ナルブフィン

DEA NFLIS-Drug Category -> Narcotic Analgesics

Pharmaceuticals -> Listed in ZINC15

Warning

H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]

P261, P264, P270, P271, P301+P317, P304+P340, P317, P319, P330, P403+P233, P405, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 5 reports by companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

The most common adverse effects following nalbuphine administration include sedation, sweating, nausea, vomiting, dizziness, vertigo, dry mouth, and headache. Anaphylactic, anaphylactoid, or severe hypersensitivity reactions have been reported in patients receiving nalbuphine, and immediate supportive medical treatment should be provided should they occur.

Signs and Symptoms of Overdose

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.

Drug-Induced Liver Injury Severity and Toxicity (DILIst)

nalbuphine

DILI Negative

Intravenous

DOI:10.1016/j.drudis.2019.09.022

N - Nervous system

QN - Nervous system

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 opoioid antagonist activity of nalbuphine is about one-fourth to that of [nalorphine] and 10 times to 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.

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.

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NALBUPHINE

Mechanisms of Action [MoA] - Competitive Opioid Antagonists

Established Pharmacologic Class [EPC] - Opioid Agonist/Antagonist

Mechanisms of Action [MoA] - Partial Opioid Agonists

Nalbuphine is an Opioid Agonist/Antagonist. The mechanism of action of nalbuphine is as a Competitive Opioid Antagonist and Partial Opioid Agonist.

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. Clinical studies show that the duration of analgesic activity of the drug can range from 3 to 6 hours.

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]