info albendazol

Info on albendazol and side effects


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Albendazole
Drug Nomenclature
Date of monograph revision: 19-Sep-1997; 25-Jun-1998; 03-Jun-1999; 09-Aug-2001; 28-May-2002; 11-May-2004; 19-Jul-2006; (last modified: 21-Jan-2007)
Synonyms: Albendatsoli; Albendazol; Albendazolas; Albendazolum; SKF-62979
BAN: Albendazole
USAN: Albendazole
INN: Albendazole [rINN (en)]
INN: Albendazol [rINN (es)]
INN: Albendazole [rINN (fr)]
INN: Albendazolum [rINN (la)]
INN: Альбендазол [rINN (ru)]
Chemical name: Methyl 5-propylthio-1H-benzimidazol-2-ylcarbamate
Molecular formula: C12H15N3O2S =265.3
CAS: 54965-21-8
ATC code: P02CA03
Read CTV3: y02WX

Chemical Structure of Albendazole

Pharmacopoeias:
In Chin., Eur. (see ), Int., US, and Viet.

Ph. Eur. 5.5 (Albendazole). A white to faintly yellowish powder. Practically insoluble in water and in alcohol; very slightly soluble in dichloromethane; freely soluble in anhydrous formic acid. Protect from light.

USP 29 (Albendazole). A white to faintly yellowish powder. Practically insoluble in water and in alcohol; very slightly soluble in ether and in dichloromethane; freely soluble in anhydrous formic acid. Store in airtight containers.

Adverse Effects and Precautions
As for Mebendazole, .

Albendazole should only be used in the treatment of echinococcosis if there is constant medical supervision with regular monitoring of serum-transaminase concentrations and of leucocyte and platelet counts. Patients with liver damage should be treated with reduced doses of benzimidazole carbamates, if at all.1

1. Davis A, et al. Multicentre clinical trials of benzimidazolecarbamates in human cystic echinococcosis (phase 2). Bull WHO 1989; 67: 503–8. PubMed
Incidence of adverse effects.
Although generally well-tolerated, the following adverse reactions were reported in the first phase of WHO-coordinated studies1 involving 30 patients given high-dose therapy with albendazole for the treatment of cystic echinococcosis (hydatid disease): raised serum-transaminase levels (2 patients), reduced leucocyte counts (1 patient), gastrointestinal symptoms (1 patient), allergic conditions (1 patient), and loss of hair (1 patient). Treatment was stopped in a further patient with alveolar echinococcosis because of depressed bone-marrow activity. In the second phase of these studies,2 of 109 patients given albendazole for cystic echinococcosis, 20 experienced adverse effects; similar findings were reported with mebendazole. The range of effects with albendazole was: elevation of transaminases (5 patients), abdominal pain and other gastrointestinal symptoms (7 patients), severe headache (4 patients), loss of hair (2 patients), leucopenia (2 patients), fever and fatigue (1 patient), thrombocytopenia (1 patient), and urticaria and itching (1 patient). Albendazole had to be withdrawn in 5 patients because of adverse effects, although in 3 the withdrawal was only temporary.

1. Davis A, et al. Multicentre clinical trials of benzimidazolecarbamates in human echinococcosis. Bull WHO 1986; 64: 383–8. PubMed
2. Davis A, et al. Multicentre clinical trials of benzimidazolecarbamates in human cystic echinococcosis (phase 2). Bull WHO 1989; 67: 503–8. PubMed
Effects on growth.
A multiple-dose regimen of albendazole in children with asymptomatic trichuriasis has been reported to be associated with impaired growth in those with low levels of infection.1 However it was considered that this should not prevent the use of single doses in mass treatment programmes.2

1. Forrester JE, et al. Randomised trial of albendazole and pyrantel in symptomless trichuriasis in children. Lancet 1998; 352: 1103–8. PubMed
2. Winstanley P. Albendazole for mass treatment of asymptomatic trichuris infections. Lancet 1998; 352: 1080–1. PubMed
Effects on the liver.
In a series of 40 patients given albendazole for echinococcosis, 7 developed abnormalities in liver function tests during therapy.1 Six had a hepatocellular type of abnormality attributable to albendazole; the seventh had cholestatic jaundice which was probably not due to albendazole. See also Incidence of Adverse Effects, .

