(4R,4aS,5R,5aS,6R,12aS)-4-(dimethylamino)-1,5,6,10,11,12a-hexahydroxy-6-methyl-3,12-dioxo-4,4a,5,5a-tetrahydrotetracene-2-carboxamide

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 四环素类
• 英文名称: (4R,4aS,5R,5aS,6R,12aS)-4-(dimethylamino)-1,5,6,10,11,12a-hexahydroxy-6-methyl-3,12-dioxo-4,4a,5,5a-tetrahydrotetracene-2-carboxamide
• 化学式: C₂₂H₂₄N₂O₉
• 分子量: 460.4
• InChiKey: OWFJMIVZYSDULZ-BHOONSPOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.6
• 重原子数：
  33
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  202
• 氢给体数：
  7
• 氢受体数：
  10

ADMET

毒理性

• 相互作用

同时给予的铁（硫酸亚铁）减少了吸收，导致人体血清中...土霉素...的浓度显著下降。同时给予的牛奶使...土霉素...的吸收减少了大约50%...。

SIMULTANEOUS ADMIN IRON AS FERROUS SULFATE REDUCED ABSORPTION & CAUSED SIGNIFICANT DECR IN SERUM CONCN OF ... OXYTETRACYCLINE ... IN MAN. ... MILK GIVEN SIMULTANEOUSLY REDUCED ABSORPTION OF ... OXYTETRACYCLINE BY ABOUT 50% ... .

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

由于溴己新治疗导致鼻粘液粘度降低而产生的蒸发，使氧四环素在鼻粘液中的浓度增加...而不是因为增加膜透性。

INCR CONCN OF OXYTETRACYCLINE IN NASAL MUCUS DUE TO BROMHEXINE TREATMENT ... ATTRIBUTED TO EVAPORATION OF THE LESS VISCOUS MUCUS, ARISING FROM BROMHEXINE TREATMENT, RATHER THAN INCR MEMBRANE PERMEABILITY.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

...土霉素可能导致血糖水平不可预测的波动...通过增加胰岛素的半衰期。 ...同时...当土霉素和甲磺丁脲...同时使用。

... OXYTETRACYCLINE MAY CAUSE UNPREDICTABLE FLUCTUATIONS IN BLOOD GLUCOSE LEVELS ... BY INCR HALF-LIFE OF INSULIN. ... ALSO ... WHEN OXYTETRACYCLINE & TOLBUTAMIDE ... USED CONCURRENTLY.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

青霉素和四环素之间在肺炎球菌性脑膜炎临床上观察到了显著的拮抗作用... /四环素/

Striking antagonism between penicillin and tetracyclines has been observed clinically in pneumococcal meningitis ... /Tetracyclines/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

/SRP:/ 基本治疗：建立专利气道（如有需要，使用口咽或鼻咽气道）。如有必要，进行吸痰。密切观察呼吸不足的迹象，如有需要，进行辅助通气。通过非重复呼吸面罩以10至15升/分钟的速度给予氧气。监测肺水肿，并在必要时进行治疗……。监测休克，并在必要时进行治疗……。预防癫痫发作，并在必要时进行治疗……。对于眼睛污染，立即用水冲洗眼睛。在转运过程中，用0.9%的生理盐水（NS）持续冲洗每只眼睛……。不要使用催吐剂。对于摄入，如果患者能够吞咽、有强烈的干呕反射且不流口水，则用温水冲洗口腔，并给予5毫升/千克，最多200毫升的水进行稀释……。在去污后，用干燥的无菌敷料覆盖皮肤烧伤……。/毒药A和B/

/SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 ml/kg up to 200 ml of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poisons A and B/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

血清半衰期...在马中是...静脉注射后15.7小时和肌肉注射后10.5小时。...可能是剂量依赖性动力学的影响...。

SERUM HALF-LIFE ... IN HORSES IS ... 15.7 HR & 10.5 HR AFTER IV & IM INJECTIONS, RESPECTIVELY. ... /A FACTOR/ MAY BE THE INFLUENCE OF DOSE-DEPENDENT KINETICS ... .

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

四环素类药物口服剂量吸收率（胃空腹时）可达60%至80%...单次口服剂量后，2至4小时可达四环素血药浓度峰值...其半衰期在6至12小时之间...通常每日2至4次给药...每6小时给药250毫克可产生2至2.5微克/毫升的血药峰值浓度...将剂量增加到每6小时超过1克并不会显著提高血药浓度...大约10%至35%的四环素剂量以活性形式在尿液中排出，给药后30分钟内可检测到，大约5小时后达到峰值浓度。

The percentage of an oral dose that is absorbed (when the stomach is empty) ... for oxytetracycline /is/ 60 to 80% ... After a single oral dose, the peak plasma concn /of oxytetracycline/ is attained in 2 to 4 hr. /It has a half-life/ in the range of 6 to 12 hr and ... frequently admin 2 to 4 times daily ... The admin of 250 mg every 6 hr produces peak plasma concn of 2 to 2.5 ug/mL ... Increasing the dosage above 1 g every 6 hr does not produce significantly higher plasma concn ... Approx 10 to 35% of a dose of oxytetracycline is excreted in active form in urine, in which it is detectable within 30 min and reaches a peak concn about 5 hr after it is admin.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

四环素与血浆蛋白的结合率大约为20-25%。

/Oxytetracycline is/ bound to plasma proteins ... approx ... 20-25%.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

吸收从下...道...胆汁浓度...比...血浆高5到10倍。/四环素/

/Absorption is/ much less complete from lower ... tract ... Biliary concn ... /is/ 5 to 10 times higher than ... plasma. /Tetracyclines/

来源:Hazardous Substances Data Bank (HSDB)

反应信息

• 作为反应物：
  描述：

  (4R,4aS,5R,5aS,6R,12aS)-4-(dimethylamino)-1,5,6,10,11,12a-hexahydroxy-6-methyl-3,12-dioxo-4,4a,5,5a-tetrahydrotetracene-2-carboxamide 生成 doxycycline
  参考文献：
  名称：

  Process for the catalytic reduction of 6-hydroxy hydronaphthacenes

  摘要：

  公开号：

  US03019260A1