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Talinolol is a long-acting, highly selective β1-adrenergic receptor antagonist (beta blocker) primarily used for the management of hypertension, angina pectoris, and various cardiac arrhythmias. By selectively blocking β1-adrenergic receptors in the heart, it reduces heart rate and contractility, delays AV node conduction, and diminishes the effects of catecholamines during physical or emotional stress. This results in decreased blood pressure and reduced frequency/severity of angina attacks. Talinolol has minimal activity at β2 receptors at therapeutic doses and lacks partial agonist activity or membrane-stabilizing effects. It is rapidly absorbed orally but has moderate bioavailability due to P-glycoprotein-mediated efflux; most of the drug is excreted unchanged in urine. Its half-life (~12 hours) allows for once-daily dosing. Talinolol also exhibits antioxidant properties and is sometimes used as a probe substrate for P-glycoprotein function in pharmacokinetic studies[1][5][6].
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