Albendazole

Albendazole is a synthetic nitroimidazole with wide spectrum coverage as an antiparasitic drug.

Bioavailability of albendazole  is poor, but is increased when ingested with food, particularly high-fat foods.

Albendazole is rapidly converted to albendazole sulfoxide via first pass hepatic metabolism, peaking levels 2–5 hours after ingestion.

Conversion to albendazole sulfoxide also occurs in the gut, where it is then excreted directly into the lumen

Albendazole sulfoxide is 70% protein bound in plasma and is widely distributed throughout the body; it has been detected in urine, bile, liver, cyst wall, cyst fluid, and cerebral spinal fluid (CSF).

The mean half-life is 8–12 hours depending on the dose, with excretion probably through the biliary system.

Following oral administration, albendazole has not been detected in human urine.

Urinary excretion of albendazole sulfoxide is a minor elimination pathway with less than 1% of the dose recovered in the urine.

Significant toxicity and mortality were shown in male and female mice at doses exceeding 5,000 mg/kg; in rats, at estimated doses between 1,300 and 2,400 mg/kg.
With high-dose or prolonged therapy, elevated levels of hepatic enzymes, dizziness, neutropenia, and alopecia are most common.

Serum hepatic enzyme levels and the blood count should be monitored after overdose

In case of overdosage, symptomatic therapy and general supportive measures are recommended

Since food increases systemic absorption of albendazole, an overdosed patient should have nil by mouth.

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