Guanfacine (Intuniv, Tenex)

Class

Alpha-2 adrenergic agonist

Mechanism

Selectively stimulates central alpha-2A adrenergic receptors, reducing sympathetic outflow, which lowers blood pressure and enhances prefrontal cortical regulation of attention and impulse control.

FDA-Approved Use

Hypertension, attention-deficit/hyperactivity disorder (ADHD)

Off-Label Use

Tic disorders, sleep disturbances, agitation and aggression in neurodevelopmental disabilities (especially with hyperactivity or impulsivity)

Formulation

Immediate-release tablets (Tenex), extended-release tablets (Intuniv)

Titration

Start at 1 mg p.o. nightly, titrate slowly based on clinical response, typical dose range 1–4 mg/day

Dose Range

1–4 mg/day

Kinetics

Immediate-release half-life approximately 10–17 hours; extended-release half-life approximately 17 hours. Metabolized hepatically (CYP3A4), excreted renally.

Common AEs

Drowsiness, headache, abdominal pain, dry mouth

Serious/Rare AEs

Hypotension, bradycardia (monitor especially in elderly or cardiac patients)

Monitoring

Monitor blood pressure and heart rate regularly; assess sedation

Black Box Warning

None

Considerations

Use caution in elderly patients due to increased risk of hypotension and orthostatic falls. Guanfacine may benefit individuals with neurodevelopmental disorders by improving attention and reducing tics. Dose adjustments may be necessary in hepatic impairment.