Beta Receptor Antagonist

List classes of beta blockers

- first gen

- second gen

- third gen

- intrinsic sympathomimetic

- membrane-stabilizing activity

- lipophilic vs hydrophilic

Defining feature of first gen beta blockers

- blocks b1 and b2

- non-selective

Defining feature of second gen beta blockers

- B1 selective

- Dose dependent

- cardioselective

Defining feature of third gen beta blockers

a1 blockade added

Defining feature of intrinsic sympathomimetic activity beta blockers

- partial agonists

- less resting bradycardia

Defining feature of membrane-stabilizing activity beta blockers

minor local anesthetic effect

List example of non selective beta blockers

- propranolol/inderal

- nadolol/corgard

- timolol/blocarden

- pindolol/visken

- penbutolol/levatol

- sotalol/betaspace

Which non selective beta blockers have ISA activity

- pindolol

- penbutolol

Which non selective beta blockers are class III antiarrhythmic

sotalol

Major clinical uses of propranolol

- HTN

- angina

- arrhythmia

- tremor

- migraine prophylaxis

- hyperthyroidism

- portal HTN

Adverse effects of propranolol

- bradycardia

- fatigue

- depression

- bronchospasm

- sexual dysfunction

Drug interaction of propranolol

- verapamil/diltiazem: increase heart block

- digoxin: increase bradycardia

- clonidine withdrawal: masks hypoglycemia w insulin

Counseling point for propranolol

- avoid in asthma/COPD

- highly lipophilic = CNS effects

Major clinical uses of nadolol

- HTN

- angina

Adverse effects of nadolol

- bradycardia

- fatigue

Drug interaction of nadolol

- verapamil/diltiazem

- digoxin

- clonidine

Counseling point of nadolol

- long half life

- renal elimination

Major clinical use of timolol

- HTN

- glaucoma

Common adverse effects of timolol

- bradycardia

- bronchospasm

Drug interaction of timolol

additive bradycardia w Ca channel blockers

Counseling point of timolol

ophthalmic drops can still produce systemic beta-blockade

Common side effects of pindolol

HTN: rarely used

Common adverse effects of pindolol

less resting bradycardia

Major drug interaction of pindolol

- digoxin

- verapamil/diltiazem

- clonidine

Counseling point of pindolol

intrinsic sympathomimetic activity

Major clinical use of penbutolol

HTN

Common adverse effects of penbutolol

- fatigue

- dizziness

Major drug interaction of penbutolol

- diltiazem/verapamil

- digoxin

- clonidine

Counseling point of penbutolol

partial agonist activity

Major clinical use of sotalol

atrial and ventricular arrythmias

Common adverse effects of sotalol

- bradycardia

- QT prolongation

- torsades

Drug interaction of sotalol

- QT-prolonging drugs

- electrolyte abnormalities

Counseling point of sotalol

monitor QT interval and renal function

List examples of B1 selective blockers

- metoprolol: lopressor/toprol

- atenolol: tenormin

- bisoprolol: zebeta

- esmolol: brevibloc

- acebutolol: sectral

- betaxolol: kerlone

- nebivolol: bystolic

List the B1 selective blockers with other properties and what those properties are

- acebutolol: B1/ISA

- nebivolol: B1/nitric oxide release

Major clinical use of metoprolol

- HTN

- HF

- angina

- MI

- AF rate control

Common adverse effects of metoprolol

- bradycardia

- fatigue

Major drug interaction of metoprolol

- verapamil

- diltiazem

- digoxin

- CYP2D6 inhibitors

- all increase levels

Counseling point of metoprolol

1/3 to reduce mortality in systolic failure

Major clinical use of atenolol

- HTN

- angina

Common adverse effect of atenolol

- bradycardia

- fatigue

Drug interaction of atenolol

- verapamil

- diltiazem

- digoxin

- CYP2D6 inhibitors

Counseling point of atenolol

renally eliminated

Major clinical use of bisoprolol

- HTN

- heart failure

Common adverse effect of bisoprolol

bradycardia

Major drug interaction of bisoprolol

- verapamil

- diltiazem

- digoxin

- CYP2D6 inhibitors

Counseling point of bisoprolol

1/3 beta blocker to stop systolic heart failure

Major clinical use of esmolol

- acute tachyarrhythmias

- perioperative HTN

Common adverse effects of esmolol

- hypotension

- bradycardia

Major drug interaction of esmolol

- additive AV blockade

Counseling point of esmolol

ultra-short acting IV beta-blocker

Major clinical uses of acebutolol

- HTN

- arrythmias

Common adverse effects of acebutolol

fatigue

Major drug interaction of acebutolol

- verapamil

- diltiazem

- digoxin

- CYP2D6 inhibitors

Counseling point of acebutelol

partial agonist

Major Clinical Uses of betaxolol

- HTN

- glaucoma

Adverse effects of betaxolol

bradycardia

Drug interaction of betaxolol

- verapamil

- digoxin

- diltiazem

- CYP2D6 inhibitors

Counseling point of betaxolol

topical use for glaucoma

Major clinical use of nebivolol

HTN

Common adverse effect of nebivolol

- headache

- fatigue

Major drug interaction of nebivolol

CYP2D6 inhibitors increase its levels

Counseling point of nebivolol

causes additional vasodilation via NO

Give examples of mixed adrenergic blockers

- carvedilol/coreg: B1/B2/a1

- labetalol/normodyne/trandate: B1/B2/a1

Major clinical uses of carvedilol

- heart failure

- HTN

- post-MI

- LV dysfunction

Common adverse effects of carvedilol

- orthostatic hypotension

- bradycardia

- dizziness

Major drug interaction of carvedilol

- verapamil

- diltiazem

- digoxin

- insulin

- clonidine

Counseling point of carvedilol

- 1/3 beta blockers to reduce mortality from systolic heart failure

- take with food

Clinical uses of labetalol

- HTN

- hypertensive emergency

- pregnancy-induced HTN

Adverse effects of labetalol

- orthostatic hypotension

- fatigue

Major drug interaction of labetalol

- verapamil

- diltiazem

- digoxin

- insulin

- clonidine

Give example of non-beta blocker heart rate lowering agent

ivabradine/corlanor: funny channel inhibitor

Clinical use of ivabradine

systolic hear failure with resting HR >/= 70 bpm despite maximally tolerated beta-blocker

Common adverse effects of ivabradine

- bradycardia

- atrial fibrillation

- luminous phenomena: phosphenes

Drug interaction of ivabradine

- verapamil

- diltiazem

- CYP3A4 inhibitors: clarithromycin/ketoconazole

Counseling point of ivabradine

- not beta-blocker

- lowers heart rate without affecting contractility or BP