Allosteric binding within the spinal cord and motor neurons is the primary mediator of the myorelaxant effects seen with diazepam. Specifically, the allosteric binding within the limbic system leads to the anxiolytic effects seen with diazepam.
This shift in charge leads to a hyperpolarization of the neuronal membrane and reduced neuronal excitability. The allosteric binding of diazepam at the GABA-A receptor increases the frequency at which the chloride channel opens, leading to an increased conductance of chloride ions. īenzodiazepines exert their effects by facilitating the activity of gamma-aminobutyric acid(GABA) at various sites. Specifically, benzodiazepines bind at an allosteric site at the interface between the alpha and gamma subunits on GABA-A receptor chloride ion channels. Off-label (non-FDA approved) use for diazepam includes sedation in the ICU and short-term treatment of spasticity in children with cerebral palsy. ĭiazepam is FDA approved for the management of anxiety disorders, short-term relief of anxiety symptoms, spasticity associated with upper motor neuron disorders, adjunct therapy for muscle spasms, preoperative anxiety relief, management of certain refractory epilepsy patients, and adjunct in severe recurrent convulsive seizures, and an adjunct in status epilepticus. Benzodiazepines have largely replaced barbiturates in treating anxiety and sleep disorders because of their improved safety profile, fewer side effects, and flumazenil(antagonist) availability that can reverse oversedation in cases of benzodiazepine intoxication.
In acute alcohol withdrawal, diazepam is useful for symptomatic relief of agitation, tremor, alcoholic hallucinosis, and acute delirium tremens.
It is a fast-acting, long-lasting benzodiazepine commonly used to treat anxiety disorders and alcohol detoxification, acute recurrent seizures, severe muscle spasms, and spasticity associated with neurologic disorders. Diazepam is an anxiolytic benzodiazepine, first patented and marketed in the United States in 1963.
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