- Tablets 200 mg
Inhibitory effect on tubulin polymerization, resulting in loss of cytoplasmic microtubules.
Albendazole is poorly absorbed from the GI tract; however, it is rapidly converted to its primary active metabolite, albendazole sulfoxide, prior to reaching systemic circulation. Fatty meals enhance bioavailability, as indicated by up to a 5-fold increase in plasma concentration in albendazole sulfoxide. Albendazole sulfoxide plasma concentrations are dose-dependent. C max is achieved in 2 to 5 h and ranges from 0.46 to 1.58 mcg/mL, when given with a fatty meal.
Albendazole sulfoxide is 70% protein bound and widely distributed throughout the body.
After metabolism in the liver to albendazole sulfoxide, it is further metabolized to albendazole sulfone and other oxidative metabolites.
Albendazole sulfoxide elimination half-life is 8 to 12 h. Biliary elimination of albendazole sulfoxide results in biliary concentrations similar to plasma concentration. Urinary excretion is a minor elimination pathway (less than 1%).
Special PopulationsRenal Function Impairment
Pharmacokinetics have not been studied in patients with renal impairment, but it is unlikely that clearance of albendazole and albendazole sulfoxide would be affected, given the negligible renal elimination.Hepatic Function Impairment
Systemic availability of albendazole sulfoxide is increased in patients with extrahepatic obstruction.Elderly
Data suggest pharmacokinetics are similar to those in younger, healthy subjects.Children
Albendazole sulfoxide pharmacokinetics are similar to those observed in adults.
Indications and Usage
Treatment of parenchymal neurocysticercosis due to active lesions caused by larval forms of pork tapeworm, Taenia solium ; treatment of cystic hydatid disease of the liver, lung, and peritoneum caused by larval forms of dog tapeworm, Echinococcus granulosus .
For the treatment of single and mixed intestinal nematode infections, including ascariasis, enterobiasis, hookworm, strongyloidiasis, trichuriasis, capillariasis, gnathostomiasis, trichostrongyliasis, tissue nematode infections, cutaneous larva migrans, toxocariasis, ancylostoma caninum, gongylonemiasis, and trichinosis; in combination with other anthelmintics in the management of the filarial nematode infection lymphatic filariasis; for microsporidial intestinal infections in patients with AIDS.
Hypersensitivity to benzimidazole compounds or any component of the product.
Dosage and AdministrationHydatid Disease
Adults and Children
PO For patients weighing 60 kg or more, 400 mg twice daily with meals for a 28-day cycle followed by a 14-day albendazole-free interval, for a total of 3 cycles. For patients weighing less than 60 kg, 15 mg/kg/day in divided doses twice daily with meals (max, 800 mg/day) for a 28-day cycle followed by a 14-day albendazole-free interval, for a total of 3 cycles. In the presurgical or postsurgical setting, optimal killing of cyst contents is achieved with 3 courses of therapy.Neurocysticercosis
Adults and Children
PO For patients weighing 60 kg or more, 400 mg twice daily with meals for 8 to 30 days. For patients weighing less than 60 kg, 15 mg/kg/day in divided doses twice daily with meals (max, 800 mg/day) for 8 to 30 days.
- Albendazole should be taken with food.
- If difficulty swallowing the tablets occurs, tablets may be crushed or chewed with a little water.
- Patients being treated for neurocysticercosis should receive appropriate steroid and anticonvulsant therapy as required. Oral or IV corticosteroids should be considered to prevent cerebral hypertensive episodes during the first week of treatment.
Store between 68° and 77°F.
In patients with hydatid cyst, albendazole sulfoxide concentrations in bile and cystic fluid may be increased about 2-fold; however, plasma levels are unchanged 4 h after dosing.Dexamethasone
Albendazole C trough at steady state was about 56% higher when coadministered with dexamethasone 8 mg. Monitor the patient for albendazole adverse reactions. If an interaction is suspected, adjust the albendazole dose as needed.Grapefruit juice
Albendazole plasma concentrations may be elevated and the half-life may be shortened, increasing the risk of adverse reactions. Patients should avoid grapefruit products while taking albendazole.Praziquantel
Albendazole sulfoxide C max may be elevated about 50%, increasing the risk of adverse reactions. Monitor the patient for albendazole adverse reactions. If an interaction is suspected, adjust the albendazole dose as needed.Theophylline
Although theophylline pharmacokinetics are unchanged by albendazole, monitor theophylline plasma concentrations during and after albendazole treatment. Adjust the theophylline dose as needed.
Headache (11%); raised intracranial pressure (2%); dizziness/vertigo, meningeal signs (1%).
Reversible alopecia (2%); erythema multiforme, Stevens-Johnson syndrome (postmarketing).
Abdominal pain, nausea/vomiting (6%).
Abnormal LFTs (16%); acute liver failure, hepatitis (postmarketing).
Agranulocytosis, granulocytopenia, leukopenia, pancytopenia, thrombocytopenia (less than 1%); aplastic anemia, bone marrow suppression, neutropenia (postmarketing).
Fever (1%); acute renal failure (postmarketing).
Monitor CBCs and liver function (transaminases) at the beginning of each 28-day cycle of therapy and every 2 wk while on therapy. Discontinue therapy if liver enzymes are significantly increased. Treatment can be resumed when hepatic enzymes have returned to pretreatment levels, but perform lab tests frequently during repeat therapy.
Category C .
Experience in children younger than 6 y of age is limited.
Patients with abnormal LFTs are at increased risk for hepatotoxicity and bone marrow suppression.
May cause occasional (less than 1%) reversible reductions in total white blood cell count. More significant reductions, including agranulocytosis, granulocytopenia, or pancytopenia, have been rarely reported. Rare deaths due to granulocytopenia or pancytopenia have also been reported. Agranulocytosis, aplastic anemia, and bone marrow suppression have been reported in patients with and without underlying hepatic dysfunction.
Mild to moderate elevations of hepatic enzymes may occur; these elevations generally return to normal upon discontinuation of albendazole. Cases of acute liver failure and hepatitis have also been reported.
Preexisting neurocysticercosis may also be uncovered in patients treated with albendazole for other conditions. Patients may experience neurological symptoms (eg, seizures, increased IOP) as a result of an inflammatory reaction caused by death of the parasite within the brain. Cysticercosis may rarely involve the retina. Patients should be examined for retinal lesions prior to initiation of treatment for neurocysticercosis. If lesions are present, weigh the need of anticysticercal therapy against the possibility of retinal damage caused by albendazole-induced changes to the retinal lesion.
No untoward effects have been reported with doses of 16 g or more over 12 h.
- Instruct patient to take with food; inform patient that the tablets may be crushed or chewed and swallowed with a drink of water if they are unable to swallow the tablets whole.
- Advise women that drug may cause fetal harm and to begin therapy after a negative pregnancy test has been obtained.
- Caution women of childbearing age to avoid becoming pregnant while on this drug or within 1 mo of completing treatment.
- Advise patient to contact health care provider immediately if pregnancy occurs while taking this drug.
- Advise patients that routine (every 2 wk) monitoring of CBCs and LFTs will take place during therapy.
Copyright © 2009 Wolters Kluwer Health.
More about albendazole
- Other brands: Albenza