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抗丝虫病及抗利什曼原虫病药

丝虫病是由丝虫寄生在人体淋巴系统引起的传染病。主要治疗药物包括乙胺嗪、呋喃嘧酮和舒拉明钠等。乙胺嗪能够有效杀灭马来、班氏、帝汶、罗阿和盘尾丝虫的微丝蚴,自1947年起便成为治疗淋巴丝虫病的首选药物,并可用于盘尾丝虫病和罗阿丝虫病的治疗。

利什曼原虫病主要分布在热带和亚热带地区,传播媒介如白蛉属和罗蛉属生活在这些区域。感染发生在网状内皮细胞中存在无鞭毛型(amastigote)利什曼原虫时。东半球以白蛉为传播媒介,西半球则通过罗蛉传播。啮齿动物和其他小型哺乳动物是贮存宿主。

人类可因脏器、皮肤黏膜或皮肤感染而遭受感染,症状从轻微和自限性到严重不一。由杜氏利什曼原虫引起的内脏利什曼病即黑热病,在免疫缺陷个体中可能致命;但在免疫功能正常者体内,它可能会潜伏多年,仅在宿主因任何原因导致免疫力下降时显现。此外,并非所有患者都会表现出明显的免疫抑制而出现内脏利什曼病。

内脏利什曼病通常表现为逐渐发热、体重减轻、肝脾肿大及肝功能异常、低蛋白血症、高丙种球蛋白血症、全血细胞减少和出血等症状。在疫区,部分病人可能无症状或症状轻微,即便未经治疗,感染也不一定发展;但另一方面,感染亦可能致命,特别是对于免疫缺陷者而言。营养不良也是导致内脏利什曼病的重要危险因素之一。

南美的皮肤黏膜利什曼病主要由巴西利什曼原虫引起,需要积极治疗,因为口腔、腭、咽和鼻部的黏膜溃疡可能会造成明显的面部改变。皮肤利什曼病(东方疮)则可由热带或大型利什曼原虫以及巴西、墨西哥或秘鲁利什曼原虫引起,在北至美国德克萨斯州的地方也有报道,症状通常首先在昆虫叮咬处出现一小结节,随后结痂或破溃,并愈合缓慢。从皮肤溃疡边缘采集组织样本进行培养或检测,常能发现利什曼原虫。

中文名称 英文名称 CAS号 化学式 结构式图片
羟芪巴脒 Hidroxiestilbamidina 495-99-8 C16H16N4O
羟芪巴脒
枸橼酸乙胺嗪 N,N-diethyl-4-methylpiperazine-1-carboxamide dihydrogen citrate 1642-54-2 C6H8O7*C10H21N3O
枸橼酸乙胺嗪
斯锑黑克 Stibogluconate 100817-46-7 C12H20O17Sb2
斯锑黑克
喷他脒 pentamidine 100-33-4 C19H24N4O2
喷他脒
伊维菌素 B1a 5-O-demethyl-22,23-dihydro-avermectin A1a 71827-03-7 C48H74O14
伊维菌素 B1a
乙胺嗪 diethylcarbamazine 90-89-1 C10H21N3O
乙胺嗪
—— (1R,4S,5'S,6R,6'R,8R,12S,13S,20R,21R,24S)-6'-[(2S)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one 70288-86-7 C48H74O14
(1R,4S,5'S,6R,6'R,8R,12S,13S,20R,21R,24S)-6'-[(2S)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
—— (1R,4S,5'S,6R,6'R,8R,10E,13S,14E,16E,20R,21R,24S)-6'-[(2S)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one 70288-86-7 C48H74O14
(1R,4S,5'S,6R,6'R,8R,10E,13S,14E,16E,20R,21R,24S)-6'-[(2S)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
—— (1R,4S,6R,10E,14E,16E,21R)-6'-butan-2-yl-21,24-dihydroxy-12-[(2R,4S,6S)-5-[(2S,4S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one 70288-86-7 C48H74O14
(1R,4S,6R,10E,14E,16E,21R)-6'-butan-2-yl-21,24-dihydroxy-12-[(2R,4S,6S)-5-[(2S,4S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
—— Hydroxystilbamidine 495-99-8 C16H16N4O
Hydroxystilbamidine
—— 2-epi-Ivermectin B1a 70288-86-7 C48H74O14
2-epi-Ivermectin B1a
—— (1R,4S,5'S,6R,6'S,8R,10E,12S,13S,14E,16E,20R,21R,24S)-6'-[(2S)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one 70288-86-7 C48H74O14
(1R,4S,5'S,6R,6'S,8R,10E,12S,13S,14E,16E,20R,21R,24S)-6'-[(2S)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
—— Pentostam 16037-91-5 C12H37Na3O26Sb2
Pentostam
—— (1R,4S,5'S,6R,6'R,8R,12S,13S,20R,21R,24S)-6'-[(2R)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one 70288-86-7 C48H74O14
(1R,4S,5'S,6R,6'R,8R,12S,13S,20R,21R,24S)-6'-[(2R)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
—— Pharmakon1600-01300027 70288-86-7 C48H74O14
Pharmakon1600-01300027
—— (6R,24S)-6'-butan-2-yl-21,24-dihydroxy-12-[5-(5-hydroxy-4-methoxy-6-methyloxan-2-yl)oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one 70288-86-7 C48H74O14
(6R,24S)-6'-butan-2-yl-21,24-dihydroxy-12-[5-(5-hydroxy-4-methoxy-6-methyloxan-2-yl)oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
—— ivermectin 70288-86-7 C48H74O14
ivermectin
—— Sodium stibogluconate 16037-91-5 C12H36Na3O26Sb2+
Sodium stibogluconate
—— (1R,4S,5'S,6R,6'R,8R,12S,13S,14E,16E,20R,21R,24S)-6'-[(2S)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one 70288-86-7 C48H74O14
(1R,4S,5'S,6R,6'R,8R,12S,13S,14E,16E,20R,21R,24S)-6'-[(2S)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
—— (1S,4S,5'S,6R,6'R,8R,10E,12S,13S,14E,20R,21R,24S)-6'-[(2S)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one 70288-86-7 C48H74O14
(1S,4S,5'S,6R,6'R,8R,10E,12S,13S,14E,20R,21R,24S)-6'-[(2S)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
—— (1R,4S,5'S,6R,6'R,8R,10E,12S,13S,14E,16E,20R,21R,24S)-6'-[(2S)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6R)-5-[(2S,4S,5S,6R)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one 70288-86-7 C48H74O14
(1R,4S,5'S,6R,6'R,8R,10E,12S,13S,14E,16E,20R,21R,24S)-6'-[(2S)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6R)-5-[(2S,4S,5S,6R)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
—— (1R,4S,5'S,6R,6'R,8R,10E,12S,13S,14E,20R,21R,24S)-6'-[(2S)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one 70288-86-7 C48H74O14
(1R,4S,5'S,6R,6'R,8R,10E,12S,13S,14E,20R,21R,24S)-6'-[(2S)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
—— 6'-Butan-2-yl-21,24-dihydroxy-12-[5-(5-hydroxy-4-methoxy-6-methyloxan-2-yl)oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one 70288-86-7 C48H74O14
6'-Butan-2-yl-21,24-dihydroxy-12-[5-(5-hydroxy-4-methoxy-6-methyloxan-2-yl)oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one