What is the role of benzodiazepines and barbiturates in the treatment of epilepsy?

Updated: Jan 28, 2020
  • Author: Juan G Ochoa, MD; Chief Editor: Selim R Benbadis, MD  more...
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A seizure reflects an imbalance between excitatory and inhibitory activity in the brain, with an increment of excitation over inhibition. The most important inhibitory neurotransmitter in the brain is gamma-aminobutyric acid (GABA).

GABA-A receptors have multiple binding sites for benzodiazepines, barbiturates, and other substances (eg, picrotoxins, bicuculline, and neurosteroids). These drugs bind to different receptor sites to exert their action, but the clinical implications of each receptor site are not well understood.

The benzodiazepines most commonly used for treatment of epilepsy are lorazepam, diazepam, clonazepam, and clobazam. The first 2 drugs are used mainly for emergency treatment of seizures because of their quick onset of action, availability in intravenous (IV) forms, and strong anticonvulsant effects. Their use for long-term treatment is limited because of the development of tolerance.

The 2 barbiturates mostly commonly used in the treatment of epilepsy are phenobarbital (PHB) and primidone. They bind to a barbiturate-binding site of the benzodiazepine receptor to affect the duration of chloride channel opening. They have been used widely throughout the world. They are very potent anticonvulsants, but they have significant adverse effects that limit their use. With the development of new drugs, the barbiturates now are used as second-line drugs for the treatment of chronic seizures.

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