Drug Guide
Alprazolam
Classification
Therapeutic: Anti-anxiety agent, Anxiolytic
Pharmacological: Benzodiazepine
FDA Approved Indications
- Anxiety disorders
- Panic disorder with or without agoraphobia
Mechanism of Action
Alprazolam enhances the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABA-A receptor, resulting in sedative, anxiolytic, muscle relaxant, and anticonvulsant properties.
Dosage and Administration
Adult: Initial dose is usually 0.25 to 0.5 mg three times daily. Dosage may be increased gradually based on response and tolerability. Max dose typically not exceeding 4 mg/day.
Pediatric: Use is not generally recommended for children due to safety concerns.
Geriatric: Start at lower doses (e.g., 0.25 mg twice daily) and titrate carefully, considering increased sensitivity and risk of sedation and falls.
Renal Impairment: Use with caution; may require dose adjustment.
Hepatic Impairment: Use with caution; lower doses recommended due to reduced metabolism.
Pharmacokinetics
Absorption: Rapidly absorbed following oral administration.
Distribution: Widely distributed in body tissues, crosses blood-brain barrier.
Metabolism: Metabolized in the liver mainly via CYP3A4 to inactive metabolites.
Excretion: Excreted primarily via the urine as inactive metabolites.
Half Life: Approx. 11-16 hours, longer in the elderly.
Contraindications
- Hypersensitivity to benzodiazepines or any component of the formulation.
- Pregnancy (especially in the first trimester) and breastfeeding.
Precautions
- Use with caution in patients with a history of substance abuse, CNS depression, hepatic impairment, or respiratory impairment. Risk of dependence, tolerance, and withdrawal with extended use.
Adverse Reactions - Common
- Drowsiness (Common)
- Dizziness (Common)
- Fatigue (Common)
- Memory impairment (Common)
Adverse Reactions - Serious
- Respiratory depression (Rare)
- Anterograde amnesia (Rare)
- Dependence and withdrawal syndrome (Serious if misuse or abrupt discontinuation)
Drug-Drug Interactions
- CNS depressants (opioids, alcohol, other sedatives) increase risk of respiratory depression and sedation.
- Hepatic enzyme inhibitors (e.g., ketoconazole, clarithromycin) can increase alprazolam levels.
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor for signs of sedation, respiratory depression, dependence, and withdrawal. Assess anxiety levels and mental status.
Diagnoses:
- Risk for overdose related to potentiation by other CNS depressants.
- Risk for injury due to sedation or impaired coordination.
Implementation: Administer doses as prescribed. Caution patients to avoid alcohol and other CNS depressants. Gradually taper to discontinue to avoid withdrawal.
Evaluation: Evaluate patient's response, side effects, and signs of dependence or overdose.
Patient/Family Teaching
- Instruct patients to follow the prescribed dose and not to self-medicate.
- Warn against alcohol and other CNS depressants while taking alprazolam.
- Advise about the potential for dependence and the importance of not stopping abruptly.
Special Considerations
Black Box Warnings:
- Use with extreme caution in the elderly due to risk of cognitive impairment, falls, fractures, and increased mortality.
- Risks of dependence, abuse, and withdrawal with prolonged use.
Genetic Factors: Metabolism varies with CYP3A4 activity; some populations may have altered drug levels.
Lab Test Interference: None known.
Overdose Management
Signs/Symptoms: Extreme sedation, confusion, diminished reflexes, coma, respiratory depression, hypotension.
Treatment: Supportive care with monitoring vital signs. Activated charcoal if ingestion is recent. Flumazenil can be used as an antidote in some cases, but risk of seizures and withdrawal must be considered.
Storage and Handling
Storage: Store at room temperature 20-25°C (68-77°F), away from moisture, heat, and light.
Stability: Stable under proper storage conditions.