R E V I E W Transdermal buprenorphine in the management of persistent pain – safety aspects Rudolf Likar Pain Clinic, General Hospital Klagenfurt, Klagenfurt, Austria Correspondence: Rudolf Likar General Hospital Klagenfurt, St. Veither Strasse 47, 9026 Klagenfurt, Austria Tel +43 463 5382 6120 Fax +43 463 5382 3070 Email r.likar@aon.at Abstract: By virtue of their efficacy, opioid analgesics have long been used for the treatment of both acute and chronic pain. Concerns regarding their safety and tolerability have frequently prevented this class of drugs achieving their full therapeutic potential, and their reported association with drug abuse and dependence has led to a reduced acceptance by many patients. Indeed, there is a variety of opioid-like side effects which are common to all members of the class, but some opioids have a more favourable safety profile than others. Buprenorphine is a semisynthestic opioid with a µ-agonistic and κ-antagonistic receptor-binding profile. Studies over the past two decades have shown buprenorphine to have a complex and unique pharmacological profile, which results in enhanced therapeutic benefits combined with a favourable safety profile. Having been underused before, the development of a new transdermal drug delivery system for buprenorphine has revived interest in this substance. Transdermal buprenorphine (Gruenenthal GmbH, Aachen, Germany) provides a noninvasive method of rate-controlled drug release ensuring constant and predictable serum buprenorphine levels over a prolonged period. This preparation has been shown to be advantageous for long-term treatment of chronic pain patients providing reliable pain control, few adverse events, and good patient acceptance. Keywords: opioids, chronic pain, buprenorphine, transdermal buprenorphine, safety Introduction Opioid analgesics play an important role in the management of acute and chronic pain of both cancer and non-cancer origin, particularly where non-opioid analgesics have proven to be not effective. The World Health Organisation (WHO) guidelines for cancer pain management propose the use of an analgesic pain ladder, suggesting the use of mild opioids such as codeine for mild to moderate pain (step II) progressing to the use of strong opioids such as morphine to control severe pain (step III) (WHO 1996). Despite their proven efficacy for the control of chronic pain, the use of opioids have frequently been curtailed due to concerns regarding safety and tolerability. By its very nature, persistent pain necessitates the use of long-term therapy, which in the case of opioids leads to mostly unsubstantiated fears concerning drug abuse, addiction, and dependency. For many patients with chronic pain, however, opioid therapy may be the only effective treatment. Side effects and safety are of paramount importance in these cases where quality of life is often compromised. A number of treatment goals have now been proposed for improved patient therapy, most of which are based on the WHO recommendations. These include providing a stable plasma drug concentration to ensure long lasting and effective pain relief, formulations that provide a long duration of action, noninvasive administration, and an improved quality of life. Therapeutics and Clinical Risk Management 2006:2(1) 115 –125 © 2006 Dove Medical Press Limited. All rights reserved 115