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关于美拉胂醇( Cymelarsan )对感染布氏布氏锥虫和伊氏锥虫家畜的疗效的初步观察

Preliminary observations on the efficacy of mel Cy (Cymelarsan) in domestic animals infected with stocks of Trypanosoma brucei brucei and T.b. evansi.

作者信息

Zweygarth E, Ngeranwa J, Kaminsky R

机构信息

Kenya Trypanosomiasis Research Institute (KETRI), Kikuyu.

出版信息

Trop Med Parasitol. 1992 Dec;43(4):226-8.

PMID:1293725
Abstract

The trypanocidal activity of an arsenical compound (RM 110; mel Cy; Cymelarsan) was evaluated against Trypanosoma brucei brucei and T. brucei evansi in cultures, in goats and pigs. The trypanosome stocks used differed in their levels of susceptibility to cymerlarsan in an in vitro test, their IC50 values (drug concentration which inhibits growth by 50%) ranging from 4.8-5.1 nM for susceptible, and 26.9 nM for a resistant stock. Goats infected with a susceptible T.b. evansi stock were cured after a single injection of 0.3 mg/kg cymelarsan. In three out of four goats chronically infected with the same stock a single injection of 0.625 mg/kg cymelarsan effected a cure, whereas the goat in which the infection relapsed was finally cured after injection of 0.625 mg/kg on each of three consecutive days. A single dose of 2.5 mg/kg did not cure goats infected with an arsenical-resistant T.b. brucei stock. One of two pigs chronically infected with arsenical-susceptible stocks of T.b. brucei was cured after a single injection of 0.625 mg/kg cymelarsan, whereas the other one relapsed and died. In conclusion, the results may indicate that the dose of 0.25 mg/kg recommended by the manufacturer is too low and that a single may not cure animals with CNS involvement with certainty. The recommended dose might therefore have been applied strictly for the treatment of camels only.

摘要

在培养物、山羊和猪中评估了一种砷化合物(RM 110;美拉胂醇; Cymelarsan)对布氏布氏锥虫和伊氏锥虫的杀锥虫活性。所使用的锥虫株在体外试验中对美拉胂醇的敏感性水平不同,其IC50值(抑制生长50%的药物浓度)对于敏感株为4.8 - 5.1 nM,对于耐药株为26.9 nM。感染敏感伊氏锥虫株的山羊单次注射0.3 mg/kg美拉胂醇后治愈。在四只长期感染同一株的山羊中,有三只单次注射0.625 mg/kg美拉胂醇后治愈,而感染复发的那只山羊在连续三天每天注射0.625 mg/kg后最终治愈。单剂量2.5 mg/kg不能治愈感染砷耐药布氏锥虫株的山羊。两只长期感染砷敏感布氏锥虫株的猪中,一只单次注射0.625 mg/kg美拉胂醇后治愈,而另一只复发并死亡。总之,结果可能表明制造商推荐的0.25 mg/kg剂量过低,单次给药可能无法肯定治愈有中枢神经系统受累的动物。因此,推荐剂量可能仅严格适用于骆驼的治疗。

相似文献

1
Preliminary observations on the efficacy of mel Cy (Cymelarsan) in domestic animals infected with stocks of Trypanosoma brucei brucei and T.b. evansi.关于美拉胂醇( Cymelarsan )对感染布氏布氏锥虫和伊氏锥虫家畜的疗效的初步观察
Trop Med Parasitol. 1992 Dec;43(4):226-8.
2
Evaluation of an arsenical compound (RM 110, mel Cy, Cymelarsan) against susceptible and drug-resistant Trypanosoma brucei brucei and T.b. evansi.一种砷化合物(RM 110、美拉胂醇、环美胂醇)对敏感及耐药布氏布氏锥虫和伊氏锥虫的评估。
Trop Med Parasitol. 1990 Jun;41(2):208-12.
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Use of cymelarsan in goats chronically infected with Trypanosoma evansi.氰胺胂在慢性感染伊氏锥虫的山羊中的应用。
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Efficacy of Cymelarsan in the treatment of natural chronic Trypanosoma evansi infection in camels in the Sudan.赛米胂治疗苏丹骆驼自然慢性伊氏锥虫感染的疗效
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Chemotherapy of CNS-trypanosomiasis: combination chemotherapy with a 5-nitroimidazole (MK 436), an arsenical (Cymelarsan) and suramin.中枢神经系统锥虫病的化疗:5-硝基咪唑(MK 436)、砷剂(美拉胂醇)和苏拉明联合化疗。
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Relative efficacy of melarsen oxide compared with mel Cy (Cymelarsan) when used in combination with difluoromethylornithine in the treatment of trypanosomiasis of the central nervous system.
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Cymelarsan in the treatment of buffaloes naturally infected with Trypanosoma evansi in south China.
Acta Trop. 1991 Aug;49(3):233-6. doi: 10.1016/0001-706x(91)90042-i.

引用本文的文献

1
Contribution of dithiol ligands to in vitro and in vivo trypanocidal activities of dithiaarsanes and investigation of ligand exchange in an aqueous solution.二硫醇配体对二硫砷烷体外和体内杀锥虫活性的贡献以及水溶液中配体交换的研究。
Antimicrob Agents Chemother. 2000 Nov;44(11):2954-61. doi: 10.1128/AAC.44.11.2954-2961.2000.
2
Properties of melarsamine hydrochloride (Cymelarsan) in aqueous solution.盐酸美拉胂胺(拜耳205)在水溶液中的性质。
Antimicrob Agents Chemother. 1994 Jun;38(6):1298-302. doi: 10.1128/AAC.38.6.1298.