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DRUG RECORD

 

ALBENDAZOLE

OVERVIEW
Albendazole

 

Introduction

Albendazole is an antihelmintic agent used predominantly in treatment of echinococcosis, a parasitic worm that causes cysts in liver and lung.  Albendazole therapy is commonly associated with mild and transient serum enzyme elevations and rarely can lead to clinically apparent acute liver injury.

 

Background

Albendazole (al ben' da zole0 is a benzimidazole antihelmintic agent similar in structure and mechanism of action to thiabendazole and mebendazole.  The benzimidazoles act by selective binding to beta-tubulin of parasitic worms, causing their immobilization and death.  Albendazole has proven efficacy against several parasitic worms and was approved for use in the United States in 1996.  Currently indications for albendazole include echnicoccosis, cysticercosis and strongyloidiasis against which it is more effective than mebendazole (largely because it is better absorbed).  Albendazole is also used for hookworm, whipworm and pinworm infestations.  Albendazole is available in tablets of 200 mg under the trade name of Albenza.  The dose and duration of albendazole therpay varies by indication, being a single dose of 400 mg orally for minor infestations (which can be repeated a few weeks later), and 400 mg twice daily for 1 to 2 weeks or for up to 6 months for more serious systemic infections.  Albendazole is generally well tolerated; side effects include gastrointestinal upset, headaches and hair loss.

 

Hepatotoxicity

Albendazole therapy has been associated with transient and asymptomatic elevations in serum aminotransferase levels in up to 50% of patients treated for more than a few weeks.  These abnormalities rapidly improve with stopping therapy which is rarely required (~4%).  Albendazole has also been associated with rare instances of clinically apparent liver injury.  The onset of injury has been within a few days to as long as 2 months of starting therapy or more rapidly with multiple courses of treatment.  The injury can also arise 1 to 2 weeks after a short course of albdenazole (1-3 days).  The pattern of serum enzyme elevations is typically hepatocellular or mixed.  Allergic features (rash, fever, eosinophilia) may be present but are not prominent.  Most cases have been mild and recovery rapid once the drug is stopped.  Rapid recurrence with rechallenge has been reported.

 

Mechanism of Injury

Albendazole acts by binding tubulin in parasitic worms which it does with greater avidity than the tubulin in mammalian cells, but some of the toxicity of the benzimidazoles may be related to this tubulin-binding activity.  In most instances of clinically apparent liver injury, hypersensitivity appears to be the cause.

 

Outcome and Management

Albendazole is usually well tolerated and the liver injury reported with its use has been mild and self-limited in course.  Patients with acute liver injury attributed to albendazole should avoid repeat exposure.  Albendazole has not been associated with acute liver failure or chronic liver injury.  It is unknown whether there is cross sensitivity with other benzimidazoles (such as mebendazole), but there probably is and switching to another class of antihelmintic agents is appropriate if therapy is still needed.

 

Drug Class:  Antihelmintic Agents

 

 

 

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PRODUCT INFORMATION
Albendazole

 

REPRESENTATIVE TRADE NAMES
Albendazole – Albenza®

 

 

DRUG CLASS
Antihelmintic Agents

 

COMPLETE LABELING

Product labeling at DailyMed, National Library of Medicine, NIH


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DRUG CAS REGISTRY NUMBER MOLECULAR FORMULA STRUCTURE
Albendazole 54965-21-8 C12-H15-N3-O2-S Albendazole Chemical Structure

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REFERENCES
Albendazole

 

References Last Updated: 06 August 2013

 

  1. Zimmerman HJ. Antihelminthics. Hepatic injury from antimicrobial agents. In, Zimmerman HJ. Hepatotoxicity: the adverse effects of drugs and other chemicals on the liver. 2nd ed. Philadelphia: Lippincott, 1999, pp. 626-8.  (Expert review of hepatotoxicity of antihelmintics written in 1999; albendazole is associated with serum aminotransferase elevations in 20% of patients and has been linked to rare instances of acute liver injury).

  2. McCarthy J, Loukas A, Hotez PJ. Chemotherapy of helminth infections. In, Brunton LL, Chabner BA, Knollman BC, eds. Goodman & Gilman’s the pharmacological basis of therapeutics. 12th ed. New York: McGraw-Hill, 2011, pp. 1443-61.  (Textbook of pharmacology and therapeutics).

  3. Morris DL, Smith PG. Albendazole in hydatid disease—hepatocellular toxicity. Trans R Soc Trop Med Hyg 1987; 81: 343-4. PubMed Citation  (Among 40 patients treated for echinococcosis, 6 had ALT elevations [62-970 U/L, Alk P ~360 U/L] and 1 jaundice [bilirubin 5.7 mg/dL], with rapid resolution on stopping; 2 had positive rechallenge).

  4. Choudhuri G, Prasad RN. Jaundice due to albendazole. Indian J Gastroenterol 1988; 7: 245-6. PubMed Citation  (30 year old man with echinococcal cyst developed jaundice 2.5 months after starting albenazole [bilirubin 5.6 mg/dL, ALT 320 U/L, Alk P 1.8 times ULN], resolving within 10 days of stopping; positive rechallenge with appearance of jaundice within two days).

