Acyclovir forte - description of the drug, instructions for use, reviews. Medicinal guide geotar Use by pregnant and lactating mothers

Compound

One tablet contains:

active substance: acyclovir - 400 mg

Excipients: potato starch, lactose (milk sugar), povidone, sugar (sucrose), sodium lauryl sulfate, magnesium stearate.

Description

Tablets are white, biconvex, oblong in shape with rounded ends, scored on one side.

Pharmacotherapeutic group

Antiviral drug

Pharmacological properties

An antiviral drug, a synthetic analog of an acyclic purine nucleoside with a highly selective effect on herpes viruses. Inside the virus-infected cells, under the action of viral thymidine kinase, a series of successive reactions of acyclovir transformation into acyclovir mono-, di- and triphosphate takes place. Acyclovir a triphosphate is integrated into the viral DNA chain and blocks its synthesis through competitive inhibition of the viral DNA polymerase.

In vitro, acyclovir is effective against the herpes simplex virus - Herpes simplex types I and II, against the Varicella zoster virus; higher concentrations are required to inhibit the Epstein-Barr virus.

Pharmacokinetics

When taken orally, bioavailability is 15-30%. Acyclovir penetrates well into all organs and tissues of the body, including the brain and skin. Plasma protein binding is 9-33% and does not depend on its plasma concentration. The concentration in the cerebrospinal fluid is about 50% of its plasma concentration. Acyclovir crosses the placental barrier and accumulates in breast milk. The maximum concentration after oral administration of 200 mg 5 times a day is 0.7 μg / ml, the time to reach the maximum concentration is 1.5-2 hours.

It is metabolized in the liver with the formation of a pharmacologically inactive compound 9-carboxymethoxymethylguanine. The elimination half-life in adults with normal renal function is 2-3 hours. In patients with severe renal insufficiency, the half-life is 20 hours, with hemodialysis - 5.7 hours (in this case, the plasma concentration of acyclovir decreases to 60% of the initial value). About 84% is excreted by the kidneys unchanged and 14% - in the form of a metabolite. The renal clearance of acyclovir is 75-80% of the total plasma clearance. Less than 2% of acyclovir is excreted from the body through the intestines.

Indications for use

Treatment of infections of the skin and mucous membranes caused by viruses Herpes simplex type I and II, both primary and secondary, including genital herpes.

Prevention of exacerbations of recurrent infections caused by viruses Herpes simplex type I and II in patients with normal immune status.

Prevention of primary and recurrent infections caused by viruses Herpes simplex type I and II in patients with immunodeficiency.

· As part of the complex therapy of patients with severe immunodeficiency: with HIV infection (AIDS stage, early clinical manifestations and a detailed clinical picture) and in patients who underwent bone marrow transplantation.

Treatment of primary and recurrent infections caused by the virus Varicella zoster(chicken pox, as well as shingles - herpes zoster).

Contraindications

Hypersensitivity to acyclovir, ganciclovir or any excipient of the drug.

Taking the drug is contraindicated during lactation.

Children's age up to 3 years (for this dosage form).

Galactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Carefully

Pregnancy; the elderly and patients receiving large doses, especially against the background of dehydration; impaired renal function; neurological disorders or neurological reactions to the intake of cytotoxic drugs (including history).

Pregnancy and lactation

Acyclovir crosses the placental barrier and accumulates in breast milk.

Use during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. If necessary, taking acyclovir during lactation requires interruption of breastfeeding.

Method of application and dosage

inside. The drug is taken during or immediately after a meal and washed down with a sufficient amount of water.

The dosage regimen is set individually depending on the severity of the disease.

In the treatment of infections of the skin and mucous membranes caused by Herpes simplex types I and II Adults

the drug is prescribed 200 mg 5 times a day for 5 days at 4-hour intervals during the day and at 8-hour intervals at night. In more severe cases of the disease, the course of treatment can be extended by a doctor's prescription up to 10 days. As part of complex therapy for severe immunodeficiency, including with an advanced clinical picture of HIV infection (including early clinical manifestations of HIV infection and the stage of AIDS), after bone marrow implantation, 400 mg is prescribed 5 times a day.

