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Pronunciation:

(al BEN da zole)

U.S. Brand Names:

Albenza®

Generic Available:

No

Use:

Treatment of parenchymal neurocysticercosis caused by Taenia solium and cystic hydatid disease of the liver, lung, and peritoneum caused by Echinococcus granulosus

Use - Unlabeled/Investigational:

Albendazole has activity against Ascaris lumbricoides (roundworm); Ancylostoma caninum; Ancylostoma duodenale and Necator americanus (hookworms); cutaneous larva migrans; Enterobius vermicularis (pinworm); Gnathostoma spinigerum; Gongylonema sp; Hymenolepis nana sp (tapeworms); Mansonella perstans (filariasis); Opisthorchis sinensis and Opisthorchis viverrini (liver flukes); Strongyloides stercoralis and Trichuris trichiura (whipworm); visceral larva migrans (toxocariasis); activity has also been shown against the liver fluke Clonorchis sinensis, Giardia lamblia, Cysticercus cellulosae, and Echinococcus multilocularis. Albendazole has also been used for the treatment of intestinal microsporidiosis (Encephalitozoon intestinalis), disseminated microsporidiosis (E. hellem, E. cuniculi, E. intestinalis, Pleistophora sp, Trachipleistophora sp, Brachiola vesicularum), and ocular microsporidiosis (E. hellem, E. cuniculi, Vittaforma corneae).

Pregnancy Risk Factor:

C

Pregnancy Implications:

Albendazole has been shown to be teratogenic in laboratory animals and should not be used during pregnancy, if at all possible. Women should be advised to avoid pregnancy for at least 1 month following therapy. Discontinue if pregnancy occurs during treatment.

Lactation:

Excretion in breast milk unknown/not recommended

Contraindications:

Hypersensitivity to albendazole or any component of the formulation

Warnings/Precautions:

Discontinue therapy if LFT elevations are significant; may restart treatment when decreased to pretreatment values. Becoming pregnant within 1 month following therapy is not advised.

Neurocysticercosis: Corticosteroids should be administered 1-2 days before albendazole therapy to minimize inflammatory reactions. Steroid and anticonvulsant therapy should be used concurrently during the first week of therapy to prevent cerebral hypertension. If retinal lesions exist, weigh risk of further retinal damage due to albendazole-induced changes to the retinal lesion vs benefit of disease treatment.

Adverse Reactions:

N = Neurocysticercosis; H = Hydatid disease

>10%:

Central nervous system: Headache (11% - N; 1% - H)

Hepatic: LFTs Increased (~15% - H; <1% - N)

1% to 10%:

Central nervous system: Dizziness, vertigo, fever (1%); intracranial pressure increased (1% - N), meningeal signs (1% - N)

Dermatologic: Alopecia (2% - H; <1% - N)

Gastrointestinal: Abdominal pain (6% - H; 0% - N); nausea/vomiting (3% to 6%)

Hematologic: Leukopenia (reversible) (<1%)

Miscellaneous: Allergic reactions (<1%)

<1%: Acute renal failure, agranulocytopenia, allergic reaction, granulocytopenia, pancytopenia, rash, thrombocytopenia, urticaria

Drug Interactions:

Substrate (minor) of CYP1A2, 3A4; Inhibits CYP1A2 (weak)

Ethanol/Nutrition/Herb Interactions:

Food: Albendazole serum levels may be increased if taken with a fatty meal (increases the oral bioavailability by 4-5 times).

Mechanism of Action:

Active metabolite, albendazole, causes selective degeneration of cytoplasmic microtubules in intestinal and tegmental cells of intestinal helminths and larvae; glycogen is depleted, glucose uptake and cholinesterase secretion are impaired, and desecratory substances accumulate intracellulary. ATP production decreases causing energy depletion, immobilization, and worm death.

Pharmacodynamics/Kinetics:

Absorption: <5%; may increase up to 4-5 times when administered with a fatty meal

Distribution: Well inside hydatid cysts and CSF

Protein binding: 70%

Metabolism: Hepatic; extensive first-pass effect; pathways include rapid sulfoxidation (major), hydrolysis, and oxidation

Half-life elimination: 8-12 hours

Time to peak, serum: 2-2.4 hours

Excretion: Urine (<1% as active metabolite); feces

Dosage:

Oral:

Children:

Cysticercus cellulosae (unlabeled use): 15 mg/kg/day (maximum: 800 mg/day) in 2 divided doses for 8-30 days; may be repeated as necessary

Echinococcus granulosus (tapeworm) (unlabeled use): 15 mg/kg/day (maximum: 800 mg) divided twice daily for 1-6 months

Children and Adults:

Neurocysticercosis:

<60 kg: 15 mg/kg/day in 2 divided doses (maximum: 800 mg/day) for 8-30 days

60 kg: 400 mg twice daily for 8-30 days

Note: Give concurrent anticonvulsant and steroid therapy during first week.

Hydatid:

<60 kg: 15 mg/kg/day in 2 divided doses (maximum: 800 mg/day)

60 kg: 400 mg twice daily

Note: Administer dose for three 28-day cycles with a 14-day drug-free interval in between.

