E2: Beta Adrenergic Antagonists Flashcards by Jenna Wilkerson

Nonselective beta-blocker (which receptors)
Lipophilicity

Propranolol-Inderal
ß1,ß2
high lipophilicity ( ↑ CNS penetration)

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Cardio selective beta-blocker (which receptors)

Atenolol-Tenormin
ß1

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mixed adrenergic antagonist
selective and vasodilating beta-blocker (which receptors)

Carvedilol-Coreg, Labetelol-trandate
ß1>ß2, α1 antagonist

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Cardio selective beta-blocker w/unique vasodilating properties (which receptors)

Nebivolol-Bystolic
ß1 (stimulate eNOS, nitric oxide producing)

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8 indications of beta blockers

Open angle glaucoma
Hypertension (Not first line agents)
Cardiac arrhythmias
Ischemic heart disease: angina and MI (Decrease work demands on the heart (by ↓ CO and HR))
Migraine prophylaxis
Stage fright/phobias
Essential tremor
Heart Failure (↓ hospitalizations/mortality)

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Dosing beta-blockers in HF and why

must TITRATE doses, can’t be started in conventional doses because negative inotropic and chronotropic effects can worsen HF initially

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General info of pharmacologic effects of beta blockers in all organs (2)

all have competitive reversible action on Beta receptors
Cardioselectivity is lost w/increasing doses

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pharmacologic effects of beta blockers in eye

↓ IOP by 25-30%
–↓aq production by ciliary epithelium
–outweighs the blockade of trabecular network outflow (ß2)

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pharmacologic effects of beta blockers in blood vessels (arteries/veins)

A. acute ↑ in vasoconstriction
1) blockade of ß mediated vasodilatory effects
2) especially non-selectives
delayed fall in TPR in arteries

B. over time and overall effect is to ↓ BP when on beta blockers
1)↓tonic sympathetic outflow to the periphery from the CNS
2) blockade of renal renin release

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what are the causes of renal renin release

↓AngII, ↓Aldosterone
↓TPR, ↓BP
↓water loss, Na+ loss, ↓vasoconstriction

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cardiac pharmacologic effects of beta blockers

1) overall ↓ force of contraction (neg. inotropic)
2) ↓ SA and AV nodal impulse conduction (neg. chronotropic) to ↓ HR
3) when sympathetic tone is high, these agents work best (little effect on resting HR)
4) some agents act as partial agonists/ intrinsic sympathomimetic activity (ISA)

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what agent acts as a partial agonist/intrinsic sympathomimetic activity (ISA)

labetalol-Trandate

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which beta blockers are Class I antiarrhythmic agents and what are their pharmacological effect

-Labetalol-Trandate, Metoprolol-Lopressor, propranolol-Inderal
-local anesthetic/membrane stabilizing action (MSA)
1) Additional blockade of Na channel dependent depolarization in heart muscle
2) may aid in antiarrhythmic actions to ↓ action potential generation therefore delaying muscle contraction

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what is intrinsic sympathomimetic activity (ISA)

stimulate receptors when NE, EPI low
1. prevents bradycardia
2. potential benefit in patients w/severe peripheral arterial disease, dyslipidemia
3. ↓ precipitation of asthma, ↓ rebound symptoms upon discont

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which beta blockers are Class II antiarrhythmic agents and what are their pharmacological effect

All beta blockers
delay action potential generation

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-What class antiarrhythmic agent are beta blockers

Class II antiarrythmic agnets
or
Class I

pharmacologic effects of beta blockers in ischemic heart disease

↓HR, ↓contractility, –> ↓O2 demands –> ↓ ischemia in heart
beta blockers produce a fall in O2 consumption

beta blockers that have ISA have been show to _____ _________ in angina and MI patients
Drug ex

↑ mortality
Labetalol-Trandate

beta blocker indication in heart failure

in HF, cardiac remodeling observed (heart becomes larger, more globular)
Beta blocker: slow/reverse the detrimental effects resulting from chronic endogenous adrenergic stimulation
↓ SNSA, ↓tachycardia
↓ arrhythmia potential
5.↑ LVEF w/long term therapy
↓RAAS

ADR of beta blockers

1) CNS: drowsiness, fatigue, depression (more likely w/lipophyllic B-blockers)
2) Cardiac: bradycardia, heart block
3) pulmonary (ß2): bronchospasm and asthma exacerbation (non-cardioselectives&raquo_space;cardioselectives)

DI of beta blockers
CI of beta blockers

Calcium channel blockers w/cardio depressant effects
Verapamil-Calan, Diltiazem-Cardiazem

CI:
bronchospastic reactive disease
– mild: advantages > risks
–severe disease: selectives and non-selectives are CI

heart block, bradycardia

Warnings/Precautions of Beta blockers

abrupt cessation can cause rebound angina/ischemic cardiac effect
1. FDA black-box warning
2. beta receptor supersensitivity may occur w/LT use (effector organs may ↑ receptor #s when antagonists given)
3. rebound effect more likely in drugs w/short t1/2 and pre-existing ischemic heart disease (propranolol, metoprolol tartrate-Lopressor)

What can happen to the # of post-synaptic receptors w/LT use of beta blocker’s? What must be done to combat this?

supersensitization (↑ number of post-synaptic receptors
Taper dose upon withdrawal

4 components of the ß blocker SAR

Aryl
Oxy
Propranol
Amine

Substitution off amine leads to ____ receptor binding over _____ receptors for beta blockers

beta binding over alpha

most beta antagonists contain ______ bridges

oxymethylene

ß1 selective agents have ________ ________ _______

1 aromatic ring; para substituent

ß1ß2 non-selective antagonists have ______ ______ ______

2 aromatic rings

________ adrenergic antagonists tend to be more hydrophillic

selective B1 adrenergic antagonists

Atenolol-Tenormin Class Use Chemistry

Class: beta-1 selective adrenergic antagonist Use: angina, post MI, HTN Chemistry: hydrophyllic, doesn't cross BBB

Esmolol-Brevibloc IV Class Pharmacokinetics Uses

Class: beta-1 selective antaongist Pharmacokinetics: ultra short acting, hydrolysis of plasma esterases excreted as zwitteronic metabolite Use: perioperative HTN and antiarrhythmic

Metoprolol tartrate-Lopressor Class Use

Class: beta-1 selective (cardioselective) adrenergic antagonists Use: HTN, hyperthyroidism, arrythmia, MI

Metoprolol succinate- Toprol XL Class Use Pharmacology DIs

beta-1 selective cardioselective adrenergic antagonist Use: Heart failure, arrythmia, HTN, hyperthyroidism Pharmacology: antiarrythmic w/MSA Metabolized by CYP26, inhibited by diphenhydramine, fluoxetine-Prozac

Nebivolol-Bystolic Class Indication MOA Important pharmacology Warning

3rd gen B1 cardioselective antagonist w/vasodilating properites Indication: HTN, prevent arrythmias MOA: cardioselective B1 adrenergic receptor antagonist Important pcol: stimulate eNOS, suppression of renin Warning: taper dose w/discont.; CYP2D6 metabolism

Labetalol-Trandate Class: Indication: MOA:

Non-selective beta blocker w/alpha-1 blockade (mixed alpha-1 + beta-1, beta-2 antagonist) Indication: chronic HTN, hypertensive emergencies, HTN during PG MOA: reversible blockade of a1,B1,B2 in competition w/NE or EPI

Carvedilol-Coreg Dosing: Class: Indication: MOA:

Dose: Requires titration, take w/food Indication: HTN, HF, Post-MI MOA: net effect is reversible blockade of a1,B1,B2 in competition w/NE or EPI