Phenobarbital
CAS number:50-06-6
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Molecular Formula:
C12H12N2O3
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Molecular Weight:
232.23g/mol
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Brief Introduction:
Phenobarbital is a long-acting barbiturate with sedative-hypnotic and anticonvulsant properties. It has been used in various medical contexts. In the treatment of sedative-hypnotic withdrawal syndrome in intensive care units, phenobarbital shows promise as an alternative treatment, especially when traditional methods fail, as demonstrated in a case report of a 26-year-old female with Tuberculous meningitis who was successfully weaned off prolonged sedation with phenobarbital. In the emergency department for alcohol withdrawal, a systematic review and meta-analysis found that phenobarbital does not significantly reduce ICU admissions, hospital admissions, ED readmissions, or adverse events compared to benzodiazepines. For neonatal cholestasis, a study showed that phenobarbital combined with ursodeoxycholic acid can improve liver function and reduce serum bilirubin concentration more effectively than phenobarbital alone, with good clinical efficacy and safety.
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Properities:
IUPAC name: 5-ethyl-5-phenyl-1,3-diazinane-2,4,6-trione [1] pKa: 7.63[1] Therapeutic concentration range: 15-40 µg/L [1] Use: Hypnotic and sedative properties, first choice for treating epilepsy. [1]
Increase the metabolism of perampanel and for seizure prophylaxis. [2]
Administration: Directly acts on the GABA receptor to increase inhibitory tone [4] Mechanism of action: Shown to inhibit glutamate response at NMDA receptors [4] Withdrawal symptoms: Long-term use can cause dependence, and withdrawal syndrome is more likely to occur after stopping the drug [3] -
References:
[1] Multi-metal oxide/N-doped reduced graphene oxide modified electrode for ultrasensitive determination of phenobarbital
[2] Phenobarbital use in pediatric perampanel overdose with coma, respiratory compromise
[3] Clinical efficacy of phenobarbital combined with ursodeoxycholic acid in the treatment of neonatal patients with cholestasis
[4] Does phenobarbital reduce the hospital length of stay for patients suffering from severe alcohol withdrawal? A retrospective comparison of phenobarbital to lorazepam infusions
Barbiturates
Phenobarbital is a member of the barbiturate class of drugs. Barbiturates are derivatives of barbituric acid and are known for their sedative, hypnotic, and anticonvulsant properties. They act by enhancing the effects of gamma-aminobutyric acid (GABA) in the central nervous system, leading to sedation and muscle relaxation.
Sedative-Hypnotics
Phenobarbital is classified as a sedative-hypnotic agent. These drugs are used to induce sleep (hypnotic effect) and reduce anxiety or agitation (sedative effect). Phenobarbital’s rapid onset of action and effectiveness in managing withdrawal symptoms make it useful in certain clinical settings.
Anticonvulsants
Phenobarbital also functions as an anticonvulsant. It is used to prevent or control seizures by stabilizing neuronal activity in the brain. Its mechanism of action involves binding to GABAA receptors, which increases the duration of chloride channel openings, leading to neuronal hyperpolarization and reduced excitability.
GABAergic Agents
Phenobarbital is a GABAergic agent, meaning it enhances the effects of GABA, the primary inhibitory neurotransmitter in the central nervous system. By binding to the GABAA receptor complex, phenobarbital prolongs the opening of chloride channels, increasing chloride ion flow into neurons, which results in neuronal hyperpolarization and reduced neuronal excitability.
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