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大环内酯类药

大环内酯类(Macrolides)是由链霉菌产生的弱碱性抗生素,因其分子结构中含有一个十四员或十六员的大环内酯结构而得名。这类抗生素作用于细菌细胞核糖体50 S亚单位,阻碍蛋白质的合成,属于生长期抑菌剂。大环内酯类药物具有相似的抗菌谱和活性,主要针对革兰阳性菌、军团菌属、衣原体属、支原体属以及厌氧菌等。

大环内酯类的主要适应证包括:

  1. 由青霉素耐药的革兰阳性球菌(特别是葡萄球菌属)引起的感染。
  2. 军团菌病。
  3. 支原体属感染。
  4. 衣原体属感染。
  5. 百日咳。
  6. 白喉带菌者。
  7. 风湿热和心内膜炎的预防,尤其是对青霉素过敏的患者。这类药物特别适用于轻至中度呼吸系统感染患者的口服治疗。

大环内酯类的不良反应包括:

  1. 肝毒性:表现为胆汁淤积、肝酶升高,通常在停药后可恢复。
  2. 耳鸣和听觉障碍:静脉给药时可能出现,通过减少剂量或停止给药可以缓解。
  3. 过敏反应:主要表现为药物热、皮疹和荨麻疹等。
  4. 局部刺激:注射给药可能引起局部刺激,因此不宜肌注;静滴时应稀释(<0.1%)并缓慢推注以减少静脉炎的发生。
中文名称 英文名称 CAS号 化学式 结构式图片
—— [6-[3-acetyloxy-4-(dimethylamino)-6-methyloxan-2-yl]oxy-8-(5-acetyloxy-4-methoxy-6-methyloxan-2-yl)oxy-5,7,9,12,13,15-hexamethyl-10,16-dioxo-1,11-dioxaspiro[2.13]hexadecan-14-yl] acetate 2751-09-9 C41H67NO15
[6-[3-acetyloxy-4-(dimethylamino)-6-methyloxan-2-yl]oxy-8-(5-acetyloxy-4-methoxy-6-methyloxan-2-yl)oxy-5,7,9,12,13,15-hexamethyl-10,16-dioxo-1,11-dioxaspiro[2.13]hexadecan-14-yl] acetate
—— 8-[4-(Dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-9-methoxy-1,5,7,9,11,13-hexamethyl-15-[4-(4-pyridin-3-ylimidazol-1-yl)butyl]-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,6,12,16-tetrone 191114-48-4 C43H65N5O10
8-[4-(Dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-9-methoxy-1,5,7,9,11,13-hexamethyl-15-[4-(4-pyridin-3-ylimidazol-1-yl)butyl]-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,6,12,16-tetrone
—— [6-[4-(Dimethylamino)-3-hydroxy-5-(4-hydroxy-4,6-dimethyl-5-propanoyloxyoxan-2-yl)oxy-6-methyloxan-2-yl]oxy-10-hydroxy-5-methoxy-9,16-dimethyl-2-oxo-7-(2-oxoethyl)-1-oxacyclohexadeca-11,13-dien-4-yl] propanoate 35457-80-8 C41H67NO15
[6-[4-(Dimethylamino)-3-hydroxy-5-(4-hydroxy-4,6-dimethyl-5-propanoyloxyoxan-2-yl)oxy-6-methyloxan-2-yl]oxy-10-hydroxy-5-methoxy-9,16-dimethyl-2-oxo-7-(2-oxoethyl)-1-oxacyclohexadeca-11,13-dien-4-yl] propanoate
—— [6-[6-[[4-Acetyloxy-10-hydroxy-5-methoxy-9,16-dimethyl-2-oxo-7-(2-oxoethyl)-1-oxacyclohexadeca-11,13-dien-6-yl]oxy]-4-(dimethylamino)-5-hydroxy-2-methyloxan-3-yl]oxy-4-hydroxy-2,4-dimethyloxan-3-yl] 3-methylbutanoate 16846-24-5 C42H69NO15
[6-[6-[[4-Acetyloxy-10-hydroxy-5-methoxy-9,16-dimethyl-2-oxo-7-(2-oxoethyl)-1-oxacyclohexadeca-11,13-dien-6-yl]oxy]-4-(dimethylamino)-5-hydroxy-2-methyloxan-3-yl]oxy-4-hydroxy-2,4-dimethyloxan-3-yl] 3-methylbutanoate
—— butanedioic acid O4-[4-(dimethylamino)-2-[[14-ethyl-7,12,13-trihydroxy-4-[(5-hydroxy-4-methoxy-4,6-dimethyl-2-oxanyl)oxy]-3,5,7,9,11,13-hexamethyl-2,10-dioxo-oxacyclotetradec-6-yl]oxy]-6-methyl-3-oxanyl] ester O1-ethyl ester 1264-62-6 C43H75NO16
butanedioic acid O4-[4-(dimethylamino)-2-[[14-ethyl-7,12,13-trihydroxy-4-[(5-hydroxy-4-methoxy-4,6-dimethyl-2-oxanyl)oxy]-3,5,7,9,11,13-hexamethyl-2,10-dioxo-oxacyclotetradec-6-yl]oxy]-6-methyl-3-oxanyl] ester O1-ethyl ester