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：
- 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。
- 军团菌病。
- 支原体属感染。
- 衣原体属感染。
- 百日咳。
- 白喉带菌者。
- 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：
- 肝毒性：表现为胆汁淤积、肝酶升高，通常在停药后可恢复。
- 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。
- 过敏反应：主要表现为药物热、皮疹和荨麻疹等。
- 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 |
|---|---|---|---|---|
| 麦迪霉素 | Midecamycin | 35457-80-8 | C41H67NO15 |
|
| 阿波霉素 | Albomycin | 1414-39-7 | C36H58FeN10O18S+3 |
|
| 阿奇霉素 | Zithromax(R) | 83905-01-5 | C38H72N2O12 |
|
| 醋酸麦迪霉素 | miokamycin | 55881-07-7 | C45H71NO17 |
|
| 酒石酸吉他霉素 | Kitasamycin tartrate | 37280-56-1 | C40H67NO18 |
|
| 螺旋霉素 | ex Streptomyces ambofaciens | 8025-81-8 | C43H74N2O14 |
|
| 罗红霉素杂质D | (Z)-roxithromycin | 134931-00-3 | C41H76N2O15 |
|
| 罗红霉素 | roxithromycin | 80214-83-1 | C41H76N2O15 |
|
| 罗他霉素 | rokitamycin | 74014-51-0 | C42H69NO15 |
|
| 红霉素 | erythromycin | 114-07-8 | C37H67NO13 |
|
| 竹桃霉素三乙酸酯 | troleandomycin | 2751-09-9 | C41H67NO15 |
|
| 竹桃霉素 | oleandomycin phosphate | 7060-74-4 | C35H61NO12*H3O4P |
|
| 硬脂酸红霉素 | erythromycin stearate | 643-22-1 | C18H36O2*C37H67NO13 |
|
| 琥乙红霉素 | erythromycin ethylsuccinate | 1264-62-6 | C43H75NO16 |
|
| 环酯红霉素 | Erythromycin A cyclic 11,12-carbonate | 55224-05-0 | C38H65NO14 |
|
| 泰利霉素 | telithromycin | 191114-48-4 | C43H65N5O10 |
|
| 氟红霉素 | Flurithromycin | 82664-20-8 | C37H66FNO13 |
|
| 柱晶白霉素 | 2-[(4R,5S,6S,7R,9R,10R,16R)-6-[(2S,3R,4R,5S,6R)-5-[(2S,4R,5S,6S)-4,5-dihydroxy-4,6-dimethyloxan-2-yl]oxy-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-4,10-dihydroxy-5-methoxy-9,16-dimethyl-2-oxo-1-oxacyclohexadeca-11,13-dien-7-yl]acetaldehyde | 1392-21-8 | C35H59NO13 |
|
| 地红霉素 | Dirithromycin | 62013-04-1 | C42H78N2O14 |
|
| 克拉霉素 | clarithromycin | 81103-11-9 | C38H69NO13 |
|
| 依托红霉素 | erythromycin estolate | 3521-62-8 | C12H26O4S*C40H71NO14 |
|
| 交沙霉素 | josamycin | 16846-24-5 | C42H69NO15 |
|
| 乳糖酸红霉素 | erythromycin lactobionate | 3847-29-8 | C12H22O12*C37H67NO13 |
|
| 乙酰螺旋霉素 | Acetylspiramycin | 24916-51-6 | C45H76N2O15 |
|
| —— | (7R,13S)-6-[(2S)-4-(Dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-4-[(4R)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-10-(2-methoxyethoxymethoxyimino)-3,5,7,9,11,13-hexamethyl-oxacyclotetradecan-2-one | 80214-83-1 | C41H76N2O15 |
|
| —— | (3S,5S,6S,7R,8S,9R,12R,13R,14S,15R)-6-[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-14-hydroxy-8-[(2R,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-5,7,9,12,13,15-hexamethyl-1,11-dioxaspiro[2.13]hexadecane-10,16-dione;phosphoric acid | 7060-74-4 | C35H64NO16P |
|
| —— | [(11E,13E)-6-[(2S,3R,4R,5S,6R)-4-(dimethylamino)-3-hydroxy-5-[(2S,4R,5R,6R)-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 |
|
| —— | 2-[(4R,5S,6S,7R,9R,10R,11E,13E,16S)-6-[(2S,3R,4R,5S,6R)-5-[(2R,4S,5R,6R)-4,5-dihydroxy-4,6-dimethyloxan-2-yl]oxy-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-10-[(2R,5S,6S)-5-(dimethylamino)-6-methyloxan-2-yl]oxy-4-hydroxy-5-methoxy-9,16-dimethyl-2-oxo-1-oxacyclohexadeca-11,13-dien-7-yl]acetaldehyde | 8025-81-8 | C43H74N2O14 |
|
| —— | Ketek (TN) | 191114-48-4 | C43H65N5O10 |
|