1. Morris DL, Smith PG. Albendazole in hydatid disease—hepatocellular toxicity. Trans R Soc Trop Med Hyg 1987; 81: 343–4. PubMed
Pregnancy.
Albendazole is teratogenic in some animals and the manufacturers note that there are no adequate and well controlled studies in human pregnancy. Albendazole is therefore usually contra-indicated during pregnancy and the manufacturers caution against becoming pregnant while taking albendazole or within one month of completing treatment.

Interactions
Anthelmintics.
The plasma concentration of albendazole sulfoxide has been increased by praziquantel,1 although the practical consequences of this were considered uncertain.

1. Homeida M, et al. Pharmacokinetic interaction between praziquantel and albendazole in Sudanese men. Ann Trop Med Parasitol 1994; 88: 551–9. PubMed
Corticosteroids.
Plasma concentrations of the active metabolite of albendazole (albendazole sulfoxide) were reported to be raised by about 50% in a study in 8 patients receiving dexamethasone.1

1. Jung H, et al. Dexamethasone increases plasma levels of albendazole. J Neurol 1990; 237: 279–80. PubMed
Histamine H2-antagonists.
Concentrations of albendazole sulfoxide have been found to be raised in bile and hydatid cyst fluid when albendazole was given with cimetidine, which may increase effectiveness in the treatment of echinococcosis.1

1. Wen H, et al. Initial observation on albendazole in combination with cimetidine for the treatment of human cystic echinococcosis. Ann Trop Med Parasitol 1994; 88: 49–52. PubMed
Pharmacokinetics
Absorption of albendazole from the gastrointestinal tract is poor but may be enhanced by a fatty meal. Albendazole rapidly undergoes extensive first-pass metabolism. Its principal metabolite albendazole sulfoxide has anthelmintic activity and a plasma half-life of about 8.5 hours. Albendazole sulfoxide is widely distributed throughout the body including into the bile and the CSF. It is about 70% bound to plasma protein. Albendazole sulfoxide is eliminated in the bile; only a small amount appears to be excreted in the urine.

References.

1. Marriner SE, et al Pharmacokinetics of albendazole in man. Eur J Clin Pharmacol 1986; 30: 705–8. PubMed
2. Morris DL, et al. Penetration of albendazole sulphoxide into hydatid cysts. Gut 1987; 28: 75–80. PubMed
3. Steiger U, et al. Albendazole treatment of echinococcosis in humans: effects on microsomal metabolism and drug tolerance. Clin Pharmacol Ther 1990; 47: 347–53. PubMed
4. Jung H, et al. Clinical pharmacokinetics of albendazole in patients with brain cysticercosis. J Clin Pharmacol 1992; 32: 28–31. PubMed
5. Jung H, et al. Clinical pharmacokinetics of albendazole in children with neurocysticercosis. Am J Ther 1997; 4: 23–6. PubMed
Uses and Administration
Albendazole is a benzimidazole carbamate anthelmintic structurally related to mebendazole () and with similar activity. It is used in relatively high doses in the treatment of the cestode infections cysticercosis and echinococcosis (hydatid disease). In some countries albendazole is used in the treatment of single and mixed intestinal nematode infections including ascariasis, enterobiasis, hookworm, strongyloidiasis, and trichuriasis. It may also be used in the treatment of capillariasis, gnathostomiasis, and trichostrongyliasis. Albendazole may be effective in the treatment of the tissue nematode infections cutaneous larva migrans, toxocariasis, and trichinosis and, with other anthelmintics, in the management of the filarial nematode infection lymphatic filariasis. For discussions of these infections and their treatment, see under Choice of Anthelmintic (), and under the individual headings below.

