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地尔硫䓬。其药理特性与治疗效果综述。

Diltiazem. A review of its pharmacological properties and therapeutic efficacy.

作者信息

Chaffman M, Brogden R N

出版信息

Drugs. 1985 May;29(5):387-454. doi: 10.2165/00003495-198529050-00001.

DOI:10.2165/00003495-198529050-00001
PMID:3891302
Abstract

Diltiazem is an orally and intravenously active calcium channel blocking agent shown to be an effective and well-tolerated treatment for stable angina and angina due to coronary artery spasm. Its efficacy in these diseases has generally been similar to that of nifedipine or verapamil - alternative calcium channel blockers with which diltiazem has many electrophysiological, haemodynamic, and antiarrhythmic similarities. The antianginal mechanism of diltiazem cannot be precisely described; however, it appears to increase myocardial oxygen supply and decrease myocardial oxygen demand, mainly by coronary artery dilatation and/or via both direct and indirect haemodynamic alterations. Diltiazem has also shown substantial efficacy in the treatment of unstable angina, hypertension, and supraventricular tachyarrhythmias, but further study is necessary before its place in the treatment of these diseases may be clearly established. Although headache due to peripheral vasodilatation and depression of atrioventricular nodal conduction may be troublesome, side effects occur in only 2 to 10% of patients receiving diltiazem and are generally minor in nature. Thus, diltiazem offers a worthwhile alternative to other agents currently available for the treatment of angina pectoris. Although the infrequency of serious side effects may offer an advantage, its relative place in therapy compared with that of other calcium channel blockers remains to be clarified.

摘要

地尔硫䓬是一种口服和静脉给药均有效的钙通道阻滞剂,已被证明是治疗稳定型心绞痛和冠状动脉痉挛所致心绞痛的有效且耐受性良好的药物。它在这些疾病中的疗效通常与硝苯地平或维拉帕米相似,硝苯地平和维拉帕米是其他钙通道阻滞剂,地尔硫䓬与它们在许多电生理、血流动力学和抗心律失常方面具有相似性。地尔硫䓬的抗心绞痛机制尚不能精确描述;然而,它似乎主要通过冠状动脉扩张和/或直接和间接的血流动力学改变来增加心肌氧供并降低心肌氧需求。地尔硫䓬在治疗不稳定型心绞痛、高血压和室上性快速心律失常方面也显示出显著疗效,但在明确其在这些疾病治疗中的地位之前,还需要进一步研究。虽然外周血管扩张引起的头痛和房室结传导抑制可能会带来麻烦,但接受地尔硫䓬治疗的患者中只有2%至10%会出现副作用,且一般性质轻微。因此,地尔硫䓬为目前可用于治疗心绞痛的其他药物提供了一种有价值的替代选择。虽然严重副作用发生率低可能是一个优势,但其与其他钙通道阻滞剂相比在治疗中的相对地位仍有待明确。

相似文献

1
Diltiazem. A review of its pharmacological properties and therapeutic efficacy.地尔硫䓬。其药理特性与治疗效果综述。
Drugs. 1985 May;29(5):387-454. doi: 10.2165/00003495-198529050-00001.
2
Calcium-channel blocking agents.钙通道阻滞剂
Clin Pharm. 1982 Jan-Feb;1(1):17-33.
3
The use of diltiazem hydrochloride in cardiovascular disorders.
Pharmacotherapy. 1982 May-Jun;2(3):121-33. doi: 10.1002/j.1875-9114.1982.tb04518.x.
4
Calcium antagonism--with special reference to diltiazem.钙拮抗作用——特别提及地尔硫䓬
J Clin Hosp Pharm. 1986 Jun;11(3):159-74. doi: 10.1111/j.1365-2710.1986.tb00841.x.
5
Comparative pharmacology of calcium antagonists: nifedipine, verapamil and diltiazem.钙拮抗剂的比较药理学:硝苯地平、维拉帕米和地尔硫䓬。
Am J Cardiol. 1980 Dec 1;46(6):1047-58. doi: 10.1016/0002-9149(80)90366-5.
6
The haemodynamic effects of nifedipine, verapamil and diltiazem in patients with coronary artery disease. A review.硝苯地平、维拉帕米和地尔硫䓬对冠心病患者的血流动力学影响。综述。
Drugs. 1986 Jul;32(1):66-101. doi: 10.2165/00003495-198632010-00004.
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Diltiazem. A reappraisal of its pharmacological properties and therapeutic use.地尔硫䓬。对其药理特性和治疗用途的重新评估。
Drugs. 1990 May;39(5):757-806. doi: 10.2165/00003495-199039050-00009.
8
Haemodynamic and electrophysiologic effects of diltiazem.地尔硫䓬的血流动力学和电生理效应。
Acta Pharmacol Toxicol (Copenh). 1985;57 Suppl 2:21-30. doi: 10.1111/j.1600-0773.1985.tb03571.x.
9
Haemodynamic effects of intravenous diltiazem at rest and exercise in patients with coronary artery disease.
Eur Heart J. 1984 Jun;5(6):456-63. doi: 10.1093/oxfordjournals.eurheartj.a061691.
10
[Dilzem - a new calcium antagonist is introduced].[地尔硫䓬——一种新型钙拮抗剂被引入]
ZFA (Stuttgart). 1982 Feb 20;58(5):292-6.

