What are the Important Side effects of Lucemyra (Lofexidine)?

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Lofexidine lucemyra side effects moa opioid withdrawal

Lucemyra side effects are primarily because of its mechanism of action. Lucemyra is the brand name of Lofexidine hydrochloride. It is the first FDA-approved treatment of opioid withdrawal that is unrelated to the opioid class of medicines.

Briefly about the treatment of Opioid withdrawal:

Opioid withdrawal symptoms may manifest as nausea, vomiting, sweating, hot and cold flashes, inability to sleep, diarrhea, watery discharge from the nose and eyes, and muscle cramps. So, the treatment is aimed to manage these withdrawal symptoms and simultaneously slowly taper off the opioids.

One strategy of opioid withdrawal treatment is to administer a lower potency opioid such as codeine phosphate, buprenorphine, and methadone. However, giving opioids to patients addicted to opioids has its challenges and needs close monitoring and follow-ups.

The other strategy is to treat the patient symptomatically. This strategy is helpful only n patients addicted to mild opioids. Among the non-opioid medications, clonidine and Lofexidine can be used in patients with moderate to severe symptoms of opioid withdrawal.

What is the MOA of Lucemyra (Lofexidine)?

Lucemyra (Lofexidine) helps patients with symptoms of opioid withdrawal by inhibiting the neurochemical surge associated with it. Lucemyra binds to the alpha 2A and alpha 2C adrenergic receptors and inhibits the release of catecholamine.

The catecholamine surge associated with opioid withdrawal causes most of the symptoms of opioid withdrawal including aggression, insomnia, palpitations, flushing, hypertension, and muscle cramps. Inhibiting the release of catecholamine results in an improvement in these symptoms.

Lucemyra inhibits the Catecholamine Surge


Side effects of Lucemyra (Lofexidine):

The most common side effects that affect more than 10% of the patients are related to low catecholamine levels in the blood. Since catecholamines cause vasoconstriction, increase the heart rate, and elevate the blood pressure, their inhibition with lofexidine results in the opposite symptoms.

  • Postural Hypotension:

    • Patients may report syncope and dizziness. This is mostly due to the low blood pressure when the person is in the erect posture or standing after prolonged sitting. Syncope, dizziness, and postural hypotension are common in dehydrated and volume-depleted patients. Also, if the person is taking medications that lower the blood pressure, the likelihood of postural hypotension is more.

Syncope and Postural hypotension

  • Other cardiovascular side effects:

    • Lofexidine may cause bradycardia. Bradycardia is common in patients on concomitant AV-nodal blocking drugs and beta-blockers. Bradycardia and hypotension are also common in patients with kidney disease, those who have had a recent myocardial infarction or angina, and those with a low baseline heart rate.
    • Lofexidine (Lucemyra) is also associated with QT-interval prolongation. The QT-interval prolongation is more common if the patient is taking concomitant drugs that prolong the QT interval and in patients with electrolyte disorders. QT-interval prolongation may result in cardiac arrhythmias including ventricular tachycardia and ventricular fibrillation. Patients should have a baseline ECG done and monitored periodically. Patients with liver and kidney disease should be advised Lofexidine with caution.

Bradycardia and QT-interval Prolongation

  • Central nervous system side effects:

    • The loss of catecholamine surge results in dizziness, drowsiness, and central nervous system depressant effect. Patients may notice an impairment of physical and mental abilities and may not be able to perform tasks that require mental and physical alertness. Patients should be advised to avoid driving, operating heavy machinery, or perform other tasks that require mental alertness.
    • Some patients may also report insomnia. This could be a sign of opioid withdrawal or an inadequate dose of lofexidine. However, lack of sleep has been reported in patients on treatment with lofexidine.

Impaired mental and physical abilities

  • Other Side effects of Lucemyra:

    • Other relatively less common side effects reported with lofexidine are dry mouth and tinnitus. A dry mouth may be a sign of opioid withdrawal or an incomplete lofexidine dose. Tinnitus is a sensation of ringing bells in the ears. It could be secondary to vasodilation or opioid withdrawal.

Xerostomia and Tinnitus

  • Oversensitivity to opioids:

    • Patients on treatment with Lofexidine may become oversensitive to small doses of opioids. This could result in the life-threatening toxicity of opioids. Patients may become drowsy and develop shallow breathing, bradycardia, and low blood pressure.
    • It is important to warn the patients when initiating treatment with Lucemyra.

Oversensitivity to Opioids