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NERVOUS SYSTEM › PSYCHOLEPTICS › HYPNOTICS AND SEDATIVES › Benzodiazepine derivatives
loprazolam
N05CD11
Forms & Strengths
- Tablets 1 mg
- Tablets 2 mg
Adult Dosing
- Insomnia: 1 to 2 mg orally once daily immediately before bedtime
- Max duration of treatment: 2 to 4 weeks including tapering phase
- Elderly or debilitated patients: Initial 1 mg once daily
Pediatric Dosing
- Safety and efficacy not established in patients under 18 years of age
- Not recommended for pediatric use
Indications
- Short-term management of severe, disabling insomnia
Mechanism of Action
- Binds to benzodiazepine receptors on the GABAA ligand-gated chloride channel complex
- Enhances GABA-induced chloride conductance, producing central nervous system depression
Contraindications
- Known hypersensitivity to loprazolam or other benzodiazepines
- Myasthenia gravis
- Severe hepatic insufficiency
- Severe respiratory insufficiency or sleep apnea syndrome
- Acute pulmonary insufficiency
Adverse Reactions
- Drowsiness and daytime sedation
- Dizziness and ataxia
- Muscle weakness
- Confusion and amnesia
- Dependence and withdrawal symptoms upon discontinuation
- Paradoxical reactions such as excitation, aggression, or irritability
Drug Interactions
- Central nervous system depressants (opioids, antipsychotics, antidepressants, sedating antihistamines) cause additive CNS depression
- Alcohol concurrent use strongly potentiates sedation and respiratory depression
- CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) may increase plasma concentrations of loprazolam
Curated Content: Needs Vetting Before Put to Clinical Use