Search
- Page Path
- HOME > Search
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
- 65,535 View
- 2,452 Download
- 21 Citations
-
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.
-
Citations
Citations to this article as recorded by
- Home blood pressure-lowering effect of esaxerenone versus trichlormethiazide for uncontrolled hypertension: a predefined subanalysis of the EXCITE-HT randomized controlled trial by basal calcium channel blocker versus angiotensin receptor blocker
Kazuomi Kario, Hiroyuki Ohbayashi, Masami Hashimoto, Naoki Itabashi, Mitsutoshi Kato, Kazuaki Uchiyama, Kunio Hirano, Noriko Nakamura, Takahide Miyamoto, Hirotaka Nagashima, Hidenori Ishida, Yusuke Ebe, Tsuguru Hatta, Toshiki Fukui, Tatsuo Shimosawa, Tomo
Hypertension Research.2025; 48(2): 506. CrossRef - Synthesis, Characterization, DFT Analysis, Pharmacokinetics, and Inhibition of Mpro and RdRp of SARS-CoV-2 by Two Dihydropyrimidines Derivatives
Samia Mammeri, Rachida Kerkour, Nadjib Chafai, Hassina Harkat, Saleh Chafaa
Journal of Molecular Structure.2025; 1324: 140797. CrossRef - Rationale and Design of a Randomized, Open‐Label, Parallel‐Group Study of Esaxerenone Versus Angiotensin Receptor Blockers in Older Patients With Uncontrolled Hypertension on Calcium Channel Blocker Monotherapy (ESCORT‐HT)
Kazuomi Kario, Tomohiro Katsuya, Tatsuo Shimosawa, Takashi Taguchi, Ayumi Tanabe, Mitsuru Ohishi
The Journal of Clinical Hypertension.2025;[Epub] CrossRef - Discovering the natural source-derived antihypertensive compounds aspiring current therapeutic targets by computer-based drug design
Nail Besli, Nilufer Ercin, Rabia Kalkan-Cakmak, Bahar Sarikamis-Johnson, Merve Beker, Ulkan Celik
Biochemical and Biophysical Research Communications.2025; 759: 151685. CrossRef - Biginelli dihydropyrimidines and their acetylated derivatives as L‐/T‐type calcium channel blockers: Synthesis, enantioseparation, and molecular modeling studies
Miyase Gözde Gündüz, Cagatay Dengiz, Katrin Denzinger, Sun Huang, J. T. Lee, Jordan W. Nafie, Daniel W. Armstrong, Gerhard Wolber, Gerald W. Zamponi
Archiv der Pharmazie.2025;[Epub] CrossRef - Cerebral Small Vessel Disease: Therapeutic Approaches Targeting Neuroinflammation, Oxidative Stress, and Endothelial Dysfunction
Habibe Yılmaz, Ulvi Bayraktutan
Current Issues in Molecular Biology.2025; 47(4): 232. CrossRef - Mitigating morphine dependence and withdrawal: The role of venlafaxine and calcium channel blockers in mitochondrial damage and oxidative stress in the brain
Radman Amiri, Faezeh Fallah, Behnam Ghorbanzadeh, Ali Akbar Oroojan, Mohammad Amin Behmanesh, Soheila Alboghobeish
Brain Research Bulletin.2025; 226: 111364. CrossRef - Enantioselective toxicity of (S)-amlodipine towards zebrafish embryos: Abnormal ocular development, cardiac dysfunction, and malformed intersegmental vessels
Chaeeun Kim, Donghyeon Kim, Sung-Eun Lee
Ecotoxicology and Environmental Safety.2025; 298: 118315. CrossRef - Visible Light‐Driven Multicomponent Reactions for the Synthesis of Diverse Heterocyclic Frameworks
Narsimhaswamy Dubasi, Ravi Varala, Murali Mohan Achari Kamsali, Mohammed Mujahid Alam
European Journal of Organic Chemistry.2025;[Epub] CrossRef - A Simple and Rapid Analytical Method to Detect and Quantify the N‐Nitroso Desmethyl Diltiazem Impurity by Liquid Chromatography‐Tandem Mass Spectrometry in Diltiazem Hydrochloride
Manoj Kumar Mandapaka, Veeraswami Boddu
SEPARATION SCIENCE PLUS.2025;[Epub] CrossRef - Natural products and derivatives hold promise to improve treatment of unresponsive tumours
Rosa Jahangiri
Natural Product Research.2025; : 1. CrossRef - Optimization and Validation of an Eco-friendly Stability Indicating UPLC Analytical Method for Amlodipine Besylate Determination
Mohamed Abbas Ibrahim, Mohammed Abdulhadi Alasimi, Doaa Hasan Alshora, Abdelrahman Y. Sherif, Fars Alanazi
Oriental Journal Of Chemistry.2025; 41(3): 984. CrossRef - Nifedipine's Synergistic Therapeutic Potential: Overcoming Challenges and Embracing Novel Applications in Pharmacotherapy
Muneeb Ur Rahman, Hafiz Rashid Hussain, Habiba Akram, Faisal Gulzar, Muhammad Nouman, Hassan Farooq, Arslan Ashfaq, Zaha Kalsoom
Prospects in Pharmaceutical Sciences.2025; 23(2): 101. CrossRef - The Application of Mesoporous Silica Nanoparticles in Enhancing the Efficacy of Anti-Atherosclerosis Therapies: A Review
Arif Budiman, Luthfiyyah Mutmainah, Martina Anjelina, Mila Fitriawati, Eufrasia Pilihanto, Salma Amaliah, Diah Aulifa
International Journal of Nanomedicine.2025; Volume 20: 9825. CrossRef - Repurposing calcium channel blockers and cholinesterase inhibitors for antisnake venom therapy: a mechanistic literature review
Amina Jega Yusuf, Tule Terpase Christian, Nasir Ibrahim, Yusuf Ibrahim Alkali, Jamila Aminu, Sonia Kamran, Abubakar S. Barau, Naushad Hussain, Nurhuda Manshoor, Mustapha Salihu
Discover Chemistry.2025;[Epub] CrossRef - Naringenin promotes coronary vasodilation via inhibition of L-type calcium channels (CaV1.2): Evidence from tissue bath and molecular studies
Puneet Sharma, Pratishtha Sharma, Ashok Gaur, Kirti Purva, Ajay Bhati, Devendra Singh, Lakshmi Kant, Shivangi Gaur, Amit Kumar Pandey
European Journal of Pharmacology.2025; 1008: 178342. CrossRef - Problems associated with the ATC system of drug classification
Lilly Josephine Bindel, Roland Seifert
Naunyn-Schmiedeberg's Archives of Pharmacology.2025;[Epub] 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
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 - Endothelial Cell Dysfunction: Onset, Progression, and Consequences
Hojjat Naderi-Meshkin, Wiwit Ananda Wahyu Setyaningsih
Frontiers in Bioscience-Landmark.2024;[Epub] CrossRef - Angiotensin II Exposure In Vitro Reduces High Salt-Induced Reactive Oxygen Species Production and Modulates Cell Adhesion Molecules’ Expression in Human Aortic Endothelial Cell Line
Nikolina Kolobarić, Nataša Kozina, Zrinka Mihaljević, Ines Drenjančević
Biomedicines.2024; 12(12): 2741. CrossRef
- Home blood pressure-lowering effect of esaxerenone versus trichlormethiazide for uncontrolled hypertension: a predefined subanalysis of the EXCITE-HT randomized controlled trial by basal calcium channel blocker versus angiotensin receptor blocker
First
Prev
