Adrenergics and Adrenergic Blockers

I. Adrenergics/ Sympathomimetics
• mimic effects of NE by stimulating SNS.

A. Effects of Adrenergics at receptor sites

Alpha 1 Receptors Alpha 2 receptors

• vasoconstriction (skin & mucous membrane) • decrease NE release

• increase BP • decrease BP
• pupil dilation • decrease GI motility
• closure of urinary bladder sphincter
• thickened salivary secretions
• goosebumps
• ejaculation

Beta 1 receptors Beta 2 receptors

 increase HR  bronchodilation
 Increase cardiac contraction  vasodilation (skeletal muscle)
 increase cardiac conduction  relaxation of uterus
 lipolylis  relaxation of GIT & decrease GI secretions
 relaxation fo urinary bladder
 increase blood sugar

B. Inactivation of NE:
1. reuptake of NE back into the neuron.
2. enzymatic degradation - MAO & COMT
3. diffusion away from transmitter

C. Classification of Adrenergics/ Sympathomimetics

I. Direct Acting Adrenergic

• epinephrine

II. Indirect Acting Adrenergic

• amphetamine

III. Mixed Acting Adrenergic

• ephedrine
A. Nonselective Adrenergics
 endogenous catecholamines
• epinephrine*
• norepinephrine
• dopamine

 synthetic catecholamine
• dobutamine

Epinephrine

Indications: tx of allergic reaction, anaphylaxis, bronchospasm, cardiac arrest.

Mechanism of Action (MOA):

 acts on alpha 1 , to increase vasoconstriction & BP
 acts on beta 1, to increase heart rate
 acts on beta 2, to promote bronchodilation

B. Alpha selective- adrenergics

 Alpha 1 & 2 adrenergic
• phenylephrine*

 Alpha 2 adrenergics
• clonidine
• methyldopa

phenylephrine

Indications: Tx of cold & allergies, shock

MOA: alpha adrenergic that causes vasoconstriction & increase BP

C. Beta selective adrenergics

 Beta 1 & 2 adrenergics (beta agonists)
• Isoproterenol*
• ritodrine

 Beta 2 selective adrenergics

• terbutaline
• albuterol

Isoproterenol
 Indications : tx of congestive heart failure, asthma

MOA: beta adrenergic, increases heart rate & contractility & bronchodilation

 Common S/E & adverse reactions of adrenergics:

• hypertension
• tachycardia , palpitations & tremors
• dizziness
• urinary retention
• pallor
• nausea & vomiting ( N & V)
• blood glucose may increase

 Lifethreatening effect: cardiac dysrhythmias

II. Adrenergic Blockers/ Sympatholytics

• block alpha & beta receptors, blocking sympathetic responses

A. Effects of adrenergic blockers at receptor sites:

Alpha 1 receptor Alpha 2 receptor

 vasodilation & decrease BP

 reflex tachycardia
 miosis
 suppress ejaculation
 reduce contraction of bladder sphincter & prostate
gland

Beta 1 receptor Beta 2 receptor

 decrease HR & contraction  bronchoconstriction

 uterine contraction
 decrease blood sugar

C. Classification of Adrenergic Blockers/ Sympatholytics

 Direct Acting
 Indirect acting

A. Alpha & Beta adrenergic Blockers (Nonselective Adrenergic blockers)

 carvedilol
 labetolol*
 indications: tx of hypertension & angina pectoris

MOA: blocks alpha & beta receptors in SNS causing decrease BP without
reflex tachycardia & decrease renin

B. Alpha 1 selective adrenergic blockers

 phentolamine*
 doxazosin
 prazosin

Indications: Tx of peripheral vascular disease, pheochromocytoma, acute HPN,

benign prostatic hypertrophy

MOA: blocks alpha 1, producing vasodilation & decrease BP & decrease contraction of
prostate

SE/ Adverse effects of alpha blockers:

• flush & nasal stuffiness
• orthostatic hypotension & dizziness
• reflex tachycardia

Lifethreatening effect: cardiac dysrhythmias

C. Beta 1 and 2 adrenergic blockers (Nonselective beta blockers)

 propanolol*
 sotalol
 timolol
 nadolol
 pindolol

propanolol

Indications: Tx of cardiac dysrhythmias, HPN, angina, myocardial infarction (MI)

MOA: blocks beta 1 & 2 adrenergic receptors, causes decrease HR & BP as well
as bronchoconstriction & uterine contraction

S/E & Adverse effects of beta blockers:

• bradycardia
• hypotension & dizziness
• headache
• hypoglycemia
• visual hallucinations & mood changes
• thrombocytopenia

Lifethreatening effects: laryngospasm, heart block

D. Beta 1 selective adrenergic blockers
 metoprolol*
 atenolol
 acebutolol
 esmolol
 bisoprolol
 betaxolol
 esmolol

Indications: Tx of HPN, angina pectoris , myocardial infarction

MOA: blocks beta 1, to decrease HR & BP

 Alpha blockers (ie prazosin) & beta blockers (ie propanolol, metoprolol, pindolol)
• may cause impotence or decrease in libido

E. Adrenergic Neuron blockers

 guanethidine
 guanadrel

Whatsoever you sow, that you shall reap.