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Benzodiazepines and Second

Benzodiazepines and Second - Benzodiazepines and...

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Benzodiazepines and Second-Generation Anxiolytics Benzos have anxiolytic (anti-anxiety), sedative, anticonvulsant, muscle relaxant, intravenous anesthetics, amnestic, and relaxant properties Can cause cognitive dysfunction and increased risk of falls and bone fractures in elderly Examples: o Diazepam (valium) o Chlorodiazepoxide (Librium) o Alprazolam (xanax) o Clonazepam (klonopin) o Lorazepam (ativan) o Triazoplam (halcyon) SSRI’s are replacing benzos for anxiety disorders because they don’t have the same long term dependency problems Anticonvulsants are also being shown to be effective in treatment of generalized anxiety disorder and social anxiety disorder (such as pregabalin/lyrica), but are not yet approved by FDA so would be considered “off label” Agonist of the GABA benzodiazepine chloride receptor, facilitate binding of GABA Benzos exert anxiolytic properties by acting at limbic center, and actions at other regions produce side effects such as sedation/increased seizure threshold/cognitive impairment and muscle relaxation Lesions of the amygdala produce anxiolytic effects, as does blockage of GABAergic function Blocking function of GABA receptors indicates that increased activity of amygdala cunction produces anxiogenic responses (increased heart rate and blood pressure) Absorption and distribution Well absorbed when taken orally One hour to peak plasma concentration (differs) Clorazepate is metabolized in gastric juice to nordiazepam, the active metabolite, which can be completely absorbed.
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