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10 Cards in this Set
- Front
- Back
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Class 1A
-MOA -Effect on primarily which ion -Effect on phase of AP |
*Na+ channel blocker
*Na+ inward *Phase 0, Lengthens AP |
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Class 1B
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*Na+ channel blocker
*Na+ inward *Phase 0, little change in AP length |
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Class 1C
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Na+ channel blocker
Na+ inward Phase 0, slows conduction |
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Class 1 with regards to dissociation rate
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1A= intermediate
1B= Fast (least potent) 1C= slow (most potent) |
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Class II
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Beta-antagonists (block Beta-receptor on Ca++ channels causing decreased Ca++ influx and increased time required for repolarization in phase II.
Na+ inward, K+ outward Phases I,II,IV, slows conduction |
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Class III
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K+ channel blocker
K+ outward Phase III, lengthens AP |
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Class IV
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Ca++ channel blockers
Ca++ inward Phase II, slows conduction |
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SAR of Na+ channel blockers (Class 1A)
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1. Functional group that mimics Na+ (able to be ionized)
2.Hydrophobic bulk to physically block the Na+ channel |
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If a class 1A agent is acetylated, what effect does it have on the drug?
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NAPA (N-acetyl procainamide): 25% activity of parent
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SAR of Na+ channel blockers (Class 1B)
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1. Reverse amide
2. Ortho bulk 3. Functional gp that mimics Na+ (able to be ionized=amine,+, Nitrogen,-,) |
