Effect of parenterally injected benzimidazole compounds on Echinococcus multilocularis and Taenia crassiceps metacestodes in laboratory animals.
In mice infected with metacestodes of Taenia crassiceps, the following compounds were at least partially effective when injected intraperitoneally at the dosage indicated: cambendazole (500 mg/kg), mebendazole (6.25 mg/kg), oxibendazole (500 mg/kg), 5-benzamido-2(4-thiazolyl)benzimidazole (500 mg/kg), 2-carboethoxyamino benzimidazole (125 mg/kg), and 2-carbomethoxyamino benzimidazole (500 mg/kg). The following were inactive at the dosage indicated: parbendazole (500 mg/kg), thiabendazole (1,000 mg/kg), and fenbendazole (1,000 mg/kg). Mebendazole, which showed some activity at 6.25 mg/kg, was highly active as a single intraperitoneal dose at 25 mg/kg. When injected subcutaneously, mebendazole was much less active than when given intraperitoneally. In mice infected with metacestodes of Echinococcus multilocularis, intraperitoneal injection of mebendazole at 75 to 150 mg/kg, daily for 3 days, was highly effective (95 to 100% reduction in cyst mass). In contrast, oral administration at 1,000 mg/kg, daily for 3 days, was only partially effective. The drug was also effective when given intraperitoneally to infected cotton rats. A water-soluble benzimidazole, carboxymethyleneamino cambendazole, was approximately 50% effective in mice when injected daily for 3 days at a dosage of 75 or 150 mg/kg. The results suggest that, in metacestode infections of medical importance, it may be possible to kill the parasite by delivering a drug to its immediate vicinity, and so to reduce the required dosage with respect to the host.
D000284:Administration, Oral; D000818:Animals; D001562:Benzimidazoles / Q000008:administration & dosage* / Q000627:therapeutic use; D002159:Cambendazole / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000627:therapeutic use; D002219:Carbamates / Q000008:administration & dosage / Q000627:therapeutic use; D004443:Echinococcosis / Q000188:drug therapy* / Q000469:parasitology; D005260:Female; D007274:Injections, Intraperitoneal; D007279:Injections, Subcutaneous; D008463:Mebendazole / Q000008:administration & dosage / Q000627:therapeutic use; D051379:Mice; D051381:Rats; D013622:Taeniasis / Q000188:drug therapy* / Q000469:parasitology
D001562:Benzimidazoles; D002219:Carbamates; C011321:oxibendazole; D002159:Cambendazole; D008463:Mebendazole