Atsiklovir-akos

General characteristics. Structure:

Tablets of white color, ploskotsilindrichesky, with a facet and risky.

Active ingredient:  acyclovir  of 200 mg

Excipients: potato starch, magnesium stearate, talc.

Pharmacological properties:

Antiviral drug, the synthetic analog of an acyclic purine nucleoside possessing highly selective effect on herpes viruses. 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.

In vitro an acyclovir is active concerning Herpes simplex of type 1 and 2, Varicella zoster; higher concentration are required for inhibition of a virus of Epstein-Burra.

In vivo an acyclovir therapeutic and preventively is effective first of all at the viral infections caused by Herpes simplex.

 

Pharmacokinetics. Absorption

At intake bioavailability of an acyclovir makes 15-30%. Cmax after administration of drug inside in a dose of 200 mg of 5 times/days is reached in 1.5-2 h and makes 0.7 mkg/ml.

Distribution

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.

Metabolism

It is metabolized in a liver with formation pharmacological of an inactive metabolite of a 9-karboksimetoksimetilguanin.

Removal

T1/2 at adult patients with normal function of kidneys makes 2-3 h. The renal clearance of an acyclovir makes 75-80% of the general plasma clearance. Less than 2% of an acyclovir are brought out of an organism through intestines, about 84% are removed by kidneys in not changed look and 14% - in the form of a metabolite.

Pharmacokinetics in special clinical situations

Patients with a heavy renal failure have T1/2 - 20 h, at a hemodialysis – 5.7 hour (at the same time concentration of an acyclovir in plasma decreases to 60% of a reference value).

Indications to use:

— treatment of infections of skin and the mucous membranes caused by the Herpes simplex virus of type 1 and 2 both primary, and secondary, including genital herpes;

— prevention of exacerbations of the recurrent infections caused by the Herpes simplex virus of type 1 and 2 in patients with the normal immune status;

— prevention of primary and recurrent infections caused by the Herpes simplex virus of type 1 and 2 at patients with an immunodeficiency;

— as a part of complex therapy at patients with the expressed immunodeficiency: at HIV infection (a stage AIDS, early clinical manifestations and the developed clinical picture) and at the patients who transferred transplantation of marrow;

— treatment of primary and recurrent infections caused by the Varicella zoster virus (chicken pox, shingles).

Route of administration and doses:

The mode of dosing is set individually depending on severity of a disease.

At the treatment of infections of skin and mucous membranes caused by the Herpes simplex virus of type 1 and 2, to adults and children 2 years drug are more senior appoint 200 mg of 5 times / within 5 bucketed days of 4 h during the day and with an interval of 8 h to night. In more hard cases of a disease increase in a course of treatment is possible.

As a part of complex therapy at the expressed immunodeficiency, including at the developed clinical picture of HIV infection (including early clinical displays of HIV infection and a stage AIDS), after implantation of marrow appoint 400 mg of 5 times /

For prevention of a recurrence of the infections caused by the Herpes simplex virus of type 1 and 2 to patients with the normal immune status and at a recurrence of a disease 4 each 6 h appoint 200 mg.

For prevention of the infections caused by the Herpes simplex virus of type 1 and 2, to adults and children 2 years with an immunodeficiency are more senior, drug is appointed on 200 mg by 4 each 6 h, the maximum dose - 400 mg of 5 times/days.

At treatment of the infections caused by the Varicella zoster virus adult appoint 800 mg of 5 bucketed times/days of 4 h during the day and with an interval of 8 h to night. Duration of a course of treatment is 7-10 days. To children 2 years are more senior appoint on 20 mg/kg of body weight 4 within 5 days, to children weighing more than 40 kg appoint drug in the same dosage, as the adult.

At treatment of the surrounding herpes (Herpes zoster), adult each 6 h within 5 days appoint 800 mg 4sut.

At patients with the expressed renal failures (KK <10 ml/min.) at treatment and prevention of the infections caused by the Herpes simplex virus, appoint drug on 200 mg of 2 bucketed 12 h.

At treatment of the infections caused by the Varicella zoster virus, to patients with KK <10 ml/min. appoint drug on 800 mg of 2 bucketed 12 h; at KK from 10 to 25 ml/min. - on 800 mg of 3 bucketed 8 h.

Drug should be accepted in time or right after meal and to wash down with enough water.

Ointment is applied on the struck surface of 5 times / (in 4 h). Treatment duration - 5-10 days.

Features of use:

With care patients should appoint drug with renal failures, the patient of advanced age in connection with increase in an elimination half-life of an acyclovir.

At use of drug it is necessary to provide receipt of enough liquid.

An eye, genitalias since development of the expressed local inflammation is possible is not recommended to apply ointment on mucous membranes of an oral cavity.

Efficiency of treatment at ointment use by that will be higher, than earlier it is begun.

Patients to an immunodeficiency at repeated repeated courses of treatment sometimes have a formation of resistance of viruses to an acyclovir.

At administration of drug it is necessary to control function of kidneys (level of urea of blood and creatinine of a blood plasma).

Side effects:

From the alimentary system: in isolated cases - abdominal pains, nausea, vomiting, diarrhea; seldom - tranzitorny increase in activity of enzymes of a liver, a hyperbilirubinemia.

From system of a hemopoiesis: seldom - a leukopenia, an erythropenia.

From TsNS: seldom - a headache, weakness; in some cases - a tremor, dizziness, increased fatigue, drowsiness, hallucinations.

Allergic reactions: skin rash; seldom - allergic dermatitis (at ointment use).

Local reactions: at use of ointment it is possible - reddening, an itch, a peeling, burning or a pricking.

Others: seldom - an alopecia, fever, increase in levels of urea and creatinine.

Interaction with other medicines:

At simultaneous use with probenetsidy the average elimination half-life increases and the clearance of an acyclovir decreases.

At a concomitant use with nephrotoxic drugs the risk of development of disturbances of functions of kidneys increases.

At external use of Atsiklovira-AKOS interaction with other medicines is not revealed.

Contraindications:

— hypersensitivity to an acyclovir, a gantsiklovir or components of drug;

— period of a lactation (breastfeeding).

With care it is necessary to appoint drug at dehydration, a renal failure, neurologic disturbances, including in the anamnesis.

 

Use of drug ATSIKLOVIR-AKOS at pregnancy and feeding by a breast
Use of drug at 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.

 

Use at renal failures
At patients with the expressed renal failures (KK <10 ml/min.) at treatment and prevention of the infections caused by the Herpes simplex virus, appoint drug on 200 mg of 2 bucketed 12 h.

At treatment of the infections caused by the Varicella zoster virus, to patients with KK <10 ml/min. appoint drug on 800 mg of 2 bucketed 12 h; at KK from 10 to 25 ml/min. - on 800 mg of 3 bucketed 8 h.

Overdose:

Now about cases of overdose of the drug Atsiklovir-AKOS it was not reported.

Storage conditions:

Drug in the form of tablets should be stored in dry, protected from light, the place, unavailable to children, at a temperature not above 25 °C. List B. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

10 - planimetric strip packagings (2) - packs cardboard.
10 - planimetric strip packagings (3) - packs cardboard.