Nalbuphine (nalbuphine hydrochloride) is a synthetic opioid used commercially as an analgesic under a variety of trade names, including Nubain. It is noteworthy in part for the fact that at low dosages, it is found much more effective by women than by men, and may even increase pain in men, leading to its discontinuation in the UK in 2003.
Nalbuphine is also available in a sulfite and paraben-free formulation in two concentrations, 10 mg and 20 mg of nalbuphine hydrochloride per mL. One mL of each strength contains 0.94% sodium citrate hydrous, 1.26% citric acid anhydrous; pH is adjusted, if necessary, with hydrochloric acid. The 10 mg/mL strength contains 0.2% sodium chloride.
Nalbuphine is a potent analgesic. Its analgesic potency is essentially equivalent to that of morphine on a milligram basis. Its onset of action 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.
Although Nalbuphine possesses narcotic antagonist activity, there is evidence that in nondependent patients it will not antagonize a narcotic analgesic administered just before, concurrently, or just after an injection. Therefore, patients receiving a narcotic analgesic, general anesthetics, phenothiazines, or other tranquilizers, sedatives, hypnotics, or other CNS depressants (including alcohol) concomitantly with Nalbuphine may exhibit an additive effect. When such combined therapy is contemplated, the dose of one or both agents should be reduced.
The use of NUBAIN as a supplement to balanced anesthesia requires larger doses than those recommended for analgesia. Induction doses of NUBAIN range from 0.3 mg/kg to 3.0 mg/kg intravenously to be administered over a 10 to 15 minute period with maintenance doses of 0.25 to 0.50 mg/kg in single intravenous administrations as required.
In case of overdose or adverse reaction, the immediate intravenous administration of naloxone (Narcan) is a specific antidote. Oxygen, intravenous fluids, vasopressors and other supportive measures should be used as indicated.
Other, less frequent reactions are: feeling sweaty/clammy 99 (9%), nausea/vomiting 68 (6%), dizziness/vertigo 58 (5%), dry mouth 44 (4%), and headache 27 (3%). Other adverse reactions which may occur (reported incidence of 1% or less) are:
Other possible, but rare side effects include speech difficulty, urinary urgency, blurred vision, flushing and warmth.
WIPO PUBLISHES PATENT OF DEBREGEAS ASSOCIES PHARMA FOR "NALBUPHINE-BASED FORMULATIONS AND USES THEREOF" (FRENCH INVENTORS)
Feb 29, 2012; GENEVA, Feb. 27 -- Publication No. WO/2012/022919 was published on Feb. 23. Title of the invention: "nalbuphine-BASED...