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Nalbuphine

产品号 DB00844 公司名称 DrugBank
CAS号 20594-83-6 公司网站 http://www.ualberta.ca/
分子式 C21H27NO4 电 话 (780) 492-3111
分子量 357.44338 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 722

产品价格信息

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产品别名

标题
Nalbuphine
IUPAC标准名
(1S,5R,14S,17S)-4-(cyclobutylmethyl)-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7(18),8,10-triene-10,14,17-triol
IUPAC传统名
nalbuphine
商标名
Nalbufina [DCIT]
Nubain
Nalbuphine HCL
Nalbuphinum [INN-Latin]

产品登记号

CAS号 20594-83-6

产品性质

疏水性(logP) 1.4
溶解度 35.5 mg/mL at 25 oC as HCl salt

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved
Description A narcotic used as a pain medication. It appears to be an agonist at kappa opioid receptors and an antagonist or partial agonist at mu opioid receptors. [PubChem]
Indication For the relief of moderate to severe pain.
Pharmacology Nalbuphine is a synthetic opioid agonist-antagonist analgesic of the phenanthrene series. Nalbuphine's analgesic potency is essentially equivalent to that of morphine on a milligram basis. The opioid antagonist activity of nalbuphine is one-fourth as potent as nalorphine and 10 times that of pentazocine. Nalbuphine by itself has potent opioid antagonist activity at doses equal to or lower than its analgesic dose. When administered following or concurrent with mu agonist opioid analgesics (e.g., morphine, oxymorphone, fentanyl), nalbuphine may partially reverse or block opioid-induced respiratory depression from the mu agonist analgesic. Nalbuphine may precipitate withdrawal in patients dependent on opioid drugs. Nalbuphine should be used with caution in patients who have been receiving mu opioid analgesics on a regular basis.
Toxicity Oral, acute LD50 is 1100 mg/kg in dog. Symptoms of overdose include primarily sleepiness and mild dysphoria.
Affected Organisms
Humans and other mammals
Absorption The mean absolute bioavailability was 81% and 83% for the 10 and 20 mg intramuscular doses, respectively, and 79% and 76% following 10 and 20 mg of subcutaneous nalbuphine.
Half Life The plasma half-life of nalbuphine is 5 hours, and in clinical studies the duration of analgesic activity has been reported to range from 3 to 6 hours.
Protein Binding Not appreciably bound.
References
Gear RW, Miaskowski C, Gordon NC, Paul SM, Heller PH, Levine JD: The kappa opioid nalbuphine produces gender- and dose-dependent analgesia and antianalgesia in patients with postoperative pain. Pain. 1999 Nov;83(2):339-45. [Pubmed]
External Links
Wikipedia
RxList
Drugs.com

参考文献

  • Gear RW, Miaskowski C, Gordon NC, Paul SM, Heller PH, Levine JD: The kappa opioid nalbuphine produces gender- and dose-dependent analgesia and antianalgesia in patients with postoperative pain. Pain. 1999 Nov;83(2):339-45. Pubmed