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Chapter 44
Calcium Channel Blockers
27
Pharmacology
Undergraduate 3
12/11/2011

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Term
Role of Calcium Channel Blockers?
Definition
Prevent calcium ions from entering the cells. plays a critical role in the function of vascular smooth muscles (coronary vessels and within the heart)
Term
3 Role of calcium channel blockers within the heart?
Definition
Myocardium (force of contractions)
SA Node (heart rate)
AV Node (conduction of impulse)
Term
Three calcium channel blockers
Definition
Dihydropyridines (nifedipine)
verapamil
Diltiazem
Term
Two main direct effects of verapamil
Definition
Blocks Calcium channels on VSM (relax of VSM =relaxation)
Blocks Calcium Channels in the myocardium (most effects here. increasing rate force of contraction and)
Term
Where are most of verapamil effects on?
Definition
myocardium
Term
What are 3 verapamil effects on the myocardium?
Definition
decreases rate, decreases force of contraction, decreases amount of blood pumped with each contraction.
Term
What are 1 verapamil effects on VSM
Definition
relaxation of VSM, therefore decrease in blood pressure
Term
Indirect effect of Verapamil ( this does not always neutralize the slowing of the heart rate, some people will have slowing of heart rate and significant decrease in heart contraction which can lead to heart failure. Depends on indv. patient and how healthy their heart is)
Definition
By decreasing the blood pressure that comes from the relaxation of vascular smooth muscle in the arteries, the baroreceptor reflex takes place to increase the heart rate. The direct effect on the heart is that this decreases the heart rate, so in many cases, it neutralizes. You would think major outcome is decreased blood pressure which counteracts slowing of heart rate but this is only true if heart is healthy (which wouldn't happen in a patient on verapamil) so in patients on verapamil, there is usually slowing on heart rate.
Term
First pass effect with Verapamil
Definition
Large amount changed as it is absorbed acrossGI mucosa, by the time it gets to the blood stream, dose of drug is significantly lower than the amount the patient swallowed
Term
Where is verapamil metabolized
Definition
LIver
Term
4 Major ADR of Verapamil
Definition
(all related to blocking of calcium channel blockers)
-Constipation (most common)
- Vasodilation causes dizziness, headache, edema of feet
- Gingival hyperplasia
-Cardiac Effects (heart block and bradycardia can be seen with too much effects of what the drug is given for)
Term
Where are major sites of actions of Diltiazem?
Definition
predominant action on myocardium (decrease heart rate, decrease conduction, decrease force of conduction
also has some effect on VSM vasodilation
Term
First pass effect of diltiazem
Definition
has some first pass effect, less so than verapamil
Term
2 major S/E of dilizaem
Definition
-Constipation (less than verapamil)
- less likely to cause bradycardia
Term
4 major Uses for diltiazem and verapamil
Definition
Angina
Hypertension
Dysrhythmias
Migrane prophylaxis
Term
Differences between side effects of diltiazem and verapamil
Definition
Verapamil more likely to cause constipation and more likely to cause cardiac effects (bradycardia, heart block)
Term
Major effects of Nifedipine?
Definition
action on VSM causing vasodilation, which activates baroreceptors. Almost no direct effect on the myocardium (no decreasing in heart rate, force of contraction)
Term
2 common clinical application of Nifedipine?
Definition
to treat high blood pressure mostly and also angina
Term
Indirect effect of Nifedipine?
Definition
Baroreceptor reflex. This is more likely. Tachycardia comes from lowering blood pressure
Term
ADR's of Nifedipine?
Definition
-Vasodilation (most common) dizziness, HA, edema (ALMOST ALWAYS HAVE EDMA THROUGHOUT ENTIRE TIME ON DRUG)
Term
What happens to patient with underlying angina that then takes Nifedipine?
Definition
reflex tacycardia increases oxygen demand of the heart cells, and can make angina worse. So not usually used in people with angina because worsens problems in some people
Term
What do all dihydropyridines end in?
Definition
ipine
Term
What dihydropyridine is NOT used for HT or angina and what is it used for?
Definition
Nimodipine - not used for cardiac. It has specific effects on arterioles inside the cranium. It's application is to prevent arterial spasm in a patient that has a sub-aracnoid bleed.
Term
What is the only dihydropyridine that is given intravenously?
Definition
Clevidipine
Term
Drug most likely to cause Heart Block?
Definition
Verapamil
Term
Drug most likely to cause Constipation?
Definition
Verapamil
Term
Most Likely to cause ankle edema?
Definition
Nifedipine
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