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Anxiolytics
- Meprobamate
- Benzodiazepines (BZ)
- Second generation anxiolytics
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Benzodiazepines
- Chlordiazepoxide (Librium)
- Diazepam (Valium)
- Oxazepam (Sevax)
- Nitrazepam (Moyodon)
- Flurazepam (Dalmane)
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2nd generation anxiolytics
- Buspirone
- Serotonergic action
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Medical uses
- Pathological anxiety - not so much
- Severe emotional distress
- Relief from agitation and alcohol withdrawal
- Sedation
- Presurgery sedation
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Side effects
- Motor incoordination
- Intoxication
- Memory loss
- Sedation and sleep
- Deep sleep and coma
- Respiratory depression
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Abuse
- Not self-adminstered, low preference
- Controversy about over-prescription
- Date rape
- Rohypnol - "ruffies"
- Micky finn
- GBH
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Mechanisms of action
- Discovery of BZ binding sites (1977)
- Concentrated in newly evolved structures
- Correlate with anxiolytic effects
- Closely related to GABAa receptor sites
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GABA neurotransmission
- Ubiquitous inhibitory NT -> let's Cl ions go through
- Hyperpolarizes neurons
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GABA synthesis
- GAD - glutamic acid decarboxylase
- Glutamate -> GABA
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GABAa
- Ionotropic (channels)
- 5 parts -> form Cl channel
- GABA increases Cl conductance
- Hyperpolarization (inhibition)
- Agonist - Muscimol
- Antagonist - bicuculline
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GABAb
Metabotropic (G-protein)
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Different action of frequency vs duration of Cl channel
- Barbiturates
- Increase duration open
- No change in number of openings
- BZ
- No change in duration
- Change in openings
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Beta-carbolines
- Inverse agonists
- Negatively modulates GABAa receptor
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