Nubain

[The Profiler]

Nubain


Generic Name: nalbuphine hydrochloride
Dosage Form: Injection


Nubain Description



Nubain (nalbuphine hydrochloride) is a synthetic opioid agonist-antagonist analgesic of the phenanthrene series. It is chemically related to both the widely used opioid antagonist, naloxone, and the potent opioid analgesic, oxymorphone. Chemically nalbuphine hydrochloride is 17-(cyclobutylmethyl)-4,5α-epoxymorphinan-3,6α,14-triol hydrochloride. Nalbuphine hydrochloride molecular weight is 393.91 and is soluble in H2O (35.5 mg/mL @ 25ºC) and ethanol (0.8%); insoluble in CHCl3 and ether. Nalbuphine hydrochloride has pKa values of 8.71 and 9.96. The molecular formula is C21H27NO4 · HCl. The structural formula is:

Nubain is a sterile solution suitable for subcutaneous, intramuscular, or intravenous injection. Nubain is available in two concentrations, 10 mg and 20 mg of nalbuphine hydrochloride per mL. Both strengths in 10 mL vials contain 0.94% sodium citrate hydrous, 1.26% citric acid anhydrous, and 0.2% of a 9:1 mixture of methylparaben and propylparaben as preservatives; pH is adjusted, if necessary, to 3.5 to 3.7 with hydrochloric acid. The 10 mg/mL strength contains 0.2% sodium chloride.
Nubain is also available in ampuls in a sterile, 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, and 1.26% citric acid anhydrous; pH is adjusted, if necessary, to 3.5 to 3.7 with hydrochloric acid. The 10 mg/mL strength contains 0.2% sodium chloride.

Nubain - Clinical Pharmacology

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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[Stalking Horse]

Yes yes, but do you sell nalbuphine hydrochloride? lol

[skip]

man used to love that stuff,skip