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Guanfacine

TENEX

What it isSelective alpha-2A agonist; ADHD and hypertension.

Why this oneUnlike stimulants, it is noncontrolled and can reduce hyperactivity, impulsivity, and comorbid tics.

What limits itSedation and hypotension are worst during titration. Abrupt withdrawal causes rebound hypertension; ER is not interchangeable with IR.

FDA-approved for

Off-label

FDA label

FDA dosingPopulationStartTargetMax
Hypertension (alone or with other antihypertensives, especially thiazides)Adults1 mg QHS1–2 mg QD3 mg/day (adverse reactions increase significantly above 3 mg)

Titration If 1 mg gives inadequate result after 3–4 weeks, increase to 2 mg.

Renal Use the low end of the dosing range in renal impairment; dialysis patients can receive usual doses (poorly dialyzed).

Hepatic Undefined

Instructions

Cautions

Adverse reactions

Pregnancy Not recommended for acute hypertension of pregnancy toxemia; effects on labor and delivery unknown.

Lactation Not known whether excreted in human milk (excreted in rat milk); use caution in nursing women.

NO BOXED WARNINGS

Principal riskSedation and hypotension; rebound on abrupt withdrawal

Cost, est. cash$5–$150/month

Generic entry1995

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4
Overdose danger1 / 4
Weight-gain liability0 / 4
Sedation liability1 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk1 / 4

Legacy pregnancy categoryC

Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.

Mechanism of action: Guanfacine ballicule

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

Open Guanfacine in the interactive console ↗

Memory aids: mascots and interaction avatars

Guanfacine TENEX mascot mnemonic cartoon
“Gun facing Ten X’s”
Orange plus signs → α2 agonist
Guanfacine CYP3A4 substrate avatar
CYP3A4 substrate

Open Guanfacine in the interactive console ↗