Atsiklovir-Pharmak (tablets)

General characteristics. Structure:

Active ingredient: aciclovir;

1 tablet contains an acyclovir in terms of 100% substance of 0,20 g;

excipients: potato starch, cellulose microcrystallic, sodium of a kroskarmeloz, povidone, polyethyleneglycol 4000, silicon dioxide colloid anhydrous, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Antiviral means. Vysokoizbiratelno is active concerning viruses of herpes of the person (including the Herpes simplex virus of the 1st and 2nd types), the Varicella zoster virus, Epstein-Burra's virus and a cytomegalovirus. The mechanism of antiviral activity consists in suppression of replication of viruses by competitive interaction with a virus thymidinekinase, inhibition of a DNA polymerase and blockade of replication of virus DNA. 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. It is soaked up from digestive tract not completely (about 20% of the accepted dose), irrespective of meal. The maximum concentration is reached in 1,5-2 hours. Linkng with proteins of plasma insignificant (9-33%). It is a little metabolized by a liver. Gets through hematoencephalic and placental barriers, it is allocated with breast milk. It is brought out of an organism by kidneys by glomerular filtering and canalicular secretion: 85-90% in not changed look, 10-15% - in the form of a metabolite (9-karboksimetoksimetilguanin). The elimination half-life makes about 3 hours. At a renal failure (deterioration in glomerular filtering) the elimination half-life increases. At decrease in glomerular filtering lower than 10 ml/min. a dose of an acyclovir need to be adjusted towards reduction.
Pharmaceutical characteristics.

Main physical and chemical properties: tablets of white or almost white color with a flat surface, a hyphen and a facet.

Indications to use:

Treatment and prevention of primary and recurrent herpetic damages of skin and the mucous membranes caused by the Herpes simplex viruses of types 1 and 2 (including genital herpes).
Treatment of the infections caused by Varicella zoster (shingles, chicken pox).
Treatment of the infections caused by Herpes simplex in patients with an immunodeficiency.
Prevention and treatment of the infections caused by a herpes virus in patients with a heavy immunodeficiency namely: at patients with the developed HIV infection stage  (at patients of patients with AIDS, at patients with the AIDS-associated complexes) and after transplantation of marrow.

Route of administration and doses:

Treatment of the infections caused by a herpes simplex virus.

The acyclovir is accepted on 200 mg of 5 times a day by each 4 hours, excepting the night period. The course of treatment – 5 days, in case of a heavy current can be continued up to 10 days.
At patients with an immunodeficiency (for example, after transplantation of marrow) or at patients with reduced comprehensibility in intestines the dose makes 400 mg.

To children of 2 years with reduced immunity the same doses, as the adult are applied to treatment and prevention of herpes infections.

Treatment needs to be begun in a prodromal stage (at a disease recurrence) or after emergence of the first signs of damage of skin.

Prevention of a recurrence of the infections caused by a herpes simplex virus.

At patients with normal immunity the acyclovir is accepted on 200 mg by 4 times a day each 6 hours or on 400 mg 2 times a day with a 12-hour interval.
At patients with an immunodeficiency (for example, after transplantation of marrow) or at patients with reduced comprehensibility in intestines the dose makes 400 mg.
Duration of preventive use depends on risk period duration.

Treatment of chicken pox and shingles.

The acyclovir is accepted on 800 mg of 5 times a day by each 4 hours, excepting the night period. A course of treatment – 7 days.
For treatment of chicken pox to children from 2 to 6 years appoint 400 mg 4 times a day each 6 hours, to children of 6 years – 800 mg 4 times a day. Treatment duration - 5 days.
For achievement of the best result treatment should be begun with the advent of the first rashes.

Prevention and treatment of the infections caused by a herpes virus in patients with a heavy immunodeficiency.

At patients with considerably reduced immunity the dose of an acyclovir makes 800 mg 4 times a day.
Treatment duration at patients after transplantation of a brain makes 6 months. At patients with the developed stage of HIV infection makes 12 months, for preservation of effect it is desirable to prolong a course of treatment.

Elderly patients.

Such patients have a probability of a renal failure therefore the dose of drug needs to be changed. It is necessary to support the adequate level of hydration.

Patients with a renal failure.

At a renal failure at adults (clearance of creatinine less than 10 ml/min.) for treatment and prevention of the infections caused by the Herpes simplex virus, drug is appointed on 1 tablet (200 mg) by 2 times a day. For treatment of chicken pox, the surrounding herpes, and also patients with the expressed immunodeficiency are recommended to appoint: at clearance of creatinine less than 10 ml/min. – on 4 tablets (800 mg) 2 times a day; at clearance of creatinine of 10-25 ml/min. – on 4 tablets (800 mg) 3 times a day.

