of enzymes of both the cell and the virus itself. Further, this substance is integrated into the DNA molecule of the virus, causing a chain break and blocking the replication process ( breeding) of its genome. With a moderate course of the disease, adults and children are recommended to combine the systemic use of the drug with local forms.

Children under 2 years of age are prescribed 100 mg 5 times a day. The last dose of the drug should be carried out at least 2 to 3 hours before bedtime.

Outwardly, 5% ointment or cream is used 4-5 times a day, applying it in a thin layer, without rubbing it into the affected skin.

With a more severe course of the disease, treatment begins with the appointment of the drug intravenously in the form of droppers 3 times a day, 5-10 mg / kg or 0.5 g / m 2 in one dropper for both adults and children. Drip prescription of the drug involves being under the constant supervision of medical personnel.

In addition, it is important to monitor hourly diuresis ( excretion of urine) in order to determine the possible first signs of acute renal failure in time.

The rate of administration of the drug should be slow, not more than 250 ml of a standard solution in 1 hour. After the patient's condition improves and a clear positive dynamics is determined, the patient is transferred to the tablet form of the drug.

With concomitant herpetic keratitis, 3% eye ointments are used. They are laid behind the lower eyelid with a strip 0.5 - 1 cm long 5 times a day for 5 - 10 days.

Shingles
(herpes zoster)
Since this member of the herpes virus family is less responsive to treatment with this drug, increased doses of the drug are used to improve the therapeutic effect.

The optimal oral dose for adults and children over 2 years of age is 800 mg 5 times a day.

For children under 2 years of age, 400 mg 5 times a day is indicated. The course of treatment takes from 7 to 15 days, and in some cases even up to one month.

Drip and externally, the drug is prescribed in the same way as with the herpes simplex virus.

Chicken pox
(chickenpox)
Doses in the treatment of chickenpox are identical to those for herpes zoster and are 800 mg and 400 mg for adults and for children under 2 years old, respectively, 5 times a day. However, due to the fact that chickenpox is more often more severe in adults, treatment with the drug is indicated for this particular age group.

Treatment of chickenpox in children with this drug is not recommended for two reasons. Firstly, chickenpox goes away on its own with traditional treatment with brilliant green and paracetamol. Secondly, with the use of this drug, a weaker immunity against this infection is developed, which contributes to its relapse ( re-aggravation) throughout life.

Cytomegalovirus With these diseases, treatment is prescribed by a doctor on an individual basis, depending on the goals ( prevention or cure) and comorbidities of the patient.
Epstein-Barr virus

How to apply the medication?

Acyclovir is released to the pharmaceutical market in the form of four dosage forms:
  • tablets;
  • powder for solution for intravenous drip infusion;
  • cream / ointment for external use;
  • eye ointment.

Each of these forms is available in various dosages, and also has some application features.

Tablets

Tablets are available in standard doses of 200, 400 and 800 mg. Reception of acyclovir should be carried out 5 times a day only in the daytime, when the drug is not deposited in the kidneys and does not cause side effects from the genitourinary system. Food intake does not affect the absorption of acyclovir in the gastrointestinal tract, therefore, when scheduling the daily intake of this drug, one should not focus on daily meals.

The systemic use of this medicine involves some precautions. First, it is necessary to consume an increased volume of fluid during the entire period of treatment. This reduces the concentration of the drug in the urine and prevents the development of kidney disorders. Secondly, it is important to adhere to the rule - to use the last dose of the drug at least 2 - 3 hours before going to bed. Thus, at night, when the physical activity of a person is minimal, the concentration of the drug in the urine decreases. This leads to a decrease in the likelihood of acyclovir sedimentation in the renal tubules and the prevention of acute renal failure. Thirdly, it is not recommended to drink alcohol during treatment with acyclovir. These substances are neutralized in the liver by one enzyme system. When used together, the rate of neutralization of each of them decreases, which leads to two effects - severe alcohol intoxication after drinking small doses of alcohol with a severe hangover and an overdose of acyclovir. The latter effect, similar to the previous one, is dangerous for the development of acute renal failure.

