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Guanfacine (GUA)

Children's Hospital Medical Center, Cincinnati · FDA-approved active Small molecule

Guanfacine is an alpha-2A adrenergic receptor agonist that reduces norepinephrine release in the brain, decreasing sympathetic nervous system activity.

Guanfacine is an alpha-2A adrenergic receptor agonist that reduces norepinephrine release in the brain, decreasing sympathetic nervous system activity. Used for Attention-deficit/hyperactivity disorder (ADHD) in children and adolescents, Hypertension.

At a glance

Generic nameGuanfacine (GUA)
SponsorChildren's Hospital Medical Center, Cincinnati
Drug classAlpha-2A adrenergic receptor agonist
TargetAlpha-2A adrenergic receptor
ModalitySmall molecule
Therapeutic areaNeurology / Psychiatry
PhaseFDA-approved

Mechanism of action

By selectively binding to alpha-2A adrenergic receptors in the prefrontal cortex and other brain regions, guanfacine decreases norepinephrine signaling, which improves attention, impulse control, and reduces hyperactivity. This mechanism makes it particularly useful for conditions characterized by executive dysfunction and hyperarousal, such as ADHD and hypertension.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results