In the treatment of echinococcosis, albendazole is given by mouth with meals in a dose of 400 mg twice daily for 28 days for patients weighing over 60 kg. A dose of 15 mg/kg daily in two divided doses (to a maximum total daily dose of 800 mg) is used for patients weighing less than 60 kg. For cystic echinococcosis, the 28-day course may be repeated after 14 days without treatment to a total of 3 treatment cycles. For alveolar echinococcosis, cycles of 28 days of treatment followed by 14 days without treatment may need to continue for months or years.

In the treatment of neurocysticercosis, albendazole 400 mg twice daily for patients weighing over 60 kg (or 15 mg/kg daily in two divided doses to a maximum total daily dose of 800 mg in those weighing less than 60 kg) is given by mouth for 8 to 30 days.

Albendazole is given by mouth, usually as a single dose, in the treatment of single or mixed intestinal nematode infections. The usual dose for adults and children aged 2 years or over with ascariasis, enterobiasis, hookworm infections, or trichuriasis is 400 mg as a single dose. In enterobiasis, the dose may be repeated in 1 to 4 weeks. Some consider that children of 1 to 2 years of age may be given 200 mg for enterobiasis. In strongyloidiasis, 400 mg is given once or twice daily for 3 consecutive days; this may be repeated after 3 weeks if necessary.

Albendazole has also been used to treat giardiasis (); suggested doses are 400 mg daily by mouth for 5 days.

Ascariasis.
Albendazole is used as an alternative to mebendazole in the treatment of ascariasis (). Both drugs are equally highly effective with a cure rate greater than 98% reported for albendazole in one study.1

1. Albonico M, et al. A randomized controlled trial comparing mebendazole and albendazole against Ascaris, Trichuris and hookworm infections. Trans R Soc Trop Med Hyg 1994; 88: 585–9. PubMed
Capillariasis.
Albendazole in a dose of 400 mg daily for 10 days has been suggested1 as an alternative to mebendazole for the treatment of capillariasis ().

1. Medical Letter on Drugs and Therapeutics. Drugs for parasitic infections (issued August 2004). Available at: online (accessed 02/06/06)
Cutaneous larva migrans.
Albendazole has been reported1-4 to be effective in the treatment of cutaneous larva migrans () and is an alternative to tiabendazole or ivermectin. Albendazole, generally in a dose of 400 mg daily for three1 or five2 days, has alleviated the discomfort of cutaneous larva migrans; treatment for seven days may be more effective and has not been associated with an increased incidence of adverse effects.4 A single dose of 400 mg has also been effective.3

1. Jones SK, et al. Oral albendazole for the treatment of cutaneous larva migrans. Br J Dermatol 1990; 122: 99–101. PubMed
2. Sanguigni S, et al. Albendazole in the therapy of cutaneous larva migrans. Trans R Soc Trop Med Hyg 1990; 84: 831. PubMed
3. Oriheula AR, Torres JR. Single dose of albendazole in the treatment of cutaneous larva migrans. Arch Dermatol 1990; 126: 398–9. PubMed
4. Veraldi S, Rizzitelli G. Effectiveness of a new therapeutic regimen with albendazole in cutaneous larva migrans. Eur J Dermatol 1999; 9: 352–3. PubMed
Cysticercosis.
Albendazole is used in the treatment of neurocysticercosis () as an alternative to praziquantel;1,2 some consider albendazole to be preferable.3-5 Albendazole has also been reported to be effective in extra-ocular cysticercosis.6

1. Sotelo J, et al. Short course of albendazole therapy for neurocysticercosis. Arch Neurol 1988; 45: 1130–3. PubMed
2. Botero D, et al. Short course albendazole treatment for neurocysticercosis in Columbia. Trans R Soc Trop Med Hyg 1993; 87: 576–7. PubMed
3. Cruz M, et al. Albendazole versus praziquantel in the treatment of cerebral cysticercosis: clinical evaluation. Trans R Soc Trop Med Hyg 1991; 85: 244–7. PubMed
4. Takayanagui OM, Jardim E. Therapy for neurocysticercosis: comparison between albendazole and praziquantel. Arch Neurol 1992; 49: 290–4. PubMed
5. Mehta SS, et al. Albendazole versus praziquantel for neurocysticercosis. Am J Health-Syst Pharm 1998; 55: 598–600. PubMed
6. Sihota R, Honavar SG. Oral albendazole in the management of extraocular cysticercosis. Br J Ophthalmol 1994; 78: 621–3. PubMed
Echinococcosis.
Albendazole is used in the treatment of echinococcosis () as an adjunct to, or instead of, surgery. It is generally preferred to mebendazole.

