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Pharmacology: Felodipine is a dihydropyridine Class a calcium antagonist which lowers the arterial blood pressure by decreasing vascular resistance. In-vitro selectivity for smooth muscle in the arterioles is exhibited by Felodipine. In therapeutic doses, Felodipine has no direct effect on cardiac contractility. Felodipine does not affect venous smooth muscle or adrenergic vasomotor control.
It has been shown by electro-physiological studies that Felodipine has no direct effect on conduction in the specialized conducting system of the heart and has no effect on the AV nodal refractoriness.
Felodipine produces an increase in heart rate which is counteracted when concurrent beta receptor blockers are administered.
Pharmacokinetics: Felodipine is almost completely absorbed from the gastrointestinal tract after oral doses but undergoes extensive first-pass metabolism, with a bioavailability of about 15% (range 10 to 25%). It is extensively metabolized in the gut and the liver and is excreted almost entirely as metabolites, about 70% of a dose being excreted in urine and the remainder in feces. The terminal elimination half-life is reported to be about 11 to 16 hours after oral administration of an immediate-release preparation, but longer with a modified release formulation. Felodipine is about 99% bound to plasma proteins.
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