Calcium Channel Blockers

Calcium channel blockers are medications that reduce calcium entry through voltage-gated channels, helping regulate blood pressure, cardiac workload, and heart rhythm in clinical care. They primarily inhibit L-type channels in vascular smooth muscle and cardiac tissue: reduced calcium influx relaxes arteries, while decreased myocardial contractility and slowed atrioventricular conduction can lower cardiac demand and control certain tachyarrhythmias. Dihydropyridine drugs are used mainly for hypertension and angina through vasodilation, whereas non-dihydropyridines such as verapamil and diltiazem also target cardiac conduction and rate. These drugs provide important treatments for cardiovascular disease, but require careful selection because their effects vary among agents and patients.

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JoVE Core - Pharmacology

Antiepileptic Drugs: Calcium Channel Blockers

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2024

Calcium channel blockers, a class of antiepileptic drugs, regulate the flow of calcium ions within neurons. Calcium channel blockers exert their antiepileptic effects by targeting T-type calcium channels, which are integral to transmitting nerve signals in the central nervous system. These channels allow the passage of calcium ions, which are vital for neuronal communication. By inhibiting T-type calcium channels, calcium channel blockers effectively reduce the release of neurotransmitters and...

Antianginal Drugs: Calcium Channel Blockers and Ranolazine

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2024

Angina pectoris, a primary symptom of ischemic heart disease, requires careful pharmacological interventions. In this context, calcium channel blockers (CCBs) and ranolazine have emerged as crucial pharmacotherapeutic agents, providing deep insights into the complexities of angina management. CCBs, a diverse class that includes dihydropyridines (nifedipine) and diphenylalkylamines (verapamil and diltiazem), exert their effect by blocking calcium channels in cardiac and smooth muscle cells. This...

Antihypertensive Drugs: Action of Calcium Channel Blockers

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2024

Calcium ions are essential to contract smooth muscle cells in blood vessels. They enter these cells through voltage-dependent calcium channels, specifically L-type calcium channels in the cell membrane. These L-type calcium channels are integral to the excitation-contraction coupling process in smooth muscle. When a stimulus is received by smooth muscle cells, their membrane depolarizes. This alteration in membrane potential instigates the opening of L-type calcium channels. As a result,...

Antiarrhythmic Drugs: Class IV Agents as Calcium Channel Blockers

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2024

Class IV antiarrhythmic drugs, such as verapamil and diltiazem, block calcium channels. They primarily affect the heart, slowing the conduction in calcium-dependent tissues like the SA and AV nodes. These drugs manage reentrant supraventricular tachycardia (SVT) and reduce ventricular rate in atrial flutter/fibrillation. Verapamil, a calcium channel blocker, inhibits calcium movement across myocardial cell membranes and vascular smooth muscle. This results in the dilation of coronary and...

Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers

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2024

Receptor tyrosine kinase inhibitors (TKIs) and calcium channel blockers (CCBs) are two critical categories of drugs employed in the treatment of pulmonary artery hypertension (PAH). PAH is a disease that causes high blood pressure in the pulmonary arteries, resulting in chest pain, fatigue, and shortness of breath. TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...

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