Nemozol, 100 mg/5 ml suspension 20 ml

Nemozolol is an anthelmintic drug. Main mechanism of action is connected with inhibiting effect on polymerization of beta-tubulin, which leads to destruction of cytoplasmic micro-channels of cells of intestinal tract of helminthes; it changes course of biochemical processes (inhibits utilization of glucose), blocks movement of secretory granules and other organelles in muscle cells of roundworms, causing their death. It is most active against larval forms of cestodes – Echinococcus granulosus and Taenia solium, against nematodes – Strongyloides stercolatis.

Pharmacokinetics

Intake and distribution

After oral administration it is poorly absorbed from the gastrointestinal tract, unchanged is not determined in plasma. Bioavailability when ingested is low, about 30%. Simultaneous use with fatty food increases absorption and Cmax value in blood plasma by 5 times.

Metabolism and excretion

Albendazole is rapidly biotransformed in the liver into the primary metabolite – albendazole sulfoxide, which also has anthelminthic activity. Cmax of albendazole sulfoxide in blood plasma is reached within 2 to 5 hours, the binding with plasma proteins is 70%. Albendazole sulfoxide is almost completely distributed throughout the body; it is found in the urine, bile, liver, cyst wall and cystic fluid, cerebrospinal fluid.

Albendazole sulfoxide is converted in the liver to albendazole sulfone (secondary metabolite) and other oxidized products. T1/2 of albendazole sulfoxide is 8-12 hours. It is excreted as different metabolites in the urine.

Pharmacokinetics in special clinical cases

The excretion of albendazole and its main metabolite does not change with impaired renal function.

In patients with impaired liver function the bioavailability is increased, Cmax of albendazole sulfoxide in plasma is increased by 2 times, T1/2 is prolonged. Albendazole is an inducer of microsomal enzymes of cytochrome P450 system; it accelerates metabolism of many drugs.

Indications

Active ingredient

Composition

5 ml of suspension contains:

The active ingredient:

albendazole 100 mg;

Associates:

Microcrystalline cellulose,

sodium carboxymethylcellulose,

glycerin (glycerol),

benzoic acid,

potassium hydrochloride,

sorbic acid,

polysorbate-80,

sorbitol solution,

mixed fruit flavor essence,

cream essence,

purified water.

How to take, the dosage

Nemozolol is administered orally, with meals or after meals, the tablets are not chewed and are washed down with water. The use of laxatives and a special diet are not required. It is recommended to treat all members of the family at the same time.

The dose of Nemozole is set individually, depending on the type of helminth and body weight of the patient.

Nemozole administration in children under 2 years old

Cysticercosis of the brain (neurocysticercosis): 15 mg/kg/day for 8 days, repeated if necessary.

Ankylostomidosis, enterobiasis, ascariasis: 200 mg once, repeated in 3 weeks if necessary.

Strongyloidiasis and cestodiasis: 200 mg once daily for 3 days, if necessary it is repeated in 3 weeks.

Nemozole administration in children over 2 years old and adults

Neurocysticercosis and echinococcosis: Patients with a body weight of 60 kg or more Nemozolol is prescribed at 400 mg 2 times a day, with a body weight less than 60 kg the dose is set at the rate of 15 mg/kg/day, divided into 2 doses; the maximum daily dose is 800 mg; treatment course for neurocysticercosis is 8-30 days; for echinococcosis – 3 cycles of 28 days with a 14-day interval between cycles.

Ascaridosis, trichocephaliasis, enterobiasis and ankylostomidosis: 400 mg once, repeated in 3 weeks if necessary.

Strongyloidiasis and cestodiasis: 400 mg once daily for 3 days, repeated in 3 weeks if necessary.

Lambliosis: 400 mg once daily for 3 days or at the rate of 10-15 mg/kg once daily for 5-7 days.

Toxocarosis: to adults and children over 14 years old with body weight over 60 kg Nemozolol is used in a single dose of 400 mg, in those with body weight less than 60 kg – 200 mg, in children under 14 years the dose is 10 mg/kg, 2 times a day and the therapy duration is 7-14 days.

Special Instructions

The therapy should be discontinued if leukopenia develops.

In neurocysticercosis with ocular lesions the retina should be examined before starting treatment (risk of exacerbating its pathology). Women of reproductive age are tested for the absence of pregnancy before starting treatment. During therapy reliable contraception is mandatory.

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

Contraindications

Hypersensitivity, pregnancy, lactation, childhood (under 6 years – safety not determined).

With caution: inhibition of medullary hematopoiesis, hepatic failure, cirrhosis of the liver, retinal pathology.

Side effects

Digestive system disorders: abdominal pain, nausea, vomiting, increased activity of “liver” transaminases.

Nervous system disorders: headache, dizziness, meningeal symptoms.

Hematopoietic disorders: leukopenia, granulocytopenia, agranulocytosis, thrombocytopenia, pancytopenia. Allergic reactions: skin rash, itching.

Others:Hyperthermia, increased BP, impaired renal function, alopecia, acute renal failure.

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