钙通道阻滞剂的临床应用

钙通道阻滞剂是一种选择性阻滞细胞上慢通道(钙通道)抑制电位依赖性钙离子向细胞内流入的药物。它可使平滑机松弛,心肌收缩减弱和冠状动脉张力降低而发挥临床治疗作用。从作为降压和冠心病治疗药物开始迄今,又有新的发展。     

钙通道阻滞剂的临床应用

为促进临床合理用药，全面阐述钙通道阻滞剂的药理，化学结构，深入探讨钙通道阻滞剂的临床应用，指出该类药物不仅是心血管病重要而常用的治疗药物，而且目前其治疗范围已延伸至其他领域。     

钙通道阻滞剂的临床应用

钙通道阻滞剂(CCB)能阻滞钙离子进入细胞内,引起各组织系统的平滑肌松弛,减轻缺血性细胞中毒。CCB在结构上主要分四类:二氢吡啶类、硫氮(艹卓)酮类、异搏定类、氟桂嗪类。 二氢吡啶类常用的有非洛地平(波依定)、尼索地平、硝苯地平、尼莫地平、氨氯地平(络活喜)、尼群地平等。硫氮(艹卓)酮类有地尔硫(艹卓)(恬尔心)等。维拉帕米类有维拉帕米(异搏定)等。氟桂嗪类有氟桂利嗪(西比灵)等。 本文对CCB的应用作一概述。 1 治疗心肌缺血和心绞痛 短期急性心肌缺血会导致代谢紊乱,包括ATP耗竭,细胞外钾离子积聚,细胞内钠离子积聚而失去细胞内对钙离子转运的正常机制,结果增加了细胞内钙离子的水平,厌氧代谢变成需氧代谢,糖原贮存被耗竭,伴酸中毒和线粒体     

钙通道阻滞剂在心血管系统的临床应用

本文对钙通道阻滞剂在抗高血压，抗心绞痛、抗心律失常及抗心衰和改善左室功能等方面的临床应用机理及疗效作了评述。     

T型钙通道阻滞剂的临床应用进展

T型钙通道是一种低电压钙通道,在体内分布广泛,参与多种生理过程。T型钙通道阻滞剂是目前关注较多的一种新型钙通道阻滞剂,除具备与传统钙通道阻滞剂相似的降压作用外,还具有如降低心肌自律性、抗心肌重塑、保护肾功能、抗交感神经等药理作用。对T型钙通道阻滞剂的药理作用、药物相互作用与不良反应等研究进展进行综述,从而了解T型钙通道阻滞剂在临床实践中的应用现状,探索和开发其在临床实践中的新使用价值。     

钙通道阻滞剂临床应用进展

钙通道阻滞剂（calcium channel blockers,CCB）又称Ca^2＋拮抗剂，是药理学、化学结构、生理作用和临床应用呈多样性的～组药物，是心血管病药物治疗学发展中继B受体阻滞剂后的又一个具有重要地位的药物。CCB不仅是治疗心血管病重要而常用的药物之一，目前其治疗范围又扩增至其他领域．现将其临床应用进展综述如下。     

钙通道阻滞剂对血管平滑肌的作用机制与临床应用

目的：评价钙通道阻滞剂（calcium channel blockers,CCB）的临床疗效及安全性,以供临床医师合理用药参考。方法：根据国内、外近期有关CCB的试验结果和文献进行评价、分析。结果：CCB已成为治疗心血管疾病的基本药物之一,特别是在抗高血压方面尤为突出。结论：钙通道阻滞剂对血管平滑肌、支气管平滑肌、泌尿道平滑肌、子宫平滑肌、胆道平滑肌有明显的作用,在临床上有着广泛的应用前景。     

临床应用二氢吡啶类钙通道阻滞剂的循证医学评价

目的：评价二氢吡啶类钙通道阻滞剂（DHP—CCB）的临床应用进展,及其有效性和安全性。方法：搜集DHP—CCB临床应用相关的系统评价及大规模临床对照研究,对DHP—CCB和安慰剂或者其它药物进行比较,评价其有效性和安全性。结果：共检索到3项大型临床研究和20项系统评价,对DHP—CCB应用于高血压、心绞痛、蛛网膜下腔出血、抑制分娩等症状的有效性和安全性进行评价。结论：DHP—CCB在控制收缩压和舒张压上和其它药物效果相同,与其它降压药合用,效果和安全性更好。在老年单纯收缩期高血压患者,应用DHP—CCB明显降低肾功能不全和痴呆。DHP—CCB与β-受体阻滞剂合用于冠心病患者中,效果和安全性更好。DHP—CCB能够改善蛛网膜下腔出血预后。在抑制分娩中,DHP—CCB较其它抑制分娩药更有效,安全性更好。DHP—CCB应用于缺血性卒中的安全性和有效性尚待进一步的临床数据证实。     

