10/16/2020 Calcium channel blockers - AMBOSS

Calcium channel blockers

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Summary

Calcium channel blockers (CCBs) are drugs that bind to and block the L-type calcium
channel. The L-type channels are the predominant calcium channels in the myocardium
and the vascular smooth muscles. By blocking these channels, CCBs cause peripheral
arterial vasodilation and myocardial depression, which leads to a drop in blood pressure
and negative chronotropic, inotropic, and dromotropic effects on the myocardium. The
most common indications for CCB use are hypertension, angina, and supraventricular
arrhythmias. CCBs are also beneficial in the treatment of cardiomyopathy,
thromboangiitis obliterans, Raynaud's phenomenon, and cluster headaches. CCBs are
divided into three classes based on their effects: dihydropyridines (e.g., nifedipine,
amlodipine) are potent vasodilators, phenylalkylamines (verapamil, gallopamil) are
potent myocardial depressants, and benzothiazepines (diltiazem) are moderate
vasodilators and myocardial depressants. The main side effects of dihydropyridines are
caused by vasodilation (headaches, peripheral edema, reflex tachycardia), and those of
phenylalkylamines by myocardial depression (bradyarrhythmias, atrioventricular block).
The side effects of benzothiazepines are generally similar but milder compared to those of
the other CCB classes. CCBs are contraindicated in patients with pre-existing cardiac
conduction disorders (e.g., atrioventricular block, sick sinus syndrome), symptomatic
hypotension, and acute coronary syndrome.

Overview

Class of CCB Examples Effects

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Class of CCB Examples Effects

Dihydropyridines [1][2] Short-acting Potent

vasodilator
: nifedipine,
clevidipine Minimal
Medium- myocardial
acting depressant
activity
: nitrendipine,
nicardipine,
lercanidipine
Long-acting

: amlodipine

Non- Benzothiazepines Diltiazem Moderate

dihydropyridine vasodilator
CCBs Moderate
myocardial
depressant
activity

Phenylalkylamines Verapamil Less potent

Gallopamil vasodilator than
dihydropyridines

Potent
myocardial
depressant

References:[3]

Pharmacodynamics

CCBs bind to and block L-type calcium channels

→ decreased frequency of Ca2+ channel opening in response to cell membrane

depolarization

→ decreased transmembrane Ca2+ current

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Effects of decreased Ca2+ influx

Vascular smooth muscle relaxation

→ vasodilation → decreased peripheral vascular resistance → decreased

afterload → decreased blood pressure
Decreased cardiac muscle contractility (negative inotropic action) →
decreased cardiac output → decreased blood pressure
Decreased SA node discharge rate (negative chronotropic action)

→ decreased heart rate (bradycardia) → decreased cardiac output →

decreased blood pressure
Decreased AV node conduction (negative dromotropic action) → termination
of supraventricular arrhythmias

Dihydropyridine CCBs (e.g., nifedipine, amlodipine) primarily act on vascular

smooth muscles. Nondihydropyridine CCBs (diltiazem < verapamil) primarily act on the
heart.
References:[4][5]

Adverse effects

Dihydropyridines Effects due to vasodilation

Peripheral edema (esp. amlodipine)

Headaches, dizziness
Facial flushing, feeling feverish
Reflex tachycardia (esp. nifedipine)

May worsen symptoms of angina

Gingival hyperplasia

Benzothiazepines Side effects similar to the other classes of CCBs, but

milder

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Phenylalkylamines Reduced contractility/bradyarrhythmia and drug-induced

atrioventricular block

Constipation

Phenylalkylamines (verapamil) primarily affect the calcium channels of the heart

and are contraindicated in cases of heart failure because of their negative effect on
myocardial contractility!

References:[6][7][8][9][10][11][12]
We list the most important adverse effects. The selection is not exhaustive.

Indications

Common indications for CCBs

Arterial hypertension (esp. amlodipine)

Angina (all CCBs except for nifedipine)

Stable angina (for patients with contraindications or who are not
responsive to β blockers)

Vasospastic angina (variant or Prinzmetal's angina)

Supraventricular arrhythmias (esp. verapamil and diltiazem

Supraventricular tachycardia
Atrial fibrillation

Less common indications

Cardiomyopathy

Raynaud's phenomenon
Thromboangiitis obliterans
Cluster headache
Achalasia

References:[13]

Contraindications

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All classes of CCB

Allergy/hypersensitivity to CCBs
Symptomatic hypotension

Acute coronary syndrome

Dihydropyridines

Hypertrophic obstructive cardiomyopathy (HOCM)

Severe stenotic heart valve defects

Benzothiazepines and phenylalkylamines

Pre-existing cardiac conduction disorders

Wolff-Parkinson-White syndrome

Sick sinus syndrome

Systolic dysfunction (in congestive heart failure)
Bradycardia
Second or third-degree atrioventricular block
Combination with beta blockers → risk of AV block

References:[14][6][7][15][16][17][18][19][20][21][22][23]

We list the most important contraindications. The selection is not exhaustive.

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