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Journal of Opioid Management 2021Buprenorphine's unique pharmacologic mechanisms of action lend itself to a higher level of complexity than its typical characterization as a partial agonist at µ-opioid... (Review)
Review
Buprenorphine's unique pharmacologic mechanisms of action lend itself to a higher level of complexity than its typical characterization as a partial agonist at µ-opioid receptors. It is well-documented that its additional activity at Δ- and κ-opioid receptors, and opioid receptor ligand 1 may be associated with varying degrees of analgesia and usual opioid-related adverse effects. However, novel downstream molecular and cellular mechanisms from µ-opioid receptor activation contain potential new insights into its overall unique effects. These include buprenorphine's peculiar ability to induce analgesia at escalating doses, while exhibiting a plateaued effect on respiratory depression, euphoria, gastrointestinal (GI) motility, depression, anxiety, and addictive potential. Thus, this review aims to discuss several of these emerging mechanisms to gain a better understanding of these curious actions, as well as support much of this in vitro evidence with various human clinical trial data to further support buprenorphine's place on the analgesic ladder.
Topics: Analgesia; Analgesics, Opioid; Buprenorphine; Humans; Pain; Receptors, Opioid
PubMed: 34520023
DOI: 10.5055/jom.2021.0639 -
Balkan Medical Journal Aug 2020The opioid epidemic has emerged as a major health and social problem over the last few decades. An increasing number of patients with opioid use disorder are presenting... (Review)
Review
The opioid epidemic has emerged as a major health and social problem over the last few decades. An increasing number of patients with opioid use disorder are presenting for perioperative management. These patients are either on buprenorphine or methadone for the maintenance and treatment of opioid addiction or chronic pain. In the settings of acute pain, the optimal management of patients with opioid use disorder is challenging, and recovery can be jeopardized secondary to the unique pharmacology of these agents. The purpose of this narrative review is to summarize the existing studies on the perioperative management of patients who are using buprenorphine and methadone and provide guidance for the management of patients with opioid use disorder during the perioperative period.
Topics: Buprenorphine; Humans; Methadone; Pain Management; Perioperative Care
PubMed: 32407063
DOI: 10.4274/balkanmedj.galenos.2020.2020.5.2 -
Journal of Substance Abuse Treatment Sep 2002Although pharmacotherapy has been a mainstay in opiate addiction, not much research in the development of new opiate medications has been translated into clinical... (Review)
Review
Although pharmacotherapy has been a mainstay in opiate addiction, not much research in the development of new opiate medications has been translated into clinical practice. In part, this is because opiate pharmacotherapy has not been an integral element of mainstream medical practice and because new medications developed by research are not available to clinicians. All that will change with the availability of buprenorphine for addiction treatment. For the first time in nearly a century, clinicians will be able to treat opiate addicts in the general medical setting, in the same manner they treat other patients. The unique pharmacological properties of buprenorphine, with its high patient acceptance, favorable safety profile, and ease of clinical administration, should facilitate its clinical integration. However, successful implementation will require changes in the understanding and attitude of clinicians, policymakers, and society.
