:

Adrenergic System

What is Adrenergic System ?

Adrenergic system means "having to do

with adrenaline (epinephrine) or
noradrenaline (norepinephrine)".
Uses adrenaline (epinephrine) and
noradrenaline (norepinephrine) as
neurotransmitters.

Adrenergic receptor
The adrenergic receptors (or adrenoceptors) are a class
of G protein-coupled receptors that are targets of the
catecholamines, especially norepinephrine
(noradrenaline) and epinephrine (adrenaline).
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 widening the pupils of the eye, mobilizing
energy, and diverting blood flow from non-essential
organs to skeletal muscle.

Neurotransmission at
adrenergic neurons
Neurotransmission at adrenergic neurons
closely resembles that described for the
cholinergic neurons, except that
norepinephrine is the neurotransmitter
instead of acetylcholine.

Categories of Adrenergic
receptor
There are two main groups of adrenergic
receptors, Alpha ( ) and beta ( ) , with
several subtypes :
receptors have the subtypes
1 and 2

receptors have the subtypes

1 and 2

Pharmacological effect of
activation of receptors :
Alpha 1 ( 1) :
Blood vessels : vasoconstriction , increase
peripheral resistance and increase blood
pressure
Eye : Mydriasis (dilatation of pupil)
Sphincter smooth muscle : Contraction

Diagram of effect of
1 receptors

Pharmacological effect of
activation of receptors :
Alpha 2 ( 2) :
Decrease nor epinephrine release.
Decrease insulin release

Pharmacological effect of
activation of receptors :
Beta 1 ( 1):
Heart: increase contractibility and heart rate.
Metabolism: lipolysis , increase free fatty acid
in blood.
Glands: increase rennin secretion from
juxtaglomerular.

Diagram of Pharmacological effect

of activation of 1 receptors :

Pharmacological effect of
activation of receptors :
Beta 2 ( 2 ) :
Blood vessels: dilatation ( skeletal muscles
,coronary )
Smooth muscles: relaxation ( bronchioles, git,
urinary bladder and uterus )
Metabolism: Glycogenolysis, hyperglycemia,
increase output of glycogen

Adrenergic agonist &

antagonist
An adrenergic agonist is a drug that
stimulates a response from the adrenergic
receptors
An Adrenergic antagonist is a
pharmaceutical substance that acts to
inhibit the action of catecholamines at the
adrenergic receptors.

Adrenergic agonist :
A- Direct action
Epinephrine (adrenalin) : affect all types of
adrenergic receptors.
Action:

Heart
Blood vessels
Respiratory system
Hyperglycemia
Lipolysis

Adrenergic agonist :
A- Direct action
Therapeutic uses of Epinephrine :
Asthma: in treatment of acute asthma, after few
minutes of Subcutaneous administration greatly
improved respiratory exchange is improved.
Glaucoma: In ophthalmology, a 2% Epinephrine
solution may be used topically to reduce intraocular
pressure (IOP) in open-angle glaucoma.
Anaphylactic shock: in treatment of type I
hypersensitivity reactions.
Local anesthetic

Epinephrine Drug

Adrenergic agonist :
A- Direct action
Nor epinephrine (nor adrenalin): is a
catecholamine with multiple roles including
those as a hormone and a neurotransmitter. It is
the hormone and neurotransmitter most
responsible for vigilant concentration in contrast
to its most chemically similar hormone,
dopamine, which is most responsible for
cognitive alertness. more effect on receptors.

Adrenergic agonist :
A- Direct action
Therapeutic uses:
Its never used for asthma or in combination with
local anesthetics.
it's a potent vasoconstrictor and will cause
extravasation (discharge of blood from vessel into
tissues) along the injection site.

Adrenergic agonist :
A- Direct action
Isoproternol (Isuprel) : is a medication
used for the treatment of bradycardia
(slow heart rate), heart block, and rarely
for asthma. It is a non-selective betaadrenergic agonist and structurally similar
to adrenaline.

Adrenergic agonist :
A- Direct action
Isoproternol (Isuprel) : act on receptors
(no effects)
Increase heart rate (1)
Lipolysis (1)
Pulmonary (2)
Glycogenolysis (1)

Adrenergic agonist :
A- Direct action
Dopamine: is a hormone and neurotransmitter
of the catecholamine family that plays a number
of important roles in the human brain and body.
Affects receptor at high dose and receptors
at low dose.

Dopamine Drug
Dopamine: Affects receptor at high dose
and receptors at low dose.
Action:
Cardiovascular
Renal and vesceral: dilutes renal and
splanchnic arterioles, thus increase blood
flow to the kidneys and other viscera.

Dopamine Drug
Therapeutic uses:
Shock: given by iv infusion (because of short
action), stimulate heart by 1 action, enhance
renal circulation.

