(3S,4R,5R,6S,7S,9S,12R,14S)-6-[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-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-oxacyclotetradecane-2,10-dione;octadecanoic acid

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (3S,4R,5R,6S,7S,9S,12R,14S)-6-[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-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-oxacyclotetradecane-2,10-dione;octadecanoic acid
• 化学式: C55H103NO15
• 分子量: 1018.4
• InChiKey: YAVZHCFFUATPRK-JGJPHTNUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  8.12
• 重原子数：
  71
• 可旋转键数：
  23
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.95
• 拓扑面积：
  231
• 氢给体数：
  6
• 氢受体数：
  16

ADMET

代谢

它在小肠和组织中被水解以产生红霉素。

IT IS HYDROLYZED IN SMALL INTESTINE & IN TISSUES TO YIELD ERYTHROMYCIN.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

据报道，一位77岁的妇女每天维持服用7.5毫克的华法林，在服用口服红霉素硬脂酸酯，500毫克，每日四次后，其凝血酶原时间延长至64秒（正常对照为11秒）。

A 77-YR-OLD WOMAN IS REPORTEDLY MAINTAINED ON 7.5 MG OF WARFARIN DAILY IN WHOM THE ADMIN OF ORAL ERYTHROMYCIN STEARATE, 500 MG 4 TIMES A DAY, RESULTED IN A PROTHROMBIN TIME OF 64 SECONDS (CONTROL, 11 SECONDS).

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

在所有过敏反应中，包括发热、嗜酸性粒细胞增多和皮肤疹，这些症状可能会单独出现或组合出现；每种症状都会在停止治疗后不久消失。...常产生刺激性影响。口服给药...常伴有上腹部不适，可能非常严重。/红霉素/

AMONG ALLERGIC REACTIONS ARE FEVER, EOSINOPHILIA, & SKIN ERUPTIONS, WHICH MAY OCCUR ALONE OR IN COMBINATION; EACH DISAPPEARS SHORTLY AFTER THERAPY IS STOPPED. ...OFTEN PRODUCES IRRITATIVE EFFECTS. ORAL ADMIN...FREQUENTLY ACCOMPANIED BY EPIGASTRIC DISTRESS, WHICH MAY BE QUITE SEVERE. /ERYTHROMCYIN/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

静脉注射超过100毫克的量会产生极度剧烈的疼痛，持续数小时。静脉滴注1克剂量...几乎经常会导致血栓性静脉炎。/红霉素/

IM INJECTION OF QUANTITIES LARGER THAN 100 MG PRODUCES EXTREMELY SEVERE PAIN THAT PERSISTS FOR HOURS. IV INFUSION OF 1-G DOSES...ALMOST REGULARLY IS FOLLOWED BY THROMBOPHLEBITIS. /ERYTHROMYCIN/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

...SGOT/血清谷草转氨酶/轻度升高也出现在...97名使用硬脂酸红霉素治疗的病人中的3名...

...MILD ELEVATIONS OF THE SGOT /SERUM GLUTAMIC-OXALOACETIC TRANSAMINASE/ WERE ALSO NOTED IN...3 OF 97 PT TREATED WITH ERYTHROMYCIN STEARATE...

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

一位60岁的男性在服用两片红霉素硬脂酸酯片后出现了严重的呼吸窘迫。作者们建议，在临床病程中，I型和III型过敏反应参与了病情的发展。

SEVERE RESP DISTRESS DEVELOPED IN A 60-YR-OLD MAN AFTER INGESTION OF 2 TABLETS OF ERYTHROMYCIN STEARATE. AUTHORS SUGGEST AN ALLERGIC REACTION OF TYPE 1 & TYPE 3 PARTICIPATED IN COURSE OF CLINICAL PICTURE.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

血浆中峰值浓度...口服250毫克碱基后4小时为0.3-0.5微克/毫升，500毫克片剂后为0.3-1.9微克/毫升。已经制备了红霉素的各种酯以...提高稳定性和促进吸收。如果口服硬脂酸盐，血浆中的红霉素浓度几乎没有差异。

PEAK CONCN IN PLASMA...0.3-0.5 UG/ML 4 HR AFTER ORAL ADMIN OF 250 MG OF BASE & ARE 0.3-1.9 UG/ML AFTER...500-MG TABLET. VARIOUS ESTERS OF ERYTHROMYCIN HAVE BEEN PREPARED TO...IMPROVE STABILITY & FACILITATE ABSORPTION. ...CONCN OF ERYTHROMYCIN IN PLASMA ARE LITTLE DIFFERENT IF STEARATE IS GIVEN ORALLY.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

...容易扩散进入细胞内液体，& 抗菌活性...在...所有部位实现，除了大脑和脑脊液。 ...是少数能够渗透到前列腺液的抗生素之一，浓度大约是...血浆的40%。与血浆蛋白的结合程度...各不相同...可能超过所有.../药物形态的70%。 /红霉素/

...DIFFUSES READILY INTO INTRACELLULAR FLUIDS, & ANTIBACTERIAL ACTIVITY... ACHIEVED AT...ALL SITES EXCEPT BRAIN & CSF. ...ONE OF FEW ANTIBIOTICS THAT PENETRATES INTO PROSTATIC FLUID, CONCN ARE APPROX 40% OF...PLASMA. EXTENT OF BINDING...TO PLASMA PROTEINS VARIES...PROBABLY EXCEEDS 70% IN ALL.../FORMS OF DRUG/. /ERYTHROMYCIN/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

红霉素碱从小肠上段被充分吸收；它会被胃液灭活...胃中的食物会延迟其最终吸收。/红霉素/

ERYTHROMYCIN BASE IS ADEQUATELY ABSORBED FROM UPPER PART OF SMALL INTESTINE; IT IS INACTIVATED BY GASTRIC JUICE... FOOD IN STOMACH DELAYS ITS ULTIMATE ABSORPTION. /ERYTHROMYCIN/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

红霉素可穿过胎盘屏障；胎儿血浆中的药物浓度约为母体循环中浓度的5-20%。/红霉素/

ERYTHROMYCIN TRAVERSES PLACENTAL BARRIER; & CONCN OF DRUG IN FETAL PLASMA ARE ABOUT 5-20% OF THOSE IN MATERNAL CIRCULATION. /ERYTHROMYCIN/

来源:Hazardous Substances Data Bank (HSDB)