Beta-Blockers and Heart Rate-Lowering Agents Pharmacology

Vocabulary-style flashcards covering nonselective, beta-1 selective, mixed alpha/beta blockers, and heart rate-lowering agents based on clinical uses, selectivity, adverse effects, and key clinical pearls.

Propranolol (Inderal)

A 1st generation nonselective $\beta_1 + \beta_2$ blocker used for HTN, angina, arrhythmias, essential tremor, migraine prophylaxis, hyperthyroidism, and portal hypertension. It is highly lipophilic (causing CNS effects) and should be avoided in asthma/COPD.

Nadolol (Corgard)

A 1st generation nonselective $\beta_1 + \beta_2$ blocker indicated for HTN and angina, characterized by a long half-life and renal elimination.

Timolol (Blocadren)

A 1st generation nonselective $\beta_1 + \beta_2$ blocker used for HTN and ophthalmic glaucoma. Ophthalmic drops can still produce systemic $\beta$-blockade.

Pindolol (Visken)

A 1st generation nonselective $\beta_1 + \beta_2$ blocker with Intrinsic Sympathomimetic Activity (ISA) used rarely for hypertension; it results in less resting bradycardia.

Penbutolol (Levatol)

A 1st generation nonselective $\beta_1 + \beta_2$ blocker with Intrinsic Sympathomimetic Activity (ISA) and partial agonist activity, used for hypertension.

Sotalol (Betapace)

A 1st generation nonselective $\beta_1 + \beta_2$ blocker with Class III antiarrhythmic properties used for atrial and ventricular arrhythmias. Requires monitoring of QT interval and renal function due to risks of QT prolongation and torsades.

Metoprolol (Lopressor, Toprol XL)

A 2nd generation $\beta_1$-selective blocker used for HTN, HF, angina, MI, and AF rate control. It is one of three $\beta$-blockers proven to reduce mortality in HFrEF, and its levels are increased by CYP2D6 inhibitors (fluoxetine, paroxetine).

Atenolol (Tenormin)

A 2nd generation $\beta_1$-selective blocker used for HTN and angina that is renally eliminated.

Bisoprolol (Zebeta)

A 2nd generation $\beta_1$-selective blocker used for HTN and heart failure; it is one of three $\beta$-blockers proven to reduce mortality in HFrEF.

Esmolol (Brevibloc)

A 2nd generation $\beta_1$-selective ultra-short acting IV $\beta$-blocker with a $\text{half-life} \thinspace \text{of} \thinspace \thicksim 9 \thinspace \text{minutes}$, used for acute tachyarrhythmias and perioperative HTN.

Acebutolol (Sectral)

A 2nd generation $\beta_1$-selective blocker with Intrinsic Sympathomimetic Activity (ISA) and partial agonist activity, used for HTN and arrhythmias.

Betaxolol (Kerlone)

A 2nd generation $\beta_1$-selective blocker used for HTN, with a topical form used for glaucoma.

Nebivolol (Bystolic)

A 2nd generation $\beta_1$-selective blocker that causes additional vasodilation via nitric oxide (NO) release, used for hypertension.

Carvedilol (Coreg)

A 3rd generation mixed $\beta_1 + \beta_2 + \text{a}_1$ blocker used for heart failure, HTN, and post-MI LV dysfunction. It is one of three $\beta$-blockers proven to reduce mortality in HFrEF and should be taken with food.

Labetalol (Normodyne, Trandate)

A 3rd generation mixed $\beta_1 + \beta_2 + \text{a}_1$ blocker. It is the preferred IV agent for hypertensive emergencies and is commonly used during pregnancy.

Ivabradine (Corlanor)

An $I_f$ ("funny") channel inhibitor (not a $\beta$-blocker) indicated for HFrEF with resting $\text{HR} \thicksim 70 \thinspace \text{bpm}$ despite maximally tolerated $\beta$-blockers. Lowers heart rate without affecting contractility or blood pressure; unique adverse effects include luminous phenomena (phosphenes).

Mortality-Reducing Beta-Blockers in HFrEF

The three $\beta$-blockers proven to reduce mortality in Heart Failure with Reduced Ejection Fraction (HFrEF): Metoprolol (Toprol XL), Bisoprolol (Zebeta), and Carvedilol (Coreg).