Vasodilating Versus First- Generation β-blockers for Cardiovascular Protection Scott Morgan MSIII...
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Vasodilating Versus First-Generation -βblockers for Cardiovascular ProtectionScott Morgan MSIIINovember 2012
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Introduction
• Hypertension (HTN)• Defined as BP >140/90 mmHg• Prevalence in US adults is 29% or approximately 59 million• Risk factor for several diseases:• Cardiovascular (CV) • Cerebrovascular • Renovascular
• β-blockers • Discovered in mid 1960s• Were first-line HTN treatment previously• Currently falling out of favor due to side effects
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-blocker Classesβ
Generation Properties Examples
First Nonselective w/o Vasodilation Propanolol, pindolol, nadolol, tindolol, sotalol
Second β1-selective w/o Vasodilation Atenolol, bisoprolol, metoprolol
Third Nonselective w/ Vasodilation
β1-selective w/ Vasodilation
Carvedilol, bucindolol, labetalol
Nebivolol
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Vasodilating Effects
• First and Second-Generation (older generation)• No vasodilation
• Third-Generation• Nonselective w/ Vasodilation• Block vascular α-receptors• Carvedilol, bucindolol, labetalol
• β1-selective w/ Vasodilation• Increase NO• Nebivolol
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1st Generation Pharmacology• Inhibits catecholamines acting on β1-receptors in heart• Decreases HR and contractility• Leads to decrease CO (SV x HR) and BP• Decreases cardiac work and oxygen demand
• Inhibits β1-receptors on juxtaglomerular apparatus in kidneys• Decreases renin release• Leads to decreased activation of renin angiotensin
aldosterone system (RAAS)
• Inhibits presynaptic transmission in CNS• Decreases catecholamine release
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Older Gen Clinical Indications• Coronary heart disease• Heart failure• Reduce mortality by 30% in HF w/o preserved ejection
fraction• Post-myocardial infarction• Prevent catecholamine arrhythmogenic effects such as
ventricular tachyarrhymias• Chronic stable angina• Reduction in cardiovascular events• PTs with• advanced age• LV dysfunction• Anterior MI
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Older Gen for Blood Pressure
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Compliance Issues• Lethargy• Drowsiness• Depression• Peripheral vascular effects• Cold extremities
• Sexual side effects• Erectile dysfunction• Orgasmic dysfunction
• Can worsen• Diabetes mellitus• Decreased insulin release by block β2 receptors in pancreas
• COPD• PVD
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Nonselective 3rd Gen β-blockers• Carvedilol, bucindolol, metoprolol• Block vascular α-receptors
• Decreased PVR and increased glucose delivery to muscles• Increases insulin sensitivity• Normally vasodilates by NO, but vasoconstricts by SNS• Diabetes and HTN blunt NO effects allowing SNS to increase PVR
• Can raise HDL and lower LDL levels• Increases renal blood flow • Less activation of RAAS• Reduces microalbuminuria• No negative BUN/creatinine effects
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Carvedilol• Better tolerated in elderly• Body already has β-blocker like effects
• Decreased β-adrenergic response and increased catecholamine levels
• Less β-blocking effects and more vasodilation
• Less sympathetic activation• Fewer adverse effects• More compliance
• Most common side effects• HA• Dizziness• Orthostatic hypotension
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Nebivolol
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β-blocker Properties
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Summary• Third generation β-blockers are more effective at controlling
HTN than traditional
• More favorable metabolic effects• Better choice with multiple comorbid conditions• Safer in elderly and black populations
• Fewer side effects
• Older generation β-blockers are still useful for treatment of other cardiovascular diseases
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Citation
• Fares, Hassan et al. Vasodilating Versus First-Generation β-blockers for Cardiovascular Protection. Postgraduate Medicine. Volume 124; Issue 2: 7-14. March, 2011.