Composition
of 1 tab. : – acyclovir 400 mg
Auxiliary substances:
Ingredients: povidone,
sodium carboxymethyl starch,
microcrystalline cellulose,
colloidal silicon dioxide,
magnesium stearate.
Shell composition:
Opadry Pink OY-24926 (hypromellose, titanium dioxide, macrogol, iron oxide dye red, iron oxide dye yellow).
Pharmacological action
Pharmaceutical group: antiviral agent.
Pharmaceutical action: Acyclovir is an antiviral drug, a synthetic analog of acyclic purine nucleoside, which has a highly selective effect on herpes viruses. Inside virus-infected cells, viral thymidine kinase undergoes a series of sequential reactions of transformation of acyclovir into mono -, di-and triphosphate of acyclovir. Acyclovir triphosphate is incorporated into the viral DNA chain and blocks its synthesis by competitive inhibition of viral DNA polymerase.
In vitro, acyclovir is effective against herpes simplex virus-Herpes simplex type I and II, against Varicella zoster virus; higher concentrations are required to inhibit Epstein-Barr virus.
In vivo, acyclovir is therapeutically and prophylactically effective primarily for viral infections caused by Herpes simplex.
Pharmacokinetics: Oral bioavailability is 15-30%. Acyclovir penetrates well into all organs and tissues of the body, including the brain and skin. Binding to plasma proteins is 9-33% and does not depend on its concentration in plasma. The concentration in the cerebrospinal fluid is about 50% of its concentration in plasma. Acyclovir crosses the placental barrier and accumulates in breast milk. Cmax after oral use of 200 mg 5 times a day – 0.7 mcg/ml, Tmax – 1.5-2 hours.
It is metabolized in the liver to form the pharmacologically inactive compound 9-carboxymethoxymethylguanine. T1 / 2 in adults with normal renal function is 2-3 hours.
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).
About 84% is excreted unchanged by the kidneys and 14% in the form of a metabolite. The renal clearance of acyclovir is 75-80% of the total plasma clearance. Less than 2% of acyclovir is eliminated from the body through the intestines.
Indications
- Treatment of infections of the skin and mucous membranes caused by Herpes simplex virus type 1 and 2, both primary and secondary, including genital herpes;
- prevention of exacerbations of recurrent infections caused by the Herpes simplex virus type 1 and 2 in patients with normal immune status;
- prevention of primary and recurrent infections caused by the virus Herpes simplex type 1 and 2, in patients with immunodeficiency;
- in the complex therapy in patients with severe immunodeficiency: HIV infection (AIDS, early clinical manifestations and comprehensive clinical picture) and in patients undergoing bone marrow transplantation;
- treatment of primary and recurrent infections caused by the virus Varicella zoster (chickenpox, shingles).
Use during pregnancy and lactation
Use during pregnancy is only possible if the intended benefit to the mother outweighs the potential risk to the fetus. If it is necessary to use the drug during lactation, stop breastfeeding.
Contraindications
-hypersensitivity to acyclovir, ganciclovir, famciclovir, valacyclovir or any excipient of the drug Acyclovir Belupo;- lactation period— – children under 3 years of age (for this dosage form). With caution: dehydration, renal failure, neurological disorders, including in the anamnesis.
Side effects
The drug Acyclovir Belupo is usually well tolerated.
From the digestive system: in isolated cases – abdominal pain, nausea, vomiting, diarrhea.
From the laboratory parameters: transient slight increase in the activity of liver enzymes, rarely-a slight increase in urea and creatinine levels, hyperbilirubinemia, leukopenia, erythropenia.
From the central nervous system and peripheral nervous system: rarely-headache, weakness; in some cases-tremor, dizziness, fatigue, drowsiness, confusion, hallucinations, paresthesia, agitation.
Allergic reactions: anaphylactic reactions, allergic skin reactions (pruritus, Lyell’s syndrome, urticaria, erythema multiforme, including Stevens-Johnson syndrome), peripheral edema.
Other: rarely-alopecia, fever, myalgia, visual impairment, lymphadenopathy.
