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-[(2S,4S,5R,6R)-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

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 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-[(2S,4S,5R,6R)-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
• 化学式: C₄₃H₇₅NO₁₆
• 分子量: 862.1
• InChiKey: NSYZCCDSJNWWJL-ZTMHJJSSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  60
• 可旋转键数：
  14
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.91
• 拓扑面积：
  226
• 氢给体数：
  4
• 氢受体数：
  17

ADMET

毒理性

• 人类毒性摘录

在超敏反应中包括发热、嗜酸性粒细胞增多和皮肤疹，每一种都可能出现单独或联合；停止治疗不久后它们就会消失。...可能会产生刺激性影响。口服给药...常伴有上腹部不适，可能相当严重。/红霉素/

AMONG HYPERSENSITIVITY REACTIONS ARE FEVER, EOSINOPHILIA, & SKIN ERUPTIONS, EACH OF WHICH MAY OCCUR ALONE OR IN COMBINATION; THEY DISAPPEAR SHORTLY AFTER THERAPY IS STOPPED. ...MAY PRODUCE IRRITATIVE EFFECTS. ORAL ADMIN...FREQUENTLY ACCOMPANIED BY EPIGASTRIC DISTRESS, WHICH MAY BE QUITE SEVERE. /ERYTHROMYCIN/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

静脉注射超过100毫克的剂量会产生...严重疼痛...持续数小时；静脉输注1克剂量...几乎经常会导致血栓性静脉炎。 ...6名患者...在以4克/天...静脉给药治疗期间出现了听力困难。 ...停止治疗后...听力完全恢复正常... /红霉素/

IM INJECTION OF QUANTITIES LARGER THAN 100 MG PRODUCES...SEVERE PAIN... PERSISTS FOR HR: IV PERFUSIONS OF 1-G DOSES...ALMOST REGULARLY IS FOLLOWED BY THROMBOPHLEBITIS. ...6 PT...DEVELOPED DIFFICULTY IN HEARING WHILE BEING TREATED WITH 4 G/DAY...IV. ... CESSATION...LED TO COMPLETE RETURN OF NORMAL HEARING... /ERYTHROMYCIN/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

一个60岁女性因使用红霉素乙基琥珀酸酯治疗导致肝毒性的病例报告。

A CASE REPORT OF HEPATOTOXICITY RESULTING FROM ERYTHROMYCIN ETHYLSUCCINATE THERAPY IN 60-YR-OLD FEMALE IS DESCIRBED.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

红霉素琥乙酯在肠道中部分解离；红霉素和未解离的酯都能被吸收，在血液中，酯被水解以释放游离的红霉素。

ERYTHROMYCIN ETHYLSUCCINATE IS PARTIALLY DISSOCIATED IN INTESTINE; BOTH ERYTHROMYCIN & UNDISSOCIATED ESTER ARE ABSORBED &, IN THE BLOOD, THE ESTER IS HYDROLYZED TO RELEASE FREE ERYTHROMYCIN.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

红霉素琥乙酯...在口服给药后能够充分吸收，尤其是当胃部为空时。在服用500毫克片剂后1到2小时内，血浆中的峰浓度达到1.5微克/毫升（0.5微克/毫升的碱基）。

ERYTHROMYCIN ETHYLSUCCINATE...IS ADEQUATELY ABSORBED FOLLOWING ORAL ADMINISTRATION, PARTICULARLY WHEN THE STOMACH IS EMPTY. PEAK CONCENTRATIONS IN PLASMA ARE 1.5 UG/ML (0.5 UG/ML OF BASE) 1 TO 2 HR AFTER ADMINISTRATION OF A 500 MG TABLET.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

在患者中，红霉素的平均胆汁水平大约是静脉注射（红霉素乳糖酸盐）和肌肉注射（红霉素琥珀酸酯）1小时后相应血清浓度的10倍。

IN PATIENTS, MEAN BILE LEVELS OF ERYTHROMYCIN WERE APPROXIMATELY 10 TIMES HIGHER THAN CORRESPONDING SERUM CONCN 1 HR AFTER IV (ERYTHROMYCIN LACTOBIONATE) & IM (ERYTHROMYCIN SUCCINATE) INJECTION.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

在健康的成年受试者以及患有支气管感染的成年患者中，研究了不同剂型的红霉素的药代动力学。红霉素琥乙酯比红霉素硬脂酸盐更适合口服治疗，因为它的吸收快速且一致。

IN HEALTHY ADULT SUBJECTS & IN ADULT PATIENTS WITH BRONCHIAL INFECTIONS, PHARMACOKINETICS OF VARIOUS FORMULATIONS OF ERYTHROMYCIN WERE STUDIED. ERYTHROMYCIN ETHYLSUCCINATE WAS BETTER THAN ERYTHROMYCIN STEARATE FOR ORAL TREATMENT IN THAT IT WAS RAPIDLY & CONSISTENTLY ABSORBED.

来源:Hazardous Substances Data Bank (HSDB)