| —— | (2R,3S,4R,5R,8R,10R,11R,13S,14R)-11-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-3,4,10-trihydroxy-13-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-3,5,6,8,10,12,14-heptamethyl-1-oxa-6-azacyclopentadecan-15-one | 83905-01-5 | C38H72N2O12 |
|
| —— | [(2S,3S,4R,6S)-6-[(2R,3S,4R,5R,6S)-6-[[(4R,5S,6S,7R,9R,10R,16R)-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 |
|
| —— | Eromycin | 3521-62-8 | C52H97NO18S |
|
| —— | Oleandocetin | 2751-09-9 | C41H67NO15 |
|
| —— | 4-O-[(2R,3S,4R,6S)-4-(dimethylamino)-2-[[(3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-3,5,7,9,11,13-hexamethyl-2,10-dioxo-oxacyclotetradec-6-yl]oxy]-6-methyloxan-3-yl] 1-O-ethyl butanedioate | 1264-62-6 | C43H75NO16 |
|
| —— | (2R,3S,4R,5R,8S,10R,11R,12S,13S,14R)-11-[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-3,4,10-trihydroxy-13-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-3,5,6,8,10,12,14-heptamethyl-1-oxa-6-azacyclopentadecan-15-one | 83905-01-5 | C38H72N2O12 |
|
| —— | [(4R,5S,6S,7R,9R,10R,16R)-6-[(2S,3R,4R,5S,6R)-4-(dimethylamino)-3-hydroxy-5-[(2S,4R,5S,6S)-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 |
|
| —— | (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-11-{[4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy}-2-ethyl-3,4,10-trihydroxy-13-[(5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl)oxy]-3,5,6,8,10,12,14-heptamethyl-1-oxa-6-azacyclopentadecan-15-one | 83905-01-5 | C38H72N2O12 |
|
| —— | (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-11-[(3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyl-tetrahydropyran-2-yl]oxy-2-ethyl-3,4,10-trihydroxy-13-[(4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyl-tetrahydropyran-2-yl]oxy-3,5,6,8,10,12,14-heptamethyl-1-oxa-6-azacyclopentadecan-15-one | 122463-26-7 | C38H72N2O12 |
|
| —— | Spiramycin II | 24916-51-6 | C45H76N2O15 |
|
| —— | Leucomycin V, 9-O-((2R,5S,6R)-5-(dimethylamino)tetrahydro-6-methyl-2H-pyran-2-yl)-, 3-acetate | 24916-51-6 | C45H76N2O15 |
|
| —— | Spiramycin I | 8025-81-8 | C43H74N2O14 |
|
| —— | troleandomycin (TAO) | 2751-09-9 | C41H67NO15 |
|
| —— | (10E)-6-[4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-4-(5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl)oxy-10-(2-methoxyethoxymethoxyimino)-3,5,7,9,11,13-hexamethyl-oxacyclotetradecan-2-one | 80214-83-1 | C41H76N2O15 |
|
| —— | 2-[(11Z,13Z)-6-[5-(4,5-dihydroxy-4,6-dimethyloxan-2-yl)oxy-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-10-[5-(dimethylamino)-6-methyloxan-2-yl]oxy-4-hydroxy-5-methoxy-9,16-dimethyl-2-oxo-1-oxacyclohexadeca-11,13-dien-7-yl]acetaldehyde | 8025-81-8 | C43H74N2O14 |
|
| —— | (3R,4S,5S,6R,7R,9R,10Z,11S,12R,13S,14R)-6-[4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-4-(5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl)oxy-10-(2-methoxyethoxymethoxyimino)-3,5,7,9,11,13-hexamethyl-oxacyclotetradecan-2-one | 80214-83-1 | C41H76N2O15 |
|
| —— | Medemycin | 35457-80-8 | C41H67NO15 |
|
| —— | [(4R,5S,6S,7R,9R,10S,16R)-6-[(2R,3R,4R,5S,6R)-4-(dimethylamino)-3-hydroxy-5-[(2S,4R,5S,6S)-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 |
|
| —— | [(11E,13Z)-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 |
|
| —— | Rovamycin | 8025-81-8 | C43H74N2O14 |
|
| —— | [6-[6-[[(4R,5S,6S,7R,9R,10R,11E,13E,16R)-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 |
|
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