With herpes simplex virus type 1 and 2, acyclovir is prescribed for adults and children over 2 years old, 200 mg 5 times a day. Children under 2 years of age are shown 100 mg 5 times a day. With the herpes virus Zoster ( shingles) adults and children over 2 years old take 800 mg of the drug 5 times a day. Children under 2 years old - 400 mg 5 times a day. With the varicella-zoster virus, the dosages are the same as for herpes zoster, but this treatment is recommended only for adults, since children tolerate this infection much more easily. Treatment with acyclovir of cytomegalovirus and Epstein-Barr virus is variable and depends on many factors, so the dose is set by the attending physician individually in each case.

Powder for solution for intravenous drip infusion

This drug is available as a lyophilisate, packaged in 250 mg, 500 mg and 1 g in 15 ml and 20 ml vials. A solution for intravenous administration is prepared as follows. First, the amount of saline required according to the instructions is added to the vial with the drug. The resulting suspension is shaken until a clear concentrated solution is formed. The resulting solution is then added to a large dropper bottle ( not less than 250 ml) after which it is stirred again until the final solution is obtained.

Before the first intravenous administration, it is mandatory to conduct a skin prick test to exclude the patient from an allergy to acyclovir. To do this, a shallow scratch is made on the palmar surface of the forearm with a scarifier or a needle point, onto which a drop of the test substance is applied ( in this case, acyclovir solution). The test is considered positive if, 5-10 minutes after the application of the substance, a pronounced area of ​​​​inflammation appears around the scratch. In this case, administering the drug intravenously is strictly contraindicated. If inflammation is not observed, then you can safely proceed to the introduction of the drug.

An important feature of the parenteral administration of acyclovir is that its concentration in the body should not increase sharply. According to numerous studies, this leads to acute renal failure. In order to avoid this complication, it is necessary that a single dose of the drug is administered for at least one hour, and preferably even more than one hour.

Doses of acyclovir for intravenous administration are approximately the same for all diseases of the herpes family. For adults and children, it is calculated based on the patient's body weight. On average, the drug is prescribed at 5 mg / kg 3 times a day. In herpetic encephalitis, the dose is doubled to 10 mg/kg 3 times a day. Thus, the maximum daily dose is 30 mg/kg. In addition, it is possible to dose the drug based on the surface area of ​​the patient's skin. This technique is more often used in the treatment of pediatric patients. According to her, acyclovir should be prescribed at a maximum dose of 1.5 g per 1 m 2 of skin surface per day, divided into 3 doses. The duration of the course of treatment depends on the severity of the disease and the tolerance of the treatment by the patient due to possible adverse reactions.

Cream / ointment for external use

Acyclovir in the form of a cream or ointment is available in aluminum tubes of 2, 5 and 10 g, in which the content of acyclovir is 5%. The drug is applied to the skin, practically without rubbing into the affected area, 5 times a day. Treatment should be started at the first signs of the disease ( local itching, mild soreness, first bullae, etc.) The duration of the drug is on average from 5 to 10 days. Acyclovir helps to reduce the growth rate of the area of ​​the affected skin, as well as the faster formation of a crust and healing of the defect. It is recommended to stop using this drug after 2-3 days after the disappearance of the focus of inflammation.

If itching, redness, swelling or other manifestations of an allergic reaction occur at the site of application of the ointment or cream, the drug should be immediately washed off the skin surface and not used in the future. In addition, you should consult a doctor to replace acyclovir with another drug that does not cause allergies.

During treatment with acyclovir, it is not recommended to independently remove the crusts that form on the surface of the vesicles. This slows down the healing process and contributes to the infection of people in contact with the sick. It is also important not to apply a topical cream or ointment to mucous membranes. This increases the likelihood of developing a local inflammatory process.

It is important to consider that acyclovir does not prevent the transmission of viruses during sexual intercourse, therefore, in order to protect both partners, it is recommended to use condoms. However, there is one feature associated with them. Vaseline, which is part of the ointment, interacts with the latex that makes up the condom, and weakens its mechanical properties. In other words, when using acyclovir ointments, the risk of condom rupture increases.

Eye ointment

Eye ointment is produced at a concentration of 3% or 30 mg / g and is found in aluminum tubes with a volume of 4.5 and 5 g. The ointment is placed behind the lower eyelid in the form of a strip 0.5 - 1 cm long. in order for the drug to spread along the cornea and be absorbed into the surrounding tissues. The ointment is applied 5 times a day. The duration of the course of treatment is from 5 to 10 days. If there are signs of allergic conjunctivitis, the use of the ointment should be discontinued and a doctor should be consulted to replace the drug.

