Belupo's acyclovir

General characteristics. Structure:

Active agent: acyclovir of 50 mg

Excipients: propylene glycol; mix glyceryl of monostearate and macrogoal-100 of stearate; cetostearyl alcohol (cetyl alcohol of 60%, stearyl alcohol of 40%); oil mineral; vaseline; sodium lauryl sulfate; water; Acidum hydrochloricum.

Pharmacological properties:

Pharmacodynamics. An acyclovir — antiviral drug, a synthetic analog of an acyclic purine nucleoside — a dezoksiguanidin, possessing highly selective effect on viruses of herpes and being the DNA component. 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. The acyclovir triphosphate is built in a chain of virus DNA and blocks its synthesis by means of competitive inhibition of a virus DNA polymerase. Thus, defective virus DNA forms that leads to suppression of replication of new generations of viruses.

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 is required for inhibition of a virus of Epstein - In vivo Barrel an acyclovir therapeutic and preventively is effective first of all at the viral infections caused by Herpes simplex.

Pharmacokinetics. 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. Cmax after appointment in 200 mg of 5 times a day — 0,7 mkg/ml, Tmax — 1,5–2 h.

It is metabolized in a liver with formation pharmacological of inactive connection — a 9-karboksimetoksimetilguanin.

T1/2 at adults with normal function of kidneys makes 2–3 h. Patients with a heavy renal failure have T1/2 — 20 h, at a hemodialysis — 5,7 h (at the same time concentration of an acyclovir in plasma decreases to 60% of a reference value).
About 84% are allocated with 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 plasmatic clearance. Less than 2% of an acyclovir are brought out of an organism through intestines.

Indications to use:

The skin infections caused by the Herpes simplex virus of types I and II, genital herpes, shingles, chicken pox.

Route of administration and doses:

Outwardly. Drug is applied on the damaged sites of skin of 5 times a day (each 4 h) with a thin layer on the sites of skin struck and adjoining on them. Cream is applied with a cotton plug, or clean hands to avoid additional infection of affected areas. Therapy should be continued till that time while on bubbles the crust is not formed or until they completely begin to live. Treatment duration — not less than 5 days, at most — 10 days.

Features of use:

For achievement of the maximum therapeutic effect it is necessary to begin to use drug as soon as possible after the beginning of an infection (at the first symptoms of a disease: burning, itch, pricking, feeling of tension and reddening). Cream is not recommended to be applied on mucous membranes of an oral cavity and eyes since development of the expressed local inflammation is possible.

The acyclovir does not prevent transfer of herpes sexually therefore during treatment it is necessary to abstain from sexual contacts, even in the absence of clinical manifestations.

Side effects:

Hyperemia, dryness, skin peeling; burning, an inflammation at hit on mucous membranes. Development of allergic dermatitis is possible.

Interaction with other medicines:

Strengthening of effect at co-administration of an immunostimulator is possible.

Contraindications:

- the skin infections caused by the Herpes simplex virus of types I and II, genital herpes, shingles, chicken pox.
- hypersensitivity to an acyclovir, a gantsiklovir, a famtsiklovir, a valatsiklovir or any excipient of drug.

With care:
dehydration;
renal failure;
neurologic disturbances, including in the anamnesis.

Use at pregnancy and feeding by a breast
Use during pregnancy is possible only in that case when the estimated advantage for mother exceeds potential risk for a fruit.
The acyclovir gets through a placental barrier and collects in breast milk. In need of reception of an acyclovir in the period of a lactation breastfeeding interruption is required.

Overdose:

Hyperemia, dryness, skin peeling; burning, an inflammation at hit on mucous membranes. Development of allergic dermatitis is possible.

Storage conditions:

At a temperature not above 25 °C.
To store in the place, unavailable to children.

Issue conditions:

Without recipe

Packaging:

In tubas of aluminum 2, 5 or 10 g; in a pack a cardboard 1 tuba.