Topics: Australia; Buprenorphine; Clinical Trials as Topic; France; Humans; Narcotic Antagonists; Opioid-Related Disorders; Substance Abuse Treatment Centers; United States
PubMed: 12220606
DOI: 10.1016/s0740-5472(02)00257-x -
Drugs Feb 1979Buprenorphine, a derivative of the morphine alkaloid thebaine, is a strong analgesic with marked narcotic antagonist activity. In studies in relatively small groups of... (Review)
Review
Buprenorphine, a derivative of the morphine alkaloid thebaine, is a strong analgesic with marked narcotic antagonist activity. In studies in relatively small groups of postoperative patients with moderate to severe pain, one or a few doses of buprenorphine parenterally (by intramuscular or slow intravenous injection) or sublingually were at least as effective as standard doses of other strong analgesics such as morphine, pethidine or pentazocine, and buprenorphine was longer acting than these agents. Only a small number of patients with chronic pain have received repeated doses, but in such patients there was no need for increased doses during several weeks to months of treatment. Buprenorphine appears to produce side effects which are similar to those seen with other morphine-like compounds, including respiratory depression. There is apparently no completely reliable specific antagonist for buprenorphine's respiratory depressant effect, since even very high doses of the antagonist drug naloxone may produce only a partial reversal. The respiratory stimulant drug doxapram has overcome respiratory depression in volunteers and in a few patients in a clinical setting, but such studies have not been done in an overdose situation. Animal studies and a direct addiction study in a few volunteers suggest that the dependence liability of buprenorphine may be lower than that of other older morphine-like drugs. However, a slowly emerging abstinence syndrome did occur on withdrawal after very high doses administered for 1 to 2 months. A definitive statement on the drug's dependence liability and abuse potential cannot be made until it has had much wider use for a longer period of time.
Topics: Animals; Buprenorphine; Hemodynamics; Humans; Intestinal Absorption; Kinetics; Morphinans; Narcotic Antagonists; Narcotics; Respiration; Substance-Related Disorders; Tissue Distribution
PubMed: 378645
DOI: 10.2165/00003495-197917020-00001 -
Connecticut Medicine May 1988
Review
Topics: Buprenorphine; Drug Administration Schedule; Drug Interactions; Humans
PubMed: 3042275
DOI: No ID Found -
American Journal of Health-system... Feb 2007The clinical issues surrounding the use of buprenorphine for the treatment of opioid dependence are reviewed. (Review)
Review
PURPOSE
The clinical issues surrounding the use of buprenorphine for the treatment of opioid dependence are reviewed.
SUMMARY
Opioids continue to be some of the most frequently reported prescription medications in substance abuse- related cases. A semisynthetic derivative of thebaine, buprenorphine hydrochloride is a partial mu-opioid receptor agonist and kappa-receptor antagonist with a long duration of action. The pharmacokinetic and pharmacodynamic profiles of buprenorphine are not well characterized. The ethical and legal issues associated with the maintenance treatment of opioid dependence are complex. Clinical trials have compared the efficacy of methadone, buprenorphine, and buprenorphine-naloxone for the detoxification and maintenance treatment of opioid dependence. Based on the available literature, it appears that buprenorphine, buprenorphine-naloxone, and methadone are similarly efficacious for the treatment of opioid-dependent patients. Buprenorphine-naloxone has less potential for abuse and diversion. The adverse-effect profiles for buprenorphine, buprenorphine-naloxone, and methadone are similar. Once-weekly office visits for patient evaluation and dispensing of buprenorphine seem feasible and convenient for both practitioners and patients. The three phases of opioid maintenance treatment are induction, stabilization, and maintenance. It is good practice for the admitting physician to consult with the patient's addiction treatment provider, when possible, to obtain the patient's treatment history.
CONCLUSION
Buprenorphine is an attractive option for the pharmacologic treatment of opioid dependence. Compliance and adherence to buprenorphine therapy for opioid-dependent patients remain clinical issues. Future research efforts should focus on improving compliance and adherence to buprenorphine therapy.
