Acyclovir

General characteristics. Structure:

Active agent: acyclovir of 200 mg.

Pharmacological properties:

Antiviral means. The thymidinekinase of the cells infected with a virus actively will transform an acyclovir through a number of consecutive reactions to mono - di - and acyclovir triphosphate. The last interacts with a virus DNA polymerase and is built in DNA which is synthesized for new viruses. Thus, "defective" virus DNA forms that leads to suppression of replication of new generations of viruses.
The acyclovir is active concerning the Herpes simplex virus of types 1 and 2, the Varicella zoster virus, Epstein-Barre's virus and a cytomegalovirus.

Pharmacokinetics. At intake bioavailability makes 15-30%. It is widely distributed in fabrics and fluid mediums of an organism. Linkng with proteins of plasma makes 9-33%. It is metabolized in a liver. T1/2 at intake is 3.3 h, at in introduction - 2.5 h. It is removed with urine, in insignificant quantity - with a stake.

Indications to use:

For system use (inside and in/in): the infections caused by the Herpes simplex viruses of types 1 and 2 and Varicella zoster; prevention of the infections caused by the Herpes simplex and Varicella zoster viruses (including at patients with reduced immunity); as a part of complex therapy at the expressed immunodeficiency (including at a clinical picture of HIV infection) and at the patients who transferred transplantation of marrow; prevention of a Cytomegaloviral infection after transplantation of marrow.
For topical administration in ophthalmology: a keratitis and other damages of eyes caused by the Herpes simplex virus.
For external use: the infections of integuments caused by the Herpes simplex and Varicella zoster viruses.

Route of administration and doses:

Inside to adults and children 2 years - on 200-400 mg of 3-5 times/days, if necessary - on 20 mg/kg (to 800 mg on reception) are more senior than 4 times/days. At children under 2 years apply in the dose equal to a half of a dose to adults. Treatment duration - 5-10 days. At a renal failure correction of the mode of dosing is recommended.
In kapelno adults and children 12 years - on 5-10 mg/kg, an interval between introductions - 8 h are more senior. To children aged from 3 months up to 12 years - on 250-500 mg/sq.m of a body surface, an interval between introductions - 8 h. For newborns the dose makes 10 mg/kg, an interval between introductions - 8 h.
At a renal failure correction of the mode of dosing is necessary.
Locally and outwardly apply 5 times/days. The dose and duration of treatment depend on indications and the used dosage form.
Maximum doses: for adults at in introduction - 30 mg/kg/days.

Features of use:

Use at heavy renal failures is not recommended.

It is necessary to consider that at use of an acyclovir development of an acute renal failure owing to formation of a deposit from acyclovir crystals is possible that it is especially probable at bystry in introduction, simultaneous use of nephrotoxic drugs, at patients with renal failures and at insufficient water loading.

At use of an acyclovir it is necessary to control function of kidneys (determination of level of an urea nitrogen in blood and creatinine in a blood plasma).

Treatment of patients of advanced age should be carried out at sufficient increase in water loading and under observation of the doctor since at this category of patients the acyclovir elimination half-life increases.

At treatment of genital herpes it is necessary to avoid sexual contacts or to use condoms since use of an acyclovir does not prevent transfer of a virus to partners.

The acyclovir in the form of dosage forms for external use should not be applied on mucous membranes of an oral cavity, an eye, vaginas.

Side effects:

At intake: nausea, vomiting, diarrhea, abdominal pain, skin rash, headache, dizziness, increased fatigue, decrease in concentration of attention, hallucination, drowsiness or sleeplessness, fever; seldom - a hair loss, passing increase in concentration in blood of bilirubin, urea, creatinine, activity of liver enzymes, a lymphocytopenia, an erythropenia, a leukopenia.
At in introduction: an acute renal failure, a crystalluria, encephalopathy (confusion of consciousness, a hallucination, excitement, a tremor, spasms, psychosis, drowsiness, a coma), phlebitis or an inflammation in an injection site, nausea, vomiting.
At topical administration: a burning sensation in the place of application, a superficial dot keratitis, a blepharitis, conjunctivitis.
At external use: in the place of application the burning sensation, skin rash, an itch, a peeling, an erythema, a xeroderma are possible; at hit on mucous membranes - an inflammation.

Interaction with other medicines:

At simultaneous use пробенецид reduces canalicular secretion of an acyclovir and by that increases concentration in a blood plasma and an acyclovir elimination half-life.

At simultaneous use of an acyclovir with nephrotoxic drugs the risk of development of nephrotoxic action increases (especially at patients with an impaired renal function).

Strengthening of effect of an acyclovir is noted at co-administration of immunostimulators.

When mixing solutions it is necessary to consider alkali reaction of an acyclovir for in/in introductions (рН 11).

Contraindications:

Hypersensitivity to an acyclovir and a valatsiklovir; at in introduction - a lactation (breastfeeding).

Use at pregnancy and feeding by a breast
Use of an acyclovir at pregnancy is possible in cases when the estimated advantage for mother exceeds potential risk for a fruit.
In/in use of an acyclovir in the period of a lactation contraindicated (it is allocated with breast milk).
In pilot studies on animals it is shown that the acyclovir gets through a placental barrier.

Use at renal failures
Use at heavy renal failures is not recommended.
At a renal failure correction of the mode of dosing is necessary.
It is necessary to consider that at use of an acyclovir development of an acute renal failure owing to formation of a deposit from acyclovir crystals is possible that it is especially probable at bystry in introduction, simultaneous use of nephrotoxic drugs, at patients with renal failures and at insufficient water loading.
At use of an acyclovir it is necessary to control function of kidneys (determination of level of an urea nitrogen in blood and creatinine in a blood plasma).

Use for elderly patients
Treatment of patients of advanced age should be carried out at sufficient increase in water loading and under observation of the doctor since at this category of patients the acyclovir elimination half-life increases.

Use for children
Inside to children 2 years - on 200-400 mg of 3-5 times/days, if necessary - on 20 mg/kg (to 800 mg on reception) are more senior than 4 times/days. At children under 2 years apply in the dose equal to a half of a dose to adults. Treatment duration - 5-10 days.

Overdose:

It is not described.

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets of 200 mg: 20 pieces.