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The main mechanism of action of beta-blockers is to block the effects of adrenaline and noradrenaline on beta-adrenergic receptors. Beta-adrenergic receptors are found throughout the body, including in the heart, lungs, and blood vessels. By blocking these receptors, beta-blockers effectively reduce heart rate, decrease myocardial contractility, and lower blood pressure. This action helps manage various cardiovascular conditions, such as hypertension, angina, and heart failure.

In addition to their effects on the cardiovascular system, blocking beta receptors also has implications for other systems; for instance, it can reduce anxiety and migraines and manage certain forms of tremors. The selectivity of the beta-blocker for the different types of beta-receptors (beta-1, beta-2) is also crucial, influencing the specific clinical applications.

While reuptake inhibition of norepinephrine, insulin release stimulation, and potassium retention are all significant biochemical processes, they do not accurately describe the primary function of beta-blockers. Instead, the focus on blocking the action of adrenaline on the beta receptors directly aligns with the therapeutic effects of these medications.