  5. Jagota SC. Jaundice due to albendazole. Indian J Gastroenterol 1989; 8: 58. PubMed Citation  (Letter in response to Choudhuri and Prasad recommending limiting dose of albendazole to 400 mg twice daily in cycles of 28 days. Reply by authors stresses the elements of hypersensitivity in the case report).

  6. el-Mufti M, Kamag A, Ibrahim H, Taktuk S, Swaisi I, Zaidan A, Sameen A, et al. Albendazole therapy of hydatid disease: 2-year follow-up of 40 cases. Ann Trop Med Parasitol 1993; 87: 241-6. PubMed Citation  (Among 40 Egyptian patients with echinococcal cysts treated with albendazole [usually in three 28 day cycles], hepatotoxicity arose in 2 patients [5%], both resolving on discontinuation; details not given, but Alk P said to be unreliable as a marker of liver injury because it is often raised before therapy).

  7. Gil-Grande LA, Rodriguez-Cabeiro F, Prieto JG, Sanchez-Ruano JJ, Brasa C, Agular L, Garcia-Hoz F, et al. Randomised controlled trial of efficacy of albendazole in intra-abdominal hydatid disease. Lancet 1983; 342: 1269-72. PubMed Citation  (Among 43 patients treated with albendazole [10 mg/kg/day] for 10-111 days, 27 had ALT elevations during therapy, which were > twice ULN in 21 and >200 U/L in 4; liver biopsies showed “toxic hepatitis” and changes correlated with higher drug levels in liver; no jaundice or clinically apparent injury and all resolved).

  8. Klion AD, Massougbodji A, Horton J, Ekoué S, Lanmasso T, Ahouissou NL, Nutman TB. Albendazole in human loiasis: results of a double-blind, placebo-controlled trial. J Infect Dis 1993; 168: 202-6. PubMed Citation  (23 patients with loiasis were treated with albendazole [n=11: 200 mg twice daily] or placebo [n=12] for 21 days; none developed ALT elevations or evidence of liver injury).

  9. Misra PK, Kumar A, Agarwal V, Jagota SC. A comparative clinical trial of albendazole versus metronidazole in children with giardiasis. Indian Pediatr 1995; 32: 779-82. PubMed Citation  (Randomized trial of albendazole [400 mg/day for 5 days] vs metronidazole [7.5 mg/kg thrice daily for 5 days] in 64 children with giardiasis; all children were cured and side effects were similar, no differences in biochemical test results).

  10. Horton RJ. Albendazole in treatment of human cystic echinococcosis: 12 years of experience. Acta Trop 1997; 64: 79-93. PubMed Citation  (Current dose of albendazole for therapy of echinococosis is 800 mg daily for ~3 months; serum enzyme elevations occurred in 10-20% of patients, requiring discontinuation in 4%, all cases were reversible, some possibly due to underlying liver cyst disease).

  11. Molina JM, Chastang C, Goguel J, Michiels JF, Sarfati C, Desportes-Livage I, Horton J, et al. Albendazole for treatment and prophylaxis of microsporidiosis due to Encephalitozoon intestinalis in patients with AIDS: a randomized double-blind controlled trial. J Infect Dis 1998; 177: 1373-7. PubMed Citation  (Controlled trial of albendazole vs placebo in 8 patients with HIV and E. intestinalis infection; ALT elevations occurred in 1 patient in each group).

  12. Inkatanuvat S, Suntharasamai P, Vutikes S, Riganti M. Changes of liver functions after albendazole treatment in human gnathostomiasis. J Med Assoc Thai 1998; 81: 735-40. PubMed Citation  (98 patients with “gnathostomiasis” were given albendazole [800 mg daily] for 14 days; ALT elevations were present in 44% at day 14, 18% at day 28, peak values of 482 U/L, but all were asymptomatic and most returned to normal by 6 months).

  13. Dunyo SK, Nkrumah FK, Simonsen PE. A randomized double-blind placebo-controlled field trial of ivermectin and albendazole alone and in combination for the treatment of lymphatic filariasis in Ghana. Trans R Soc Trop Med Hyg 2000; 94: 205-11. PubMed Citation  (Placebo controlled trial of single dose of albendazole, ivermectin or the combination of both in 1425 persons from filariasis-endemic villages; albendazole therapy was associated with a modest but delayed reduction in microfilarial levels; side effects were mild and self-limited and not different from placebo; no mention of jaundice or hepatitis).

  14. Shenoy RK, Suma TK, John A, Arun SR, Kumaraswami V, Fleckenstein LL, Na-Bangchang K. The pharmacokinetics, safety and tolerability of the co-administration of diethylcarbamazine and albendazole. Ann Trop Med Parasitol 2002; 96: 603-14. PubMed Citation  (Pharmacokinetic studies of single oral doses of diethylcarbamazine and albendazole reported no drug-drug interactions and no adverse events).

