Nalbuphine, (Nubain), is a prescription opioid analgesic used to manage moderate to severe pain.
It is frequently administered in medical settings for preoperative and postoperative pain relief, as well as during labor and delivery.
Additional uses include supplement to balanced anesthesia, preoperative and postoperative analgesia, and obstetrical analgesia during labor and delivery.
The drug should not be used for extended periods unless pain remains severe enough to require an opioid analgesic and alternative options remain inadequate.
Nalbuphine hydrochloride injection is indicated for the management of pain severe enough to require an opioid analgesic when alternative treatments are inadequate.
It is a mixed agonist-antagonist.
It primarily acts as an agonist at kappa-opioid receptors, providing pain relief, and an antagonist at mu-opioid receptors.
Nalbuphine is a synthetic mixed opioid agonist-antagonist analgesic that acts as an agonist at kappa opioid receptors and an antagonist at mu opioid receptors.
It is chemically related to both naloxone and oxymorphone and belongs to the phenanthrene series.
Nalbuphine is a potent analgesic with analgesic potency essentially equivalent to morphine on a milligram basis up to approximately 30 mg.
Its opioid antagonist activity is one-fourth as potent as nalorphine and 10 times that of pentazocine.
Unlike many other opioids, nalbuphine exhibits a ceiling effect for respiratory depression; meaning beyond a certain dose, increased amounts do not further depress breathing: doses greater than 30 mg do not produce further respiratory depression in the absence of other CNS-active medications.
For patients with with idiopathic pulmonary fibrosis and chronic cough treatment with nalbuphine ER decreased cough frequency and improved patient outcomes at six weeks.
It is not a controlled substance under the Controlled Substances Act, though it still carries risks of addiction and misuse.
It is typically administered via injection (intravenous, intramuscular, or subcutaneous).
Oral agents are available.
Most patients experience mild side effects, which may include:
Sedation (the most frequent effect) Dizziness or vertigo Nausea and vomiting Sweating and dry mouth Sphincter of Oddi spasm, increase seizure frequency in patients with seizure disorders, and impair mental or physical abilities needed for driving or operating machinery.
Using nalbuphine with alcohol, benzodiazepines, or other CNS depressants can lead to life-threatening respiratory depression or coma.
When administered with or following mu agonist opioids (morphine, fentanyl, oxymorphone), it may partially reverse or block opioid-induced respiratory depression and may precipitate withdrawal in opioid-dependent patients.
Because of its mu-antagonist properties, nalbuphine can precipitate withdrawal symptoms in individuals who are already physically dependent on full opioid agonists, like morphine or oxycodone.
It should be used with extreme caution in patients with head injuries, impaired renal or hepatic function, or severe asthma.
Nalbuphine is primarily sold as an injectable solution in various strengths.
The initial adult dose is 10 mg for a 70 kg individual, repeated every 3 to 6 hours as necessary.
The maximum single dose is 20 mg and maximum total daily dose is 160 mg.
For anesthesia induction, doses range from 0.3 mg/kg to 3 mg/kg intravenously over 10-15 minutes, with maintenance doses of 0.25 to 0.5 mg/kg as needed.
The drug can be administered subcutaneously, intramuscularly, or intravenously.
Nalbuphine has potent opioid antagonist activity at doses equal to or lower than its analgesic dose