Possible side effects

Acyclovir causes the most pronounced side effects when used systemically. When using a skin ointment, cream or eye ointment, adverse reactions are only local inflammatory-allergic in nature.

The systemic use of acyclovir is fraught with the development of disorders from:

  • digestive tract;
  • nervous system;
  • hematopoietic systems;
  • of cardio-vascular system;
  • urinary system, etc.
Gastrointestinal disorders:
  • liquid stool, etc.
Nervous system disorders:
  • dizziness;
  • excitation;
  • confusion;
  • delirium, etc.
Disorders of the hematopoietic system:
  • hemolytic anemia ( a decrease in the number of red blood cells and / or hemoglobin due to their destruction);
  • DIC ( disseminated intravascular coagulation syndrome);
  • leukopenia/leukocytosis ( decrease / increase in the number of white blood cells) and etc.
Cardiovascular disorders:
  • strong heartbeat;
  • tachycardia ( increase in heart rate);
  • functional heart murmurs;
  • chest pain;
  • cardiac arrhythmias, etc.
Urinary system disorders:
  • acute renal failure with rapid intravenous administration;
  • increase in urea and creatinine in blood serum.

If a scarification allergic test for acyclovir perfusion solution is not performed in a patient with an increased allergic background, the likelihood of developing anaphylactic shock is high.

Approximate cost of medication

The cost of acyclovir varies greatly depending on factors such as the form of release, dose, manufacturer, etc. In addition, there are also transportation costs, registration fees and mark-ups of various pharmacy chains, which can significantly change the price of the drug.

The average cost of acyclovir in various regions of the Russian Federation

City Price
Tablets
(200 mg - 20 pcs.)
Powder for solution for intravenous drip
(250 mg - 1 pc.)
Ointment / cream for external use
(5% - 5 g)
Eye ointment
(3% - 5 g)
Moscow 29 rubles 17 rubles 17 rubles 69 rubles
Kazan 32 rubles 17 rubles 19 rubles 63 rubles
Tyumen 20 rubles 16 rubles 19 rubles 62 rubles
Krasnoyarsk 24 rubles 12 rubles 18 rubles 59 rubles
Samara 20 rubles 16 rubles 18 rubles 64 rubles
Chelyabinsk 28 rubles 15 rubles 17 rubles 61 ruble

Reviews




Can acyclovir be used in children?

Acyclovir is approved for use by children of all ages.

Despite the fact that there are certain differences between the physiology of a child and an adult, the drug manufacturers do not limit its use to patients under the age of 18 years.

Acyclovir in the form of an ointment or cream for external use is prescribed for children in the same way as for adults - 5 times a day, applied to the foci of rashes on the skin. There are also no differences in the use of eye ointment. A strip of ointment 0.5 - 1 cm long is placed in the space between the eye and the lower eyelid. Then the eye is closed for a few minutes, so that the medicine spreads over the surface of the cornea and is absorbed. Such procedures are carried out 5 times a day. The duration of treatment is from 5 to 10 days. During treatment with eye ointment, it is recommended to refrain from using contact lenses in order to avoid reactive inflammation and damage to the lenses themselves.

Acyclovir tablets are prescribed for children over 2 years of age in the same dosage as for adult patients. For children under 2 years of age, acyclovir is indicated at a half dose with the same frequency of administration. Thus, with herpes types 1 and 2, children over 2 years old are shown 200 mg 5 times a day, and children under 2 years old - 100 mg 5 times a day. With herpes zoster, children over 2 years old are prescribed 800 mg 5 times a day, and children under 2 years old - 400 mg 5 times a day. The same principle applies to cytomegalovirus, varicella-zoster virus, and Epstein-Barr virus.

When using acyclovir in the form of a lyophilisate for the preparation of a solution for intravenous administration, the dose is calculated based on the patient's body weight or skin surface area in both adults and children of all ages. Thus, the optimal dose for drip administration of acyclovir is 5-10 mg/kg every 8 hours. The maximum daily dose is 30 mg/kg or 1.5 g/m 2 divided into 3 doses. The drug should be administered slowly at least 1 hour) under the supervision of medical personnel and under the control of endogenous creatinine clearance ( a laboratory indicator that evaluates kidney function).

