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Albendazole
Pronunciation
U.S. Brand Names
Generic Available
Pharmacological Index
Use
Pregnancy Risk Factor
Pregnancy/Breast-Feeding Implications
Contraindications
Warnings/Precautions
Adverse Reactions
Drug Interactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Monitoring Parameters
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Dosage Forms
References

Pronunciation
(al BEN da zole)

U.S. Brand Names
Albenza®

Generic Available

No


Pharmacological Index

Anthelmintic


Use

Treatment of parenchymal neurocysticercosis and cystic hydatid disease of the liver, lung, and peritoneum; albendazole has activity against Ascaris lumbricoides (roundworm), Ancylostoma duodenale and Necator americanus (hookworms), Enterobius vermicularis (pinworm), Hymenolepis nana and Taenia sp (tapeworms), Opisthorchis sinensis and Opisthorchis viverrini (liver flukes), Strongyloides stercoralis and Trichuris trichiura (whipworm); activity has also been shown against the liver fluke Clonorchis sinensis, Giardia lamblia, Cysticercus cellulosae, Echinococcus granulosus, Echinococcus multilocularis, and Toxocara sp.


Pregnancy Risk Factor

C


Pregnancy/Breast-Feeding Implications

Albendazole has been shown to be teratogenic in laboratory animals and should not be used during pregnancy, if at all possible


Contraindications

Patients with hypersensitivity to albendazole or its components; pregnant women, if possible


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. Corticosteroids should be administered 1-2 days before albendazole therapy in patients with neurocysticercosis to minimize inflammatory reactions and steroid and anticonvulsant therapy should be used concurrently during the first week of therapy for neurocysticercosis to prevent cerebral hypertension. If retinal lesions exist in patients with neurocysticercosis, 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

Dermatologic: Alopecia/rash/urticaria (<1%)

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

Hematologic: Leukopenia (reversible) (<1%); granulocytopenia/agranulocytopenia/pancytopenia (rare)

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

Miscellaneous: Allergic reactions (<1%)


Drug Interactions

May inhibit CYP1A2 enzyme (mild)

Increased effect: Dexamethasone increases plasma levels of albendazole metabolites; praziquantel may increase plasma concentrations of albendazole by 50%; albendazole inhibits hepatic cytochrome P-450 1A and may consequently interact by increasing the concentrations of many drugs which are metabolized by this route; food (especially fatty meals) 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: Oral absorption is poor (<5%); may increase up to 4-5 times when administered with a fatty meal

Distribution: Well distributed inside hydatid cysts; excellent CSF concentrations

Protein binding: 70%

Metabolism: Extensive first-pass metabolism; metabolic pathways include rapid sulfoxidation (major), hydrolysis, and oxidation

Half-life: 8-12 hours

Time to peak serum concentration: 2-2.4 hours

Elimination: Active and inactive metabolites excreted in urine


Usual Dosage

Oral:

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

greater than or equal to 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 with meals (maximum: 800 mg/day) for three 28-day cycles with 14-day drug-free interval in-between

greater than or equal to 60 kg: 400 mg twice daily for 3 cycles as above

Strongyloidiasis/tapeworm:

less than or equal to 2 years: 200 mg/day for 3 days; may repeat in 3 weeks

>2 years and Adults: 400 mg/day for 3 days; may repeat in 3 weeks

Giardiasis: Adults: 400 mg/day for 3 days

Hookworm, pinworm, roundworm:

less than or equal to 2 years: 200 mg as a single dose; may repeat in 3 weeks

>2 years and Adults: 400 mg as a single dose; may repeat in 3 weeks


Dietary Considerations

Administer with a high fatty diet


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


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.


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

Take according to prescribed dosage schedule with meals. You may experience loss of hair (reversible); dizziness or headaches (use caution when driving or engaging in tasks that require alertness until response to drug is known). Report unusual fever, abdominal pain, unresolved 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 be pregnant. Breast-feeding is not recommended.


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.

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


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