INSTRUCTION
medical use of the drug
acyclovir
Title of Commerce
acyclovir
Mezhdunarodnoe Title
INN:
Aciclovir
Latynskoe Title
ACICLOVIR
General characteristics
General characteristics:
International and chemical name:
aciclovir; 2-amino-9 - [(2-hidroksietoksi) methyl] -1,9-dihydro-6H-purine-6-one;
basic physical and chemical properties:
White round biconvex tablets;
Composition: 1 tablet containing acyclovir 0.2 g;
Excipients:
lactose monohydrate, magnesium stearate, corn starch.
Form of issue
Product:
Tablets 200 mg number 10, number 10x2 in blisters (in bulk packaging from the manufacturer "Layfsors Heltker", India)
Farmhruppa
Pharmacological group.
Antiviral medications for regular use.
ATC code J05AB01
Farmakolohycheskye properties
Pharmacological properties.
Pharmacodynamics.
Acyclovir? antiviral drug, relatively highly active herpes simplex virus (Herpes simplex (VHS)) Type 1 and 2, the virus shingles (Varicella zoster (VZV)), varicella zoster virus, Epstein-Barr virus and to a lesser extent - to cytomegalovirus.
Acyclovir is a synthetic purine nucleoside analogue - dezoksyhuanidynu, the normal component of DNA. After rooting acyclovir in the affected cell virus enzyme thymidine kinase under the influence, which identifies the virus, acyclovir acyclovir goes in-monophosphate. Under the influence of cell-huanilatkinazy acyclovir monophosphate is converted to acyclovir diphosphate, which enzymes cells - master (virus) is converted to the active form - acyclovir-triphosphate. Interacting with DNA - polymerase (VHS and VZV), inhibits the replication of viral DNA. With viral DNA polymerase acyclovir-triphosphate can be built into the growing DNA chain, resulting in DNA chain defect arises and growth of a new generation of viruses stops. The drug has a high selectivity of the synthesis of viral DNA. In human cells the DNA replication acyclovir-triphosphate virtually no effect.
Acyclovir herpes with new elements prevents acne, reduces the likelihood of skin dissemination and visceral complications accelerates education crusts, debilitating pain in the acute phase of herpes zoster.
The drug produces immunostimulatory effect.
Pharmacokinetics
Pharmacokinetics.
After oral drug only partially absorbed from the gut. The drug simultaneously with food has little effect on its absorption. Bioavailability is 15-30%. The concentration in the blood depending on the dose. The binding protein is 9-30%.
The drug is widely distributed in body fluids and tissues, including the brain, kidneys, lungs, liver, cerebrospinal fluid, tears, intestines, muscle tissue, spleen, semen, secret and mucous membranes of the vagina, uterus, breast milk, cerebrospinal fluid and fluid herpetic vesicles.
The highest concentrations are found in the kidneys, liver and intestines. The concentration in cerebrospinal fluid is approximately 50% of plasma concentrations.
When oral drug 1g daily concentrations in breast milk may exceed its concentration in the plasma of 0.6 - 4.1 times in the amniotic fluid? 3-6 times, in such cases, the child's mother's milk comes in doses of acyclovir 0,0003 g / kg per day. Therefore, you must carefully prescribe the drug to women who are breastfeeding.
Long-term or repeated courses of the drug in patients with lowered immunity can lead to viral strains insensitive to acyclovir. This can be caused by viral thymidine kinase deficiency or restructuring thymidine kinase and DNA polymerase.
The natural metabolite of acyclovir is 9 karboksymetoksymetylhuanin.
Antiviral activity of this metabolite is not known.
The half when taken internally adults - 3.3 hours. Time to reach maximum concentration in serum after oral administration? 7.7 hours.
The average maximum concentration in serum (stable) when taken internally in adults is:
at a dose of 0.2 g (2.5 mmol / l) every 4 hours? 0.6 mg / ml,
at a dose of 0.4 g (5.3 mmol / l) every 4 hours? 1.2 mg / ml,
at a dose of 0.8 g (6.9 mmol / l) every 4 hours? 1.6 mg / ml.
The volume of distribution (Vold) (at achieving a stable concentration):
adults: about 48 l / m2 body surface (37-57 l / m2)
children and adolescents (1-18 years): about 45 l / m2.
When kidney disease in the terminal stage: about 41 l / m2.
When taken internally about 14% of the dose is excreted unchanged in the urine, most of the drug - as metabolites; a small portion excreted in the faeces. In the process of withdrawal of the drug along with glomerular filtration participates likely mechanism of tubular secretion. The rate of withdrawal of drug from the body slows down with age, but regardless of the half-life of the drug is increasing slightly.
