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NERVOUS SYSTEM › PSYCHOLEPTICS › HYPNOTICS AND SEDATIVES › Barbiturates, plain
heptabarbital
N05CA11
Adult Dosing
- Sedation: 50 mg to 100 mg orally 2 to 3 times daily
- Hypnotic/Insomnia: 100 mg to 200 mg orally at bedtime
Pediatric Dosing
- Safety and efficacy in pediatric patients not well established; use generally avoided or restricted based on clinical discretion
Indications
- Short-term management of insomnia
- Pre-anesthetic sedation
- Management of anxiety states
Mechanism of Action
- Barbiturate derivative that binds to GABA-A receptors in the central nervous system
- Enhances GABA-mediated chloride influx, prolonging channel opening
- Suppresses the reticular activating system and inhibits neuronal firing
Contraindications
- Hypersensitivity to barbiturates
- History of manifest or latent porphyria
- Severe respiratory insufficiency
- Severe hepatic impairment
Adverse Reactions
- Drowsiness and lethargy
- Respiratory depression
- Paradoxical excitement or confusion in elderly patients
- Physical dependence and tolerance with prolonged use
- Hypotension
Drug Interactions
- Central nervous system depressants (alcohol, opioids, benzodiazepines) increase risk of profound sedation and respiratory depression
- Induces hepatic CYP enzymes (e.g., CYP3A4), potentially decreasing efficacy of oral contraceptives, anticoagulants, and corticosteroids
- Valproic acid inhibits barbiturate metabolism, increasing serum concentrations and toxicity risk
Curated Content: Needs Vetting Before Put to Clinical Use