 Sympathomime agonist

Direct agonist Indirect agonist

Alpha agonist Beta agonist

Beta 2
Alpha 2
selective selective Non se-
lective
Beta 1
Alpha 1 Non selective selective
selective
 Releasers
 Reuptake inhibitor
 Stimulates the “fight or fight” reaction
 Increased plasma glucose levels
 Increased cardiovascular function
 Increased metabolic function
 Decreased gastrointestinal and
genitourinary function
 Drugs that partially or completely mimic
the actions or nor epinephrine (NE) and
epinephrine (Epi).
 Act either - directly on α- and/or β-
adrenoceptors or indirectly on
presynaptic terminals, usually by causing
the release of NE.
 β2-Adrenoceptor Agonists – cause
bronchial dilation - used for the treating
asthma, prevent pre-term labor (relaxing
uterine muscle).
 β1-Adrenoceptor Agonists – (e.g.,
dobutamine) sometimes used to increase
the force of heart contraction in severe
low-output heart failure.
 α1-Agonists – (e.g., Phenylephrine) – used as
mydriatics, decongestants.
 α2-Agonists – (e.g., clonidine, methyldopa)
– centrally acting hypertensive drugs.
 Transported into nerve terminals where they
displace vesicular NE into the cytoplasm.
Some is metabolized by MAO, but the
remainder is released by carrier-mediated
transport to activate adrenoceptors.
 Amphetamines – resistant to MAO.
- Peripheral actions - tachycardia,
hypertension - mainly caused by
catecholamine release.
 Cocaine – NE reuptake inhibitor (also
dopamine) – Intense central stimulant 
popular drug of abuse.
 Effects in humans depends on their receptor
specificity (α and/or β) and on the compensatory
reflexes they evoke.
 Epi increase BP by stimulating the rate and force of
the heart beat (β1 effects).
 Stimulation of vascular α-receptors causes
vasoconstriction (viscera, skin).
 Stimulation of vascular β2-receptors vasodilatation
(skeletal muscle).
 total peripheral resistance may actually decrease.
 The resulting rise in BP and slows the heart, usually
overcoming the direct β1-stimulant action on the
heart rate.
 Isoprenaline – stimulates all β-receptors
 inc rate and force of heart beat and
 vasodilatation  dec. diastole , with
little change in systolic pressure.
 β2-Adrenoceptor Agonists – relatively
selective class of drugs that produce
bronchodilator – used for asthma
(resistant to MAO, not uptake into
neurons).
 Increase systolic BP and mean arterial
pressure.
 Direct stimulate the heart rate.
 Rarely used therapeutically.
 Only use to treat hypotension during
anesthesia.
 Activate β1-2 and alpha adrenoceptor.
 Increase systolic BP by β1receptor.
 Increase coronary blood flow.
 Increase the drainage of aqueous
humor and use in open angle glaucoma
and dilate the pupil.
 Relax bronchial smooth muscle.
 Drug of choice in Anaphylactic shock.
 β1 adrenoceptor to increase heart rate
and contractility.
 Increase renal blood flow.
 Dobutamine is a synthetic
catecholamine use for congestive heart
failure.
 Septic shock
 Congestive heart failure increase ion
tropic and chronotropic effects on heart.
Cause vasoconstriction
increase blood pressure.
To provide local vasoconstriction.
As a 10% ophthalmic solution.
As an adjunct to local anesthetics.
Nasal congestant.
 Alpha 2 agonist produce sympathetic
vasomotor center in CNS.
 Migraine
 Insomnia
 Obsessive compulsive disorder.
 Narcotics (Opiates) withdrawal
symptoms.
 In CVS it cause vasoconstriction,
cardiac stimulation…… increase BP.
 Use in Nasal decongestion
 Chronic bronchial asthma
 Mydriatic
 Improve motor function in Myasthenia
gravis
 Phenylephrine, Methoxamine,
Metaraminol direct alpha 1 receptor
stimulant.
 Terbutaline (Bricanyl), albuterol ,
salbutamol ,(ventoline), metaproterenol
cause relax bronchial smooth cell use in
asthma and COPD.
 Isoprosterenol dilate bronchial smooth
cell but increase heart rate.
 In Cardiovascular system short- term
hypotensive emergencies.
 Epinephrine for anaphylactic shock.
 Dobutamine for congestive heart failure.
 Hay fever and rhinitis use Phenylephrine.
 Isoproterenol and epinephrine for
cardiac arrest and heart block.
 Epinephrine is use for spinal anesthesia.
 Ritodrine and terbutaline use for suppress
premature labor by relaxing uterine
smooth muscles.
 Cause sever hypertension leading to
cerebral hemorrhage, pulmonary
edema and cardiac arrhythmias.
 Increase intra ocular pressure.
 Withdrawal symptoms like headache,
tachycardia and high blood pressure.