血管舒张药的临床药物动力学。我一部分。

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克里斯汀•R,纳尔逊·K,克里斯汀•D, Heintz B

血管舒张药的临床药物动力学。我一部分。

Pharmacokinet。1998年6月,34 (6):457 - 82。

PubMed ID
9646008 (在PubMed
]
文摘

了解行动的机制,通过药物的药代动力学性质有助于优化在临床实践中使用。它应该记住一个药物属于一个类,但一个不同的实体,有时来自一个原型来实现一个特定的效果。最常见的药物药代动力学改进是开发一种药物的半衰期足够长的允许足够的每日一次剂量。开发一种控释制剂可以增加药物的半衰期明显。改变分子结构也可能增加原型药物的半衰期。另一个理想的改进是增加药物的特异性,这可能导致更少的副作用,或更多的功效在目标站点。这通过药物可能尤其重要管理几十年来治疗高血压,通常不影响主观幸福感。遵从性大大增加了每日一次给药。通过引起放松通过胞质钙减少,增加一氧化氮(NO)或通过抑制肌球蛋白轻链激酶。他们分为9类:钙拮抗剂,钾离子通道打开,血管紧张素转换酶抑制剂、血管紧张素ⅱ受体拮抗剂,者和咪唑受体拮抗剂,β1-adrenergic受体激动剂,磷酸二酯酶抑制剂、二十烷类和捐助者。 Despite chemical differences, the pharmacokinetic properties of calcium antagonists are similar. Absorption from the gastrointestinal tract is high, with all substances undergoing considerable first-pass metabolism by the liver, resulting in low bioavailability and pronounced individual variation in pharmacokinetics. Renal impairment has little effect on pharmacokinetics since renal elimination of these agents is minimal. Except for the newer drugs of the dihydropyridine type, amlodipine, felodipine, isradipine, nilvadipine, nisoldipine and nitrendipine, the half-life of calcium antagonists is short. Maintaining an effective drug concentration for the remainder of these agents requires multiple daily dosing, in some cases even with controlled release formulations. However, a coat-core preparation of nifedipine has been developed to allow once-daily administration. Adverse effects are directly correlated to the potency of the individual calcium antagonists. Treatment with the potassium channel opener minoxidil is reserved for patients with moderately severe to severe hypertension which is refractory to other treatment. Diazoxide and hydralazine are chiefly used to treat severe hypertensive emergencies, primary pulmonary and malignant hypertension and in severe preeclampsia. ACE inhibitors prevent conversion of angiotensin-I to angiotensin-II and are most effective when renin production is increased. Since ACE is identical to kininase-II, which inactivates the potent endogenous vasodilator bradykinin, ACE inhibition causes a reduction in bradykinin degradation. ACE inhibitors exert cardioprotective and cardioreparative effects by preventing and reversing cardiac fibrosis and ventricular hypertrophy in animal models. The predominant elimination pathway of most ACE inhibitors is via renal excretion. Therefore, renal impairment is associated with reduced elimination and a dosage reduction of 25 to 50% is recommended in patients with moderate to severe renal impairment. Separating angiotensin-II inhibition from bradykinin potentiation has been the goal in developing angiotensin-II receptor antagonists. The incidence of adverse effects of such an agent, losartan, is comparable to that encountered with placebo treatment, and the troublesome cough associated with ACE inhibitors is absent.

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药物
药物靶点
药物 目标 类 生物 药理作用 行动
米诺地尔 ATP-sensitive内向整流钾通道1 蛋白质 人类
是的
诱导物
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