ADRENERGIC

ANTAGONIST

BY: MADINNE PAULINE TOLENTINO

 ADRENERGIC ANTAGONIST
• Is a drug that inhibits the function of adrenergic
receptors.
• Antagonists reduces or block the signals of
agonist, which a substance which interferes with
or inhibits the physiological action of another
• It reverses the natural cardiovascular effect,
based on the type of adrenoreceptor being
blocked. For example, if the natural activation of
the α1-adrenergic receptor leads to 
vasoconstriction, an α1-adrenergic antagonist
will result in vasodilation.
ADRENERGIC ANTAGONIST

• Some adrenergic antagonists, mostly β

antagonists, passively diffuse from the
gastrointestinal tract. From there, they bind to 
albumin and α1-acid glycoprotein in the plasma
, allowing for a wide spread through the body.
From there, the lipophilic  antagonists are
metabolized in the liver and eliminated with
urine while the hydrophilic ones are eliminated
unchanged
 ADRENERGIC ANTAGONIST
• have inhibitory or opposing effects on the receptors in the
adrenergic system
• modulates the fight-or-flight response. Since this response,
which is mostly seen as an increase in blood pressure, is
produced by the release of the
endogenous adrenergic ligands, administration of an
adrenergic antagonist results a decrease in blood pressure,
which is controlled by both heart rate and vasculature tone
• are mostly used for cardiovascular disease
• are wildly used for lowering blood pressure and relieving 
hypertension
• have a been proven to relieve the pain caused by 
myocardial infarction, and also the infarction size, which
correlates with heart rate
ADRENERGIC ANTAGONIST
Phentolamine, an adrenergic antagonist
Visual definition of an antagon
where it
compared to agonists and
reverse agonists
ADRENERGIC ANTAGONIST
• There are Three (3) common examples:
a. ALPHA BLOCKERS Alpha blockers
P Phentalomine
b. BETA BLOCKERS
Propranolol Nadolol
Nebivilol Pindolol
Atenolol Esmolol
Oxprenolol Acebutolol
Metropolol Sotalol
Talinolol Timolol
Pindolol Betaxolol
c. MIXED ACTION
Labetaol Carvetidol
 ADRENERGIC ANTAGONIST
SIDE EFFECTS AND TOXICITY
While adrenergic antagonists have been used for years,
there are multiple issues with using this class of drug. When
overused, adrenergic antagonists can result in  bradycardia, 
hypotension,  hyperglycemia and even hypodynamic shock.
This is because adrenergic stimulation by agonists, results in
normal calcium channel regulation. If these adrenergic
receptors are blocked too often, there will be an excess in
calcium channel inhibition, which causes most of these
problems.
 ADRENERGIC RECEPTORS
• Also known as ADRENOCEPTORS
• are aclassof G protein-coupled receptors that are
targets of the catecholamines, especially  
norepinephrine  (noradrenaline), a hormone which is
released by the adrenal medulla and by the
sympathetic nerves and functions as a
neurotransmitter. It is also used as a drug to raise
blood pressure; and epinephrine (adrenaline), a
hormone secreted by the adrenal glands that increases
rates of blood circulation, breathing, and carbohydrate
metabolism and prepares muscles for exertion
 ADRENERGIC RECEPTORS
• Many cells possess these receptors, and the
binding of a catecholamine to the receptor will
generally stimulate the
sympathetic nervous system. The sympathetic
nervous system is responsible for the 
fight-or-flight response, which includes dilating the 
pupil, increasing heart rate, mobilizing energy, and
diverting blood flow from non-essential organs to 
skeletal muscle.
ADRENERGIC RECEPTORS

• DIVIDED INTO TWO GROUPS:

a. beta (β) adrenergic receptors
 β1, β2, and β3
b. the alpha (α) adrenoreceptors

 α1 and α2
• Are located near the  heart,  kidneys,  lungs,and 
gastrointestinal tract
• There are also α-adreno receptors that are
located on vascular smooth muscle