• Title/Summary/Keyword: $\beta$-Blockers

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Medical Management of Patients With Heart Failure and Reduced Ejection Fraction

  • Barry Greenberg
    • Korean Circulation Journal
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    • v.52 no.3
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    • pp.173-197
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    • 2022
  • Treatment options for patients with heart failure (HF) with reduced ejection fraction (HFrEF) have expanded considerably over the past few decades. Whereas neurohormonal modulation remains central to the management of patients with HFrEF, other pathways have been targeted with drugs that have novel mechanisms of action. The angiotensin receptor-neprilysin inhibitors (ARNIs) which enhance levels of compensatory molecules such as the natriuretic peptides while simultaneously providing angiotensin receptor blockade have emerged as the preferred strategy for inhibiting the renin angiotensin system. Sodium glucose cotransporter 2 (SGLT2) inhibitors which were developed as hypoglycemic agents have been shown to improve outcomes in patients with HF regardless of their diabetic status. These agents along with beta blockers and mineralocorticoid receptor antagonists are the core medical therapies for patients with HFrEF. Additional approaches using ivabradine to slow heart rate in patients with sinus rhythm, the hydralazine/isosorbide dinitrate combination to unload the heart, digoxin to provide inotropic support and vericiguat to augment cyclic guanosine monophosphate production have been shown in well-designed trials to have beneficial effects in the HFrEF population and are used as adjuncts to the core therapies in selected patients. This review provides an overview of the medical management of patients with HFrEF with focus on the major developments that have taken place in the field. It offers prospective of how these drugs should be employed in clinical practice and also a glimpse into some strategies that may prove to be useful in the future.

Drug Use Evaluation of Antihypertensive Agents by JNC VI Guidelines (고혈압 치료 지침 Vl에 의한 항고혈압제의 사용평가)

  • Kim, Kyung Hwa;Lee, Suk Hyang
    • Korean Journal of Clinical Pharmacy
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    • v.12 no.1
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    • pp.29-38
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    • 2002
  • Hypertension is an important public health problem because it increases the risk of stroke, angina, myocardial infarction, heart failure, and end-stage renal disease. If it is not actively treated, morbidity and mortality increase with hypertension-induced complications and quality of life decreases. This study was to evaluate the use of antihypertensive drugs and blood pressure changes and to compare algorithms chosen (or the 1st and 2nd line therapy of hypertension based on the JNC VI recommendations. The medical charts of 222 patients with essential hypertension at St. Vincent's Hospital in Suwon from January 1997 to January 2000 were reviewed retrospectively. Data collection and analysis included baseline BP underlying diseases and complications, administered antihypertensives, BP changes, changes of antihypertensive regimen, and adverse effects with treatments. As results, the higher BP the patients had, the more frequent they had target organ damages and clinical cardiovascular diseases. Mean duration to reduce blood pressure less than 140/90 mmHg was 8 weeks in $85.3\%$ of the patients. The rate of control in BP was $82.4\%$ at 6 months. The major antihypertensive drugs prescribed were calcium channel blockers $(61.8\%)$ , ACE inhibitors $(19.1\%),\;\beta-blockers\;(13.7\%)$ and diuretics $(5.3\%)$ as the 1st-line monotherapy. The methods of treatment used as the 1st-line therapy were monotherapy$(59\%)$ and combination therapy $(41\%)$. Blood pressure change was significantly greater for combination therapy than monotherapy$(-26.2\pm21.4\;vs.\;-18.56\pm16.7$ mmHg for systolic blood pressure; P<0.003, $-16.9\pm13.2\;vs.\;-9.2\pm12.8$ mmHg for diastolic blood pressure; p<0.001). When blood pressure was not completely controlled with the first antihypertensive selected, the 2nd line therapy had 4 options: addition of 2nd agent from different class; $66.2\%$, substitution with another drug, $21.9\%$ increase dose $11.9\%$ continue first regimen $27.9\%$ Calcium channel blockers were the most frequently prescribed agents. This was not comparable to the JNC VI guideline which recommended diuretics and $\beta-blockers$ for the 1st-line therapy. Most of patients achieved the goal BP and maintained it until 6 months, but the remaining patients should be controlled more tightly to improve their BP with combination of life style modification, patient education, and pharmacotherapy.

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β-Adrenergic Receptor and Insulin Resistance in the Heart

  • Mangmool, Supachoke;Denkaew, Tananat;Parichatikanond, Warisara;Kurose, Hitoshi
    • Biomolecules & Therapeutics
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    • v.25 no.1
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    • pp.44-56
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    • 2017
  • Insulin resistance is characterized by the reduced ability of insulin to stimulate tissue uptake and disposal of glucose including cardiac muscle. These conditions accelerate the progression of heart failure and increase cardiovascular morbidity and mortality in patients with cardiovascular diseases. It is noteworthy that some conditions of insulin resistance are characterized by up-regulation of the sympathetic nervous system, resulting in enhanced stimulation of ${\beta}$-adrenergic receptor (${\beta}$AR). Overstimulation of ${\beta}$ARs leads to the development of heart failure and is associated with the pathogenesis of insulin resistance in the heart. However, pathological consequences of the cross-talk between the ${\beta}$AR and the insulin sensitivity and the mechanism by which ${\beta}$AR overstimulation promotes insulin resistance remain unclear. This review article examines the hypothesis that ${\beta}$ARs overstimulation leads to induction of insulin resistance in the heart.

