Prescribing information for norvasc amlodipine .
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Extensively metabolized by livertitrate dose slowly with severe hepatic impairment.
Amlodipine is a dihydropyridine calcium antagonistcalcium ion antagonist or slow-channel blockerthat inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscleExperimental data suggest that amlodipine binds to both dihydropyridine and nondihydropyridine binding sitesThe contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channelsAmlodipine inhibits calcium ion influx across cell membranes selectivelywith a greater effect on vascular smooth muscle cells than on cardiac muscle cellsNegative inotropic effects can be detected in vitro but such effects have not been seen in intact animals at therapeutic dosesSerum calcium concentration is not affected by amlodipineWithin the physiologic pH rangeamlodipine is an ionized compoundpKa=8.6and its kinetic interaction with the calcium channel receptor is characterized by a gradual rate of association and dissociation with the receptor binding siteresulting in a gradual onset of effect.
Worsening of angina and acute myocardial infarctionMIcan develop after dose is started or increasedparticularly with severe obstructive CAD.
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