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NERVOUS SYSTEM › PSYCHOLEPTICS › HYPNOTICS AND SEDATIVES › Barbiturates, combinations
combinations of barbiturates
N05CB01
Forms & Strengths
- Oral tablets containing fixed-dose combinations of short-acting and intermediate-acting barbiturates (e.g., phenobarbital, butabarbital, secobarbital)
- Oral elixirs and capsules containing barbiturate combination formulations
- Parenteral solutions for injection containing barbiturate combinations
Adult Dosing
- Sedation: 30 mg to 50 mg orally 3 times daily as needed
- Insomnia/Hypnotic: 100 mg to 200 mg orally at bedtime
- Preoperative sedation: 100 mg to 200 mg orally 60 to 90 minutes before surgery
Pediatric Dosing
- Sedation: 2 mg/kg to 6 mg/kg/day divided into 3 doses orally
- Preoperative sedation: 1 to 3 mg/kg orally or intramuscularly 60 to 90 minutes prior to procedure
- Use in pediatric patients is largely restricted due to paradoxical excitation risks and availability of safer alternatives
Indications
- Short-term management of insomnia
- Preoperative sedation and anxiety reduction
- Adjunctive treatment in tension headaches or specific psychoneurotic conditions
Mechanism of Action
- Enhances GABA-mediated synaptic inhibition by binding to GABA-A receptors in the central nervous system
- Prolongss the duration of chloride channel opening, decreasing neuronal excitability
- Depresses the sensory cortex, decreases motor activity, and alters cerebellar function
Contraindications
- Hypersensitivity to barbiturates
- History of manifest or latent porphyria
- Severe respiratory depression or chronic obstructive pulmonary disease
- Severe hepatic impairment or nephrotic syndrome
Adverse Reactions
- CNS depression, drowsiness, lethargy, hangover effect, and paradoxical excitement in elderly or pediatric patients
- Respiratory depression and apnea, especially with rapid intravenous administration
- Physical dependence, tolerance, and severe withdrawal syndrome upon abrupt cessation
- Hypotension and bradycardia with high doses
Drug Interactions
- Potent CYP450 enzyme induction (CYP3A4, 2C9, 2C19), decreasing efficacy of oral contraceptives, warfarin, and corticosteroids
- Additive central nervous system depression when co-administered with alcohol, opioids, benzodiazepines, or antihistamines
- Increased risk of central nervous system and respiratory toxicity when combined with valproic acid, which inhibits barbiturate metabolism
Curated Content: Needs Vetting Before Put to Clinical Use