Thiacetarsamide (adulticide) versus melarsomine (RM 340) developed as macrofilaricide (adulticide and larvicide) to cure canine heartworm infection in dogs.

J P Raynaud
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Abstract

To implement a new macrofilaricide, treatment of heartworm infection or disease in dogs was checked in all the clinical situations ie from subclinical to severe disease. After preliminary toxicity and efficacy models on experimentally infected dogs, in addition, to the reference posology (2.5 mg of melarsomine (RM 340)/kg twice, 24 h apart by deep IM injection) a more practical program for vet practitioners was suggested (2.2 mg/kg twice, 3 h apart) using modelization of the pharmacokinetic data. The two treatments were equivalent as shown on models with experimental infection of dogs, critical tests on naturally infected dogs and clinical trials in veterinary practice. We advise using specific and well adapted therapeutic programs for each of the clinical classes (class 1: subclinical, class 2: moderate, class 3: severe). The safety margin is respectively x 3 or x 2.5 in contrast with thiacetarsamide which, being hepatotoxic, has no safety margin, and sometimes is nephrotoxic at the recommended dose. RM 340 is fully effective on D immitis adults (even on young ones of 7 months old) and L5 immatures (4 months old) when thiacetarsamide is poorly effective on 7 months or ineffective on 4-month-old parasites. Clinical trials in veterinary practice showed that the programs are well adapted to many clinical situations. The product is effective, relatively safe and easy to handle by IM injection. Preliminary results show its possible use as tactical treatment (2.2 mg/kg twice, 3 h apart) twice a year in mid August and December-January to prevent heartworm disease.

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硫乙酰胺(杀虫剂)与黑拉素(RM 340)作为大丝虫杀虫剂(杀虫剂和杀幼虫剂)治疗犬心丝虫感染。
为了实施一种新的大丝虫杀灭剂,对犬心丝虫感染或疾病的治疗进行了从亚临床到严重疾病的所有临床情况的检查。在对实验感染犬进行初步的毒性和疗效模型后,除了参考剂量(2.5 mg (RM 340)/kg两次,间隔24 h深注射IM)外,还通过药代动力学数据建模,提出了更实用的兽医方案(2.2 mg/kg两次,间隔3 h)。这两种治疗方法在狗的实验感染模型、对自然感染狗的关键测试和兽医实践中的临床试验中都是相同的。我们建议针对每个临床类别(1类:亚临床,2类:中度,3类:重度)使用特定且适应性良好的治疗方案。与噻乙酰胺相比,其安全范围分别为x3或2.5,噻乙酰胺具有肝毒性,没有安全范围,在推荐剂量下有时还具有肾毒性。当硫乙酰胺对7个月大或4个月大的寄生虫效果不佳时,RM 340对D型寄生虫成虫(甚至对7个月大的幼虫)和L5型寄生虫(4个月大)完全有效。兽医实践的临床试验表明,该方案很好地适应了许多临床情况。本品注射IM有效,相对安全,操作方便。初步结果表明,可在每年8月中旬和12 - 1月两次(2.2 mg/kg 2次,间隔3 h)作为预防心丝虫病的战术治疗。
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