guanfacine extended-release INTUNIV
Class: Alpha 2 Adrenergic Agonist/Phenylacetyl Guanidine DerivativeFDA Indications: ADHD
Off-Label Use:
Prescribing
Forms: 1, 2, 3, 4mg ER TabletsDose Range: 1-4 mg/day
Starting: 0.05 to 0.12 mg/kg once daily
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: sedation/somnolence, dizziness, headache, weakness/asthenia, bradycardia, xerostomia, bradycardia
Pharmacodynamics
1° MOA: Selective α2A-adrenergic receptor agonism enhances PFC functioning → strengthens working memory, ↓ susceptibility to distraction, ↑ attention, ↑ behavioral inhibition, & ↑ impulse controlTarget: 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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