References.

1. Teggi A, et al. Therapy of human hydatid disease with mebendazole and albendazole. Antimicrob Agents Chemother 1993; 37: 1679–84. PubMed
2. Gil-Grande LA, et al. Randomised controlled trial of efficacy of albendazole in intra-abdominal hydatid disease. Lancet 1993; 342: 1269–72. PubMed
3. Wen H, et al. Initial observation on albendazole in combination with cimetidine for the treatment of human cystic echinococcosis. Ann Trop Med Parasitol 1994; 88: 49–52. PubMed
4. Wen H, et al. Albendazole chemotherapy for human cystic and alveolar echinococcosis in north-western China. Trans R Soc Trop Med Hyg 1994; 88: 340–3. PubMed
5. Liu Y, et al. Continuous long-term albendazole therapy in intraabdominal cystic echinococcosis. Chin Med J (Engl) 2000; 113: 827–32. PubMed
6. Keshmiri M, et al. Albendazole versus placebo in treatment of echinococcosis. Trans R Soc Trop Med Hyg 2001; 95: 190–4. PubMed
Gnathostomiasis.
Albendazole has been reported to be effective in the treatment of gnathostomiasis (). Doses of 400 mg once or twice daily have been given for 2 or 3 weeks.1-4

1. Kraivichian P, et al. Albendazole for the treatment of human gnathostomiasis. Trans R Soc Trop Med Hyg 1992; 86: 418–21. PubMed
2. Suntharasamai P, et al. Albendazole stimulates outward migration of Gnathostoma spinigerum to the dermis in man. Southeast Asian J Trop Med Public Health 1992; 23: 716–22. PubMed
3. Nontasut P, et al. Comparison of ivermectin and albendazole treatment for gnathostomiasis. Southeast Asian J Trop Med Public Health 2000; 31: 374–7. PubMed
4. Medical Letter on Drugs and Therapeutics. Drugs for parasitic infections (issued August 2004). Available at: online (accessed 02/06/06)
Hookworm infections.
Hookworm infections () are commonly treated with benzimidazole carbamates such as albendazole. In 77 patients with light necatoriasis (Necator americanus infection) albendazole, in a single 400-mg dose, produced an 84% cure rate and an 82% reduction in egg count in those patients not cured.1 In another study,2 although the cure rate was only 56.8% following a single 400-mg dose of albendazole this was superior to treatment with mebendazole which had a cure rate of 22.4%. A further study3 comparing albendazole with mebendazole and pyrantel in the treatment of necatoriasis also found albendazole to be the most effective.

Albendazole is given in mass treatment programmes to reduce the overall burden of infection.1,4

1. Nahmias J, et al. Evaluation of albendazole, pyrantel, bephenium, pyrantel-praziquantel and pyrantel-bephenium for single-dose mass treatment of necatoriasis. Ann Trop Med Parasitol 1989; 83: 625–9. PubMed
2. Albonico M, et al. A randomized controlled trial comparing mebendazole and albendazole against Ascaris, Trichuris and hookworm infections. Trans R Soc Trop Med Hyg 1994; 88: 585–9. PubMed
3. Sacko M, et al. Comparison of the efficacy of mebendazole, albendazole and pyrantel in treatment of human hookworm infections in the southern region of Mali, West Africa. Trans R Soc Trop Med Hyg 1999; 93: 195–203. PubMed
4. Idris MA, et al Effective control of hookworm infection in school children from Dhofar, Sultanate of Oman: a four-year experience with albendazole mass chemotherapy. Acta Trop 2001; 80: 139–43. PubMed
Lymphatic filariasis.
Albendazole is used in the management of lymphatic filariasis (). In endemic areas where more than 5% of the population is infected, mass treatment of the entire population (excluding neonates, pregnant women, and debilitated individuals) can reduce the intensity of transmission and the incidence of disease. A global elimination campaign launched by WHO, with other international agencies, advocates a single dose of albendazole 400 mg with either a single dose of ivermectin 200 micrograms/kg (for bancroftian filariasis if there is co-endemic loiasis or onchocerciasis) or with a single dose of diethylcarbamazine 6 mg/kg (if there is no co-endemic loiasis or onchocerciasis); these doses are given once each year for 4 to 6 years.