Can aciclovir be used by pregnant and breastfeeding women?

Acyclovir is not contraindicated during pregnancy and lactation, however, its use is recommended only if the expected benefit outweighs the potential harm to the mother and the growing fetus.

This drug has a pronounced purposeful action. In other words, it affects only cells in which DNA is present ( deoxyribonucleic acid is a large molecule in which the gene is encoded) virus. Healthy body cells are absolutely not damaged by acyclovir. Thus, this antiviral agent does not cause developmental anomalies or retardation in mental and physical development in newborns. This fact was confirmed in the study of teratogenic ( causing developmental anomalies) the effect of acyclovir on rats treated with high doses of the drug for a long time. As a result of the study, it turned out that even after exorbitant doses, offspring were born without bodily defects.

On humans, such experiments have not been carried out, since they are inhumane. However, observational studies show that the percentage of children born with developmental anomalies in women who took acyclovir in the first trimester of pregnancy does not differ from those who did not take this drug. In view of the foregoing, we can conclude that this drug is safe for pregnant women, but there are some clarifications.

The first clarification is the fact that an insufficient number of women participated in the described study, which casts doubt on the correctness of the original conclusions. Secondly, among other things, acyclovir has a number of side effects that occur not only in pregnant women, but also in ordinary patients. Thus, it can cause disorders in the gastrointestinal tract, nervous system, genitourinary system, etc., which can significantly affect the course of pregnancy.

However, if there is still a need to resort to the use of this medication, then it is advisable to use only local forms, that is, ointments and creams. They do not create high concentrations of the active substance in the blood, therefore they are less dangerous in terms of side effects. The use of tablets and especially solutions for intravenous drip infusion should be avoided.

However, in exceptional cases, when there are vital indications for the use of acyclovir, the systemic forms of the drug are preferred, but under the strict supervision of medical personnel.

Is it possible to smear with acyclovir in the mouth?

Acyclovir should not be smeared in the mouth, as this may cause a local mucosal inflammatory reaction or more severe complications.

Each form of medicinal substance is intended exclusively for strictly defined routes of administration. In other words, tablets administered orally should be swallowed and only in the stomach begin to act. Powders for the preparation of solutions for intravenous drip can only be administered parenterally, since when taken orally, they will, at best, have no effect. Similarly, ophthalmic ointment and topical creams should only be used as directed.

Such restrictions are determined by the properties of the active substance. In particular, acyclovir is a rather strong irritant for the oral mucosa and in most cases causes local inflammation at the site of contact. In addition, in addition to the active substance, the cream or ointment contains many ballast substances that are not intended to be swallowed. They are most likely to cause gastrointestinal disturbances such as nausea, vomiting, epigastric pain, diarrhea, etc.

The outcome of using an ointment or cream of acyclovir in the oral cavity in a patient who does not know that he is allergic to this substance can be much more deplorable. Such cases, unfortunately, are not uncommon. The speed and severity of an allergic reaction often depends on the way the allergen enters the body. Thus, skin contact with an allergen is more likely to cause hives or allergic dermatitis. Tablets and intravenous agents are more likely to cause shock in a patient who is allergic to the injected substance. If the urticaria disappears after using several suprastin tablets, then anaphylactic shock requires urgent measures to save the patient's life, which can only be provided by medical personnel who have the necessary medicines at their disposal.

Considering that the rate of absorption of substances from the oral cavity is equivalent to intramuscular injection, with good reason one should be wary of the development of severe allergic complications in patients with an increased allergic background. These complications include angioedema (angioneurotic edema). angioedema) and anaphylactic shock. The first is manifested by progressive swelling of the soft tissues of the face with spread to the neck and upper chest. The greatest danger is the transition of edema to the glottis, leading to its closure. The second complication is anaphylactic shock, which is manifested by a sharp drop in blood pressure and loss of consciousness.

Is it possible to combine acyclovir with alcohol?

The use of alcoholic beverages during treatment with acyclovir is strongly discouraged by drug manufacturers and physicians. However, an amendment should be made that we are talking only about the use of this drug systemically, that is, in the form of tablets and droppers. Skin creams and ointments, as well as eye ointments, do not create high concentrations of the active substance in the blood, so this prohibition does not apply to them.

