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NERVOUS SYSTEM › PSYCHOLEPTICS › HYPNOTICS AND SEDATIVES › Benzodiazepine derivatives
brotizolam
N05CD09
Adult Dosing
- Short-term management of insomnia: 0.25 mg orally once daily immediately before bedtime
- Elderly or debilitated patients: 0.125 mg orally once daily immediately before bedtime
- Duration of treatment should be as short as possible, generally not exceeding 2 weeks
Pediatric Dosing
- Safety and efficacy in pediatric patients under 18 years have not been established; use is not recommended
Indications
- Short-term treatment of severe or disabling insomnia
Mechanism of Action
- Thienodiazepine derivative that binds to benzodiazepine receptors on the GABA-A receptor complex
- Enhances the inhibitory effects of gamma-aminobutyric acid (GABA), leading to increased chloride conductance, neuronal hyperpolarization, and sedative-hypnotic effects
Contraindications
- Known hypersensitivity to brotizolam, thienodiazepines, or benzodiazepines
- Severe hepatic insufficiency
- Severe respiratory insufficiency or sleep apnea syndrome
- Myasthenia gravis
- Acute pulmonary insufficiency
Adverse Reactions
- Drowsiness, daytime fatigue, dizziness, and headache
- Cognitive impairment, amnesia, and confusion (especially in elderly patients)
- Muscle weakness and ataxia
- Paradoxical reactions such as restlessness, agitation, irritability, and aggression
- Tolerance, physical dependence, and withdrawal symptoms upon abrupt discontinuation
Drug Interactions
- Central nervous system (CNS) depressants (alcohol, opioids, antipsychotics, antidepressants, antihistamines) enhance sedative effects and risk of severe respiratory depression
- CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) may increase plasma concentrations of brotizolam
- CYP3A4 inducers (e.g., rifampin, carbamazepine) may decrease plasma concentrations and therapeutic efficacy of brotizolam
Curated Content: Needs Vetting Before Put to Clinical Use