Launching Simposium PIT IDI Kota Bogor 2013

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1. BETA BLOCKER USE IN CARDIOVASCULAR DISEASES Dr. dr. Hendro Darmawan, SpJP, FIHA PIT VI IDI Kota Bogor, 9 Nopember 2013 2. CVD (focused on) : 3. Classification of…
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  • 1. BETA BLOCKER USE IN CARDIOVASCULAR DISEASES Dr. dr. Hendro Darmawan, SpJP, FIHA PIT VI IDI Kota Bogor, 9 Nopember 2013
  • 2. CVD (focused on) :
  • 3. Classification of β-blockers Table 6: Classification of ß-blockers 1st Generation Non-selective Propranolol 2nd Generation β1-selective Atenolol Metoprolol Betaxolol Bisoprolol 3rd Generation Additional properties, for example vasodilation Carvedilol Nebivolol
  • 4. 1-selectivity of various blockers Bisoprolol 1:75 Atenolol Betaxolol 1:35 1:35 Metoprolol increasing ß 1-selectivity 1:20 no selectivity 1.8:1 Propranolol increasing ß 2-selectivity 300:1 ICI 118.551 Ratio of constants of inhibition Wellstein A et al. J Cardiovasc Pharmacol 1986; 8 (Suppl. 11): 36-40 Wellstein A et al. Eur Heart J 1987; 8 (Suppl. M): 3–8
  • 5. Beta 1 VS Beta 2 Selectivity
  • 6. Elimination routes of various beta blockers from body
  • 7. MECHANISM OF BETA BLOCKERS IN HEART FAILURE  Upregulation of β receptors and improved β      adrenergic signaling. Reducing the hyperphosphorylation of calcium release channels of sarcoplasmic reticulum and normalizing their function Bradycardia (↑ coronary blood flow and decreased myocardial oxygen demand). Protection from catecholamine myocyte toxicity. Suppression of ventricular arrhythmias. Anti-apoptosis. β2 receptors, which are relatively increased, are coupled to inhibitory G protein & block apoptosis.
  • 8. Mechanism of β-blocker benefits in ischemic heart disease • Reduction in myocardial oxygen requirements via a decrease in heart rate, blood pressure and ventricular contractility. • Slowing of the heart rate prolongs coronary diastolic filling period. • Redistribution of coronary
  • 9. Mechanism of β-blocker benefits in ischemic heart disease • Increases threshold to ventricular fibrillation. • Reduction in infarct size and reduction in the risk of cardiac rupture. • Reduction in the rate of reinfarction. • Regression of the atheromatous
  • 10. Summary of Trials of Beta-Blocker Therapy Phase of Treatment Total No. Patients RR (95% CI) Acute treatment 28,970 0.87 (0.77-0.98) Secondary prevention 24,298 0.77 (0.70-0.84) Overall 53,268 0.81 (0.75-0.87) 2 1 0.5 Relative risk (RR) of death Placebo Beta blocker better better Antman E, Braunwald E. Acute Myocardial Infarction. In: Braunwald E, Zipes DP, Libby P, eds. Heart Disease: A textbook of Cardiovascular Medicine, 6th ed., Philadelphia, PA: W.B. Sanders, 2001, 1168.
  • 11. MAINTATE Usefulness of beta-blocker therapy in patients with diabetes mellitus and CAD (BIP) 1.00 0.90 0.85 Mortality 42% Withß-blockers Withoutß-blockers 0.80 P = 0.0001 0.75 1 14.417 pts 2 3 Year 4 5 Jonas et al. Am J Cardiol 1996; 77: 1273 et seqq. Survival rate 0.95
  • 12. BP and -BLOCKERS Central effects Baroreceptor reflexes  Carotid sinus ? Stellate ganglion NE   E  Renin  Sinus rate Stroke volume Cardiac output Terminal neurone Angio I Angio II Systemic vascular resistance NE  Initial rise then fall
  • 13. BisoDIAS Endgültig 28 Bisoprolol: Long-term treatment of hypertension 140 SBP(mm Hg) 100 DBP(mm Hg) HR(beats/min) 60 0 n = 102 12 15 18 21 24 27 30 33 36 months 102 97 102 101 102 102 102 100 102 Giesecke HG et al. J Cardiovasc Pharmacol 1990; 16 (Suppl 5): 175 180
  • 14. This is how braunwald’s textbook summarizes the use of betablockers in hypertension  “Beta blockers are specifically recommended for hypertensive patients with concomitant coronary disease, particularly after a myocardial infarction, congestive heart failure, or tachyarrhythmias.”  “If a beta blocker is chosen, the agents that are more cardioselective offer the likelihood of fewer perturbations of lipid and carbohydrate metabolism and, because of fewer side effects (except for bradycardia), better adherence to therapy.”  “Long-acting formulations are better for once-daily dosing.” Page 945 braunwald’s textbook of medicine 9th edition
  • 15. From: Cardiovascular Protection Using Beta-Blockers: A Critical Review of the Evidence J Am Coll Cardiol. 2007;50(7):563-572. doi:10.1016/j.jacc.2007.04.060 Figure Legend: Proposed Use of Beta-Blockers for Hypertension In patients with uncomplicated hypertension, beta-blockers should not be used as first-line agents. However, in patients with uncontrolled hypertension on various other antihypertensive agents and in those with complicated hypertension, betablockers should be considered in the armamentarium of treatment. CHF = chronic heart failure; MI = myocardial infarction. College of Cardiology. Copyright © The American All rights reserved.
  • 16. Bisoprolol experience in Indian patients Mar 2012
  • 17. Bisoprolol in hypertension Objectives: This study was aimed to evaluate the efficacy and tolerability of bisoprolol, in Indian patients diagnosed with stage I essential hypertension as first line drug. Primary and secondary outcomes measures: The primary outcome measure was percentage of patients achieving blood pressure (BP) <140/90 mm Hg at the end of 12 weeks, while Channaraya V, Marya RK, Somasundaram M, et al. BMJ Open 2012;2:e000683 multiple secondary outcome 
  • 18. RESULT 2131 (96.44%) patients n: 2418 achieved BP control.
  • 19. Different beta blockers and sexual dysfunction versus placebo
  • 20. Conclusion: Cardioselective beta-blockers (Bisoprolol) is important part of CVD management
  • 21. THANK YOU!
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