Transdermal Buprenorphine

Abstract

Buprenorphine is a low molecular weight, lipophilic, opioid analgesic. Recently, a transdermal matrix patch formulation of buprenorphine has become available in three dosage strengths designed to release buprenorphine at 35, 52.5 and 70 micro g/h over a 72-hour period. At least satisfactory analgesia with minimal requirement for rescue medication (</=0.2 mg/day sublingual buprenorphine) was achieved by 34-50% of patients with chronic pain treated with transdermal buprenorphine 35, 52.5 or 70 micro g/h and 31% of placebo recipients, in one double-blind, placebo-controlled, randomised trial. In one trial involving patients unsuccessfully treated with weak opioids or morphine, 36.6% and 47.5% of buprenorphine 35 micro g/h and 52.5 micro g/h recipients, respectively, experienced at least satisfactory analgesia and received </=0.2 mg/day of sublingual buprenorphine compared with 16.2% of placebo recipients (both p </= 0.032). The requirement for rescue medication was reduced from baseline in >50% of patients treated with transdermal buprenorphine, in two trials. Furthermore, despite the availability of rescue medication to all patients, those receiving transdermal buprenorphine tended to experience greater pain relief, reduced pain intensity and longer pain-free sleep. Transdermal buprenorphine was generally well tolerated. Systemic adverse events were typical of opioid treatment or were attributable to the underlying disease.

Buprenorphine via drinking water and combined oral-injection protocols for pain relief in mice

“…This possible advantage of the oral over the injection route is also supported by a study performed by Kalliokoski et al (Kalliokoski, Jacobsen et al 2011), in which buprenorphine administered with Nutella® led to higher serum concentrations compared to those in mice provided with buprenorphine subcutaneously. In humans, the blood serum concentration of buprenorphine leading to effective analgesia is targeted to be approximately 0.5 ng/mL or higher (Evans and Easthope 2003), whereas in rodents blood serum concentrations of 1 ng/mL are assumed to be effective (Yassen, Olofsen et al 2005). In our study we observed higher mean and in many cases higher individual blood serum concentrations after oral administration of buprenorphine (1 mg/kg) than after subcutaneous injections (0.1 mg/kg).…”

Managing severe cancer pain: the role of transdermal buprenorphine: a systematic review

“…The 19 published articles described 16 different studies: Radbruch 29 presented the aggregated data from Bohme, 28 Sittl, 31 and Sorge; 32 Evans reported efficacy and safety data by pooling the 3 placebo-controlled RCTs; 25 and Radbruch 30 and Apolone 35 reported the preliminary information later published by Griessinger 33 and Apolone, 46 respectively. Nine were clinical trials 28,31,32,37,[39][40][41][42]44 and 7 were observational (non-intervention) studies.…”

“…The continuous release from the matrix across the skin and then into the systemic circulation is regulated mainly by the concentration gradient across the skin and the patch. 25 In the matrix patch, the drug is an integral part of the polymer structure, Buprenorphine TDS for the treatment of cancer pain Dovepress submit your manuscript | www.dovepress.com Dovepress making the delivery system more robust than the reservoir patch. This feature prevents "dose-dumping" and potential overdosing either intentionally or unintentionally, as damaging the patch does not interfere with the controlled release of medication.…”

“…TDS containing buprenorphine is available with release rates of 35, 52.5, and 70 µg/hour (Transtec ® ) that correspond to 0.8, 1.2, and 1.6 mg/day of buprenorphine or 60, 90, and 120 mg/day equivalent of oral morphine, respectively. 25,26 Recently, low-dose patches (5 to 20 µg/hour released for 7 days) have been marketed in a few countries. 26 …”

Pharmacological Management of Cancer-Related Pain

“…96 Patches reach steady state after the third consecutive application. 97 Bioavailability of the transdermal formulation is 60% compared with the intravenous route. 98 Effective plasma levels occur within 12 to 24 hours and last for 72 hours.…”