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Guanfacine ER

INTUNIV

What it isGuanfacine ER (INTUNIV, 2009) is a selective alpha-2A agonist for nonstimulant ADHD treatment; approved ages: 6-17.

Why this oneDuration of action 24 h (Carlat Table 1); greater alpha-2A selectivity makes it less sedating and hypotensive than clonidine.

What limits itER is NOT 1:1 with IR; no high-fat meals. Sedation, bradycardia and hypotension limit use; taper rather than stopping abruptly to prevent rebound hypertension.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
ADHD (monotherapy or adjunct to stimulants)Children/adolescents 6-17 yr1 mg QD0.05-0.12 mg/kg/day (1-7 mg)4 mg/day (ages 6-12); 7 mg/day (ages 13-17)

Titration Adjust in increments of no more than 1 mg/week

Renal May need dosage reduction in significant renal impairment

Hepatic May need dosage reduction in significant hepatic impairment

Halve dose with strong/moderate CYP3A4 inhibitors; consider doubling with CYP3A4 inducers

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy Available data over decades have not identified a drug-associated risk; use in pregnancy has been infrequent

Lactation No data on presence in human milk; monitor breastfed infant for hypotension/bradycardia (sedation, lethargy, poor feeding)

NO BOXED WARNINGS

Principal riskSedation and hypotension; rebound on abrupt withdrawal

Classes and tags

Clinical profile

Direct muscarinic antagonism0 / 4

Mechanism of action: Guanfacine ER ballicule

Guanfacine ER ballicule: receptor binding, kinetics and half-life diagram

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Memory aids: mascots and interaction avatars

Guanfacine ER INTUNIV mascot mnemonic cartoon
“Gun facing In-tune tuna”
Orange plus signs → α2 agonist
Guanfacine ER CYP3A4 substrate avatar
CYP3A4 substrate

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