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CALCIUM CHANNEL BLOCKERS IN CARDIOVASCULAR SYSTEM DISEASES

Yıl 2025, Cilt: 49 Sayı: 2, 22 - 22

İrem Harmanşah , Sümeyye Güney Kalkan , Meltem Ünlüsoy

https://doi.org/10.33483/jfpau.1597966

Öz

Objective: Calcium calcium channel blockers (CCBs) have been shown to reduce arterial constriction by blocking calcium entry and interacting with binding sites identified on voltage-gated calcium channels. These compounds reduce arterial pressure by reducing total peripheral resistance. They improve myocardial oxygenation by disloading the heart and increasing coronary blood flow. In this study, an exploration has been undertaken concerning the makeup, variations, and attributes of calcium channels. Furthermore, an examination has been conducted regarding the categorization of compounds that block calcium channels, encompassing their molecular structure, mechanism of aciton, structure-activity relationships, metabolic pathways, recognized therapeutic applications in cardiovascular conditions, and broader therapeutic implications.
Result and Discussion: Hypertension represents a substantial strategy to reduce the burden of cardiovascular and renal diseases associated with hypertension. Rational, integrated, and synergistic combination therapies which are recommended as a first-line strategy aimed at achieving the blood pressure targets. Among the currently available classes of antihypertensive drugs for the clinical treatment of hypertension, both in monotherapy and combination therapy, it has been shown that drugs inhibiting the renin-angiotensin system and calcium channel blockers (CCBs) are effective and safe in lowering and reaching the target blood pressure levels. Due to extensive scientific evidence demonstrating their efficacy in mitigating cardiovascular and renal complications linked to hypertension, calcium channel blockers have gained widespread use as a preferred class of antihypertensive medications over the last two decades, primarily attributed to their favorable tolerability profile.

Anahtar Kelimeler

Calcium channels calcium channel blockers hypertension types of calcium channels

Kaynakça

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KARDİYOVASKÜLER SİSTEM HASTALIKLARINDA KALSİYUM KANAL BLOKÖRLERİ

Yıl 2025, Cilt: 49 Sayı: 2, 22 - 22

İrem Harmanşah , Sümeyye Güney Kalkan , Meltem Ünlüsoy

https://doi.org/10.33483/jfpau.1597966

Öz

Amaç: Kalsiyum kanal blokörü bileşiklerin (KKB'ler) kalsiyum girişini engelleyerek ve voltaja bağlı kalsiyum kanallarında tanımlanan bağlanma bölgeleriyle etkileşime girerek arterlerin kasılmasını azalttıkları gösterilmiştir. Bu bileşikler toplam periferik direnci azaltarak arteriyel basıncı düşürür. Kalbin yükünü boşaltarak ve koroner kan akışını artırarak miyokard oksijenlenmesini iyileştirir. Bu çalışmada kalsiyum kanal yapısı, alt tipleri ve özellikleri; KKB'lerin sınıflandırılması, yapı-aktivite ilişkileri, kimyasal yapısı, metabolizması, farmakolojik özellikleri, bunların kardiyovasküler bozukluklar için yerleşik terapötik kullanımları ve genel terapötik endikasyonları hakkında bilgi verilmesi amaçlanmıştır.
Sonuç ve Tartışma: Hipertansiyonun etkili tedavisi, hipertansiyona bağlı kardiyovasküler ve böbrek hastalıklarının yükünü azaltmak için önemli bir stratejiyi temsil eder. Rasyonel, entegre ve sinerjik kombinasyon tedavileri, birinci basamak strateji olarak önerilen kan basıncı hedeflerine ulaşmayı amaçlamıştır. Hipertansiyonun klinik tedavisi için halihazırda mevcut olan olası antihipertansif ilaç sınıfları içinde, hem monoterapi hem de kombinasyon terapisinde, renin-anjiyotensin sistemini inhibe eden ilaçların ve kalsiyum kanal blokörlerinin (KKB'ler), kan basıncı seviyelerini düşürmede ve hedefe ulaşmada etkili aynı zamanda güvenli olduğu gösterilmiştir. İyi bir tolere edilebilirlik profiline sahip olan KKB'ler kan basıncını düşürmedeki etkinlikleri, hipertansiyonun kardiyovasküler ve renal sonuçlarını azaltmaya yönelik çok sayıda bilimsel kanıt nedeniyle son 20 yılda en yaygın kullanılan antihipertansif sınıflarından biri olmuştur.