The Relationship of in vitro Dissolution and Intestinal Membrane Permeability with in vivo Bioavailability (시험관내 용출 및 장관막 투과도와 생체이용률과의 상관성)

  • 서수경;손수정;박인숙;최기환;김순선;유태무;조혜영;이용복;김동섭
    • YAKHAK HOEJI
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    • v.44 no.5
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    • pp.424-431
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    • 2000
  • A biopharmaceutics drug classification system for correlation between in vitro dissolution and in vivo bioavailability is proposed based on recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling the rate and extent of drug absorption. The objective of this study was to assess whether in vitro dissolution profiles of immediate-release beta-blocker tablets can be correlated with intestinal membrane permeability and/or in vivo bioavailability In vitro dissolution of the beta-blocker tablets was examined using KP VII Apparatus II methods at various pH. Intestinal membrane permeability was determined in vitro using the diffusion chamber method. Bioavailablity parameters were cited from literatures. The dissolution profiles did not accurately represent the in vivo bioavailablity However there were good correlations between intestinal membrane permeability and log P (noctanol/buffer). The correlations obtained in this study indicated that in vitro diffusion chamber method could be used to predict intestinal absorption in vivo.

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Retrospective Evaluation for Efficacy and Tolerance of beta-blocker in Heart Failure Patients with Concomitant Diabetes (당뇨를 동반한 심부전 환자에 대한 beta-blocker의 유효성 평가)

  • Jang, Sun-Mi;Kang, Min-Hee;Lim, Sung-Cil;Lee, Jun-Seop;Lee, Myung-Koo
    • Korean Journal of Clinical Pharmacy
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    • v.16 no.2
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    • pp.113-122
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    • 2006
  • Purpose: A retrospective study was performed to assess the efficacy and tolerance of ${\beta}-blocker$ administration in patients with heart failure and diabetes. Method: Records of 164 patients who were treated for the heart failure condition more than a year were studied retrospectively. Patients were divided into 4 groups based on their diabetes(DM) status and the administration of ${\beta}-blockers$ ($DM+{\beta}-blocker$ group: 14, DM w/o ${\beta}-blocker$: 19, No DM + ${\beta}-blocker$: 62, No DM + no ${\beta}-blocker$: 69). All patients had been receiving conventional therapy such as digoxin, ACE-I, ARB, diuretics, nitrates, aspirin, anticoagulants or lipid-lowering agents. The primary endpoints (death and hospital admission) were recorded during 1 year period and hemodynamic factors (HR, LVEF, SBP, DBP) were obtained from all patient groups before and after 12 months of ${\beta}-blocker$ treatment. To evaluate toxicity of ${\beta}-blocker$, SCr, BUN, AST, ALT and Alkaline phosphatase were obtained. Result: There were less death and hospital admission in DM + ${\beta}-blocker$ group than in DM without ${\beta}-blocker$ group (p=0.014). Relative risk of hospital admission for $DM+{\beta}-blocker$ group over no DM group was 1.17. Long term ${\beta}-blocker$ administration was associated with an improvement of heart rate in patients with DM (P< 0.02) with no significant improvement of LVEF, SBP, DBP. in DM patient. In patient without DM, ${\beta}-blocker$ was associated with improvement in LVEF, HR and DBP (P<0.01, P<0.03), but not in SBP. The incidence of toxicity was similar between the four group with no significant difference. Conculsion: Treatment of heart failure patients with ${\beta}-blocker$ appears to be beneficial in terms of hospital admission event and several hemodynamic factors. The toxicities of ${\beta}-blocker$ treatment were not significant and the treatment is generally well-tolerated in most of the heart failure patients.

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Congenital LQT Syndromes: From Gene to Torsade de Pointes

  • Carmeliet, Edward
    • The Korean Journal of Physiology and Pharmacology
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    • v.6 no.1
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    • pp.1-7
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    • 2002
  • Congenital Long QT syndrome (LQTs) is a relatively rare pathologic disorder but results frequently in sudden cardiac death. Of the six LQTs that have been clinically described, five have been worked out for their genetic and biophysical profile. Most are generated by mutations which cause a loss of function in two delayed $K^+$ currents, $i_{Ks}\;and\;i_{Kr}.$ One syndrome is generated by mutations in the $Na^+$ channel which causes essentially a gain of function in the channel. Clinically the syndromes are characterized by slowed repolarization of the cardiac ventricular action potential and the occurrence of typical arrhythmias with undulating peaks in the electrocardiogram, called Torsade de Pointes. Arrhythmias are initiated by early or delayed afterdepolarizations and continue as reentry. Triggers for cardiac events are exercise (swimming; LQT1), emotion (arousal; LQT2) and rest/sleep (LQT3). ${\beta}-blockers$ have a high efficacy in the treatment of LQT1 and LQT2. In LQT3 their use is questionable. The study of congenital LQTsyndromes is a remarkable example of how basic and clinical science converge and take profit of each other's contribution.