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albendazole (Albenza)
Tradename: Albenza.
Indications:
- treatment of parasitic diseases, including:
a) Hydatid disease caused by Echinococcus granulosus
b) neurocysticercosis
- preferably in combination with corticosteroids
c) pinworms
Contraindications: pregnancy
Dosage:
1) 400 mg PO BID, max 800 mg QD
2) 15 mg/kg/day if < 60 kg
3) duration variable; 2 weeks suggested
4) pinworms: 400 mg PO once [5]
5) hookworms & whipworms: 400 mg PO QD for 3 days [5]
Tabs: 200 mg
Pharmacokinetics:
1) poorly absorbed from GI tract due to low water solubility
-> absorption increased with concurrent oral fat
2) rapidly converted to sulfoxide metabolite before reaching systemic circulation
3) antihelminthic activity is due to primary metabolite albendazole sulfoxide
4) plasma levels of albendazole sulfoxide maximal 2-5 hours after oral dose of albendazole
5) therapeutic plasma levels of 0.46-1.59 ug/mL
6) 70% binding to plasma proteins (albendazole sulfoxide)
7) terminal elimination 1/2life of albendazole sulfoxide is 8-12 hours
8) widely distributed
9) pentrates into CSF
Adverse effects: (less toxic than older benzimidazoles)
1) occasional diarrhea
2) abdominal pain
3) increase in serum transaminases & alkaline phosphatase
4) leukopenia
5) granulocytopenia
6) thrombocytopenia
7) seizures
8) hydrocephalus
9) alopecia
Drug interactions:
- cimetidine decreases elimination & increases concentration of albendazole
Mechanism of action:
1) binds to free B-tubulin in parasite cells
2) inhibits parasite microtubule polymerization
Interactions
drug interactions
General
antihelmintic
benzimidazole
Properties
MISC-INFO: elimination route LIVER
1/2life 8-12 HOURS
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM cid=2082
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996.
- Harrison's Principles of Internal Medicine, 14th ed.
Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 1171
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Physician's Desk Reference (PDR) 52nd edition, Medical
Economics, 1998
- Prescriber's Letter 19(3): 2012
Alternatives to Vermox for Treatment of Intestinal Worms
Detail-Document#: 280308
(subscription needed) http://www.prescribersletter.com