In chronic liver failure half-life value is an average of 19.5 hours. In the case of drug in plasma is reduced to 60% of the original value (after a single 6-hour session). In peritoneal dialysis clearance of the drug did not significantly zminyuyetsya.Pokazanyya for prymenenyyuPokazannya zastosuvannya.- for the treatment of herpes genital: primary and recurrent cases of severe herpes disturbed and undisturbed imunitetom.- genital herpes Prevention: frequently recurrent (6 cases per year) in patients with impaired and unimpaired imunitetom.- treatment of herpes simplex caused by virus types 1 and 2 (VHS-VHS-1 and 2) in patients with impaired immunity and undisturbed - primary and recurrent lesions of the skin and mucous obolonok.- Prevention of herpes simplex patients with impaired immune systems, including transplant patients after receiving immunosuppressive agents, HIV infection, during himioterapiyi.- treatment of herpes zoster (Varicella zoster virus (VZV) in adult patients (treatment is most effective if it is to begin within 48 hod.pislya occurrence of rash) .- Treatment of varicella in patients with impaired immunity (therapy begins within 24 hours after the appearance of a typical rash) .Sposob of application and use and dozыSposib dozy.Atsyklovir administered internally. Treatment should begin at the first signs and symptoms of herpes simplex or infections caused by VZV. Treatment of chicken pox is most effective if its start in the first or second day after the onset of rash. In patients with impaired immunity for healing skin lesions and mucous membranes duration of therapy can be increased, the appearance of scabs or epithelialization. Acyclovir can be taken with meals, as it has virtually no effect on absorbability. It is recommended to drink a glass of water. Some patients may be an effective short-term intermittent treatment of recurrent herpes genitals, if the patient starts in the prodrome or at the first sign zahvoryuvannya.Seredni doses for adults and adolescents: - genital herpes (primary infection): 0.2 g 5 times a day for 10 days. The course, further treatment strategy determined individually. In patients with lowered immunity (including transplant organs or bone marrow) 0.4 g administered 5 times a day. The course of treatment? at least 5 days, if necessary? 10 days - recurrent infections, intermittent therapy: 0.2 g 5 times a day for 5 days - recurrent infections, long-term therapy depressing: 0.4 g 2 times a day or 0.2 g 3? 5 times a day - the treatment of herpes simplex lesions of the skin and mucous membranes, 0.2? 0.4 g 5 times a day for 10 days. Patients with impaired immunity appoint 0.2 g 4 times a day, with distress, the dose may be doubled, and when there is a need to switch to intravenous - for the prevention of herpes simplex skin and mucous membranes, 0.4 g each 12 hours. The duration of prophylactic course is determined by the duration of risk - herpes zoster: 0.8 g 5 times a day for 7? 10 days. For patients with pronounced immunodeficiency should consider intravenous version - chicken pox, 0.8 g 4 times a day for 5 days. Treatment should begin at the first signs or symptoms of varicella vispy.Pobochnыe эffektыPobichna diya.Pry use of the drug can occur from the gastrointestinal tract and liver, if prolonged use of high doses in isolated cases - nausea, vomiting, diarrhea, sore zhyvoti.Pry long-term administration of the drug at the recommended doses in patients with impaired renal function were observed accumulation of acyclovir above safe levels. When used in high doses rarely formed crystals of acyclovir in renal tubules. In this case it is necessary to increase the use ridyny.Dermatolohichni reactions: skin rash, which passes quickly after discontinuation of the drug. In the rare cases in patients receiving the drug inside diffuse alopecia observed, however acyclovir role in the development of this side effect is not clearly vyznachena.Z the central nervous system and mental status, high concentrations of drug in plasma was observed in isolated cases headache, "chronic fatigue syndrome" , excitement, somnolence, tremor. These reactions are most likely in patients with impaired immunity in older patients and generally are reversible harakter.Za performance laboratory / physiological tests may be increased: - the level of urea nitrogen in the blood - serum creatinine level krovi.ProtyvopokazanyyaProtypokazannya.Pidvyschena sensitivity to acyclovir or to any component preparatu.Vzaymodeystvye s second lekarstvennыmy sredstvamyVzayemodiya with other medicinal zasobamy.Pry concomitant use of nephrotoxic drugs acyclovir increases nephrotoxicity of the latter, especially in renal impairment. When combined use of acyclovir and probenitsydu reduced tubular secretion of acyclovir, zbihemodialysis, the figure is 5.7 hours, and the concentration increases the half-life and its concentration in serum and cerebrospinal fluid. Simultaneous treatment with acyclovir and zydovudinu HIV infection does not affect the kinetics of preparativ.PeredozyrovkaPeredozuvannya.Holovnyy pain, nausea, vomiting, diarrhea, shortness of breath, kidney failure, lethargy, convulsions, coma. Acyclovir was absorbed from the gastrointestinal tract, so it is unlikely that taking 5 grams of the drug once cause serious toxic effects. Since no specific antidote, treatment of adverse effects or overdose should be symptomatic and supportive. It is recommended to conduct dialysis, particularly in patients with severe renal insufficiency. Increase the flow of fluids in the body to prevent the formation of crystals in the renal kanaltsyah.Osobennosty prymenenyyaOsoblyvosti zastosuvannya.Preparat not recommended during pregnancy and lactation (during treatment should stop lactation) .Pid treatment should monitor kidney function (determination of urea nitrogen in the blood and creatinine in blood plasma). If women with herpes genital within 1 week condition does not improve, we need a gynecological examination (in patients with herpes genital increased risk of cervical cancer, so you should perform Pap test 1 per year to identify early changes in the cervix) .pri treatment of genital herpes should avoid sexual kontaktiv.Pry chickenpox therapy is more effective if it is to begin within 24 hours after discovery of typical vysypu.Preparat it can be taken with the timing and yizheyu.Uslovyya hranenyyaUmovy term zberihannya.V and dry, the light at a temperature of 15 to 25 S.Zberihaty the reach of children mistsi.Termin life? 3 roky.Proyzvodytel and ego adresVyrobnyk country by "Lekhim Kharkiv", Kharkiv,