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