Adrenergic agonist :
A- Direct action
Dobtuamine: is a sympathomimetic drug used in
the treatment of heart failure and cardiogenic
shock. Its primary mechanism is direct
stimulation of 1 receptors of the sympathetic
nervous system.

Adrenergic agonist :
A- Direct action
Dobtuamine: affects on 1
Action: increase cardiac output and rate
Therapeutic uses: in congestive heart failure, increase
cardiac output without increase cardiac rate

Adrenergic agonist :
A- Direct action
Phenylphrine: is a selective 1-adrenergic
receptor agonist of the phenethylamine class
used primarily as a decongestant, as an agent to
dilate the pupil, and to increase blood pressure.

Adrenergic agonist :
A- Direct action
Methoxamine: is an 1-adrenergic receptor
agonist, similar in structure to phenylephrine.
The drug induces vasoconstriction of skin and
splanchnic blood vessels, thereby increasing
peripheral vascular resistance and raising mean
arterial blood pressure. Because of its
hypertensive effects.

Adrenergic agonist :
A- Direct action
Clonidine: (trade names Catapres, Kapvay,
Nexiclon, Clophelin, and others) is a
sympatholytic medication used to treat
high blood pressure, attentiondeficit/hyperactivity disorder, anxiety
disorders, migraine, menopausal flushing,
diarrhea, and certain pain conditions. It is
classified as a centrally acting 2
adrenergic agonist .

Clonidine

Adrenergic agonist :
A- Direct action
Metaproterenol (2): (trade name: Alupent ,
Metaprel ) is a bronchodilator used in the
treatment of asthma. metaproterenol is a
moderately selective beta2-adrenergic receptor
agonist that stimulates receptors of the smooth
muscle in the lungs, uterus, and vasculature
supplying skeletal muscle, with minimal or no
effect on alpha-adrenergic receptors.

Metaproterenol

Adrenergic agonist :
B- Indirect action
Amphetamine: this drug has marked CNS
stimulation, increase BP , the CNS effects
is abused, but it is useful in depression,
hyperactivity in children, sleeping sickness
(narcolepsy) and appetite control
(treatment of obesity)

Adrenergic agonist :
B- Indirect action
Tyramine
Mechanism of action for Amphetamine
and Tyramine is mixed action:
Cause release of stored catecholamine.
Direct action on adrenergic receptors.

Adrenergic agonist :
B- Indirect action
Ephedrine: is a sympathomimetic amine
commonly used as a stimulant, concentration
aid, decongestant, appetite suppressant, and to
treat hypotension associated with anaesthesia.
Ephedrine is similar in molecular structure to the
important neurotransmitter epinephrine
(adrenaline). It works mainly by increasing the
activity of norepinephrine (noradrenaline) on
adrenergic receptors.

Adrenergic agonist :
B- Indirect action
Cocaine: is obtained from the leaves of
the coca plant. It is a stimulant, an
appetite suppressant, and a nonspecific
voltage gated sodium channel blocker,
which in turn causes it to produce
anaesthesia at low doses. Biologically,
cocaine acts as a serotonin
norepinephrinedopamine reuptake
inhibitor.

Adrenergic Antagonist
A- Direct antagonist:
1. Alpha Adrenergic blocking agents:
. Phenoxybenzamine: (marketed under the
trade name Dibenzyline) is a nonselective, irreversible alpha antagonist.

Phenoxybenzamine :
Therapeutic uses:
It is used in the treatment of hypertension, and
specifically that caused by pheochromocytoma. It has
a slower onset and a longer lasting effect compared
with other alpha blockers.
It was also the first alpha blocker to be used for
treatment of benign prostatic hyperplasia, although it
is currently seldom used for that indication due to
unfavourable side effects.
It has been used in the treatment of hypoplastic left
heart syndrome.

Adrenergic Antagonist
A- Direct antagonist:
Phentolamine: (Regitine) is a reversible
nonselective alpha-adrenergic antagonist.
Mechanism :
Its primary action is vasodilation due to 1
blockade.
It also can lead to reflex tachycardia
because of hypotension and 2 inhibition,
which increases sympathetic tone.

Phentolamine
Uses:
The primary application for phentolamine is
for the control of hypertensive emergencies,
most notably due to pheochromocytoma.
It also has usefulness in the treatment of
cocaine-induced cardiovascular complications
Phentolamine has recently been introduced in
the dental field as a local anesthetic reversal
agent.

Adrenergic Antagonist
A- Direct antagonist:
Parzosin: ( trade names Minipress, Vasoflex,
Pressin and Hypovase) is a sympatholytic drug
used to treat high blood pressure and anxiety,
PTSD, and panic disorder. It is an alphaadrenergic blocker that is specific for the alpha-1
receptors. These receptors are found on
vascular smooth muscle, where they are
responsible for the vasoconstrictive action of
norepinephrine.

