Acyclovir

General characteristics. Structure:

Active ingredient: 5 g of an acyclovir in 100 g of cream.

Excipients: propylene glycol - 8,0 g; liquid paraffin (liquid paraffin) - 12,0 g; cetyl alcohol - 6,0 g; a macrogoal the 6th cetostearyl ether - 1,5 g; a macrogoal the 25th cetostearyl ether - 1,5 g; methylparahydroxybenzoate (methylparaben, нипагин) - 0,15 g; пропилпарагидроксибензоат (propylparaben, нипазол) - 0,05 g; the water purified - to 100,0 g.

Antiviral means for topical administration.

Pharmacological properties:

Pharmacodynamics. Antiviral drug - a synthetic analog of a nucleoside of thymidine. In the infected cells containing a virus thymidinekinase there is a phosphorylation and transformation in ацикловирмонофосфат. Under the influence of guanylate cyclase ацикловирмонофосфат it will be transformed in ацикловирдифосфат and under the influence of several cellular enzymes - in ацикловиртрифосфат. Sharp selectivity of action and a hypotoxicity for the person are caused by lack of necessary enzyme for formation of an atsiklovirtrifosfat in intact cells of a macroorganism.

Atsiklovirtrifosfat, "being built in" the deoxyribonucleic acid (DNA) synthesized by a virus, blocks reproduction of a virus. Specificity and very high selektivost 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 virus; the virus causing chicken pox and shingles (Varicella zoster); Epstein-Barre's virus (types of viruses are specified in ascending order of the size of the minimum overwhelming concentration (MOC) of an acyclovir). It is moderately active concerning a cytomegalovirus (TsMV).

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 shingles.

Pharmacokinetics. At use of cream 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:

Herpes simplex of skin and mucous membranes, genital herpes (primary and recurrent); the localized shingles (auxiliary therapy).

Route of administration and doses:

Outwardly. Locally. Cream the Acyclovir is applied with a thin layer (about 1,25 cm of a strip of cream on 25 cm2 of the affected skin) on affected areas of 4 - 6 times a day. It is important to begin treatment as soon as possible at the beginning of development of a disease, it is the best of all — during a prodromal stage.

Cream is applied with either a cotton plug, or clean hands to avoid additional infection of affected areas.

Treatment duration – not less than 5 days, at most 10 days. If symptoms of a disease do not disappear after 10 days of treatment, the patient should see a doctor.

Features of use:

To apply with care during pregnancy and during breastfeeding.

Cream should not be applied on mucous membranes of an oral cavity and eyes.

Efficiency of treatment by that will be higher, than therapy (is begun at the first symptoms of an infection earlier).

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.

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) should see a doctor as against the background of topical administration of cream of an acyclovir it is necessary to appoint system administration of drug, just as in case of a heavy and recurrent current of a herpes infection.

Influence on ability of control of vehicles and mechanisms. There are no data

Side effects:

Hyperemia, burning sensation, morbidity, itch, skin rash, vulvitis on site uses. Development of allergic reactions is possible.

Post-marketing experience: hypostasis in a site of application.

Interaction with other medicines:

Strengthening of effect is noted at co-administration of immunostimulators.

Contraindications:

Hypersensitivity to any component of drug.

Overdose:

Symptoms (at an accidental proglatyvaniye): headache, neurologic disturbances, short wind, nausea, vomiting, diarrhea, renal failure.

Treatment: maintenance of the vital functions, hemodialysis.

Storage conditions:

In the dry place at a temperature not over 25 ºС. To store in the place, unavailable to children. Period of validity 2 years.

Issue conditions:

According to the recipe

Packaging:

Cream for topical and external use of 5%. On 2 g, 5 g or 10 g in tubas aluminum. Each tuba together with the application instruction in a pack from a cardboard.