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NERVOUS SYSTEM › PSYCHOLEPTICS › HYPNOTICS AND SEDATIVES › Barbiturates, plain
cyclobarbital
N05CA10
Adult Dosing
- Insomnia: 100 mg to 200 mg orally at bedtime
- Preoperative sedation: 200 mg to 400 mg orally 30 to 60 minutes before surgery
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established; use generally avoided
Indications
- Short-term management of severe insomnia
- Preoperative sedation
Mechanism of Action
- Barbiturate derivative that binds to GABA-A receptor complexes in the central nervous system
- Enhances GABA-mediated inhibitory neurotransmission and prolongs chloride channel opening
- Suppresses the reticular activating system, leading to sedation, hypnosis, and anticonvulsant effects
Contraindications
- Hypersensitivity to barbiturates
- History of manifest or latent porphyria
- Severe respiratory insufficiency or chronic obstructive pulmonary disease
- Severe hepatic impairment
- History of drug or alcohol dependence
Adverse Reactions
- Drowsiness, lethargy, and hangover effect
- Paradoxical excitement or confusion in elderly patients
- Respiratory depression
- Hypotension
- Physical dependence and tolerance with prolonged use
- Withdrawal syndrome upon abrupt cessation
Drug Interactions
- CNS depressants (alcohol, opioids, benzodiazepines): additive central nervous system and respiratory depression
- CYP450 enzyme inducers/substrates: hepatic enzyme induction can decrease efficacy of oral contraceptives, anticoagulants, and corticosteroids
- Valproic acid: inhibits barbiturate metabolism, increasing toxicity risk
Curated Content: Needs Vetting Before Put to Clinical Use