  15. Matthaiou DK, Panos G, Adamidi ES, Falagas ME. Albendazole versus praziquantel in the treatment of neurocysticercosis: a meta-analysis of comparative trials. PLoS Negl Trop Dis 2008; 2: e194. PubMed Citation  (Systematic review of efficacy of albendazole versus praziquantel; no differences in rates of adverse events, but no details given).

  16. Keiser J, Utzinger J. Efficacy of current drugs against soil-transmitted helminth infections: systematic review and meta-analysis. JAMA 2008; 299: 1937-48. PubMed Citation  (Systematic review of efficacy and safety of albendazole, mebendazole and pyrantel pamoate as therapy of A. Lumbricoides, hookworm and T. Tichiura; albendazole was well tolerated in most studies, no significant adverse events were reported).

  17. Choi GY, Yang HW, Cho SH, Kang DW, Go H, Lee WC, Lee YJ, et al. Acute drug-induced hepatitis caused by albendazole. J Korean Med Sci 2008; 23: 903-5. PubMed Citation  (47 year old man developed fever and rash 2 days after single dose of albendazole and 2 days later was jaundiced [bilirubin 2.8 mg/dL, ALT 4,622 U/L, Alk P 40 U/L, INR 1.44]; rapid recovery).

  18. Jevtić M, Mikić D, Arsić-Komljenović G, Stanković N, Ristanović E, Sjenicić G, Janićijević-Hudomal S. [Adverse effects of longterm, continual administration of high doses of albendazole in the treatment of echinococcal disease]. Vojnosanit Pregl 2008; 65: 539-44. Serbian. PubMed Citation  (Among 42 patients with echinococcosis treated wtih albendazole for 4 to 6 months, ALT elevations occurred in 36% and led to discontinuation in 7%, subsequently resolving in all).

  19. Mikić D, Jevtić M, Arsić-Komljenović G, Ristanović E, Stanković N, Sjenicić G, Janićijević-Hudomal S. [Impossibility of the treatment of inoperable liver multicystic echinococcosis due to adverse reactions to antihelminitics]. Vojnosanit Pregl 2009; 66: 833-9. Serbian. PubMed Citation  (27 year old with echinococcal cysts developed ALT elevations after 2 months of albendazole therapy [800 mg daily] and also did not tolerate praziquantel [rash] leaving no options).

  20. Amoruso C, Fuoti M, Miceli V, Zito E, Celano MR, De Giorgi A, Nebbia G. [Acute hepatitis as a side effect of albendazole: a pediatric case]. Pediatr Med Chir 2009; 31: 176-8. Italian. PubMed Citation  (7 year old girl with pinworms developed jaundice during third course of albendazole [bilirubin 6.4 mg/dL, ALT 2200 U/L, GGT 58 U/L, Alk P 899 U/L], resolving rapidly upon stopping). 

  21. Drugs for parasitic infections. Treat Guidelines Med Ltr 2010; 8: e1-e20. Not in PubMed.  (Brief description of drugs for parasitic infections in adults and children as well as a table of their major side effects: albendazole is the drug of choice for ascariasis, cutaneous larva migrans, pinworm, hookworm, whipworm, trichinellosis, and several less common parasitic infections; side effects include ALT elevations). 

  22. Namwanje H, Kabatereine N, Olsen A. A randomised controlled clinical trial on the safety of co-administration of albendazole, ivermectin and praziquantel in infected schoolchildren in Uganda. Trans R Soc Trop Med Hyg 2011; 105: 181-8. PubMed Citation(Trial comparing a 7 day course of the combination of albendazole, ivermectin and praziquantel to standard therapy in 235 children with lymphatic filariasis, schistosomiasis or helminthiasis found no differences in efficacy in decreasing egg counts or microfilariae and no change in liver tests).

  23. Marin Zuluaga JI, Marin Castro AE, Perez Cadavid JC, Restrepo Gutierrez JC. Albendazole-induced granulomatous hepatitis: a case report. J Med Case Rep 2013; 7: 201. [Epub ahead of print] PubMed Citation.   (25 year old woman developed jaundice 2 weeks after receiving albendazole [bilirubin 13.8 mg/dL, ALT 1649 U/L, Alk P 145 U/L], biopsy showing epithelioid granulomas, resolving within 2 months).

  24. Gözüküçük R. Albendazole-induced toxic hepatitis: A case report. Turk J Gastroenterol 2013; 24: 82-3. PubMed Citation.   (28 year old man developed abnormal liver tests 20 days after starting albendazole for hydatid cyst disease [bilirubin not given, ALT 968 U/L, Alk P 209 U/L] resolving rapidly upon stopping and recurring within 3 days of restarting albendazole).

 

 

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OTHER REFERENCE LINKS
Albendazole

 

  1. PubMed logoRecent References on Albendazole

  2. Clinical Trials logoTrials on Albendazole

  3. TOXLINE logoTOXLINE Citations on Albendazole

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