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Guanfacine

Alpha-2 Agonist · Agent for Attention Deficit Hyperactivity Disorder

Also known as Intuniv, Tenex, Guanfacine hydrochloride

Alpha-2 AgonistAgent for Attention Deficit Hyperactivity DisorderATC C02AC02
CDSCO approvedSchedule HATC C02AC02
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Manufacturer advises avoid unless potential
FDA category + note
Top interactionssee all 12
  • AmprenavirSevereDatabaseDDInter
  • ApalutamideSevereDatabaseDDInter
  • AprepitantSevereDatabaseDDInter
  • AtazanavirSevereDatabaseDDInter

Mechanism

Guanfacine is a selective alpha-2 receptor agonist. It lowers blood pressure by activating brainstem receptors, leading to suppression of sympathetic activity and a reduction in sympathetic tone in the CNS. This sympatholytic action is responsible for its therapeutic effects in conditions like hypertension and ADHD.

Indications

ADHD (children aged 6-17 years)HypertensionTourette's syndrome (off-label)Hyperhidrosis (off-label)Mania (off-label)Posthepatic neuralgia (off-label)Psychosis (off-label)Restless leg syndrome (off-label)Ulcerative colitis (off-label)Allergy-induced inflammatory reactions in patients with extrinsic asthma (off-label)attention-deficit/hyperactivity disorder (ADHD)

Dosing

Adult
with guanfacine p. 370 treatment, the dose should be reduced or an alternative treatment offered. h Other treatment options such as bupropion hydrochloride p. 521, modafinil p. 514, tricyclic antidepressants, and venlafaxine p. 386 [all unlicensed] have been used in the management of ADHD, but due to limited evidence their use is not recommended without specialist advice.…

Pharmacokinetics

Half-life
12-24 hours
Bioavailability
Well absorbed after oral administration
Metabolism
The rest is metabolized
Excretion
About 50% appears unchanged in the urine

Contraindications

  • abrupt discontinuation (withdrawal syndrome)

Side effects

Common
DizzinessSyncopeSedationdry mouthBradycardiaFatigueConstipationOrthostatic hypotension
Serious
  • Withdrawal syndrome (upon abrupt discontinuation)
  • Hypotension
  • Cardiovascular adverse effects
  • Hypertensive crisis following abrupt withdrawal

Pregnancy & lactation

Pregnancy

Manufacturer advises avoid unless potential

Drug interactions

Amprenavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Apalutamide
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Aprepitant
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Atazanavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Berotralstat
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Boceprevir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Bosentan
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Carbamazepine
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Cenobamate
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Ceritinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Chloramphenicol
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Ciprofloxacin
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Related guidelines

Other Alpha-2 Agonist drugs

Ask House about Guanfacine

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Sources: Goodman & Gilman 14e, Harrison 22e, BNF·Verified: 2026-05-13 · House clinical team