Topics: Analgesics, Opioid; Buprenorphine; Humans; Narcotic Antagonists; Substance-Related Disorders; United States
PubMed: 17244875
DOI: 10.2146/ajhp060403 -
Journal of Psychoactive Drugs May 2004Buprenorphine's physiological effects are produced when it attaches to specific opiate receptors that are designated mu, kappa, or delta. Buprenorphine, a partial... (Review)
Review
Buprenorphine's physiological effects are produced when it attaches to specific opiate receptors that are designated mu, kappa, or delta. Buprenorphine, a partial agonist at the mu receptor and an antagonist at the kappa receptor, produces typical morphine-like effects at low doses. At higher doses, it produces opiate effects that are less than those of full opiate agonists. Knowledge of the physiological effects of opiate receptors and the way they interact with opiate agonists, partial opiate agonists, and opiate antagonists is fundamental to understanding the safety and efficacy of buprenorphine in treatment of pain and opiate addiction. Knowledge of the historical and social context of opiate agonist treatment of opiate dependence is fundamental to understanding how nonpharmacological factors may limit the clinical adoption and utility of a safe and effective medication in treatment of opiate dependence. This article reviews the pharmacology of sublingual buprenorphine and the historical context of opiate agonist therapy; delineates classes of opiate receptors and their interaction with opiate agonists, partial agonists, and antagonists; and describes the commercially available pharmaceutical formulations of buprenorphine. It focuses on sublingual buprenorphine tablets, Subutex and Suboxone, the FDA-approved formulations of buprenorphine for treatment of opiate dependence. Sublingual buprenorphine, and the combination of sublingual buprenorphine/naloxone, have unique pharmacological properties that make them a logical first-line intervention in the treatment of opioid dependence.
Topics: Administration, Sublingual; Buprenorphine; Drug Combinations; Humans; Naloxone; Narcotic Antagonists; Opioid-Related Disorders; Private Practice; United States
PubMed: 15279124
DOI: 10.1080/02791072.2004.10400047 -
The American Journal on Addictions 2004This overview of the March 2003 conference on the U.S. national buprenorphine implementation program is developed to inform the practitioner about the positive... (Comparative Study)
Comparative Study Review
This overview of the March 2003 conference on the U.S. national buprenorphine implementation program is developed to inform the practitioner about the positive experience that has been accumulated worldwide on the use of buprenorphine for office-based practice. The first paper delineates the challenges for American psychiatry in moving buprenorphine forward into general practice. Most psychiatrists are unprepared to work with opiate-dependent patients or to use buprenorphine. The international successes with office-based buprenorphine from France and Australia are presented in the next papers, followed by presentations on several U.S. studies using buprenorphine in the community for detoxification and office-based maintenance. These experiences have thus far confirmed buprenorphine's utility and promise for opiate addiction treatment in the U.S. Finally, two national monitoring programs have been implemented to assess the public health impact of this new treatment opportunity. This opportunity has a three-year window, however, and a critical need will be to attract a sufficient number of physicians into prescribing buprenorphine/naloxone in order to allow our patients increased access to this treatment.
Topics: Attitude of Health Personnel; Buprenorphine; Community Health Services; Cross-Cultural Comparison; Diffusion of Innovation; Family Practice; Heroin Dependence; Humans; Narcotic Antagonists; Narcotics; Office Visits; Opioid-Related Disorders; Product Surveillance, Postmarketing; Psychiatry; Treatment Outcome; United States
PubMed: 15204671
DOI: 10.1080/10550490490440744 -
NIDA Research Monograph 1992
Review
Topics: Animals; Buprenorphine; Humans; Opioid-Related Disorders
PubMed: 1406910
DOI: No ID Found -
ACS Chemical Neuroscience May 2020Buprenorphine has not only had an interdisciplinary impact on our understanding of key neuroscience topics like opioid pharmacology, pain signaling, and reward...
Buprenorphine has not only had an interdisciplinary impact on our understanding of key neuroscience topics like opioid pharmacology, pain signaling, and reward processing but has also been a key influence in changing the way that substance use disorders are approached in modern medical systems. From its leading role in expanding outpatient treatment of opioid use disorders to its continued influence on research into next-generation analgesics, buprenorphine has been a continuous player in the ever-evolving societal perception of opioids and substance use disorder. To provide a multifaceted account on the enormous diversity of areas where this molecule has made an impact, this article discusses buprenorphine's chemical properties, synthesis and development, pharmacology, adverse effects, manufacturing information, and historical place in the field of chemical neuroscience.
Topics: Analgesics, Opioid; Buprenorphine; Humans; Narcotic Antagonists; Opioid-Related Disorders; Reward
PubMed: 32302475
DOI: 10.1021/acschemneuro.0c00100