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FIU - Na Channels
Na channels
20
Pharmacology
Graduate
12/07/2011

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Cards

Term
ALADME
Definition
○ Administration
○ Liberation
○ Absorption
○ Distribution
○ Metabolism
○ Excretion
Term
what is absorbed in stomach? intestines?
Definition
stomach - weak acids
intestine - weak bases
Term
uses of Na-channel blockers?
Definition
local anesthetics, Anti-arrhythmics, anti-epileptics
Term
Ester LAs, 1/2 life? metabolism?examples?
Definition
-short 1/2 life, rapid metabolism by plasma esterases
-procaine and cocaine
Term
amide LAs; 1/2 life? metabolism? examples?
Definition
-longer 1/2 life, hepatic metabolism
-lidocaine, etidocaine, prilocaine (2 "i"s in name)
Term
5 Vaughan-Williams classes of anti-arrhythmics
Definition
I - Na channel blockers
II - beta blockers
III - K channel blockers
IV - Ca channel blockers
V - vagus boosters
Term
VW class IA; action? ex's?
Definition
decrease pohase 0 and decrease phase 3
can result in tosade de pointe
quinidine, procainamide, disopyramide
Term
VW class IB; action? ex's?
Definition
-decrease phase 0 and increase phase 3
-Lidocaine, mexiletine
Term
VW class IC; action? ex's?
Definition
-decrease phase 0, no effect on phase 3
-flecainide
Term
carbemazipine; type? channel? SEs (and cause)?
Definition
Anti-epileptic
Na channel blocker - membrane stabilization
CYP P450 3A4 inducer
SEs (similar to TCA)
sedation - H1 receptorblocker
dry mouth - M-receptor blocker
arrhythmia Na and K channel blocker
hypotension - alpha-R blocker
weight gain - 5-HT
Term
CYP P450 3A4 substrates
Definition
Ca blockers, statins, macrolide antibiotics, benzodiazepines, HIV antivirals, antihistamines
Term
Phenytoin; type? channel? SEs?
Definition

anti-epileptic Na and Ca channel blocker

CYP 3A4 inducer

0 order kinetics

SEs - gum hyperplasia, megaloblastic anemia, folate/B12 deficiency, peripheral neuropathy, skin rash, hirsuitism

Term
substrates w/ saturabale hepatic metabolism (zero order kinetics)
Definition
ethanol, ASA (aspirin), heparin, Theophyllin, phenytoin
Term
folate antagonists
Definition
triamterene, dapsone, phenytoin, trimethoprim, methotrexate
Term
procaine; action? type?
Definition
Na channel blocker
LA ester
Term
lidocaine; channel? type?
Definition
Na channel blocker
LA amide and VW Class IB anti-arrhythmic
Term
quinidine; action? type? SEs?
Definition
Na channel blocker
VW Class IA anti-arrhythmics
atropine-like effects (anticholinergic)
SEs - cinchonism (blurred vision, tinnitus, headaches) increased digoxin leves, N & V, arrhythmia
Term
procainamide; action? type?
Definition

"VW class IA"

 technically it is a VW IC (Na blocker only) but is metabolized to NAPA, a VW class III (K-blocker)

*fast metabolizers at higher risk for torsades de pointes

Term
flecainide; action? type?
Definition
Na channel blocker
VW class IC anti-arrhythmic
Term
what causes the following SEs? sedation, dry mouth, arrhythmia, hypotension, weight gain
Definition
sedation - H1 (histamine) blocker
dry mouth - Muscarinic receptor blocker
arrhythmia - Na or K channel blocker
Hypotension - Alpha-R blocker
Weight gain - 5-HT (seratonin)
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