LUCEMYRA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LUCEMYRA (LUCEMYRA).
LUCEMYRA (lofexidine) is a central alpha-2 adrenergic agonist that reduces the release of norepinephrine in the brain, thereby alleviating opioid withdrawal symptoms.
| Metabolism | Primarily metabolized by CYP2D6; minor contributions from CYP1A2 and CYP2C19. |
| Excretion | Renal: 63% as unchanged drug; fecal: 27% (mostly unchanged); biliary: minimal (<5%). |
| Half-life | Terminal half-life approximately 5-6 hours; no clinically significant accumulation with twice-daily dosing. |
| Protein binding | Approximately 93-94% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | 1.2-2.5 L/kg; indicates extensive tissue distribution. |
| Bioavailability | Oral: approximately 24-29% due to extensive first-pass metabolism. |
| Onset of Action | Oral: 1-2 hours for reduction of opioid withdrawal symptoms; subjective effects may begin within 30-60 minutes. |
| Duration of Action | 12-14 hours with twice-daily dosing; symptom control for most withdrawal manifestations lasts throughout dosing interval. |
18 mg orally 5-6 times daily (maximum 108 mg/day) for 7-14 days then tapered over 4-6 weeks.
| Dosage form | TABLET |
| Renal impairment | eGFR 30-59 mL/min: 18 mg every 8 hours (maximum 54 mg/day). eGFR <30 mL/min: Not recommended. |
| Liver impairment | Child-Pugh A: 18 mg every 6 hours (maximum 72 mg/day). Child-Pugh B: 18 mg every 8 hours (maximum 54 mg/day). Child-Pugh C: 18 mg every 12 hours (maximum 36 mg/day). |
| Pediatric use | Not approved for use in pediatric patients. |
| Geriatric use | Start at 18 mg every 6-8 hours; titrate cautiously due to increased sensitivity and risk of QT prolongation. Maximum 72 mg/day. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LUCEMYRA (LUCEMYRA).
| Breastfeeding | No human data on lofexidine excretion in breast milk; M/P ratio unknown. Based on low molecular weight and high protein binding, excretion is likely low. Caution is advised; monitor infant for sedation, bradycardia, and hypotension. |
| Teratogenic Risk | First trimester: Lofexidine is an alpha-2 adrenergic agonist. Human data are insufficient to determine risk; animal studies show no teratogenicity at clinically relevant doses. Second and third trimesters: Monitor for maternal hypotension and fetal bradycardia; risk of neonatal withdrawal (irritability, hypertonia, poor feeding) if used near term. |
■ FDA Black Box Warning
Risk of hypotension, bradycardia, and syncope; monitor vital signs and educate patients.
| Serious Effects |
["Concomitant use with opioid agonists (e.g., methadone, buprenorphine) except for acute detoxification","Severe coronary insufficiency, recent myocardial infarction, or cerebrovascular disease","Bradycardia or hypotension at baseline","History of syncope"]
| Precautions | ["Hypotension and orthostatic hypotension","Bradycardia","QT prolongation with electrolyte abnormalities or concomitant QT-prolonging drugs","CNS depression (avoid driving or hazardous activities)","Potential for opioid overdose (does not treat opioid use disorder)"] |
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| Fetal Monitoring | Monitor maternal blood pressure and heart rate regularly; assess for orthostatic hypotension. Fetal monitoring may include heart rate assessments; consider non-stress test in third trimester. Newborn monitored for symptoms of withdrawal if used near delivery. |
| Fertility Effects | No human studies on fertility; animal studies show no adverse effects on fertility or reproductive performance at clinically relevant doses. |