Oxytetracycline, disodium salt, dihydrate | 6153-65-7

• 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: Oxytetracycline, disodium salt, dihydrate
• 英文别名: disodium;(5S,5aR,6S,6aR,7S,10aR)-9-carbamoyl-7-(dimethylamino)-5,6,10,10a-tetrahydroxy-5-methyl-8,11-dioxo-5a,6,6a,7-tetrahydrotetracene-1,12-diolate;dihydrate
• CAS: 6153-65-7
• 化学式: C22H26N2Na2O11
• 分子量: 540.4
• InChiKey: WIEGFTCXYMUOEJ-ODQZHCRPSA-L

计算性质

• 辛醇/水分配系数(LogP)：
  -10.87
• 重原子数：
  37
• 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：
  210
• 氢给体数：
  7
• 氢受体数：
  12

ADMET

毒理性

• 相互作用

同时服用铁剂（硫酸亚铁）显著降低了人体中...土霉素...的血清浓度。同时给予牛奶会减少大约50%的...土霉素...吸收。

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

土霉素可能会导致血糖水平出现不可预测的波动...通过增加胰岛素的半衰期。同时使用土霉素和甲磺丁脲时也应注意。

... 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的临床观察中发现了显著的拮抗作用... /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，协助通气。通过非循环呼吸面罩以10至15升/分钟的速度给予氧气。监测肺水肿，如有必要，进行治疗……。监测休克，如有必要，进行治疗……。预防癫痫发作，如有必要，进行治疗……。对于眼睛污染，立即用水冲洗眼睛。在运输过程中，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...分别为静脉注射和肌肉注射后的15.7小时和10.5小时。...一个因素/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

当胃为空时，口服剂量的吸收百分比（对于土霉素）为60至80%... 单次口服剂量后，土霉素的血浆峰浓度在大约2到4小时内达到... 它的半衰期在6到12小时之间... 通常每天给药2到4次... 每6小时给药250毫克可产生2至2.5微克/毫升的血浆峰浓度... 将剂量增加到每6小时超过1克并不会显著提高血浆浓度... 大约10到35%的土霉素剂量以活性形式在尿液中排出，在给药后30分钟内可检测到，大约在给药后5小时达到峰值浓度。

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

/土霉素与血浆蛋白的结合...大约...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

吸收在下半身要少得多......胆汁浓度......是血浆的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)