Microsporidiosis.
Albendazole has been tried1-5 in the treatment of the protozoal infection microsporidiosis () in patients with AIDS. Albendazole has also been used empirically in the treatment of HIV-associated infections and complications ().

1. Blanshard C, et al. Treatment of intestinal microsporidiosis with albendazole in patients with AIDS. AIDS 1992; 6: 311–13. PubMed
2. Dieterich DT, et al. Treatment with albendazole for intestinal disease due to Enterocytozoon bieneusi in patients with AIDS. J Infect Dis 1994; 169: 178–82. PubMed
3. Franzen C, et al. Intestinal microsporidiosis with Septata intestinalis in a patient with AIDS—response to albendazole. J Infect 1995; 31: 237–9. PubMed
4. Dore GJ, et al. Disseminated microsporidiosis due to Septata intestinalis in nine patients infected with the human immunodeficiency virus: response to therapy with albendazole. Clin Infect Dis 1995; 21: 70–6. PubMed
5. Molina J-M, et al. Albendazole for treatment and prophylaxis of microsporidiosis due Encephalitozoon intestinalis in patients with AIDS: a randomized double-blind controlled trial. J Infect Dis 1998; 177: 1373–7. PubMed
Strongyloidiasis.
Albendazole is generally preferred to tiabendazole or mebendazole in the treatment of strongyloidiasis () although some authorities now consider ivermectin to be the drug of choice.

References.

1. Rossignol JF, Maisonneuve H. Albendazole: placebo-controlled study in 870 patients with intestinal helminthiasis. Trans R Soc Trop Med Hyg 1983; 77: 707–11. PubMed
2. Chanthavanich P, et al. Repeated doses of albendazole against strongyloidiasis in Thai children. Southeast Asian J Trop Med Public Health 1989; 20: 221–6. PubMed
3. Mojon M, Nielsen PB. Treatment of Strongyloides stercoralis with albendazole: a cure rate of 86 per cent. Zentralbl Bakteriol Mikrobiol Hyg [A] 1987; 263: 619–24. PubMed
4. Archibald LK, et al. Albendazole is effective treatment for chronic strongyloidiasis. Q J Med 1993; 86: 191–5. PubMed
Toxocariasis.
Albendazole is one of the drugs that might be used for the treatment of toxocariasis () and in a small study1 it produced improvement similar to that achieved with tiabendazole but with fewer problems.

1. Stürchler D, et al. Thiabendazole vs albendazole in treatment of toxocariasis: a clinical trial. Ann Trop Med Parasitol 1989; 83: 473–8. PubMed
Trichinosis.
Albendazole may be effective in the treatment of trichinosis (). A retrospective study in 44 patients with trichinosis comparing albendazole treatment with tiabendazole found that, while the two drugs were of comparable efficacy, albendazole was the better tolerated.1 Albendazole has been used to treat a patient infected with Trichinella pseudospiralis, an organism related to T.spiralis, the usual cause of trichinosis.2

1. Cabié A, et al. Albendazole versus thiabendazole as therapy for trichinosis: a retrospective study. Clin Infect Dis 1996; 22: 1033–5. PubMed
2. Andrews JRH, et al. Trichinella pseudospiralis in humans: description of a case and its treatment. Trans R Soc Trop Med Hyg 1994; 88: 200–3. PubMed
Trichostrongyliasis.
Albendazole in a single dose of 400 mg has been suggested1 as an alternative to pyrantel embonate or mebendazole in the treatment of trichostrongyliasis ().

