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Adrenergic Antagonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
β adrenoceptor antagonistic action depends on their relative affinity toward β1, β2 adrenoceptors, their action on α receptor, lipid solubility, ability to cause vasodilation, and their pharmacokinetic parameters (Frishman et al., 2011). All these characteristics are useful in the appropriate drug selection for the patient. β antagonists can be categorized as non-selective, selective, and those with additional cardiovascular activity in connection to β adrenoceptor antagonism. Some β blockers partially activate the β adrenoceptor without catecholamines presence. So, these partial agonists possess a slight sympathomimetic activity. For example, acebutolol, pindolol. Some other β antagonists possess a feature like inverse agonism nature. Many β antagonists like propranolol, pindolol, acebutolol, metoprolol, carvedilol, and so on possess a membrane stabilizing or local anesthetic action similar to lidocaine. Some β antagonists like bucindolol, carvedilol, and labetalol blocks α1 along with β receptors. Many other β antagonists along with these also cause vasodilator activity (Brubacher, 2015; Brunton et al., 2011). The mechanism by which β antagonists acts and its action on different organs is demonstrated in Figure 4.5.
Cardiac physiology
Published in ILEANA PIÑA, SIDNEY GOLDSTEIN, MARK E DUNLAP, The Year in Heart Failure, 2005
Ghali JK, Krause-Steinrauf HJ, Adams Jr KF, eta/. JAm Col/ Cardio/2003 ; 42:2128-34 B A c KG R o u N o. The goal of this study was to determine the influence of gender on baseline characteristic responses to treatment and prognosis in patients with heart failure secondary to impaired systolic function. Women have been underrepresented in heart failure trials. The Beta-blocker Evaluation of Survival Trial (BEST) randomized 2708 patients with New York Heart Association class III-IV heart failure to either bucindolol or placebo. Although the trial did not show overall mortality benefits from bucindolol, the trial is replete with Important data. There were 593 women In the study. The women were younger, more likely to be black and had a higher number of dilated cardiomyopathies. lschaemic aetiology and measures of heart failure severity were prognostic predictors In both men and women. Coronary artery disease and LVEF appeared to be stronger predictors of prognosis In women (Fig. 2.3).
Ex ante economic evaluation of genetic testing for the ARG389 beta1-adrenergic receptor polymorphism to support bucindolol treatment decisions in Stage III/IV heart failure
Published in Expert Review of Precision Medicine and Drug Development, 2018
Nimer S. Alkhatib, Kenneth Ramos, Marion Slack, Brian Erstad, Mahdi Gharaibeh, Walter Klimecki, Jason H Karnes, Nancy K. Sweitzer, Ivo Abraham
A two-branch decision-tree with a time-horizon of 18 months comprised of three replicative 6-month cycles each was specified (Figure 1). In keeping with Liggett et al. [18], the first branch assumed that the Arg389 genetic test is carried out and patients are designated either Arg389-positive (homozygote) or Arg389-negative (not homozygote). In line with their BEST sub-analyses [15,18], Arg389-positive patients were treated with bucindolol. Conversely, and in keeping with the COPERNICUS trial, Arg389-negative patients were treated with carvedilol [24]. The second branch represents the alternative that the Arg389 genetic test is not performed. In this branch, and consistent with the overall BEST findings [14], patients were assumed to be treated empirically with bucindolol. Bucindolol is assumed to be discontinued and carvedilol salvage treatment initiated if patients experience uncontrolled blood pressure, worsening of HF, or frequent hospitalization. Our model specifies three major HF health states within each of the three 6-month cycles: alive, which may be either stable (compensated) or hospitalized (decompensated), and death.