Hypertensive patients can benefit from a new generation of calcium channel blockers.
Claudio Borghi
Abstract
Claudio Borghi
Abstract
Calcium channel blocker (CCB’s) are widely used for the treatment of hypertension (HTN) alone or in combination with first line antihypertensive drugs both in the general hypertensive population and in a wide range of patients. Between them Lercanidipine, a third-generation dihydropyridine calcium channel blocker, inhibits calcium entry through L-type calcium channels in smooth muscle cells of the cardiovascular system, leading to peripheral vasodilatation and so exerting its antihypertensive effect. It is a highly lipophilic drug and has a slower onset and longer duration of action than other dihydropyridines. Furthermore, the drug is highly vasoselective because of the high proportion of L-type calcium channels in arteries and has shown less in vitro and in vivo negative inotropic activity than some other dihydropyridines. Lercanidipine is also a well tolerated drug with a low adverse event rate due to its long-lasting and vasoselective calcium entry blocking activity, and does not cause sympathetic activation and reflex tachycardia. As a result, the overall adverse event rate is lower than that observed with other dihydropyridines. The efficacy of lercanidipine has been evaluated in both noncomparative and comparative studies with other calcium channel blockers and different antihypertensive drugs, showing comparable effects in all cases. Furthermore, Lercanidipine has a peculiar antioxidant and metabolic profile that might favorably interact with other antihypertensive drugs. Finally, in clinical trials lercanidipine have been demonstrated anti-atherosclerotic effects and left ventricular hypertrophy reduction.
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Calcium channel blocker (CCB’s) are widely used for the treatment of hypertension (HTN) alone or in combination with first line antihypertensive drugs both in the general hypertensive population and in a wide range of patients. Between them Lercanidipine, a third-generation dihydropyridine calcium channel blocker, inhibits calcium entry through L-type calcium channels in smooth muscle cells of the cardiovascular system, leading to peripheral vasodilatation and so exerting its antihypertensive effect. It is a highly lipophilic drug and has a slower onset and longer duration of action than other dihydropyridines. Furthermore, the drug is highly vasoselective because of the high proportion of L-type calcium channels in arteries and has shown less in vitro and in vivo negative inotropic activity than some other dihydropyridines. Lercanidipine is also a well tolerated drug with a low adverse event rate due to its long-lasting and vasoselective calcium entry blocking activity, and does not cause sympathetic activation and reflex tachycardia. As a result, the overall adverse event rate is lower than that observed with other dihydropyridines. The efficacy of lercanidipine has been evaluated in both noncomparative and comparative studies with other calcium channel blockers and different antihypertensive drugs, showing comparable effects in all cases. Furthermore, Lercanidipine has a peculiar antioxidant and metabolic profile that might favorably interact with other antihypertensive drugs. Finally, in clinical trials lercanidipine have been demonstrated anti-atherosclerotic effects and left ventricular hypertrophy reduction.
Key concepts: Calcium channel, Calcium, Channel (broadcasting), Medicine, Internal medicine, Cardiology, Computer science, Computer network