Antifilarial activity of macrocyclic lactones: comparative studies with ivermectin, doramectin, milbemycin A4 oxime, and moxidectin in Litomosoides carinii, Acanthocheilonema viteae, Brugia malayi, and B. pahangi infection of Mastomys coucha.
The avermectins ivermectin and doramectin and the milbemycins milbemycin A4 oxime and moxidectin were tested for filaricidal activity in Mastomys coucha infected with Litomosoides carinii, Acanthocheilonema viteae, Brugia malayi, and B. pahangi. Single subcutaneous doses of 0.005-5 mg/kg (L. carinii), 0.0005-0.5 mg/kg (A. viteae), 0.5 and 5 mg/kg (B. malayi), and 5 mg/kg (B. pahangi) were injected. Necropsies were performed 42 days after treatment. The avermectins caused a strong and rapid reduction of microfilaraemia in L. carinii and A. viteae infections within a few hours after treatment but showed only moderate efficacies on microfilariae of Brugia spp. The effects of the milbemycin derivatives on L. carinii and A. viteae microfilariae were generally weaker than those of the avermectins. However, moxidectin was comparatively active against microfilariae of Brugia spp. Subsequently the parasitaemia levels of L. carinii and A. viteae infected animals remained either almost completely depressed or tended to reincrease in a dose dependent manner whereas there was generally a continuous decrease of microfilaraemia levels in Brugia spp. infected animals. Adulticidal effects were limited to A. viteae although with neither dose of neither drug > 95% reductions of adult worm counts were reached. However, pathogenic influences of the drugs were observed on intrauterine embryonic stages of the parasites.
Schares
G
G
Institute for Parasitology, Justus Liebig University Giessen, Germany.
Hofmann
B
B
Zahner
H
H
D000818:Animals; D000871:Anthelmintics / Q000494:pharmacology / Q000627:therapeutic use*; D000900:Anti-Bacterial Agents / Q000494:pharmacology / Q000627:therapeutic use*; D002009:Brugia / Q000187:drug effects; D004153:Dipetalonema / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D005260:Female; D005368:Filariasis / Q000097:blood / Q000188:drug therapy*; D005370:Filarioidea / Q000187:drug effects; D007559:Ivermectin / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use*; D018942:Macrolides; D008297:Male; D008842:Microfilariae / Q000187:drug effects; D009115:Muridae; D018512:Parasitemia / Q000097:blood / Q000188:drug therapy; D012008:Recurrence
D000871:Anthelmintics; D000900:Anti-Bacterial Agents; D018942:Macrolides; C078973:milbemycin oxime; D007559:Ivermectin; C084101:doramectin; C027837:moxidectin