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PHRM 844 > Calcium Blockers > Flashcards

Calcium Blockers Flashcards

1
Q

what is an ion channel

A

protein that form pores in plasma membrane

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2
Q

what determines direction of flow?

A

concentration gradient
electrical gradient

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3
Q

K+, Na+, and Ca2+ conc inside and outside cell

A

K+ high inside, low outside
Na+ high outside, low inside
Ca2+ high outside, very low inside

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4
Q

what is kcsa channel

A

H+ gated K+ channel in closed state

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5
Q

what is mthK channel

A

Ca2+ gated K+ channel in open state, opens when it binds calcium, crystallized in presence of calcium

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6
Q

location and function of L type channel Cav 1.2

A

cardiac, smooth muscle
Ca entry triggers contraction

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7
Q

block of calcium channels in vascular smooth muscle effect and uses?

A

vasodilation
used for angina and blood pressure decrease

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8
Q

block of calcium channels in cardiac muscle and SA/AV node uses?

A

antiarrhythmic

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9
Q

vascular smooth muscle mechanism

A

calcium induced calcium release
Ca influx via Cav 1.2 releases Ca from intracellular stores via ryanodine (RYR2) in the SR
calcium calmodulin binds myosin LC kinase which becomes myosin LC and gets phosphorylated then acts with actin to contraction

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10
Q

what is required for contraction of cardiac and smooth muscle?

A

extracellular Ca

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11
Q

how can PKA increase Ca influx

A

phosphorylation of Cav1.2
increases contractility and av node conduction rate

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12
Q

cardiac muscle contraction mechanism

A

Ca ions released from SR binds troponin C
displacement of tropomyosin
myosin binds actin and contraction

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13
Q

skeletal muscle contraction? is Ca required?

A

coupling between Cav1.1 and RYR1
extracellular calcium not required
calcium blockers don’t do much here

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14
Q

what do calcium channel blockers treat?

A

decrease blood pressure, angina, arrhythmia

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15
Q

three classes of CCbs

A

dihydropyridines
phenylalkylamines
benzothiazepines

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16
Q

dihydropyridine members

A

nifedipine
amlodipide
clevidipine
nimodipine

17
Q

what is clevidipine

A

short acting DHP
given IV for hypertension when they can’t PO
esterases cleave rapidly

18
Q

mechanism of DHPs

A

interferes with gating via enantiomers
+ blocks current
- potentiates current

19
Q

tissue selectivity of DHPs

A

vascular smooth muscle, do not compromise cardiac function

20
Q

are dihydropyridines voltage dependent?

A

yes

21
Q

do dihydropyridines bind to open or closed channels?

A

closed to prevent openeing - tonic block

22
Q

are dihydropyridines frequency dependent?

A

no

23
Q

vascular selectivity of DHPs

A

arterial dilation
decreased afterload

24
Q

nimodipine use and selectivity

A

selective for cerebral arteries
used in sub-arachnoid hemorrhage

25
Q

which DHP does not have reflex tachycardia secondary to vasodilation

A

amlodipine

26
Q

amlodipine onset and duration

A

slow onset
long duration

27
Q

nifedipine can cause what

A

prompt release can cause heart attach, reflex tachycardia serious

28
Q

phenylalkylamine drug

A

verapamil

29
Q

verapamil does what

A

slows conduction through SA/AV (reduce HR and contraction force)
less potent vasodilation
blunted reflex tachycardia

30
Q

verapamils inhibitory effect on the heart is due to ____

A

frequency dependent block

31
Q

channel has to be ____ for verapamil to enter pore

A

open (frequency dependent)

32
Q

does verapamil have tonic block

A

very little tonic block

33
Q

benzothiazepine drug

A

diltiazem

34
Q

diltiazem inhibits the heart _____ than verapamil

A

less

35
Q

does diltiazem have frequency dependent block?

A

yes

36
Q

does diltiazem have tonic block

A

some tonic block

37
Q

DHPs side effects

A

ankle edema
flushing
tachycardia

38
Q

verapamil side effects

A

ankle edema
constipation

39
Q

diltiazem side effects

A

ankle edema

PHRM 844 (16 decks)

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