Acyclovir

General characteristics. Structure:

Active ingredient: an acyclovir - 200 mg. Excipients: sugar milk, aerosil, polyvinylpirrolidone low-molecular, potato starch, magnesium stearate.

Description. Tablets of white color, a ploskotsillindrichesky form, with a facet and risky.

Pharmacological properties:

Antiviral drug, the synthetic analog of an acyclic purine nucleoside possessing highly selective effect on herpes viruses. In the cells infected with a virus under the influence of a virus thymidinekinase there takes place a number of consecutive reactions of transformation of an acyclovir in mono - di - and acyclovir triphosphate. Atsiklovirtrifosfat is built in a chain of virus DNA and blocks its synthesis by means of competitive inhibition of a virus DNA polymerase.

In vitro an acyclovir is effective against a herpes simplex virus - Herpes simplex of type I and II, against the Varicella zoster virus; higher concentration are required for inhibition of a virus of Epstein - In vitro Barrel an acyclovir therapeutic and preventively is effective first of all at the viral infections caused by Herpes simplex.

At intake biological availability makes 15-30%. The acyclovir well gets into all bodies and body tissues, including a brain and skin. Linkng with proteins of plasma makes 9-33% and does not depend on its concentration in plasma. Concentration in cerebrospinal fluid makes about 50% of its concentration in plasma. The acyclovir gets through a placental barrier and collects in breast milk. The maximum concentration after intake of 200 mg of 5 times a day - 0,7 mkg/ml, time of achievement of the maximum concentration - 1,5-2 hours.

It is metabolized in a liver with formation pharmacological of inactive connection of a 9-karboksimetoksimetilguanin. The elimination half-life at adults with normal function of kidneys makes 2-3 hours. Patients with a heavy renal failure have an elimination half-life - 20 hours, at a hemodialysis - 5,7 hours (at the same time concentration of an acyclovir in plasma decreases to 60% of a reference value). About 84% are removed by kidneys in not changed look and 14% - in the form of a metabolite. The renal clearance of an acyclovir makes 75-80% of the general plasma clearance. Less than 2% of an acyclovir are brought out of an organism through intestines.

Indications to use:

• Treatment of infections of skin and the mucous membranes caused by the Herpes simplex viruses of type I and II both primary, and secondary, including genital herpes.
• Prevention of exacerbations of the recurrent infections caused by the Herpes simplex 1 and 2 viruses of types at patients with the normal immune status.
• Prevention of exacerbations of the recurrent infections caused by the Herpes simplex viruses of type I and II at patients the normal immune status.
• Prevention of primary and recurrent infections caused by the Herpes simplex viruses of type I and II in patients with an immunodeficiency.
• As a part of complex therapy of patients with the expressed immunodeficiency: at HIV infection (AIDS stage, early clinical manifestations and the developed clinical picture) and at the patients who transferred transplantation of marrow.
• Treatment of primary and recurrent infections caused by the Varicella zoster virus (chicken pox, and also shingles - Herpes zoster).

Route of administration and doses:

Is established individually depending on severity of a disease.

At the treatment of infections of skin and mucous membranes caused by Herpessimplex of type I and Iivzroslym and to children 2 years drug are more senior appoint 200 mg of 5 times a day within 5 days with 4-hour intervals during the day and from the 8th an hour interval to night. In more hard cases of a disease the course of treatment can be prolonged on doctor's orders. As a part of complex therapy at the expressed immunodeficiency, including at the developed clinical picture of HIV infection (including early clinical displays of HIV infection and a stage of AIDS), after transplantation of marrow appoint 400 mg of 5 times a day.

For prevention of a recurrence of the infections caused by the Herpessimplextipa I and II viruses to patients with the normal immune status and at a recurrence of a disease appoint 200 mg 4 times a day each 6 hours.

For prevention of the infections caused by the Herpessimplextipa I and II viruses, to adults and children is more senior than 2 years with an immunodeficiency, drug is recommended to appoint on 200 mg 4 times a day each 6 hours, the maximum dose - to 400 mg of an acyclovir of 5 times a day depending on weight of an infection.

At treatment of the infections caused by Varicellazoster adult appoint 800 mg of 5 times a day each 4 hours in the afternoon and from the 8th an hour interval to night. Duration of a course of treatment is 7-10 days. To children 2 years are more senior appoint 20 mg/kg 4 times a day within 5 days, to children with body weight more than 40 kg appoint drug in the same dosage, as the adult.

At treatment of the infections caused by Herpes zoster adult appoint 800 mg 4 times a day each 6 hours within 5 days.

At patients with a renal failure. At treatment and prevention of the infections caused by Herpes simplex at patients with clearance of creatinine a dosage of drug it is necessary to lower less than 10 ml/min. to 200 mg 2 times a day from 12 hour intervals.

At treatment of the infections caused by Varicella zoster at patients with clearance of creatinine less than 10 ml/min. are recommended to lower a drug dosage to 800 mg 2 times a day from 12 hour intervals; at clearance of creatinine to 25 ml/min. about 800 mg 3 times a day with the 8th hour intervals are appointed. Drug is accepted in time or right after meal and is washed down with enough water.

Features of use:

To apply strictly on doctor's orders in order to avoid complications at adults and children is more senior than 2 years.

With care appoint to patients with renal failures, patients of advanced age in connection with increase in an elimination half-life of an acyclovir.

At use of drug it is necessary to provide receipt of enough liquid.

At administration of drug it is necessary to control function of kidneys (level of urea of blood and creatinine of a blood plasma).

Side effects:

Drug is usually well transferred.

From a GIT: in isolated cases - abdominal pains, nausea, vomiting, diarrhea.

In blood: passing slight increase of activity of enzymes of a liver, is rare - small increase in levels of urea and creatinine, a hyperbilirubinemia, a leukopenia, an erythropenia.

From TsNS: seldom - a headache, weakness; in some cases tremor, dizziness, increased fatigue, drowsiness, hallucinations.

Allergic reactions: skin rash.

Others. seldom - an alopecia, fever.

Contraindications:

Hypersensitivity to an acyclovir, a gantsiklovir or any excipient of drug.

Administration of drug is contraindicated in the period of a lactation.

With care - dehydration, a renal failure, neurologic disturbances, including in the anamnesis.

Overdose:

Overdose cases after oral administration of an acyclovir are not registered.

Storage conditions:

List B. In the dry, protected from light place, at a temperature not above 25 °C, the place, unavailable to children.

Period of validity. 2 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets on 200 mg. On 10 tablets in a blister strip packaging. 2 blister strip packagings together with the application instruction place in a pack cardboard.