Lofexidine: A Newly FDA-Approved, Nonopioid Treatment for Opioid Withdrawal

Objective: To review the pharmacology, efficacy, and safety of lofexidine for the treatment of opioid withdrawal secondary to the recent Food and Drug Administration (FDA) approval.

Data Sources: A literature search using PubMed was conducted (inception to December 2018) using the terms lofexidine, opioid, opiate, and withdrawal. References from retrieved articles and the prescribing information were reviewed for any additional material.

Study Selection/data Extraction: The literature search was limited to human studies published in English that pertained to human pharmacology, pharmacokinetics, pharmacodynamics, dosing, efficacy, and safety regarding opioid withdrawal. Phase I, II, and III studies of lofexidine for opioid withdrawal were reviewed for inclusion.

Data Synthesis: Lofexidine is newly FDA approved in the United States for the treatment of opioid withdrawal symptoms in adults. Several randomized controlled trials and a Cochrane review noted the effectiveness of lofexidine versus placebo for this indication. The efficacy of lofexidine has also been shown to be comparable to that of other indicated first- and second-line pharmacological agents. Relevance to Patient Care and Clinical Practice: This article examines the trials that led to lofexidine's new FDA-approved indication as well as other recent literature published since its last major review, seeking to guide providers in the appropriate use of lofexidine for its new indication.

Conclusions: Lofexidine is an effective and safe agent in treating symptoms related to opioid withdrawal in adults when compared with placebo; although it is more widely accessible than other first-line therapies, its use in practice may be limited by cost.