User:Mr. Ibrahem/Nalbuphine

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Not to be confused with Nalorphine.
Mr. Ibrahem/Nalbuphine
Skeletal formula
Ball-and-stick model of nalbuphine
Clinical data
Trade namesNubain, Nalpain, Nalbuphin, others
AHFS/Drugs.comMonograph
MedlinePlusa682668
Pregnancy
category
  • B
Routes of
administration		Intravenous, intramuscular, subcutaneous
Drug classOpioid[1]
Legal status
Legal status
  • AU: S4 (Prescription only)
  • CA: Schedule IV
  • US: Rx only (unscheduled) Schedule IV in some states
  • Federally Uncontrolled (RX-only) , except in KY , C-IV
Pharmacokinetic data
Bioavailability• Oral: 11% (young adults), >44% (elderly)[2]
• IMTooltip Intramuscular injection: 81% (10 mg), 83% (20 mg)
• SCTooltip Subcutaneous injection: 76% (20 mg), 79% (10 mg)[3]
Protein binding50%[2]
MetabolismLiver (glucuronidation)[5][2]
MetabolitesGlucuronide conjugates (inactive), others[4][5][2]
Onset of action• Oral: <1 hour[2]
• Rectal: <30 minutes[2]
• IVTooltip Intravenous injection: 2–3 min[1]
• IMTooltip Intramuscular injection: <15 minutes[1]
• SCTooltip Subcutaneous injection: <15 minutes[1]
Elimination half-life~5 hours (3–6 hours)<[4]
Duration of action3–4 hours[6]
ExcretionUrine, bile, feces;[2] 93% within 6 hours[7]
Identifiers
  • (–)-17-(cyclobutylmethyl)-4,5α-epoxymorphinan-3,6α,14-triol
Chemical and physical data
FormulaC21H27NO4
Molar mass357.450 g·mol−1
3D model (JSmol)
  • O[C@@H]4[C@@H]5Oc1c2c(ccc1O)C[C@H]3N(CC[C@]25[C@@]3(O)CC4)CC6CCC6
  • InChI=1S/C21H27NO4/c23-14-5-4-13-10-16-21(25)7-6-15(24)19-20(21,17(13)18(14)26-19)8-9-22(16)11-12-2-1-3-12/h4-5,12,15-16,19,23-25H,1-3,6-11H2/t15-,16+,19-,20-,21+/m0/s1 checkY
  • Key:NETZHAKZCGBWSS-CEDHKZHLSA-N checkY
  (verify)

Nalbuphine, sold under the brand names Nubain among others, is an opioid which is used to treat moderate to severe pain.[1] It is given by injection into a vein, muscle, or under the skin.[1] When given by injection onset of effects is within 15 minutes and lasts for about 3 to 4 hours.[1][6]

Common side effects include sleepiness, sweatiness, nausea, dizziness, dry mouth, and headache.[8] While it causes some respiratory depression at low doses this does not increase significantly with larger doses.[4] Other side effects may include abuse and anaphylaxis.[8] It is an opioid of the partial agonist type.[8]

Nalbuphine was patented in 1963 and was approved for medical use in the United States in 1979.[9] It is available as a generic medication.[8] In the United States it costs about 4 USD per 10 mg dose as of 2021.[10] It is marketed in many countries.[11] It is not a controlled substance in the United States.[4]

References[edit]

  1. ^ a b c d e f g h Howard S. Smith; Marco Pappagallo (6 September 2012). Essential Pain Pharmacology: The Prescriber's Guide. Cambridge University Press. pp. 343–. ISBN 978-0-521-75910-6. Archived from the original on 28 October 2021. Retrieved 24 October 2021.
  2. ^ a b c d e f g Bruno Bissonnette (14 May 2014). Pediatric Anesthesia. PMPH-USA. pp. 398–. ISBN 978-1-60795-213-8. Archived from the original on 28 October 2021. Retrieved 24 October 2021.
  3. ^ Excerpta medica. Section 24: Anesthesiology. 1988. Archived from the original on 2021-10-28. Retrieved 2021-10-24. 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.
  4. ^ a b c d Narver HL (March 2015). "Nalbuphine, a non-controlled opioid analgesic, and its potential use in research mice". Lab Anim (NY). 44 (3): 106–10. doi:10.1038/laban.701. PMID 25693108. S2CID 25378355.
  5. ^ a b Steven D. Waldman (9 June 2011). Pain Management E-Book. Elsevier Health Sciences. pp. 910–. ISBN 978-1-4377-3603-8. Archived from the original on 28 October 2021. Retrieved 24 October 2021.
  6. ^ a b Greaves, Ian; Porter, Keith; Smith, Jason (7 June 2016). Practical Prehospital Care E-book: The Principles and Practice of Immediate Care. Elsevier Health Sciences. p. 166. ISBN 978-0-7020-4896-8. Archived from the original on 13 November 2021. Retrieved 11 November 2021.
  7. ^ Yoo YC, Chung HS, Kim IS, Jin WT, Kim MK (Mar–Apr 1995). "Determination of Nalbuphine in Drug Abusers' Urine". Journal of Analytical Toxicology. 19 (2): 120–123. doi:10.1093/jat/19.2.120. PMID 7769781.
  8. ^ a b c d e "Nalbuphine Monograph for Professionals". Drugs.com. Archived from the original on 27 January 2021. Retrieved 11 November 2021.
  9. ^ Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 528. ISBN 9783527607495. Archived from the original on 2021-08-29. Retrieved 2021-10-24.
  10. ^ "Nalbuphine Prices, Coupons & Patient Assistance Programs". Drugs.com. Retrieved 11 November 2021.
  11. ^ "Nalbuphine". Archived from the original on 2018-06-18. Retrieved 2021-10-24.
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