Antihypertensive Drug Classes
Giuseppe Mancia, Guido Grassi, Konstantinos P. Tsioufis, Anna F. Dominiczak, Enrico Agabiti Rosei in Manual of Hypertension of the European Society of Hypertension, 2019
Currently used beta-blockers can be divided into three groups (2) (Table 40.5) based on their pharmacodynamics properties: Nonselective beta-blockers. They block both beta 1 and beta 2 receptors without selectivity.Cardioselective beta-blockers. They block beta 1 receptors, for example in the heart, with higher selectivity than beta 2 receptors, for example in the lung, when used in approved doses. Overall, cardioselectivity of these drugs is still weak, dose-dependent and decreases with higher doses.Beta-blockers with additional vasodilatory effects. Carvedilol and labetalol exhibit additional vasodilatory effects by blocking adrenergic alpha 1 receptors in arteries, while both compounds are non-selective blockers of both beta 1 and beta 2 receptors. Nebivolol is the beta-blocker with the highest beta 1 selectivity and induces its vasodilatory effect by activating nitric oxide (NO). The vasodilation enhances the BP-lowering effect of these compounds and may improve their tolerability and metabolic profile.
Drug therapy in the cardiac catheterisation laboratory: A guide to commonly used drugs
John Edward Boland, David W. M. Muller in Interventional Cardiology and Cardiac Catheterisation, 2019
Cardiovascular tissues contain alpha-1 receptors and two types of beta receptors, called beta 1 (β1) and beta 2 (β2). Alpha and beta receptors are found mainly in myocardium and vascular smooth muscle cells. Alpha receptor activation causes a small increase in myocardial contraction, and vasoconstriction in vascular walls. Beta receptor activation induces increased myocardial contractility and vasodilatation (with a decrease in blood pressure) in vessel walls. β1 receptors are found mainly in the lungs, heart and blood vessels. β2 receptors are found in the lungs. Activation of β2 lung receptors by drugs such as salbutamol (Ventolin) dilates pulmonary airways. Beta blockers, as implied by name, do the opposite, causing airway constriction by inhibiting beta receptor activity (Table 23.9).
Anesthesia for Patients with Ventricular Assist Devices
Wayne E. Richenbacher in Mechanical Circulatory Support, 2020
Special attention is given to cardiovascular and pulmonary function. A concern for the anesthesiologist is the recognized defect of adrenergic mechanisms that modulate the heart’s inotropic state. A reduction of beta1 adrenergic receptor density in the failing heart has been demonstrated. This finding is thought to represent receptor down regulation produced by chronic exposure of the heart to I excessive catecholamine levels. Although myocardial norepinephrine stores are decreased in advanced heart failure, circulating norepinephrine levels are elevated. I The majority of patients scheduled for VAD(s) implantation are receiving high doses of inotropes. As these drugs act by stimulation of beta adrenergic receptors, maximal doses of inotropes often produce little effect on blood pressure and cardiac output. Usually more than two inotropes are given at any time and higher doses will be required during the administration of anesthetics.
β1-Adrenoceptor antibodies induce PPCM via inhibition of PGC-1α related pathway
Published in Scandinavian Cardiovascular Journal, 2021
Yuan Zhang, Jia Liu, Linying Shi, Mulei Chen, Jiamei Liu
Beta-1-adrenoceptor (β1AR) belongs to the family of G-protein-coupled receptors. In heart, β1AR induce positive chronotropic, inotropic and dromotropic action on myocardial through stimulatory Gs protein [5]. In the past two decades, β1 AR antibodies were found in the serum of healthy people as well as patients with several cardiovascular diseases characterized by heart failure [6–8]. Moreover, it is worth noting that although patients with PPCM have no prior history of heart disease and there are no other known possible causes of heart failure, our previous study found that there was a high correlation between β1AR antibodies and the development of PPCM [9]. However, at present, there is no direct evidence that β1AR antibodies can induce PPCM and the mechanisms that how the β1AR antibodies cause the disease remain completely unclear.
The current and future status of inotropes in heart failure management
Published in Expert Review of Cardiovascular Therapy, 2023
Angelos Arfaras-Melainis, Ioannis Ventoulis, Effie Polyzogopoulou, Antonios Boultadakis, John Parissis
Beta agonists exert their effects by binding to the beta-1 adrenergic receptor located on the sarcolemma of cardiomyocytes. This binding event initiates a signaling cascade that involves the activation of intracellular adenylate cyclase, leading to increased production of cAMP and increased subsequent release of Ca2+ from the sarcoplasmic reticulum. The resulting increase in Ca2+ concentration within the cardiomyocyte leads to enhanced actin-myosin cross-bridging, ultimately culminating in increased contractility on the one hand and increased demand for myocardial oxygen on the other hand. The pharmacological and mechanistic properties of beta agonists differ among various agents due to their distinct affinity for beta-1 receptors and their effects on other receptors [7,8,14].
Rationale for administering beta-blocker therapy to patients undergoing coronary artery bypass surgery: a systematic review
Published in Expert Opinion on Drug Safety, 2018
Arushi Thaper, Alexander Kulik
Individual beta-blockers are typically classified as beta-1 selective or nonselective, depending on the specific adrenergic receptors that are competitively antagonized. Beta-blockers can also vary based on a variety of additional characteristics, such as intrinsic sympatho-mimetic activity, alpha-adrenergic receptor blockade, or vasodilatory effects [9]. Metoprolol, for example, selectively inhibits cardiac beta-1 receptors, but not beta-2 receptors. Carvedilol, on the other hand, inhibits postsynaptic cardiac beta-1, beta-2, and alpha-1 receptors, as well as pre-synaptic beta-2 receptors, and is believed to have antioxidant and free-radical scavenging effects [10]. Carvedilol also appears to have some benefits for patients with diabetes mellitus, with documented improvements in insulin sensitivity and glycemic control, compared to the use of metoprolol for patients with diabetes [11].
Related Knowledge Centers
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