For the prevention of recurrence of infections caused by Herpessimplex type I and II viruses, patients with a normal immune status and with a relapse of the disease are prescribed 200 mg 4 times a day every 6 hours, the duration of the course is from 6 to 12 months.

For the prevention of infections caused by Herpes simplex type I and II viruses, adults with immunodeficiency, the drug is recommended to prescribe 200 mg 4 times a day every 6 hours, the maximum dose is up to 400 mg of acyclovir 5 times a day, depending on the severity of the infection.

for infection caused herpes simplex and prevention of this infection in immunocompromised patients, children over 3 years of age receive the same dose as adults.

Varicella zoster adults

the drug is prescribed 800 mg 5 times a day every 4 hours during the day and with an 8-hour interval at night. The duration of the course of treatment is 7-10 days.

for chicken pox, 20 mg / kg 4 times a day for 5 days (maximum single dose 800 mg), children from 3 years to 6 years: 400 mg 4 times a day, over 6 years: 800 mg 4 times a day within 5 days.

In the treatment of infections caused by herpes zoster, adults are prescribed 800 mg 4 times a day every 6 hours for 5 days.

In patients with impaired renal function

in the treatment and prevention of infections caused by herpes simplex, in patients with creatinine clearance less than 10 ml / min, the dosage of the drug should be reduced to 200 mg 2 times a day at 12-hour intervals.

In the treatment of infections caused by Varicella zoster, in patients with creatinine clearance less than 10 ml / min, it is recommended to reduce the dosage of the drug to 800 mg 2 times a day at 12-hour intervals; with creatinine clearance up to 25 ml / min, 800 mg is prescribed 3 times a day at 8-hour intervals.

Side effect

The drug is usually well tolerated.

From the gastrointestinal tract: in isolated cases - abdominal pain, nausea, vomiting, diarrhea.

In blood: a transient slight increase in the activity of liver enzymes, rarely - a slight increase in the levels of urea and creatinine, hyperbilirubinemia, leukopenia, erythropenia.

From the side of the central nervous system: rarely - headache; weakness; in some cases, tremor, dizziness, fatigue, exhaustion, drowsiness, insomnia, paresthesia, confusion, hallucinations, decreased concentration, agitation.

Allergic reactions: anaphylactic reactions, skin rash, itching, Lyell's syndrome, urticaria, erythema multiforme exudative, incl. Stevens-Johnson syndrome, fever.

Others: rarely - alopecia, peripheral edema, visual impairment, lymphadenopathy, myalgia, malaise.

Overdose

There have been no cases of overdose after oral administration of acyclovir.

Acyclovir forte: instructions for use and reviews

S.01.A.D Antivirals

- Treatment of infections of the skin and mucous membranes caused by virusesHerpes simplex type I and II,both primary and secondary, including genital herpes.

- Prevention of exacerbations of recurrent infections caused by virusesHerpes simplex type I and II,patients with normal immune status.

- Prevention of primary and recurrent infections caused by virusesHerpes simplex typelull atpatients with immunodeficiency.

- Treatment of primary and recurrent viral infectionsVaricella zoster(chicken pox, as well as shingles -Herpes zoster).

List B.

In a dry, dark place at a temperature not exceeding 25 ° C. Keep out of the reach of children.

2 years.

Do not use after the expiration date.

