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BMS60042

Drugs acting at the sodium channel

QuestionAnswerDrugs
Na Channel Blocker uses local anesthetics, anti-arrhythmic, anti-epileptics
- caine local anesthetics
LA with one "i" ester
LA with two "i"s amide
cocaine only LA with vasoconstrictor
Differences between ester and amide LA t1/2: short/longer metabolism: rapid/plasma; complex/hepatic allergic rxns: possible; rare/non-existent toxicity: low; higher/dose dependent
Class I A block phase 0 (Na) and phase 3 (K); torsade de pointes Quinidine, Procainamide, Disopyramide
Class I B block phase 0 and increases phase 3 Lidocaine, Mexiletine
Class I C only blocks phase 0 Flecainide
Procaineamide metabolized to NAPA
Carbamazepine tricyclic SE: H1 receptor blocker, M receptor blocker, Na-channel blocker, K-channel blocker, alpha receptor blocker, 5-HT blocker
TCA side effects H1 receptor blocker: sedation M receptor blocker: dry mouth Na channel blocker: arrhythmia K channel blocker: arrhythmia alpha receptor blocker: hypotension 5-HT: weight gain
3A4 substrates Ca channel blockers; HMG CoA reductase inhibitors, macrolide antibiotics, benzodiazepines, HIV antivirals, antihistamines
Phenytoin 3A4 inducer, Na and Ca channel blocker, gum hyperplasia, megaloblastic anemia (folate/B12 def), zero order kinetics
Folate antagonism triamterene, dapsone, phenytoin, trimethoprim, methotrexate
What Vaughan-Williams class are Na channel blockers? Class I
Created by: cbart004
Popular Pharmacology sets

 

 



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