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Abstract
Oxycodone is among the most commonly used opioid analgesics for the relief of moderate-to-severe pain and is pharmacodynamically comparable to morphine. Oxycodone is available in the United States in oral dosage forms and controlled-release tablets. Studies have demonstrated marked interindividual variation in the pharmacokinetics of oxycodone. The pharmacokinetics of oral oxycodone differs from oral morphine in that it has a higher bioavailability, a slightly longer half-life, and is hepatically metabolized by cytochrome P450 rather than undergoing glucuronidation. Understanding oxycodone pharmacokinetics favors safe and effective use of this analgesic in a wide variety of patients with different levels of organ function. A MEDLINE search was conducted to identify literature published between 1966 and May 2004 relevant to the pharmacokinetics of oxycodone. These publications were reviewed and the literature summarized regarding unique and clinically important elements of oxycodone disposition including its absorption profile (immediate release, controlled release, rectal administration, and intranasal administration), distribution, and its metabolism/excretion. Special populations, including children and those with liver/renal failure, have a unique oxycodone pharmacokinetic profile that must be taken into account in order to maximize analgesic efficacy and reduce the risk of adverse events.
Additional information
Notes on contributors
Steven E. Kern
Cherokee Layson-Wolf, PharmD, is Assistant Professor at the University of Maryland School of Pharmacy. At the time that this review was conducted, she was a Community Care Pharmacy Practice Resident at Virginia Commonwealth University.
Perry G. Fine, MD, is Professor of Anesthesiology, School of Medicine and Associate Medical Director, Pain Management Center at the University of Utah Health Sciences Center, Salt Lake City; and National Medical Director, VistaCare, based in Scottsdale, AZ. This commentary is based on an article in Dr. Fine’s VistaCare Palliative Medicine Monitor.
Jonathan R. Gavrin, MD, is the Internet editor for the Journal. He is Associate Professor of Anesthesiology and Adjunct Associate Professor of Medicine at the University of Washington School of Medicine; Associate Member, Fred Hutchinson Cancer Research Center; and Associate Director for Clinical Anesthesia Services, Harborview Medical Center.
Philip J. Wiffen, is the Regional Pharmaceutical and Prescribing Adviser, Anglia & Oxford Region of the National Health Service Executive, a member of the Oxford Regional Pain Relief Unit and Coordinating Editor of the Cochrane Collaboration Pain Palliative and Supportive Care Collaborative Review Group.
Philip J. Wiffen, BPharm, MRPharmS, MFPHM (Hon) is Regional Pharmaceutical and Prescribing Adviser, Anglia & Oxford Region of the National Health Service Executive, a member of the Pain Relief Unit, Churchill Hospital, and Coordinating Editor, Cochrane Collaboration Pain Palliative and Supportive Care Collaborative Review Group.
Howard A. Heit, practices pain medicine and addiction medicine in Fairfax, Virginia, and is Assistant Clinical Professor of Medicine at Georgetown University, Washington, DC. Dr. Heit was a member of the Liaison Committee on Pain and Addiction.
Last Acts is a Robert Wood Johnson Foundation funded campaign to improve end-of-life care by a coalition of professional and consumer organizations. This coalition works to improve palliative care, focused on managing pain and making life better for individuals and families facing death. Last Acts envisions a world in which dying people and their loved ones receive excellent care and are honored and supported by their community.
S. R. Ghooi, MBBS, is a Medical Consultant in New Delhi.
Gustavo G. De Simone is Medical Oncologist (with Diploma in Palliative Medicine) and Pallium Latinoamérica Association Medical Director and Chief, Section on Palliative Care, Hospital Bonorino Udaondo, Bonpland 2287 (1425) Ciudad de Buenos Aires, Argentina ( [email protected].
The Reverend John S. Lunn, RN, MDiv, is Palliative Care and Hospice Consultant, Global Ministries for the Disciples of Christ and United Church of Christ, and former President, Board of Directors, Kauai Hospice, Hawaii.
Jan Stjernswärd, MD, PhD, FRCP (Edin), is Former Chief, Cancer and Palliative Care, World Health Organization, Geneva, Switzerland, and International Director of the Oxford University International Centre for Palliative Care and World Health Organization Collaborating Centre for Palliative Care, Churchill Hospital, Oxford, UK. He also serves on the Steering Committee of the Diana Palliative Care Initiative, Diana Princess of Wales Memorial Fund in the UK, as a Consultant to the Open Society Institute in New York, and continues to serve as a World Health Organization advisor.
Barbara L. Kass-Bartelmes, MPH, CHES, and Ronda Hughes, PhD, wrote this report for the Agency for Health Care Research and Quality (AHRQ) of the U.S. Public Health Service.
Robert J. Adams, PharmD, was at the time of this study Primary Care Resident, Pharmacy Service, Carl T. Hayden Veterans Affairs Medical Center, Phoenix, AZ.
Stephen P. Lordon, MD, was at the time of this study, Attending Physician in the Pain Management Center, University Hospitals and Clinics, and Clinical Assistant Professor of Anesthesiology, School of Medicine;
Arthur G. Lipman, PharmD, is Professor of Pharmacotherapy, College of Pharmacy, Adjunct Professor of Anesthesiology, School of Medicine and Director of Clinical Pharmacology, Pain Management Center, University Hospitals and Clinics; University of Utah Health Sciences Center.
Christopher Stock, PharmD, is Clinical Pharmacist, Substance Abuse Treatment Programs Pharmacist at the George E. Wahlen Veterans Affairs Salt Lake City Health Care System, and Clinical Associate Professor, College of Pharmacy, University of Utah
Phillip J. Wiffen, BPharm, MRPharmS, MFPHM(Hon), is Director of Training for the U.K. Cochrane Center, a member of the Oxford Regional Pain Relief Unit at Churchill Hospital, and Coordinating Editor of the Cochrane Collaboration Pain Palliative and Supportive Care Collaborative Review Group.