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Anxiolytics
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Anxiolytics
Meprobamate
Benzodiazepines (BZ)
Second generation anxiolytics
Benzodiazepines
Chlordiazepoxide (Librium)
Diazepam (Valium)
Oxazepam (Sevax)
Nitrazepam (Moyodon)
Flurazepam (Dalmane)
2nd generation anxiolytics
Buspirone
Serotonergic action
Medical uses
Pathological anxiety - not so much
Severe emotional distress
Relief from agitation and alcohol withdrawal
Sedation
Presurgery sedation
Side effects
Motor incoordination
Intoxication
Memory loss
Sedation and sleep
Deep sleep and coma
Respiratory depression
Abuse
Not self-adminstered, low preference
Controversy about over-prescription
Date rape
Rohypnol - "ruffies"
Micky finn
GBH
Mechanisms of action
Discovery of BZ binding sites (1977)
Concentrated in newly evolved structures
Correlate with anxiolytic effects
Closely related to GABAa receptor sites
GABA neurotransmission
Ubiquitous inhibitory NT -> let's Cl ions go through
Hyperpolarizes neurons
GABA synthesis
GAD - glutamic acid decarboxylase
Glutamate -> GABA
GABAa
Ionotropic (channels)
5 parts -> form Cl channel
GABA increases Cl conductance
Hyperpolarization (inhibition)
Agonist - Muscimol
Antagonist - bicuculline
GABAb
Metabotropic (G-protein)
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
Beta-carbolines
Inverse agonists
Negatively modulates GABAa receptor
Author
LT24
ID
32347
Card Set
Anxiolytics
Description
Lecture #7
Updated
2010-09-02T01:25:43Z
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