Adrenergic drugs
(Sympathomimetics )
Adrenergic
transmission
drugs
Lippincott’s pharmacology 4th edition
Adrenergic receptors
The adrenergic receptors are classified as αand
β receptors. Both classes have subtypes :
⚫ Alpha adrenoceptors (α): α1 adrenergic receptors
α 2 adrenergic receptors
Beta- receptors (β):Beta 1 (β1)
Beta 2 (β2)
Beta 3 (β3)
Dopaminergic receptors (D)
Major effects mediated by adrenoceptors
Lippincott’s pharmacology 4th edition
Presynaptic β2
facilitate release
of noradrenaline
β3
Increase lipolysis
Drugs Act on sympathetic
nervous system
⚫ Drugs that produce sympathetic like action =
Sympathomimetics = Adrenergics
⚫ Drugs that oppose sympathetic = Sympatholytics
= Antiadrenergics
Sympathomimetic drugs
Drugs have effects similar to those produced by activity of
sympathetic nerve stimulation
Mechanism of action of the adrenergic
agonists
Direct-acting Mixed-acting Indirect- acting
Releasing Uptake
Selective Non-selective agent inhibitors
Amphetamine Cocaine
α1:phenylephrine
α1,α2,β1,β2: Ephedrine
α2:clonidine adrenaline
Alpha methyl Dopa α1,α2,β1:
noradrenaline
β1:dobutamine β1,β2:
β2:salbutamol isoprinaline
Mechanism of action of
the adrenergic agonists
Lippincott’s pharmacology 4th edition
stimulation
Effector organs Effects of sympathetic
stimulation
Eye Mydriasis
Heart ↑ heart rate
↑ force of contraction
↑ blood pressure
Blood vessels Dilatation of coronary arteries
Dilatation of blood vessels
supply skeletal muscle
Stomach and Intestine Inhibits Peristalsis and ↑ the
tone of sphincters and
inhibits defecation
Urinary bladder Relaxes bladder wall
↑ the tone of sphincters
inhibits micturation
Respiratory system Dilatation of bronchi
liver Glycogenlysis
Adrenaline
α1, α2, β1 and β2 agonist
Can be administered by :
-- subcutaneous -- inhalation -- eye drops -- intracardiac
Actions similar to sympathetic stimulation
Cardiovascular system
❖ Heart : ↑all cardiac properties (↑contractility, heart rate , AV
conduction, excitability, automaticity
❖ Blood vessels:
● Vasoconstriction (skin, mucous membrane, renal)
● Vasodilatation (skeletal muscle, coronary blood vessels)
❖ Blood pressure:
● ↑systolic blood pressure, ↓ diastolic blood pressure
Adrenaline actions (cont.)
Respiratory system
Bronchodilatation (β2)
Decongestion of bronchial mucosa (α1)
urinary bladder and Gastrointestinal tract
Spasm of spincters (α1)
Relaxation of the wall (β2)
urinary retention and inhibits defecation
Skeletal muscle
Facilitate NM transmission
Anti fatigue
Vasodilatation (β2)
Adrenaline actions (cont.)
Eye
Vasoconstriction of conjunctival blood vessels
(decongestion)
↓intraocular pressure
Mydriasis
Antiallergic
Adrenaline is Physiological antagonist of histamine
Metabolism
✔ Increase blood glucose
✔ Lipolysis
✔ General stimulation of metabolic activity
Adrenaline
Uses
With local anesthetic (delay absorption and prolong
duration of drugs)
Open angle glaucoma (eye drops)
Epistaxis (haemostatic nasal pack)
Anaphylactic shock
Cardiac resuscitation in cardiac arrest
Acute bronchial asthma
Adrenaline
Adverse effects
Gangrene if injected around finger toes
Hypertension , leads to cerebral hemorrhage
Tachycardia, palpitation, angina and arrhythmia
Contraindications
Injection Around finger or toe
Hypertension
coronary heart disease
Arrhythmia
Thyrotoxicosis
Dopamine
Non-selective α , β , D agonists
Actions
❑ Small dose:D1»vasodilatation--------------»↑renal blood flow
❑ Moderate dose:D1+β1-------» positive inotropic effect
❑ Large dose:α1 ------»vasoconstriction »↑peripheral resistance
Uses
✔ Shock
✔ Resistant heart failure
Dobutamine (dobutrex)
❑ Selective β1agonist
❑ positive inotropic 🡲 ↑ Cardiac output
❑ Used by I.V. infusion in treatment of
-Cardiogenic shock,
-Resistant heart failure
-Resistant heart block.
❑ Side effects:
Angina and arrhythmias
Phenylephrine
Selective α1 – agonists
Action
stimulates α-receptors leading to VC and ↑ blood pressure
VC of mucous membrane blood vessels so promote drainage in
nasal passages
Uses:
Nasal congestion,
Hypotensive states (shock)
To prolong action of local anesthetics
Fundoscopic examination of eye
Clonidine
Selective α2 agonist
Actions
● Stimulates α2 receptors in C.N.S leading to decreasing
sympathetic outflow to the periphery .
⚫ Uses
Hypertension
Prophylaxis of migraine headache .
opiates or benzodiazepines withdrawal symptoms
Alpha methyl Dopa
Selective α2 – agonists
Agonists of α2 receptors in VMC in brain leading to:
↓ sympathetic Outflow from vaso Motor Centre (VMC)
It inhibits synthesis of catecholamine, dopamine and
serotonin .
Uses
Hypertension especially in: Renal impairment.
Pregnancy.