Ancylostoma caninum, Ascaris lumbricoides (roundworm), Ancylostoma duodenale, and Necator americanus (hookworms) (unlabeled use): 400 mg as a single dose

Clonorchis sinensis (Chinese liver fluke) (unlabeled use): 10 mg/kg for 7 days

Cutaneous larva migrans (unlabeled use): 400 mg once daily for 3 days

Enterobius vermicularis (pinworm) (unlabeled use): 400 mg as a single dose; may repeat in 2 weeks

Gnathostoma spinigerum (unlabeled use): 400 mg twice daily for 21 days

Gongylonemiasis (unlabeled use): 10 mg/kg/day for 3 days

Mansonella perstans (unlabeled use): 400 mg twice daily for 10 days

Visceral larva migrans (toxocariasis) (unlabeled use): 400 mg twice daily for 5 days

Adults:

Cysticercus cellulosae (unlabeled use): 400 mg twice daily for 8-30 days; may be repeated as necessary

Disseminated microsporidiosis (unlabeled use): 400 mg twice daily

Echinococcus granulosus (tapeworm) (unlabeled use): 400 mg twice daily for 1-6 months

Intestinal microsporidiosis (unlabeled use): 400 mg twice daily for 21 days

Ocular microsporidiosis (unlabeled use): 400 mg twice daily, in combination with fumagillin

Administration:

Administer with meals; administer anticonvulsant and steroid therapy during first week of neurocysticercosis therapy

Monitoring Parameters:

Monitor fecal specimens for ova and parasites for 3 weeks after treatment; if positive, retreat; monitor LFTs, and clinical signs of hepatotoxicity; CBC at start of each 28-day cycle and every 2 weeks during therapy

Dietary Considerations:

Should be taken with a high-fat meal.

Patient Education:

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. Take as directed, with meals. Follow prescriber's suggestions to prevent reinfection. May cause loss of hair (reversible); nausea or vomiting (small, frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help); or dizziness or headaches (use caution when driving or engaging in tasks that require alertness until response to drug is known). Report unusual fever, persistent or unresolved abdominal pain, vomiting, yellowing of skin or eyes, darkening of urine, or light colored stools. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Breast-feeding is not recommended.

Dental Health: Effects on Dental Treatment:

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

No information available to require special precautions

Mental Health: Effects on Mental Status:

None reported

Mental Health: Effects on Psychiatric Treatment:

May rarely cause bone marrow suppression; use caution with clozapine and carbamazepine. Carbamazepine may increase the metabolism of albendazole.

Dosage Forms:

Tablet: 200 mg

International Brand Names:

Abentel® (BD, TH); Adazol® (EC); Alba® (BD); Albatel® (TH); Alben® (BD, BR, TH); Albenda® (TH); Albendazol® (BR, EC); Albendazol Genfar® (EC); Albendazol MK® (CO); Albenzol® (EC); Albezole® (IN); Albizol® (BD); Alda® (TH); Alentin® (BD); Alfuca® (TH); Alin® (BR); Almex® (BD); Alphin® (BD); Alzed® (BD); Alzental® (SG); Analon Galeno® (CO); Andazol® (TR); Anthel® (TH); Apardu-6® (DO); Asen® (BD); Avadyl® (DO); Avir® (EC); Azol® (BD); Ben-A® (BD); Bendapar® (MX); Bendex-400® (ZA); Bentel® (BD); Bentiamin® (BR); Bimenal® (YU); Ceprazol® (CL); Chuben® (BD); Ciclopar® (CO); Dalben® (HR, SI); Digezanol® (MX); Duador® (RO); Emanthal® (IN); Endoplus® (MX); Eskazole® (AT, AU, DE, ES, IL, MX, NL, RO); Estazol® (BD); Ethizol® (DO); Fagol® (EC); Gascop® (MX); Gendazel® (TH); Getzol® (CO); Helben® (ID); Imavermil® (BR); Italbenzol® (EC); Labenda® (TH); Leo (TH); Librabendazol® (EC); Lurdex® (MX); Mebel® (BD); Mebenix® (BR); Mesin® (TH); Monodox® (CO); Monozol® (BR); Mycotel® (TH); Nemozole® (IN); Obedozol® (CO); Parasin® (BR); Reben® (BD); Rotopar® (EC, HN, PA, SV); Sintel® (BD); Triben® (BD); Unizol® (DO); Vastus® (AR); Vermid® (BD); Vermigen® (EC); Vermital® (BR); Vermixide® (TH); Vermoil® (CL); Xadem® (CO); Zeben® (TH); Zentel® (AU, BR, CH, CL, CO, CR, CY, DO, EC, EG, FR, GT, HN, IN, IT, JO, KW, LB, MT, MX, PA, PL, PT, RO, SG, SV, SY, TH, ZA); Zenzera® (TH); Zestaval® (CY); Zoben® (BD); Zolben® (BR)

References

de Silva N, Guyatt H, and Bundy D, "Anthelmintics. A Comparative Review of Their Clinical Pharmacology,"Drugs, 1997, 53(5):769-88.

Liu LX and Weller PF, "Antiparasitic Drugs,"N Engl J Med, 1996, 334(18):1178-84.

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