Abstract
An investigation of the chemotherapeutic effects of 2 anthelmintics, albendazole (ABZ, methyl 5-[propylthio]benzimidazole-2-carbamate) and mebendazole (MBZ, methyl 5-[benzoyl]benzimidazole-2-carbamate), onHymenolepis microstoma andHymenolepis diminuta in experimentally infected mice and rats is reported. Single (50 mg/kg) or multiple daily oral doses (50 mg kg−1 day−1 for 3 consecutive days) of MBZ had no effect onH. microstoma; at necropsy, the drug treated mice harbored appreciable numbers of the parasite in the bile duct and biliary passages. ABZ was also inactive when given as a single oral 50 mg/kg dose on day 27 PI. Better results were obtained when ABZ was administered at a dosage of 50 mg kg−1 day−1 for 3 consecutive days; the reduction in worm burden obtained with this treatment regimen was 50%. These results are in marked contrast to those obtained with the same anthelmintics against enteralH. diminuta in rats which succumbed at lower dosages. A review was made of the published reports on the pharmacokinetic behavior of these benzimidazole carbamate anthelmintics and a hypothesis for the inactivity of MBZ againstH. microstoma is proposed.
Similar content being viewed by others
References
Allan RJ, Watson TR (1982) Identification of biliary metabolites of mebendazole. Eur J Durg Metab Pharmacokinet 6:131–136
Allan RJ, Watson TR (1983) The metabolic and pharmacokinetic disposition of mebendazole in the rat. Eur J Drug Metab Pharmacokinet 8:373–381
Barrett J (1989) Detoxification reactions in panasitic helminths. In: Bennet E-M, Behm C, Bryant C (eds) Comparative biochemistry of parasitic helminths. Chapman and Hall, New York, pp 109–114
Brody G, Elward TE (1971) Comparative activity of 29 known anthelmintics under standardized drug-diet and gavage medication regimens against four helminth species in mice. J Parasitol 57:1068–1077
Delatour P, Parish RC (1986) Benzimidazole anthelmintics and related compounds: toxicity and evaluation of residues. In: Rico AG (ed) Drug residues in animals. Academic, New York, pp 175–204
Delatour P, Parish RC, Gyurik RJ (1981) Albendazole: a comparison of relay embryotoxicity with embryotoxicity of individual metabolites. Ann Rech Vet 12:159–167
Delatour P, Garnier F, Benoit E, Longin C (1984) A correlation of toxicity of albendazole and of oxfendazole with their free metabolites and bound residues. J Vet Pharmacol Ther 7:139–145
Delatour P, Benoit E, Caude M, Tambute A (1990) Species differences in the generation of the chiral sulfoxide metabolite of albendazole in sheep and rats. Chirality 2:156–160
Dvorak JA, Jones AW, Kuhlman HH (1961) Studies on the biology ofHymenolepis microstoma (Dujardin, 1845). J Parasitol 47:833–838
Evans WS, Novak M (1976) The effect of mebendazole on the development ofHymenolepis diminuta inTribolium confusum. Can J Zool 56:1079–1083
Evans WS, Gray M, Novak M (1979) Effect of mebendazole on the larval development of three hymenolepidid cestodes. J Parasitol 65:31–34
Evans WS, Hardy M, Novak M (1980) A comparison of the effect of albendazole, cambendazole, and thiabendazole on the larval development of three hymenolepidid cestodes. J Parasitol 66:935–940
Gottschall DW, Theodorides VJ, Wang R (1990) The metabolism of benzimidazole anthelmintics. Parasitol Today 6:115–124
Greenblatt DJ, Koch-Weser J (1975a) Clinical pharmacokinetics (first of two parts). N Engl J Med 293:702–705
Greenblatt DJ, Koch-Weser J (1975b) Clinical pharmacokinetics (second of two parts). N Engl J Med 293:964–970
Gyurik RJ, Chow AW, Zaber B, Brunner EL, Miller JA, Villani AJ, Petka LA, Parish RC (1981) Metabolism of albendazole in cattle, sheep, rats, and mice. Drug Metab Dispos 9:503–508
Hennessy DR (1985) Manipulation of anthelmintic pharmacokinetics. In: Anderson N, Waller PJ (eds) Resitance in nematodes to anthelmintic drugs. CSIRO Animal Health/Australian Wool Corporation, Sydney, pp 79–85
Hennessy DR, Steel JW, Lacey E, Eagleson GK, Prichard RK (1989) The disposition of albendazole in sheep. J Vet Pharmacol Ther 12:421–429
Kirk RE (1968) Experimental design: procedures for the behavioral sciences. Brooks/Cole Publishing Co., Inc., Belmont, California, pp 493–497
Kunkle DW, Theodorides VJ (1971) Activity of parbendazole against cestodes in mice. J Parasitol 57:319
Kwan LC, Gyurik RJ, Freeman JF, Chimes N, Ritch GM, Theodorides VJ (1988) Influence of dosing regimens on the anthelmintic activity of albendazole in sheep. J Controlled Release 8:31–38
Marriner SE, Morris DL, Dickson B, Bogan JA (1986) Pharmacokinetics of albendazole in man. Eur J Clin Pharmacol 30:705–708
McCracken RO, Lipkowitz KB (1990) Experimental and theoretical studies of albendazole, oxibendazole, and tioxidazole. J Parasitol 76:180–185
McCracken RO, Nierste DM, Moss J, Garcia A (1984) Oxfendazole: regimen dependent expression of drug efficacy againstTrichinella spiralis. Int J Parasitol 14:309–312
Meuldermans WEG, Hurkmans RMA, Lauwers WFJ, Heykants JJP (1976) The in vitro metabolism of mebendazole by pig, rat and dog liver fractions. Eur J Drug Metab Pharmacokinet 1:35–40
Novak M, Evans WS (1978) The effect of mebendazole on different developmental stages ofHymenolepis diminuta cysticercoids. Can J Zool 56:604–607
Novak M, Hardy M, Evans WS (1982) A comparison of the effects of ten, 5-substituted benzimidazolyl carbamates on larval development of three hymenolepidid tapeworms. J Parasitol 68:1165–1167
Read CP, Rothman JH, Simmons JE (1963) Studies on membrane transport, with special reference to parasite-host integration. Ann New York Acad Sci 113:154–205
Souhaili-El Amri H, Fargetton X, Benoit E, Totis M, Batt A-M (1988a) Inducing effect of albendazole on rat liver drug-metabolizing enzymes and metabolite pharmacokinetics. Toxicol Appl Pharmacol 92:141–149
Souhaili-El Amri H, Mothe O, Totis M, Masson C, Batt A-M, Delatour P, Siest G (1988b) Albendazole sulfonation by rat liver cytochrome P-450c. J Pharmacol Exp Ther 246:758–764
Townsend LB, Wise DS (1990) The synthesis and chemistry of certain anthelmintic benzimidazoles. Parasitol Today 6:107–112
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
McCracken, R.O., Lipkowitz, K.B. & Dronen, N.O. Efficacy of albendazole and mebendazole againstHymenolepis microstoma andHymenolepis diminuta . Parasitol Res 78, 108–111 (1992). https://doi.org/10.1007/BF00931650
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00931650