Acyclovir (tablets 0,2 g)
– Tabulettae Acycloviri 0,2
international nonproprietary name
Antiviral (antiherpetic) agent.
Composition of the preparation
1 tablet contains 200 mg of Acyclovir.
Acyclovir shows activity in relation to herpes simplex virus (Herpes simplex) 1 and 2 types, shingles virus (Varicella zoster), and also Epstein-Barra virus. Cytomegalovirus is less sensitive to acyclovir action. The molecular and biological mechanism of acyclovir antiviral activity is due to competitive interaction with virusthymidine kinase and step-by-step phosphorylation with formation of mono-, di- and triphosphate. Acyclovir triphosphate is built in instead of deoxyguanosine in virus DNA, inhibits DNA-polymerase of the last and suppresses replication process. At herpes acyclovir prevents the formation of new elements of an eruption, reduces probability of dermal dissemination and visceral complications, accelerates formation of crusts. Promotes pain relief in an acute phase of shingles.
About 20 % of Acyclovir is absorbed at intake, irrespective of food intake. Binding with plasma proteins is rather insignificant (9-33 %). Concentration in cerebrospinal fluid is approximately 50 % of concentration in plasma. The maximal concentration is determined after 1,5-2 h. The period of Acyclovir half-elimination is about 4 hours. It is eliminated mainly by kidneys in unchanged form, partially (10-15 %) in the form of metabolite – 9- carboxymethoxymethylguanin. The period of half-elimination is considerably increased (up to 19,5 h) at renal failure. Acyclovir passes through hematoencephalic and placental barriers, extracted with breast milk.
Tablets of acyclovir 0,2 g are indicated at primary and relapsing infections of skin and mucosa caused by virus of herpes simplex of 1 or 2 types (including genital and rectal herpes); for prophylaxis of the infections of skin and mucosa caused by virus of herpes simplex of 1 or 2 types in patients with immune system disorders; for treatment of the infections caused by viruses of shingles and chicken pox.
Treatment is recommended to start at the very first signs of disease.
Dosage and method of administration
Preparation is taken per orally, washing down with a plenty of water.
For treatment of infections of skin and mucosa caused by viruses of herpes simplex should be administrated per 1 tablet (0,2 g), 5 times a day (except for night).
For prophylaxis of infections of skin and mucosa caused by viruses of herpes simplex in patients with immune system disorders should be administrated to the adults per 1 tablet (0,2 g) 4 times a day.
For treatment of the infections caused by shingles viruses should be administrated per 4 tablets (0,8 g) 4-5 times a day.
At rectal herpetic infections should be administrated per 2 tablets (0,4 g) 5 times a day for 10 days.
At genital herpes should be administrated per 1 tablet (0,2 g) 5 times a day; for prophylaxis of genital herpetic infections relapses; 2-5 times a day for 5 days.
To the children in the age under two years should be administrated per half of dose for adults; to children elder than 2 years a dose for adults should be administrated.
Duration of course of treatment is usually 5 days. At the infections caused by shingles viruses the treatment should be continued for 3 days after disappearance of disease signs.
Preventive treatment at transplantation of organs is carried out for 6 weeks.
Application of the preparation for newborns is not recommended.
Signs: headache, neurological disorders, dyspnea, nausea, vomiting, diarrhea, renal failure, lethargy, convulsions, coma.
Treatment: maintenance of the vital functions, hemodialysis.
The intake of a plenty is recommended during treatment for the prevention of crystallization in tubular apparatus.
Headache, undue fatiguability, neurological disorders, nausea, vomiting, diarrhea, increase of contents bilirubin, urea and creatinine in blood serum, transitional increase of hepatic transaminases activity are possible at the preparation intake. Dermal allergic reactions, fever, edemas, are possible.
Hypersensitivity to Acyclovir. Restrictions to the preparation intake: pregnancy and lactation (for the period of treatment breast feeding should be stopped).
Interactions with other medicinal preparations
Probenecid decrease Acyclovir elimination(blocks tubular secretion).
The form of release
200 mg tablets. 25, 50 tablets in vials, 10 tablets in uncelled blister, 10 tablets in a blister.