• Title/Summary/Keyword: ${\beta}$-blockers

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Beta Blockers in Contemporary Cardiology: Is It Better to Cast Them Out?

  • Javaid Ahmad Dar;John Roshan Jacob
    • Korean Circulation Journal
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    • v.54 no.4
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    • pp.165-171
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    • 2024
  • Beta blockers are one of the commonest prescription drugs in medicine and they have been thought to revolutionize the treatment of heart failure (HF) with reduced ejection fraction (HFrEF) in the last century. In addition to HFrEF, they are prescribed for a variety of diseases in cardiology from hypertension to HF, angina, and stable coronary artery disease (CAD). The increased prescription of beta blockers in conditions like HF with preserved ejection fraction (HFpEF), and stable CAD may be doing more harm than good as per the data we have so far. The available data shows that beta blockers are associated with increased stroke risk and atrial fibrillation (AF) in hypertension and in patients with HFpEF, they have been associated with decreased exercise capacity. In patients with stable CAD and patients with myocardial infarction with normal systolic functions, beta blockers don't offer any mortality benefit. In this article, we critically review the common indications and the uses of beta blockers in patients with HFpEF, CAD, hypertension and AF and we propose that beta blockers are overprescribed under the shadow of their beneficial effects in patients with HFrEF.

Separation of the Enantiomers of β-Blockers Using Brush Type Chiral Stationary Phase Derived from Conformationally Rigid α-Amino β-Lactam

  • Pirkle, William H.;Lee, Won-Jae
    • Bulletin of the Korean Chemical Society
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    • v.31 no.3
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    • pp.620-623
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    • 2010
  • A brush type chiral stationary phase (CSP 2) derived from ${\alpha}$-amino ${\beta}$-lactam was prepared for the separation of the enantiomers of ${\beta}$-blockers. Compared to the CSP derived from ${\alpha}$-amino phosphonate (CSP 1), in general, the conformationally rigid CSP 2 showed greater scope and much enhanced enantioselectivity for the resolution of ${\beta}$-blockers. The effect of various salt additives on enantioseparation of ${\beta}$-blockers in the mobile phase was investigated. The unusual effect of temperature on the chromatographic behaviors was observed on CSP 2. It also afforded appreciable increases in enantioselectivity without significantly affecting resolution, as the column temperature was reduced.

Are Beta Blockers New Potential Anticancer Agents?

  • Akbar, Shahid;Alsharidah, Mansour Saleh
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.22
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    • pp.9567-9574
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    • 2014
  • ${\beta}$-Blockers have been one of the most widely used and versatile drugs for the past half a century. A new potential for their use as anti-cancer drugs has emerged in the past few years. Various retrospective case control studies have been suggestive that use of ${\beta}$-blockers before the diagnosis of cancer could have preventive and protective effects against non-small cell lung carcinoma, melanoma, and breast, pancreatic and prostate cancers. Experimental and clinical observations are still inconclusive with some inconsistent findings. However, indications are pointing toward a positive role of some ${\beta}$-blockers against certain forms of cancers. This mini review is an effort to present the up to date published results of case-control studies and experimental findings.

Characterization of Adsorbents for the Simultaneous Solid-Phase Extraction of Trace $\beta$-Blockers from Biological Samples (생체시료로부터 미량 $\beta$-Blockers의 동시고상추출에 사용될 흡착제들의 특성)

  • Kim, Kyoung Rae;Kim, Do Jeong
    • Analytical Science and Technology
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    • v.6 no.4
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    • pp.375-381
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    • 1993
  • The efficiencies of four different solid absorbents were evaluated for the simultaneous solid-phase extraction of six ${\beta}$-blockers from biological sample. Chromosorb 107 using methanol as the eluting solvent gave the highest solid-phase extraction yield. From the breakthrough studies of ${\beta}$-blockers, the excellent sorption and desorption properties of the Chromosorb 107 column were verified. The usefulness of Chromosorb 107/methanol was examined for the simultaneous solid-phase extraction of the ${\beta}$-blockers from serum in the concentration range of 2~8ppm.

