(5R)-2-[4-amino-3-[[3-amino-6-(aminomethyl)-3,4-dihydro-2H-pyran-2-yl]oxy]-6-(ethylamino)-2-hydroxycyclohexyl]oxy-5-methyl-4-(methylamino)oxane-3,5-diol

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (5R)-2-[4-amino-3-[[3-amino-6-(aminomethyl)-3,4-dihydro-2H-pyran-2-yl]oxy]-6-(ethylamino)-2-hydroxycyclohexyl]oxy-5-methyl-4-(methylamino)oxane-3,5-diol
• 化学式: C₂₁H₄₁N₅O₇
• 分子量: 475.6
• InChiKey: CIDUJQMULVCIBT-BWFLUJJFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -4.2
• 重原子数：
  33
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.9
• 拓扑面积：
  200
• 氢给体数：
  8
• 氢受体数：
  12

ADMET

毒理性

• 相互作用

通过任何途径同时和/或连续使用2种或更多氨基糖苷类药物，或同时使用卡普霉素和氨基糖苷类药物应予以避免，因为耳毒性、肾毒性和神经肌肉阻滞的可能性可能会增加；听力损失可能会发生，即使在停药后也可能进展为耳聋；听力损失可能是可逆的，但通常是永久性的；神经肌肉阻滞可能导致骨骼肌无力、呼吸抑制或麻痹（呼吸暂停）。此外，同时使用2种或更多氨基糖苷类药物可能会导致每种药物的细菌摄取减少，因为药物竞争同一摄取机制。/氨基糖苷类药物/

Concurrent and/or sequential use of 2 or more aminoglycosides by any route or concurrent use of capreomycin with aminoglycosides should be avoided since the potential for ototoxicity, nephrotoxicity, and neuromuscular blockade may be increased; hearing loss may occur and may progress to deafness even after discontinuation of the drug; loss of hearing may be reversible, but usually is permanent; neuromuscular blockade may result in skeletal muscle weakness and respiratory depression or paralysis (apnea). Also, concurrent use of 2 or more aminoglycosides may result in reduced bacterial uptake of each one since the medications compete for the same uptake mechanism. /Aminoglycosides/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

同时使用具有神经肌肉阻滞活性的药物，包括卤化烃吸入性麻醉药、阿片类止痛药和大量输注柠檬酸盐抗凝血液，与氨基糖苷类药物同时使用时应仔细监测，因为神经肌肉阻滞作用可能会增强，导致骨骼肌无力、呼吸抑制或麻痹（呼吸暂停）；在手术期间或术后期间同时使用这些药物和氨基糖苷类药物时应谨慎，尤其是在术后神经肌肉阻滞可能不完全逆转的情况下；使用抗胆碱酯酶药物或钙盐可能有助于逆转阻滞。 /氨基糖苷类药物/

Concurrent use of medications with neuromuscular blocking activity, including halogenated hydrocarbon inhalation anesthetics, opioid analgesics, and massive transfusions with citrate anticoagulated blood, with aminoglycosides should be carefully monitored since neuromuscular blockade may be enhanced, resulting in skeletal muscle weakness and respiratory depression or paralysis (apnea); caution is recommended when these medications and aminoglycosides are used concurrently during surgery or in the postoperative period, especially if there is a possibility of incomplete reversal of neuromuscular blockade postoperatively; treatment with anticholinesterase agents or calcium salts may help reverse the blockade. /Aminoglycosides/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

万古霉素和氨基糖苷类抗生素通常需要同时使用，以预防细菌性心内膜炎，治疗由链球菌和棒状杆菌引起的心内膜炎，治疗耐药性葡萄球菌感染，或者在青霉素过敏的患者中；适当的监测将有助于减少肾毒性或耳毒性的风险；可能需要测定肾功能、血清氨基糖苷类和万古霉素浓度、减少剂量和/或调整剂量间隔，或者更换其他抗生素。/氨基糖苷类/

Vancomycin and aminoglycosides must often be administered concurrently in the prophylaxis of bacterial endocarditis, in the treatment of endocarditis caused by streptococci and Corynebacteria species, in the treatment of resistant staphylococcal infections, or in penicillin-allergic patients; appropriate monitoring will help to reduce the risk of nephrotoxicity or ototoxicity; renal function determinations, serum aminoglycoside and vancomycin concentrations, dosage reductions, and/or dosage interval adjustments, or alternate antibacterials, may be required. /Aminoglycosides/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

