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NERVOUS SYSTEM › PSYCHOLEPTICS › ANXIOLYTICS › Benzodiazepine derivatives
ethyl loflazepate
N05BA18
Forms & Strengths
- Tablets: 1 mg
- Tablets: 2 mg
Adult Dosing
- Anxiety: Initially 1 to 2 mg orally once daily, adjusted based on clinical response up to a maximum of 4 mg daily.
- Geriatric/Debilitated patients: Start with 0.5 to 1 mg daily.
Pediatric Dosing
- Safety and efficacy in pediatric patients under 18 years have not been established.
Indications
- Management of anxiety disorders
- Short-term relief of anxiety symptoms
Mechanism of Action
- Binds to benzodiazepine binding sites on GABAA receptor complexes in the central nervous system.
- Enhances GABA-mediated inhibitory neurotransmission, leading to anxiolytic, sedative, muscle relaxant, and anticonvulsant effects.
Contraindications
- Hypersensitivity to benzodiazepines or ethyl loflazepate
- Acute narrow-angle glaucoma
- Severe respiratory insufficiency
- Severe hepatic impairment
- Sleep apnea syndrome
Adverse Reactions
- Drowsiness and sedation
- Dizziness and lightheadedness
- Ataxia and muscular weakness
- Cognitive impairment and confusion
- Dependence and withdrawal syndrome with prolonged use
Drug Interactions
- Central nervous system depressants (opioids, alcohol, barbiturates): Enhanced sedative and respiratory depressant effects.
- CYP3A4 inhibitors (ketoconazole, erythromycin): May increase plasma concentrations of active metabolites.
- CYP3A4 inducers (rifampin, carbamazepine): May decrease plasma concentrations and efficacy of ethyl loflazepate.
Curated Content: Needs Vetting Before Put to Clinical Use