Belupo's acyclovir

General characteristics. Structure:

Active agent: acyclovir of 400 mg

Excipients: tablet kernel: povidone; sodium carboxymethylstarch; MKTs; silicon dioxide colloid; magnesium stearate  

Tablet cover: Opadry Pink OY24926 (gipromeloza, titanium dioxide, macrogoal, dye ferrous oxide red, dye ferrous oxide yellow).

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:

treatment of infections of skin and the mucous membranes caused by the Herpes simplex viruses of type I and II both primary, and secondary, including genital herpes.

prevention of exacerbations of the recurrent infections caused by the Herpes simplex viruses of type I and II at patients with the normal immune status;

prevention of primary and recurrent infections caused by the Herpes simplex viruses of type I and II at patients with an immunodeficiency.
as a part of complex therapy at patients with the expressed immunodeficiency: at HIV infection (a stage of 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, and also shingles — Herpes zoster).

Route of administration and doses:

Inside, in time or right after meal, washing down with enough water.
Treatment needs to be begun as soon as possible, right after emergence of the first symptoms of a disease.
The dose is established individually depending on severity of a disease.
At the treatment of infections of skin and mucous membranes caused by Herpes simplex of type I and II, to adults and children 3 years drug are more senior appoint 200 mg of 5 times a day within 5 days with 4-hour intervals during the day and with a 8-hour interval to night. In more hard cases of a disease the course of treatment can be prolonged on doctor's orders.

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

For prevention of a recurrence of the infections caused by the Herpes simplex viruses of type I and II to patients with the normal immune status and at a recurrence of a disease each 6 h appoint 200 mg 4 times a day.

For prevention of the infections caused by the Herpes simplex viruses of type I and II, to adults and children 3 years with an immunodeficiency are more senior, drug is recommended to appoint on 200 mg 4 times a day each 6 h, the maximum dose — to 400 mg of an acyclovir of 5 times a day depending on weight of an infection.

At treatment of the infections caused by Varicella zoster adult each 4 h and with a 8-hour interval appoint in the afternoon 800 mg of 5 times to night a day. Duration of a course of treatment is 7–10 days. To children 3 years are more senior appoint 20 mg/kg 4 times a day within 5 days, to children with body weight more than 40 kg appoint drug in the same dosage, as the adult.

At treatment of the infections caused by Herpes zoster adult each 6 h within 5 days appoint 800 mg 4 times a day.

At patients with a renal failure:

At treatment and prevention of the infections caused by Herpes simplex at patients with clearance of creatinine a dosage of drug it is necessary to lower less than 10 ml/min. to 200 mg 2 times a day with 12-hour intervals.

At treatment of the infections caused by Varicella zoster at patients with clearance of creatinine less than 10 ml/min. are recommended to lower a drug dosage to 800 mg 2 times a day with 12-hour intervals; at creatinine Cl to 25 ml/min. about 800 mg 3 times a day with 8-hour intervals are appointed.

Features of use:

Prolonged or repeated treatment by an acyclovir of patients with reduced immunity can lead to emergence of strains of viruses, insensitive to its action. To apply strictly on doctor's orders in order to avoid complications at adults and children 3 years are more senior.

With care appoint to patients with renal failures, patients 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.

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

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:

Drug is usually well transferred.
From a GIT: in isolated cases — abdominal pains, nausea, vomiting, diarrhea.
Laboratory indicators: the activities of enzymes of a liver passing slight increase, it is rare — small increase in levels of urea and creatinine, a hyperbilirubinemia, a leukopenia, an erythropenia.
From TsNS: seldom — a headache, weakness; in some cases tremor, dizziness, increased fatigue, drowsiness, confusion of consciousness, hallucination, paresthesia, agitation.
Allergic reactions: anaphylactic reactions, skin allergic reactions (itch, Lyell's disease, small tortoiseshell, multiformny exudative erythema, including Stephens-Johnson's syndrome), peripheral hypostases.
Others: seldom — an alopecia, fever, a mialgiya, a vision disorder, a lymphadenopathy.

Interaction with other medicines:

Simultaneous use with probenetsidy leads to increase in an average elimination half-life and decrease in clearance of an acyclovir.
At a concomitant use with nephrotoxic drugs the risk of disturbance of functions of kidneys increases.
Strengthening of effect is noted at co-administration of immunostimulators.

Contraindications:

Hypersensitivity to an acyclovir, a gantsiklovir, a famtsiklovir, a valatsiklovir or any excipient of drug.
lactation period;
children's age up to 3 years.

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:

Symptoms: oral administration of 20 g of an acyclovir did not lead to development of specific symptoms. By-effects from TsNS can be shown — spasms, a tremor, a lethargy.

Treatment: it is necessary to cause vomiting (best of all within 30 min. after administration of drug) and to accept absorbents. In case of an acute renal failure and an anury — maintenance of the vital functions, a hemodialysis.

Storage conditions:

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

Issue conditions:

According to the recipe

Packaging:

In a blister strip packaging of 7 pieces; in a pack of cardboard 5 packagings.