What is suboxone?

History of Use

Buprenorphine has been available since the 1980s in injectable and sublingual dosage forms prescribed for pain management. Since 2002, sublingual formulations with and without naloxone have been used primarily as safer alternates to methadone in opioid detoxification and dependence programs. Subutex, a formulation containing only buprenorphine, is sometimes ground up and injected or inhaled by patients to maximize the euphoric effects of the drug. Including naloxone in a one-to-four-part ratio with buprenorphine limits the abuse potential of the drug; naloxone blocks the effects of opiates such as heroin and leads to immediate withdrawal symptoms.

Use in the United States is limited by the Drug Addiction Treatment Act of 2000. A Risk Evaluation and Mitigation Strategy, approved by the US Food and Drug Administration, is available for the drug to ensure proper medication use and to limit abuse and diversion; this program allows primary care physicians to prescribe the medication, improving access to treatment. A transdermal patch containing buprenorphine (Butrans) is available for pain management only.

Effects and Potential Risks

Buprenorphine is a potent partial agonist at the mu (µ) opioid receptor. Because buprenorphine binds more strongly than other opioids to receptors in the brain, it limits the effect of opioids in patients taking buprenorphine and can effectively block the effect of high-dose heroin, making it ideal for opioid treatment programs.

The side-effect profile is similar to that of other opioids, including nausea, vomiting, constipation, sweating, headache, drowsiness, and dizziness; side effects are less frequent than with morphine. Respiratory depression is not likely to occur unless buprenorphine is taken with central nervous system depressants, such as alcohol or benzodiazepine; deaths have been reported in persons taking benzodiazepine who also inject buprenorphine products.

Naloxone is a mu (µ) antagonist used in opioid overdose, primarily in cases involving heroin or morphine. It is not an effective antagonist to buprenorphine because of the high binding affinity of buprenorphine to the opioid receptors. The drug combination is preferred in cases where unsupervised administration of the drug is occurring, as both buprenorphine and naloxone can block or reverse opiate effects from other opioids such as heroin, morphine, and methadone; intravenous abuse of Suboxone leads to immediate withdrawal symptoms in persons continuing to abuse other opioids.

Bibliography

Collins, Gregory B., and Mark S. McAllister. “Buprenorphine Maintenance: A New Treatment for Opioid Dependence.” Cleveland Clinic Journal of Medicine 74 (2010): 514–20. Print.

Kahan, Meldon, et al. “Buprenorphine: New Treatment of Opioid Addiction in Primary Care.” Canadian Family Physician 57 (2011): 281–89. Print.

Lang Walter, et al. “From Research to the Real World: Buprenorphine in the Decade of the Clinical Trials Network.” Journal of Substance Abuse and Treatment 38, suppl. 1 (2010): S53–60. Print.

MacGillis, Alec. "The Wonder Drug: Why Are Drug Courts Denying Heroin Addicts the Medicine They Need?" Slate. Slate, 9 Feb. 2015. Web. 10 Nov. 2015.

Reilly, Adam. "Suboxone: A Miracle Drug or Merely a Step in the Right Direction?" WGBH. WGBH, 9 Nov. 2015. Web. 10 Nov. 2015.

Svrluga, Susan. "The Drug Suboxone Could Combat the Heroin Epidemic. So Why Is It So Hard to Get?" Washington Post. Washington Post, 13 Jan. 2015. Web. 10 Nov. 2015.