Aciclovir-Acrihin, 5% ointment 5 g

Pharmacodynamics

Antiviral drug – synthetic analog of thymidine nucleoside.In infected cells containing viral thymidine kinase, phosphorylation and conversion to acyclovir monophosphate occurs. Under the influence of guanylate cyclase acyclovir monophosphate is converted into diphosphate and under the influence of several cellular enzymes into triphosphate.

High selectivity and low toxicity for humans is conditioned by the absence of required enzyme for acyclovir triphosphate formation in intact cells of macroorganism.

Acyclovir triphosphate “integrates” into DNA synthesized by virus and blocks virus multiplication. Specificity and very high selectivity of action are also due to its predominant accumulation in cells affected by the herpes virus. It is highly active against Herpes simplex virus types 1 and 2; Varicella zoster virus and shingles virus; Epstein-Barr virus. Moderately active against cytomegaloviruses.

Pharmacokinetics

When used on intact skin: absorption is minimal; not detected in blood and urine. On affected skin:absorption is moderate; in patients with normal renal function the serum concentration is up to 0.28 µg/ml, in patients with chronic renal failure (CRF) up to 0.78 µg/ml. Excreted by the kidneys (up to 9.4% of the daily dose).

Indications

– skin infections caused by Herpes simplex virus types 1 and 2,

– genital herpes,

– herpes zoster,

– chicken pox.

Pharmacological effect

Pharmacodynamics

The antiviral drug is a synthetic analogue of thymidine nucleoside. In infected cells containing viral thymidine kinase, phosphorylation occurs and is converted into acyclovir monophosphate. Under the influence of acyclovir guanylate cyclase, monophosphate is converted into diphosphate and, under the action of several cellular enzymes, into triphosphate.

High selectivity of action and low toxicity to humans are due to the absence of the necessary enzyme for the formation of acyclovir triphosphate in intact cells of the macroorganism.

Acyclovir triphosphate, “integrating” into the DNA synthesized by the virus, blocks the reproduction of the virus. The specificity and very high selectivity of action are also due to its predominant accumulation in cells affected by the herpes virus. Highly active against Herpes simplex virus types 1 and 2; the virus that causes chickenpox and herpes zoster (Varicella zoster); Epstein-Barr virus. Moderately active against cytomegaloviruses.

Pharmacokinetics

When used on intact skin: absorption is minimal; not detected in blood and urine. On affected skin: absorption is moderate; in patients with normal renal function, the concentration in the blood serum is up to 0.28 mcg/ml, in patients with chronic renal failure (CRF) – up to 0.78 mcg/ml. Excreted by the kidneys (up to 9.4% of the daily dose).

Special instructions

To achieve the maximum therapeutic effect, it is necessary to use the drug as early as possible (at the first signs of the disease: burning, itching, tingling, a feeling of tension and redness).

The ointment is not recommended to be applied to the mucous membranes of the mouth and eyes, as severe local inflammation may develop.

When treating genital herpes, you should avoid sexual intercourse or use condoms, since the use of acyclovir does not prevent transmission of the virus to partners.

Active ingredient

Acyclovir

Composition

100 g ointment contains:

active substance:

acyclovir in terms of 100% substance – 5 g;

excipients:

propylene glycol – 40 g,

Vaseline – 12.5 g,

Vaseline oil – 7.5 g,

emulsion wax – 5 g,

macrogol (polyethylene oxide 1500)—1 g,

purified water – up to 100 g.

Pregnancy

The use of the drug is indicated only in cases where the expected benefit to the mother outweighs the potential risk to the fetus.

During the treatment period, it is necessary to decide on stopping breastfeeding.

Contraindications

Hypersensitivity to acyclovir and other components of the drug.

With caution – pregnancy, lactation, dehydration, renal failure.

Side Effects

– hyperemia, dryness, peeling of the skin;

– burning, inflammation upon contact with mucous membranes.

Allergic dermatitis may develop.

Interaction

When used externally, no interactions with other drugs were detected.

An enhanced effect is observed with the simultaneous administration of immunostimulants.

Overdose

Symptoms (if accidentally swallowed):

– headache,

– neurological disorders,

– shortness of breath,

– nausea,

– vomit,

– diarrhea,

– renal dysfunction,

– lethargy,

– convulsions,

– coma.

Treatment:

– maintaining vital functions,

– hemodialysis.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life

3 years.

Manufacturer

Akrikhin JSC, Russia