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Guanfacine – Alpha-2A Adrenergic Agonist for ADHD (Rx)

Guanfacine is a selective alpha-2A adrenergic receptor agonist indicated for the treatment of attention deficit hyperactivity disorder (ADHD) in children, adolescents, and adults (depending on region and formulation). It works by strengthening prefrontal cortex regulation, improving attention, impulse control, and working memory.

Unlike stimulant medications, guanfacine does not directly increase dopamine release but instead modulates noradrenergic signaling, making it a suitable option for patients who cannot tolerate stimulants or require adjunctive therapy.

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It is commonly available in extended-release (ER) formulations for once-daily dosing.

Tärkeimmät tiedot

• Active Ingredient: Guanfacine
• Drug Class: Alpha-2A adrenergic receptor agonist
• Käyttöaiheet:
  • ADHD (monotherapy or adjunct to stimulants)
• Mechanism of Action: Enhances prefrontal cortical function via α2A receptor stimulation
• Therapeutic Effects: Improved attention, reduced impulsivity, behavioral regulation
• Reseptistatus: Vain reseptillä myytävä lääke

Määrittelyt

• Dosage Forms: Extended-release tablets
• Common Strengths: 1 mg, 2 mg, 3 mg, 4 mg
• Administration: Oral, once daily (usually evening or morning)
• Onset of Effect: Gradual (over several days to weeks)
• Half-Life: ~17 hours
• Metabolism: Hepatic via CYP3A4
• Excretion: Renal (and hepatic metabolites)
• Varastointi: Huoneenlämpö

Annostus ja antotapa

• Initial dose: Typically 1 mg once daily
• Gradual titration based on response and tolerability
• Maximum dose varies (commonly up to 4–7 mg depending on guidelines)
• Tablets should be swallowed whole (not crushed or chewed)

Yhteensopivuus / Soveltuvuus

• Children and adolescents with ADHD
• Patients who do not tolerate stimulant medications
• Individuals requiring adjunct therapy with stimulants
• Suitable for patients with sleep disturbances or tics (where stimulants may worsen symptoms)
• Requires medical supervision and monitoring

Lääkkeiden yhteisvaikutukset

• CYP3A4 inhibitors (e.g., ketoconazole): Increased guanfacine levels
• CYP3A4 inducers (e.g., rifampicin): Reduced effectiveness
• CNS depressants: Increased sedation
• Antihypertensives: Additive blood pressure-lowering effects

Why Choose Guanfacine?

Guanfacine offers a non-stimulant alternative for ADHD management, with benefits in improving attention and impulse control while also helping with associated symptoms like sleep disturbances and hyperactivity. Its once-daily dosing makes it convenient for long-term therapy.