Lofexidine

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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

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

References