Anxiolytics

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Author:
LT24
ID:
32347
Filename:
Anxiolytics
Updated:
2010-09-01 21:25:43
Tags:
Barbiturates
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Description:
Lecture #7
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  1. Anxiolytics
    • Meprobamate
    • Benzodiazepines (BZ)
    • Second generation anxiolytics
  2. Benzodiazepines
    • Chlordiazepoxide (Librium)
    • Diazepam (Valium)
    • Oxazepam (Sevax)
    • Nitrazepam (Moyodon)
    • Flurazepam (Dalmane)
  3. 2nd generation anxiolytics
    • Buspirone
    • Serotonergic action
  4. Medical uses
    • Pathological anxiety - not so much
    • Severe emotional distress
    • Relief from agitation and alcohol withdrawal
    • Sedation
    • Presurgery sedation
  5. Side effects
    • Motor incoordination
    • Intoxication
    • Memory loss
    • Sedation and sleep
    • Deep sleep and coma
    • Respiratory depression
  6. Abuse
    • Not self-adminstered, low preference
    • Controversy about over-prescription
    • Date rape
    • Rohypnol - "ruffies"
    • Micky finn
    • GBH
  7. Mechanisms of action
    • Discovery of BZ binding sites (1977)
    • Concentrated in newly evolved structures
    • Correlate with anxiolytic effects
    • Closely related to GABAa receptor sites
  8. GABA neurotransmission
    • Ubiquitous inhibitory NT -> let's Cl ions go through
    • Hyperpolarizes neurons
  9. GABA synthesis
    • GAD - glutamic acid decarboxylase
    • Glutamate -> GABA
  10. GABAa
    • Ionotropic (channels)
    • 5 parts -> form Cl channel
    • GABA increases Cl conductance
    • Hyperpolarization (inhibition)
    • Agonist - Muscimol
    • Antagonist - bicuculline
  11. GABAb
    Metabotropic (G-protein)
  12. 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
  13. Beta-carbolines
    • Inverse agonists
    • Negatively modulates GABAa receptor

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