Drug Guide
Ethinamate
Classification
Therapeutic: Anxiolytic, Sedative
Pharmacological: Barbiturate, GABA-A receptor agonist
FDA Approved Indications
- Sedation prior to medical procedures
Mechanism of Action
Enhances the activity of gamma-aminobutyric acid (GABA) at GABA-A receptors, leading to increased chlorid ion influx and neuronal hyperpolarization, producing sedative and anxiolytic effects.
Dosage and Administration
Adult: Typically 200-400 mg orally at bedtime or divided doses. Exact dosing varies based on clinical response.
Pediatric: Use is generally not recommended due to safety concerns.
Geriatric: Start at lower doses due to increased sensitivity; monitor closely.
Renal Impairment: Adjust dose accordingly, as clearance may be reduced.
Hepatic Impairment: Use with caution; dose adjustments may be necessary.
Pharmacokinetics
Absorption: Rapidly absorbed orally.
Distribution: Widely distributed throughout body tissues; crosses the blood-brain barrier.
Metabolism: Metabolized primarily in the liver.
Excretion: Excreted mainly via the kidneys as metabolites.
Half Life: Approximately 4-6 hours.
Contraindications
- Hypersensitivity to barbiturates
- Porphyria
Precautions
- History of drug dependence
- Respiratory depression
- Pregnancy category D; can cause fetal harm
Adverse Reactions - Common
- Drowsiness (Common)
- Dizziness (Common)
- Nausea (Less common)
Adverse Reactions - Serious
- Respiratory depression (Rare)
- Hypersensitivity reactions (Rare)
- Dependence and withdrawal issues (Potential with prolonged use)
Drug-Drug Interactions
- Other CNS depressants (e.g., benzodiazepines, opioids)
Drug-Food Interactions
- Alcohol
Drug-Herb Interactions
N/ANursing Implications
Assessment: Monitor sedative effects, respiratory status, and signs of dependence.
Diagnoses:
- Risk for respiratory depression
- Risk for substance dependence
Implementation: Administer with caution, monitor patient responses, and educate about sedation effects.
Evaluation: Assess efficacy and monitor for adverse effects.
Patient/Family Teaching
- Avoid alcohol and other CNS depressants.
- Do not operate heavy machinery until effects are known.
- Report any signs of allergic reactions or unusual sedation.
Special Considerations
Black Box Warnings:
- Significant risk of respiratory depression leading to death, especially when combined with other CNS depressants.
- Risk of dependence and withdrawal.
- Use only for short-term treatment.
Genetic Factors: None specifically identified.
Lab Test Interference: May alter liver function tests.
Overdose Management
Signs/Symptoms: Profound sedation, respiratory depression, coma, hypotension.
Treatment: Supportive care, airway management, oxygen therapy, and possibly dialysis; activated charcoal if ingestion is recent.
Storage and Handling
Storage: Store at room temperature, away from light and moisture.
Stability: Stable when stored properly.