The reason for the incompatibility lies in the fact that both acyclovir and ethyl alcohol are neutralized in the liver using a single enzyme system. As a result, each of the substances slows down the neutralization of a competitor, leading to its accumulation in the body.

Slow excretion of ethyl alcohol leads to the fact that the patient's resistance to alcoholic beverages is significantly reduced. In other words, when drinking even a small dose of alcohol, a person quickly gets drunk and slowly sobers up. The consequence is an increase in the toxic effect of alcohol and its metabolites ( more toxic than ethyl alcohol itself) on the central nervous system and internal organs. In addition to all of the above, the next morning the patient will experience a severe hangover.

Slow elimination of acyclovir from the body leads to its accumulation and, ultimately, to an overdose with all the ensuing side effects. The most severe of these is acute renal failure, requiring the patient to prescribe extracorporeal methods for removing creatinine, urea and other protein breakdown products. In the absence of these funds ( simple or peritoneal dialysis) the patient runs the risk of entering a uremic coma. Even with assistance at this stage, there is a high probability of serious brain damage. In the absence of assistance and in the future, the patient dies in less than 1 week.

Which of the analogues of acyclovir is more effective?

To date, the vast majority of acyclovir analogues are drugs of the same high quality level. However, in rare cases, you can buy, frankly, a fake, although recently there have been fewer and fewer such cases.

Medicines are divided into 2 groups - originals and generics. Original drugs are those that were released for the first time by one of the pharmaceutical companies that spent certain resources on its development. Such companies issue a patent for an invention, according to which other competing companies do not have the right to produce the same drug for an average of 5 to 10 years. After this time, the inventing company must disclose the formula of the drug and methods of its manufacture so that other companies can release it on the market at a lower target, which would make the drug more accessible to the masses. This copy of the drug is called a generic.

However, in practice things are different. The company-inventor announces the formula and the main points of the process of obtaining the drug, keeping many secrets in secret in order to maintain market leadership for some time. Competing companies take on average another 5 to 10 years to bring the quality of their drug to the level of the original.

The result is the following picture. The first 5 - 10 years the original drug is unique in its kind. In the next 5 - 10 years, its numerous analogues appear, which are actually inferior to it in quality. In total, from 10 to 20 years after the invention of the drug, the originals are superior in quality to generics. Further, analogues are equalized with the original, which is certainly beneficial for the patient who purchases a quality product at a lower price.

Acyclovir was invented over 25 years ago. Based on the foregoing, one can easily conclude that all self-respecting pharmaceutical concerns have been producing a drug that is not inferior in quality to the original for at least 5 years. Thus, we can conclude that all generics of acyclovir are equally good for treatment.

Nevertheless, there remains, albeit small, but the chance that some unscrupulous company produces a fake product. In order to reduce the likelihood of its acquisition, it is recommended to buy medicines in large pharmacies. Such pharmacies often work with trusted suppliers who guarantee a quality product.

Will acyclovir help with herpes?

Acyclovir is highly likely to help with the herpes simplex virus. However, there are also acyclovir-resistant strains of the virus that need treatment with other drugs.

The mechanism of action of acyclovir causes the suppression of activity and the destruction of the herpes simplex virus, thereby justifying its effectiveness. According to clinical guidelines, acyclovir and similar drugs are prescribed primarily in the treatment of herpetic viral infections, regardless of the severity of the viral process. The most successful therapeutic results are noted with the early appointment of this drug.

The therapeutic effects of this drug are:

  • a significant reduction in the duration of the acute period of the disease ( the period of appearance of new rashes);
  • early formation of crusts on the surface of the rash;
  • suppression of the spread of herpetic eruptions;
  • reduction of pain intensity and general intoxication syndrome;
  • reduction in the frequency of relapses;
  • reduction in the frequency and severity of complications, etc.

The effectiveness of the treatment of the herpes virus in the acute period of the disease increases with the simultaneous use of two drug forms of the drug - oral ( tablets) and local ( ointments and creams). This ensures the suppression of viral activity both in the patient's blood and directly in the affected area. This combination is acceptable for mild and moderate forms of infection.

For the treatment of severe common forms of herpes with simultaneous damage to the eyes, skin, mucous membranes and internal organs, acyclovir is prescribed in the form of intravenous drip infusions. In parallel with this, local forms are also applied.