1. Medical Letters on Drugs and Therapeutics. Drugs for parasitic infections (issued August 2004). Available at: online (accessed 02/06/06)
Trichuriasis.
Albendazole is used in the treatment of trichuriasis (). It is normally given in a single dose and is often used in mixed intestinal nematode infections.1 However, it has been reported1-3 that in children with mixed intestinal worm infections single doses of albendazole are ineffective in eliminating Trichuris trichiura and multiple doses are required to produce worthwhile reductions in egg production. Treatment for 3 days has been used4 (but for a suggestion that such regimens may be associated with impaired growth in less heavily infected children, see Effects on Growth under Adverse Effects, ). Combined use of albendazole with ivermectin may prove useful.5

1. Hall A, Anwar KS. Albendazole and infections with Trichuris trichiura and Giardia intestinalis. Southeast Asian J Trop Med Public Health 1991; 22: 84–7. PubMed
2. Hall A, Nahar Q. Albendazole and infections with Ascaris lumbricoides and Trichuris trichiura in children in Bangladesh. Trans R Soc Trop Med Hyg 1994; 88: 110–12. PubMed
3. Albonico M, et al. A randomized controlled trial comparing mebendazole and albendazole against Ascaris, Trichuris and hookworm infections. Trans R Soc Trop Med Hyg 1994; 88: 585–9. PubMed
4. Medical Letter on Drugs and Therapeutics. Drugs for parasitic infections (issued August 2004). Available at: online (accessed 02/06/06)
5. Ismail MM, Jayakody RL. Efficacy of albendazole and its combinations with ivermectin or diethylcarbamazine (DEC) in the treatment of Trichuris trichiura infections in Sri Lanka. Ann Trop Med Parasitol 1999; 93: 501–4. PubMed
Preparations
Single-ingredient Preparations
The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.

Argentina: Vastus; Australia: Eskazole; Zentel; Austria: Eskazole; Brazil: Alba-3; Alben; Albendrox; Albendy; Albenix; Albentel; Albenzonil; Albezin; Alib; Alin; Alzoben; Amplozol¤; Bentiamin; Benzol ; Dazol¤; Helmintal¤; Imavermil; Mebenix; Monozol; Neo Bendazol; Parasin; Totelmin; Verdazol; Vermiclase; Vermital; Zentel; Zolben; Zoldan; Chile: Ceprazol; Vermoil; Zentel; Czech Republic: Zentel; France: Eskazole¤; Zentel; Germany: Eskazole; Greece: Eskazole; Zentel; India: Albezole; Bendex; Combantrin-A; Emanthal; Nemozole; Olworm; Zentel; Israel: Eskazole; Italy: Zentel; Malaysia: Albendol; Champs D-Worms; Thelban¤; Vemizol; Zentel; Zoben; Mexico: Albensil; Alfazol; Bendapar; Bradelmin; Dabenzol¤; Dazocan; Dazolin; Dezabil; Digezanol; Entoplus; Eskazole; Euralben¤; Flatezol; Gascop; Helmisons¤; Loveral; Lurdex; Olbendital; Rivazol; Serbendazol; Tenibex; Veranzol; Vermilan¤; Vermin Plus; Vermisen; Zelfin; Zenaxin; Zentel; Netherlands: Eskazole; Portugal: Zentel; Russia: Nemozole (Немозол); South Africa: Bendex; Paranthil¤; Zentel; Singapore: Alzental; Zentel; Spain: Eskazole; Switzerland: Zentel; Thailand: Abentel; Albatel; Alben; Albenda; Alda¤; Alfuca; Alzol; Anthel¤; Gendazel; Labenda; Leo-400; Manoverm; Masaworm¤; Mesin; Mycotel; Vermixide; Zeben; Zela; Zentel; Zenzera; Turkey: Andazol; United Arab Emirates: Albenda; United Kingdom: Eskazole¤; United States: Albenza; Venezuela: Albicar ; Bevindazol; Helal; Sostril; Taron; Vendazol; Zentel;

Multi-ingredient Preparations
The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.

Mexico: Oxal;

Pharmacopoeial Preparations