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British Journal of Anaesthesia, 2003, Vol. 90, No. 6 722-724
© 2003 The Board of Management and Trustees of the British Journal of Anaesthesia

III. Old dog—new (ma)trix{dagger}

K. Budd1 and B. J. Collett2

1 ‘Newlands’, Chevin Avenue, Menston, Ilkley LS29 6E, West Yorkshire, UK E-mail: keithbudd@tiscali.co.uk 2 Pain Management Centre, Leicester Royal Infirmary, Leicester LE1 5WW, UK E-mail: wreake@aol.com

{dagger}Declaration of interest. Dr Collett was a member of the Transtec Advisory Board (two Meetings) organised by Napp Pharmaceuticals and has been in receipt of three travel grants from that company over the last 5 years. Dr Budd was a member of the Transtec Advisory Boards of Napp Pharmaceuticals and Grunenthal GmbH and has received lecture and travel expenses from both companies.

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Buprenorphine has been an enigmatic opioid since it was first launched for clinical use in 1979. Whilst having significant potential as a strong opioid, perhaps even rivalling morphine, it has never achieved the promising future predicted for it. Why?

The main problem appears to be that a number of misconceptions arose early in buprenorphine’s pre-clinical and clinical exposure relating to a lack of scientific studies in specific areas of its pharmacological activity. These included buprenorphine’s partial agonism and the associated ceiling effect with its implied limitation of analgesia. There were also difficulties in understanding of the ‘bell-shaped’ dose–response curve, and the possibility that blockade of the mu-opioid receptor by the avid binding of buprenorphine led to the inability of other opioids to bind and be effective. Non-naloxone reversibility . . . [Full Text of this Article]


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