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NERVOUS SYSTEM › PSYCHOLEPTICS › ANXIOLYTICS › Benzodiazepine derivatives
pinazepam
N05BA14
Forms & Strengths
- Tablets: 5 mg
- Tablets: 10 mg
Adult Dosing
- Anxiety: 10 mg to 20 mg orally once daily in the evening
- Maximum daily dose: 40 mg
Pediatric Dosing
- Safety and efficacy not established in pediatric patients under 18 years of age
Indications
- Short-term management of severe generalized anxiety disorder
- Anxiety-related insomnia
Mechanism of Action
- Binds to allosteric benzodiazepine binding sites on GABAA receptors in the central nervous system
- Enhances GABA-mediated chloride influx, producing hyperpolarization, neuronal inhibition, and anxiolytic effects
Contraindications
- Known hypersensitivity to pinazepam or other benzodiazepines
- Severe respiratory insufficiency
- Severe hepatic impairment
- Sleep apnea syndrome
- Myasthenia gravis
Adverse Reactions
- Drowsiness and sedation
- Dizziness and lightheadedness
- Ataxia and muscle weakness
- Cognitive impairment and confusion
- Tolerance and physical dependence with prolonged use
- Respiratory depression at high doses
Drug Interactions
- Central nervous system depressants (opioids, alcohol, antipsychotics, sedatives) increase risk of profound sedation, respiratory depression, and coma
- CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) may decrease clearance and increase plasma concentrations of pinazepam metabolites
- CYP3A4 inducers (e.g., rifampin, carbamazepine) may decrease therapeutic efficacy
Curated Content: Needs Vetting Before Put to Clinical Use