![]() ![]() 6, 7, 8īuprenorphine acts as a partial mu-opioid receptor agonist with a high affinity for the receptor, but lower intrinsic activity compared to other full mu-opioid agonists such as heroin, oxycodone, or methadone. Buprenorphine may also be a preferred agent over methadone (which is also commonly used to treat severe pain and opioid use disorder), as it has less effect on Qtc interval prolongation, 9, 10 fewer drug interactions, reduced risk of sexual side effects, 17 and an improved safety profile with a lower risk of overdose and respiratory depression. Use of once-daily buprenorphine may benefit individuals who have developed tolerance to other potent opioids and who require larger and more frequent doses. 13 For example, buprenorphine dissociates from opioid receptors very slowly, resulting in a long duration of action and relief from pain or withdrawal symptoms for upwards of 24-36 hours. ![]() 14, 20, 21 Buprenorphine has poor gastrointestinal absorption and is therefore formulated as a sublingual tablet.īuprenorphine has a number of unique pharmacokinetic and pharmacodynamic properties that make it a preferred agent for the treatment of conditions requiring high doses of strong opioids. Combination with naloxone is intended to reduce the abuse potential of Suboxone, as naloxone is poorly absorbed by the oral route (and has no effect when taken orally), but would reverse the opioid agonist effects of buprenorphine if injected intravenously. 20, 21 Buprenorphine is commercially available as the brand name product Suboxone which is formulated in a 4:1 fixed-dose combination product along with naloxone, a non-selective competitive opioid receptor antagonist. ![]() 12, 15 It is also commonly used as an alternative to methadone for the treatment of severe opioid addiction. Belbuca, Buprenex, Buprenorphine, Butrans, Probuphine, Sublocade, Suboxone, Subutex, Zubsolv Generic Name Buprenorphine DrugBank Accession Number DB00921 Backgroundīuprenorphine is a weak partial mu-opioid receptor agonist and a weak kappa-opioid receptor antagonist used for the treatment of severe pain. ![]()
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