Pharmacology: Pharmacodynamics: Levamlodipine, the chirally pure form of Amlodipine is a calcium channel antagonist belonging to the dihydropyridine class. The S (-) isomer of Amlodipine is found to possess greater pharmacological effects than R (+) Amlodipine.
Levamlodipine is 1000 times more potent than the R (+) isomer binding to the dihydropyridine receptor. In humans, the dominant effects of Amlodipine are consequent to vasodilation. Levamlodipine lowers peripheral vascular resistance without causing reflex tachycardia. It is effective as a once daily dosage in the control of hypertension.
Pharmacokinetics and Metabolism: Administration of Levamlodipine 5 mg as a single dose in the fasting state produced maximum plasma concentration (Cmax) of 8.30±1.071 ng/mL in 2.73±0.88 hrs. (Tmax). Amlodipine is extensively (about 90%) converted to inactive metabolites via hepatic metabolism with 10% of the parent compound and 60% of the metabolites excreted in the urine. Ex-vivo studies have shown that approximately 93% of the circulating drug is bound to plasma proteins in hypertensive patients. The mean AUC0-t value (t=48 hrs.) of tablet S (-) Amlodipine (5 mg) is 95.33±14.45 ng.hr/mL. The AUC0-∞ value is recorded to be 140.91. Plasma elimination half life of S (-) Amlodipine has been found to be 31.09±12.65 hrs.
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