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Brand names,
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Analogs
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Brand Names Mixture
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Chemical_Formula
C21H27NO4
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RX_link
http://www.rxlist.com/cgi/generic3/nalbuphine.htm
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fda sheet
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msds (material safety sheet)
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Synthesis Reference
No information avaliable
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Molecular Weight
357.443 g/mol
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Melting Point
230 oC as HCl salt
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H2O Solubility
35.5 mg/mL at 25 oC as HCl salt
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State
Solid
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LogP
1.939
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Dosage Forms
Solution (suitable for subcutaneous, intramuscular, or intravenous injection - available as 10 mg or 20 mg of nalbuphine hydrochloride per mL)
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Indication
For the relief of moderate to severe pain.
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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.
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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.
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side effects and Toxicity
ORAL (LD50): Acute: 1100 mg/kg [Dog]. Symptoms of overdose include primarily sleepiness and mild dysphoria.
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Patient Information
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Organisms Affected
Humans and other mammals