CH 48 Calcium Channel Blockers
Calcium Channel Blockers aka Calcium antagonists, slow channel blockers
Overall effects and MOA
Drugs that prevent calcium from entering cells
Greatest impact on heart and blood vessels
Therapeutic Uses of calcium channel blockers
Hypertension
Angina pectoris
Cardiac dysrhythmias
* controversy of safety for patients with hypertension and diabetes
Physiologic Functions and Consequences of a Blockade
Vascular Smooth Muscle
Calcium channels open= contractile process
Calcium channels closed = vasoconstriction
Therapeutic doses
Selectively act on peripheral arterioles and arteries
Selectively act on peripheral arterioles of the heart
No significant effect on veins
Verapamil and Diltiazem (Nondihydropyridines)
^Act on arterioles and the heart
Overall effects and MOA
Direct effects on the heart and blood vessels
Indirect reflex effects (heart rate increases and blood pressure decreases)
Five direct hemodynamic effects of verapamil and diltiazem
Blockade at peripheral arterioles
(reduces arterial pressure)
Blockade at arteries and arterioles of heart
(increases coronary perfusion)
Blockade at SA node
(reduces heart rate)
Blockade at AV node **MOST IMPORTANT
(Decreases AV nodal Conduction )
Blockade in the Myocardium
(decreases force of contraction)
Indirect hemodynamic effects of verapamil and diltiazem
Baroreceptor reflex (pressure sensor to maintain Blood Pressure)
Net effects of verapamil and diltiazem
little/no effect on cardiac performance
Vasodilation accompanied by reduced arterial pressure and increased coronary perfusion
Therapeutic uses of verapamil
Angina pectoris (vasospastic angina and angina of effort)
Essential hypertension (second line agent after thiazide diuretics)
Cardiac dysrhythmias (atrial flutter, atrial fibrillation, paroxysmal supraventricular tachycardia
** supraventricular tachycardia: heart rate of 150+; heart rate so fast that chambers cannot fill adequately
Migraine
Adverse effects of verapamil
^Beta Blockers INTENSIFY adverse effects
Constipation **most common
Results blockade of calcium channels in smooth muscle of intestines (decreased peristalsis)
Especially severe for older adults
Can be decreased by increasing fiber and fluids
Dizziness
Facial flushing: : due to relaxed arteries
Headache
Edema of ankles and feet: due to relaxed arteries
Gingival hyperplasia: gum swelling
Heart block: electrical pathway is impaired; communication not working
Drug interactions of verapamil
Digoxin: slows down heart rate
Beta-adrenergic blocking agents
Verapamil Toxicity
Severe hypotension
Bradycardia and AV block
Ventricular tachydysrhythmias
To treat toxicity perform Gastric lavage (wash out stomach with saline) and activated charcoal
Note: IV verapamil for dysrhythmias can be used for severe cardiovascular effects (Monitor Blood pressure and ECG; resuscitation equipment should be immediately available)
Nifedipine [adalat, Nifedical, Nifediac, Procardia] (Dihydropyridines)
^Act mainly on vascular smooth muscle
Overall effects and MOA
Significant blockade of calcium channels in blood vessels
Minimal blockade of calcium channels in heart
Results in vasodilation
Cannot be used to treat dysrhythmias
Less likely than verapamil to exacerbate preexisting cardiac disorders
Direct effects of Nifedipine
Blockade of calcium channels in vascular smooth muscle
Vasodilation by blocking calcium channels
Indirect effects of Nifedipine
Lowered Blood pressure and activates baroreceptor reflex (Primarily with immediate vs sustained release)
Increased heart rate
Increased contractile force
Therapeutic uses of Nifedipine
Angina pectoris
Hypertension
Relieve migraine and suppress preterm labor (investigational basis)
Adverse effects of Nifedipine
^Beta Blockers decrease adverse effects
Flushing
Dizziness
Headache
Peripheral edema
Gingival hyperplasia
Chronic eczematous rash in older patients
Increases cardiac oxygen demand
Reflex tachycardia (can be combined with beta blocker to prevent reflex tachycardia)
**Note: Immediate release/rapid acting Calcium Channel blockers have been associated with increased mortality in patients with MI and unstable angina