guanfacine extended-release INTUNIV

Class: Alpha 2 Adrenergic Agonist/​Phenylacetyl Guanidine Derivative
FDA Indications: ADHD
Off-Label Use:
Prescribing
Forms: 1, 2, 3, 4mg ER Tablets
Dose Range: 1-4 mg/day
Starting: 0.05 to 0.12 mg/kg once daily

NAMI drug fact sheet

Precautions
Contraindications: Use with caution in patients at risk for hypotension, bradycardia, heart block, or syncope (e.g., those taking antihypertensives).
Serious Side Effects: Hypotension, bradycardia, syncope
Side Effects: headache, sedation/somnolence, dizziness, weakness/asthenia, xerostomia, bradycardia, bradycardia
Pharmacodynamics
1° MOA: Selective α2A-adrenergic Receptor Agonism Enhances PFC Functioning → Strengthens Working Memory, ↓ Susceptibility To Distraction, ↑ Attention, ↑ Behavioral Inhibition, & ↑ Impulse Control
Target: α2A
Pharmacokinetics
t½: 12.7 (10-30)° TMAX: 6.5°
Substrate of: 3A4
Inhibits: ∅ ; Induces:
Active Metabolites:
DDIs
  • - can potentiate the action of, other CNS depressants, such as opiates or other analgesics, barbiturates or other sedatives, anesthetics, or alcohol
  • - 3A4 inhibitors can ↑ levels; likewise, 3A4 inducers can ↓ levels
Misc
  • - much more selective for α2A receptors than clonidine and also exhibits therapeutic efficacy with a reduced side-effect profile compared to clonidine
  • - 15-60X more selective for α2A than for α2B and α2C
  • - 10X weaker than clonidine at inducing sedation and ↓ blood pressure, yet it is 25X more potent in enhancing PFC function
  • - high-fat meals will ↑ absorption of the drug—Cmax ↑'s by 75% and area under the plasma concentration time curve ↑'s by 40%
Special Populations

Category B—Limited Human Data—Animal Data Suggest Low Risk

No Human Data—Potential Toxicity


Prescribe with caution d/t ↑ risk of adverse CNS effects; may cause bradycardia and orthostatic hypotension; generally not recommended

Dose reduction may be required in patients with clinically significant impairment

Dose reduction may be required in patients with clinically significant impairment

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Last updated June 10 2018 15:40:14. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.