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      Efficacy of bolus injections of landiolol hydrochloride as premedication in coronary artery CT angiography

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          Abstract

          Purpose

          To assess the efficacy of bolus injections of landiolol hydrochloride as premedication in coronary artery CT angiography (CCTA).

          Methods

          The study population consisted of 37 patients (17 female; median age, 56 years; IQR, 19 years; range, 19–88 years) who underwent CCTA after intravenous injection of landiolol hydrochloride due to a heart rate > 60 bpm. Landiolol hydrochloride was administered in a stepwise manner until a heart rate of ≤ 60 bpm was achieved or a maximum dose of 60 mg was reached after six injections. Heart rates routinely displayed continuously on the CT scanner before the start of the landiolol hydrochloride injection (HR PRE), after each partial dose (HR 1–6), during the CT scan (HR CT), and after the examination before moving from the CT table (HR POST) were recorded. Furthermore, the blood pressure routinely measured before (BP PRE) and after the examination before moving from the CT table (BP POST) was recorded.

          Results

          A HR CT of ≤ 60 bpm was achieved in 13 patients (35%) and a HR CT ≤ 65 bpm was achieved in 25 patients (68%). The mean difference (± SD) between HR PRE and HR CT was −11 ± 9 bpm in total, −14 ± 10 bpm in patients without oral beta-blocker premedication and −6 ± 5 bpm in patients with oral Beta-blocker premedication.

          Conclusions

          Landiolol hydrochloride enables a reduction of the heart rate in patients with and without oral beta-blocker premedication, whereby the use of serial partial doses is a simple and effective approach in clinical routine.

          Critical relevance statement

          In cardiac CT, weight-independent, stepwise landiolol hydrochloride injection up to 40 mg reduces heart rate by −14 bpm without and −5 bpm with oral beta-blocker premedication, and achieves heart rates of ≤ 65 bpm in a significant proportion of patients.

          Key Points

          • The ideal heart rate for cardiac CT is ≤ 60–65 bpm, which improves image quality and reduces radiation dose.

          • In cardiac CT, landiolol hydrochloride intravenously reduces heart rate by −14 bpm.

          • Heart rate of ≤ 65 bpm can be achieved in a significant proportion of patients.

          Graphical Abstract

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          Most cited references19

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          The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.

          Beta-adrenoceptor antagonists ("beta-blockers") are one of the most widely used classes of drugs in cardiovascular medicine (hypertension, ischaemic heart disease and increasingly in heart failure) as well as in the management of anxiety, migraine and glaucoma. Where known, the mode of action in cardiovascular disease is from antagonism of endogenous catecholamine responses in the heart (mainly at beta1-adrenoceptors), while the worrisome side effects of bronchospasm result from airway beta2-adrenoceptor blockade. The aim of this study was to determine the selectivity of beta-antagonists for the human beta-adrenoceptor subtypes. (3)H-CGP 12177 whole cell-binding studies were undertaken in CHO cell lines stably expressing either the human beta1-, beta2- or the beta3-adrenoceptor in order to determine the affinity of ligands for each receptor subtype in the same cell background. In this study, the selectivity of well-known subtype-selective ligands was clearly demonstrated: thus, the selective beta1 antagonist CGP 20712A was 501-fold selective over beta2 and 4169-fold selective over beta3; the beta2-selective antagonist ICI 118551 was 550- and 661-fold selective over beta1 and beta3, respectively, and the selective beta3 compound CL 316243 was 10-fold selective over beta2 and more than 129-fold selective over beta1. Those beta2-adrenoceptor agonists used clinically for the treatment of asthma and COPD were beta2 selective: 29-, 61- and 2818-fold for salbutamol, terbutaline and salmeterol over beta1, respectively. There was little difference in the affinity of these ligands between beta1 and beta3 adrenoceptors. The clinically used beta-antagonists studied ranged from bisoprolol (14-fold beta1-selective) to timolol (26-fold beta2-selective). However, the majority showed little selectivity for the beta1- over the beta2-adrenoceptor, with many actually being more beta2-selective. This study shows that the beta1/beta2 selectivity of most clinically used beta-blockers is poor in intact cells, and that some compounds that are traditionally classed as "beta1-selective" actually have higher affinity for the beta2-adrenoceptor. There is therefore considerable potential for developing more selective beta-antagonists for clinical use and thereby reducing the side-effect profile of beta-blockers.
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            Comparison of the β-Adrenergic Receptor Antagonists Landiolol and Esmolol: Receptor Selectivity, Partial Agonism, and Pharmacochaperoning Actions.