Anahtar Kelimeler

Hipertansiyon kalsiyum kanalları kalsiyum kanal blokörleri kalsiyum kanal tipleri

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  • 103. Budriesi, R., Cosimelli, B., Ioan, P., Carosati, E., Ugenti, P.M., Spisani, R. (2007). Diltiazem analogues: The last ten years on structure activity relationships. Current Medicinal Chemistry, 14(3), 279-287. [CrossRef]
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  • 108. Steuber, T.D., Lee, J., Holloway, A., Andrus, M.R. (2019). Nondihydropyridine calcium channel blockers for the treatment of proteinuria: A review of the literature. Annals of Pharmacotherapy, 53(10), 1050-1059. [CrossRef]
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  • 110. Zhou, P.Z., Babcock, J., Liu, L.Q., Li, M., Gao, Z.B. (2011). Activation of human ether-a-go-go related gene (hERG) potassium channels by small molecules. Acta Pharmacologica Sinica, 32(6), 781-788. [CrossRef]
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  • 114. Cole, P.L., Beamer, A.D., McGowan, N., Cantillon, C.O., Benfell, K., Kelly, R.A., Hartley, L.H., Smith, T.W., Antman, E.M. (1990). Efficacy and safety of perhexiline maleate in refractory angina. A double-blind placebo-controlled clinical trial of a novel antianginal agent. Circulation, 81(4), 1260-1270. [CrossRef]
  • 115. Ren, Z., Chen, S., Seo, J.E., Guo, X., Li, D., Ning, B., Guo, L. (2020). Mitochondrial dysfunction and apoptosis underlie the hepatotoxicity of perhexiline. Toxicol In Vitro, 69, 104987. [CrossRef]
  • 116. Kazatani, T., Higaki, A., Tanaka, Y., Kawada, Y., Hiasa, G., Yamada, T., Okayama, H. (2022). Bepridil monotherapy failed to prevent coronary vasospasm in a Brugada syndrome patient. Oxford Medical Case Reports, 2022(8). [CrossRef]
  • 117. Asai, Y., Arihara, H., Omote, S., Tanio, E., Yamashita, S., Higuchi, T., Hashimoto, E., Yamada, M., Tsuji, H., Kondo, Y., Hayashi, M., Yamamoto, Y. (2023). Effect of polypharmacy on plasma bepridil concentration in patients with heart failure: A multicenter retrospective study. Journal of Pharmaceutical Health Care and Sciences, 9(1), 10. [CrossRef]
  • 118. Awni, W.M., Halstenson, C.E., Nayak, R.K., Opsahl, J.A., Desiraju, R.K., Minn, F.L., Matzke, G.R. (1995). Pharmacokinetics of bepridil and two of its metabolites in patients with end-stage renal disease. The Journal of Clinical Pharmacology, 35(4), 379-383. [CrossRef]
  • 119. Vatansever, E.C., Yang, K.S., Drelich, A.K., Kratch, K.C., Cho, C.C., Kempaiah, K.R., Hsu, J.C., Mellott, D.M., Xu, S., Tseng, C.K., Liu, W.R. (2021). Bepridil is potent against SARS-CoV-2 in vitro. Proceedings of the National Academy of Sciences of the United States of America, 118(10). [CrossRef]
  • 120. Johansen, L.M., DeWald, L.E., Shoemaker, C.J., Hoffstrom, B.G., Lear-Rooney, C.M., Stossel, A., Nelson, E., Delos, S.E., Simmons, J.A., Grenier, J.M., Pierce, L.T., Pajouhesh, H., Lehár, J., Hensley, L.E., Glass, P.J., White, J.M., Olinger, G.G. (2015). A screen of approved drugs and molecular probes identifies therapeutics with anti-Ebola virus activity. Science Translational Medicine, 7(290), 290ra289-290ra289. [CrossRef]
  • 121. Renneberg, D., Hubler, F., Rey, M., Hess, P., Delahaye, S., Gatfield, J., Iglarz, M., Hilpert, K. (2015). Discovery of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers. Bioorganic & Medicinal Chemistry Letters, 25(18), 3941-3946. [CrossRef]
  • 122. Souza Bomfim, G.H., Mitaishvili, E., Aguiar, T.F., Lacruz, R.S. (2021). Mibefradil alters intracellular calcium concentration by activation of phospholipase C and IP(3) receptor function. Molecular Biomedicine, 2(1), 12. [CrossRef]
  • 123. Mullins, M.E., Horowitz, B.Z., Linden, D.H., Smith, G.W., Norton, R.L., Stump, J. (1998). Life-threatening interaction of mibefradil and beta-blockers with dihydropyridine calcium channel blockers. Jama, 280(2), 157-158. [CrossRef]
Toplam 122 adet kaynakça vardır.

