Alprazolam (Xanax)

Class

Benzodiazepine

Mechanism

Potentiates the effects of GABA at the GABA-A receptor by increasing the frequency of chloride channel opening, resulting in anxiolytic, sedative, muscle-relaxant, and anticonvulsant effects.

FDA-Approved Use

Generalized anxiety disorder (GAD), panic disorder

Off-Label Use

Acute agitation, refractory anxiety symptoms, short-term management of severe situational anxiety

Formulation

Oral tablet, orally disintegrating tablet (ODT), extended-release tablet, oral solution

Titration

Start at 0.25–0.5 mg orally three times daily; titrate gradually based on response and tolerability

Dose Range

0.25–4 mg/day in divided doses

Kinetics

Rapid onset of action with short half-life (typically 6–12 hours); metabolized via CYP3A4; high risk of withdrawal symptoms with abrupt discontinuation

Common AEs

Sedation, dizziness, memory impairment, fatigue, emotional blunting, reduced concentration

Serious/Rare AEs

Dependence, withdrawal (including seizures), respiratory depression, mood lability, paradoxical disinhibition (especially in elderly)

Monitoring

Monitor for sedation, cognitive and psychomotor effects, mood changes, and signs of misuse or dependence; reassess need regularly

Black Box Warning

Risk of profound sedation, respiratory depression, coma, and death when used with opioids. Risk of dependence, misuse, and withdrawal with prolonged use.

Considerations

Use with caution in elderly adults and patients with dementia due to elevated risks of falls, delirium, and cognitive impairment. The short half-life and rapid onset increase the likelihood of rebound anxiety and withdrawal, particularly with abrupt discontinuation. Avoid in patients with a history of substance use disorder unless closely monitored. If used, prescribe the lowest effective dose for the shortest necessary duration.