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NERVOUS SYSTEM › PSYCHOLEPTICS › ANXIOLYTICS › Benzodiazepine derivatives
alprazolam
N05BA12
Forms & Strengths
- Tablet: 0.25 mg, 0.5 mg, 1 mg, 2 mg
- Tablet, extended-release (XR): 0.5 mg, 1 mg, 2 mg, 3 mg
- Oral concentrate: 1 mg/mL
- Orally disintegrating tablet (ODT): 0.25 mg, 0.5 mg, 1 mg, 2 mg
Adult Dosing
- Anxiety: 0.25 mg to 0.5 mg PO TID; titrate to max 4 mg/day in divided doses
- Panic disorder: 0.5 mg PO TID; titrate gradually (max 1 mg/day increase every 3-4 days); typical dose 1-10 mg/day (immediate-release) or max 6-10 mg/day (extended-release)
- Geriatric/Debilitated: 0.25 mg PO BID to TID
Pediatric Dosing
- Safety and efficacy not established in patients under 18 years of age
Indications
- Management of generalized anxiety disorder (GAD)
- Panic disorder with or without agoraphobia
- Short-term relief of anxiety symptoms
Mechanism of Action
- Binds to GABA-A receptors in the central nervous system
- Enhances the inhibitory effects of gamma-aminobutyric acid (GABA)
- Increases chloride ion conductance, resulting in neuronal hyperpolarization, reducing CNS excitability
Contraindications
- Hypersensitivity to alprazolam or other benzodiazepines
- Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole)
- Acute narrow-angle glaucoma
Adverse Reactions
- Drowsiness, sedation, fatigue
- Lightheadedness, dizziness, impaired coordination
- Memory impairment, cognitive dysfunction
- Dry mouth, constipation, increased appetite
- Dependence, withdrawal symptoms, and rebound anxiety upon discontinuation
Drug Interactions
- CNS depressants (opioids, alcohol, other sedatives): increase risk of severe sedation, respiratory depression, and death
- CYP3A4 inhibitors (ketoconazole, fluconazole, erythromycin): significantly increase alprazolam plasma concentrations and toxicity
- CYP3A4 inducers (rifampin, carbamazepine): decrease alprazolam efficacy
- Opioids: FDA boxed warning regarding profound sedation, respiratory depression, coma, and death with concomitant use
Curated Content: Needs Vetting Before Put to Clinical Use