LOFEXIDINE

Class

• Centrally acting alpha 2 agonist

LOFEXIDINE commonly prescribed for

(Bold for FDA approved)

How LOFEXIDINE works

• Stimulates alpha 2 adrenergic receptors in the brain stem, reducing sympathetic outflow from the CNS, which in turn results in improvement in withdrawal symptoms

How long until LOFEXIDINE works

• Can begin relieving withdrawal symptoms within the first day of dosing

Notable Side Effects

• Orthostatic hypotension, hypotension, dizziness, sedation, dry mouth

Life Threatening Side Effects

• Bradycardia

weight gain

unusual

sedation

common

What to do about LOFEXIDINE side effects

• Reduce dose; in particular, lower doses may be appropriate as withdrawal symptoms wane

usual dosage range

• 0.54 mg 4 times daily at 5- to 6-hour intervals

Dosage Forms

• Tablet 0.18 mg

long term use

• Not a long-term treatment

habit forming

• No

Renal Impairment

• Dose adjustment not necessary for mild impairment

• For moderate impairment, the recommended dose is 0.36 mg 4 times daily

• For severe impairment, the recommended dose is 0.18 mg 4 times daily

Hepatic Impairment

• For mild impairment, the recommended dose is 0.54 mg 4 times daily

• For moderate impairment, the recommended dose is 0.36 mg 4 times daily

• For severe impairment, the recommended dose is 0.18 mg 4 times daily

Cardiac Impairment

• Use with caution in patients at risk for hypotension, bradycardia, heart block, or syncope

Elderly

• Some patients may tolerate lower doses better

Children and Adolescents

• Safety and efficacy have not been established

Pregnancy

• Effective June 30, 2015, the FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001

• Controlled studies have not been conducted in pregnant women

• In rats and rabbits, administration of lofexidine during organogenesis caused a reduction in fetal weights, increases in fetal resorption, and litter loss at exposures below the maximum recommended human dose (MRHD)

• In rats and rabbits, administration of lofexidine during organogenesis through lactation resulted in increased stillbirths and litter loss, and offspring exhibited delays in sexual maturation, auditory startle, and surface righting, at exposures below the MRHD

• In rats, administration of lofexidine during organogenesis resulted in maternal toxicity, including death, at exposures below the MRHD

Breast Feeding

• Unknown if lofexidine is secreted in human breast milk, but all psychotropics are assumed to be secreted in breast milk