Clinical Pharmacology of Long-Acting Calcium Antagonists

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Abstract
The pharmacologic goals of long-acting calcium (Ca) antagonists are to obtain effective drug concentrations with low interdose fluctuations and therefore a more efficacious hypotensive effect throughout the interval of administration, with a reduction in blood pressure variability. The therapeutic relevance of these pharmacologic properties could be more efficient prevention of target-organ damage (TOD) and improvement of treatment compliance. Because TOD seems to be more closely related to 24-h mean blood pressure and blood pressure variability, effective control of blood pressure throughout the entire dosage interval, with a concomitant reduction in blood pressure variability, may reduce TOD. However this hypothesis awaits validation in prospective studies. Long-acting Ca antagonists can improve medication compliance through the following mechanisms: a more favorable dosage schedule by avoidance of more than two doses daily during combination therapy and by allowing choice of timing of dosing; efficacy in reducing blood pressure, which can be assessed by the patients themselves; and reduction in incidence and severity of side effects. Lacidipine, a long-acting dihydropyridine Ca antagonist, when given at the dose of 4 mg once daily has a favorable trough:peak efficacy and reduces blood pressure variability. Moreover, compared with a shorter-acting dihydropyridine drug, lacidipine caused a lower incidence of adverse effects linked to vasodilation.

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