Parzosin

Adrenergic Antagonist
A- Direct antagonist:
doxasin: (Trade name: Cardura and
Carduran) is an 1-selective alpha blocker
used to treat high blood pressure and
urinary retention associated with benign
prostatic hyperplasia (BPH).

Doxasin or Doxazosin
It is an alpha-1 adrenergic receptor blocker that
inhibits the binding of norepinephrine (released
from sympathetic nerve terminals) to the alpha-1
receptors on the membrane of vascular smooth
muscle cells. The primary effect of this inhibition
is relaxed vascular smooth muscle tone
(vasodilation), which decreases peripheral
vascular resistance, leading to decreased blood
pressure.

Doxasin or Doxazosin

Adrenergic Antagonist
A- Direct antagonist:
2. Beta Adrenergic blocking agents:
Propranolol (Inderal): -blockers
Therapeutic uses are:
o Hypertension
o Hyperthyroidism: prevent cardiac arrhythmia
o Glaucoma: chronic treatment (timolol is perfect)
o Migraine: by blocking catecholamines induce
vasodilation in the brain vessels.
o Angina pectoris: decrease demand for oxygen.
o Inferction

Propranolol (Inderal) Drug

Adrenergic Antagonist
A- Direct antagonist:
2. Beta Adrenergic blocking agents:
Timolol: is a non-selective
beta-adrenergic receptor
antagonist indicated for
treating glaucoma, hypertension
and migraine headache.

Adrenergic Antagonist
A- Direct antagonist:
2. Beta Adrenergic blocking agents:
Nadolol: (Corgard) is a non-selective beta
blocker used in the treatment of high
blood pressure and chest pain.
Additionally, it is often prescribed in the
treatment of atrial fibrillation, migraine
headaches, and complications of cirrhosis.

Nadolol: (Corgard)
2. Beta Adrenergic blocking agents:

Adrenergic Antagonist
A- Direct antagonist:
2. Beta Adrenergic blocking agents:
Atenolol: is a selective 1 receptor antagonist, a
drug belonging to the group of beta blockers
(sometimes written -blockers), a class of drugs used
primarily in cardiovascular diseases. Introduced in
1976, atenolol was developed as a replacement for
propranolol in the treatment of hypertension. It works
by slowing down the heart and reducing its workload.
Unlike propranolol, atenolol does not pass through the
bloodbrain barrier thus avoiding various central
nervous system side effects.

Adrenergic Antagonist
A- Direct antagonist:
2. Beta Adrenergic blocking agents:
Atenolol: is commonly used as antihypertensive drug in IRAQ
(25mg,50mg and 100mg)

Adrenergic Antagonist
A- Direct antagonist:
2. Beta Adrenergic blocking agents:
Esmolol: (trade name Brevibloc) is a cardioselective
beta1 receptor blocker with rapid onset, a very short
duration of action. Esmolol decreases the force and rate
of heart contractions by blocking beta-adrenergic
receptors of the sympathetic nervous system, which are
found in the heart and other organs of the body. Esmolol
prevents the action of two naturally occurring
substances: epinephrine and norepinephrine.

Esmolol

Adrenergic Antagonist
A- Direct antagonist:
2. Beta Adrenergic blocking agents:
Pindolol: (trade name: Visken, Betapindol, Blockin L,
Blocklin L, Calvisken, Cardilate, Decreten, Durapindol,
Glauco-Visken, Pectobloc, Pinbetol, Prindolol, Pynastin)
is a nonselective beta blocker with partial betaadrenergic receptor agonist activity. This means that
pindolol, particularly in high doses, exerts effects like
epinephrine or isoprenaline (increased pulse rate,
increased blood pressure, bronchodilation), but these
effects are limited.

Pindolol

Adrenergic Antagonist
A- Direct antagonist:
2. Beta Adrenergic blocking agents:
Acebutolol: (trade names Sectral, Prent) is
a beta blocker for the
treatment of hypertension
and arrhythmias.

Adrenergic Antagonist
A- Direct antagonist:
2. Beta Adrenergic blocking agents:
Labetalol: (trade names Normodyne and
Trandate) is a mixed alpha/beta
adrenergic antagonist that is used to treat
high blood pressure.

Labetalol (Trandate)

Adrenergic Antagonist
B- Indirect antagonist:
Reseprine: is antipsychotic and
antihypertensive drug that has been used for the
control of high blood pressure and for the relief
of psychotic symptoms, although because of the
development of better drugs for these purposes
and because of its numerous side-effects, it is
rarely used today.

Guanethidine: is an antihypertensive drug that

reduces the release of catecholamines, such as
norepinephrine.