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Buprenorphine

From Wikipedia
buprenorphine
type of chemical entity
Subclass ofmorphinan alkaloid Edit
Get useMedication Edit
Chemical formulaC₂₉H₄₁NO₄ Edit
Canonical SMILESCC(C)(C)C(C)(C1CC23CCC1(C4C25CCN(C3CC6=C5C(=C(C=C6)O)O4)CC7CC7)OC)O Edit
Isomeric SMILESC[C@]([C@H]1C[C@@]23CC[C@@]1([C@H]4[C@@]25CCN([C@@H]3CC6=C5C(=C(C=C6)O)O4)CC7CC7)OC)(C(C)(C)C)O Edit
Active ingredient inBuprenex, BuTrans, Probuphine, Belbuca Edit
World Health Organisation international non-proprietary namebuprenorphine Edit
Found insyd taxonPapaver somniferum Edit
Physically dey interact plusopioid receptor kappa 1, opioid receptor mu 1 Edit
Route of administrationintravenous infusion and defusion, intramuscular injection, sublingual administration Edit
Legal status (medicine)boxed warning Edit
Pregnancy categoryAustralian pregnancy category C, US pregnancy category C Edit
Subject has roleopioid antagonist, opioid, narcotic Edit

Buprenorphine be an opioid dem use to treat opioid use disorder, acute pain, den chronic pain.[1] E fi be used under de tongue (sublingual), insyd de cheek (buccal), by injection (intravenous den subcutaneous), as a skin patch (transdermal), anaa as an implant.[1][2]

Insyd de United States, de combination formulation of buprenorphine/naloxone (Suboxone) usually be prescribed to discourage misuse by injection.[1] Maximum pain relief generally be within an hour plus effects up to 24 hours.[1] Buprenorphine dey affect different types of opioid receptors insyd different ways.[1] Dey depend on de type of opioid receptor, e fi be an agonist, partial agonist, anaa antagonist.[1] Buprenorphine ein activity as an agonist/antagonist be important insyd de treatment of opioid use disorder: e dey relieve withdrawal symptoms from oda opioids den dey induce sam euphoria (primarily wen first dey start treatment if one no already be opioid tolerant/dependent), buh sanso dey block de ability give chaw oda opioids, wey dey include heroin, to cause an effect. Unlike full agonists like heroin anaa methadone, buprenorphine get a ceiling effect, such that taking more medicine past a certain point no go increase de effects of de drug.[3]

Being a partial MOR agonist, buprenorphine dey offer flexibility to prescribers treating opioid use disorder as de dosage fi be easily adjusted.

Side effects fi include respiratory depression (decreased breathing), sleepiness, adrenal insufficiency, changes insyd heart electrophysiology (QT prolongation), low blood pressure, allergic reactions, constipation, den opioid addiction.[1][4] Among those plus a history of seizures, a risk exists of further seizures.[1] Opioid withdrawal dey follow stopping buprenorphine generally be less severe dan plus oda opioids.[1] Whether ein use during pregnancy be safe be unclear, buh ein use while breastfeeding probably be safe, since de dose de infant receive be 1–2% dat of de maternal dose, on a weight basis.[1][5]

Dem patent buprenorphine insyd 1965, FDA approve give medical use as an analgesic insyd 1981, wey FDA approve for treating opioid use disorder insyd 2002.[6][7] E dey on de World Health Organization's List of Essential Medicines.[8] Despite dem originally market am as an analgesic e be far more commonly prescribed den used to treat opioid use disorders, such as addiction to heroin.[9] Insyd 2020, e be de 186th most commonly prescribed medication insyd de United States, plus more dan 2.8 million prescriptions.[10][11]

Buprenorphine generally be used as a medication for treating opioid use disorder. Insyd de United States, buprenorphine hydrochloride (den a combination formula, buprenorphine hydrochloride/naloxone,) be schedule III controlled substances.

Buprenorphine no dey produce de same sense of euphoria den/anaa "sense of well-being" as dem report in use of full-agonist opioids. A "ceiling effect"[12] be observed in regards to de potentially fatal side effects of oda opioids, such as respiratory depression. While de medication fi produce comparably mild side effects to dat of oda drugs insyd ein classification, e still dey carry sam abuse potential.

References

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  1. 1 2 3 4 5 6 7 8 9 10 "Buprenorphine Hydrochloride". drugs.com. American Society of Health-System Pharmacists. 26 January 2017. Archived from the original on 18 July 2017. Retrieved 17 March 2017.
  2. ↑ "FDA approves first buprenorphine implant for treatment of opioid dependence" (Press release). U.S. Food and Drug Administration. 26 May 2016. Archived from the original on 30 November 2017. Retrieved 12 December 2017.
  3. ↑ Whelan PJ, Remski K (January 2012). "Buprenorphine vs methadone treatment: A review of evidence in both developed and developing worlds". Journal of Neurosciences in Rural Practice. 3 (1): 45–50. doi:10.4103/0976-3147.91934. PMC 3271614. PMID 22346191.
  4. ↑ "Buprenorphine". The Substance Abuse and Mental Health Services Administration. 15 June 2015. Archived from the original on 26 August 2020. Retrieved 14 October 2020.
  5. ↑ "Buprenorphine use while Breastfeeding". Drugs.com. Archived from the original on 10 November 2020. Retrieved 7 February 2021.
  6. ↑ "Buprenorphine Hydrochloride". drugs.com. American Society of Health-System Pharmacists. 26 January 2017. Archived from the original on 18 July 2017. Retrieved 17 March 2017.
  7. ↑ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 528. ISBN 978-3-527-60749-5. Archived from the original on 10 January 2023. Retrieved 29 May 2020.
  8. ↑ Organization WH (2021). World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.
  9. ↑ "Buprenorphine". SAMHSA Center for Substance Abuse Treatment (CSAT). July 2019. Archived from the original on 20 August 2020. Retrieved 9 January 2020.
  10. ↑ "The Top 300 of 2020". ClinCalc. Archived from the original on 12 February 2021. Retrieved 7 October 2022.
  11. ↑ "Buprenorphine – Drug Usage Statistics". ClinCalc. Archived from the original on 11 October 2022. Retrieved 7 October 2022.
  12. ↑ Infantino R, Mattia C, Locarini P, Pastore AL, Maione S, Luongo L (May 2021). "Buprenorphine: Far Beyond the "Ceiling"". Biomolecules. 11 (6): 816. doi:10.3390/biom11060816. PMC 8230089. PMID 34072706.
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