Nemozol, 400 mg

Albendazole is an anthelmintic drug, pharmacological properties of which are due to the action of the active substance – albendazole. Albendazole belongs to the group of carbamate benzimidazoles. The mechanism of action of albendazole is its ability to disrupt the activity of microtubule system of cells of the intestinal canal of helminths, causing damage to tubulin protein.

The consequence of this is biochemical disorders in the cell – inhibition of glucose transport and fumaratreductase, which underlies the suppression of cell division at the metaphase stage and which is associated with inhibition of oviposition and development of helminth larvae. Albendazole blocks movement of secretory granules and other organelles in muscle cells of roundworms, causing their death.

Albendazole is effective against most intestinal nematodes and larval (larval stages) of cestodes as well as giardia. Albendazole as an antiparasitic drug has a fairly broad spectrum of action.

Pharmacokinetics

Absorption. After oral administration the drug is poorly absorbed in the gastrointestinal tract and is not determined in unchanged form in blood plasma. Bioavailability is low when taken orally. Fatty food increases absorption and maximum concentration by 5 times.

Metabolism. Albendazole is rapidly converted in the liver to the primary metabolite – albendazole sulfoxide, which also has anthelmintic activity.

Distribution. Maximum plasma concentration of albendazole sulfoxide is reached 2-5 hours after administration. By 70% metabolite is bound to plasma proteins and completely distributed throughout the body: detected in urine, bile, liver, in the wall and fluid of helminth cysts, cerebrospinal fluid.

Extraction. Albendazole sulfoxide in the liver is converted into albendazole sulfone (secondary metabolite) and other oxidized products. Half-life of albendazole sulfoxide is 8-12 hours. It is excreted through the kidneys in the form of various metabolites. Excretion of albendazole and albendazole sulfoxide through the kidneys is insignificant. Clearance does not change in patients with impaired renal function.

In patients with liver damage – bioavailability is increased, maximum concentration of albendazole sulfoxide in blood plasma is increased by 2 times and the half-life is prolonged.

Albendazole induces cytochrome SUR1A2 in human liver cells and accelerates metabolism of many drugs.

Indications

Nematodes (ascariasis, enterobiasis, hookworm disease, necatoriasis, trichocephalosis);
mixed helminthic infestations;
strongyloidiasis;
neurocysticercosis caused by the larval form of Taenia solium;
echinococcosis of the liver, lungs, peritoneum, caused by the larval form of Echinococcus granulosus;
giardiasis;
toxocariasis;
as an adjuvant in the surgical treatment of echinococcal cysts.

Pharmacological effect

Albendazole is an anthelmintic drug, the pharmacological properties of which are determined by the action of the active substance – albendazole. Albendazole belongs to the group of carbamate benzimidazoles. The mechanism of action of albendazole is its ability to disrupt the activity of the microtubular system of the cells of the intestinal canal of helminths, thereby causing damage to the tubulin protein.

The consequence of this is biochemical disturbances in the cell – inhibition of the transport of glucose and fumarate reductose, which underlies the suppression of cell division at the metaphase stage and with which the inhibition of oviposition and the development of helminth larvae is associated. Albendazole blocks the movement of secretory granules and other organelles in the muscle cells of roundworms, causing their death.

Albendazole is effective against most intestinal nematodes, as well as larval (larval stages) cestodes, as well as Giardia. Albendazole as an antiparasitic drug has a fairly wide spectrum of action.

Pharmacokinetics

Suction. After oral administration, the drug is poorly absorbed from the gastrointestinal tract and is not detected in unchanged form in the blood plasma. Bioavailability when taken orally is low. Eating fatty foods increases absorption and maximum concentration by 5 times.

Metabolism. Albendazole is quickly converted in the liver into the primary metabolite, albendazole sulfoxide, which also has anthelmintic activity.

Distribution. The maximum plasma concentration of albendazole sulfoxide is achieved 2-5 hours after administration. 70% of the metabolite is bound to plasma proteins and is completely distributed throughout the body: found in urine, bile, liver, in the wall and fluid of helminth cysts, and cerebrospinal fluid.

Excretion. Albendazole sulfoxide is converted in the liver to albendazole sulfone (a secondary metabolite) and other oxidized products. The half-life of albendazole sulfoxide is 8-12 hours. It is excreted through the kidneys in the form of various metabolites. Renal excretion of albendazole and albendazole sulfoxide is negligible. In patients with impaired renal function, clearance does not change.

In patients with liver damage, bioavailability increases, the maximum concentration of albendazole sulfoxide in the blood plasma increases by 2 times, and the half-life is extended.

Albendazole induces cytochrome CYP1A2 in human liver cells and accelerates the metabolism of many drugs.

Special instructions

It is necessary to discontinue therapy if leukopenia develops. In case of neurocysticercosis with eye damage, before starting treatment, it is necessary to examine the retina (risk of worsening its pathology).

Women of reproductive age are tested to determine if they are not pregnant before starting treatment. Reliable contraception is required during therapy.

Patients receiving high doses should be closely monitored, with constant monitoring of blood status and liver function.

Active ingredient

Albendazole

Composition

1 tablet contains:

Active substance:

albendazole 400 mg;

Excipients:

corn starch,

sodium lauryl sulfate,

povidone-30,

methylparaben,

propylparaben,

gelatin,

purified talc,

sodium starch glycolate,

colloidal silicon dioxide,

magnesium stearate;

Shell composition:

hydroxypropyl methylcellulose, titanium dioxide, propylene glycol; isopropanol, methylene chloride (evaporate during drying).

Pregnancy

The drug albendazole is contraindicated during pregnancy and breastfeeding.

Contraindications

– Hypersensitivity to albendazole, other components of the drug and other benzimidazole derivatives;
– pathology of the retina;
– children under 3 years of age (for this dosage form);
– pregnancy and breastfeeding period

With caution
The drug albendazole is used with caution in cases of liver dysfunction (it is necessary to regularly monitor liver function before and during treatment), inhibition of bone marrow hematopoiesis, and liver cirrhosis.

Side Effects

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

From the nervous system: headache, dizziness, meningeal symptoms.

From the hematopoietic organs: leukopenia, granulocytopenia, agranulocytosis, thrombocytopenia, pancytopenia. Allergic reactions: skin rash, itching.

Other: hyperthermia, increased blood pressure, renal dysfunction, alopecia, acute renal failure.

Interaction

Concomitant use of albendazole with iraziquantel, dexamethasone and cimetidine may increase the concentration of albendazole sulfoxide in the blood.

Storage conditions

In a dry place, protected from light, at a temperature below 25 °C

Shelf life

3 years

Manufacturer

Ipka Laboratories Limited, India