Acyclovir Akrikhin pills 200mg N20
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Active ingredients
Acyclovir
Release form
Pills
Composition
Active ingredient: Acyclovir Concentration of active ingredient (mg): 200 mg
Pharmacological effect
Antiviral drug, synthetic analog of acyclic purine nucleoside, which has a highly selective effect on herpes viruses. In infected cells containing viral thymidine kinase, phosphorylation occurs and monophosphate is converted to acyclovir. Under the influence of acyclovir guanylate cyclase, monophosphate is converted into diphosphate and under the action of several cellular enzymes into triphosphate. Aciclovir triphosphate is inserted 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. It is highly active against the Herpes simplex type 1 and type 2 virus; varicella-zoster virus (Varicella zoster); Epstein-Barr virus. Moderately active against cytomegalovirus. When herpes prevents the formation of new elements, reduces the likelihood of skin dissemination and visceral complications, accelerates the formation of crusts, reduces pain in the acute phase of herpes zoster.
Pharmacokinetics
Absorption and distribution When ingested, bioavailability is 15-30%. Cmax in the blood plasma after taking the drug intravenously at a dose of 200 mg 5 times / day is 0.7 mcg / ml. The time to reach Cmax in blood plasma is 1.5-2 hours. Binding to plasma proteins is 9-33%. Acyclovir penetrates well into all organs and tissues of the body; concentration in the cerebrospinal fluid is 50% concentration in plasma. It penetrates the BBB and placental barrier, is excreted in breast milk. Metabolism and elimination Metabolized in the liver with the formation of a pharmacologically inactive metabolite - 9-carboxymethoxymethylguanine. T1 / 2 when ingested is 2-3 hours. in the form of a metabolite (about 14%). Less than 2% is excreted through the digestive tract; Trace amounts are determined in exhaled air. Pharmacokinetics in special clinical situations in patients with severe renal insufficiency T1 / 2 - 20 hours, with hemodialysis - 5.7 hours (while the concentration of acyclovir in plasma decreases to 60% of the initial value).
Indications
treatment of infections of the skin and mucous membranes caused by the virus Herpes simplex type 1 and 2, both primary and secondary, including genital herpes, prevention of exacerbations of recurrent infections caused by the virus Herpes simplex type 1 and 2 in patients with normal immune status; recurrent infections caused by the Herpes simplex type 1 and 2 virus in patients with immunodeficiency; as part of complex therapy in patients with severe immunodeficiency: in HIV infection (AIDS stage, early clinical manifestations and developed clinical th picture) and in patients undergoing bone marrow transplants, treatment of primary and recurrent infections caused by virus Varicella zoster (chickenpox, shingles).
Contraindications
Hypersensitivity to acyclovir, ganciclovir, valacyclovir or components of the drug, lactation period, children under 3 years old. ).
Precautionary measures
Do not exceed the recommended dose. With caution, you should prescribe the drug during dehydration, renal failure, neurological disorders or neurological reactions to the use of cytotoxic drugs (including history), pregnancy, elderly patients.
Use during pregnancy and lactation
Use of the drug during pregnancy is possible only when the intended benefit to the mother exceeds the potential risk to the fetus. If necessary, use of the drug during lactation should decide whether to stop breastfeeding.
Dosage and administration
Inside, during or immediately after a meal, drink plenty of water. The dosage regimen is set individually depending on the severity of the disease. In case of infections of the skin and mucous membranes caused by the Herpes simplex type 1 and type 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 with a developed clinical picture of HIV infection (including early clinical manifestations of HIV infection and the AIDS stage), after bone marrow implantation, 400 mg is prescribed 5 times a day. To prevent recurrences of infections caused by the Herpes simplex virus 1 and 2 types patients with normal immune status in Adults - 200 mg 4 times a day every 6 hours, course duration from 6 to 12 months. To prevent infections caused by the Herpes simplex type 1 and 2 virus, in patients with immune deficiency Adults - 200 mg 4 times per day every 6 hours, maximum This dose is up to 400 mg 5 times a day, depending on the severity of the infection. When treating herpes zoster, it is 800 mg 5 times a day (every 4 hours during wakefulness, except for a night's sleep) for 7-10 days. 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 at the rate 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 amount 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 of the drug should be reduced to 400 mg, dividing it into 2 doses (with intervals of at least 12 hours, ie 200 mg 2 times day). When treating infections caused by Varicella zoster, and with maintenance therapy 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 less than 10 ml / min - 800 mg 2 times a day with an interval of 12 hours.
Side effects
On the part of the digestive system: nausea, vomiting, diarrhea, abdominal pain; rarely - a reversible increase in the content of bilirubin and the activity of "liver" enzymes. From the hematopoietic system: very rarely - anemia, leukopenia, thrombocytopenia. From the urinary system: rarely - an increase in urea and creatinine in the blood; very rarely - acute renal failure. From the central nervous system: headache, weakness, dizziness, fatigue, confusion, hallucinations, drowsiness, paresthesias, convulsions, decreased concentration, agitation. Allergic reactions: itching, rash, Lyell's syndrome, urticaria, exudative erythema multiforme, incl.Stevens-Johnson syndrome, angioedema, anaphylaxis. Others: fever, lymphadenopathy, peripheral edema, blurred vision, myalgia, alopecia.
Overdose
Symptoms: agitation, coma, convulsions, lethargy. Aciclovir can precipitate in the renal tubules if its concentration exceeds the solubility in the renal tubules (2.5 mg / ml). Treatment: symptomatic therapy.
Interaction with other drugs
Simultaneous use with probenecid leads to an increase in the average T1 / 2 and reduced clearance of acyclovir. When used simultaneously with nephrotoxic drugs, the risk of renal dysfunction increases.
special instructions
When taking the drug, it is necessary to control the kidney function (blood urea and plasma creatinine levels). When using the drug, it is necessary to ensure sufficient fluid intake. Long-term or repeated treatment of acyclovir patients with impaired immunity can lead to the appearance of virus strains that are not sensitive to its action. Most of the isolated strains of acyclovir-insensitive viruses show a relative shortage of viral thymidine kinase; strains with altered thymidine kinase or with altered DNA polymerase were isolated. The in vitro effect of acyclovir on isolated strains of the Herpes simplex virus can cause the appearance of less sensitive strains. Aciclovir does not prevent the transmission of herpes through sexual contact, therefore during treatment it is necessary to refrain from sexual intercourse, even in the absence of clinical manifestations. Impact on the ability to drive vehicles and control mechanisms the period of treatment should be careful when driving and doing other potentially hazardous activities that require higher Concentration of attention and speed of psychomotor reactions.