TABLE 4-1Characteristics of Medications for the Treatment of Opioid Use Disorder

CharacteristicMethadoneBuprenorphineNaltrexone
Selected BrandsDolophine, MethadoseSubutex,* Suboxone, ZubsolvDepade, Revia, Vivitrol
ClassAgonist (fully activates opioid receptors)Partial agonist (activates opioid receptors but produces a diminished response even with full occupancy)Antagonist (blocks the opioid receptors and interferes with the rewarding and analgesic effects of opioids)
Use and EffectsTaken once per day orally to reduce opioid cravings and withdrawal symptomsTaken orally or sublingually (usually once per day) to relieve opioid cravings and withdrawal symptomsTaken daily orally or monthly by injection to diminish the reinforcing effects of opioids (potentially extinguishing the association between conditioned stimuli and opioid use)
AdvantagesHigh strength and efficacy as long as oral dosing (which slows brain uptake and reduces euphoria) is adhered to; excellent option for patients who have no response to other medicationsEligible to be prescribed by certified physicians, nurse practitioners, and physician assistants, which eliminates the need to visit specialized treatment clinics and thus widens availability; lower risk of overdoseNot addictive or sedating and does not result in physical dependence; a recently approved depot injection formulation, Vivitrol, eliminates the need for daily dosing
DisadvantagesMostly available through approved outpatient treatment programs, which patients must visit daily; respiratory depression; abuse liabilitySubutex* has measurable abuse liability; Suboxone diminishes this risk by including naloxone, an antagonist that induces withdrawal if the drug is injected; for Subutex and Suboxone, withdrawal in patients dependent on methadone or short-acting prescription opioidsPoor patient compliance with the oral form (but Vivitrol should improve compliance); initiation requires attaining prolonged (e.g., 7-day) abstinence, during which withdrawal, relapse, and early dropout may occur; overdose fatality due to self-discontinuation and hypersensitized µ opioid receptors
*

Subutex (a single-agent buprenorphine product) is no longer on the market in the United States. However, multiple other generic single-agent buprenorphine products are available.

SOURCE: Adapted from Volkow et al., 2014.

From: 4, Trends in Opioid Use, Harms, and Treatment

Cover of Pain Management and the Opioid Epidemic
Pain Management and the Opioid Epidemic: Balancing Societal and Individual Benefits and Risks of Prescription Opioid Use.
National Academies of Sciences, Engineering, and Medicine; Health and Medicine Division; Board on Health Sciences Policy; Committee on Pain Management and Regulatory Strategies to Address Prescription Opioid Abuse; Phillips JK, Ford MA, Bonnie RJ, editors.
Washington (DC): National Academies Press (US); 2017 Jul 13.
Copyright 2017 by the National Academy of Sciences. All rights reserved.

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