Withdrawal symptoms are caused by rebound hyperactivity of the biological systems suppressed by opioids

Watch how LUCEMYRA® helps alleviate symptoms of opioid withdrawal

Opioid use leads to inhibition of an enzyme (adenylyl cyclase) in the brain resulting in reduced levels of norepinephrine1

Levels of norepinephrine in the brain and effects of opioid use - LUCEMYRA
  • Over time, the brain compensates for the chronic inhibition of norepinephrine by producing higher levels of the enzyme that produces the hormone

When opioids are discontinued after chronic use, the inhibitory effect on the enzyme is lost—resulting in excessively high levels of norepinephrine1

Sudden overproduction of norepinephrine - LUCEMYRA
  • This surge of norepinephrine is what causes the clinical symptoms of withdrawal

LUCEMYRA is a central alpha-2 adrenergic agonist that binds to receptors in the brain2

LUCEMYRA binds to alpha-2 adrenergic receptors in the brain
  • This reduces the release of norepinephrine and mitigates the symptoms of noradrenergic hyperactivity (withdrawal symptoms) that occur when the inhibitory effect of opioids is removed following abrupt opioid discontinuation

References:

  1. Kosten TR, George TP. The neurobiology of opioid dependence: implications for treatment. Sci Pract Perspect. 2002;1(1):13-20.
  2. LUCEMYRA® (lofexidine) [Prescribing Information]. USWM, LLC; 2020.