二氢吡啶类钙通道阻滞剂控制血压的临床评价

目的:阐述二氢吡啶类钙通道阻滞剂的进展和临床应用的历程,评价其疗效与安全性.方法:查阅近期国内外相关文献进行评价与分析.结果与结论:二氢吡啶类钙通道阻滞剂近年来进展迅猛,已成为治疗心血管疾病的基本药物之一,尤其在对抗高血压上效果突出,已被多项应用循证医学方法的临床研究所证实.     

Pharmacodynamic Profiles of Different Calcium Channel Blockers

Abstract: The cardiovascular effects of different calcium channel blockers (CCB), exemplified by nifedipine, verapamil and diltiazem, are not identical. Some of these differences in effect may be due to the different CCBs interacting with different calcium channel subtypes in the tissues, and/or that the drug-receptor sites are separate. The drugs also have different abilities to activate the sympathetic nervous system, nifedipine increasing and diltiazem decreasing the baroreflex sensitivity. Verapamil, but not nifedipine and diltiazem, has a postjunctional α-adrenoceptor blocking effect, and can also increase the release of noradrenaline from adrenergic nerves by blocking pre-junctional α-adrenoceptors. In addition, verapamil may have a reserpine-like action on sympathetic nerves. The vasodilator actions of CCBs are not uniform, but seem to vary between species, different vascular regions, and different agents. Mechanisms other than blockade of influx of calcium from the extracellular medium have been suggested to explain these differences, including inhibition of intracellular calcium release, blockade of postjunctional α – adrenoceptors, interaction with calmodulin, inhibition of cyclic AMP phosphodiesterase, stimulation of Na⁺ –, K⁺ -activated ATPase, stimulation of a calcium pump, and a direct interaction with the contractile proteins. The heterogeneity in pharmacodynamic profile characterizing the CCBs is conspicuous, and may be of importance when selecting agents for the treatment of various cardiovascular and non-cardiovascular disorders.     

钙离子拮抗剂类降压药的临床应用及不良反应

目的 对钙离子拮抗剂在临床中的临床应用及不良反应做系统的分析,总结钙离子拮抗剂在临床中的应用及注意事项,为药师在临床用药监测中提供了理论支持。方法 通过查阅文献的方式,系统学习钙离子拮抗剂的临床应用及不良反应。结果 钙离子拮抗剂广泛应用于心血管等多种疾病,其不良反应有心律失常、低血压、房室传导阻滞、心力衰竭、牙龈增生、外周水肿、便秘等。药物使用应关注其常见和罕见的不良反应,促进合理用药。结论 药物在使用过程中,不仅要注重药物的药理作用及临床疗效,最好在使用之前就预见药物的不良反应,才能做到及时防治,最大地发挥药物疗效。     

钙通道阻滞剂治疗220例高血压的临床体会

目的考察钙通道阻滞剂对高血压的临床治疗效果。方法将220例高血压患者随机分为观察组和对照组各110例,观察组采用非洛地平缓释片进行治疗,对照组采用硝苯地平片进行治疗。结果两组治疗后的SBP和DBP均优于较治疗前有显著改善(P<0.05),且观察组SBP和DBP下降程度明显低于对照组(P<0.05);总有效率观察组为91.82%,对照组为78.18%,比较具统计学意义(P<0.05);不良反应发生率观察组为5.5%,对照组为13.64%,观察组显著优于对照组(P<0.05)。结论非洛地平缓释片治疗高血压疗效理想,安全可靠,值得在临床中推广应用。     

Effects of Calcium Channel Blockers on the Female Genital Tract

Abstract: Contractile activity and vascular resistance in the female genital tract are influenced by several smooth muscle tissues with individual mechanisms for control of mechanical activation. Calcium channel blockers have potent relaxant effects on preparations of human myometrium. The myometrial arteries utilize multiple sources of calcium for contractile activation, and excitation-contraction coupling in isolated vessels from non-pregnant uteri seems comparatively less sensitive to nifedipine than in corresponding myometrial preparations. Contractile activation of myometrial and placental arteries at term is inhibited by nitrendipine and nifedipine. Human oviductal smooth muscle depends on superficially bound calcium for mechanical activation, but only phasic contractions can be abolished by nifedipine, while tonic contractions induced by various agents are more resistant to the calcium channel blocker. Menstrual uterine contractions and pain are effectively counteracted by nifedipine in normal and dysmenorrhoeic women. Such therapy may represent an alternative principle in the treatment of dysmenorrhea. Nifedipine has potent relaxant effects on the mid-term pregnant and the post-partum uterus and calcium channel blockers may prove useful in the treatment of premature labor. Nifedipine and related compounds may further show effective in the treatment of pregnancy-associated hypertension. Whether such treatment in late pregnancy involves maintained or even improved placental perfusion could be assumed from in vitro data but needs further studies.     

