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Owner/Registrar
Chemical and pharmaceutical plant AKRIKHIN, JSC
International Classification of Diseases (ICD-10)
A60 Anogenital herpetic viral infection B00 Herpes virus infections B01 Chickenpox B02 Herpes zosterPharmacological group
pharmachologic effect
An antiviral drug, a synthetic analogue of an acyclic purine nucleoside, which has a highly selective effect on herpes viruses. In infected cells containing viral thymidine kinase, phosphorylation occurs and is converted to acyclovir monophosphate. Under the influence of acyclovir guanylate cyclase, monophosphate is converted into diphosphate and, under the action of several cellular enzymes, into triphosphate.
Acyclovir triphosphate is integrated into the viral DNA chain and blocks its synthesis through competitive inhibition of 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 against Herpes simplex virus types 1 and 2; the virus that causes chickenpox and herpes zoster (Varicella zoster); Epstein-Barr virus. Moderately active against cytomegaloviruses.
In case of herpes, it prevents the formation of new elements, reduces the likelihood of skin dissemination and visceral complications, accelerates the formation of crusts, reduces pain in acute phase herpes zoster.
Pharmacokinetics
Suction and distribution
When taken orally, bioavailability is 15-30%. C max in blood plasma after taking the drug internally at a dose of 200 mg 5 times a day is 0.7 mcg/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; concentration in cerebrospinal fluid is 50% of the concentration in blood plasma. Penetrates through the BBB and placental barrier, excreted in breast milk.
Metabolism and excretion
Metabolized in the liver to form a pharmacologically inactive metabolite - 9-carboxymethoxymethylguanine.
T1/2 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 failure T1/2 - 20 hours, with hemodialysis - 5.7 hours (at the same time, 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 patients with immunodeficiency;
Included complex therapy in patients with severe immunodeficiency: with HIV infection (stage AIDS, early clinical manifestations and detailed clinical picture) and in patients who underwent transplantation bone marrow;
Treatment of primary and recurrent infections caused by the Varicella zoster virus ( chicken pox, herpes zoster).
Childhood up to 3 years;
Lactation period;
Hypersensitivity to acyclovir, ganciclovir, valacyclovir or auxiliary components of the drug.
WITH caution the drug should be prescribed for dehydration, renal failure, neurological disorders or neurological reactions to cytotoxic drugs medicines(including history), pregnancy, elderly patients.
From the outside digestive system: nausea, vomiting, diarrhea, abdominal pain; rarely - a reversible increase in bilirubin content and liver enzyme activity.
From the hematopoietic system: very rarely - anemia, leukopenia, thrombocytopenia.
From the urinary system: rarely - increased levels of urea and creatinine in the blood; very rarely - acute renal failure.
From the side of the central nervous system: headache, weakness, dizziness, increased fatigue, confusion, hallucinations, drowsiness, paresthesia, convulsions, decreased concentration, agitation.
Allergic reactions: itching, rash, Lyell's syndrome, urticaria, erythema multiforme, incl. Stevens-Johnson syndrome, angioedema, anaphylaxis.
Others: fever, lymphadenopathy, peripheral edema, blurred vision, 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: carrying out symptomatic therapy.
special instructions
When taking the drug, kidney function should be monitored (blood urea and plasma creatinine levels).
When using the drug, it is necessary to ensure the supply of a sufficient amount of fluid.
Long or re-treatment acyclovir in patients with reduced immunity can lead to the emergence of strains of viruses that are insensitive to its action. Most isolated strains of viruses that are insensitive to acyclovir show a relative lack of viral thymidine kinase; strains with altered thymidine kinase or with altered DNA polymerase were isolated. In vitro, the effect of acyclovir on isolated strains of the Herpes simplex virus may cause the emergence of less sensitive strains.
Acyclovir does not prevent the sexual transmission of herpes, so during the treatment period it is necessary to abstain from sexual intercourse, even in the absence of clinical manifestations.
Impact on the ability to drive vehicles and operate machinery
During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous species activities requiring increased concentration attention and speed of psychomotor reactions.
For renal failure
The drug should be prescribed with caution in case of renal failure.
Elderly
Prescribe with caution to elderly patients.
Use during pregnancy and breastfeeding
The use of the drug during pregnancy is possible only if the expected benefit to the mother exceeds potential risk for the fetus.
If it is necessary to use the drug during lactation, the issue of stopping breastfeeding should be decided.
Drug interactions
Concomitant use with probenecid leads to an increase in mean T1/2 and a decrease in the clearance of acyclovir.
When used simultaneously with nephrotoxic drugs, the risk of renal dysfunction increases.
The drug is taken orally, during or immediately after a meal, with sufficient quantity 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 prescribe 200 mg 5 times a day (every 4 hours during wakefulness, with the exception of 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. when deployed clinical picture HIV infection (including early clinical manifestations of HIV infection and stage of AIDS), after bone marrow transplantation prescribed 400 mg 5 times a day.
For prevention of relapse of infections caused by Herpes simplex viruses types 1 and 2 in patients with normal immune status adults Prescribe 200 mg 4 times a day every 6 hours. Course duration is from 6 to 12 months.
For prevention of infections caused by Herpes simplex virus types 1 and 2 in patients with immunodeficiency adults prescribed 200 mg 4 times a day every 6 hours, maximum dose- up to 400 mg of acyclovir 5 times a day, depending on the severity of the infection.
At treatment of herpes zoster- 800 mg 5 times a day (every 4 hours while awake, excluding night sleep) for 7-10 days.
Children over 3 years of age the drug is prescribed in the same dose as for adults.
At treatment of chickenpox adults and children over 6 years old prescribed 800 mg 4 times/day; children aged 3-6 years- 400 mg 4 times/day. More accurately, the dose can be determined at the rate of 20 mg/kg. The course of treatment is 5 days.
U patients with impaired renal function It is necessary to adjust the dose and dosage regimen depending on the size of the CC and the type of infection. At treatment of infection caused by Herpes simplex, at CC less than 10 ml/min daily dose 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 a 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 a day with an interval of 8 hours, with CC less than 10 ml/min- 800 mg 2 times a day with an interval of 12 hours.
Storage conditions and shelf life
The drug should be stored out of the reach of children, in a dry place, protected from light, at a temperature not exceeding 25°C. Shelf life - 4 years. Do not use after expiration date.
Active substance: Acyclovir.
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