Drug intelligence / Profile preview

diazepam + phenobarbital

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Rectal, Nasal Spray (for Diazepam)
01

Overview

Diazepam + phenobarbital is a combination of two central nervous system depressants used primarily for their anticonvulsant, sedative, anxiolytic, and muscle relaxant properties. Diazepam is a long-acting benzodiazepine that enhances the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at GABAA receptors, producing anxiolytic, anticonvulsant, sedative, and muscle relaxant effects. Phenobarbital is a barbiturate that also acts on GABAA receptors but with a different binding site and mechanism; it increases the duration of chloride channel opening leading to neuronal inhibition. The combination may be used in treatment-resistant cases such as severe alcohol withdrawal or refractory seizures to take advantage of diazepam’s titratability and phenobarbital’s potency. However, concomitant use increases risks such as additive CNS depression including dizziness, drowsiness, confusion, respiratory depression and requires careful monitoring.[1][2][4][6][7]

Other names
diazepam + phenobarbital
02

Targets

GABAA (Gamma-aminobutyric acid receptor)BZD site (GABA-A receptor benzodiazepine site)

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