NUBAIN is a potent analgesic. Its analgesic potency is essentially equivalent to that of morphine on a milligram basis. Receptor studies show that NUBAIN binds to mu, kappa, and delta receptors, but not to sigma receptors. NUBAIN is primarily a kappa agonist/partial mu antagonist analgesic.

The onset of action of NUBAIN occurs within 2 to 3 minutes after intravenous administration, and in less than 15 minutes following subcutaneous or intramuscular injection. 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.

The opioid antagonist activity of NUBAIN is one-fourth as potent as nalorphine and 10 times that of pentazocine.

NUBAIN may produce the same degree of respiratory depression as equianalgesic doses of morphine. However, NUBAIN exhibits a ceiling effect such that increases in dose greater than 30 mg do not produce further respiratory depression in the absence of other CNS active medications affecting respiration.

NUBAIN 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), NUBAIN may partially reverse or block opioid-induced respiratory depression from the mu agonist analgesic. NUBAIN may precipitate withdrawal in patients dependent on opioid drugs. NUBAIN should be used with caution in patients who have been receiving mu opioid analgesics on a regular basis.

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