Frohlich E D
Alton Ochsner Medical Foundation, New Orleans, LA 70121.
Am J Hypertens. 1991 Jul;4(7 Pt 2):430S-433S. doi: 10.1093/ajh/4.7.430s.
Most symposia concerned with the therapeutic roles of calcium antagonists first emphasize their extreme structural, chemical, and pharmacological heterogeneity. However, following these considerations, clinical discussions usually suggest that these agents are clinically and physiologically similar. Thus, investigators acknowledge greater vasodilating and hypotensive capabilities of one or another compound and rank these potencies clinically, emphasizing similar physiological actions on the target organs of hypertensive disease. This discussion concerns differences among these agents with respect to their cardiovascular and renal effects. Although most calcium antagonists are potent vasodilators, and reduce arterial pressure through a fall in total peripheral resistance, not all have this general effect. For example, nimodipine has little antihypertensive effectiveness; it is used as a cerebrovascular vasodilator. Certain agents may have greater negative chronotropic and inotropic cardiac effects; others may be devoid of these actions and, in fact, may be associated only with reflex cardiac stimulation. Thus, verapamil has great negative chronotropic effects--it was approved initially for this action--and inotropic effects; nifedipine is at the other extreme, while diltiazem is moderate. Most of these compounds reduce cardiac mass, but they may not produce only left ventricular mass reduction. Recent experimental studies show a contemporaneous increase in right ventricular mass. Finally, whereas most of these compounds reduce renal vascular resistance, some, such as diltiazem, nitrendipine, and clindiazem increase renal blood flow while reducing glomerular hydrostatic pressure. These effects may relate to their ability to diminish proteinuria, which suggests potential for reversing hypertensive and diabetic nephropathy. Thus, the calcium antagonists are far more heterogeneous than other classes of antihypertensive agents in their physiological and clinical actions.(ABSTRACT TRUNCATED AT 250 WORDS)
大多数关于钙拮抗剂治疗作用的研讨会首先强调其在结构、化学和药理学方面存在极大的异质性。然而，在考虑这些因素之后，临床讨论通常表明这些药物在临床和生理方面具有相似性。因此，研究人员认可某一种或另一种化合物具有更强的血管舒张和降压能力，并在临床上对这些效能进行排序，强调它们对高血压疾病靶器官具有相似的生理作用。本讨论涉及这些药物在心血管和肾脏效应方面的差异。虽然大多数钙拮抗剂是强效血管舒张剂，并通过降低总外周阻力来降低动脉血压，但并非所有药物都有这种普遍作用。例如，尼莫地平几乎没有降压效果；它被用作脑血管舒张剂。某些药物可能具有更强的负性变时性和变力性心脏效应；其他药物可能没有这些作用，事实上，可能仅与反射性心脏刺激有关。因此，维拉帕米具有很强的负性变时性作用——它最初就是因这一作用而获批——以及变力性作用；硝苯地平则处于另一个极端，而地尔硫䓬的作用适中。这些化合物大多可减轻心脏重量，但它们可能并非只减轻左心室重量。最近的实验研究表明，右心室重量会同时增加。最后，虽然这些化合物大多可降低肾血管阻力，但有些药物，如地尔硫䓬、尼群地平和克林地尔，在降低肾小球静水压的同时会增加肾血流量。这些效应可能与其减少蛋白尿的能力有关，这表明它们具有逆转高血压和糖尿病肾病的潜力。因此，钙拮抗剂在生理和临床作用方面比其他类别的抗高血压药物具有更大的异质性。（摘要截选至250词）
