• James Colson, Standiford Helm, and Sanford M Silverman.
• West Virginia University Hospitals, Morgantown, WV 26506, USA. colsonj@wvuhealthcare.com
• Pain Physician. 2012 Jul 1;15(3 Suppl):ES231-6.

BackgroundOpioid misuse and abuse occurring in association with the treatment of chronic non-cancer pain are not new phenomena, but their increasing prevalence in recent years is unprecedented. Advancements in pharmaceutical technologies have provided opioid-related drugs, which lack the pure mu agonist activity characteristic of the typical opioid congeners. This absent or altered mu receptor activity imparts an opioid receptor antagonistic or partial agonistic pharmacologic action, which serves to modulate the development of opioid-induced tolerance and physical dependence and facilitate detoxification and withdrawal from opioids. Opioid antagonists and partial agonists are being used in abuse deterrent strategy regimens to prevent opioid tolerance and the development of dependence, as well as in the management of opioid detoxification and treatment of withdrawal. The specific opioid antagonists and partial agonists used in these various therapeutic modalities will be the focus of this review.ObjectivesEvaluate the comparative therapeutic utility of opioid antagonists and partial agonists in preventing the development of opioid tolerance and treating opioid dependence, detoxification, and withdrawal. A primary focus is the use of opioid antagonists and partial agonists within an office-based practice.MethodsA narrative review of the current literature involving the therapeutic use of opioid antagonists and partial agonists in the management of opioid tolerance, dependence, detoxification, and withdrawal. A computerized literature search in the PubMed, EMBASE, BioMed, and Cochrane Library review databases from 2008 through 2010 was performed. This search included systematic and narrative reviews, prospective and retrospective studies, as well as cross-references from bibliographies of notable primary and review articles and abstracts from scientific meetings. US Food and Drug Administration records and pharmaceutical manufacturers' product literature were also used in the search.ConclusionOpioid dependency, whether it results from the misuse or abuse of prescription or street drugs, continues to be a significant public health issue. Passage of DATA 2000 and US Food and Drug Administration approval of buprenorphine and buprenorphine/ naloxone has revolutionized opioid dependence therapy. The traditional addiction medicine therapy regimen of methadone maintenance, with its inherent legal limitations and restrictions, has been challenged by an office-based dependence practice with buprenorphine serving as a prominent therapeutic tool.

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