Selective Beta-2 agonists
⚫ Short acting: salbutamol, terbutaline, Ritodrine (
Duration 4-6 h)
⚫ Long acting: salmeterol, formoterol. Duration 12
h (Used for prophylaxis)
⚫ Used mainly in treatment of bronchial asthma
either taken orally or as nebulizer
Selective Beta-2 agonists
Actions:
Bronchodilation
e.g. Salbutamol
Uterine relaxation
Relaxation of uterine smooth muscle e.g. Ritodrine
Vasodilatation
e.g. Isoxuprine & Ritodrine
Selective Beta-2 agonists
Therapeutic uses of selective β2 agonists:
❑ Bronchial asthma: acute attack, prophylaxis & status
asthmaticus.
❑ Congestive heart failure.
❑ premature labor
❑ Peripheral vascular diseases.
Adverse effects (large oral doses)
Tremors, tachycardia, palpitation, flushing
headache , Insomnia and confusion
Hyperglycemia
Sever hypokalemia in chronic uses
Selective Beta-2 agonists
Advantages of selective β2 agonists:
●Effective by all routes
●Long duration of action
●Selective with minimal C.V.S side effects
●Rapid onset of action
●Anti-inflammatory effects (salmeterol).
Thank you
THANK YOU
(Anti-Adrenergic drugs
(Sympatholytic agents)
(Dr. Heba A. Mahmoud
SYMPATHETIC DEPRESSANTS
Adrenergic Receptor
Blockers
Adrenergic Neuron Depressants
Ganglion Blockers
Centrally Acting Alpha-2 Agonists
Vasomotor center Depressants
Adrenergic Receptor Blockers
❑ ALPHA- BLOCKERS
❑Beta-Blockers
❑ alpha & beta - Blockers
NON SELECTIVE ALPHA BLOCKERS
They produce alpha blocking effect (α 1 and α 2 )
Phentolamine
Uses:
Peripheral vascular disease.
pheochromocytoma
Adverse effects
postural hypotension
Tachycardia
Arrhythmias and anginal pain
Phenoxybenzamine
Very powerful α- blocker (non selective)
It has slow onset and long duration
Uses
❑Peripheral vascular diseases.
❑Pheochromocytoma
Side effects
❑Postural hypotension
❑reflex tachycardia
Lippincott’s pharmacology 4th edition
SELECTIVE ALPHA BLOCKERS
Prazosin
Selective α1 – blocker lead to vasodilatation of both
artries and veins (mixed dilator) lead to decrease preload
and afterload of the heart
Decease in both systolic blood pressure
No discomfortable tachycardia
Uses Hypertension.
Peripheral vascular diseases.
Heart failure
Side effects Dizziness, headache, drowsiness
Salt and water retention
First dose hypotension and syncope
Yohimbine
Selective α2 blocker .
May be used in impotence ( sexual stimulant)
BETA–ADRENOCEPTOR BLOCKERS
Beta blockers are drugs which produce competitive blocking of
the effect of adrenaline & noradrenaline on beta adrenergic
receptors.
Examples Non selective: Propranolol, Timolol,
Selective: Atenolol, Esmolol
Absorption: Orally , parenterally and locally as eye drops.
Distribution: They are distributed all over the body
Some of them passes B.B.B.
BETA–ADRENOCEPTOR BLOCKERS
Actions
C.N.S. (β1):
β blockers that pass the B.B.B produce sedation, depression &
night mares.
Eye
Decrease intraocular pressure.
C.V.S
Decrease all cardiac properties
Vasoconstriction (β2 ): leading to : Decrease blood flow to all
organs except brain. Decrease hepatic blood flow
Anti-hypertensive effect
Respiratory system :(β2).
Non-selective β-blockers produce bronchospasm especially in asthmatics
Metabolism: hypoglycemia
BETA–ADRENOCEPTOR BLOCKERS
Uses:
❑ Central nervous system e.g. (Propranolol)
Essential Familial Tremors.
Anxiety & Panic disorders.
Prophylaxis of migraine headache
❑ Eye e.g.(Timolol)
Open angle glaucoma
❑ Cardiovascular system
hypertension
Angin Pectoris:
Cardiac arrhythmias
❑ Thyrotoxicosis e.g. (Propranolol)
BETA–ADRENOCEPTOR BLOCKERS
Side effects
❑C.N.S Depression, nightmares & hallucinations
❑ Heart Heart failure.
Bradycardia .
Heart block.
❑ Block B2 –receptor:
Acute bronchial asthma in Asthmatics.
hypoglycemia and Mask signs of hypoglycemia in diabetic patients
Cold extremities & intermittent claudiactions.
❑Sexual dysfunction in male patient
❑Sudden stop results in serious rebound increase of heart rate ,
angina , arrhythmia and may be infarction and death
❑G.I.T. disturbance.
❑Hypersensitivity reaction.
BETA–ADRENOCEPTOR BLOCKERS
Contraindications
Heart failure.
Heart block
Prinzemetal (Variant) Angina
Peripheral vascular disorders
Bronchial Asthma
Diabetic patients
Never stop β blocker suddenly
ADRENERGIC NEURONE BLOCKERS
Guanethidine
Reserpine
Alpha-Methyl DOPA
ADRENERGIC NEURONE BLOCKERS
The advent of newer and more effective agents, with fewer side
effects, these agents are rarely used
Guanethidine
Inhibits the release of noradrenaline from the sympathetic nerve
hypotensive drug
Reserpine
•Deplete central and peripheral catecolamine stores
•hypotensive drug & major tranquillizer
Alpha-Methyl DOPA (Aldomet)
▪Reduce central sympathetic outflow and decrease synthesis of
catecholamines
▪Used in hypertension especially in Renal impairment and Pregnancy.
Thank you
