2953 T3D2911 Nalbuphine Nalbuphine is only found in individuals that have used or taken this drug. It is 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]The exact mechanism of action is unknown, but is believed to interact with an opiate receptor site in the CNS (probably in or associated with the limbic system). The opiate antagonistic effect may result from competitive inhibition at the opiate receptor, but may also be a result of other mechanisms. Nalbuphine is thought primarily to be a kappa agonist. It is also a partial mu antagonist analgesic, with some binding to the delta receptor and minimal agonist activity at the sigma receptor. 20594-83-6 5311304 C21H27NO4 357.194010 White powder. 230°C as HCl salt 35.5 mg/mL at 25°C as HCl salt Intravenous. 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. Receptor studies show that nalbuphine exerts its action via binding to mu, kappa, and delta receptors, but not to sigma receptors. Nalbuphine is primarily a kappa agonist/partial mu antagonist analgesic. The exact mechanism of action is unknown, but is believed to interact with an opiate receptor site in the CNS (probably in or associated with the limbic system). The opiate antagonistic effect may result from competitive inhibition at the opiate receptor, but may also be a result of other mechanisms. Nalbuphine is thought primarily to be a kappa agonist. It is also a partial mu antagonist analgesic, with some binding to the delta receptor and minimal agonist activity at the sigma receptor. 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. LD50: 1100 mg/kg (Oral, Dog) (A308) No indication of carcinogenicity to humans (not listed by IARC). Nalbuphine is indicated for the relief of moderate to severe pain. It can also be used as a supplement to balanced anesthesia, for preoperative and postoperative analgesia, and for obstetrical analgesia during labor and delivery. [Wikipedia] Medical problems can include congested lungs, liver disease, tetanus, infection of the heart valves, skin abscesses, anemia and pneumonia. Death can occur from overdose. Symptoms of overdose include primarily sleepiness and mild dysphoria. The immediate intravenous administration an opiate antagonist such as naloxone or nalmefene is a specific antidote. Oxygen, intravenous fluids, vasopressors and other supportive measures should be used as indicated. (L1712) 2009-07-21T20:27:48Z 2014-12-24T20:25:53Z Nalbuphine C07251 7454 Nalbuphine DB00844 true [H][C@@]12OC3=C(O)C=CC4=C3[C@@]11CCN(CC3CCC3)[C@]([H])(C4)[C@]1(O)CC[C@]2([H])O C21H27NO4 InChI=1S/C21H27NO4/c23-14-5-4-13-10-16-21(25)7-6-15(24)19-20(21,17(13)18(14)26-19)8-9-22(16)11-12-2-1-3-12/h4-5,12,15-16,19,23-25H,1-3,6-11H2/t15-,16+,19-,20-,21+/m0/s1 InChIKey=NETZHAKZCGBWSS-CEDHKZHLSA-N 357.4434 357.194008357 Exogenous Solid 1.4 HMDB14982 CHEMBL895 4470813 <p>Michael R. Magruder, &#8220;Nalbuphine-narcotic analgesic composition and method of producing analgesia.&#8221; U.S. Patent US4366159, issued August, 1981.</p>