Calcium channel blockers Flashcards

1
Q

What is the more determining factor for ion flow? Concentration gradient or Electrical gradient?

A

Electrical Gradient

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2
Q

Where is K more highly concentrated?

A

Inside the cell

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3
Q

Where is K more lowly concentrated?

A

Outside the cell

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4
Q

Where is Na low?

A

Inside the cell

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5
Q

Where is Na high?

A

Outside

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6
Q

Ca+ is low where?

A

Inside the cell

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7
Q

Ca+ is high where?

A

Outside the cell

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8
Q

Most important Ca voltage gate you need to know for this class?

A

L-type, Ca 1.2

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9
Q

What triggers contraction of Ca 1.2?

A

Ca2+ entry

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10
Q

Ca 1.2 is found on what?

A

Cardiac and smooth muscle

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11
Q

Ca 1.3 is found where?

A

SA/AV nodes, neurons, and endocrine cells

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12
Q

What is a Ca1.3 a trigger for?

A

Hormone secretion

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13
Q

Blockage of vascular smooth muscle leads to what?

A

Vasodilation

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14
Q

Block of channels in cardiac muscle and SA/AV node results in what benefit?

A

Anti-arrhythmic

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15
Q

What are intracellular stores of Ca2+ called?

A

RYR@ (ryanodine receptor 2)

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16
Q

What REQUIRES Ca2+?

A

Cardiac and smooth muscle contraction

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17
Q

What does Ca2+ release from SR bind to?

A

Troponin C

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18
Q

Ca2+ binding of troponin c leads to what?

A

Displacement of tropomyosin

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19
Q

Displacement of Tropomyosin causes what?

A

Allows myosin to bind actin

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20
Q

What coupling allows for skeletal muscle contraction?

A

Coupling between Ca 1.1 and RYR1

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21
Q

Does skeletal muscle contraction require extracellular Ca2+?

A

No

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22
Q

Clinical applications for Calcium channel blockers? (3)

A

Angina Pectoris
Arrhythmia
Hypertension

23
Q

3 Distinct Chemical Classes of Calcium Channel blockers?

A

Dihydropyridines
Phenylalkylamines
Benzothiazepines

24
Q

Main structural feature of Dihydropyridines?

A

Dihydropyridine ring

25
Q

+ enantiomer of DHP does what?

A

Keeps gate closed and blocks current

26
Q
  • enantiomer of DHP does what?
A

Won’t let gate close and keeps current going

27
Q

When do you give Clevidipine?

A

When you want to treat hypertension immediately and oral administration isn’t possible.

28
Q

What do you have to watch out for when giving clevidipine?

A

Allergy to soy and egg

29
Q

Where are DHPs most potent?

A

Relaxing smooth muscle such as coronary artery

30
Q

Do DHPs compromise cardiac function?

A

No

31
Q

DHPs are dependent on what for their potency?

A

Voltage of membrane

32
Q

Binding sites for DHPs, PAAs, and BZPs are what?

A

Linked, but not identical

33
Q

Characteristics of DHP block?

A

No frequency dependence

Marked tonic block

34
Q

What effects does DHP have on vascular system (3)?

A

Decrease in peripheral resistance
Decreased after load
Little effect on HR or contraction

35
Q

Drug listed in packet that has the least vascular specificity?

A

Nifedipine

36
Q

Drug used in cases of sub arachnoid hemorrhage to prevent neuropathy?

A

Nimodipine

37
Q

Secondary result of DHPs on the heart?

A

Reflex tachycardia except for amlodipine

38
Q

How do DHPs reduce angina?

A

They lower the oxygen demand of the heart

39
Q

Which DHP does depress cardiac function?

A

Nifedipine

40
Q

Why is Amlodipine the most commonly prescribed calcium channel blocker?

A

It has slow onset and long duration of action

41
Q

Phenylalkylamine (PAAs) cause what?

A

Vasodilation, less potent than DHP

42
Q

Effect of PAA on SA and AV node?

A

Slows conduction through SA and AV node to reduce heart rate and force of contraction

43
Q

How severe is the reflex tachycardia from PAA?

A

Blunted

44
Q

Characteristics of PAA block?

A

Marked frequency dependence

Very little tonic block

45
Q

Benzothiazepine affects the heart how?

A

Vasodilation, slows conduction, reflex tachycardia, but inhibits less than verapamil but more than DHPs

46
Q

Characteristics of BZP block?

A

Some tonic block

Some frequency block

47
Q

Of the three types of drugs discussed which affects heart rate the most?

A

Verapamil

48
Q

Of the three types of drugs discussed which affects AV conductance/Myocardial contraction the most?

A

Verapamil

49
Q

Of the three drugs listed which affects arterial vasodilation the most?

A

DHPs

50
Q

Most important side effects of calcium channel blockers?

A

Ankle edema
Constipation
Facial flushing
Tachycardia

51
Q

Which class of drug causes the most constipation?

A

Verapamil

52
Q

Which class of drug causes the most facial flush/

A

DHPs

53
Q

Which class of drugs causes the most tachycardia?

A

DHPs

54
Q

Danger surrounding prompt release nifedipine?

A

Increased risk of subsequent heart attack due to reflex sympathetic response tachycardia