Immunosuppressive Properties of Calcium Channel Blockers

Calcium channel blockers are extensively used for their beneficial effects on the cardiovascular system. Solid organ transplant recipients commonly have cardiovascular disease and are often treated with these agents. Research demonstrates that calcium antagonists may have beneficial effects in this population that are independent of their effects on the cardiovascular system. Indeed, both in vitro and in vivo studies suggested that they may possess immunosuppressive properties. Their actions at the cellular level in both the afferent and efferent arms of the immune system indicate that alone, as well as in combination with cyclosporine, these agents possess immunosuppressive properties that may potentially benefit the transplant population.     

Migraine Treatment with Calcium Channel Blockers

Abstract: Irrespective of their mechanism of action, which so far has not been clarified, calcium channel blockers (CCBs) have a documented prophylactic effect on classical and common migraine, as well as on cluster headache. The drugs may reduce migraine prodromes, the frequency of migraine attacks, and also decrease the severity and possibly the duration of these attacks. Notably, their optimum effect is often seen after more than 2 months of treatment. Side effects seem to be few and mild. Whether or not there are differences in therapeutic efficacy between different CCBs is presently unclear. As comparisons with other alternatives of treatment are sparse, the place of CCBs in migraine therapy remains to be established.     

Calcium Channel Blockers and Pulmonary Hypertension

Abstract: In vascular smooth muscle from the pulmonary circulation, potassium evoked contractions are abolished in calcium-free medium and by calcium channel blockers (CCB). Noradrenaline, histamine, and serotonin induced contractions are partly resistant. Pulmonary arterial hypertension may occur both as a primary disorder and secondary to cardiac and pulmonary diseases; in both types there may be a component of pulmonary arterial vasoconstriction. In animal models, hypoxic pulmonary hypertension is counteracted by CCBs, nifedipine being particular effective. In patients with this disorder, CCBs also seem able to lower pulmonary arterial pressure and vascular resistance, but no controlled trials documenting their clinical efficacy have been performed. This is valid also for primary pulmonary hypertension, where some of the CCBs may have clinical value.     

口服钙通道阻滞剂的应用分析

目的 了解口服钙通道阻滞剂应用现状和发展趋势.方法 对2004年至2007年本院口服钙通道阻滞剂消耗品种、金额、用药频度(DDDs)进行统计分析.结果 口服钙通道阻滞剂的用药金额和DDDs值呈逐渐增长趋势.金额年平均增长率为6.79%、4.74%和30.66%,DDDs的增长率为7.48%、6.39%和30.46%.用药金额前3名依次为苯磺酸氨氯地平(络活喜)、非洛地平缓释片(波依定)、硝苯地平控释片(拜新同).结论 使用口服钙通道阻滞剂的结构和层次比较合理,符合我国目前口服钙通道阻滞剂的发展现状.     

集中带量采购政策下江西省口服二氢吡啶类钙离子通道阻滞剂药品临床综合评价专家共识

目的 开展口服二氢吡啶类钙离子通道阻滞剂的临床综合评价,为医疗机构降压药物的合理使用提供参考依据。方法 由南昌大学第二附属医院牵头,以江西省研究型医院学会及江西省药学会为依托,江西省25家三级甲等医院共同参与,运用文献综述及德尔菲法,通过项目启动、初稿形成后的2轮专题修订会研讨及1轮电子版反馈,最终制定本共识。结果 截至2022年2月,已纳入国家集中带量采购的钙离子通道阻滞剂2个。该共识采用百分制,从有效性、安全性、经济学、适宜性、可及性和创新性共6个维度,对涉及的10个钙离子通道阻滞剂进行了临床综合评价,并根据分值形成不同的推荐级别。结论 制定了《集中带量采购政策下江西省口服二氢吡啶类钙离子通道阻滞剂药品临床综合评价共识》,为国家和省级集中带量采购的约定采购量调整提供参考,同时也为医疗结构药品配备和采购目录的制定,药品科学化和精细化管理提供理论依据。