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Atrial fibrillation
Published in Henry J. Woodford, Essential Geriatrics, 2022
A recent open-label study compared digoxin to bisoprolol for people aged over 60 with AF, breathlessness and a pulse rate 60 or over (n = 160; mean age 76; mean baseline heart rate: ECG 100 bpm, pulse 87 bpm).58 No significant difference in quality of life, the primary outcome, was detected at six months between digoxin (mean dose 161 mcg/day) and bisoprolol (mean dose 3.2 mg/day). More adverse effects were associated with bisoprolol.
Personalized Nutrition in Hypercholesterolemia
Published in Nilanjana Maulik, Personalized Nutrition as Medical Therapy for High-Risk Diseases, 2020
Aktarul Islam Siddique, Nalini Namasivayam
Beta-blockers are mainly recommended for people who have coronary artery disease as well as high blood pressure or heart failure (Ko, Hebert et al. 2004). Besides, beta-blockers also help in relieving angina. Various types of beta-blockers are available. Among them, bisoprolol and metoprolol are the ones most commonly used. Bisoprolol and metoprolol are usually used at the dose of 2.5 to 5 mg per day and 50 to 100 mg per day respectively.
Substrates of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
Bisoprolol is a selective β1-adrenoceptor blocker indicated for hypertension and chronic heart failure (Johns and Lopez 1995; McGavin and Keating 2002). Bisoprolol has a chiral center, with S-(−)-bisoprolol being 30 to 80 times more pharmacologically active than R-(+)-bisoprolol. The oral bioavail-ability of bisoprolol is high (>90%) and the drug has a long t1/2β (11 h), which allows once-daily administration (Lancaster and Sorkin 1988). In humans, 50% of the dose is eliminated renally as unchanged drug and the other 50% is eliminated metabolically, with subsequent renal excretion of the metabolites (Leopold et al. 1986). Bisoprolol is mainly metabolized to M4 via O-deisopropylation by CYP3A4 and 2D6 (Figure 3.63) (Horikiri et al. 1998a,b). CYP2D6 metabolized bisoprolol stereoselectively (R > S), whereas the metabolism of bisoprolol by CYP3A4 is not stereoselective (Horikiri et al. 1998a). In Japanese patients, the genotype of CYP2D6 and 2C9 did not affect the pharmacokinetics of bisoprolol (Taguchi et al. 2005).
Current and emerging pharmacotherapy for the management of hypertrophic cardiomyopathy
Published in Expert Opinion on Pharmacotherapy, 2023
Akiva Rosenzveig, Neil Garg, Shiavax J. Rao, Amreen K. Kanwal, Arjun Kanwal, Wilbert S. Aronow, Matthew W. Martinez
Beta blockers have long since been regarded as the mainstay for management of HCM associated LVOTO. Mechanistic reduction in maximum contraction velocity achieved by beta blockers positively affects systolic function as well as decreases the amplitude of LVOTO in HCM patients [15]. A 2022 placebo-controlled double-blind trial found that metoprolol was linked with positive changes to the LVOT gradient, as well as decreased mitral regurgitation and increased stroke volume at rest and during exercise in HCM patients [16]. To combat LVOTO, beta blockers, such as atenolol, nadolol, bisoprolol, and metoprolol, are current treatment standards. Titration of these drugs based on cardiac response, symptoms, and vitals is best practice, as high doses are usually required and well tolerated [17]. A recent retrospective study evaluated 92 adults with obstructive HCM treated with bisoprolol. Seventeen percent of the patients met the primary endpoint (reduction of LVOT gradient to <30 mmHg and ≥1 NYHA class improvement)), 36% of the patients had the LVOT gradient reduced to <30 mmHg, and 62% of the patients had a gradient reduced to <50 mmHg [18]. This study demonstrated both the effectiveness of bisoprolol therapy as well as the need for better therapies.
Efficacy and safety of bisoprolol 5 mg plus amlodipine 5 mg in patients with hypertension uncontrolled on monotherapy with 5 mg of amlodipine, a phase III multicenter, randomized, double-blind, placebo-controlled clinical trial – the AMCOR study
Published in Current Medical Research and Opinion, 2023
Piotr Jędrusik, Grzegorz Placha, Zbigniew Gaciong
The treatment was well tolerated by the study participants. There was no serious AE in any patient during the trial and the AE rate was similar in both groups. However, in 3.9% of patients on bisoprolol, the treatment was stopped due to an AE possibly related to the study medication. The most frequent reason for treatment withdrawal was bradycardia which was not associated with any symptoms/clinical deterioration. In 5 patients, the observed AEs (bradycardia, weakness) are well-known adverse reactions listed in the summary product characteristics (SmPC) of bisoprolol as occurring with the frequency of 1–10%. Both paresthesias and laboratory signs of liver injury are also described in the SmPC of bisoprolol but with an undefined frequency. The symptoms were described as possibly related to the study medication and alleviated after its withdrawal.
Bisoprolol transdermal patch improves orthostatic hypotension in patients with chronic heart failure and hypertension
Published in Clinical and Experimental Hypertension, 2020
Shunsuke Kiuchi, Shinji Hisatake, Takayuki Kabuki, Takashi Oka, Shintaro Dobashi, Takahiro Fujii, Takahide Sano, Takanori Ikeda
In the present study, the BP-lowering effects between the two medications were equivalent; however, the bisoprolol transdermal patch improved OH. Previous studies have reported similar results (10,18). BP values were similar because they were mainly affected by the β2 receptor; however, BP variability may have been improved by the effects on RVLM via β1 receptors. The decrease in HR variability has also been reported (27,28). BB decreases sympathetic nerve activity, whereas it increases the cardiac vagal activity(13). Li et al. explained that the modulation of the HR by the sympathetic nerve is more complicated because it involves the antagonistic vagal tone. In the present study, it is unclear whether the bisoprolol transdermal patch is involved in the vagal nerve. Further exploration is warranted to assess this problem.