            Blockage of β1-adrenergic receptors is one of the most effective treatments in cardiovascular medicine. Esmolol was introduced some three decades ago as a short-acting β1-selective antagonist. Landiolol is a more recent addition. Here we compared the two compounds for their selectivity for β1-adrenergic receptors over β2-adrenergic receptors, partial agonistic activity, signaling bias, and pharmacochaperoning action by using human embryonic kidney (HEK)293 cell lines, which heterologously express each human receptor subtype. The affinity of landiolol for β1-adrenergic receptors and β2-adrenergic receptors was higher and lower than that of esmolol, respectively, resulting in an improved selectivity (216-fold versus 30-fold). The principal metabolite of landiolol (M1) was also β1-selective, but its affinity was very low. Both landiolol and esmolol caused a very modest rise in cAMP levels but a robust increase in the phosphorylation of extracellular signal regulated kinases 1 and 2, indicating that the two drugs exerted partial agonist activity with a signaling bias. If cells were incubated for ≥24 hours in the presence of ≥1 μM esmolol, the levels of β1-adrenergic-but not of β2-adrenergic-receptors increased. This effect was contingent on export of the β1-receptor from endoplasmic reticulum and was not seen in the presence of landiolol. On the basis of these observations, we conclude that landiolol offers the advantage of: 1) improved selectivity and 2) the absence of pharmacochaperoning activity, which sensitizes cells to rebound effects upon drug discontinuation.
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              Pharmacokinetic variability of beta‐adrenergic blocking agents used in cardiology

              Abstract The aim of this study was to evaluate the pharmacokinetic variability of beta‐adrenergic blocking agents used in cardiology by reviewing single‐dose and steady‐state pharmacokinetic studies from the literature. PubMed was searched for pharmacokinetic studies of beta‐adrenergic blocking agents, both single‐dose and steady‐state studies. The studies included reported maximum plasma concentration (Cmax) and/or area under the concentration curve (AUC). The coefficient of variation (CV%) was calculated for all studies, and a CV% 40% was considered high variability. The Cmax and AUC were reported a total of 672 times in 192 papers. Based on AUC, metoprolol, propranolol, carvedilol, and nebivolol showed high pharmacokinetic variability (highest first), whereas bisoprolol, atenolol, sotalol, labetalol, nadolol, and pindolol showed low to moderate variability (lowest first). We have shown a high interindividual pharmacokinetic variability that varies markedly in different beta‐adrenergic blocking agents; the extreme being steady state ratios as high as 30 in metoprolol. A more personalized approach to the medical treatment of patients may be obtained by combining known pharmacokinetic information about variability, pharmaco‐genetics and ‐dynamics, and patient characteristics, to avoid adverse events or lack of treatment effect.
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                Author and article information

                Contributors
                helmut.schoellnast@medunigraz.at
                Journal
                Insights Imaging
                Insights Imaging
                Insights into Imaging
                Springer Vienna (Vienna )
                1869-4101
                10 January 2025
                10 January 2025
                December 2025
                : 16
                : 13
                Affiliations
                [1 ]Institute of Radiology, LKH Graz II, Graz, Austria
                [2 ]Division of Neuroradiology, Vascular and Interventional Radiology, Department of Radiology, Medical University of Graz, ( https://ror.org/02n0bts35) Graz, Austria
                [3 ]Institute for Medical Informatics, Statistics and Documentation, Medical University of Graz, ( https://ror.org/02n0bts35) Graz, Austria
                [4 ]Division of General Radiology, Department of Radiology, Medical University of Graz, ( https://ror.org/02n0bts35) Graz, Austria
                Author information
                http://orcid.org/0000-0003-1442-9118
                Article
                1892
                10.1186/s13244-024-01892-5
                11723858
                39792205
                1fb79de1-15bd-4cd4-8848-80a78992ca4b
                © The Author(s) 2025

                Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/.

                History
                : 22 May 2024
                : 18 December 2024
                Categories
                Original Article
                Custom metadata
                © European Society of Radiology (ESR) 2025

                Radiology & Imaging
                multidetector computed tomography,cardiac imaging techniques,beta-adrenergic blocker,heart–drug effects,heart rate

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