Exam 1 - CCBs

Question 1

What are the types of CCBs?

Answer 1

Dihydropyridines
Non-dihydropyridines
Benzothiazepines

Question 2

Which CCBs are non-dihydropyridines?

Answer 2

Phenylalkylamine
Verapamil (verelan)

Question 2

which CCBs are dihydropyridines?

Answer 2

Amlodipine (Norvasc)
Nifedipine (adalat)
Felodipine (plendil)
Nicardipine (cardene)
Clevidipine (cleviprex)
Isradipine (dynacirc)
Nisoldipine (sular)
Nimodipine (nimotop)

(Remember -dipine)

Question 3

which type of CCB is the most smooth muscle selective?

Answer 3

dihydropyridines

Question 3

which CCB is relatively cardiac selective?

Answer 3

Phenylalkylamine

Question 4

which CCBs are benzothiazepines?

Answer 4

Diltiazem (cardizem)

Question 5

diltiazem is the intermediate between ___ and ___. Why?

Answer 5

Verapamil and dihydropyridines

Because of its selectivity for vascular Ca2+ channels

Question 6

What do CCBs bind to?

Answer 6

L-type Ca2+ channels located on the:

• Vascular smooth muscle
• Cardiac myocytes
• Cardiac nodal tissue (SA and AV nodes)

Question 7

What are Ca2+ channels responsible for? What does this do?

Answer 7

Responsible for regulating Ca2+ influx into muscle cells

Stimulates smooth muscle contraction and cardiac myocyte contraction

Question 8

what is the MOA of CCBs?

Answer 8

Bind to L-type Ca2+ channels

Blocks Ca2+ entry into cells

Vascular smooth muscle relaxation (vasodilation)

Decrease SVR

Decrease arterial BP

Question 9

what are the vascular effects of CCBs?

Answer 9

smooth muscle relaxation (vasodilation)

Question 9

what are the cardiac effects of CCBs?

Answer 9

Decrease contractility (negative inotropy)

Decrease HR (negative chronotropy)

Decrease conduction velocity (negative dromotropy)

Question 9

All dihydropyridines have a much GREATER affinity for ___ than ___, which is beneficial for treating HNT

Answer 9

Greater affinity for vascular Ca2+ channels than Ca2+ channels in the heart

Question 10

Which CCB is relatively selective for the myocardium?

Answer 10

verapamil

Question 10

what is the only diphenylalkylamine available in the US?

Answer 10

verapamil

Question 11

Verapamil is ___ effective as a systemic vasodilator drug

Answer 11

LESS

Question 12

Verapamil has a very important role in treating __ and __

Answer 12

angina, arrhythmias

Question 13

how does verapamil treat angina?

Answer 13

reduces myocardial oxygen demand and reverses coronary vasospasm

Question 14

What is the only benzothiazepine approved in the US?

Answer 14

Diltiazem

Question 15

diltiazem affects ___ and ___ cells

Answer 15

cardiac and vascular smooth muscle

Question 16

Does verapamil or diltiazem have MORE negative inotropic effect on the heart?

Answer 16

verapamil

Question 17

Why is diltiazem preferred over verapamil?

Answer 17

fewer SEs

Question 18

What can cardiac selective, non-dihydropyridine CCBs cause?

Answer 18

Excessive bradycardia

Impaired electrical conduction (like AV nodal block)

Depressed contractility

Question 19

What dihydropyridines should be avoided?

Answer 19

Short acting dihydropyridines

Especially IR nifedipine and nicardipine

Question 20

Are dihydropyridines or nondihydropyridines more potent vasodilators? What can result from this?

Answer 20

Dihydropyridines are MORE potent vasodilators They can cause: - More reflex sympathetic discharge (tachycardia) - Dizziness - Headache - Flushing - Peripheral edema

Question 21

What do dihydropyridines have additional benefits in?

Answer 21

Raynaud’s syndrome (remember that Mia takes amlodipine for hers)

Question 22

___ nondihydropyridines are preferred for HTN

Answer 22

ER

Question 23

What effect do nondihydropyridines have on HR?

Answer 23

decrease HR

Question 24

Dihydropyridines may cause ___, especially in combination with ___

Answer 24

Heart block ß blockers

Question 25

Are dihydropyridines AB rated as interchangeable on an equipotent mg per mg basis? Why or why not?

Answer 25

NO — they have different release mechanisms and different bioavailability parameters

Question 26

Which nondihydropyridines have delayed drug release for several hours after dosing?

Answer 26

Cardizem LA Covera-HS Verelan PM

Question 27

What is the benefit of dosing a nondihydropyridine with DR for several hours after dosing?

Answer 27

You can dose it in the evening to provide chronotherapeutic drug delivery that starts shortly before the person wakes up

Question 28

What condition do nondihydropyridines have additional benefits in?

Answer 28

Atrial tachyarrhythmia

Question 29

What is the brand name, class, usual dose range, and frequency of amlodipine?

Answer 29

Norvasc DHP CCB 2.5 - 10 mg/day 1 daily

Question 30

What is the brand name, class, usual dose range, and frequency of felodipine?

Answer 30

Plendil DHP CCB 5-20 mg/day 1 daily

Question 31

What is the brand name, class, usual dose range, and frequency of isradipine?

Answer 31

Dynacirc DHP CCB 5-10 mg/day 2

Question 32

What is the brand name, class, usual dose range, and frequency of isradipine SR?

Answer 32

Dynacirc SR DHP CCB 5-20 mg/day 1 daily

Question 33

What is the brand name, class, usual dose range, and frequency of nicardipine SR?

Answer 33

Cardene SR DHP CCB 60-120 mg/day 2 daily

Question 34

What is the brand name, class, usual dose range, and frequency of nifedipine long acting?

Answer 34

Adalat CC, Nifedical XL, Procardia XL DHP CCB 30-90 mg/day 1 daily

Question 35

What is the brand name, class, usual dose range, and frequency of nisoldipine?

Answer 35

Sulfar DHP CCB 10-40 mg/day 1 daily

Question 36

What is the brand name, class, usual dose range, and frequency of diltiazem SR?

Answer 36

Cardizem SR Non-DHP CCB 180-360 mg/day 2 daily