Transdermal buprenorphine in the treatment of chronic pain

Abstract

The transdermal matrix patch formulation of buprenorphine has been shown to be effective in managing moderate-to-severe cancer pain and severe pain unresponsive to nonopioid analgesics. Clinical trials have revealed that it is possible to switch from weak opioids or low doses of step III opioids to transdermal buprenorphine without any problems. With buprenorphine patches, the sublingual buprenorphine intake was dose-dependently reduced and was superior to placebo in this respect. The proportion of responders increased with the buprenorphine dose, and a higher proportion of patients receiving buprenorphine patches reported uninterrupted sleep for longer than 6 h compared with those receiving placebo. In a long-term, open, follow-up study in which the mean duration of treatment was 7.5 months, analgesia was rated as at least satisfactory by 90% of patients. Almost 60% of patients could manage their pain with one patch alone or with one additional sublingual tablet a day during the whole period of treatment, indicating a low incidence of tolerance development. The buprenorphine transdermal patch was assessed as user friendly by 94.6% of patients. In a postmarketing surveillance study, pain relief with transdermal buprenorphine was rated as good or very good by 70% of the responders. Postmarketing surveillance studies have shown that transdermal buprenorphine is also effective in the management of nociceptive and neuropathic pain, which some studies have shown to be relatively insensitive to mu-opioid analgesics, such as morphine. Transdermal buprenorphine was well tolerated. Most adverse events were either local reactions to the patch that generally subsided within 24 h or systemic events typical of treatment with opioid analgesics, such as nausea, vomiting and constipation.

Self-treatment: Illicit buprenorphine use by opioid-dependent treatment seekers

“…This association might reflect that patients with chronic pain feel that they need increased doses of buprenorphine to relieve their comorbid pain. This hypothesis is consistent with current off-label prescribing practices for chronic pain patients reported in the pain management literature, in the form of sublingual threeor four-times-a-day dosing (Heit & Gourlay, 2008) and as a transdermal formulation in Europe (Sittl, 2005). However, there are four other primary alternative possibilities: (a) Pain patients with opioid dependence, compared with heroin users without chronic pain, might have developed stronger connections with sources of illicit prescribed opioid medication (e.g., dealers who sell or family and friends who share); (b) people with chronic pain are at an increased risk of illicit use; (c) opioid-dependent patients with pain are more likely to test buprenorphine before officially seeking OBOT treatment; and finally, (d) reducing pain might merely be a marker for an inability to tolerate distress.…”

Opioids and the treatment of chronic pain: Controversies, current status, and future directions.

“…In post-marketing surveillance studies and in a multicenter randomized controlled clinical trial, the transdermal patches were reported to be effective and well-tolerated in the treatment of cancer and non-cancer chronic pain (Griessinger et al, 2005; Sittl, 2005; Sorge and Stittl, 2004; Sittl, Nuijten, & Nautru, 2006). A transdermal formulation of buprenorphine is not presently available in the United States.…”

Buprederm™, a New Transdermal Delivery System of Buprenorphine: Pharmacokinetic, Efficacy and Skin Irritancy Studies

“…However, these dosing regimens had many disadvantages such as inconvenient management of chronic pain caused by the need for frequent administrations per day, and the possibility of the manifestation of drug toxicity due to sudden peaks in plasma drug concentrations. Therefore, transdermal delivery systems (TDS) have recently been introduced to overcome such disadvantages by maintaining a constant blood drug concentration at an effective level for analgesia and eliminating the frequent dosing (25)(26)(27)(28)(29)(30)(31) required for the management of chronic pain.…”