04-10-2019 What is LUCEMYRA®?

Toxicology Question of the Week     

April 10, 2019

What is LUCEMYRA®?

What is it?

Lucemyra® (lofexidine hydrochloride): 2-(1-)2,6-dichlorophenoxy(ethyl)-2-imidazoline) was recently FDA approved for the mitigation of withdrawal symptoms to facilitate abrupt discontinuation of opioids in adults. It is the first FDA approved non-opioid treatment for the management of opioid withdrawal symptoms.

How does it work?

Lofexidine is an oral, central alpha 2-adrenergic receptor agonist that reduces the release of norepinephrine and decreases sympathetic tone. Lofexidine binds to alpha-2A and alpha-2C adrenoreceptors, and due to its high selectivity for the alpha-2A receptors, it is thought to have less potent anti-hypertensive effects than clonidine. The actions of norepinephrine in the autonomic nervous system are believed to play a role in many of the symptoms of opioid withdrawal.

What is the current treatment for Opioid withdrawal?

Opioid withdrawal symptoms include anxiety, agitation, sleep problems, muscle aches, runny nose, sweating, nausea, vomiting, diarrhea and drug craving. Opioid withdrawal is typically managed by slowly tapering opioids followed by maintenance therapy with an FDA approved medication-assisted treatment drug such as methadone, buprenorphine or naltrexone or by various medications aimed at specific symptoms. Lofexidine is the first FDA approved non-opioid drug for the treatment of opioid withdrawal symptoms.

What are the adverse effects and drug handling considerations?

  • Cardiovascular effects: bradycardia, hypotension and QT prolongation
  • CNS effects: drowsiness, dizziness, insomnia
  • Gastrointestinal: dry mouth
  • Lofexidine may cause teratogenicity and reproductive toxicity
  • Use with precautions for receiving, handling, administration, and disposal Gloves (single) should be worn during receiving, unpacking, and placing in storage

Conclusion:

When Lofexidine is stopped, patients can experience a marked increase in blood pressure. The safety and efficacy of Lofexidine have not been established in children or adolescents less than 17 years of age. Clinical studies will be required to evaluate the safety of Lofexidine in clinical situations where use could be expected to exceed the maximum 14-day treatment period for which the product is currently approved.

References:

http://online.lexi.com/lco/action/doc/retrieve/docid/patch_f/4854487#cpg

https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209229s000lbl.pdf

https://www.fda.gov/newsevents/newsroom/pressannouncements/ucm607884.htm

This question was prepared by: Suparna Kumar MD, CSPI

I am interested in any questions you would like answered in the Question of the Week.  Please email me with any suggestion at donna.seger@vumc.org.

Donna Seger, MD

Executive Director

Tennessee Poison Center

www.tnpoisoncenter.org

Poison Help Hotline: 1-800-222-1222