Name: | Nalbuphine |
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PubChem Compound ID: | 11957645 |
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. |
Molecular formula: | C21H28ClNO4 |
Molecular weight: | 393.904 g/mol |
Synonyms: |
EU-0100847
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Name: | Nalbuphine |
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Name (isomeric): | DB00844 |
Drug Type: | small molecule |
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. |
Brand: | Nubain, Nalbuphine HCL, Nalbufina [DCIT], Nalbuphinum [INN-Latin] |
Category: | Narcotic Antagonists, Narcotics, Analgesics, Opioid |
CAS number: | 20594-83-6 |
Indication: | For the relief of moderate to severe pain. |
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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 antag...
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Mechanism of Action: |
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 ag...
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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. |
Protein binding: | Not appreciably bound. |
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. |
Toxicity: | ORAL (LD50): Acute: 1100 mg/kg [Dog]. Symptoms of overdose include primarily sleepiness and mild dysphoria. |
Affected organisms: | Humans and other mammals |
Drug interaction: |
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