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.