Atsiklovir-Darnitsa, the tab. on 0,2g No. 20

General characteristics. Structure:

Active ingredient: aciclovir;

1 tablet contains an acyclovir in terms of 100% anhydrous substance of 200 mg;

excipients: potato starch, povidone, calcium stearate.

Pharmacological properties:

Pharmacodynamics. An acyclovir – antiviral drug, 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 oppression of replication of viruses by competitive interaction with a virus thymidinekinase, oppression of a DNA polymerase and blockade of replication of virus DNA.

Pharmacokinetics. It is soaked up from digestive tract not completely (    about 20% of the accepted dose), food does not influence bioavailability. The maximum concentration is reached in 1,5-2 h. 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 in breast milk. It is brought out of an organism by kidneys: 85-90% in not changed look, 10-15% – in the form of a metabolite (9-karboksimetoksimetilguanin). The elimination half-life makes about 3 h. At a renal failure (deterioration in glomerular filtering) the elimination half-life of drug increases.

Pharmaceutical characteristics.

Main physical and chemical properties: tablets of white color with a facet and risky.

Indications to use:

Prevention and treatment of primary and recurrent herpetic damages of skin and mucous membranes which are caused by the Herpes simplex viruses of types 1 and 2 (including genital herpes), Varicella zoster (surrounding herpes, chicken pox), prevention of a Cytomegaloviral infection after transplantation of marrow.

Route of administration and doses:

For treatment of the infections caused by a herpes simplex virus it is necessary to take the pill Atsiklovir-Darnitsa in a dose of 200 mg of 5 times a day with approximately 4-hour interval, except for the night period.

Treatment has to last 5 days, but in case of heavy primary infection it can be continued.

For some patients with reduced immunity (after transplantation of marrow) or for patients with reduced comprehensibility in intestines the dose can be doubled to 400 mg.

Treatment needs to be begun as soon as possible after the beginning of development of an infection. In case of recurrent herpes it is the best of all to begin treatment in a prodromal stage 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 adults.

At patients with normal immunity for prevention of a recurrence of the infections caused by a virus of a herpes simplex, the pill Atsiklovir-Darnitsa in a dose of 200 mg is taken by 4 times a day with approximately 6-hour interval.

For observation of possible changes of the natural course of a disease therapy of Atsiklovirom-Darnitsa has to be interrupted periodically with an interval of 6-12 months.

Prevention of the infections caused by a herpes simplex virus at adults.

For prevention of the infections caused by a herpes simplex virus at patients with reduced immunity of the tablet Atsiklovir-Darnitsa in a dose of 200 mg it is necessary to accept   4 times a day with approximately 6-hour interval. At patients with considerably reduced immunity (for example, after transplantation of marrow) or at patients with reduced comprehensibility in intestines the dose can be doubled to 400 mg or the corresponding dose is applied to intravenous administration.

Duration of preventive use is defined by risk period duration.

Treatment of chicken pox and the surrounding herpes at adults.

For treatment of the infections caused by viruses of chicken pox and the surrounding herpes, it is necessary to take the pill Atsiklovir-Darnitsa in a dose of 800 mg (4 tablets) of 5 times a day with approximately 4-hour interval, except for night time. Treatment has to last 7 days.

Treatment needs to be begun as soon as possible after the beginning of a disease, the result will be better if treatment to begin at once after emergence of rash.

Treatment of patients with considerable decrease in immunity.

For treatment of patients with considerable decrease in immunity it is necessary to accept 800 mg (4 tablets) of Atsiklovira-Darnitsa 4 times a day with approximately 6-hour interval. Intravenous therapy by medicine with active ingredient an acyclovir for intravenous administration within a month has to precede treatment of patients after transplantation of marrow.

Duration of treatment of patients after transplantation of marrow makes   6 months (from 1 to 7 months after transplantation).

Dosing for children.

For treatment and prevention of the infections caused by a herpes simplex virus at children with reduced immunity aged from 2 years is also more senior the dose of 400 mg/days is applied, and for children up to 2 years has to other dosage forms will be applied.

For treatment of chicken pox at children of 6 years 800 mg (4 tablets) of Atsiklovira-Darnitsa 4 times a day are appointed, children from 2 to 6 years can receive 400 mg (2 tablets) of Atsiklovira-Darnitsa 4 times a day. Children up to 2 years can accept 200 mg of Atsiklovira-Darnitsa 4 times a day. Dosing can be defined more precisely at the rate of 20 mg of Atsiklovira-Darnitsa on kilogram of body weight (no more than 800 mg) 4 times a day. Duration of treatment makes 5 days.

