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Indispensible Parameters of Bisoprolol: Objectives, Indications, Mechanism of Action, Pharmacokinetics, Adverse Effects, Contra Indications and Toxicity

Moni Theresa. Tsappidi, Srinivas G., Ramanjaneyulu D.V., Satyanarayana Murthy S., Muralinath E., Guruprasad M., Hari Kiran M., Shaik Mahabooob Basha, Kundara Giridhar Reddy, Kasireddy Gauthami, Mopoori Kalyan, Sai Charan B.

Abstract


One drug used to treat and manage congestive heart failure and hypertension is bisoprolol. The medication is classified as a selective beta-blocker and functions specifically as a cardioselective beta1-blocker (B1-blocker). Congestive heart failure is one of the heart disorders that bisoprolol primarily targets by targeting beta1 receptors in the heart. Various body systems may be impacted by the drug's failure to block unwanted B2 receptors. Selective B1-blockers, such as bisoprolol, have negative chronotropic and inotropic effects that lower heart rate and cardiac contractions. As a result, bisoprolol lessens myocardial cells' oxygen consumption, which lessens the strain on the heart. Additionally, the kidneys' juxtaglomerular cells include B1 receptors. Bisoprolol prevents the activation of the renin-angiotensin system by inhibiting these receptors, which lowers renin release. Because of its combined effects on the kidneys and heart, bisoprolol is useful in the treatment of hypertension and associated disorders.

Background: 1976 saw the patenting of bisoprolol, and 1986 saw its approval for use in medicine. In 1992, the United States authorized its usage for medical purposes. Bisoprolol is a generic drug that is listed on the World Health Organization's List of Essential Medicines

Objective:

  1. 1.      Determine which conditions, such as heart failure, hypertension, and certain arrhythmia, are suitable candidates for bisoprolol therapy.
  2. 2.      Before starting bisoprolol treatment, check patients for risk factors and contraindications, such as severe peripheral vascular disease, asthma, heart block, or bradycardia.
  3. 3.      Evaluate how well patients are responding to bisoprolol treatment by keeping an eye on heart rate, blood pressure, and any indications of side effects.
  4. 4.      Utilize professional advice and evidence-based guidelines to tailor bisoprolol treatment to each patient.

Methods: Bisoprolol inhibits these receptors, which lowers renin release and prevents the renin-angiotensin system from activating. Bisoprolol is useful in treating hypertension and associated disorders because of its dual effects on the heart and kidneys.

Results: After roughly two hours, bisoprolol begins to lower high blood pressure, but it may take up to six weeks for it to fully take effect. It's possible that using bisoprolol for high blood pressure won't affect your symptoms. This does not imply that the medication is ineffective. It's crucial to continue taking it.

Conclusion: Bisoprolol lowers cardiac strain by competitively inhibiting β1-adrenergic receptors, which decreases contractility and oxygen demand. It is also believed that bisoprolol lowers the kidneys' production of renin, which typically raises blood pressure.



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References


Minushkina, L. O. (2012). [Bisoprolol: Opportunities in the treatment of hypertension]. Kardiologiia, 52(6), 80–85. [PubMed]

Whelton, P. K., Carey, R. M., Aronow, W. S., Casey, D. E., Collins, K. J., Dennison Himmelfarb, C., DePalma, S. M., Gidding, S., Jamerson, K. A., Jones, D. W., MacLaughlin, E. J., Muntner, P., Ovbiagele, B., Smith, S. C., Spencer, C. C., Stafford, R. S., Taler, S. J., Thomas, R. J., Williams, K. A., ... Wright, J. T. (2018). 2017 ACC/AHA/AAPA/ABC/ACPM/AGS/APhA/ASH/ASPC/NMA/PCNA guideline for the prevention, detection, evaluation, and management of high blood pressure in adults. Hypertension, 71(6), e13–e115. https://doi.org/10.1161/HYP.0000000000000065

Heidenreich, P. A., Bozkurt, B., Aguilar, D., Allen, L. A., Byun, J. J., Colvin, M. M., Deswal, A., Drazner, M. H., Dunlay, S. M., Evers, L. R., Fang, J. C., Fedson, S. E., Fonarow, G. C., Hayek, S. S., Hernandez, A. F., Khazanie, P., Kittleson, M. M., Lee, C. S., Link, M. S., ... Yancy, C. W. (2022). 2022 AHA/ACC/HFSA guideline for the management of heart failure. Journal of the American College of Cardiology, 79(17), e263–e421. https://doi.org/10.1016/j.jacc.2021.12.012

Wee, Y., Burns, K., & Bett, N. (2015). Medical management of chronic stable angina. Australian Prescriber, 38(4), 131–136. https://doi.org/10.18773/austprescr.2015.046

