Pharmacology and pharmacokinetics - Vanderbilt University Medical PDF
Preview Pharmacology and pharmacokinetics - Vanderbilt University Medical
Pharmacology and pharmacokinetics Bassel Abou-Khalil, M.D. Vanderbilt University Pharmacology and Pharmacokinetics Mechanisms of drug actions n Pharmacokinetic principles, illustrate PHT n Pharmacokinetic interactions n Liver, renal disease, hemodialysis n Changes through the ages n AED main mechanisms of action Na channel blocking n Enhancing GABA n Glutamate receptor antagonism n Blocking high voltage activated calcium channels n Blocking T- calcium channels n Binding Alpha-2-delta subunit of voltage-activated n calcium channels Binding synaptic vesicle protein SV2A n K-channel opening n Na channel blocking Enhancement of fast inactivated state- blocking of n sustained repetitive firing: Phenytoin, carbamazepine, oxcarbazepine, lamotrigine, n rufinamide Selective enhancement of slow inactivation of n voltage-gated sodium channels Lacosamide n Multiple mechanisms, including effect on sodium n channels Valproate, felbamate, topiramate, zonisamide n Fast versus slow inactivation of VGSC Fast inactivation occurs on a time scale of n milliseconds. Slow inactivation occurs over the time course of n seconds to minutes. involves modification of the shape of the sodium n channel ARS SAE Question All but one of the following AEDs block sodium channels as their main mechanism of action A- carbamazepine B- lamotrigine C- levetiracetam D- phenytoin E- lacosamide ARS SAE Question All but one of the following AEDs block sodium channels as their main mechanism of action A- carbamazepine B- lamotrigine C- levetiracetam D- phenytoin E- lacosamide Enhancing GABA n Irreversible inhibition of GABA transaminase: vigabatrin n Inhibition of GABA reuptake at the synapse: tiagabine n Prolongation of GABA-mediated chloride channel openings: phenobarbital n Increased frequency of GABA-mediated chloride channel openings: benzodiazepines, topiramate (different binding site- also increases GABA levels in the brain by MRS) Enhancing GABA transmission in specific circuits: valproate n Enhancing GABA-elicited Cl − currents: felbamate n Several AEDs are associated with acute elevation of brain n GABA by MRS after single doses: 70% for topiramate, 48% with gabapentin.
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