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3 Cards in this Set
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Benzodiazepines- Physiochemical
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Diazepam, Midazolam and lorazepam all used in OR for anxiolysis and anterograde amnesia
Midazolam is most lipophilic |
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Benzodiazepines- Pharmacokinetics
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High lipid solubility leads to rapid CNS onset
Redistribution leads to termination Metabolism in liver via oxidation which is susceptible to degradation with age and cirrhosis (midazolam, diazepam) -Midazolam --> metabolized to inactive metabolite (short context sensitive h/t) (can be used continuous inf) -Diazepam --> metabolized to active metabolite (prolonged elimination half time) |
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Benzodiazepines- Pharmacodynamics
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MOA- activation of GABAa receptor complex --> increased Cl current --> hyperpolarization --> reduced excitability
GABAa receptors responsive to benzos occur almost exclusively in the cerebral cortex (minimal effects outside CNS) (lower vent dep and hypotension) CNS - sedative hypnotic and anterograde amnesia |