Update on pharmacotherapy for treatment of opioid use disorder

Expert Opin Pharmacother. 2016 Dec;17(17):2307-2318. doi: 10.1080/14656566.2016.1244529. Epub 2016 Oct 20.


Opioid Use Disorder (OUD) is a significant public health concern, negatively impacting the medical, psychological, and social domains of an individual's life as well as creating substantial burdens for society. Effective treatment interventions are necessary for reduction of OUD and its consequences. Pharmacotherapy represents a central component of management. Areas covered: This review focuses on pharmacologic strategies for OUD treatment, discussing both primary as well as adjunctive therapy modalities. We will discuss both medications used during detoxification to treat withdrawal, as well as those used as maintenance therapy. Detox medications include alpha-2 adrenergic agonists, such as clonidine, as well as the μ-opioid agonist, methadone, and the μ-opioid partial agonist, buprenorphine. Opioid maintenance treatment (OMT) is also discussed, focusing on those medications meant to substitute abused opioids and includes the agonists, methadone and buprenorphine, as well as supervised intravenous heroin, and opioid antagonist, naltrexone. Expert opinion: Medication therapy for treatment of OUD has demonstrated efficacy and is of great clinical benefit. While agonist treatment with methadone or buprenorphine remains the gold standard, there is an important place for use of long-acting antagonist therapy with naltrexone. Continued investigation into treatment paradigms and behavioral platforms which optimize medication therapy is most needed.

Keywords: Opioid use disorder; buprenorphine; methadone; naltrexone; pharmacotherapy.

Publication types

  • Review

MeSH terms

  • Adrenergic alpha-2 Receptor Agonists / administration & dosage
  • Adrenergic alpha-2 Receptor Agonists / therapeutic use*
  • Buprenorphine / administration & dosage
  • Buprenorphine / therapeutic use*
  • Clonidine / administration & dosage
  • Clonidine / therapeutic use
  • Combined Modality Therapy
  • Humans
  • Methadone / administration & dosage
  • Methadone / therapeutic use
  • Naltrexone / administration & dosage
  • Naltrexone / therapeutic use
  • Narcotic Antagonists / administration & dosage
  • Narcotic Antagonists / therapeutic use*
  • Opiate Substitution Treatment / methods*
  • Opioid-Related Disorders / drug therapy*
  • Treatment Outcome


  • Adrenergic alpha-2 Receptor Agonists
  • Narcotic Antagonists
  • Buprenorphine
  • Naltrexone
  • Clonidine
  • Methadone