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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >The relevance of T-type calcium antagonists: a profile of mibefradil.
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The relevance of T-type calcium antagonists: a profile of mibefradil.

机译：T型钙拮抗剂的相关性：米贝拉地尔的概况。

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摘要

L- and T-type voltage-dependent transmembrane calcium channels are important for normal functioning of the cardiovascular system. T-type channels are a heterogeneous group, and have physiologic and pathophysiologic relevance in a number of organ systems, including the heart and central nervous system. They appear to be involved in the control of blood pressure in patients with essential hypertension and in protection from ischemic damage. Alterations of both L- and T-type calcium channels are involved in the development of hypertension. Pharmacologic modulation of T-type calcium channels appears to reduce membrane calcium flux and ameliorate hypertension. During early ischemic damage, T-type calcium channels appear to remain functional whereas L-type channels are already inactivated. T-type calcium channels also appear to be involved in the development of supraventricular arrhythmias, some forms of arrhythmias in cardiomyopathy, and cardiac hypertrophy. The heterogeneity of T-type calcium channels should make it possible to target drugs to specific subgroups of T-type calcium channels. A new class of calcium antagonist, the benzimidazolyl-substituted tetraline derivatives, has been shown to block both L- and T-type calcium channels. The first member of this class approved for clinical use is mibefradil. Clinical studies have demonstrated the efficacy of mibefradil in lowering blood pressure and as an antianginal and antiischemic agent. At clinically recommended doses, mibefradil has a heart rate lowering effect without a negative inotropic effect, and a favorable side effect profile. Because it is metabolized by the cytochrome P450 pathway, it should be used cautiously with other agents similarly metabolized.
机译：L型和T型电压依赖性跨膜钙通道对于心血管系统的正常功能很重要。 T型通道是一个异类，在许多器官系统（包括心脏和中枢神经系统）中具有生理和病理生理相关性。它们似乎参与了原发性高血压患者的血压控制和防止缺血性损伤。 L型和T型钙通道的改变都参与高血压的发展。 T型钙通道的药理学调节似乎减少了膜钙通量并改善了高血压。在早期缺血性损伤期间，T型钙通道似乎保持功能性，而L型通道已经失活。 T型钙通道似乎也参与了室上性心律失常，心肌病中某些形式的心律失常和心脏肥大。 T型钙通道的异质性应使其有可能将药物靶向T型钙通道的特定亚组。一种新型的钙拮抗剂，苯并咪唑基取代的四氢呋喃衍生物，已被证实可以阻断L型和T型钙通道。获准用于临床的该类别的第一名成员是米贝拉地尔。临床研究表明，米贝拉地尔可以降低血压并作为抗心绞痛和抗缺血药。在临床推荐剂量下，米贝拉地尔具有降低心率的作用，而无负性变力作用，并且副作用良好。由于它是通过细胞色素P450途径代谢的，因此应谨慎与其他类似代谢的药物一起使用。

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