OXYZOL

A benzimidazole broad-spectrum anthelmintic structurally related to mebendazole that is effective against many diseases. (From Martindale, The Extra Pharmacopoeia, 30th ed, p38).

For the treatment of parenchymal neurocysticercosis due to active lesions caused by larval forms of the pork tapeworm, Taenia solium and for the treatment of cystic hydatid disease of the liver, lung, and peritoneum, caused by the larval form of the dog tapeworm, Echinococcus granulosus.

Albendazole is a broad-spectrum anthelmintic.

The principal mode of action for albendazole is by its inhibitory effect on tubulin polymerization which results in the loss of cytoplasmic microtubules.

Poorly absorbed from the gastrointestinal tract due to its low aqueous solubility.

Oral bioavailability appears to be enhanced when coadministered with a fatty meal (estimated fat content 40 g).

Rapidly converted in the liver to the primary metabolite, albendazole sulfoxide, which is further metabolized to albendazole sulfone and other primary oxidative metabolites that have been identified in human urine.

Hover over products below to view reaction partners Albendazole albendazole sulfone albendazole sulfoxide.

Albendazole is rapidly converted in the liver to the primary metabolite, albendazole sulfoxide, which is further metabolized to albendazole sulfone and other primary oxidative metabolites that have been identified in human urine.

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

Biliary elimination presumably accounts for a portion of the elimination as evidenced by biliary concentrations of albendazole sulfoxide similar to those achieved in plasma.

Terminal elimination half-life ranges from 8-12 hours (single dose, 400 mg).

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Symptoms of overdose include elevated liver enzymes, headaches, hair loss, low levels of white blood cells (neutropenia), fever, and itching.

Albendazole is contraindicated in patients with known hypersensitivity to the benzimidazole class of compounds or any components of albendazole.

Patients with known hypersensitivity to the benzimidazole class of compounds or any components of albendazole.

Patients weighing 60 kg or greater, 400 mg twice daily; less than 60 kg, 15 mg/kg/day in divided doses twice daily (maximum total daily dose 800 mg).

Albendazole tablets should be taken with food.

Hydatid disease: 28-day cycle followed by 14-day albendazole-free interval for a total of 3 cycles.

Neurocysticercosis: 8 to 30 days.

See additional important information in the Full Prescribing Information. 2.1 Dosage Dosing of albendazole will vary depending upon the indication.

Albendazole tablets may be crushed or chewed and swallowed with a drink of water.

Table 1: Albendazole Dosage Indication Patient Weight Dose Duration Hydatid Disease 60 kg or greater 400 mg twice daily, with meals 28-day cycle followed by a 14-day albendazole-free interval, for a total of 3 cycles Less than 60 kg 15 mg/kg/day given in divided doses twice daily with meals (maximum total daily dose 800 mg) Neurocysticercosis 60 kg or greater 400 mg twice daily, with meals to 30 days Less than 60 kg 15 mg/kg/day given in divided doses twice daily with meals (maximum total daily dose 800 mg) 2.2 Concomitant Medication to Avoid Adverse Reactions Patients being treated for neurocysticercosis should receive appropriate steroid and anticonvulsant therapy as required.

Oral or intravenous corticosteroids should be considered to prevent cerebral hypertensive episodes during the first week of treatment. 2.3 Monitoring for Safety Before and During Treatment Monitor blood counts at the beginning of each 28-day cycle of therapy, and every 2 weeks while on therapy with albendazole in all patients.

Monitor liver enzymes (transaminases) at the beginning of each 28-day cycle of therapy, and at least every 2 weeks during treatment with albendazole in all patients.

Obtain a pregnancy test in women of reproductive potential prior to therapy.

Each white to off-white, circular, biconvex, bevel-edged film coated, TILTAB tablet is debossed with “ap” and “550” and contains 200 mg of albendazole.

Bottles of 2 Tablets NDC 0115-1701-49 16.2 Storage and Handling Store at 20° to 25°C (68° to 77°F) .

Store at 20° to 25°C (68° to 77°F) .

There are limited data on use of albendazole in pregnant women to inform a drug-associated risk of major birth defects and miscarriage.

In published studies, single-dose albendazole exposure during pregnancy did not show evidence of an increased risk of adverse maternal or fetal outcomes; however, this finding cannot be extrapolated to multiple-dose exposures.

In animal reproductive studies, oral administration of albendazole during gestation caused embryotoxicity and skeletal malformations in pregnant rats (at oral doses of 0.10 times and 0.32 times the recommended human dose based on body surface area in mg/m 2 ) and pregnant rabbits (at oral doses of 0.60 times the recommended human dose based on body surface area in mg/m 2 ).

Albendazole was also associated with maternal toxicity in rabbits (at doses of 0.60 times the recommended human dose based on body surface area in mg/m 2 ) .

Albendazole should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Albendazole should not be used in pregnant women except in clinical circumstances where no alternative management is appropriate.

If a patient becomes pregnant while taking this drug, albendazole should be discontinued immediately.

If pregnancy occurs while taking this drug, the patient should be apprised of the potential hazard to the fetus.

The estimated background risk of major birth defects and miscarriage for the indicated population is unknown.

In the

U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is to 4% and to 20%, respectively.

Cochrane review could not provide sufficient evidence of the impact of antihelminthics (including albendazole) on the pregnancy outcomes of low birthweight, perinatal mortality and preterm birth.

In a large trial of about 2507 women, albendazole use during the second or third trimester of pregnancy had no overall effect on birth weight, perinatal mortality, or congenital anomalies.

With a limited sample size and single-does exposure, another study could not rule out a two-fold increased risk of major malformations [4.7% vs. 2.2%; OR 2.2 (95% confidence interval (CI) 0.5 to 10.1); p = 0.26.

Albendazole has been shown to be teratogenic (to cause embryotoxicity and skeletal malformations) in pregnant rats and rabbits.

The teratogenic response in the rat was shown at oral doses of and 30 mg/kg/day (0.10 times and 0.32 times the recommended human dose based on body surface area in mg/m 2, respectively) during gestation days to 15 and in pregnant rabbits at oral doses of 30 mg/kg/day (0.60 times the recommended human dose based on body surface area in mg/m 2 ) administered during gestation days to 19.

In the rabbit study, maternal toxicity (33% mortality) was noted at 30 mg/kg/day. In mice, no teratogenic effects were observed at oral doses up to 30 mg/kg/day (0.16 times the recommended human dose based on body surface area in mg/m 2 ), administered during gestation days to 15.

Females and Males of Reproductive Potential Pregnancy Testing Obtain pregnancy test prior to prescribing albendazole to women of reproductive potential.

Advise women of reproductive potential to use effective birth control for the duration of albendazole therapy and for one month after end of therapy.

Hydatid disease is uncommon in infants and young children.

In neurocysticercosis, the efficacy of albendazole in children appears to be similar to that in adults.

In patients aged and older with either hydatid disease or neurocysticercosis, there was insufficient data to determine whether the safety and effectiveness of albendazole is different from that of younger patients.