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NERVOUS SYSTEM › PSYCHOLEPTICS › HYPNOTICS AND SEDATIVES › Piperidinedione derivatives
pyrithyldione
N05CE03
Forms & Strengths
- Oral tablets: 100 mg
- Oral tablets: 200 mg
Adult Dosing
- Insomnia: 100 mg to 200 mg orally at bedtime
- Maximum daily dose: 400 mg
Pediatric Dosing
- Safety and efficacy not established in pediatric patients under 12 years of age
- Children >= 12 years: 50 mg to 100 mg orally at bedtime if indicated
Indications
- Short-term management of insomnia
- Sedative-hypnotic for sleep initiation difficulties
Mechanism of Action
- Piperidinedione derivative with central nervous system depressant properties
- Enhances gamma-aminobutyric acid (GABA) inhibitory neurotransmission, similar to barbiturates
- Depresses the reticular activating system in the brainstem
Contraindications
- Hypersensitivity to pyrithyldione or other piperidinedione derivatives
- Acute intermittent porphyria
- Severe hepatic impairment
- Respiratory depression or severe chronic obstructive pulmonary disease (COPD)
Adverse Reactions
- Drowsiness and somnolence
- Dizziness and ataxia
- Paradoxical excitement or confusion, especially in elderly patients
- Gastrointestinal upset including nausea and vomiting
- Tolerance and physical dependence with prolonged use
Drug Interactions
- Central nervous system (CNS) depressants (alcohol, opioids, benzodiazepines, antipsychotics) leading to profound sedation and respiratory depression
- CYP450 enzyme inducers that may alter metabolism
- CYP450 enzyme inhibitors that may increase plasma concentrations and toxicity
Curated Content: Needs Vetting Before Put to Clinical Use