ADRENERGIC

AGONISTS

AND bladder relaxation

glycogenolysis
ANTAGONISTS
lipolysis
Review of Adrenergic Receptors
Dopamine-1(postsynaptic) receptors
Alpha -1(postsynaptic) receptors
vasodilation
vasoconstriction
diuresis
mydriasis
Dopamine-2(presynaptic) receptors
relaxation of gastrointestinal tract
inhibition of norepinephrine release
contraction of gastrointestinal sphincters
Classification
and
Comparative
contraction of bladder sphincter
Pharmacology
Alpha-2(presynaptic) receptors
of Sympathomimetics
inhibition of norepinephrine release
1. Natural Catecholamines
sedation
Epinephrine
Alpha-2(postsynaptic) receptors
Norepinephrine
platelet aggregation
Dopamine
hyperpolarization of cells in the CNS
2. Synthetic Catecholamines
analgesia
Isoproterenol
Beta-1(postsynaptic) receptors
Dobutamine
increased conduction velocity
3. Synthetic Noncatecholamines
increased automaticity
Indirect-acting
increased contractility
Ephedrine
Beta-2(presynaptic) receptors
Mephentermine
activates norepinephrine release
Amphetamines
Beta-2(postsynaptic) receptors
Metaraminol
vasodilation
Direct-acting
bronchodilation
Phenylephrine
gastrointestinal relaxation
Methoxamine
uterine relaxation

Principal Sites of Action of Adrenergic Agonists

Agent a-1
a-2
B-1
B-2
D-1
D-2
Methoxamine
++++ ?
0
0
0
Phenylephrine
++++
?
+/0
0
Norepinephrine
++++ ++++
++
0
Epineprine
++++ +++ ++++ ++ 0
Ephedrine
++
?
+++ ++
0
Dopamine
++++ ?
++++ ++
+++
Dobutamine
+/?
++++ ++ ++
0
Dopexamine
0
0
+
++++
+
Isoproterenol
0
0
++++ ++++
Hemodynamic Effects of Adrenergic Agonists
Agent
Methoxamine
Phenylephrine

HR

CO
SVR
decreased decreased increased
decreased decreased increased

0
0
0
0
0
?
0

Norepinephrine
decreased decreased increased
Epinephrine
increased
increased increased
Ephedrine
increased
increased increased
Dopamine
no change increased no change
Dobutamine
increased
increased decreased
Isoproterenol
increased
increased decreased

Clinical Uses of Adrenergic Agonists:

1. Increase myocardial contractility
2. Vasopressor
3. Treatment of bronchospasm(albuterol)
4. Management of life-threatening allergic

Nadolol
Pindolol
Timolol
Sotalol
Cardio-selective

Beta

Adrenergic

Antagonists
Metoprolol
Atenolol
Acebutolol
Esmolol
Side Effects of Beta-Antagonists:
sympathomimetics on the heart and offsets
Cardiovascular System
the inhibitory effects of epinephrine on insulin Bradycardia,
decreased
myocardial
reactions
5. Additive to local anesthetic solutions
Alpha-Adrenergic Receptor Antagonists
-- prevents the effects of catecholamines and

secretion.
Side Effects:
1. orthostatic hypotension
2. reflex tachycardia
3. impotence
Mechanism Of Action:
1. Reversible binding with alpha-adrenergic

contractility,
enhanced pressor effects of epinephrine, cold

hands and feet

Airway Resistance
Bronchospasm
Metabolism
Decreased glycogenolysis
receptors (phentolamine, prazosin, yohimbine) Distribution of Extracellular Potassium
2. Irreversible binding with alpha-adrenergic Increased plasma potassium concentration
Nervous System
receptors(phenoxybenzamine)
Fatigue and lethargy
3. Nonselective binding with alpha-adrenergic
receptors(phentolamine, phenoxybenzamine) Clinical Uses of Beta-Antagonists:
4.
Selective
binding
at
alpha-1
1. Treatment of essential hypertension
2. Management of angina pectoris
receptors(prazosin)
3. Treatment of postmyocardial infarction
5.
Selective
binding
at
alpha-2
4. Preoperative
preparation
of
receptors(yohimbine)
hyperthyroid patients
Beta-Adrenergic Receptor Antagonists
5. Suppression of cardiac dysrhythmias
-- prevents effects of catecholamines and
6. Prevention of excess sympathetic
sympathomimetics on the heart and smooth
nervous system activity
muscle of the airways and blood vessels
Combined Alpha and Beta-Adrenergic
Mechanism of Action:
Receptor Antagonists
-- reversible binding of beta-adrenergic
A. Labetalol
-- exhibits selective alpha-1 antagonist and
antagonists to beta-adrenergic receptors
nonselective beta-1 and beta-2 antagonist
(competitive antagonism)
Side Effects:
Noncardio-selective
Beta
Adrenergic
Orthostatic hypotension(most prominent)
Antagonists:
Fluid retention
Propranolol

Bronchospasm,
blocks

cardiac

failure,

and

heart