General Information

Lucemyra (lofexidine) is a central alpha-2 adrenergic agonist.

Lucemyra is specifically indicated for mitigation of opioid withdrawal symptoms to facilitate abrupt opioid discontinuation in adults.

Lucemyra is supplied as a tablet for oral administration. The usual starting dosage is three 0.18 mg tablets taken orally 4 times daily during the period of peak withdrawal symptoms (generally the first 5 to 7 days following last use of opioid) with dosing guided by symptoms and side effects. There should be 5 to 6 hours between each dose. The total daily dosage of Lucemyra should not exceed 2.88 mg (16 tablets) and no single dose should exceed 0.72 mg (4 tablets). Lucemyra treatment may be continued for up to 14 days with dosing guided by symptoms. Discontinue Lucemyra with a gradual dose reduction over a 2- to 4-day period to mitigate Lucemyra withdrawal symptoms.

Side Effects

Adverse effects associated with the use of Lucemyra may include, but are not limited to, the following:

orthostatic hypotension

bradycardia

hypotension

dizziness

somnolence

sedation

dry mouth

Lucemyra may cause low blood pressure or slower heart rate and should be used with caution in patients diagnosed with low blood pressure, slow heart rate, any other cardiac abnormality (including prior diagnosis or family history of long QT syndrome), or prior heart attack.

Clinical Trial Results

The FDA approval of Lucemyra was based on two randomized, double-blind, placebo-controlled trials.

Study 1

Study 1 was a 2-part efficacy, safety, and dose-response study conducted in the United States in patients meeting DSM-IV criteria for opioid dependence who were physically dependent on short-acting opioids (e.g., heroin, hydrocodone, oxycodone). The first part of the study was an inpatient, randomized, double-blind, placebo-controlled design consisting of 7 days of inpatient treatment (Days 1-7) with Lucemyra 2.16 mg total daily dose (0.54 mg 4 times daily) (n=229), Lucemyra 2.88 mg total daily dose (0.72 mg 4 times daily) (n=222), or matching placebo (n=151). Patients also had access to a variety of support medications for withdrawal symptoms.The second part of the study (Days 8-14) was an open-label design where all patients who successfully completed Days 1-7 were eligible to receive open-label treatment with variable-dose Lucemyra treatment (as determined by the investigator, but not to exceed 2.88 mg total daily dose) for up to an additional 7 days (Days 8-14) in either an inpatient or outpatient setting as determined by the investigator and the patient. No patient received Lucemyra for more than 14 days. The two endpoints to support efficacy were the mean Short Opiate Withdrawal Scale of Gossop (SOWS-Gossop) total score on Days 1 – 7 of treatment and the proportion of patients that completed 7 days of treatment. Of the randomized and treated patients, 28% of placebo patients, 41% of Lucemyra 2.16 mg, and 40% of Lucemyra 2.88 mg patients completed 7 days of treatment. The difference in proportion in both Lucemyra groups was significant compared to placebo. The mean SOWS-Gossop scores for Days 1 – 7 were 8.8, 6.5, and 6.1 for placebo, Lucemyra 2.16 mg and Lucemyra 2.88 mg, respectively, which was also significant.

Study 2

This was an inpatient, randomized, multicenter, double-blind, placebo-controlled study carried out in the United States in patients meeting DSM-IV criteria for opioid dependence who were physically dependent on short-acting opioids (e.g., heroin, hydrocodone, oxycodone). Patients were treated with Lucemyra tablets (2.88 mg/day [0.72 mg four times daily]) or matching placebo for 5 days (Days 1-5). Patients also had access to a variety of support medications for withdrawal symptoms. All patients then received placebo on Days 6 and 7 and were discharged on Day 8. The two endpoints to support efficacy were the mean SOWS-Gossop total score on Days 1 – 5 of treatment and the proportion of patients that completed 5 days of treatment. The SOWS-Gossop was administered at baseline and once daily 3.5 hours after the first morning dose on Days 1 – 5. A total of 264 patients were randomized into the study. Of the randomized and treated patients, 33% of placebo patients and 49% of Lucemyra patients completed 5 days of treatment. The difference in proportion between the two groups was significant. The mean SOWS-Gossop scores for Days 1 – 5 were 8.9 and 7.0 for placebo and Lucemyra 2.88 mg, respectively, which was statistically significant.