inside. The drug is taken during or immediately after a meal and washed down with a sufficient amount of water. The dosage regimen is set by the doctor and individually, depending on the severity of the disease. In the treatment of infections of the skin and mucous membranes caused by Herpes simplex type I and II: Adults: the drug is prescribed 200 mg 5 times a day for 5 days at 4-hour intervals during the day and at 8-hour intervals at night. In more severe cases of the disease, the course of treatment can be extended by a doctor's prescription up to 10 days. As part of complex therapy for severe immunodeficiency, including with an advanced clinical picture of HIV infection (including early clinical manifestations of HIV infection and the stage of AIDS), after bone marrow implantation, 400 mg is prescribed 5 times a day. For the prevention of recurrence of infections caused by Herpes simplex type I and II viruses, patients with normal immune status and with a relapse of the disease are prescribed 200 mg 4 times a day every 6 hours, the duration of the course is from 6 to 12 months. For the prevention of infections caused by Herpes simplex type I and II viruses, adults with immunodeficiency, the drug is recommended to prescribe 200 mg 4 times a day every 6 hours, the maximum dose is up to 400 mg of acyclovir 5 times a day, depending on the severity of the infection. Children: For Herpes simplex infection and prevention of this infection in immunocompromised patients, children over 3 years of age receive the same dose as adults. In the treatment of infections caused by Varicella zoster: Adults: the drug is prescribed 800 mg 5 times a day every 4 hours during the day and at 8-hour intervals at night. The duration of the course of treatment is 7-10 days. Children: for chickenpox, 20 mg / kg are prescribed 4 times a day for 5 days (maximum single dose 800 mg), children from 3 years to 6 years: 400 mg 4 times a day, over 6 years: 800 mg 4 times per day for 5 days. In the treatment of infections caused by Herpes zoster, adults are prescribed 800 mg 4 times a day every 6 hours for 5 days. In patients with impaired renal function: In the treatment and prevention of infections caused by Herpes simplex, in patients with creatinine clearance less than 10 ml / min, the dosage of the drug should be reduced to 200 mg 2 times a day at 12-hour intervals. In the treatment of infections caused by Varicella zoster, in patients with creatinine clearance less than 10 ml / min, it is recommended to reduce the dosage of the drug to 800 mg 2 times a day at 12-hour intervals; with creatinine clearance up to 25 ml / min, 800 mg is prescribed 3 times a day at 8-hour intervals.

Compound

1 tablet contains:
active substance: acyclovir 400 mg;
Excipients: potato starch, lactose (milk sugar), povidone, sugar (sucrose), sodium lauryl sulfate, magnesium stearate.

Indications for use Acyclovir Forte

Treatment and prevention of infections caused by Herpes simplex types 1 and 2 and Varicella zoster viruses:

• simple herpes of the skin and mucous membranes (primary and recurrent);
• genital herpes (primary and recurrent);
• shingles (shingles);
• chickenpox (in the first 24 hours after the onset of a typical rash);
• in patients with severe immunodeficiency (including after transplantation, when taking immunosuppressive drugs, in HIV-infected patients, during chemotherapy).

Contraindications to the use of Acyclovir Forte

• hypersensitivity to acyclovir, ganciclovir or components of the drug;
• lactation period (breastfeeding).
• children's age up to 3 years.

FROM caution the drug should be prescribed for dehydration, renal failure, neurological disorders, incl. in history.

The dosage regimen is set individually depending on the severity of the disease.
In the treatment of infections of the skin and mucous membranes caused by the Herpes simplex virus types 1 and 2, Acyclovir is prescribed 200 mg 5 times a day for 5 days at intervals of 4 hours during the day and at intervals of 8 hours at night. In more severe cases of the disease, an increase in the course of treatment is possible.
As part of complex therapy for severe immunodeficiency, including with an advanced clinical picture of HIV infection (including early clinical manifestations of HIV infection and the stage of AIDS), after bone marrow implantation appoint 400 mg 5 times a day.
For the prevention of recurrence of infections caused by the Herpes simplex type 1 and 2 virus in patients with a normal immune status and in case of relapse of the disease appoint 200 mg 4 times a day every 6 hours.
For the prevention of infections caused by the Herpes simplex virus types 1 and 2,adults and children over 2 years old with immunodeficiency, the drug is prescribed 200 mg 4 times a day every 6 hours, the maximum dose is 400 mg 5 times a day.
, adults appoint 800 mg 5 times a day at intervals of 4 hours during the day and at intervals of 8 hours at night. The duration of the course of treatment is 7-10 days. Children over 2 years old appoint 20 mg/kg of body weight 4 times a day for 5 days, children weighing over 40 kg the drug is prescribed in the same dosage as for adults.