Acyclovir has a positive antiherpetic effect, regardless of the presence and degree of immune suppression. For this reason, it is successfully used for the prevention of herpesvirus infections in patients with severe immunodeficiency of various etiologies.

Treatment of herpes simplex virus types 1 and 2 with acyclovir is carried out in different ways, depending on the severity of the course of the disease. Based on this, various drug forms of the drug are used.

Treatment of herpes simplex with acyclovir

Pharmaceutical form Indications for use Patient's age
Adults and children over 2 years old Children under 2 years old
Ointment or cream for external use
(5% - 2, 5, 10 g)
For the first time or recurrent herpetic eruptions on the skin of the face. Ointment or cream is applied directly to the rash, covering their entire area 5 times a day. The duration of the course of treatment is 5-10 days. If skin cream / ointment gets on the oral mucosa, rinse it with plenty of water.
Eye ointment
(3% - 4.5.5 g)
Herpetic keratitis ( needs to consult an ophthalmologist). The ointment is applied to the lower eyelid in the form of a strip 0.5 - 1 cm long. Then the eyelid is lowered and the eye is closed for several minutes in order for the drug to spread and be absorbed into the cornea.

The ointment is applied 5 times a day for 5 to 10 days. During treatment, it is recommended not to use contact lenses.

Tablets
(200 mg)
The appearance of rashes on the genitals ( needs a consultation with a urologist or gynecologist). It is preferable to use tablets and cream in parallel. Acyclovir is taken 200 mg 5 times a day for 5 to 10 days.
Tablets should be taken only during the daytime, regardless of the meal. The last dose should be taken 2 to 3 hours before bedtime.
For children under 2 years of age, acyclovir is indicated at 100 mg 5 times a day for 5 to 10 days. Recommendations for use are the same as for adults.
Powder for solution for intravenous drip
(250 mg)
Severe herpetic lesions of the eyes, skin, brain and internal organs. The dose is calculated based on the patient's body weight or the area of ​​his skin. On average, 5-10 mg / kg or 500 mg / m 2 are prescribed 3 times a day. Intravenous drip administration of a single dose should last at least 1 hour. Before starting the procedure, it is necessary to conduct a scarification test to determine an allergy to the drug. It is necessary to constantly monitor the patient's condition by medical personnel. For children under 2 years old, the dose is 2 times less than in adults with the same frequency of administration. Recommendations for use are the same as for adults.

Do I need a prescription to buy acyclovir?

To date, all forms of release of acyclovir can be purchased at almost any pharmacy. However, according to the requirements and standards of the Ministry of Health, it is only possible to purchase ointments containing acyclovir as an active ingredient without a doctor's prescription. To buy tablets and solutions of this drug, you need a prescription from your doctor. This is due to the fact that acyclovir in the wrong dosages can cause serious side effects.

The most common of these are a local allergic reaction, fever, soreness at the site of application of the ointment, burning, itching, etc.

Influencing the gastrointestinal tract(gastrointestinal tract)this drug may cause:

  • nausea;
  • vomiting;
  • diarrhea
  • abdominal pain, etc.
In addition, acyclovir can adversely affect the hematopoietic system.

The most common side effects that this drug has on blood cells are:

  • hemolytic anemia ( decrease in the concentration of hemoglobin and / or erythrocytes in peripheral blood due to their premature destruction);
  • leukocytosis/leukopenia ( leukocytes in peripheral blood);
  • thrombocytosis/thrombocytopenia ( increase or decrease in the number of platelets in peripheral blood);
  • DIC ( syndrome of disseminated intravascular coagulation due to a sharp decrease in the number of platelets and clotting factors) and etc.
When taking the tablet form, crystalline forms of the drug settle in the renal tubules. To prevent this from happening, throughout the course of treatment, it is necessary to drink the tablets with plenty of liquid. It is also recommended to take the last dose of the drug at least 2 to 3 hours before bedtime, in order to reduce the concentration of the drug at night and also prevent precipitation of the drug in the kidneys. With intravenous drip, it is necessary that the rate of penetration of the drug into the blood is such that one single dose ( on average 250 - 500 mg) was administered for at least one hour.

