Product Overview
Structure
- acyclovir 400 mg.
Excipients:
microcrystalline cellulose,
polyvinylpyrrolidone,
indigo carmine,
magnesium stearate,
sodium starch glycolate,
purified water.
pharmachologic effect
An antiviral drug is a synthetic analogue of thymidine nucleoside.
In infected cells containing viral thymidine kinase, phosphorylation occurs and monophosphate becomes acyclovir. Under the influence of acyclovir guanylate cyclase, monophosphate is converted into diphosphate and, under the action of several cellular enzymes, into triphosphate. High selectivity and low toxicity to humans are due to the lack of the necessary enzyme for the formation of acyclovir triphosphate in intact cells of the macroorganism.
Acyclovir triphosphate, "integrating" into the DNA synthesized by the virus, blocks the reproduction of the virus. The specificity and very high selectivity of the action is also due to its predominant accumulation in cells affected by the herpes virus. Highly active against Herpes simplex virus type 1 and 2; chickenpox virus and herpes zoster (Varicella zoster); Epstein-Barr virus (types of viruses are listed in ascending order of magnitude of IPC acyclovir).
Moderately active against CMV. With herpes, it prevents the formation of new elements of the rash, reduces the likelihood of skin dissemination and visceral complications, accelerates the formation of crusts, and reduces pain in the acute phase of herpes zoster. It has an immunostimulating effect.
Indications
- prevention of frequently recurring (6 or more cases per year) genital herpes (including in patients with impaired immunity) - inside;
- treatment of primary and recurrent herpes simplex with damage to the skin and mucous membranes caused by Herpes simplex virus type 1 and 2, in patients with impaired immunity by mouth, parenterally;
- prevention of herpes simplex in patients with impaired immunity (including after transplantation and taking immunosuppressive drugs, HIV-infected patients, during chemotherapy) - inside;
- encephalitis caused by Herpes simplex type 1 and type 2 virus - parenterally;
- treatment of herpes zoster caused by the Varicella zoster virus, in adults, by mouth; in patients with impaired immunity and with generalized herpes zoster in patients with undisturbed immunity - parenterally;
- prevention of herpes zoster caused by the Varicella zoster virus after the initial period of use of acyclovir for parenteral use in all patients with impaired immunity (including after transplantation and when taking immunosuppressive drugs, HIV-infected patients, during chemotherapy) - by mouth;
- herpes zoster with eye damage - inside, parenteral;
- generalized infection in newborns caused by the Herpes simplex virus - parenterally;
- chickenpox in patients with undisturbed immunity within 24 hours after the appearance of a typical rash - inside, in patients with impaired immunity - parenterally.
Pregnancy and lactation
If necessary, use the drug during lactation should stop breastfeeding.
Contraindications
Carefully:
- pregnancy;
- elderly age;
- dehydration;
- renal failure;
- Neurological disorders or neurological reactions to taking cytotoxic drugs (including a history).
Side effects
From the digestive system: nausea, vomiting, diarrhea, abdominal pain; rarely, a reversible increase in bilirubin content and the activity of “liver” enzymes.
From the hemopoietic 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 central nervous system: headache, weakness, dizziness, increased fatigue, confusion, hallucinations, drowsiness, paresthesia, cramps, decreased concentration, agitation.
Allergic reactions: itching, rash, Lyell's syndrome, urticaria, erythema multiforme exudative, incl. Stevens-Johnson syndrome, angioedema, anaphylaxis.
Other : fever, lymphadenopathy, peripheral edema, visual impairment, myalgia, alopecia.
Interaction
With simultaneous use with probenecid, the average half-life increases and the clearance of acyclovir decreases.
With concomitant use with nephrotoxic drugs, the risk of developing renal dysfunction increases.
How to take, course of administration and dosage
The dosage regimen is set individually depending on the severity of the disease.
For liver infections of the skin and mucous membranes caused by Herpes simplex virus types 1 and 2
Adults - 200 mg 5 times a day (every 4 hours during wakefulness, except for night sleep) for 5 days, for the treatment of genital herpes - 10 days , if necessary, the duration of treatment can be extended.
As part of complex therapy for severe immunodeficiency, including the expanded clinical picture of HIV infection (including early clinical manifestations of HIV infection and the stage of AIDS), 400 mg 5 times a day are prescribed after bone marrow implantation.
For the prevention of relapse of infections caused by Herpes simplex virus types 1 and 2 in patients with normal immune status
Adults - 200 mg 4 times a day every 6 hours, the duration of the course is from b to 12 months.
For the prevention of infections caused by Herpes simplex virus types 1 and 2 in patients with immunodeficiency
Adults - 200 mg 4 times a day every 6 hours, the maximum dose - up to 400 mg 5 times a day, depending on the severity of the infection.
In the treatment of shingles - 800 mg 5 times a day (every 4 hours during wakefulness, with the exception of night sleep) for 7-10 days.
For children over the age of 3 years, the drug is prescribed in the same dose as adults.
Treatment of chickenpox: adults and children over 6 years old - 800 mg 4 times a day; children 3-6 years old - 400 mg 4 times a day. More precisely, the dose can be determined from the calculation of 20 mg / kg.
The course of treatment is 5 days.
In patients with impaired renal function, dose adjustment and dosing regimen are necessary depending on the size of creatinine clearance and the type of infection. For the treatment of Herpes simplex infection, when creatinine clearance is less than 10 ml / min, the daily dose 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 per day).
In the treatment of infections caused by Varicella zoster, and in the maintenance treatment of patients with severe immunodeficiency - patients with creatinine clearance of 10-25 ml / min are prescribed 800 mg 3 times a day with an interval of 8 hours, with creatinine clearance of less than 10 ml / min - 800 mg 2 times a day with an interval of 12 hours.
Special instructions
With caution, Acyclovir should be prescribed to patients with impaired renal function, elderly patients due to an increase in the half-life of acyclovir. When using the drug, it is necessary to ensure the flow of a sufficient amount of fluid.
Ointment is not recommended to be applied to the mucous membranes of the mouth, eyes, genitals, because the development of severe local inflammation is possible. The effectiveness of the treatment with the use of the ointment will be the higher the sooner it is started.
In patients with immunodeficiency with repeated repeated courses of treatment, the formation of resistance of viruses to acyclovir sometimes occurs. When taking the drug, kidney function (blood urea and blood plasma creatinine) should be monitored.
Release form
Acyclovir-Acre tablets of blue color with dark and light blue spots and possible white spots, flat-cylindrical, with chamfer and risk.
