Sanoxal, 400 mg

Sanoxal is an anthelminthic and antiprotozoal agent. It selectively inhibits polymerization of beta-tubulin, which leads to destruction of cytoplasmic microchannels 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 effective against larval forms of cestodes – Echinococcus granulosus and Taenia solium; nematodes – Strongyloides stercolatis.

Pharmacokinetics

absorption

After oral administration it is poorly absorbed from the gastrointestinal tract due to poor water solubility. The drug is quickly metabolized during the “first passage” through the liver, so plasma concentrations of albendazole in unchanged form are negligible and undetectable. Bioavailability when ingested is low. However, simultaneous intake of fatty food significantly increases absorption and concentration of albendazole in blood plasma (by 5 times). Cmax of albendazole sulfoxide is reached in 2-5 hours.

Distribution

Binding to plasma proteins is 70%. Albendazole is well distributed in the body, reaching high concentrations in the urine and bile, liver, wall and fluid of parasitic cysts, cerebrospinal fluid.

Metabolism

Albendazole is rapidly metabolized in the liver to form the primary metabolite, albendazole sulfoxide, which also has anthelminthic activity. Albendazole sulfoxide in turn transforms into albendazole sulfone (secondary metabolite) and other oxidized products with no pharmacological activity.

Albendazole is an inducer of microsomal CYP1A2 enzymes in human liver cells.

Elimation

The T1/2 of albendazole sulfoxide is 8-12 hours. The drug is excreted as various metabolites in the urine and bile, with insignificant renal excretion (less than 1%).

Pharmacokinetics in special clinical cases

The bioavailability of albendazole is increased against the background of liver damage. Cmax of albendazole sulfoxide increases 2-fold and T1/2 is prolonged.

In patients with impaired renal function the clearance of albendazole and its metabolites does not change.

Indications

Active ingredient

Composition

1 tablet contains:

Active substance:

albendazole400 mg;

Associates:

sucrose – 382 mg,

lactose – 200 mg,

sodium benzoate – 1 mg,

sunset yellow dye (sunset yellow dye) – 0.2 mg,

purified water – 0.1 mg,

magnesium stearate – 6 mg,

talc – 10.6 mg,

Peppermint flavoring (essence of peppermint) – 0.008 mg,

menthol (levomenthol) – 0.2 mg.

How to take, the dosage

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

In neurocysticercosis and echinococcosis patients with body weight of 60 kg or more are prescribed 400 mg twice a day, in patients with body weight less than 60 kg – in dose 15 mg/kg/day in 2 doses. The maximum daily dose is 800 mg. The course of treatment in neurocysticercosis is 8-30 days, in echinococcosis – 3 cycles of 28 days with 14 day break between cycles. With surgical treatment the duration of drug treatment is 3 cycles.

When ascariasis, trichocephaliasis, enterobiasis, ankylostomidiasis for adults and children over 3 years old – 400 mg once, if necessary the treatment is repeated in 3 weeks.

In Giardiasis for adults and children over 3 years old – 400 mg once a day for 3 days.

In Strongyloidiasis and cestodiasis for adults and children over 3 years old – 400 mg once a day for 3 days, repeated after 3 weeks if necessary.

The tablets can be chewed or swallowed whole.

Interaction

When used together, dexamethasone, cimetidine, praziquantel increase the blood concentration of albendazole sulfoxide.

Contraindications

With cautions:inhibition of medullary hematopoiesis, hepatic failure, cirrhosis of the liver, cysticercosis with retinal involvement.

Side effects

Disorders of the digestive system:disorders of liver function with changes in liver function tests (mild to moderate increase in transaminase activity), abdominal pain, nausea, vomiting.

With the hematopoietic system:inhibition of medullary hematopoiesis (leukopenia, granulocytopenia, agranulocytosis, thrombocytopenia, pancytopenia).

Nervous system disorders:headache, dizziness, meningeal symptoms.

Allergic reactions:skin rash, itching.

Others:increased body temperature, increased BP, acute renal failure, reversible alopecia.

Similarities