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30 Cards in this Set
- Front
- Back
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BZ actions
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anxiolytic
sedative/hypnotic anticonvulsants preanesthetic muscle relaxant |
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Diazepam
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BZ agonist; positive modulator of GABA inhibitory function
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Flumazenil
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BZ antagonist
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Beta Carbolines
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inverse BZ agonist; negatively modulate GABA function
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Zolpidem
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novel BZ agonist
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Ramelteon
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melatonin agonist; hypnotic
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Buspirone
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partial 5HT agonist; anxiolytic
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alpha subunit of GABA-AR
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BZ binding site
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beta subunit
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GABA binding site
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alpha 1 subunit
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anticonvulsant and hypnotic actions
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alpha 2 subunit
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anxiolytic actions
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BZ therapeutic index
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is very high
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used to treat panic disorder
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clonazepam and alprazolam
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BZ effects on sleep
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decrease all stages, except increase stage 2 sleep
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Zolpidem and Zaleplon
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non-BZ hypnotics; may produce increased dreaming or nightmares on withdrawal
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sleep apnea
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avoid BZs
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Use as anticonvulsants
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diazepam, lorazepam, clonazepam
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Muscle relaxant
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diazepam
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BZ preanesthetic action
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anxiolytic
sedative anterograde amnesia NO analgesia diazepam and midazolam |
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Anxiolytic and hypnotic tolerance
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little or none develops
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anticonvulsant tolerance
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develops
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ataxia and incoordination tolerance
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develops rapidly
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Tolerance develops more slowly to this BZ
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clonazepam
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BZ drug interactions
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additive CNS depression
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metabolized to active metabolites
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diazepam and flurazepam
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Ramelteon metabolism
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inhibited by fluvoxamine
induced by rifampin |
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Ramelteon and hormones and contraindications
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decreases testosterone and increses prolactin levels
avoid in pregnant patients |
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GAD
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buspirone
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Buspirone interactions
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hypertension with MAOIs
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Buspirone inhibits
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5HT2 and D2 receptors
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