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77 Cards in this Set

  • Front
  • Back
most important ca channel
L type
where's the L type located
sacrolemma: in membrane of muscle cell
ligands in L type
phenylyaklyamines

benzothiazepines

dihydropyridines
benzothiazepines med
diltiazem
phenylyaklyamine med
verapamil
which ligands are ndhp
phenylaklyamines

benzothiazepines
physiological roles of L type
AV nodal conduction

exicitation-contraction coupling
pore forming binding site of ccb
A1C
where does diltiazem bind
cytoplasmic bridge btw seg 5-6, motif 3 and 4
verapamil binds to motif --
4
action potential phases
0: upstroke

1. early-fast repolarization

2. plateau

3. repolarization

4. diastole
lenght for all myocytes to be activated
qrs
length of electrical depolarization to go from atrium to av node
pr
length of how long action potential lasts
qt
what type brings Ca into the cell
L
the --- exhchanger brings ca out of the cell
Na-Ca

ncx
which receptor senses increase in Ca and opens up and allows Ca to leave the sr
rynodine
what works to bring the Ca back into the SR
SERCA
what stores Ca
CaS

high storage protein
during relaxation what % of ca go back into the sr?

what % leaves via the Ca/Na exchanger
80%

15%
during exicitation what % of Ca comes in from the L type channel
15%

80% comes from the SR
when ---- phosphorylated the Ca is squestered in the SR
phospholambam
what do ccbs block
L type Ca channel

SR release of Ca

Calmodulin
ccb's at tx dose are --- at decreasing venous tone
ineffective
at tx doses ccb's decrease ---- and have no effect on ----
decrease afterload

no effects on preload
effects on nodal Ca ch is dependent on whether agent delays recovery of the --- -----
slow channel (l type)
which slow inward current and decrease rate of recovery
nonDHP
which slows AV conduction
NDHP
which reduces slow inward current but does not affect rate of recovery of slow Ca channels
DHP
which has no effect on AV conduction
DHP
w/ ccb --- is reduced
motility

leads to constipation
w/ ccb lower ----- --- reduced
espohageal contraction

GERD
ccb can --- insulin secretion
decrease
platelets decrease ---- ---- in vitro
plt aggregation
which ccb vasodilate and suppresses cardiac contractility, automaticity, and conduction the most
varapamil
t/f

dhp suppresses cardiac contractility more than diltiazem
f

dhp has very little effect on cardiac contractility
what does dhp do more than verapamil and diltiazem
vasodilate
tx uses of ccb
angina

htn

arrhythmias

diastolic hf

cerebral ischemia

migraine prophylaxis
benzothizazepines/diltiazem is very potent at:
suppressing automaticity and conduction
routh for diltiazem
iv

po
approved indication for diltiazem
angina

htn

svt: afib or flutter, paroxysmal supraventricular tachycardia
diltiazem is metabolized by cyp----
3A
how much of diltiazem is renally excreted
very little: 2-4%
ae of diltiazem:
peripheral vasodilation

neg inotrophic effects

gi

cns

gynecomastia/sex dysfunction

gingival hyperplasia

skin rxn: steven johnson's syndrome
peripheral vasodilation can lead to
flushing

ha

hypotension

peripheral edema

dizziness
neg inotrophic effects can lead to
1st degree block

bradycardia

exacerbation of chf

exacerbatio of pulmonary edema
adverse gi effects:
n/v/d

anorexia

constipation
cns ae in diltiazem
fatigue

nervousness

drowsiness

dizziness

depression

insomnia

confusion
what kind of skin rxn w/ diltiazem
steven johnson's
diltiazem ci w/
advanced heart block

hypotension
relative ci w/ diltiazem
heart failure

liver disease

GERD
diltiazem can a cyp3a4 inhibitor and can increase conc of the following meds
statins

carbamazepine

propranolol

tacrolimus

prednisone
diltiazem as a p glycoprotein inhibitor can increase
dig

tacrolimus

cyclosporin
diltiazme w/ atazanavir will
have PR interval prolongation
diltiazem w/ amiodarone will slow ---- --- or worsen --- ---
sinus rate

AV block
diltiazem and ---- will increase conc of diltiazem
antiretrovirals
route of verapamil
iv

po
approved indications of verapamil
angina

htn

a fib

a flutter

paroxysmal supraventricular tachycardia
t/f

verapamil is largely protein bound
t

90%
ci w/ verapamil
heart block

hypotension
relative ci w/ verapamil
hf

liver disease

gerd
which dhp is not used for htn
nimodipine

used for subarachnoid hemmorhage
route of dhp's
po
w/ dhp what should you avoid in dosing
short acting formulations
t/f

all ccbs have neg inotrophic effects
t
why no or very little suppression of cardiac contractility w/ dhp
due to reflex tachycardia
which dhp has the shortest t 1/2
clevidipine
which dhp is the only iv route
clevidipine
which dhp is very potent
amlodipine
which dhp crosses the bbb
nimodipine
most common ae w/ dhp
peripheral edema
what do you use to tx dhp induced edema
arb


acei
how does peripheral edema occur w/ dhp
dilate arteries

veins constricted
dhp ae include
dyspnea

wheezing

gi effects

cns effects

skin reactions

bezoars

gynecomastia

gingival hyperplasia
which causes gingival hyperplasia more nifedipine and diltiazem
nifedipine
dhp ci
severe aortic stenosis

unstable angina or recent MI
why dhp ci w/ recent mi and ir formulation
due to potent stimulatin of sympathetic activation