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User:Mr. Ibrahem/Buprenorphine

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Mr. Ibrahem/Buprenorphine
Skeletal formula of buprenorphine
Ball-and-stick model of the buprenorphine molecule
Clinical data
Trade namesSubutex, Sublocade, others
AHFS/Drugs.comMonograph
MedlinePlusa605002
License data
Pregnancy
category
Dependence
liability		Psychological: High
Physical: Moderate[2]
Routes of
administration		Under the tongue, through the cheek, IM, transdermal, intranasal, rectally, by mouth
Drug classOpioid
Legal status
Legal status
Pharmacokinetic data
BioavailabilitySublingual: 30%[4]
Intranasal: 48%[5]
Buccal: 65%[6][7]
Protein binding96%
MetabolismLiver (CYP3A4, CYP2C8)
Onset of actionWithin 30 min[8]
Elimination half-life37 hours (range 20–70 hours)
Duration of actionUp to 24 hrs[8]
ExcretionBiliary and kidney
Identifiers
  • (2S)-2-[(5R,6R,7R,14S)-17-cyclopropylmethyl-4,5-epoxy-6,14-ethano-3-hydroxy-6-methoxymorphinan-7-yl]-3,3-dimethylbutan-2-ol
Chemical and physical data
FormulaC29H41NO4
Molar mass467.650 g·mol−1
3D model (JSmol)
  • Oc7ccc5c1c7O[C@H]3[C@]6(OC)[C@H](C[C@@]2([C@H](N(CC[C@@]123)CC4CC4)C5)CC6)[C@@](O)(C)C(C)(C)C
  • InChI=1S/C29H41NO4/c1-25(2,3)26(4,32)20-15-27-10-11-29(20,33-5)24-28(27)12-13-30(16-17-6-7-17)21(27)14-18-8-9-19(31)23(34-24)22(18)28/h8-9,17,20-21,24,31-32H,6-7,10-16H2,1-5H3/t20-,21-,24-,26+,27-,28+,29-/m1/s1 checkY
  • Key:RMRJXGBAOAMLHD-IHFGGWKQSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Buprenorphine, sold under the brand name Subutex, among others, is an opioid used to treat opioid use disorder, acute pain, and chronic pain.[8] It can be used under the tongue, in the cheek, by injection, as a skin patch, or as an implant.[8][11] For opioid use disorder, it is typically started when withdrawal symptoms have begun and for the first two days of treatment under direct observation of a health care provider.[8] The combination formulation of buprenorphine/naloxone (Suboxone) is recommended to discourage misuse by injection.[8] Maximum pain relief is generally within an hour with effects up to 24 hours.[8]

Side effects may include respiratory depression (decreased breathing), sleepiness, adrenal insufficiency, QT prolongation, low blood pressure, allergic reactions, and opioid addiction.[8] Among those with a history of seizures, there is a risk of further seizures.[8] Opioid withdrawal following stopping buprenorphine is generally less severe than with other opioids.[8] It is unclear if use during pregnancy is safe and use while breastfeeding is not recommended.[8] Buprenorphine affects different types of opioid receptors in different ways.[8] Depending on the type of receptor it may be an agonist, partial agonist, or antagonist.[8]

Buprenorphine was patented in 1965 and approved for medical use in the United States in 1981.[8][12] It is on the World Health Organization's List of Essential Medicines as an alternative to methadone.[13] In 2017, 14.6 million prescriptions for the medication were written in the United States.[14] It is also a common drug of abuse, being used in place of heroin.[14] Buprenorphine may be used recreationally by injection or in the nose for the high it produces.[14] In the United States, it is a Schedule III controlled substance.[14] In 2021 a daily 8mg sublingual dose costs slightly over US$2 in the United States,[15] and costs the NHS in the UK slightly less than £2.50.[16]

References edit

  1. ^ a b "Buprenorphine Use During Pregnancy". Drugs.com. 14 October 2019. Archived from the original on 10 November 2020. Retrieved 17 May 2020.
  2. ^ Bonewit-West, Kathy; Hunt, Sue A.; Applegate, Edith (2012). Today's Medical Assistant: Clinical and Administrative Procedures. Elsevier Health Sciences. p. 571. ISBN 9781455701506. Archived from the original on 28 July 2020. Retrieved 29 July 2020.
  3. ^ Health Canada (6 December 2004). "ARCHIVED - Report Stakeholder Workshop on a National Buprenorphine Program". aem. Archived from the original on 26 March 2020. Retrieved 10 January 2020.
  4. ^ Mendelson J, Upton RA, Everhart ET, Jacob P, Jones RT (January 1997). "Bioavailability of sublingual buprenorphine". Journal of Clinical Pharmacology. 37 (1): 31–7. doi:10.1177/009127009703700106. PMID 9048270.
  5. ^ Eriksen J, Jensen NH, Kamp-Jensen M, Bjarnø H, Friis P, Brewster D (November 1989). "The systemic availability of buprenorphine administered by nasal spray". The Journal of Pharmacy and Pharmacology. 41 (11): 803–5. doi:10.1111/j.2042-7158.1989.tb06374.x. PMID 2576057.
  6. ^ "Buprenorphine / Naloxone Buccal Film (BUNAVAIL) C-III" (PDF). Pharmacy Benefits Management (PBM) Services. September 2014. Archived (PDF) from the original on 20 October 2020.
  7. ^ [https://web.archive.org/web/20201030071038/https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205637s000lbl.pdf Archived 30 October 2020 at the Wayback Machine BUNAVAIL (buprenorphine and naloxone) buccal film, CIII [prescribing information online]]. BioDelivery BioDelivery Sciences International, Inc. (BDSI), Raleigh, NC. Jun 2014.
  8. ^ a b c d e f g h i j k l m n o p "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.
  9. ^ "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 7 August 2020. Retrieved 9 September 2020.
  10. ^ "Interpreting Urine Drug Tests (UDT)". Archived from the original on 25 October 2023. Retrieved 24 October 2023.
  11. ^ "Press Announcements – FDA approves first buprenorphine implant for treatment of opioid dependence". FDA. Archived from the original on 30 November 2017. Retrieved 12 December 2017.
  12. ^ Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 528. ISBN 9783527607495. Archived from the original on 29 August 2021. Retrieved 29 July 2020.
  13. ^ World Health Organization (2023). The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). Geneva: World Health Organization. hdl:10665/371090. WHO/MHP/HPS/EML/2023.02.
  14. ^ a b c d Drug Enforcement Administration (July 2019). "Buprenorphine" (PDF). DEA. Archived (PDF) from the original on 11 November 2020. Retrieved 3 December 2017.
  15. ^ "Buprenorphine Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 13 February 2021. Retrieved 13 February 2021. {{cite web}}: |archive-date= / |archive-url= timestamp mismatch; 10 November 2020 suggested (help)
  16. ^ BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 468-474. ISBN 978-0-85711-369-6.{{cite book}}: CS1 maint: date format (link)
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