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42 Cards in this Set
- Front
- Back
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What drugs have been primarily used in recent years for treating Anxiety and Insomnia?
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Benzodiazepines
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What drug has bene used in treatment of generalized anxiety disorders?
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Buspirone
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What is the target of action of the Benzodiazepines and Barbiturates?
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GABA-a receptor Chloride ion channel complex
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At what sites is the GABA-A receptor associated w/ Cl ion channel found in high conc?
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-Striatum
-Hippocampus -Spinal cord |
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What happens when GABA binds to this GABA-A receptor?
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It increases chloride conductance
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So where is the actual Benzodiazepine receptor?
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On one of the subunits of the GABA receptor-Cl channel complex
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What effect is seen when Benzodiazepines bind to their receptor on the GABA rec-Cl channel complex?
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Enhanced action of GABA - increased frequency of the Cl channel opening
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Where is the Barbiturate binding site?
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At a site separate form the Benzodiazepine site
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What is a drug that is a pure ANTAGONIST of the benzodiazepine receptor?
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Flumazenil
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What is the mechanism of Buspirone's action?
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Partial agonist of 5-HT1A receptors and also binds to D2 receptors
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How do the benzodiazepines compare to each other in general?
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-Qualitatively similar
-Markedly differ in metabolism and pharmacokinetics |
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What clinically used benzodiazepines have hypnotic actions?
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They all do!
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What 3 benzodiazepines are primarily used as hypnotics to promote sleep?
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-Flurazepam
-Triazolam -Lorazepam |
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What determines the pharmacokinetics of the BDZ hypnotics?
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Their relative lipophilicity
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Which hypnotic BDZ is most rapidly absorbed?
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Diazepam
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What does the lipophilicity of the benzodiazepines in turn determine?
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Their rate of entry into the CNS
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What determines the duration of action after a single dose of a benzodiazepine?
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The rate of redistribution from the CNS
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Why do the effects of some benzodiazepines last for so long?
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Because most are metabolized to active metabolites with very long half lives
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Which benzodiazepine does NOT form an active metabolite?
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Lorazepam
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What are 4 effects of the benzodiazepines due to their actions on the CNS?
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-Decreased anxiety
-Anticonvulsant action -Sedation -Hypnosis |
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What is an additional CNS effect specific to Diazepam?
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Muscle relaxation
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What CNS effect results from IV administration of benzodiazepines?
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Anterograde amnesia
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What are 2 non-CNS effects of benzodiazepines? How serious are they?
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-CV and respiratory actions
-Minimal at therapeutic doses |
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What are 2 types of drug interactions seen with benzodiazepines?
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-Additive effects with other CNS depressant drugs
-Drugs that affect hepatic metabolism |
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What are 3 CNS-depressant drugs that can add to the CNS depression caused by BDZ's?
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-Ethanol
-Sedative hypnotics -Sedating antihistamines |
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What are the 3 main pharmacokinetic points to remember about Diazepam?
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-Long duration dt active metabolites
-Lipophilic - fast onset -Rapid redistribution |
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What are 3 clinical uses of diazepam?
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-Anxiolytic (check this)
-Muscle relaxant -IV sedation and anesthesia |
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What are the 2 types of anxiety states treated with BDZ's?
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-Generalized anxiety disorder
-Panic disorder |
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What are the 2 drugs used for treating panic disorder?
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-Alprazolam
-Clonazepam |
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What is the main difference between Alprazolam and Clonazepam?
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Alprazolam = med action duration
Clonazepam = potent, long acting |
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What is Clonazepam used for treating in addition to Panic disorder?
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Manic - acute manic episodes (remember the board review Q?)
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What are 2 other clinical uses of the benzodiazepines?
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-Sleep disorders
-Seizures |
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What are the 2 main side effects of Benzodiazepines?
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-Tolerance
-Dependence and withdrawal |
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What do you have to keep in mind with Benzodiazepines?
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How to treat abuse
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How is Buspirone related to the Benzodiazepines?
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It's NOT - not chemically, nor pharmacologically.
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What is the target of action of Buspirone?
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5-HT1A receptors
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How does Buspirone act at the 5-HT1A receptors? What is its elimination T1/2?
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As a partial agonist
T1/2 = 2-11 hrs |
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How do the effects of Buspirone compare to the other BDZ's?
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Less sedating, no cross-tolerance
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How do the effects of Buspirone mix with other sedative-hypnotic drugs and depressants?
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Buspirone does not potentiate their effects, nor suppress symptoms of their withdrawal
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What is Buspirone used for treating clinically?
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Generalized Anxiety syndrome
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How long do the effects of Buspirone take to kck in?
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1-2 weeks
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What are 2 other types of drugs used for treating anxiety?
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-SSRI's
-B-blockers |
