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