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Owner/Registrar
Chemical-pharmaceutical plant AKRIKHIN, JSC
International Classification of Diseases (ICD-10)
A60 Anogenital herpes virus infection B00 Herpesvirus infections B01 Chickenpox B02 ShinglesPharmacological group
Antiviral drug
pharmachologic effect
An antiviral drug, a synthetic analog of an acyclic purine nucleoside with a highly selective effect on herpes viruses. In infected cells containing viral thymidine kinase, phosphorylation and conversion to acyclovir monophosphate occurs. Under the influence of acyclovir guanylate cyclase, monophosphate is converted to diphosphate and, under the action of several cellular enzymes, to triphosphate.
Acyclovir triphosphate is integrated into the viral DNA chain and blocks its synthesis through competitive inhibition of the viral DNA polymerase. The specificity and very high selectivity of action are also due to its predominant accumulation in cells affected by the herpes virus.
Highly active towards herpes simplex virus types 1 and 2; the virus that causes varicella and shingles (Varicella zoster); Epstein-Barr virus. moderately active for cytomegaloviruses.
With herpes, it prevents the formation of new elements, reduces the likelihood of skin dissemination and visceral complications, accelerates the formation of crusts, and reduces pain in the acute phase of herpes zoster.
Pharmacokinetics
Suction and distribution
When taken orally, bioavailability is 15-30%. C max in plasma after taking the drug intravenously at a dose of 200 mg 5 times / day is 0.7 μg / ml. The time to reach Cmax in blood plasma is 1.5-2 hours.
Plasma protein binding - 9-33%. Acyclovir penetrates well into all organs and tissues of the body; the concentration in the cerebrospinal fluid is 50% of the concentration in the blood plasma. Penetrates through the BBB and the placental barrier, excreted in breast milk.
Metabolism and excretion
It is metabolized in the liver with the formation of a pharmacologically inactive metabolite - 9-carboxymethoxymethylguanine.
T 1/2 when taken orally is 2-3 hours. It is excreted by the kidneys unchanged (about 84%) and in the form of a metabolite (about 14%). Less than 2% is excreted through the gastrointestinal tract; trace amounts are determined in exhaled air.
Pharmacokinetics in special clinical situations
In patients with severe renal insufficiency T 1/2 - 20 hours, with hemodialysis - 5.7 hours (in this case, the concentration of acyclovir in plasma decreases to 60% of the initial value).
Treatment of infections of the skin and mucous membranes caused by Herpes simplex viruses types 1 and 2, both primary and secondary, including genital herpes;
Prevention of exacerbations of recurrent infections caused by Herpes simplex viruses types 1 and 2 in patients with normal immune status;
Prevention of primary and recurrent infections caused by Herpes simplex viruses types 1 and 2 in immunocompromised patients;
As part of complex therapy in patients with severe immunodeficiency: with HIV infection (AIDS stage, early clinical manifestations and a detailed clinical picture) and in patients who underwent bone marrow transplantation;
Treatment of primary and recurrent infections caused by the Varicella zoster virus (chickenpox, herpes zoster).
Children's age up to 3 years;
lactation period;
Hypersensitivity to acyclovir, ganciclovir, valaciclovir or auxiliary components of the drug.
FROM caution the drug should be prescribed for dehydration, renal failure, neurological disorders or neurological reactions to the intake of cytotoxic drugs (including history), pregnancy, elderly patients.
From the digestive system: nausea, vomiting, diarrhea, abdominal pain; rarely - a reversible increase in bilirubin and liver enzymes.
From the hematopoietic system: very rarely - anemia, leukopenia, thrombocytopenia.
From the urinary system: rarely - an increase in the content of urea and creatinine in the blood; very rarely - acute renal failure.
From the side of the central nervous system: headache, weakness, dizziness, fatigue, confusion, hallucinations, drowsiness, paresthesia, convulsions, decreased concentration, agitation.
Allergic reactions: itching, rash, Lyell's syndrome, urticaria, erythema multiforme exudative, incl. Stevens-Johnson syndrome, angioedema, anaphylaxis.
