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Calcium (Calcium-) Antagonists (Calcium Channel Blockers)

Mechanism of Action Hypertension Medication Calcium Antagonist

As a hypertension medication, calcium antagonists (calcium channel blockers) such as amlodipine, diltiazem, nifedipine, nitrenidipine, verapamil, and the like are also used.
Calcium (calcium) is an essential mineral due to its various functions in the body. The most well-known effect is on the bones: if too little calcium is supplied through food or if the body can absorb too little, the risk of osteoporosis increases. However, calcium also plays an important role in blood pressure and the excitation or contraction of the heart. It acts as a messenger between cells, as it can enter or exit the cell through special channels in the cell membrane. These channels are of utmost importance for blood pressure and the heart. When calcium is released from the storage of the vascular cell, it triggers a series of reactions that can lead to the narrowing of the vessel and thus an increase in blood pressure.

The effect in the heart is similar. The calcium flowing into the heart muscle cells causes the heart muscle to contract more strongly. Calcium also affects the conduction of impulses in the heart. It primarily triggers the excitation formation and conduction in the AV node. The faster calcium flows in, the faster the heart beats.

Calcium Antagonists: Effect

Muscle cells need calcium to contract. Calcium channel blockers inhibit the influx of calcium into the smooth muscle of blood vessels. This leads to arterial dilation and thus a reduction in blood pressure. In heart muscle cells, calcium channel blockers reduce the ability to contract (contractility) and inhibit conductivity, resulting in a slower pulse.
Calcium channel blockers are classified into 2 classes depending on their main site of action (sometimes also into 3 classes according to literature):
  • Dihydropyridines (amlodipine, nifedipine): primarily act on the vessels
    Medications of this type can also be used for symptom control of stable angina pectoris.
  • Non-dihydropyridines (verapamil, diltiazem): primarily act on the heart and on impulse generation and conduction
     
    Calcium antagonists of the diltiazem type hold a special position here, influencing all different target organs. In addition to their use as hypertension medication, these substances are also used in stable angina pectoris, cardiac arrhythmias with tachycardia, and atrial fibrillation.
In most cases, calcium antagonists are used in combination with other hypertension medications.

Calcium Antagonists: Side Effects

Calcium antagonists of the dihydropyridine type (amlodipine, nifedipine), which primarily act on vascular smooth muscle, often cause side effects such as water retention in the ankles (edema), facial flushing (flush), increased awareness of heartbeat (palpitations), and headaches.
For non-dihydropyridine preparations (verapamil, diltiazem), constipation and a slowed heart rate occur more frequently.
It is crucial to ensure that simultaneous treatment with beta-blockers and non-dihydropyridine calcium channel blockers (verapamil, diltiazem) is only carried out by experienced practitioners when specifically necessary. Normally, they should not be combined.
For completeness, please read the package insert.

Calcium Antagonists: Active Ingredients

amlodipine, diltiazem, felodipine, isradipine, manidipine, nifedipine, nilvadipine, nisoldipine, nitrenidipine, verapamil

Calcium Antagonists: Examples of Active Ingredients and Approved Medicinal Substances

Sources


By Sabine Croci. This article is medically reviewed. Last updated (03/2024).
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