Patients of advanced age.

It must be kept in mind a possibility of a renal failure at patients of advanced age, and the drug dose for them has to be respectively changed. It is necessary to support the adequate level of hydration of an organism.

Renal failure.

Atsiklovir-Darnitsa it is necessary to appoint with care the patient with a renal failure. It is necessary to support the adequate level of hydration of an organism.

At treatment of the infections caused by a herpes simplex virus at patients with a renal failure the recommended peroral doses do not lead to accumulation of an acyclovir which level would exceed the safe level established for intravenous administration. Nevertheless, for patients with a heavy renal failure (clearance of creatinine less than 10 ml/min.) 2 times a day with an interval about 12 h are recommended to establish a dose of 200 mg.

At treatment of the infections caused by viruses of chicken pox and the surrounding herpes at patients with considerably reduced immunity it is recommended at a heavy renal failure (clearance of creatinine less than 10 ml/min.) to establish a dose of 800 mg 2 times a day with approximately 12-hour interval, and for patients with a moderate renal failure (clearance of creatinine within 10-25 ml/min.) – 800 mg 3 times a day with an interval about 8 h.

At use of high peroral doses of an acyclovir adequate hydration of these patients has to be supported.

Features of use:

The acyclovir is brought out of an organism by renal clearance therefore patients with a renal failure need to reduce a dose (see. "Route of administration and doses"). Patients of old age have also high probability of a renal failure therefore reduction of a dose can be necessary for this group of patients too. Both of these groups (patients with a renal failure and patients of old age) are risk groups because of emergence of neurologic side effects and therefore have to be under fixed observation for identification of these side reactions. It agrees the obtained data, such reactions are in general reverse in case of the treatment termination by drug.

During treatment it is necessary to refrain by drug from the use of alcoholic drinks.

Ability to influence the speed of reactions at control of motor transport or work with other mechanisms. Drug does not influence speed of response at control of motor transport or other mechanisms.

Side effects:

From TsNS: headache, increased fatigue, drowsiness, disorders of diction, confusion of consciousness, hallucination, insanity, psychomotor excitement, tremor, spasms, coma, ataxy, encephalopathy.

From Zhkt:boli in a stomach, nausea, vomiting, diarrhea, a loss of appetite, gastritis, a hyperbilirubinemia and tranzitorny increase in activity of enzymes of a liver, jaundice, hepatitis.

From system krovetvoreniya:snizheniye of hematologic indicators (anemia, thrombocytopenia, leukopenia).

From outside to a cardiovascular sistemy:oshchushchenia of heartbeat, thorax pain.

From urinary a sistemy:umenshenny diuresis, in single cases small increase in concentration of urea and creatinine in blood.

Allergic reaktsii:kozhny rashes, Quincke's disease, small tortoiseshell.

Dermatological reaktsii:fotosensibilization, reddening, itch and enanthesis, allopecia.

General disturbances: fever, the complicated breath and swallowing.

Interaction with other medicines:

The acyclovir is allocated mainly in not changed look with kidneys by canalicular secretion therefore any medicine which had the similar mechanism of allocation can increase concentration of an acyclovir in plasma.

Probenetsid and Cimetidinum reduce removal of an acyclovir by 30% that causes increase in time of semi-removal of an acyclovir.

Cyclosporine – nephrotoxicity development cases are given.

Nephrotoxic or neurotoxic medicines – risk of development of nephrotoxic or neurotoxic effect.

At simultaneous use with immunosuppressants at treatment of patients after organ transplantation in plasma the level of an acyclovir and inactive metabolite of immunosuppressive drug also increases, but owing to a wide therapeutic index of an acyclovir it is not necessary to adjust a dose.

Contraindications:

Hypersensitivity to an acyclovir or a valatsiklovir, drug components. Children's age up to 2 years. Pregnancy, feeding period breast.

Use during pregnancy or feeding by a breast. It is not recommended to appoint drug during pregnancy, except for cases when the potential advantage of drug exceeds possible risk.

In case of drug use by women who nurse feeding needs to be stopped.

Children. Drug is used at children of 2 years.

Overdose:

Symptoms: From a GIT: nausea and vomiting.

From urinary sistemy:ostry renal failure.

From ЦНС:головная pain, confusion of consciousness, hallucination, psychomotor excitement, epileptic seizures, coma.

Treatment: actions for removal of drug – a gastric lavage, purpose of absorbents, in hard cases – a hemodialysis. Symptomatic therapy.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging; on the 2nd blister strip packagings in a pack.