Buprenorphine: Considerations for Pain Management

• Published in: Journal of pain and symptom management 2005-03, Vol.29 (3), p.297-326
• Main Authors: Johnson, Rolley E., Fudala, Paul J., Payne, Richard
• Format: Article
• Language: English
• Subjects: Analgesics, Opioid - pharmacology; Analgesics, Opioid - therapeutic use; Buprenorphine; Buprenorphine - pharmacology; Buprenorphine - therapeutic use; formulations; Humans; opioids; Pain - drug therapy; pain management; partial agonists; pharmacodynamics; pharmacokinetics; pharmacology
• ISSN: 0885-3924; 1873-6513
• DOI: 10.1016/j.jpainsymman.2004.07.005

New effective analgesics are needed for the treatment of pain. Buprenorphine, a partial mu-opioid agonist which has been in clinical use for over 25 years, has been found to be amenable to new formulation technology based on its physiochemical and pharmacological profile. Buprenorphine is marketed as parenteral, sublingual, and transdermal formulations. Unlike full mu-opioid agonists, at higher doses, buprenorphine's physiological and subjective effects, including euphoria, reach a plateau. This ceiling may limit the abuse potential and may result in a wider safety margin. Buprenorphine has been used for the treatment of acute and chronic pain, as a supplement to anesthesia, and for behavioral and psychiatric disorders including treatment for opioid addiction. Prolonged use of buprenorphine can result in physical dependence. However, withdrawal symptoms appear to be mild to moderate in intensity compared with those of full mu agonists. Overdoses have primarily involved buprenorphine taken in combination with other central nervous system depressants.