Current Knowledge of Buprenorphine and Its Unique Pharmacological Profile
Joseph Pergolizzi MD,
Anna Maria Aloisi MD, PhD, Albert Dahan MD, PhD,
Joerg Filitz MD,
Richard Langford MD, PhD,
Rudolf Likar MD, FRCA,
Sebastiano Mercadante MD,
Bart Morlion MD, Robert B. Raffa PhD,
Rainer Sabatowski MD,
Paola Sacerdote PhD,
Luis M. Torres MD, PhD,
Avi A. Weinbroum MD,
Corresponding Author
Joseph Pergolizzi MD
Johns Hopkins University, Baltimore, Maryland, U.S.A.;
Joseph Pergolizzi, MD, 4840 Sycamore Drive, Naples, FL 34119, U.S.A. E-mail: [email protected].Search for more papers by this authorAlbert Dahan MD, PhD
Leiden University Medical Center, Department of Anesthesiology, Leiden, The Netherlands;
Search for more papers by this authorJoerg Filitz MD
Department of Anesthesiology, University Hospital Erlangen, Erlangen, Germany;
Search for more papers by this authorRichard Langford MD, PhD
St Bartholomew's Hospital, London, U.K.;
Search for more papers by this authorRudolf Likar MD, FRCA
Pain Clinic, General Hospital Klagenfurt, Klagenfurt, Austria;
Search for more papers by this authorSebastiano Mercadante MD
La Maddalena Cancer Centre, Palermo, Sicily, Italy;
Search for more papers by this authorRobert B. Raffa PhD
School of Pharmacy and School of Medicine, Temple University, Philadelphia, Pennsylvania, U.S.A.;
Search for more papers by this authorRainer Sabatowski MD
Department of Anesthesiology and Intensive Care, University Hospital Carl Gustav Carus, Dresden, Germany;
Search for more papers by this authorPaola Sacerdote PhD
Department of Pharmacology, University of Milan, Milan, Italy;
Search for more papers by this authorLuis M. Torres MD, PhD
Anesthesiology, Intensive Care and Pain Unit Department, University Hospital, Puerta del Mar, Cadiz, Spain;
Search for more papers by this authorAvi A. Weinbroum MD
Post Anesthesia Care Unit, Tel Aviv Sourasky Medical Center, Tel Aviv, Israel
Search for more papers by this authorJoseph Pergolizzi MD,
Anna Maria Aloisi MD, PhD, Albert Dahan MD, PhD,
Joerg Filitz MD,
Richard Langford MD, PhD,
Rudolf Likar MD, FRCA,
Sebastiano Mercadante MD,
Bart Morlion MD, Robert B. Raffa PhD,
Rainer Sabatowski MD,
Paola Sacerdote PhD,
Luis M. Torres MD, PhD,
Avi A. Weinbroum MD,
Corresponding Author
Joseph Pergolizzi MD
Johns Hopkins University, Baltimore, Maryland, U.S.A.;
Joseph Pergolizzi, MD, 4840 Sycamore Drive, Naples, FL 34119, U.S.A. E-mail: [email protected].Search for more papers by this authorAlbert Dahan MD, PhD
Leiden University Medical Center, Department of Anesthesiology, Leiden, The Netherlands;
Search for more papers by this authorJoerg Filitz MD
Department of Anesthesiology, University Hospital Erlangen, Erlangen, Germany;
Search for more papers by this authorRichard Langford MD, PhD
St Bartholomew's Hospital, London, U.K.;
Search for more papers by this authorRudolf Likar MD, FRCA
Pain Clinic, General Hospital Klagenfurt, Klagenfurt, Austria;
Search for more papers by this authorSebastiano Mercadante MD
La Maddalena Cancer Centre, Palermo, Sicily, Italy;
Search for more papers by this authorRobert B. Raffa PhD
School of Pharmacy and School of Medicine, Temple University, Philadelphia, Pennsylvania, U.S.A.;
Search for more papers by this authorRainer Sabatowski MD
Department of Anesthesiology and Intensive Care, University Hospital Carl Gustav Carus, Dresden, Germany;
Search for more papers by this authorPaola Sacerdote PhD
Department of Pharmacology, University of Milan, Milan, Italy;
Search for more papers by this authorLuis M. Torres MD, PhD
Anesthesiology, Intensive Care and Pain Unit Department, University Hospital, Puerta del Mar, Cadiz, Spain;
Search for more papers by this authorAvi A. Weinbroum MD
Post Anesthesia Care Unit, Tel Aviv Sourasky Medical Center, Tel Aviv, Israel
Search for more papers by this authorDisclosure: Dr. Pergolizzi is a consultant for Grünenthal GmbH. There was industry funding involved in the Expert meeting sponsored by Grünenthal GmbH, Aachen, Germany and editorial support.
Abstract
Despite the increasing clinical use of transdermal buprenorphine, questions have persisted about the possibility of a ceiling effect for analgesia, its combination with other μ-opioid agonists, and the reversibility of side effects. In October 2008, a consensus group of experts met to review recent research into the pharmacology and clinical use of buprenorphine. The objective was to achieve consensus on the conclusions to be drawn from this work. It was agreed that buprenorphine clearly behaves as a full μ-opioid agonist for analgesia in clinical practice, with no ceiling effect, but that there is a ceiling effect for respiratory depression, reducing the likelihood of this potentially fatal adverse event. This is entirely consistent with receptor theory. In addition, the effects of buprenorphine can be completely reversed by naloxone. No problems are encountered when switching to and from buprenorphine and other opioids, or in combining them. Buprenorphine exhibits a pronounced antihyperalgesic effect that might indicate potential advantages in the treatment of neuropathic pain. Other beneficial properties are the compound's favorable safety profile, particularly in elderly patients and those with renal impairment, and its lack of effect on sex hormones and the immune system. The expert group agreed that these properties, as well as proven efficacy in severe pain and favorable tolerability, mean that buprenorphine can be considered a safe and effective option for treating chronic cancer and noncancer pain.
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