Nemozole^® (Tablets, Suspension) Instructions for Use

ATC Code

P02CA03 (Albendazole)

Active Substance

Albendazole (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Anthelmintic drug

Pharmacotherapeutic Group

Anthelmintic agents; agents for the treatment of nematode infections; benzimidazole derivatives

Pharmacological Action

Anthelmintic agent with a broad spectrum of action; a benzimidazole carbamate derivative. It selectively inhibits the polymerization of beta-tubulin, leading to the destruction of the cytoplasmic microtubules in the intestinal tract cells of helminths.

It causes an irreversible impairment of glucose utilization in the helminth’s body and inhibits ATP synthesis.

It blocks the movement of secretory granules and other organelles in the muscle cells of roundworms, causing their death.

It is most effective against the larval forms of cestodes – Echinococcus granulosus and Taenia solium; and nematodes – Strongyloides stercoralis.

Pharmacokinetics

When taken orally, Albendazole is poorly absorbed from the gastrointestinal tract, is not detected in the plasma in its unchanged form, and has low bioavailability.

Taking with fatty food increases absorption and C_max by 5 times.

The time to reach C_max of albendazole sulfoxide is 2-5 hours.

Plasma protein binding is 70%; it penetrates in significant amounts into bile, liver, cerebrospinal fluid, urine, and the wall and fluids of helminth cysts.

It is metabolized in the liver to form the primary metabolite (albendazole sulfoxide), which has anthelmintic activity.

Albendazole sulfoxide is metabolized to albendazole sulfone (a secondary metabolite) and other oxidized products.

The T_1/2 of albendazole sulfoxide is 8-12 hours.

It is excreted with bile through the intestines in the form of the active metabolite albendazole sulfoxide, with only a small amount excreted in the urine.

In liver impairment, bioavailability increases, with the C_max of albendazole sulfoxide increasing by 2 times and the T_1/2 lengthening.

It is an inducer of the CYP1A2 isoenzyme in human liver cells.

Indications

Nematodoses: ascariasis, trichuriasis, ancylostomiasis, enterobiasis, trichinellosis, toxocariasis, giardiasis, strongyloidiasis; mixed helminthiases.

Tissue cestodoses: neurocysticercosis, hydatid echinococcosis of the liver, lungs, peritoneum; as an adjuvant in the surgical treatment of alveolar echinococcosis.

ICD codes

Dosage Regimen

Administer orally with a meal, as fatty food significantly increases absorption.

The standard single dose for adults and children over 2 years is 400 mg.

For intestinal nematodoses (ascariasis, trichuriasis, enterobiasis, hookworm), administer a single 400 mg dose; repeat after 3 weeks if necessary.

For strongyloidiasis and taeniasis, administer 400 mg once daily for 3 consecutive days.

For giardiasis in children, administer 400 mg once daily for 5 days.

For neurocysticercosis, the dose is weight-based: administer 400 mg twice daily for patients weighing 60 kg or more; for patients under 60 kg, administer 15 mg/kg/day in two divided doses (max 800 mg/day). Continue therapy for 8-30 days.

For hydatid echinococcosis, the dose is weight-based: administer 400 mg twice daily for patients weighing 60 kg or more; for patients under 60 kg, administer 15 mg/kg/day in two divided doses (max 800 mg/day). Administer treatment in cycles of 28 days, separated by a 14-day drug-free interval; repeat for 3 cycles.

In patients with impaired liver function, monitor closely and adjust dose if necessary due to increased bioavailability.

For children aged 1 to 2 years, a single 200 mg dose is recommended for intestinal nematodes; use the suspension for accurate dosing.

Contraindicated in children under 1 year for all dosage forms.

For all conditions, consult specific treatment protocols. Monitor blood counts and liver function during prolonged high-dose therapy.

Adverse Reactions

From the digestive system: abdominal pain, nausea, vomiting, increased activity of hepatic transaminases.

From the central nervous system: headache, dizziness, meningeal symptoms, increased intracranial pressure.

From the hematopoietic system: leukopenia, granulocytopenia, agranulocytosis, thrombocytopenia, pancytopenia.

Allergic reactions: skin rash, itching.

From the urinary system: impaired renal function, acute renal failure.

Other: hyperthermia, increased blood pressure, alopecia.

Contraindications

Retinal pathology, pregnancy, lactation (breastfeeding), children under 1 year of age (for all dosage forms); toxocariasis in adults and children over 14 years of age and with a body weight less than 60 kg; hypersensitivity to albendazole and other benzimidazole derivatives.

With caution

Impaired liver function, bone marrow hematopoiesis suppression, liver cirrhosis.

Use in Pregnancy and Lactation

Albendazole is contraindicated for use during pregnancy and during lactation (breastfeeding).

Women of childbearing potential are advised to use non-hormonal contraceptive methods during treatment. It is not known whether Albendazole and its active metabolite are excreted in breast milk.

In experimental studies on animals, the teratogenicity of albendazole has been shown.

Use in Hepatic Impairment

Albendazole should be prescribed with caution to patients with hepatic insufficiency, liver cirrhosis.

Use in Renal Impairment

In patients with impaired renal function, the clearance of albendazole does not change.

Pediatric Use

Contraindicated for use in children under 1 year of age (for all dosage forms).

In children over 1 year of age, appropriate dosage forms are used.

In children, the use of albendazole in high doses for a long time should be avoided.

Geriatric Use

There are no specific restrictions.

Special Precautions

Therapy must be discontinued if leukopenia develops.

In neurocysticercosis with ocular involvement, an examination of the retina is necessary before starting treatment (the risk of worsening retinal pathology increases).

Patients receiving high doses should be under close supervision, with constant monitoring of blood counts and liver function.

In children, the use of albendazole in high doses for a long time should be avoided.

Drug Interactions

With simultaneous use with dexamethasone, praziquantel, an increase in the concentration of albendazole sulfoxide in blood plasma is possible.

An increase in the concentration of albendazole sulfoxide in bile and in the contents of an echinococcal cyst was found with the simultaneous use of albendazole and cimetidine, which may increase the effectiveness of echinococcosis treatment.

Simultaneous use with carbamazepine, phenytoin, phenobarbital, and Panax ginseng may lead to a decrease in the concentration of albendazole in plasma.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.