Acyclovir

General characteristics. Structure:

Active ingredient: 200 mg of an acyclovir in 1 tablet.

Pharmacological properties:

Pharmacodynamics. The acyclovir shows activity concerning a virus of a herpes simplex (Herpes simplex) of type 1 and 2, a virus of shingles (Varicella zoster), and also Epstein-Burra's virus. The cytomegalovirus is less sensitive to action of an acyclovir.

The molecular and biological mechanism of antiviral activity of an acyclovir is caused by competitive interaction with virus thymidine kinase and consecutive phosphorylation with education mono - di - and triphosphate. Triphosphate of an acyclovir is built in instead of a deoxyguanosine virus DNA, inhibits a DNA polymerase of the last and suppresses replication process. At herpes the acyclovir prevents formation of new elements of rash, reduces probability of skin dissimination and visceral complications, accelerates formation of crusts. Promotes decrease in pain in an acute phase of the surrounding herpes.

Pharmacokinetics. At intake, irrespective of meal, about 20% of an acyclovir are absorbed. Linkng with proteins of plasma is rather small (9 — 33%). Concentration in cerebrospinal fluid makes about 50% of concentration in plasma. The maximum concentration is defined by 1,5 — 2 h. The acyclovir elimination half-life at intake makes about 4 hours.

It is allocated generally with kidneys in an invariable look, partially (10 — 15%) in the form of a metabolite — a 9-karboksimetoksimetilguanin. At a renal failure the elimination half-life considerably increases (up to 19,5 h). The acyclovir gets through hematoencephalic and placental barriers, is allocated with breast milk.

Indications to use:

Tablets of an acyclovir of 0,2 g apply at primary and recurrent infections of skin and mucous membranes caused by viruses of a herpes simplex of 1 or 2 types (including genital and rectal herpes); for the prevention of infections of skin and mucous membranes caused by viruses of a herpes simplex of 1 or 2 types in patients with disturbances of immune system; for treatment of the infections caused by viruses of shingles, chicken pox.

Route of administration and doses:

Drug is accepted inside, washing down with a large amount of water.

For the treatment of infections of skin and mucous membranes caused by herpes simplex viruses appoint on 1 tablet (0,2 g) of 5 times a day (except for night).

For the prevention of infections of skin and mucous membranes caused by herpes simplex viruses in patients with disturbances of immune system appoint the adult on 1 tablet (0,2 g) 4 times a day.

For treatment of the infections caused by shingles viruses appoint 4 tablets (0,8 g) of 4 — 5 times a day.

At a rectal herpes infection appoint 2 tablets (0,4 g) of 5 times a day within 10 days.

At genital herpes appoint on 1 tablet (0,2 g) of 5 times a day; for prevention of a recurrence of a genital herpes infection — 2 — 5 times a day within 5 days.

To children under two years appoint a half of a dose of adults; to children 2 years are more senior appoint in a dose for adults.

Duration of a course of treatment makes usually 5 days. At the infections caused by viruses of the surrounding herpes, treatment is continued within 3 days after disappearance of symptoms of a disease.

Preventive treatment at organ transplantation is carried out within 6 weeks.

Use of drug for newborns is not recommended.

Features of use:

Treatment is recommended to be begun at emergence of the very first symptoms of a disease.

Precautionary measures. For the prevention of crystallization in the tubular device reception of a large amount of liquid during treatment is recommended.

Side effects:

At administration of drug the headache, increased fatigue, neurologic disturbances, nausea, vomiting, diarrhea, increase in content in blood serum of bilirubin, urea and creatinine, tranzitorny increase in activity of hepatic transaminases are inside possible. Skin allergic reactions, fervescence, hypostases, a limfoadenopatiya are possible.

Interaction with other medicines:

Probenetsid slows down removal of an acyclovir (blocks canalicular secretion).

Contraindications:

Hypersensitivity to an acyclovir. Restrictions to administration of drug are pregnancy and a lactation (for the period of treatment feeding by a breast should be stopped).

Overdose:

Symptoms. Headache, neurologic disturbances, short wind, nausea, vomiting, diarrhea, renal failure, lethargy, spasms, coma.

Treatment. Maintenance of the vital functions, hemodialysis.

Issue conditions:

According to the recipe

Packaging:

Tablets on 200 mg No. 10 (10x1 in a blister strip packaging) or No. 20 (10x2 in blister strip packagings).