Acyclovir Belupo, 400 mg 35 pcs

Pharmgroup:antiviral drug.

Pharm Action: Acyclovir is an antiviral drug, a synthetic analog of acyclic purine nucleoside, which has highly selective action on herpes viruses. A series of sequential reactions of acyclovir transformation into mono-, di- and triphosphate acyclovir takes place inside virus-infected cells under the action of viral thymidine kinase. Acyclovir triphosphate integrates 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 virus types I and II, against Varicella zoster virus; higher concentrations are required for inhibition of Epstein-Barr virus.

In vivo acyclovir is therapeutically and prophylactically effective primarily in viral infections caused by Herpes simplex.

Pharmacokinetics: The bioavailability is 15-30% when taken orally. 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. Concentration in cerebrospinal fluid is about 50% of its concentration in plasma. Acyclovir penetrates the placental barrier and accumulates in breast milk. Cmax after oral administration of 200 mg 5 times per day is 0.7 mcg/ml, Tmax is 1.5-2 hours.

Metabolized in the liver to form 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 is 20 h, in hemodialysis – 5.7 h (while the concentration of acyclovir in plasma decreases to 60% of the initial value).

Indications

Active ingredient

Composition

1 tablet:
– acyclovir 400 mg

Supplementary substances:

povidone,

sodium carboxymethyl starch,

microcrystalline cellulose,

colloidal silicon dioxide,

magnesium stearate.

Composition of the shell:

Opadry Pink OY-24926 (hypromellose, titanium dioxide, macrogol, iron oxide red dye, iron oxide yellow dye).

How to take, the dosage

The treatment should be started as soon as possible, immediately after the appearance of the first symptoms of the disease.
Dosing 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 the preparation Acyclovir Belupo is administered 200 mg five times per day during five days with 4-hour intervals during the day and with 8-hour intervals at night. In more severe cases of the disease, the course of treatment may be prolonged by doctor’s prescription.

As part of complex therapy in cases of severe immunodeficiency including developed clinical picture of HIV infection (including early clinical manifestations of HIV infection and AIDS stage) and after bone marrow implantation it is prescribed by 400 mg 5 times per day.
For prophylaxis of recurrence of infections caused by Herpes simplex viruses of types I and II in patients with normal immune status and at disease relapse it is prescribed 200 mg 4 times per day every 6 hours.

For prevention of infections caused by Herpes simplex viruses type I and II in 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 acyclovir 5 times/day depending on the severity of infection.

In the treatment of infections caused by Varicella zoster, adults are prescribed 800 mg 5 times per day every 4 hours during the day and with 8 hours interval at night. The course of treatment is 7-10 days. Children over 3 years old are prescribed 20 mg/kg 4 times/day for 5 days; children with body weight over 40 kg are prescribed in the same dosage as adults.

In treatment of infections caused by Herpes zoster in adults 800 mg 4 times per 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 a CKR less than 10 ml/min, the drug dose should be reduced to 200 mg 2 times a day at 12-hour intervals.

In the treatment of infections caused by Varicella zoster, in patients with a CK of less than 10 ml/min, the drug dose should be reduced to 800 mg 2 times/day at 12-hour intervals; for CK of up to 25 ml/min, 800 mg 3 times/day at 8-hour intervals.
The drug Acyclovir Belupo is taken during or immediately after meals and with plenty of water.

Interaction

Concomitant use with probenecid leads to increased mean half-life and decreased clearance of acyclovir.

Concomitant use with nephrotoxic drugs increases the risk of impaired renal function.

A strengthening of the effect is noted with concomitant administration of immunostimulants.

Special Instructions

Prolonged or repeated treatment with acyclovir in patients with reduced immunity may lead to the emergence of virus strains that are insensitive to its action. Use strictly according to the prescription to avoid complications in adults and children over 3 years.
Caution is prescribed for patients with impaired renal function, the elderly due to the increased half-life of acyclovir.

When using the drug Acyclovir Belupo it is necessary to ensure adequate intake of fluids.
While taking the drug, renal function (blood urea and plasma creatinine levels) 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.

Contraindications

– hypersensitivity to acyclovir, ganciclovir, famciclovir, valacyclovir or any excipient of the drug Acyclovir Belupo;
– lactation period;
– children under 3 years (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.

Digestive system disorders: in single cases – abdominal pain, nausea, vomiting, diarrhea.

Laboratory disorders: transient slight increase in liver enzyme activity, rarely – small increase in urea and creatinine levels, hyperbilirubinemia, leukopenia, erythropenia.

CNS and peripheral nervous system: rarely – headache, weakness; in some cases – tremor, dizziness, fatigue, somnolence, mental confusion, hallucinations, paresthesia, agitation.

Allergic reactions: anaphylactic reactions, skin allergic reactions (pruritus, Lyell’s syndrome, urticaria, erythema multiforme, including Stevens-Johnson syndrome), peripheral edema.

Others: rarely – alopecia, fever, myalgia, visual impairment, lymphoadenopathy.

Overdose

Oral administration of 20 g of acyclovir did not lead to the development of specific symptoms.

CNS side effects may occur – seizures, tremors, lethargy.

In case of 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.

Pregnancy use

Similarities