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Review Article
- Calcium channel blockers for hypertension: old, but still useful
- Eun Mi Lee
- Cardiovasc Prev Pharmacother. 2023;5(4):113-125. Published online October 30, 2023
- DOI: https://doi.org/10.36011/cpp.2023.5.e16
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- 2 Citations
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Abstract
PDF - Calcium channel blockers (CCBs) constitute a heterogeneous class of drugs that can be divided into dihydropyridines (DHPs) and non-DHPs. DHP-CCBs are subcategorized into four generations based on the duration of activity and pharmacokinetics, while non-DHP-CCBs are subcategorized into phenylethylamine and benzodiazepine derivatives. DHP-CCBs are vascular-selective and function as potent vasodilators, whereas non-DHP-CCBs are cardiac-selective and are useful for treating tachyarrhythmia, but reduce cardiac contractility and heart rate. Traditional DHP-CCBs (nifedipine) mainly block L-type calcium channels, whereas novel CCBs block N-type (amlodipine) and/or T-type channels (efonidipine) in addition to L-type channels, leading to organ-protective effects. DHP-CCBs have a potent blood pressure–lowering effect and suppress atherosclerosis and coronary vasospasm. Diltiazem, a non-DHP-CCB, is highly effective for vasospasm control. CCBs reduce left ventricular hypertrophy and arterial stiffness. Amlodipine, a DHP-CCB, reduces blood pressure variability. L/N- and L/T-type CCBs combined with renin-angiotensin system blockers reduce proteinuria and improve kidney function compared with L-type CCBs. According to large-scale trials, DHP-CCBs reduce cardiovascular events in patients with isolated systolic hypertension, as well as in elderly and high-risk patients. Accordingly, CCBs are indicated for hypertension in elderly patients, isolated systolic hypertension, angina pectoris, and coronary vasospasm. Non-DHP-CCBs are contraindicated in high-grade heart block, bradycardia (<60 beats per minute [bpm]), and heart failure with reduced ejection fraction (HFrEF). DHP-CCBs should be used with caution in patients with tachyarrhythmia, HFrEF, and severe leg edema, and non-DHP-CCBs should be used carefully in those with constipation. Each CCB has distinct pharmacokinetics and side effects, underscoring the need for meticulous consideration in clinical practice.
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Citations
Citations to this article as recorded by
- Design of Experimental Approach for Development of Rapid High Performance Liquid Chromatographic Process for Simultaneous Estimation of Metoprolol, Telmisartan, and Amlodipine from Formulation: Greenness and Whiteness Evaluation
Mahesh Attimarad, Mohammed Jassim Alali, Hussain Ali Alali, Dana Hisham Alabdulmuhsin, Aljohara Khalid Alnajdi, Katharigatta Narayanaswamy Venugopala, Anroop B. Nair
Molecules.2024; 29(5): 1087. CrossRef - The Evolving Role of Calcium Channel Blockers in Hypertension Management: Pharmacological and Clinical Considerations
Kamryn E. Jones, Shaun L. Hayden, Hannah R. Meyer, Jillian L. Sandoz, William H. Arata, Kylie Dufrene, Corrado Ballaera, Yair Lopez Torres, Patricia Griffin, Adam M. Kaye, Sahar Shekoohi, Alan D. Kaye
Current Issues in Molecular Biology.2024; 46(7): 6315. CrossRef
- Design of Experimental Approach for Development of Rapid High Performance Liquid Chromatographic Process for Simultaneous Estimation of Metoprolol, Telmisartan, and Amlodipine from Formulation: Greenness and Whiteness Evaluation
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