If these conditions are not observed, the following side effects from the urinary system may occur:

  • hematuria ( the presence of blood in the urine);
  • acute renal failure with rapid intravenous administration ( a sharp decrease in the excretory function of the kidneys, accompanied by the accumulation of urea and residual nitrogen in the blood).
Aciclovir should be used with caution in patients with psychiatric disorders, as its use may lead to an aggravation of the mental state.
From the side of the nervous system, the appearance of:
  • dizziness;
  • hallucinations;
  • confusion of consciousness;
  • delirium, etc.
When breastfeeding, acyclovir passes into breast milk at approximately the same concentration as in the blood of the mother ( 0,6-1,4 ). This makes it necessary to prescribe this drug to nursing mothers with great care, only in isolated cases and according to strict indications.

What is aciclovir used for?

Acyclovir is a fairly effective antiviral agent, the most active against many viruses, which are based on a DNA molecule ( deoxyribonucleic acid - a large molecule that carries information about the genome of the virus).

However, the main field of application of this drug is the fight against herpes family viruses. This family includes 8 types of viruses, and the degree of antiviral action of acyclovir on them is different. The most pronounced effect is manifested in relation to the herpes simplex virus 1( facial) and 2 ( genital) type. Followed by herpes zoster ( shingles), varicella-zoster virus ( chickenpox), Epstein-Barr virus and cytomegalovirus. In the case of the last two representatives of this family, the antiviral effect is the least pronounced.

The action of the drug is directed exclusively to cells affected by the virus. Their distinctive feature is the presence of a special enzyme - viral thymidine kinase. This enzyme starts a chain of biochemical reactions by which acyclovir is converted from an inactive form to an active one - acyclovir triphosphate. This substance significantly slows down replication ( reproduction) of the virus, is embedded in its structure and leads to its instability and decay.

However, even when acyclovir is used against herpes simplex virus, for which it is the first-line drug, treatment failures occur. This is due to the fact that a fairly significant percentage of virus strains with resistance to this drug circulates in the population. Such a virus is called acyclovir-resistant and requires the appointment of more specific and narrowly targeted drugs, that is, drugs of the second and third line of treatment.

Which is better, acyclovir ointment or tablets?

When answering this question, it should be noted that it in itself is not entirely correct, since the ointment and tablets are dosage forms of the same substance. This means that their choice is based, rather, on the severity and manifestations of a particular disease, rather than on the subjective preferences of the patient.

Ointments and creams based on acyclovir have a local effect. Moreover, given the fact that they are perfectly absorbed into the skin and mucous membranes, their use in point manifestations of the disease is considered the most justified. Tablets have a systemic effect and are indicated for more severe forms of the disease with damage to internal organs and important nervous structures ( brain and spinal cord).

From the foregoing, one might get the impression that acyclovir in tablet form exhibits a more pronounced effect than in local form. However, in fact, the effect is equally strong in both cases, but the scope is different.

In addition, do not forget about the side effects of the drug, the severity of which increases several times when using tablets compared to ointments and creams for external use. In other words, if you treat, for example, small rashes around the lips for the first time with acyclovir tablets for 5-10 days at an average dose for an adult - 1 g per day, then the severity of side effects may outweigh the effect of treatment.

Fields of application of external and systemic dosage forms of acyclovir

local forms
(ointment and cream)
System forms
(tablets and droppers)
Local cutaneous forms of herpes simplex virus type 1
(new-onset or recurrent rarely)
Local forms of herpes simplex virus type 1
(often recurrent or with unusual localization (cheeks, forehead, chin, etc.))
Local, minor manifestations of the herpes virus type 2
(genital)
Abundant local or frequently recurrent manifestations of herpes simplex virus type 2
Herpetic stomatitis, pharyngitis, or tonsillitis
Chicken pox
(chickenpox)
Shingles
Epstein-Barr virus
Cytomegalovirus
Unspecified immunodeficiency
(for the treatment and prevention of a wide range of viruses)

Often, in severe viral infections involving both internal organs and skin, they resort to the parallel use of local and systemic dosage forms of acyclovir. Such treatment is recognized as more effective, but before starting it, it is imperative to consult with an infectious disease specialist or dermatologist.

Acyclovir is a modern highly effective drug designed to combat viral infections. It helps to quickly cope with diseases caused by the simplex virus (Herpes simplex), and is also prescribed for herpes zoster and "".

