Drug Guide
Estazolam
Classification
Therapeutic: Antianxiety agent, Sedative/Hypnotic
Pharmacological: Benzodiazepine
FDA Approved Indications
- Short-term treatment of insomnia
Mechanism of Action
Enhances the effects of gamma-aminobutyric acid (GABA) at the GABA-A receptor, resulting in sedative, anxiolytic, anticonvulsant, and muscle relaxant properties.
Dosage and Administration
Adult: Initial dose of 1 mg before bedtime, may be increased to 2 mg if needed. Dose should be individualized.
Pediatric: Not approved for pediatric use.
Geriatric: Start at lower doses (e.g., 0.5 mg), monitor closely due to increased sensitivity.
Renal Impairment: Use with caution; dose adjustment may be necessary.
Hepatic Impairment: Use with caution; lower initial doses recommended.
Pharmacokinetics
Absorption: Well absorbed orally.
Distribution: Widely distributed in body tissues, crosses the blood-brain barrier.
Metabolism: Primarily hepatic via CYP3A4 enzyme pathway.
Excretion: Metabolites excreted renally.
Half Life: Approximately 6-12 hours.
Contraindications
- Hypersensitivity to benzodiazepines.
- Acute narrow-angle glaucoma.
- Severe respiratory impairment.
Precautions
- Use with caution in elderly, patients with liver impairment, history of drug abuse, or psychiatric disorders.
- Potential for dependence, abuse, and Withdrawal symptoms.
Adverse Reactions - Common
- Drowsiness (Common)
- Dizziness (Common)
- Cognitive impairment (Common)
Adverse Reactions - Serious
- Respiratory depression (Rare but serious)
- Anterograde amnesia (Rare)
- Paradoxical reactions (e.g., agitation, aggression) (Rare)
Drug-Drug Interactions
- Other CNS depressants (e.g., alcohol, opioids, other sedatives),
- Theophylline (antagonist to benzodiazepines).
Drug-Food Interactions
- Limited interactions reported.
Drug-Herb Interactions
- Valerian, kava, and other herbal sedatives may increase CNS depression.
Nursing Implications
Assessment: Monitor mental status, level of sedation, respiratory function, and history of substance abuse.
Diagnoses:
- Risk for sedation-related adverse effects.
- Risk for dependence.
Implementation: Administer at bedtime, avoid alcohol and other CNS depressants, assess for effectiveness and adverse effects.
Evaluation: Assess sleep quality, sedation level, and adverse reactions regularly.
Patient/Family Teaching
- Take the medication exactly as prescribed, only at bedtime.
- Avoid alcohol, recreational drugs, and CNS depressants.
- Caution when operating machinery or driving.
- Notify healthcare provider if you experience excessive drowsiness, confusion, or difficulty breathing.
Special Considerations
Black Box Warnings:
- Potential for dependence, abuse, and withdrawal reactions.
- Use only for short-term management of insomnia.
Genetic Factors: No specific genetic considerations reported.
Lab Test Interference: May interfere with sleep studies or liver function tests.
Overdose Management
Signs/Symptoms: Excessive sedation, confusion, ataxia, respiratory depression, coma.
Treatment: Supportive care, airway management, activated charcoal if ingestion was recent, flumazenil as an antagonist in some cases under close monitoring.
Storage and Handling
Storage: Store at room temperature away from light and moisture.
Stability: Stable for use until expiration date on the package.