In the treatment of herpes zoster (Herpes zoster), adults appoint 800 mg 4 times / day every 6 hours for 5 days. Children over 6 years old - 800 mg 4 times a day; 2-6 years old - 400 mg 4 times a day; under 2 years old - 200 mg 4 times a day. More precisely, the dose can be determined at the rate of 20 mg / kg, but not more than 800 mg 4 times a day. The course of treatment is 5 days.
In patients with severe renal impairment (CK) with treatment and prevention of infections caused by the Herpes simplex virus, the drug is prescribed 200 mg 2 times a day at intervals of 12 hours.
In the treatment of infections caused by the Varicella zoster virus, for patients with CC, the drug is prescribed 800 mg 2 times a day at intervals of 12 hours; at CC from 10 to 25 ml / min- 800 mg 3 times a day at intervals of 8 hours.
The drug should be taken during or immediately after a meal and drink plenty of water.

pharmachologic effect

Acyclovir is an antiviral (antiherpetic) agent for external use - a synthetic analogue of the thymidine nucleoside, which is a natural component of DNA.
In infected cells containing viral thymidine kinase, phosphorylation and conversion to acyclovir monophosphate occurs. Under the influence of acyclovir guanylate cyclase, monophosphate is converted to diphosphate and, under the action of several cellular enzymes, to triphosphate. The high selectivity of action and low toxicity to humans are due to the lack of the necessary enzyme for the formation of acyclovir triphosphate in intact cells of the macroorganism.

Acyclovir triphosphate inhibits the synthesis (replication) of viral DNA by three mechanisms: 1) competitively replaces deoxyguanosine triphosphate in DNA synthesis; 2) "embeds" in the synthesized DNA chain and stops its elongation; 3) inhibits the enzyme DNA polymerase of viruses. As a result, the reproduction of the virus in the human body is disrupted.
The specificity and very high selectivity of action are also due to its predominant accumulation in cells affected by the herpes virus.
Highly active against Herpes simplex viruses 1 and 2 types; the virus that causes varicella and shingles (Varicella zoster); Epstein-Barr virus (types of viruses are listed in ascending order of the value of the minimum inhibitory concentration of acyclovir).

Moderately active against cytomegalovirus.
With herpes, it prevents the formation of new elements of the rash, reduces the likelihood of skin dissemination and visceral complications, accelerates the formation of crusts, and reduces pain in the acute phase of herpes zoster. It has an immunostimulating effect.

Side effects of Acyclovir Forte

From the digestive system: in isolated cases - abdominal pain, nausea, vomiting, diarrhea; rarely - a transient increase in the activity of liver enzymes, hyperbilirubinemia.
From the hematopoietic system: rarely - leukopenia, erythropenia.
From the side of the central nervous system: rarely - headache, weakness; in some cases - tremor, dizziness, fatigue, drowsiness, hallucinations.
Allergic reactions: skin rash; rarely - allergic dermatitis (when using the ointment).
Others: rarely - alopecia, fever, increased levels of urea and creatinine.

special instructions

With caution, Acyclovir should be prescribed to patients with impaired renal function, elderly patients due to an increase in the half-life of acyclovir.
When using the drug, it is necessary to ensure the flow of a sufficient amount of liquid.
The ointment is not recommended to be applied to the mucous membranes of the mouth, eyes, genitals, because. development of the expressed local inflammation is possible.
The effectiveness of treatment when applying the ointment will be the higher, the earlier it is started.
In patients with immunodeficiency with multiple repeated courses of treatment, the formation of viral resistance to acyclovir sometimes occurs.
When taking the drug, kidney function (blood urea and plasma creatinine) should be monitored.

drug interaction

With simultaneous use with probenecid, the mean half-life increases and the clearance of acyclovir decreases.
When taken simultaneously with nephrotoxic drugs, the risk of developing renal dysfunction increases.

Storage conditions

Store in a dry, dark place, out of the reach of children, at a temperature not exceeding 25°C.