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Analysis of $\beta$-blockers Use in Chronic Heart Failure

  • Kang, Hyo-Jin;Lee, Suk-Hyang
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.249.2-250
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    • 2003
  • ${\beta}$-blockers are considered as standard therapy for patients with stable chronic heart failure (CHF) and to prolong survival and reduce hospitalizations. We examined the effects of the ${\beta}$-blocker on mortality, hospitalization and symptoms in patients with CHF and the related factors to the use of ${\beta}$-blockers. Patients in New York Heart Association class II-IV were included if they were treated for heart failure from January 2002 to June 2002. At baseline, 6 months, and 12 months, they were assessed for the change of NYHA class and all deaths and hospital admissions. (omitted)

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Chiral Separation of ${\beta}-Blockers$ after Derivatization with a New Chiral Derivatization Agent, GATC

  • Ko, Mi-Young;Shin, Dae-Hong;Oh, Joung-Weon;Asegahegn, Workaferhaw Shibru;Kim, Kyeong-Ho
    • Archives of Pharmacal Research
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    • v.29 no.11
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    • pp.1061-1065
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    • 2006
  • A new chiral derivatization agent with sugar moiety, 2,3,4,6-tetra-O-acetyl-${\beta}$-D-galactopyranosyl isothiocyanate (GATC) was synthesized. Several ${\beta}-blockers$ were investigated for the possible separation of the enantiomers by reversed-phase HPLC after derivatization with this new chiral derivatization agent (GATC). GATC was reacted readily with ${\beta}-blockers$ at room temperature and the reaction mixture could directly be injected into the HPLC system. The corresponding diastereomers were well resolved on an ODS column with acetonitrile-ammonium acetate buffer as a mobile phase and monitored at UV 254 nm. The optimization of the derivatization procedure (concentration of GATC, reaction temperature and time) and HPLC conditions (pH and ionic strength of mobile phase) were investigated and compared with GITC.

β-Adrenergic Receptors : New Target in Breast Cancer

  • Wang, Ting;Li, Yu;Lu, Hai-Ling;Meng, Qing-Wei;Cai, Li;Chen, Xue-Song
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.18
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    • pp.8031-8039
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    • 2016
  • Background: Preclinical studies have demonstrated that ${\beta}$-adrenergic receptor antagonists could improve the prognosis of breast cancer. However, the conclusions of clinical and pharmacoepidemiological studies have been inconsistent. This review was conducted to re-assess the relationship between beta-adrenoceptor blockers and breast cancer prognosis. Materials and Methods: The literature was searched from PubMed, EMBASE and Web of Nature (Thompson Reuters) databases through using key terms, such as breast cancer and beta-adrenoceptor blockers. Results: Ten publications met the inclusion criteria. Six suggested that receiving beta-adrenoceptor blockers reduced the risk of breast cancer-specific mortality, and three of them had statistical significance (hazard ratio (HR)=0.42; 95% CI=0.18-0.97; p=0.042). Two studies reported that risk of recurrence and distant metastasis (DM) were both significantly reduced. One study demonstrated that the risk of relapse-free survival (RFS) was raised significantly with beta-blockers (BBS) (HR= 0.30; 95% CI=0.10-0.87; p=0.027). One reported longer disease-free interval (Log Rank (LR)=6.658; p=0.011) in BBS users, but there was no significant association between overall survival (OS) and BBS (HR= 0.35; 95% CI=0.12-1.0; p=0.05) in five studies. Conclusions: Through careful consideration, it is suggested that beta-adrenoceptor blockers use may be associated with improved prognosis in breast cancer patients. Nevertheless, larger size studies are needed to further explore the relationship between beta-blocker drug use and breast cancer prognosis.

