Zahner H, Schares G
Institut für Parasitologie der Justus-Liebig-Universität, Giessen, Germany.
Acta Trop. 1993 Jan;52(4):221-66. doi: 10.1016/0001-706x(93)90010-9.
Eleven types/classes of compound with antifilarial activity were comparatively evaluated in Mastomys coucha infected with Litomosoides carinii, Acanthocheilonema viteae, Brugia malayi or B. pahangi. The paper deals with the efficacy of (i) predominantly microfilaricidal compounds [diethylcarbamazine, levamisole, avermectins (ivermectin, milbemycin), nitrofurans (nitrofurantoin, hydroxymethylnitrofurantoin, nifurtimox, furazolidone, furapyrimidone), organophosphorals (metrifonate, haloxon), and aminophenyl-amidines], (ii) predominantly macrofilaricidal compounds [suramin, benzimidazoles (flubendazole, mebendazole, oxfendazole, ciclobendazole, albendazole, cambendazole, fenbendazole), and arsenicals (thiacetarsamide, Mel PH, R7/45)], and (iii) micro- and macrofilaricidal compounds [benzazole derivatives (CGP 20376 and other benzothiazoles) and nitrophenylamines (amoscanate, CGP 6140)]. Minimum effective doses against microfilariae and minimum curative doses against adult filariae as well as detailed data on dose-efficacy relationships are reported for the various drugs. The results obtained in M. coucha are compared with those published for other experimental in vivo filarial systems, thus attempting to describe a general status of in vivo antifilarial activity of the compounds.
在感染了卡氏丝虫、旋盘尾丝虫、马来布鲁线虫或彭亨布鲁线虫的多乳鼠中，对11种具有抗丝虫活性的化合物类型/类别进行了比较评估。本文探讨了以下几类药物的疗效：（i）主要具有杀微丝蚴活性的化合物[乙胺嗪、左旋咪唑、阿维菌素（伊维菌素、米尔倍霉素）、硝基呋喃类（呋喃妥因、羟甲基硝基呋喃妥因、硝呋替莫、呋喃唑酮、呋喃嘧酮）、有机磷类（敌百虫、哈乐松）和氨基苯脒类]，（ii）主要具有杀成虫活性的化合物[苏拉明、苯并咪唑类（氟苯达唑、甲苯达唑、奥芬达唑、环苯达唑、阿苯达唑、坎苯达唑、芬苯达唑）和砷剂（硫胂密胺、Mel PH、R7/45）]，以及（iii）兼具杀微丝蚴和杀成虫活性的化合物[苯唑衍生物（CGP 20376和其他苯并噻唑）和硝基苯胺类（硝卡尼特、CGP 6140）]。报告了各种药物针对微丝蚴的最小有效剂量、针对成虫丝虫的最小治愈剂量以及剂量-疗效关系的详细数据。将在多乳鼠中获得的结果与其他体内丝虫实验系统中发表的结果进行比较，从而试图描述这些化合物体内抗丝虫活性的总体状况。
