Description
Pharmacological action
Acyclovir is an antiviral drug, a synthetic analogue of the acyclic purine nucleoside, which has a highly selective effect on herpes viruses. Inside the virus-infected cells, a series of sequential reactions of the transformation of acyclovir into acyclovir mono-, di- and triphosphate undergoes a viral thymidine kinase. Acyclovir triphosphate is integrated into the chain of viral DNA and blocks its synthesis through 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:
When administered, the 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 administration of 200 mg 5 times a day – 0.7 Ñg / ml, Tmax – 1.5-2 hours.
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 failure, T1 / 2 is 20 hours, with hemodialysis it is 5.7 hours (in this case, the concentration of acyclovir in plasma is reduced to 60% of the initial value) .
About 84% is excreted by the kidneys unchanged 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 excreted through the intestines.
Indications
Treatment of infections of the skin and mucous membranes caused by Herpes simplex virus types 1 and 2, both primary and secondary, including genital herpes
prevention of exacerbation of recurrent infections caused by Herpes simplex virus 1 and 2 types in patients with normal immune status
prevention of primary and recurrent infections caused by Herpes simplex virus types 1 and 2, in patients with
immunodeficiency as part of complex therapy in patients with severe immunodeficiency: with HIV infection (AIDS stage, early clinical manifestations and an expanded clinical picture) and in patients who underwent
bone marrow transplantation, treatment of primary and recurrent infections caused by Varicella zoster virus (chicken pox, shingles).
Contraindications
– hypersensitivity to acyclovir, ganciclovir, famciclovir, Valaciclovir or any auxiliary substance of the drug Acyclovir Belupo
– lactation period
– children’s age up to 3 years (for this dosage form).
Precautions: dehydration, renal failure, neurological disorders, including in the anamnesis.
Recommended Uses for
Inside.
Treatment should be started as soon as possible, immediately after the onset of the first symptoms of the disease.
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, for adults and children over 3 years of age, Acyclovir Belupo is prescribed 200 mg 5 times / day. for 5 days at 4-hour intervals throughout the day and with an 8-hour interval at night. In more severe cases of the disease, the course of treatment can be extended as prescribed by the doctor.
As part of complex therapy for severe immunodeficiency, including the expanded clinical picture of HIV infection (including the early clinical manifestations of HIV infection and the stage of AIDS), 400 mg 5 times / day are prescribed after bone marrow implantation.
For the prevention of relapse of infections caused by Herpes simplex viruses type I and II, patients with normal immune status and with relapse 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, 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 with an 8-hour interval at night. The duration of treatment is 7-10 days. Children over 3 years of age are prescribed 20 mg / kg 4 times / day. within 5 days, for children weighing more than 40 kg, the drug is prescribed 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 CC less than 10 ml / min, the dose 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 CC less than 10 ml / min, it is recommended to reduce the dose to 800 mg 2 times / day. with 12-hour intervals with CC up to 25 ml / min, 800 mg are prescribed 3 times / day. at 8 hour intervals.
The drug Acyclovir Belupo is taken during or immediately after a meal and washed down with a sufficient amount of water.
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 you need to use the drug during lactation, you should stop breastfeeding.
Special instructions
Prolonged or repeated treatment with acyclovir of patients with reduced immunity can lead to the appearance of strains of viruses that are insensitive to its action. Apply strictly as prescribed by the doctor to avoid complications in adults and children over 3 years old.
Use with caution 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 flow of a sufficient amount of fluid.
When taking the drug, kidney function (blood urea and blood plasma creatinine) should be monitored.
Acyclovir does not prevent sexual transmission of herpes, therefore, during treatment it is necessary to refrain from sexual intercourse, even in the absence of clinical manifestations.
Composition
1 tab.:
– acyclovir 400 mg
Excipients:
povidone,
carboxymethyl starch sodium,
microcrystalline cellulose,
silicon dioxide colloidal magnesium,
.
Shell composition:
Opadry Pink OY-24926 (hypromellose, titanium dioxide, macrogol, red iron oxide, yellow iron oxide).
Side effects
The drug Acyclovir Belupo is usually well tolerated.
From the digestive system: in isolated cases – abdominal pain, nausea, vomiting, diarrhea.
On the part of laboratory indicators: a slight increase in the activity of liver enzymes, rarely – a slight increase in the levels of urea and creatinine, hyperbilirubinemia, leukopenia, erythropenia.
From the side of the central nervous system and peripheral nervous system: rarely – headache, weakness in some cases – tremors, dizziness, increased fatigue, drowsiness, confusion, hallucinations, paresthesia, agitation.
Allergic reactions: anaphylactic reactions, skin allergic reactions (pruritus, Lyell’s syndrome, urticaria, erythema multiforme exudative, including Stevens-Johnson syndrome), peripheral edema.
Other: rarely – alopecia, fever, myalgia, visual impairment, lymphadenopathy.
Drug Interactions
Concomitant use with probenecid leads to an increase in the average half-life and a decrease in clearance of acyclovir.
Concomitant use with nephrotoxic drugs increases the risk of impaired renal function.
Strengthening of the effect is noted with the simultaneous administration of immunostimulants.
Overdose of
Oral administration of 20 g of acyclovir did not lead to the development of specific symptoms.
Side effects from the central nervous system may occur – convulsions, tremors, lethargy.
In case of an overdose after oral administration, it is necessary to induce vomiting (best within 30 minutes after taking the drug) and take adsorbents.
In case of acute renal failure and anuria: maintenance of vital functions, hemodialysis.
Storage conditions
In a dry, dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.
Expiration
4 years.
Deystvuyuschee substances
acyclovir
Pharmacy terms
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pharmacy terms of prescription
Form of Treatment
tablets
Appointment
Kormyaschym mothers on purpose doctor, Beremenn m on purpose doctor, Detyam on purpose doctor, Detyam over 3 years
Indications
Herpes, Cold