Active ingredient and pharmacy forms of Acyclovir

The active ingredient that has a detrimental effect on viruses is acyclovir - 2-Amino-1,9-dihydro-9-[(2-hydroxyethoxy)methyl]-6H-purine-6-OH (as sodium salt). The chemical formula of this substance is C8H11N5O3. It is an artificially synthesized analog of deoxyguanidine (DNA nucleotide). This compound is able to have a direct effect on the enzyme system of viruses, blocking the DNA replication of these non-cellular infectious agents.

This remedy is produced by pharmacological companies in the form of a 5% ointment for application to the skin and mucous membranes and a 3% eye ointment (supplied in tubes of 5 g). It can also be purchased in the form of tablets for oral administration (in contour packs - 10 pieces of 200 or 400 mg).

What diseases is Acyclovir prescribed for?

Acyclovir in the form of tablets for oral administration is prescribed for the treatment of viral lesions of the mucous membranes and skin.

For adult patients and children over 2 years of age, the recommended single dose is 200 mg (1 tablet). The frequency of taking the drug - 5 times a day. It is advisable to strictly maintain the time intervals between doses - 4 hours in the daytime and 8 hours at night.

Acyclovir tablets are intended for course therapy. Usually a 5-day course is prescribed.

If an immunodeficiency state is diagnosed, a single dose is twice as much - 400 mg, and the frequency of administration is similar. The required duration of the course of treatment is established by the doctor, taking into account the severity of clinical manifestations and the dynamics of the process.

If the patient's immune status is normal, but there is a need to prevent the recurrence of a herpes infection, 200 mg of Acyclovir 4 times a day is indicated for preventive purposes. In the prevention of relapse between doses, 6-hour intervals should be observed.

The permissible daily dose of this drug in the treatment of herpetic diseases is 2000 mg.

In the treatment of chickenpox ("chickenpox"), adults should take 800 mg of Acyclovir 5 times a day. The duration of the course is from 1 to 1.5 weeks. Children's dosage is determined at the rate of 20 mg / kg. The frequency of admission for children is 4 times a day, and the course continues for 5 days.

Note:if the weight of the child is from 40 kg and above, he is prescribed the same doses of the drug as adults.

It is advisable to drink the tablets during a meal or immediately after.

Important:children under 2 years old Acyclovir is not prescribed!

In the treatment of ophthalmic diseases of viral origin (herpetic keratitis), 3% Acyclovir ointment is used. A small (1 cm) strip is placed in the conjunctival sacs of both eyes 5 times a day. The drug should be taken until complete recovery, continuing the course for another 3 days after complete relief of symptoms.

Note:during the course of treatment with the use of eye ointment, it is advisable to temporarily abandon contact lenses. With a low immune status, it is recommended to use forms for external topical use in parallel and take tablets.

Mechanism of action and pharmacodynamics of Acyclovir

The active substance Acyclovir blocks the reproduction of an infectious agent. The drug shows the highest activity to herpes viruses of types 1 and 2.

Important:in the course of clinical studies it has been experimentally proven that Acyclovir is able to stop the process of reproduction and.

Frequent excess of therapeutic dosages when taking tablets can theoretically cause renal dysfunction.

Interaction of Acyclovir with other drugs

Currently, there is no data on clinically significant antagonism of Acyclovir with other drugs. The therapeutic effect is enhanced when taken in parallel with drugs,.

Probenecid is able to slow down the process of excretion from the body.

To prevent functional disorders of the kidneys, it is not recommended to take Acyclovir together with drugs that have nephrotoxic properties.

Can Acyclovir be used by pregnant and lactating women?

During pregnancy, it is undesirable to use Acyclovir in tablets, since the drug that has entered the bloodstream freely bypasses the hematoplacental barrier. The ointment can be used as prescribed by the doctor. If necessary, course treatment

dosage forms for oral administration during breastfeeding, it is desirable to transfer the baby to artificial mixtures. There are no contraindications for the use of the ointment during lactation.

How to store the drug, and what is its shelf life?

Shelf life for both tablets and ointment is 3 years. After the tube is opened, the ointment can be used for a month.

Ointment forms should be stored at temperatures ranging from +15° to +25°C.

Tablets should be kept in places shielded from sunlight and protected from moisture.

Keep away from children!

Plisov Vladimir, medical commentator

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