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Comparative effects of three calcium antagonists, diltiazem, verapamil and nifedipine, on the sinoatrial and atrioventricular nodes. Experimental and clinical studies.三种钙拮抗剂(地尔硫䓬、维拉帕米和硝苯地平)对窦房结和房室结的比较作用。实验与临床研究。
Circulation. 1981 May;63(5):1035-42. doi: 10.1161/01.cir.63.5.1035.
2
Haemodynamic effects of diltiazem in healthy volunteers.地尔硫䓬对健康志愿者的血流动力学影响。
Br J Clin Pharmacol. 1980 Dec;10(6):623-4. doi: 10.1111/j.1365-2125.1980.tb00522.x.
3
Diltiazem actions on smooth muscle cells of the porcine coronary artery and on neuromuscular junctions of the guinea-pig vas deferens.
Lipid Horizons: Recent Advances and Future Prospects in LBDDS for Oral Administration of Antihypertensive Agents.
脂质前沿:用于口服抗高血压药物的脂质体药物递送系统的最新进展与未来前景
Int J Hypertens. 2024 Feb 19;2024:2430147. doi: 10.1155/2024/2430147. eCollection 2024.
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Pregnancy Arrhythmias: Management in the Emergency Department and Critical Care.妊娠心律失常:急诊科及重症监护中的管理
J Clin Med. 2024 Feb 15;13(4):1095. doi: 10.3390/jcm13041095.
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Antioxidant and Anti-Inflammatory Properties of Quail Yolk Oil via Upregulation of Superoxide Dismutase 1 and Catalase Genes and Downregulation of EIGER and Unpaired 2 Genes in a Model.鹌鹑蛋黄油通过上调超氧化物歧化酶1和过氧化氢酶基因以及下调模型中的EIGER和未配对2基因所具有的抗氧化和抗炎特性
Antioxidants (Basel). 2024 Jan 5;13(1):75. doi: 10.3390/antiox13010075.
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Repurposing Diltiazem for Its Neuroprotective Anti-Dementia Role against Intra-Cerebroventricular Streptozotocin-Induced Sporadic Alzheimer's Disease-Type Rat Model.将地尔硫䓬重新用于其对脑室内注射链脲佐菌素诱导的散发性阿尔茨海默病型大鼠模型的神经保护抗痴呆作用。
Life (Basel). 2023 Aug 4;13(8):1688. doi: 10.3390/life13081688.
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Pharmacological interventions for preventing atrial fibrillation after lung surgery: systematic review and meta-analysis.肺手术后预防心房颤动的药物干预:系统评价和荟萃分析。
Eur J Clin Pharmacol. 2022 Nov;78(11):1777-1790. doi: 10.1007/s00228-022-03383-2. Epub 2022 Sep 22.
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Synthesis of Novel 2,3-Dihydro-1,5-Benzothiazepines as α-Glucosidase Inhibitors: , , Kinetic, SAR, Molecular Docking, and QSAR Studies.新型2,3-二氢-1,5-苯并硫氮杂䓬类α-葡萄糖苷酶抑制剂的合成:动力学、构效关系、分子对接及定量构效关系研究
ACS Omega. 2022 Aug 17;7(34):30215-30232. doi: 10.1021/acsomega.2c03328. eCollection 2022 Aug 30.
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1,5-Benzothiazepine Derivatives: Green Synthesis, In Silico and In Vitro Evaluation as Anticancer Agents.1,5-苯并硫氮杂卓衍生物的绿色合成、计算机模拟和体外评估作为抗癌剂。
Molecules. 2022 Jun 10;27(12):3757. doi: 10.3390/molecules27123757.
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Diltiazem inhibits SARS-CoV-2 cell attachment and internalization and decreases the viral infection in mouse lung.地尔硫䓬抑制 SARS-CoV-2 细胞附着和内化,并减少小鼠肺部的病毒感染。
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地尔硫䓬对猪冠状动脉平滑肌细胞及豚鼠输精管神经肌肉接头的作用。
Gen Pharmacol. 1980;11(6):561-8. doi: 10.1016/0306-3623(80)90091-9.
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Verapamil disposition in liver disease and intensive-care patients: kinetics, clearance, and apparent blood flow relationships.
Clin Pharmacol Ther. 1981 Jan;29(1):27-34. doi: 10.1038/clpt.1981.5.
5
Improved exercise performance in persons with stable angina pectoris receiving diltiazem.接受地尔硫䓬治疗的稳定型心绞痛患者运动表现改善。
Am J Cardiol. 1981 Jan;47(1):95-101. doi: 10.1016/0002-9149(81)90296-4.
6
Electrophysiologic effects of diltiazem, a calcium antagonist, in patients with impaired sinus or atrioventricular node function.
Angiology. 1980 Oct;31(10):700-9. doi: 10.1177/000331978003101006.
7
Improved performance of ischemic canine myocardium in response to nifedipine and diltiazem.硝苯地平和地尔硫䓬对缺血犬心肌的作用增强。
Am J Physiol. 1980 Nov;239(5):H658-63. doi: 10.1152/ajpheart.1980.239.5.H658.
8
Effects of intravenous and chronic oral verapamil administration in patients with supraventricular tachyarrhythmias.静脉注射和长期口服维拉帕米对室上性快速心律失常患者的影响。
Circulation. 1980 Nov;62(5):996-1010. doi: 10.1161/01.cir.62.5.996.
9
Effects of nifedipine, diltiazem and verapamil on the vasoconstrictor responses to norepinephrine and potassium ions in the rat mesenteric artery.硝苯地平、地尔硫䓬和维拉帕米对大鼠肠系膜动脉去甲肾上腺素和钾离子血管收缩反应的影响。
Arch Int Pharmacodyn Ther. 1980 Jun;245(2):211-7.
10
Protective effect of pretreatment with verapamil, nifedipine and propranolol on mitochondrial function in the ischemic and reperfused myocardium.维拉帕米、硝苯地平及普萘洛尔预处理对缺血再灌注心肌线粒体功能的保护作用。
Am J Cardiol. 1980 Aug;46(2):242-8. doi: 10.1016/0002-9149(80)90064-8.