Table of Contents

Guanfacine (Intuniv)

Primer

Pharmacokinetics

Pharmacokinetics of Guanfacine XR (Extended-Release)

Absorption Taking a high-fat meal was found to increase absorption considerably (Tmax = 5-6 hours, IR = 1-4 hours)
Distribution 6.3L/kg
Metabolism Hepatic, oxidation (phase I) and glucuronidation (phase II)
Elimination Excreted by both the liver and the kidney
Half-life • 13-14 hrs in children/adolescents

• 17-18 hours in adults

Guanfacine: Cytochrome P450 Metabolism

Substrate of (Metabolized by) 3A4 (3A5, 2C9, and 2C19)
Induces Does not induce any of the major CYP enzymes
Inhibits Does not inhibit any of the major CYP enzymes

Pharmacodynamics

Mechanism of Action

Toxicity

Indications

Dosing

Dosing for Guanfacine

Starting
Titration
Maximum
Taper Taper the daily dose no more than 1 mg every 3 to 7 days to reduce the risk of rebound hypertension.

Formulations

Monitoring

Contraindications

Absolute

Relative

Drug-Drug Interactions

Side Effects

Adverse Events

Clinical Pearls

Special Populations

Geriatric

Pediatric

Obstetric and Fetal

Medically Ill

Resources