lecture_9_notes(2010) - BENZODIAZEPINES AND RELATED...

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BENZODIAZEPINES AND RELATED ANXIOLYTICS I. General Aspects of Anxiety and Sleep Disorders Anxiety and sleep disorders have long been problems and have been the target of drug therapy. The modern treatment began in the 1960’s with benzodiazepines . Benzodiazepines have a number of complicating limitations and anxiety is now often treated with serotonin-type antidepressants and mood stabilizers . Sleep disorders are widely treated now with newer drugs that exert action on receptors affected by benzodiazepines . A. Anxiety Disorders 1. They are the most frequent psychological disorders a. May lead to high levels of medical and psychological comorbidity 2. Major forms a. Generalized anxiety disorder b. Panic disorder c. Social anxiety disorder d. Posttraumatic stress disorder 3. These symptoms may affect 30% of the general population a. Only 15 to 36% are treated B. Insomnia 1. May be of an acute or chronic form 2. It is characterized by trouble falling asleep, waking up and or lack of feeling rested C. Current Approaches 1. Treatment of Anxiety and Insomnia a. A combination of pharmacotherapy and psychological therapies is best II. Benzodiazepines A. General Aspects 1. Effects a. Anxiolytic (antianxiety) b. Sedative c. Anticonvulsant d. Amnesic e. Muscle relaxant 2. Common forms a. Diazepam (Valium®) – long-acting agent b. Chlordiazepoxide (Librium®) - – long-acting agent c. Clonazepam (Klonopin®) – intermediate-acting agent d. Lorazepam (Ativan®) – intermediate-acting agent e. Triazolam (Halcion®) – short-acting agent f. Alprazolam (Xanax®) – short-acting agent
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2 of 6 B. Definition 1. Structurally defined a. Changes in side groups or slightly modifying the basic structure 2. Benzodiazepine receptor agonists (BZRAs) a. All act at GABA receptors b. Agents Benzodiazepines Nonbenzodiazepines - Widely used to improve the quality of sleep and manage insomnia C. Mechanism of Action 1. Agonists at the GABA-benzodiazepine-chloride receptor complex a. Facilitate the binding of GABA but do not directly stimulate the receptor Increase the affinity of the receptor for GABA b. Increases the influx of chloride and hyperpolarization 2. Sites of action a. Limbic system (amygdale and orbitofrontal cortex)
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This note was uploaded on 03/25/2010 for the course PHARM 310 taught by Professor Marker during the Spring '10 term at Wisconsin.

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lecture_9_notes(2010) - BENZODIAZEPINES AND RELATED...

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