Lofexidine

Administration

• Type: Central alpha₂ adrenergic agonist, opioid withdrawal
• Dosage Forms: 0.18 mg tablets
• Routes of Administration: oral
• Common Trade Names: Lucemyra

Adult Dosing

Opioid Withdrawal

0.54 mg PO q6h during peak withdrawal symptoms

• Do not exceed 2.88 mg (16 tablets) per day
• Do not exceed 0.72 mg (4 tablets) in a single dose
  

May be continued for up to 14 days, gradually reduce dose over 2-4 days to mitigate Lofexidine withdrawal symptoms

Special Populations

Pregnancy Rating

• Limited information

Lactation risk

• Unknown

Renal Dosing

• eGFR 30 to 90: 0.36 mg q6h
• eGFR <30: 0.18 mg q6h
• ESRD/HD: 0.18 mg q6h, minimally dialyzable

Hepatic Dosing

• Mild impairment (Child-Pugh class A): no adjustment
• Moderate impairment (Child-Pugh class B): 0.36 mg q6h
• Severe impairment (Child-Pugh class C): 0.18 mg q6h

Contraindications

• Allergy to class/drug
• Caution with prior history or family history of long QT syndrome

Adverse Reactions

Serious

• Torsades de pointes

Common

• Orthostatic hypotension
• Bradycardia
• Dizziness
• Somnolence
• Sedation
• Insomnia
• Dry mouth

Pharmacology

• Half-life: 11 to 13 hours (first dose), 17 to 22 hours (steady state)
• Metabolism: First pass associated with gut absorption, hepatic via CYP2D6 (primary), CYP1A2, and CYP2C19
• Excretion: Urine (94%), Feces (1%)

Mechanism of Action

• Centrally acting alpha2 agonist that decreases sympathetic output and symptoms of withdrawal
• Thought to have less anti-hypertensive activity than Clonidine

Comments

• Patient's may respond to lower opioid doses increasing risk of overdose
• 0.18 mg tablet = $24.83

See Also

Opioid withdrawal