Determination of Stability Constants of the Inclusion Complexes of ${\beta}$-Blockers in Heptakis (2,3-Dimethyl-6-Sulfato)- ${\beta}$-Cyclodextrin

  • Phuong, Nuyen Thi;Lee, Kyung-Ah;Kim, Kyung-Ho;Choi, Jung-Kap;Kim, Jong-Moon;Kang , Jong-Seong
    • Archives of Pharmacal Research
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    • v.27 no.12
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    • pp.1290-1294
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    • 2004
  • The ${\beta}$-blockers possess at least one chiral center and the S(-)-enantiomer shows higher affinity for binding to the ${\beta}$-adrenergic receptors than antipode. The stability constants of acebutolol, celiprolol, propranolol and terbutaline in the inclusion complexes with single-isomer heptakis (2,3-dimethyl-6-sulfato)- ${\beta}$-cyclodextrin (HDMS-${\beta}$-CD) were determined by capillary electrophoresis. The approximation and linear double reciprocal methods were adapted with comparable results. Among the ${\beta}$-blockers studied, propranolol had the lowest stability constant but the highest enantioselectivity, indicating that the magnitudes of the stability constants carried little information about enantioseparation. The magnitudes of enantioselectivities between the enantiomer pair were in the order of propranolol > celiprolol > terbutaline > acebutolol.

Pharmacological Studies on the Antihypertensive Effects of Cinnarizine Coadministered with Propranolol or Metoprolol(III) -Effects on Biochemical Changes- (Cinnarizine을 Propranolol이나 Metoprolol과 병용할 때의 혈압강하효과(血壓降下效果)에 관한 약리학적(藥理學的) 연구(硏究)(III) -생화학적(生化學的) 변화(變化)에 대한 영향-)

  • Huh, In-Hoi;Ann, Hyung-Soo
    • YAKHAK HOEJI
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    • v.28 no.5
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    • pp.265-273
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    • 1984
  • The effects of cinnarizine, $Ca^{2+}-antagonist$, on the antihypertensive effect of coadministered ${\beta}-blockers$, propranolol and metoprolol, were investigated in SHR. Drugs were coadministered orally for 4 weeks. Hemodynamic and biochemical changes induced by above drugs were determined to elucidate their mechanism of action. a) Cardiohypertropy of SHR was significantly improved by the treatment of ${\beta}-blockers$ as well as combination with cinnarizine and ${\beta}-blockers$. b) $Mg^{2+}-contents$ were increased in ventricle and decreased in plasma and aorta in all of the groups, especially in the group of propranolol with cinnarizine. c) c-GMP contents in ventricle were increased when cinnarizine was coadministered with propranolol, and c-GMP contents in aorta were increased when cinnarizine was coadministered with metoprolol, camparing with propranolol or metoprolol alone-treated group. d) Plasma renin activity appeared to be increased in cinnarizine treated alone, but reduced by combination with ${\beta}-blockers$. e) Triglycerides and $Na^+$ contents in serum were decreased in the group of metoprolol with cinnarizine, comparing with metoprolol alone-treated group. Increased $K^+\;and\;Ca^{2+}$excretions in urine by ${\beta}-blockers$ were inhibited by cinnarizine, so $Na^+/K^+$ excretion ratios were increased. Diuretic effects was showed in metoprolol alone treated group, but reduced when coadministered with cinnarizine.

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Chiral separation of $\beta$-blockers after derivatizalion wilh a new chiral derivalizalion agen1.GATC and Comparison wilh GITC on derivalizing conditions and chromalographic paramelers

  • Ko, Mi-Young;Shin, Dae-Hong;Seo, Sang-Hun;Kim, Kyeong-Ho
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.398.1-398.1
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    • 2002
  • A new chiral derivatization agent with sugar moiety. 2, 3.4, 6-tetra-O-acetyl-D-galactopyranosyl isothiocyanate (GATC) was synthesized. Several $\beta$-blockers were investigated for the possible separation of the enantiomers by reversed-phase HPLC after derivatization with this new chiral derivatization agent (GATC). GATC was reacted readily with $\beta$-blockers at room temperature and the reaction mixture could directly be injected into the HPLC system. (omitted)

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