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Active ingredient: Nalbuphine - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Analgesics, Opioid
  • Narcotic Antagonists
  • Narcotics

Dosage Forms

  • Solution (suitable for subcutaneous, intramuscular, or intravenous injection - available as 10 mg or 20 mg of nalbuphine hydrochloride per mL)

Brands / Synonyms

Nalbufina [DCIT]; Nalbuphine; Nalbuphine HCL; Nalbuphinum [INN-Latin]; Nubain; Nubain

Indications

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.

Mechanism of Action

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.

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.

Toxicity

ORAL (LD50): Acute: 1100 mg/kg [Dog]. Symptoms of overdose include primarily sleepiness and mild dysphoria.

Biotrnasformation / Drug Metabolism

Not Available

Contraindications

NUBAIN should not be administered to patients who are hypersensitive to nalbuphine hydrochloride, or to any of the other ingredients in NUBAIN.

Drug Interactions

No specific information available.

 

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