Exam 1 - CCBs Flashcards
What are the types of CCBs?
Dihydropyridines
Non-dihydropyridines
Benzothiazepines
Which CCBs are non-dihydropyridines?
Phenylalkylamine
Verapamil (verelan)
which CCBs are dihydropyridines?
Amlodipine (Norvasc)
Nifedipine (adalat)
Felodipine (plendil)
Nicardipine (cardene)
Clevidipine (cleviprex)
Isradipine (dynacirc)
Nisoldipine (sular)
Nimodipine (nimotop)
(Remember -dipine)
which type of CCB is the most smooth muscle selective?
dihydropyridines
which CCB is relatively cardiac selective?
Phenylalkylamine
which CCBs are benzothiazepines?
Diltiazem (cardizem)
diltiazem is the intermediate between ___ and ___. Why?
Verapamil and dihydropyridines
Because of its selectivity for vascular Ca2+ channels
What do CCBs bind to?
L-type Ca2+ channels located on the:
- Vascular smooth muscle
- Cardiac myocytes
- Cardiac nodal tissue (SA and AV nodes)
What are Ca2+ channels responsible for? What does this do?
Responsible for regulating Ca2+ influx into muscle cells
Stimulates smooth muscle contraction and cardiac myocyte contraction
what is the MOA of CCBs?
Bind to L-type Ca2+ channels
Blocks Ca2+ entry into cells
Vascular smooth muscle relaxation (vasodilation)
Decrease SVR
Decrease arterial BP
what are the vascular effects of CCBs?
smooth muscle relaxation (vasodilation)
what are the cardiac effects of CCBs?
Decrease contractility (negative inotropy)
Decrease HR (negative chronotropy)
Decrease conduction velocity (negative dromotropy)
All dihydropyridines have a much GREATER affinity for ___ than ___, which is beneficial for treating HNT
Greater affinity for vascular Ca2+ channels than Ca2+ channels in the heart
Which CCB is relatively selective for the myocardium?
verapamil
what is the only diphenylalkylamine available in the US?
verapamil
Verapamil is ___ effective as a systemic vasodilator drug
LESS
Verapamil has a very important role in treating __ and __
angina, arrhythmias
how does verapamil treat angina?
reduces myocardial oxygen demand and reverses coronary vasospasm
What is the only benzothiazepine approved in the US?
Diltiazem
diltiazem affects ___ and ___ cells
cardiac and vascular smooth muscle
Does verapamil or diltiazem have MORE negative inotropic effect on the heart?
verapamil
Why is diltiazem preferred over verapamil?
fewer SEs
What can cardiac selective, non-dihydropyridine CCBs cause?
Excessive bradycardia
Impaired electrical conduction (like AV nodal block)
Depressed contractility
What dihydropyridines should be avoided?
Short acting dihydropyridines
Especially IR nifedipine and nicardipine
Are dihydropyridines or nondihydropyridines more potent vasodilators? What can result from this?
Dihydropyridines are MORE potent vasodilators
They can cause:
- More reflex sympathetic discharge (tachycardia)
- Dizziness
- Headache
- Flushing
- Peripheral edema
What do dihydropyridines have additional benefits in?
Raynaud’s syndrome (remember that Mia takes amlodipine for hers)
___ nondihydropyridines are preferred for HTN
ER
What effect do nondihydropyridines have on HR?
decrease HR
Dihydropyridines may cause ___, especially in combination with ___
Heart block
ß blockers
Are dihydropyridines AB rated as interchangeable on an equipotent mg per mg basis? Why or why not?
NO — they have different release mechanisms and different bioavailability parameters
Which nondihydropyridines have delayed drug release for several hours after dosing?
Cardizem LA
Covera-HS
Verelan PM
What is the benefit of dosing a nondihydropyridine with DR for several hours after dosing?
You can dose it in the evening to provide chronotherapeutic drug delivery that starts shortly before the person wakes up
What condition do nondihydropyridines have additional benefits in?
Atrial tachyarrhythmia
What is the brand name, class, usual dose range, and frequency of amlodipine?
Norvasc
DHP CCB
2.5 - 10 mg/day
1 daily
What is the brand name, class, usual dose range, and frequency of felodipine?
Plendil
DHP CCB
5-20 mg/day
1 daily
What is the brand name, class, usual dose range, and frequency of isradipine?
Dynacirc
DHP CCB
5-10 mg/day
2
What is the brand name, class, usual dose range, and frequency of isradipine SR?
Dynacirc SR
DHP CCB
5-20 mg/day
1 daily
What is the brand name, class, usual dose range, and frequency of nicardipine SR?
Cardene SR
DHP CCB
60-120 mg/day
2 daily
What is the brand name, class, usual dose range, and frequency of nifedipine long acting?
Adalat CC, Nifedical XL, Procardia XL
DHP CCB
30-90 mg/day
1 daily
What is the brand name, class, usual dose range, and frequency of nisoldipine?
Sulfar
DHP CCB
10-40 mg/day
1 daily
What is the brand name, class, usual dose range, and frequency of diltiazem SR?
Cardizem SR
Non-DHP CCB
180-360 mg/day
2 daily
