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Antiarrhythmic Drugs: Class I Agents as Sodium Channel Blockers01:22

Antiarrhythmic Drugs: Class I Agents as Sodium Channel Blockers

4.1K
Class I antiarrhythmic drugs are used to treat various types of arrhythmias or irregular heart rhythms. These drugs block the sodium (Na+) channels in the cardiac cells, thereby affecting the movement of electrical impulses across the heart. Class I antiarrhythmic drugs are divided into three subgroups: Class IA, Class IB, and Class IC, each with distinct mechanisms of action and effects on the heart.
Class 1A Antiarrhythmic Drugs: These drugs work by moderately blocking sodium channels,...
4.1K
Antiarrhythmic Drugs: Class II Agents as β-Adrenergic Blockers01:24

Antiarrhythmic Drugs: Class II Agents as β-Adrenergic Blockers

2.3K
Adrenergic stimulation generally impacts cardiac rate and rhythm. Specifically, stimulation of the β-adrenoceptors triggers an increase in intracellular calcium ion influx and pacemaker currents, which may cause arrhythmias. Catecholamines like adrenaline also demonstrate β2-adrenoceptor-mediated hypokalemia, impacting cardiac action potential and disrupting the normal cardiac rhythm. Class II antiarrhythmic drugs are β-adrenoceptor antagonists or β-blockers, which...
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Antiarrhythmic Drugs: Class IV Agents as Calcium Channel Blockers01:20

Antiarrhythmic Drugs: Class IV Agents as Calcium Channel Blockers

2.7K
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...
2.7K
Antiarrhythmic Drugs: Class III Agents as Potassium Channel Blockers01:12

Antiarrhythmic Drugs: Class III Agents as Potassium Channel Blockers

3.0K
Class III antiarrhythmic drugs are a group of medications that can prolong action potentials in the heart. They achieve this by blocking potassium channels or enhancing inward currents from sodium channels. However, these drugs have a unique property of "reverse use-dependence," which is most pronounced at slower heart rates and can lead to torsades de pointes—a specific type of arrhythmia. However, it is essential to note that excessive QT interval prolongation—a measure of...
3.0K
Depolarizing Blockers: Mechanism of Action01:28

Depolarizing Blockers: Mechanism of Action

3.5K
Depolarizing blockers act on skeletal muscle fibers' membranes and induce their depolarization. Most depolarizing blockers have two quaternary N+ atoms that bind the nicotinic acetylcholine receptors and cause neuromuscular blockade within minutes.
Succinylcholine is the most commonly used depolarizing blocker. Chemically, it constitutes two molecules of acetylcholine joined together by an acetate methyl group. They act on the receptors in the same way as acetylcholine. Because...
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Drugs Acting on Autonomic Ganglia: Blockers01:28

Drugs Acting on Autonomic Ganglia: Blockers

1.9K
Ganglionic blockers inhibit autonomic activity by blocking nicotinic receptors in the autonomic ganglia, suppressing impulse transmission. These blockers lack selectivity between sympathetic and parasympathetic ganglia and are ineffective as neuromuscular junction antagonists. They can be categorized into two groups:
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Video Experimental Relacionado

Updated: Apr 4, 2026

Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology
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Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology

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Bloqueadores de la PD-1

Jedd D Wolchok1

  • 1Department of Medicine, Memorial Sloan-Kettering Cancer Center, New York, NY 10065, USA.

Cell
|August 29, 2015
PubMed
Resumen
Este resumen es generado por máquina.

El nivolumab y el pembrolizumab son anticuerpos monoclonales que bloquean los receptores de muerte programada-1 (PD-1). Este enfoque de inmunoterapia desinhibe las respuestas inmunológicas antitumorales, lo que llevó a las recientes aprobaciones para el melanoma y el cáncer de pulmón de células no pequeñas.

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Área de la Ciencia:

  • Inmunología
  • En el campo de la oncología
  • Farmacología

Sus antecedentes:

  • Los anticuerpos monoclonales nivolumab y pembrolizumab se dirigen al receptor de la muerte programada-1 (PD-1).
  • El bloqueo del receptor PD-1 mejora las respuestas inmunes específicas del tumor.

Objetivo del estudio:

  • Para resumir el mecanismo y las recientes aprobaciones terapéuticas de los inhibidores de PD-1.
  • Para resaltar el papel del bloqueo PD-1 en el tratamiento del cáncer.

Principales métodos:

  • Revisión de la literatura científica sobre los inhibidores de la PD-1.
  • Análisis de los datos de los ensayos clínicos de nivolumab y pembrolizumab.

Principales resultados:

  • Nivolumab y pembrolizumab bloquean efectivamente el receptor PD-1.
  • Estos agentes desinhiben las respuestas inmunes antitumorales.

Conclusiones:

  • Nivolumab y pembrolizumab representan un avance significativo en la inmunoterapia contra el cáncer.
  • Las recientes aprobaciones para el melanoma metastásico y el cáncer de pulmón de células no pequeñas subrayan su utilidad clínica.