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Pharmacology: Pharmacodynamics: Mechanism of Action: Amlodipine inhibits calcium ion from entering the "slow channels" or selected voltage-sensitive areas of vascular smooth muscle and myocardium during depolarization, producing a relaxation of coronary vascular smooth muscle and coronary vasodilation; increases myocardial oxygen delivery in patients with vasospastic angina.
Pharmacokinetics: Amlodipine is well absorbed after oral doses with peak blood concentrations occurring after 6 to 12 hours. The bioavailability varies but is usually about 60 to 65%. Amlodipine is reported to be about 97.5% bound to plasma proteins. It has a prolonged terminal elimination half-life of 35 to 50 hours and steady-state plasma concentrations are not achieved until after 7 to 8 days of use. Amlodipine is extensively metabolised in the liver; metabolites are mostly excreted in urine together with less than 10% of a dose as unchanged drug. Amlodipine is not removed by dialysis.
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