Aciclovir Belupo, 400 mg 21 pcs

Acyclovir is an antiviral drug, a synthetic analog of acyclic purine nucleoside, which has a highly selective effect 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. In vitro acyclovir is effective against herpes simplex virus – Herpes simplex type 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: When taken orally 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. 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 a day is 0.7 mcg/ml, Tmax is 1.5-2 h.

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 hours, with hemodialysis – 5.7 hours (with acyclovir plasma concentration decreases to 60% of the initial value).

About 84% is excreted unchanged in the kidneys and 14% – as a metabolite. Renal clearance of acyclovir is 75-80% of the total plasma clearance. Less than 2% of acyclovir is excreted from the body through the intestine.

Indications

Treatment of infections of the skin and mucous membranes caused by the Herpes simplex virus types 1 and 2, both primary and secondary, including genital herpes;
prevention of exacerbations of recurrent infections caused by Herpes simplex virus types 1 and 2 in patients with normal immune status;
prevention of primary and recurrent infections caused by the Herpes simplex virus types 1 and 2 in patients with immunodeficiency;
as part of complex therapy in patients with severe immunodeficiency: with HIV infection (stage AIDS, early clinical manifestations and detailed clinical picture) and in patients who have undergone bone marrow transplantation;
treatment of primary and recurrent infections caused by the Varicella zoster virus (chickenpox, herpes zoster).

Pharmacological effect

Acyclovir is an antiviral drug, a synthetic analogue of an acyclic purine nucleoside, which has a highly selective effect on herpes viruses. Inside virus-infected cells, under the influence of viral thymidine kinase, a series of sequential reactions of transformation of acyclovir into mono-, di- and triphosphate of acyclovir takes place. Acyclovir triphosphate is integrated into the viral DNA chain and blocks its synthesis through competitive inhibition of viral DNA polymerase.

In vitro, acyclovir is effective against the herpes simplex virus – Herpes simplex types I and II, against the Varicella zoster virus; higher concentrations are required to inhibit Epstein-Barr virus.

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

Pharmacokinetics: When taken orally, bioavailability is 15-30%. Acyclovir penetrates well into all organs and tissues of the body, including the brain and skin. Plasma protein binding is 9-33% and is independent of its plasma concentration. 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 mcg/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 – 20 hours, with hemodialysis – 5.7 hours (in this case, the concentration of acyclovir in plasma decreases 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 from the body through the intestines.

Special instructions

Long-term or repeated treatment with acyclovir in patients with reduced immunity can lead to the emergence of strains of viruses 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.

Prescribe with caution to patients with impaired renal function and 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, kidney function should be monitored (blood urea and plasma creatinine levels).

Acyclovir does not prevent the sexual transmission of herpes, so during the treatment period it is necessary to abstain from sexual intercourse, even in the absence of clinical manifestations.

Active ingredient

Acyclovir

Composition

1 tab.:

Pregnancy

Use during pregnancy is only possible if the expected benefit to the mother outweighs the potential risk to the fetus.
If it is necessary to use the drug during lactation, breastfeeding should be stopped.

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).

Side Effects

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, increased fatigue, drowsiness, confusion, hallucinations, paresthesia, agitation.

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

Other: rarely – alopecia, fever, myalgia, blurred vision, lymphadenopathy.

Interaction

Concomitant use with probenecid leads to an increase in the mean half-life and a decrease in the clearance of acyclovir.

Overdose

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

Recommendations for use

Inside.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 ° C.

Shelf life

4 years.

Manufacturer

Belupo, medicines and cosmetics d.d., Croatia