Ayrıntılar

Birincil Dil Türkçe
Konular Farmasotik Kimya
Bölüm Derleme
Yazarlar

İrem Harmanşah 0009-0001-4508-1268

Sümeyye Güney Kalkan 0009-0007-1180-1611

Meltem Ünlüsoy 0000-0002-7070-8181

Erken Görünüm Tarihi 8 Mayıs 2025
Yayımlanma Tarihi
Gönderilme Tarihi 7 Aralık 2024
Kabul Tarihi 23 Aralık 2024
Yayımlandığı Sayı Yıl 2025 Cilt: 49 Sayı: 2

Kaynak Göster

APA Harmanşah, İ., Güney Kalkan, S., & Ünlüsoy, M. (2025). KARDİYOVASKÜLER SİSTEM HASTALIKLARINDA KALSİYUM KANAL BLOKÖRLERİ. Journal of Faculty of Pharmacy of Ankara University, 49(2), 22-22. https://doi.org/10.33483/jfpau.1597966
AMA Harmanşah İ, Güney Kalkan S, Ünlüsoy M. KARDİYOVASKÜLER SİSTEM HASTALIKLARINDA KALSİYUM KANAL BLOKÖRLERİ. Ankara Ecz. Fak. Derg. Mayıs 2025;49(2):22-22. doi:10.33483/jfpau.1597966
Chicago Harmanşah, İrem, Sümeyye Güney Kalkan, ve Meltem Ünlüsoy. “KARDİYOVASKÜLER SİSTEM HASTALIKLARINDA KALSİYUM KANAL BLOKÖRLERİ”. Journal of Faculty of Pharmacy of Ankara University 49, sy. 2 (Mayıs 2025): 22-22. https://doi.org/10.33483/jfpau.1597966.
EndNote Harmanşah İ, Güney Kalkan S, Ünlüsoy M (01 Mayıs 2025) KARDİYOVASKÜLER SİSTEM HASTALIKLARINDA KALSİYUM KANAL BLOKÖRLERİ. Journal of Faculty of Pharmacy of Ankara University 49 2 22–22.
IEEE İ. Harmanşah, S. Güney Kalkan, ve M. Ünlüsoy, “KARDİYOVASKÜLER SİSTEM HASTALIKLARINDA KALSİYUM KANAL BLOKÖRLERİ”, Ankara Ecz. Fak. Derg., c. 49, sy. 2, ss. 22–22, 2025, doi: 10.33483/jfpau.1597966.
ISNAD Harmanşah, İrem vd. “KARDİYOVASKÜLER SİSTEM HASTALIKLARINDA KALSİYUM KANAL BLOKÖRLERİ”. Journal of Faculty of Pharmacy of Ankara University 49/2 (Mayıs 2025), 22-22. https://doi.org/10.33483/jfpau.1597966.
JAMA Harmanşah İ, Güney Kalkan S, Ünlüsoy M. KARDİYOVASKÜLER SİSTEM HASTALIKLARINDA KALSİYUM KANAL BLOKÖRLERİ. Ankara Ecz. Fak. Derg. 2025;49:22–22.
MLA Harmanşah, İrem vd. “KARDİYOVASKÜLER SİSTEM HASTALIKLARINDA KALSİYUM KANAL BLOKÖRLERİ”. Journal of Faculty of Pharmacy of Ankara University, c. 49, sy. 2, 2025, ss. 22-22, doi:10.33483/jfpau.1597966.
Vancouver Harmanşah İ, Güney Kalkan S, Ünlüsoy M. KARDİYOVASKÜLER SİSTEM HASTALIKLARINDA KALSİYUM KANAL BLOKÖRLERİ. Ankara Ecz. Fak. Derg. 2025;49(2):22-.
 Kapak Resmi İndir

Kapsam ve Amaç

Ankara Üniversitesi Eczacılık Fakültesi Dergisi, açık erişim, hakemli bir dergi olup Türkçe veya İngilizce olarak farmasötik bilimler alanındaki önemli gelişmeleri içeren orijinal araştırmalar, derlemeler ve kısa bildiriler için uluslararası bir yayım ortamıdır. Bilimsel toplantılarda sunulan bildiriler supleman özel sayısı olarak dergide yayımlanabilir. Ayrıca, tüm farmasötik alandaki gelecek ve önceki ulusal ve uluslararası bilimsel toplantılar ile sosyal aktiviteleri içerir.