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1、Nifedipine,Hypertension,e.g. 50 millions Americans have hypertension.,Incidence: 10-20% in adults,* Effects of all types of calcium blockers is the inhibition of the L-calcium current in arterial smooth muscle,CCBs,* Verapamil, the first clinical useful drug of calcium channel blockers,* Nifidipine,
2、 the most extensively studied of this group,* Diltiazem, very popular and available worldwide,Hypertension,Mechanism of action: blocking L-type calcium channelOrgan system effect: relaxing smooth muscle (VSM most sensitive); reducing cardiac contractility or decreasing cardiac output;,BP= CO x PVR,A
3、ngia,The mechanism of action is not understood Relaxation and prevention of coronary artery spasm (放松和预防冠状动脉痉挛) Ruduction of Oxygen Utilization,硝苯地平,Pharmacokinetics:half-life 2h ER 7horally active agents, high first-pass effect, high plasma protein binding, and extensive metabolism,Metabolism,Nifed
4、ipine is extensively metabolized to highly water-soluble, inactive metabolites accounting for 60 to 80% of the dose excreted in the urine. The elimination half-life of nifedipine is approximately two hours. Only traces (less than 0.1% of the dose) of unchanged form can be detected in the urine. The remainder is excreted in the feces in metabolized form, most likely as a result of biliary excretion.,Reference,1The Art Of Drug Synthesis Author:Douglas S.Johnson Jie Jack LI 2007 2Nifedical XL Prescribing Information(FDA),End !,