Features of use:

Use during pregnancy or feeding by a breast.

Use of drug at pregnancy is possible if the expected positive effect for mother exceeds potential risk for a fruit. The acyclovir at oral administration of 200 mg of 5 times a day gets into breast milk in concentration 0,6-4,1 according to acyclovir level in plasma. Potentially the child can acquire an acyclovir in a dose of 0,3 mg/kg of body weight a day therefore women need to appoint an acyclovir during feeding a breast with care when the advantage for mother exceeds potential risk for the child.
Children.

The acyclovir is applied to treatment and prevention of the infections caused by a herpes simplex virus, to children with an immunodeficiency and also for treatment of chicken pox at children 2 years are more senior. This dosage form is not applied to children under 2 years.

The dose of an acyclovir should be reduced to patients with a renal failure owing to reduced renal clearance. At elderly patients the functional condition of kidneys can be broken therefore at this group of patients it is recommended to reduce a drug dose. Elderly patients and patients with a renal failure therefore they have to be under constant control for identification and treatment of side reactions treat risk groups of emergence of side reactions from a nervous system. It is noted that the arisen side reactions have reversible character after drug withdrawal. It is necessary to pay attention to adequate hydration of patients who receive high doses of an acyclovir. Prolonged treatment by drug increases risk of emergence of side effects.
Ability to influence speed of response at control of motor transport or work with other mechanisms.

Considering that sensitive patients at use of drug can have by-effects (dizziness, drowsiness, confusion of consciousness, a spasm), for the period of administration of drug it is necessary to refrain from the driving of transport and performance of work requiring special attention.

Side effects:

The side reactions which are listed below are classified by systems of an organism and frequency of their emergence. On the frequency of emergence are divided into such categories: very often ≥ 1/10, it is frequent ≥1/100 and <1/10, infrequently ≥ 1/1000 and <1/100,   is rare ≥ 1/10000 and <1/1000, is very rare <1/10000.

From system of blood and lymphatic system:

very seldom: change of hematologic indicators (lymphocytopenia, neutropenia, leukopenia, thrombocytopenia, anemia), phlebitis.

From the central nervous system:

often: headache, dizziness;

very seldom: drowsiness, excitability, irritability, confusion of consciousness, tremor, ataxy, dysarthtia, spasms, hallucinations, psychotic symptoms, encephalopathy, coma.
The specified side reactions are reversible and arise generally at patients with a renal failure and other risk factors.

From the alimentary system:

often: nausea, vomiting, diarrhea, abdominal pain;

seldom: tranzitorny increase in blood of bilirubin and liver enzymes;

very seldom: jaundice, hepatitis, anorexia.

From respiratory system:

very seldom: asthma.

From an urinary system:

seldom: increase in level of urea and creatinine, a crystalluria, pain in kidneys which can be connected with a renal failure and a crystalluria;

very seldom: acute renal failure.

From skin:

often: an itch, rashes which can be connected with a photosensitization;

infrequently: urticaria, a diffusion hair loss (accurate communication with an acyclovir is not revealed).

Allergic reactions:

seldom: Quincke's disease, Stephens-Johnson's syndrome, toxic epidermal necrolysis, reactions of immediate hypersensitivity (anaphylactic and anaphylactoid).

Others: very seldom: weakness, fatigue, temperature increase.

Interaction with other medicines:

At simultaneous use with probenetsidy, Cimetidinum slows down removal of an acyclovir, with a zidovudine – the risk of defeat of a nervous system, with nephrotoxic drugs (aminoglycosides, Amphotericinum In, bacitracin, Vancomycinum, a methotrexate, polymyxins, drugs of gold, lithium, X-ray contrast drugs, rifampicin, streptomycin, streptocides, ciprofloxacin increases, etc.) – toxic influence on kidneys increases. At simultaneous use with immunosuppressants at treatment of patients after organ transplantation acyclovir level in plasma and an inactive metabolite of immunosuppressive drug increases, but owing to a wide therapeutic index of an acyclovir to adjust a dose there is no need.

Contraindications:

Drug is contraindicated to patients with hypersensitivity to an acyclovir and a valatsiklovir.

Overdose:

Symptoms: headache, neurologic disturbances, short wind, nausea, vomiting, diarrhea, renal failure, lethargy, spasms, coma. At the patient with accidental overdose of an acyclovir in a dose of 20 g the toxic effect was not revealed. At accidental repeated overdose of a peroral acyclovir within several days there are gastroenterological (nausea, vomiting, diarrhea) also neurologic symptoms (a headache, neurologic disturbances).

Treatment: gastric lavage, symptomatic treatment, hemodialysis.

Storage conditions:

Period of validity. 3 years. To store in the place, unavailable to children, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister; on 2 blisters enclosed in a pack.