Description
Ekovir 400 (Acіclovir)
- International and chemical name:acіclovir; 2-Amino-1, 9-dihydro-9 – [(2-hydroxyethoxy) methyl] -6H-purin-6-one;
- Basic physical and chemical characteristics: white round, bulbous tablets with the seal “VS2”, diameter 12 mm and height 4, 8 ± 0, 2 mm;
- Composition:1 tablet contains aciclovir 400 mg;
- Other constituents: microcrystalline cellulose, silicon dioxide, colloidal anhydrous, magnesium stearate, copolyvidone, sodium starch glycolate.
- Form of release of the medicinal product. Pills.
- Pharmacotherapeutic group. Antiviral drugs for systemic use.
Action of the medicine.
Pharmacodynamics Ekovir 400 is an antiviral drug, especially effective against herpes simplex viruses (Herpes simplex) and herpes zoster (Varicella zoster). The similarity of the structures of acyclovir and deoxyguanidine allows acyclovir to interact with viral enzymes, which leads to an interruption in the multiplication of the virus. After the penetration of acyclovir into the herpes infected cell under the influence of thymidine kinase, which is excreted by the virus, acyclovir is converted
in acyclovir-monophosphate, which by enzymes of the host cell is converted into acyclovir-diphosphate, and then into the active form of acyclovir-triphosphate, which blocks the spread of viral DNA. Selectively acts on the synthesis of viral DNA. Acyclovir-triphosphate practically does not affect DNA replication of the host cell (human cells).
Specificity and high selectivity of action are mainly due to its accumulation in cells affected by the herpes virus. Has a high activity with respect to herpes simplex virus type I and II; a virus that causes varicella and shingles; the Epstein-Barr virus. Has moderate activity in relation to cytomegavirus. When herpes prevents the occurrence of new elements of rashes, reduces the likelihood of cutaneous dissemination and visceral complications, accelerates the formation of picks, reduces pain in the acute phase of herpes zoster. Has immunostimulating effect.
Pharmacokinetics. After oral administration, it is partially absorbed in the intestinal tract, through low lipophilicity, absorption after oral use of 400 mg is about 20%, and dose-dependent concentrations are formed sufficient to effectively treat viral diseases. The maximum concentration after oral administration is 400 mg -1, 2 μg / ml per day, and the minimum concentration is 0, 6 μg / ml. Peak maximum concentration is achieved in 1.5 – 2 hours. Penetrates through the blood-brain and placental barrier, is excreted in breast milk. It penetrates well into organs and tissues, the concentration in the cerebrospinal fluid is 50% of the blood level. After oral administration of 1 g per day, the concentration in breast milk is 60-410% of its plasma concentration (in the body of a child with breast milk, acyclovir is administered at a dose of 0.3 mg / kg per day). The connection with plasma proteins is 9-33%. Metabolised in the liver to form a metabolite of 9-carboxymethoxymethylguanine. It is excreted by the kidneys in the unchanged state, through glomerular and tubular secretion, in the form of a metabolite – 10-15%. The rate of excretion slows down with age, but the half-life of the active substance increases. In patients with severe renal insufficiency, the half-life is 20 hours, with hemodialysis – 5-7 hours (with the concentration of acyclovir in the plasma decreases to 60% of the output value).
Indications for use of Ekovir 400.
Herpes simplex infections, genital herpes on the skin and mucous membranes (most often – recurrent genital herpes ).
For the prevention of recurrence is shown to adults with complicated forms of frequent genital viral infections.
For the treatment of chickenpox and herpes zoster.
Method of use and dose of Ekovir 400.
