Acyclovir is an antiviral drug, a synthetic analog of acyclic purine nucleoside, which has a highly selective effect on herpes viruses. A series of sequential reactions of acyclovir transformation into mono-, di- and triphosphate acyclovir takes place inside virus-infected cells under the action of viral thymidine kinase. In vitro acyclovir is effective against herpes simplex virus – Herpes simplex type I and II, against Varicella zoster virus; higher concentrations are required for inhibition of Epstein-Barr virus.
In vivo acyclovir is therapeutically and prophylactically effective primarily in viral infections caused by Herpes simplex.
Pharmacokinetics: When taken orally bioavailability is 15-30%. Acyclovir penetrates well into all organs and tissues of the body, including the brain and skin. Binding to plasma proteins is 9-33% and does not depend on its concentration in plasma. Concentration in cerebrospinal fluid is about 50% of its concentration in plasma. Acyclovir penetrates the placental barrier and accumulates in breast milk. Cmax after oral administration of 200 mg 5 times a day is 0.7 mcg/ml, Tmax is 1.5-2 h.
Metabolized in the liver to form pharmacologically inactive compound 9-carboxymethoxymethylguanine. T1/2 in adults with normal renal function is 2-3 hours.
In patients with severe renal insufficiency T1/2 is 20 hours, with hemodialysis – 5.7 hours (with acyclovir plasma concentration decreases to 60% of the initial value).
About 84% is excreted unchanged in the kidneys and 14% – as a metabolite. Renal clearance of acyclovir is 75-80% of the total plasma clearance. Less than 2% of acyclovir is excreted from the body through the intestine.
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Weight | 0.029 kg |
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Shelf life | 4 years. |
Conditions of storage | In a dry, light-protected place at a temperature not exceeding 25 ° C. |
Manufacturer | Belupo,medicines and cosmetics d.d., Croatia |
Medication form | pills |
Brand | Belupo,medicines and cosmetics d.d. |
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