Albendazole
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
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.
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)
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