BIOL 3327 Lecture Notes - Lecture 44: Mexiletine, Disopyramide, Flecainide

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If the channel is depolarized and open with both gates open, that"s where we"re shooting for our drugs to activate. Our na and ca channel blocker have the property to have high affinities for the activated open state of the channel, but the low affinity for the resting channel. A drug blocks the extra electrical activity when there is fast tachycardia/many channels that are actually going. State dependence because the drug works in a particular state (when the channel is more susceptible for blocking) Especially for channel blockers, the best way to block is to get into the channel when it"s open. If the channel is closed, the drug doesn"t get in. Decrease action potential rate of rise (rise = slope; slowly reduces impulse conduction eventually throughout all the muscle cells) Related to which na+ channels it"s activating. Class ia have k+ channel blockade, which effects repolarization.

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