Calclium channel blockers
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| normal physiology of calcium channel | is COUPLED with B-1 receptors---epi/nor/agonist binds B-1---cAMP 2nd messenger opens Ca channel---Ca influx
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| once Ca in cell, what are heat targets/actions | SA node/HR-----AV node/conduction velocity-----myocardium/force of contraction
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| B-1 receptors/Ca channels also located in artery smooth muscle, what is their action | in arteries, normal action is to vasocon periph arteries/inc bp--------vasoCON coronary arteries/dec perfusion
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| so, when we BLOCK Ca channels, what is that effect on the heart | Ca can't get in--> SA/DECREASED HR-----AV/DECREASED force of conduction-----myocardium/DECREASED force of contraction
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| when we BLOCK Ca channels in arteries, what is effect | arteries vasoDIL--> increased coronary perfusion---peripheral vasoDIL/dec bp
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| two classes of calcium channel blockers | dihydropyridines ---- other class (verapamil, diltiazem)
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| MOA of verapamil (other class, drug 1) | blocks Ca channels in BOTH artery VSM (vascular smooth muscle) AND heart. net effect to dec bp/inc cardiac perfusion and dec HR/conductivity/force of contraction
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| verapamil indiacted for | indicated for essential HTN, CAD, angina pectoris, dysrhyth, tachy, migraine prophylaxis
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| compliance limiting SE verapamil | constipation - also blocks GI Ca channels
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| SEs we would expect from verapamil based on MOA | expect CARDIAC SEs ----overshoot if too high of dose-------brady----heart block (too little conduction)
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| Lesser SEs expected from verapamil | vasodil--> flushing/diz/HA/mild periph edema-------GINGIVAL HYPERPLASIA
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| MOA of diltiazem (other class, drug 2) | MOA is similar to verapamil with less potent effects on heart -----sim action on VSM to dec bp, inc coronary perfusion
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| are verapamil and diltiazem safe for RF pts | yes, they are metabilized in the liver
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| MOA of dihydriopyridienes = DHPs----AKA dipines | they ONLY act on B-1/Calcium channels on VSM. NO, NONE, NADA, ZIP action on heart except baroreceptor reflex which I am not getting into
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| DHP - dihydropyridine indicated for | HTN and angina pectoris. No indications for cardiac
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| ADRs DHP dihydropyridine | ANKLE EDEMA-----flush/HA/dizz ---some reflex tachy bwo inotropic effects, which we are not discussing
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| Name 6 DHPs ---dihydropyridines | meet the dipine family---clevidipine---nisoldipine---felodipine---amlodipine---isradipine---nicardipine
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| what 1 DHP is ONLY, ONLY, ONLY to be used to prevent cerebral vasospasm in subarachnoid bleeds | nimodipine
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| primary MOA of DHPs | major role block B-1/Ca Channels in VSM. Virtualy no direct effect on heart (indirect, but I am so not talking about it)
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| DHP given IV only | clevidipine
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| DHP 5% bioavailability | nisoldipine
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| DHP 20% bioavailability | felodipine
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| DHP very long acting | amlodipine
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| DHPs - 2 - nothing remarkable | isradipine, nicardipine
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| DHP that can't be used for HTN | nimodipine - only subarachnoid bleed-prevent vasospasm
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| What CCB has MOST ADRs | verapimil wins this prize
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| which CCB has middle ADRs | diltiazem is runner up
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| which CCB class has least ADRs | DHP class of dihydropiridines = dipines has fewest ADRs
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| which CCB is most likely to cause ADR of heart block | verapamil, followed by diltiazepam
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| which CCB is most likely to cause constipation | verapamil, less likely diltiazepam
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| which CCB is most likely to cause ankle edema | any DHP dipipine . . .except nimodipine which is only used for . . .you know it already! quiz answer was nifedipine
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