Interaction
Concomitant use with probenecid leads to an increase in the average half-life and a decrease in the clearance of acyclovir.
Concomitant use with nephrotoxic drugs increases the risk of impaired renal function.
An increase in the effect is noted with simultaneous use of immunostimulants.
How to take, course of use and dosage
Inside. Treatment should be started as soon as possible, immediately after the first symptoms of the disease appear. The dosage regimen is set individually, depending on the severity of the disease. In the treatment of infections of the skin and mucous membranes caused by Herpes simplex type I and II, adults and children over 3 years of age, Acyclovir Belupo is prescribed 200 mg 5 times a day. for 5 days at 4-hour intervals during the day and at 8-hour intervals at night. In more severe cases of the disease, the course of treatment may be extended as prescribed by a doctor.
As part of complex therapy for severe immunodeficiency, including a detailed clinical picture of HIV infection (including early clinical manifestations of HIV infection and the stage of AIDS), after bone marrow implantation,400 mg is prescribed 5 times a day. To prevent relapses of infections caused by Herpes simplex viruses type I and II, patients with normal immune status and with relapse of the disease are prescribed 200 mg 4 times / day. every 6 hours.
For the prevention of infections caused by Herpes simplex viruses type I and II, adults and children over 3 years of age with immunodeficiency, the drug Acyclovir Belupo is recommended to be prescribed 200 mg 4 times/day. every 6 hours, the maximum dose is up to 400 mg of acyclovir 5 times/day. depending on the severity of the infection.
In the treatment of infections caused by Varicella zoster, adults are prescribed 800 mg 5 times/day. every 4 hours during the day and at 8-hour intervals at night. The duration of treatment is 7-10 days. Children over 3 years of age are prescribed 20 mg / kg 4 times a day. within 5 days, children with a body weight of more than 40 kg are prescribed the drug in the same dosage as adults.
In the treatment of infections caused by Herpes zoster, adults are prescribed 800 mg 4 times a day every 6 hours for 5 days.
In patients with impaired renal function: In the treatment and prevention of infections caused by Herpes simplex in patients with creatinine clearance less than 10 ml/min, the dose of the drug should be reduced to 200 mg 2 times/day at 12-hour intervals.
In the treatment of infections caused by Varicella zoster, in patients with creatinine clearance less than 10 ml / min, it is recommended to reduce the dose of the drug to 800 mg 2 times/day with 12-hour intervals; with creatinine clearance up to 25 ml / min,800 mg is prescribed 3 times/day with 8-hour intervals. The drug Acyclovir Belupo is taken during or immediately after a meal and washed down with a sufficient amount of water.
Overdose
Oral use of 20 g of acyclovir did not lead to the development of specific symptoms.
There may be side effects from the central nervous system-convulsions, tremors, lethargy.
In case of overdose after oral use, it is necessary to induce vomiting (preferably within 30 minutes after taking the drug) and take adsorbents. In case of acute renal failure and anuria: maintenance of vital functions, hemodialysis.
Special instructions
Long-term or repeated treatment with acyclovir in patients with reduced immunity may lead to the appearance of virus strains that are insensitive to its action. Use strictly as prescribed by a doctor to avoid complications in adults and children over 3 years of age. Caution should be used in patients with impaired renal function, elderly patients due to an increase in the half-life of acyclovir.
When using the drug Acyclovir Belupo, it is necessary to ensure the intake of a sufficient amount of fluid. When taking the drug, renal function (blood urea and plasma creatinine levels) should be monitored.
Acyclovir does not prevent sexual transmission of herpes, so during treatment it is necessary to refrain from sexual contact, even in the absence of clinical manifestations.
Form of production
Pills.
Active ingredient
Acyclovir
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
Purpose
For adults as prescribed by a doctor, Pregnant women as prescribed by a doctor, Children over 3 years of age, Children as prescribed by a doctor
Indications
Cold, Cold Sores
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Side effects of Acyclovir Belupo pills 400mg, 35pcs.
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