Acyclovir 25

General characteristics. Structure:

Active ingredient: 25 mg of an acyclovir in 1 g of ointment.

Excipients: macrogoal 400, half-oxameasures, propylene glycol. macrogoal
cetostearyl ether.

Antiviral means for topical administration with the expressed activity against a herpes virus.

Pharmacological properties:

Pharmacodynamics. Antiviral means for external use - a synthetic analog of a nucleoside of the thymidine which is the is WILD natural component. In the infected cells containing a virus thymidinekinase there is a phosphorylation and transformation in an acyclovir monophosphate. Under the influence of acyclovir guanylate cyclase monophosphate will be transformed to diphosphate and under the influence of several cellular enzymes - to triphosphate. Sharp selectivity of action and a hypotoxicity for the person are caused by lack of necessary enzyme for formation of an acyclovir of triphosphate in intact cells of a macroorganism.

The acyclovir triphosphate inhibits synthesis (replication) of DNA of a virus three mechanisms: 1) competitively replaces деоксигуанозин triphosphate in DNA synthesis; 2) "is built in" a synthesizable chain of DNA and stops its lengthening; 3) DNK-polimsrazu enzyme of viruses oppresses. Reproduction of a virus in a human body is as a result broken. Specificity and very high selectivity of action are also caused by its preferential accumulation in the cells affected with a herpes virus.

It is highly active concerning the type Herpes simplex 1 and 2 viruses; the virus causing chicken pox and shingles (Varicella zoster); Epstein-Burra's virus (types of viruses are specified in ascending order of the size of the minimum overwhelming concentration of an acyclovir). It is moderately active concerning a cytomegalovirus. At herpes prevents formation of new elements of rash, reduces probability of skin dissimination and visceral complications, accelerates formation of crusts, reduces pain in an acute phase of the surrounding herpes. Has an immunopromoting effect.

Pharmacokinetics. At use of ointment on intact skin: absorption is minimum; is not defined in blood and urine. The affected skin: absorption is moderate; at patients with normal function of kidneys concentration in blood serum makes up to 0,28 mkg/ml, at patients with a chronic renal failure - to 0,78 mkg/ml. It is removed by kidneys (to 9.4% of a daily dose).

Indications to use:

Medicine the Acyclovir in the form of ointment is intended for external use at treatment of herpetic damages of skin and outside mucous membranes (at herpes of lips. external genitals) caused by the Herpes simplex viruses of types 1 and 2, Varicella zoster.

Route of administration and doses:

To apply only outwardly! It is recommended to use rubber gloves or fingerstalls for prevention of spread of an infection. It is necessary to appoint treatment at emergence of the first symptoms of a herpes infection.

Ointment is applied on the affected skin and outside mucous membranes a thin layer from calculation (for adults): the strip of ointment of 1,25 cm — on 25 cm2 of an affected area of 4-6 times a day is rubbed the easy movements. To children aged from 3 months up to 12 years ointment is applied a thin layer at the rate of an acyclovir of 250-500 mg/sq.m of a body surface (a strip of ointment of 1-2 mm on the site of 25 cm2), an interval between applications – 8 hours. Ointment needs to be applied also on the sites, neighboring to the struck surface.

It is necessary to apply ointment regularly; in case of the admission of the next application it is not necessary to double a dose during the following use of drug.

Treatment duration – not less than 5 days, at most 10 days.

In case of lack of effect at external use it is recommended to appoint drug in the tableted form for intake.

Features of use:

For achievement of the maximum therapeutic effect it is necessary to use drug already at the first symptoms of a disease (burning, an itch, a pricking, feeling of tension and reddening).

Ointment is not recommended to be applied on mucous membranes of an oral cavity and especially an eye since development of the expressed local inflammation is possible.

At treatment of genital herpes it is necessary to avoid sexual contacts since use of an acyclovir does not prevent transfer of a virus to partners.

For implementation of medical effect of an acyclovir the condition of immune system of an organism matters. Patients with reduced immunity (at HIV/AIDS or after transplantation of marrow) against the background of topical administration of ointment of an acyclovir should appoint system administration (tablets) of medicine, just as in case of a heavy and recurrent current of a herpes infection.

Side effects:

At the first applications there can be a burning sensation, a mild pain in the place of defeat, an itch. At hit on mucous membranes the inflammation can develop.

Interaction with other medicines:

At external use of drug interaction with other medicines is not revealed. It is established that immunostimulators can strengthen effect of an acyclovir at their combined use.

Contraindications:

Hypersensitivity to an acyclovir; infectious diseases with similar symptoms, but the called other activators; the period of pregnancy and feeding by a breast ( during treatment it is necessary to stop feeding by a breast); age up to 3 months.

Overdose:

 In case of long external use of ointment the erythema, a peeling, a burning sensation, a burn which pass after drug withdrawal are possible.

The overdose is possible at an accidental proglatyvaniye. Symptoms: headache, neurologic disturbances, short wind, nausea, vomiting, diarrhea, renal failure, lethargy, spasms, coma.

The treatment directed to maintenance of the vital functions including a hemodialysis, is carried out in the conditions of a hospital.

Storage conditions:

At a temperature not above +25 °C. Not to freeze! To store in the place, unavailable to children. Period of validity 2 years.

Issue conditions:

Without recipe

Packaging:

In tubas on 5,0 g, 7,0 g, 14,0 g and 20,0 g placed together with a leaf insert for the consumer in packs from a cardboard.