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77 Cards in this Set
- Front
- Back
most important ca channel
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L type
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where's the L type located
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sacrolemma: in membrane of muscle cell
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ligands in L type
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phenylyaklyamines
benzothiazepines dihydropyridines |
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benzothiazepines med
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diltiazem
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phenylyaklyamine med
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verapamil
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which ligands are ndhp
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phenylaklyamines
benzothiazepines |
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physiological roles of L type
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AV nodal conduction
exicitation-contraction coupling |
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pore forming binding site of ccb
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A1C
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where does diltiazem bind
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cytoplasmic bridge btw seg 5-6, motif 3 and 4
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verapamil binds to motif --
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4
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action potential phases
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0: upstroke
1. early-fast repolarization 2. plateau 3. repolarization 4. diastole |
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lenght for all myocytes to be activated
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qrs
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length of electrical depolarization to go from atrium to av node
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pr
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length of how long action potential lasts
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qt
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what type brings Ca into the cell
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L
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the --- exhchanger brings ca out of the cell
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Na-Ca
ncx |
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which receptor senses increase in Ca and opens up and allows Ca to leave the sr
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rynodine
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what works to bring the Ca back into the SR
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SERCA
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what stores Ca
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CaS
high storage protein |
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during relaxation what % of ca go back into the sr?
what % leaves via the Ca/Na exchanger |
80%
15% |
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during exicitation what % of Ca comes in from the L type channel
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15%
80% comes from the SR |
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when ---- phosphorylated the Ca is squestered in the SR
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phospholambam
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what do ccbs block
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L type Ca channel
SR release of Ca Calmodulin |
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ccb's at tx dose are --- at decreasing venous tone
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ineffective
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at tx doses ccb's decrease ---- and have no effect on ----
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decrease afterload
no effects on preload |
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effects on nodal Ca ch is dependent on whether agent delays recovery of the --- -----
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slow channel (l type)
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which slow inward current and decrease rate of recovery
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nonDHP
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which slows AV conduction
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NDHP
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which reduces slow inward current but does not affect rate of recovery of slow Ca channels
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DHP
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which has no effect on AV conduction
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DHP
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w/ ccb --- is reduced
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motility
leads to constipation |
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w/ ccb lower ----- --- reduced
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espohageal contraction
GERD |
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ccb can --- insulin secretion
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decrease
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platelets decrease ---- ---- in vitro
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plt aggregation
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which ccb vasodilate and suppresses cardiac contractility, automaticity, and conduction the most
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varapamil
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t/f
dhp suppresses cardiac contractility more than diltiazem |
f
dhp has very little effect on cardiac contractility |
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what does dhp do more than verapamil and diltiazem
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vasodilate
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tx uses of ccb
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angina
htn arrhythmias diastolic hf cerebral ischemia migraine prophylaxis |
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benzothizazepines/diltiazem is very potent at:
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suppressing automaticity and conduction
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routh for diltiazem
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iv
po |
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approved indication for diltiazem
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angina
htn svt: afib or flutter, paroxysmal supraventricular tachycardia |
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diltiazem is metabolized by cyp----
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3A
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how much of diltiazem is renally excreted
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very little: 2-4%
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ae of diltiazem:
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peripheral vasodilation
neg inotrophic effects gi cns gynecomastia/sex dysfunction gingival hyperplasia skin rxn: steven johnson's syndrome |
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peripheral vasodilation can lead to
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flushing
ha hypotension peripheral edema dizziness |
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neg inotrophic effects can lead to
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1st degree block
bradycardia exacerbation of chf exacerbatio of pulmonary edema |
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adverse gi effects:
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n/v/d
anorexia constipation |
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cns ae in diltiazem
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fatigue
nervousness drowsiness dizziness depression insomnia confusion |
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what kind of skin rxn w/ diltiazem
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steven johnson's
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diltiazem ci w/
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advanced heart block
hypotension |
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relative ci w/ diltiazem
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heart failure
liver disease GERD |
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diltiazem can a cyp3a4 inhibitor and can increase conc of the following meds
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statins
carbamazepine propranolol tacrolimus prednisone |
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diltiazem as a p glycoprotein inhibitor can increase
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dig
tacrolimus cyclosporin |
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diltiazme w/ atazanavir will
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have PR interval prolongation
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diltiazem w/ amiodarone will slow ---- --- or worsen --- ---
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sinus rate
AV block |
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diltiazem and ---- will increase conc of diltiazem
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antiretrovirals
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route of verapamil
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iv
po |
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approved indications of verapamil
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angina
htn a fib a flutter paroxysmal supraventricular tachycardia |
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t/f
verapamil is largely protein bound |
t
90% |
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ci w/ verapamil
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heart block
hypotension |
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relative ci w/ verapamil
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hf
liver disease gerd |
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which dhp is not used for htn
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nimodipine
used for subarachnoid hemmorhage |
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route of dhp's
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po
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w/ dhp what should you avoid in dosing
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short acting formulations
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t/f
all ccbs have neg inotrophic effects |
t
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why no or very little suppression of cardiac contractility w/ dhp
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due to reflex tachycardia
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which dhp has the shortest t 1/2
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clevidipine
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which dhp is the only iv route
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clevidipine
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which dhp is very potent
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amlodipine
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which dhp crosses the bbb
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nimodipine
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most common ae w/ dhp
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peripheral edema
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what do you use to tx dhp induced edema
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arb
acei |
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how does peripheral edema occur w/ dhp
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dilate arteries
veins constricted |
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dhp ae include
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dyspnea
wheezing gi effects cns effects skin reactions bezoars gynecomastia gingival hyperplasia |
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which causes gingival hyperplasia more nifedipine and diltiazem
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nifedipine
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dhp ci
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severe aortic stenosis
unstable angina or recent MI |
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why dhp ci w/ recent mi and ir formulation
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due to potent stimulatin of sympathetic activation
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