Unger, T., Borghi, C., Charchar, F., Khan, N. A., Poulter, N. R., Prabhakaran, D., Ramirez, A., Schlaich, M., Stergiou, G. S., Tomaszewski, M., Wainford, R. D., Williams, B., & Schutte, A. E. (2020). 2020 International Society of Hypertension global hypertension practice guidelines. Hypertension, 75(6), 1334–1357. https://doi.org/10.1161/HYPERTENSIONAHA.120.15026

Poldermans, D., Boersma, E., Bax, J. J., Thomson, I. R., Paelinck, B., van de Ven, L. L., Scheffer, M. G., Trocino, G., Vigna, C., Baars, H. F., van Urk, H., & Roelandt, J. R. (2001). Bisoprolol reduces cardiac death and myocardial infarction in high-risk patients as long as 2 years after successful major vascular surgery. European Heart Journal, 22(15), 1353–1358. https://doi.org/10.1053/euhj.2000.2566

Cruickshank, J. M. (2010). Beta-blockers and heart failure. Indian Heart Journal, 62(2), 101–110. [PubMed]

Ladage, D., Schwinger, R. H., & Brixius, K. (2013). Cardio-selective beta-blocker: Pharmacological evidence and their influence on exercise capacity. Cardiovascular Therapeutics, 31(2), 76–83. https://doi.org/10.1111/j.1755-5922.2011.00280.x

do Vale, G. T., Ceron, C. S., Gonzaga, N. A., Simplicio, J. A., & Padovan, J. C. (2019). Three generations of β-blockers: History, class differences and clinical applicability. Current Hypertension Reviews, 15(1), 22–31. https://doi.org/10.2174/1573402115666190201102340

Papadopoulos, D. P., & Papademetriou, V. (2009). Low-dose fixed combination of bisoprolol/hydrochlorothiazide as first line for hypertension: A review of the rationale and clinical evidence. Angiology, 60(5), 601–607. https://doi.org/10.1177/0003319708328542

Johns, T. E., & Lopez, L. M. (1995). Bisoprolol: Is this just another beta-blocker for hypertension or angina? Annals of Pharmacotherapy, 29(4), 403–414. https://doi.org/10.1177/106002809502900414

Galougahi, K. K., Liu, C. C., Bundgaard, H., & Rasmussen, H. H. (2012). β-Adrenergic regulation of the cardiac Na⁺-K⁺ ATPase mediated by oxidative signaling. Trends in Cardiovascular Medicine, 22(4), 83–87. https://doi.org/10.1016/j.tcm.2012.07.002

Kamp, T. J., & Hell, J. W. (2000). Regulation of cardiac L-type calcium channels by protein kinase A and protein kinase C. Circulation Research, 87(12), 1095–1102. https://doi.org/10.1161/01.RES.87.12.1095

Kushnir, A., & Marks, A. R. (2010). The ryanodine receptor in cardiac physiology and disease. Advances in Pharmacology, 59, 1–30. https://doi.org/10.1016/S1054-3589(10)59001-7

Ram, C. V. (2010). Beta-blockers in hypertension. American Journal of Cardiology, 106(12), 1819–1825. https://doi.org/10.1016/j.amjcard.2010.08.023

Ishida, K., Horie, A., Nishimura, M., Taguchi, M., Fujii, N., Nozawa, T., Inoue, H., & Hashimoto, Y. (2013). Variability of bioavailability and intestinal absorption characteristics of bisoprolol. Drug Metabolism and Pharmacokinetics, 28(6), 491–496. https://doi.org/10.2133/dmpk.DMPK-13-RG-062

Chan, S. W., Chu, T. T. W., Ho, C. S., Kong, A. P. S., Tomlinson, B., & Zeng, W. (2021). Influence of CYP2D6 and CYP3A5 polymorphisms on the pharmacokinetics and pharmacodynamics of bisoprolol in hypertensive Chinese patients. Frontiers in Medicine, 8, 683498. https://doi.org/10.3389/fmed.2021.683498

Ågesen, F. N., Weeke, P. E., Tfelt-Hansen, P., & Tfelt-Hansen, J. (2019). Pharmacokinetic variability of beta-adrenergic blocking agents used in cardiology. Pharmacology Research & Perspectives, 7(4), e00496. https://doi.org/10.1002/prp2.496

Li, G. F., Wang, K., Chen, R., Zhao, H. R., Yang, J., & Zheng, Q. S. (2012). Simulation of the pharmacokinetics of bisoprolol in healthy adults and patients with impaired renal function using whole-body physiologically based pharmacokinetic modeling. Acta Pharmacologica Sinica, 33(11), 1359–1371. https://doi.org/10.1038/aps.2012.96

Abeel, M., Gupta, A., & Constance, C. (2022). Concomitant treatment of hypertensive patients with bisoprolol and perindopril in routine clinical practice: A post hoc analysis of the CONFIDENCE II, PROTECT I, and PROTECT III observational studies. Advances in Therapy, 39(1), 391–404. https://doi.org/10.1007/s12325-021-01954-3


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