162
PART
12 Drugs Used in Tropical Medicine
162  Albendazole
Allyson K. Bloom, Edward T. Ryan
DESCRIPTION
Methyl 5-(propylthio)-2-benzimidazole carbamate.
AVAILABLE PRODUCTS
1. Albendazole 200-mg oral tablets (Albenza, Amedra Pharma-
ceuticals, Horsham, PA) are available in the United States.
2. Albendazole oral tablets are available in other countries under
other names, including Albex, Alzental, Eskazole, Helmidazole,
Parhel, and Zentel.
3. Albendazole 100 or 200 mg per 5 mL suspension is also available
in some countries.
INDICATIONS
1. Treatment of neurocysticercosis caused by Taenia solium.
2. Treatment of hydatid disease caused by Echinococcus spp.
3. Treatment of nematode infection, including those caused by
Ascaris spp., hookworm, Enterobius spp., Trichuris spp., Stron-
gyloides spp., cutaneous and visceral larva migrans, Trichinella
spp., Gnathostoma spp., Capillaria spp., and Gongylonema spp.
(unlabeled).
4. Treatment of giardiasis (unlabeled).
5. Treatment of AIDS-related microsporidiosis (unlabeled).
6. Treatment of infection caused by Clonorchis sinensis and Opis-
thorchis viverrini (unlabeled).
7. Albendazole has also been used for treatment of anisakiasis,
prevention of clinical disease in patients who may have been
exposed to Baylisascaris procyonis, and as second-line or adjunctive
therapy in filariasis (unlabeled).
MODE OF ACTION
The active metabolite of albendazole—albendazole sulfoxide—binds
to and inhibits the polymerization of beta-tubulin. This action
inhibits cytoplasmic microtubule formation and glucose uptake
within the parasite, resulting in immobilization and death of adult
worms. It also prevents parasite eggs from hatching.
PHARMACOKINETICS
Bioavailability of albendazole is poor but is increased when ingested
with food. Absorption can be increased fivefold when albendazole
is ingested with high-fat foods. Albendazole is rapidly converted to
albendazole sulfoxide via first-pass hepatic metabolism, reaching
peak levels 2 to 5 hours after ingestion. Albendazole sulfoxide
is 70% protein bound in plasma and is distributed throughout
tissue, including cerebrospinal fluid. Concentrations in hydatid
cyst fluid are higher than those seen for mebendazole. The mean
half-life is 8 to 12 hours, with excretion probably through the
biliary system. Conversion to albendazole sulfoxide also occurs in
the gut epithelium, where the metabolite is then excreted directly
into the lumen. There is significant intra- and inter-individual
variability.
DOSE ADJUSTMENTS IN RENAL FAILURE
Dose adjustments are likely unnecessary, as urinary excretion of
albendazole and its metabolites are negligible.
DOSE ADJUSTMENTS IN LIVER FAILURE
Close monitoring is recommended if biliary obstruction is present.
DOSE
For adults and children >2 years of age unless otherwise indicated.
Albendazole should be administered with fatty food unless otherwise
noted. Of note, some manufacturers have recommended ingesting
on an empty stomach when targeting certain intra-luminal intestinal
helminths; however, it is thought that the main anti-helminthic
activity of albendazole is due to the primary metabolite produced
after hepatic passage followed by biliary excretion, suggesting that
ingesting with food to increase bioavailability may be preferred.
The manufacturer of the preparation available in the United States
recommends taking with food irrelevant of targeted parasite.
• Treatment of cystic echinococcosis (E. granulosus):
15 mg/kg/day divided twice daily (800 mg maximum daily dose)
with fatty food; duration ranges from a few weeks to a
prolonged course, depending on the clinical course and
indication (often in conjunction with surgical resection/
aspiration, as clinically indicated).
• Treatment of alveolar echinococcosis (E. multilocularis):
15 mg/kg/day divided twice daily (800 mg maximum daily dose)
with fatty food for a prolonged (potentially lifelong) course
(with surgical resection).
• Treatment of neurocysticercosis (with viable cysts) caused by
T. solium:
15 mg/kg/day divided twice daily (800 mg maximum daily dose)
with fatty food for 8 to 30 days, repeated as necessary (with
corticosteroids and antiepileptic therapy; combination
therapy with praziquantel appears more effective if more
than two viable intraparenchymal cysts).
• Treatment of ascariasis and hookworm infection:
400 mg once (more effective for Ancylostoma than Necator;
increased duration to 3 days may improve efficacy).
• Treatment of enterobiasis:
400 mg once, repeated at 2 weeks.
• Treatment of chronic strongyloidiasis (second-line therapy
behind ivermectin):
400 mg twice daily for 7 days.
• Treatment of trichuriasis:
400 mg daily for 3 days (can be given as a single 400-mg dose
when combined with oxantel pamoate, if available).
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