Search

An open clinical trial of amocarzine was carried out in onchocerciasis patients in Ecuador and Guatemala. Administration after food was more effective than that during fasting. The most effective and best tolerated regimen, 3 mg/kg twice daily after food for 3 days (in 312 patients), killed 73% of 1477 female worms at nodulectomy 4 months after treatment. The mean microfilarial skin count was greatly reduced within a week (6-11% of day 0 value on day 8) and it remained low for at least 6 months (14-18% on day 180). Follow-up of a higher dose 3 day regimen taken while fasting showed microfilaridermia of 7-9% of the day 0 value 2 years after treatment.

The miracidia of four human blood flukes, Schistosoma haematobium , S. intercalatum , S. mansoni and S. japonicum , have been studied by means of the scanning electron microscope (SEM). Differences have been observed in their respective dimensions, in the configuration of their terebratoria (apical papillae), in the shape of the epidermal plates, and in the distribution of the sensory receptors. The most evident differences have been noticed on the terebratoria where two main patterns of organization of the anastomosing membrane foldings have been described: (1) a ‘rosette’ pattern observed in S. haematobium and S. intercalatum and (2) a ‘honeycomb’ pattern in S. mansoni and S. japonicum . The structure and the taxonomic importance of these morphological features are analysed.

Various formulations and dosage forms of C 9333-Go/CGP 4540 have been tested against three species of schistosomes in various hosts, three species of filariae in jirds, and two species of intestinal nematodes. Oily and aqueous suspensions of low particle size show considerably greater antiparasitic activity than active substance with a particle size of 4.23 μm. Depending on the host-parasite test system the efficacy is increased mostly by a factor of 4 to 30. Single oral doses of 4-5 mg/kg of the micronized suspensions displayed very marked anthelminthic effects in dogs, and 8-10 mg/kg were practically curative against hookworms and schistosomes in this host. No difference in activity has been observed between the oily suspension in capsules and the syrup. The former is intended as a solid dosage form for the treatment of adults and the latter as a liquid dosage form for children.