Buprenorphine in cancer pain

Abstract

Buprenorphine is a broad spectrum, highly lipophilic, and long-acting partial mu opioid receptor agonist that is noncross tolerant to other opioids. Buprenorphine can be given by several routes. Metabolism is through CYP3A4 and CYP2C8 and by conjugases. Constipation and sexual dysfunction appear to be less with buprenorphine than with other opioids. The recent development of a polymer matrix patch delivery system for buprenorphine prevents "dose dumping" and facilitates pain management in those unable to take oral analgesics. Sublingual buprenorphine has been combined with naloxone to prevent illicit conversion to parenteral administration. Buprenorphine has been used extensively to control cancer pain. In certain clinical situations, buprenorphine may have particular advantages over other opioids.

Is there a ceiling effect of transdermal buprenorphine? Preliminary data in cancer patients

“…New evidence on the pharmacology of BUP [4,5,6,8,13] availability of a transdermal formulation (TD-BUP) have offered an opportunity to expand the utility of this drug in the context of the management of cancer-related pain.…”

What is new in neuropathic pain?

“…Buprenorphine appears to have little analgesic cross-tolerance to other opioids [31]. Sublingual and parenteral formulations are available in the United States and a transdermal matrix patch in Europe [32,33].…”

“…Drug interactions are rare because the rate-limiting step is glucuronidation for both the parent drug and the major active metabolite norbuprenorphine. In addition, unlike fentanyl, buprenorphine is safe in renal failure [31]. Further research, however, is necessary in the use of buprenorphine in neuropathic pain which should be compared to other potent mu receptor agonists and tramadol.…”

Equipotent doses to switch from high doses of opioids to transdermal buprenorphine

“…Recent experimental studies have confirmed that no refractory period between the offset of action BUP and the onset of action of other opioids mu-agonists exists. The persistent receptor occupancy has been seen in isolated receptor preparation, while under in vivo conditions the accessibility of mu-receptor sites is maintained [1,2]. Experiences in cancer pain management showed that patients who switched from other opioids encountered no problems with the conversion [3,5].…”