In the treatment of herpes simplex skin and mucous membranes appoint 200 mg 5 times a day every 4 hours, with the exception of the period of night sleep. The course of treatment – 5 days, if necessary, can be continued. In cases of severe immunodeficiency (including after bone marrow transplantation or when intestinal absorption is disturbed) 400 mg 5 times a day are prescribed. Treatment should be started as soon as possible after the onset of infection. To prevent recurrence of herpes simplex, patients with normal immune status are prescribed 200 mg 4 times a day every 6 hours or 400 mg twice a day every 12 hours. When relapses begin treatment in the prodromal period or with the appearance of the first elements of rashes.
Therapy should be interrupted periodically after 6 to 12 months (to determine possible changes during the course of the disease). To prevent recurrence of herpes simplex, immunocompromised patients are prescribed 200 mg 4 times a day every 6 hours. In the case of severe immunodeficiency (after bone marrow transplantation or when intestinal absorption is abnormal), 400 mg 5 times a day. The duration of the preventive course of therapy is determined by the duration of the period when there is a risk of infection. Children from 2 years are prescribed the same doses as adults. To treat primary genital herpetic infection, 200 mg 5 times a day for 5 to 10 days, with relapse 200 mg 5 times a day for 5 days. For prophylaxis, 200 mg 4 times a day or 400 mg twice a day for 6 to 12 months; against the background of severe immunodeficiency – 400 mg 4 times a day (treatment is continued until there is a risk of risk). For the treatment of chickenpox and herpes zoster, 800 mg are prescribed intravenously 5 times a day every 4 hours, except during the night sleep. The course of treatment is 7 days. Children over 6 years – 800 mg 4 times a day; 2 – 6 years – 400 mg 4 times a day. A more accurate dose can be determined from the calculation of 20 mg / kg, but not more than 800 mg 4 times a day. The course of treatment is 5 days.
In patients with impaired renal function: in the treatment and prevention of infections caused by herpes simplex, in patients with Cl creatinine <10 ml / minute dosage is
reduce to 200 mg 2 times a day with 12-hour intervals;
In the treatment of infections caused by shingles, in patients with Cl creatinine <10 ml / min it is recommended to reduce dosages to 800 mg 2 times a day at 12-hour intervals; with Cl creatinine up to 25 ml / minute is prescribed 800 mg 3 times a day at 8-hour intervals.
Side effect of Ekovir 400
When the drug is used, skin rash, gastrointestinal disturbances such as nausea, vomiting, abdominal pain, constipation and diarrhea,
pain, fatigue, dizziness, hallucinations, hyperbilirubinemia. All these symptoms disappear after the suspension of therapy with acyclovir.
Contraindications.
Children under 2 years.
Hypersensitivity to the components of the drug.
Overdose Ekovir 400
The maximum dose of acyclovir 5 g, taken at a time, does not provoke intoxication or overdose. But patients who took a dose that exceeds 5 g should be carefully examined for signs of intoxication.
Features of use
Patients with reduced immunity (with HIV / AIDS or after bone marrow transplantation) should be given systemic use of the drug when using acyclovir cream, as in the case of severe and recurrent herpesvirus infection. Long-term or repeated treatment with acyclovir patients with reduced immunity may result in the emergence of strains of viruses that are insensitive before its action. In most isolated strains of viruses, insensitive to acyclovir, there is a relative lack of viral thymidine kinase; strains with altered thymidine kinase or with altered DNA polymerase were isolated. In-vitro action of acyclovir on isolated strains of herpes simplex virus can cause the emergence of less sensitive strains.
The use of Ekovir 400 during pregnancy is indicated in cases where the benefit to the mother exceeds the potential risk to the fetus.
In the course of therapy with high oral doses of the drug, a sufficient supply of fluid to the patient’s body should be ensured.
During therapy with Ekovir 400, breast-feeding should be discontinued.
In cases of violation of the excretory function of the kidneys and elderly people, the dose is reduced in view of the clearance of creatinine.
In case of allergic reactions, the drug should be discarded.
The interaction of Ekovir 400 with other medicines.
Probenecid reduces the excretion of acyclovir by 30%, which causes an increase in the half-life time of acyclovir.
