medicalmeds.eu Medicines Antimicrobic means for system use. Tab. acyclovir 0,2 No. 20

Tab. acyclovir 0,2 No. 20

Producer: CJSC Lekhim-Kharkiv Ukraine

Code of automatic telephone exchange: J05A B01

Release form: Firm dosage forms. Tablets.

Indications to use: (Deprive) the surrounding herpes. Chicken pox (Chicken pox).

General characteristics. Structure:

International and chemical names: aciclovir; 2-amino-9-[marked (2-hydroxy-этокси)] - 1,9 - dihydro - 6H - purine - 6 - it; main physical and chemical properties: tablets of a biconvex form from color, white to white with a yellowish shade; structure: 1 tablet contains an acyclovir 200 mg (0,2 g); excipients: starch corn, lactoses monohydrate, magnesium stearate, sodium of a kroskarmelloz.

Pharmacological properties:

Pharmacodynamics. Antiviral means. Possesses highly selective effect on herpes viruses: Herpes simplex of the 1st and 2nd types, the Varicella zoster virus, is less active in the relation to Epstein-Burra's virus and a cytomegalovirus. In the cell infected with a virus the acyclovir competitively interacts with a virus thymidinekinase and is consistently phosphorylated to mono - di - and triphosphate. An acyclovir triphosphate works as nonspecific inhibitor and substrate for a virus DNA polymerase, instead of a deoksiguanozin is built in virus DNA, causing break of a chain and blocking further replication of virus DNA without damage of cells of the owner. 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.

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 h. Linkng with proteins of plasma is insignificant (9 - 33%). It is a little metabolized by a liver. Gets through hematoencephalic and placental barriers, comes to 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 h. At a renal failure (deterioration in glomerular filtering) the elimination half-life and the general clearance of drug increase. At decrease in glomerular filtering lower than 10 ml/min. a dose of an acyclovir need to be adjusted towards reduction for prevention of cumulation of drug in an organism. At advanced age, along with decrease in clearance of creatinine, the clearance of an acyclovir decreases, however the elimination half-life of an acyclovir changes slightly.

Indications to use:

Treatment and prevention of primary and recurrent gerpesny damages of skin and the mucous membranes caused by the corresponding viruses (including genital herpes, shingles, chicken pox). Drug is used also as a part of complex therapy for treatment and prevention of an immunodeficiency, including at the developed clinical picture of HIV infection and at the patients who transferred transplantation of marrow.

Route of administration and doses:

Drug is accepted during food, washing down 150 - 200 ml of water.

To adults and children 2 years for treatment of the herpetic damages caused by the Herpes simplex virus – on 1 tablet (200 mg) of 5 times a day each 4 hours (except for the period of a night dream) within 5 days are more senior. The course can be prolonged at heavy primary infections up to 10 days. At the expressed immunodeficiency (including after transplantation of marrow and disturbance of absorption from intestines) – on 2 tablets (400 mg) of 5 times a day.

To adults and children 2 years for prevention of a recurrence of the infections caused by the Herpes simplex virus, adult with the normal immune status – on 1 tablet (200 mg) are more senior
4 times a day each 6 hours. In some cases there are effective lower doses – on 1 tablet (200 mg) 3 times a day each 8 hours. At some patients interruption of an infection can happen at reception of a total daily dose – 4 tablets (800 mg).

To adults and children 2 years for prevention of the infections caused by the Herpes simplex virus, adult with the normal immune status – on 1 tablet (200 mg) 3 - 4 times are more senior in
days each 6 - 8 hours. To patients with an immunodeficiency – on 1 tablet (200 mg) 4 times in
days each 6 hours. At the expressed immunodeficiency (after transplantation of marrow or disturbance of absorption from intestines) the dose can be increased to 2 tablets (400 mg) of 5 times a day. Duration of prevention is defined by duration of the period of risk of infection. At organ transplantation preventive treatment is carried out within 6 weeks.

To children 2 years with the normal immune status are younger and at an immunodeficiency for treatment and prevention of the infections caused by the Herpes simplex virus appoint on 1 tablet (200 mg) of time a day, or at the rate of 20 mg/kg of body weight, but no more than 800 mg a day. The course of treatment makes 5 days.

The adult at chicken pox and the surrounding herpes appoint 4 tablets (800 mg)
4 times a day each 4 hours (except for the period of a night dream); to children: 6 years – on 4 tablets (800 mg) 4 times a day are more senior; from 2 to 6 years – on 2 tablets (400 mg) 4 times a day; up to 2 years – the dose is not defined, but any toxic action or specific pediatric problems at the children receiving an acyclovir in a dose – 80 mg/kg of body weight a day were not revealed. The course of treatment makes 5 days or 2 days after the last rash.

For newborns drug is not used.

At a renal failure (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:

Treatment is recommended to be begun at emergence of the first symptoms of a disease; at a recurrence it is already recommended to appoint drug in a prodromal stage or at emergence of the first elements of herpetic rash.

The condition of immune system is important for implementation of medical effect of an acyclovir. Drug is most effective at patients with normal immunity. At an immunodeficiency after repeated repeated courses of therapy nonsensitivity or resistance of viruses to an acyclovir sometimes forms.

The patients receiving high doses of an acyclovir have to receive enough liquid.

Side effects:

From digestive tract: nausea, vomiting, diarrhea, abdominal pains, intestinal colic, reversible increase in level of bilirubin and activity of hepatic transaminases.

From the central nervous system: seldom - a headache, weakness; in some cases tremor, dizziness, fatigue, drowsiness, hallucinations.

From system of blood: anemia, leukopenia, thrombocytopenia.

Allergic reactions: skin rash, a photosensitization, a small tortoiseshell, an itch, fever, it is rare – an asthma, a Quincke's disease, an anaphylaxis.

Interaction with other medicines:

At simultaneous use with probenetsidy plasma concentration of an acyclovir can increase.

Blockers of calcium channels and Cimetidinum increase bioavailability of an acyclovir and reduce its renal clearance (dose adjustment is not required owing to the broad range of therapeutic doses of an acyclovir).

Co-administration with probenetsidy slows down drug removal.