Lofeksidin

Lofeksidin (commonly spelled lofexidine in English) is a centrally acting alpha-2 adrenergic receptor agonist used primarily to mitigate the autonomic symptoms of acute opioid withdrawal. It is non-opioid in class and reduces noradrenergic hyperactivity in the locus coeruleus, which can lessen symptoms such as sweating, agitation, muscle aches, and gastrointestinal upset during supervised opioid discontinuation.

Clinical use is generally short-term and intended to ease withdrawal symptoms to facilitate cessation of opioids; it is not an opioid replacement therapy for long-term maintenance of dependence. Treatment courses are typically administered under medical supervision, and use should be part of a broader plan that may include psychosocial support and other clinical interventions.

Common adverse effects include hypotension, bradycardia, dizziness, somnolence and dry mouth. Because of its cardiovascular effects, blood pressure and heart rate are often monitored during therapy. Lofeksidin can interact with other centrally acting drugs, antihypertensives, and agents that affect heart rhythm; concomitant use with sedatives or substances that depress respiration requires caution. Abrupt withdrawal of centrally acting alpha-2 agonists can produce rebound sympathetic activity, so clinical guidance is advised when stopping treatment.

The compound has been approved in several jurisdictions for opioid withdrawal symptom management and has a low potential for abuse. Its adoption is usually framed within integrated addiction care rather than as a standalone solution.