这些药物与氨基糖苷类药物同时或连续使用可能会增加耳毒性和肾毒性的风险；可能会出现听力损失，甚至在停药后仍可能发展为耳聋，听力损失可能是可逆的，但通常是永久性的；在与其他耳毒性抗生素同时或连续使用时，可能需要进行系列的听力功能测定；可能需要进行肾功能测定。/氨基糖苷类药物/

Concurrent or sequential use of these medications /nephrotoxic or ototoxic medications/ with aminoglycosides may increase the potential for ototoxicity or nephrotoxicity; hearing loss may occur and may progress to deafness even after discontinuation of the drug and may be reversible, but usually is permanent; serial audiometric function determinations may be required with concurrent or sequential use of other ototoxic antibacterials; renal function determinations may be required. /Aminoglycosides/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

通过静脉、肌肉和皮下途径中毒。通过静脉途径的人体系统性影响：肾、输尿管和膀胱发生变化。

Poison by intravenous, intramuscular, and subcutaneous routes. Human systemic effects by intravenous route: changes to kidney, ureter, and bladder.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

Netilmicin口服给药后从完整的胃肠道吸收不良。该药物经肌内注射给药后迅速且完全吸收。

Netilmicin is poorly absorbed from the intact GI tract following oral administration. The drug is rapidly and completely absorbed following IM administration.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

奈替米星在吸收后迅速分布到组织、痰液以及心包液、滑液和腹膜液中...主要分布在细胞外液体积中...分布容积大约是体重的20%。据报道，药物的蛋白结合率为0-30%。

Following absorption, netilmicin rapidly distributes into tissues, sputum, and pericardial, synovial, and peritoneal fluids. ...distributed principally in the extracellular fluid volume... The volume of distribution ...is approximately 20% of body weight. The drug is reportedly 0-30% protein bound.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

庆大霉素可穿过胎盘，已在脐带血中检测到。少量药物会分布到乳汁中。

Netilmicin crosses the placenta and has been detected in cord blood. Small amounts of the drug are distributed into milk.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

...不经过代谢并以原型通过肾小球滤过主要在尿液中排泄。在肾功能正常的成人中，2毫克/公斤剂量的奈替米星有74%在24小时内以原型排泄：在肌酐清除率为30-80或10-30毫升/分钟或无肾功能的成人中，24小时内分别有55%、25%或15%的剂量通过尿液排泄。

...is not metabolized and is excreted unchanged in urine mainly by glomerular filtration. In adults with normal renal function, 74% of a 2 mg/kg dose of netilmicin is excreted unchanged within 24 horus: in adults with creatinine clearances of 30-80 or 10-30 mL/min or in anephric adults, 55, 25, or 15% of the dose is excreted in urine within 24 hours, respectively.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

庆大霉素可以通过血液透析去除。该药物也可以通过腹膜透析去除，但不如血液透析容易。

Netilmicin is removed by hemodialysis. The drug is also removed by peritoneal dialysis but less readily than by hemodialysis.

来源:Hazardous Substances Data Bank (HSDB)

文献信息

• Nitric oxide-releasing antibacterial polymers and scaffolds fabricated therefrom and methods pertaining thereto
  申请人：THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL

  公开号：US11421044B2

  公开（公告）日：2022-08-23

  Several embodiments of NO releasing structures are disclosed. In some embodiments, the structures are covalently modified to store and release nitric oxide. Some embodiments pertain to methods of making and use of these structures. The covalently modified polymer structures may be tailored to release nitric oxide in a controlled manner and are useful for treatment of various medical conditions.

  本文公开了几种一氧化氮释放结构的实施方案。在某些实施方案中，这些结构经过共价修饰，可储存和释放一氧化氮。一些实施方案涉及这些结构的制造和使用方法。共价修饰的聚合物结构可定制为以受控方式释放一氧化氮，可用于治疗各种病症。
• NITRIC OXIDE-RELEASING ANTIBACTERIAL POLYMERS AND SCAFFOLDS FABRICATED THEREFROM AND METHODS PERTAINING THERETO
  申请人：THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL

  公开号：US20200216571A1

  公开（公告）日：2020-07-09

  Several embodiments of NO releasing structures are disclosed. In some embodiments, the structures are covalently modified to store and release nitric oxide. Some embodiments pertain to methods of making and use of these structures. The covalently modified polymer structures may be tailored to release nitric oxide in a controlled manner and are useful for treatment of various medical conditions.
• US9801954B2
  申请人：——

  公开号：US9801954B2

  公开（公告）日：2017-10-31