Others: fever, lymphadenopathy, peripheral edema, visual impairment, myalgia, alopecia.
Overdose
Symptoms: agitation, coma, convulsions, lethargy. Precipitation of acyclovir in the renal tubules is possible if its concentration exceeds the solubility in the renal tubules (2.5 mg / ml).
Treatment: conducting symptomatic therapy.
special instructions
When taking the drug, kidney function (blood urea and plasma creatinine) should be monitored.
When using the drug, it is necessary to ensure the flow of a sufficient amount of liquid.
Prolonged or repeated treatment with acyclovir in immunocompromised patients may lead to the emergence of virus strains that are insensitive to its action. Most isolated strains of viruses insensitive to acyclovir show a relative lack of viral thymidine kinase; strains with altered thymidine kinase or altered DNA polymerase have been isolated. In vitro action of acyclovir on isolated strains of the Herpes simplex virus may cause the appearance of less sensitive strains.
Acyclovir does not prevent sexual transmission of herpes, therefore, during the treatment period, it is necessary to refrain from sexual intercourse, even in the absence of clinical manifestations.
Influence on the ability to drive vehicles and control mechanisms
During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.
With kidney failure
With caution, the drug should be prescribed for renal failure.
Elderly
Be wary appoint elderly patients.
Use during pregnancy and lactation
The use of the drug during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus.
If necessary, the use of the drug during lactation should decide on the termination of breastfeeding.
drug interaction
Simultaneous use with probenecid leads to an increase in the average T 1/2 and a decrease in the clearance of acyclovir.
With simultaneous use with nephrotoxic drugs, the risk of impaired renal function increases.
The drug is taken orally, during or immediately after a meal, drinking plenty of water.
The dosage regimen is set individually depending on the severity of the disease.
At treatment of infections of the skin and mucous membranes caused by the Herpes simplex virus types 1 and 2, adults appoint 200 mg 5 times / day (every 4 hours during wakefulness, except for night sleep) for 5 days; at treatment of genital herpes- 10 days. If necessary, the duration of treatment can be increased.
As part of complex therapy for severe immunodeficiency, incl. with a detailed clinical picture HIV infection (including early clinical manifestations of HIV infection and stage AIDS), after bone marrow transplantation appoint 400 mg 5 times / day.
For prevention of recurrence of infections caused by Herpes simplex viruses types 1 and 2 in patients with normal immune status adults appoint 200 mg 4 times / day every 6 hours. The duration of the course is from 6 to 12 months.
For prevention of infections caused by Herpes simplex virus types 1 and 2 in patients with immunodeficiency adults appoint 200 mg 4 times / day every 6 hours, the maximum dose is up to 400 mg of acyclovir 5 times / day, depending on the severity of the infection.
At herpes zoster treatment- 800 mg 5 times / day (every 4 hours during wakefulness, except for night sleep) for 7-10 days.
Children over 3 years of age the drug is prescribed in the same dose as for adults.
At chickenpox treatment adults and children over 6 years old appoint 800 mg 4 times / day; children aged 3-6 years- 400 mg 4 times / day. More precisely, the dose can be determined at the rate of 20 mg / kg. The course of treatment is 5 days.
At patients with impaired renal function dose adjustment and dosing regimen is necessary depending on the size of the CC and the type of infection. At treatment of infection caused by Herpes simplex, at QC less than 10 ml / min the daily dose of the drug should be reduced to 400 mg, dividing it into 2 doses (with intervals between them of at least 12 hours, i.e. 200 mg 2 times / day). At treatment of infections caused by Varicella zoster, and at maintenance therapy in patients with severe immunodeficiency - patients with CC 10-25 ml / min prescribe the drug 800 mg 3 times / day with an interval of 8 hours, s QC less than 10 ml / min- 800 mg 2 times / day with an interval of 12 hours.
Storage conditions and shelf life
The drug should be stored out of the reach of children, dry, dark place at a temperature not exceeding 25°C. Shelf life - 4 years. Do not use after the expiration date.
Active ingredient: Acyclovir.
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