Buprenorphine – The ideal drug for most clinical indications for an opioid?

Abstract

In this issue of the Scandinavian Journal of Pain, Stephen Butler, ormer chief of the famous Bonica Pain Clinic at the University of ashington in Seattle, reviews new knowledge of buprenorphine 1]. During the four decades after buprenorphine became availble for clinical use persistent misunderstandings have existed in extbooks and in reviews in medical literature. These misundertandings have misled clinicians and patients so that optimal uses f this drug were reduced. This problem continues to this day [1]. The first serious misunderstanding was that buprenorphine is ot an addicting drug. It was marketed as a drug for moderate o severe pain with low risk of misuse or abuse. Clinicians and ddicted persons soon discovered that this is not true. I was surrised and very disappointed to discover soon after the sublingual uprenorphine was available in Norway, already in 1983–84, that ne of my patients sold his sublingual buprenorphine tablets n the illegal market. Addicted persons dissolved the sublingual ablets and injected the drug. So buprenorphine was soon moved n to the narcotic drug list. There are other misunderstandings about buprenorphine, ostly based on animal data. These misunderstandings came into extbooks on pharmacology and pain as “medical truths” about 0 years ago. They have been difficult to get out of textbooks and uidelines. Theycontinue to liveon in teachings tomedical students nd postgraduate training. It is by now a well-known fact that animal models of pain and nalgesia are unreliable as predictors of clinical effects in patients ith pain. In clinical practice there is nobell-shapeddose–response urve and there is no plateau on the dose–relief response curve of uprenorphine. There is also no antagonist effect from buprenorhine on othermu-opioid agonists such asmorphine or oxycodone. n the contrary, there may be supra-additive or synergistic effects etween buprenorphine and morphine, and between buprenorhine and oxycodone – for references, see [2]. Buprenorphine is an agonist on the mu-, the delta, and the ORLreceptors. Buprenorphine is an antagonist at the kappa-receptor. ctive metabolites have different effects on the four opioid recepors; all except thenorbup-3-gluareanalgesic. Buprenorphine itself