Anti Adrenergic

Drugs
Introduction

• Antagonise the receptor action of adrenaline

and related drugs
• Classified on the basis of receptors they
block primarily
• Alpha, Beta, Both
• Each has their own sub types
• Anti-adrenergics vs Adrenergic neurone
blockers
 AntiAdrenergic Drugs

Antiadrenergic agents inhibit the activity of the

sympathetic nervous system. They act by
blocking adrenergic receptors in target organs or by
inhibiting the synthesis, storage, or release of
endogenous catecholamines (mainly norepinephrine)
Alpha adrenergic blocking Drugs
• Non-equilibrium type (Non competitive):
• Beta-haloalkylamines: Phenoxybenzamines
• Equilibrium type (Competitive)
• Non-selective
• Ergot alkaloids: Ergotamine, Ergotoxin
• Hydrogenated ergot alkaloids: Dihydroergotamine (DHE),
Dihydroergotoxin
• Imidazoline: Phentolamine
• Miscellaneous: Chlorpromazine (Neuroleptics)
• Alpha1 selective: Prazosin, Terazosin, Doxazosin,
Alfuzosin, Tamsulosin
• Alpha2 selective: Yohimbine
General effects of alpha blockers
• Fall in BP
• Postural reflex interfered: marked hypotension 
dizziness, syncope
• Vasomotor reversal of Dale

• Reflex tachycardia

• Na+ retention and expansion of blood volume

General effects of alpha blockers

• Nasal stuffiness and miosis

• Increased intestinal motility

• Reduced tone of bladder trigone, sphincter and

prostate

• Inhibits ejaculation (relaxation of vas deferens and

related)
Alpha adrenergic blocking Drugs
• Uses:
• Pheochromocytoma
• Hypertension
(phenoxybenzamine/phentolamine)
• HTN d/t clonidine withdrawal, cheese reaction
• Benign hypertrophy of prostate
• Secondary shock
• Peripheral vascular disease (Raynaud’s,
acrocyanosis)
• Congestive heart failure
Alpha adrenergic blocking Drugs
• Side effects:
• Phenoxybenzamine: Postural hypotension,
palpitation, nasal blockade, miosis, inhibition of
ejaculation

• Ergot alkaloids: peripheral vascular insufficiency

and gangrene of toes and fingers (ergotism)

• Prazosin and alike : postural hypotension

Beta adrenergic blocking drugs
• Nonselective (beta-1 and beta -2)
• Without intrinsic sympathomimetic activity:
propranolol, sotalol, timolol
• With intrinsic sympathomimetic activity: pindolol
• With additional alpha blocking property:
labetolol, carvedilol
• Cardioselective (beta- 1)
• Metoprolol, Atenolol, Acebutolol, Bisoprolol,
Esmolol, Betaxolol, Celiprolol, Nebivolol
 Beta adrenergic blocking drugs
First Second Third Generation (with
Generation Generation additional alpha blocking
(Older, (β1 and/or vasodilator property)
nonselective) selective)
Propanolol Metoprolol Labetalol
Timolol Atenolol Carvedilol
Sotalol Acebutolol Celiprolol
Pindolol Bisoprolol Nebivolol
Esmolol Betaxolol
General Effects of beta blockers

• Heart:
• Decreases heart rate, force of contraction (high
dose) and cardiac output

• Reduced cardiac work and oxygen consumption

• Blood supply to sub-endocardial region not

impaired: improved oxygen supply/demand
status in angina patients
General Effects of beta blockers
• Blood vessels:
• Blocks fall in BP evoked by Isoprenaline; Enhanced
rise in BP by Adr

• Re-reversal of vasomotor reversal of Dale

• Gradual fall in BP on prolonged
administration in hypertensives
• Adaptation of resistance vessels to reduced C.O.  fall
in total peripheral resistance
eneral Effects of beta blockers
stem Effects
spiratory Increase bronchial resistance (β2 blockade)
S Subtle behaviour changes, forgetfulness, increased
dreaming and nightmares
Anti-anxiety effect (peripheral action of propranolol)
tabolic Blocks adrenergically mediated lipolysis
Inhibits glygenolysis in heart, skeletal muscles, liver
May reduce carbohydrate tolerance (decreased insulin
release)
elet Inhibits adrenergically provoked tremor (β2
blockade) Attenuate exercise capacity
scl

e Reduced secretion of aqueous humour and intra ocular

Cardio-selective beta blockers
Metoprolol, Atenolol, Acebutolol, Bisoprolol,
Nebivolol
• More potent β1 blocking action (lost at high doses)
• Low propensity to cause bronchoconstriction
• Less interference with carbohydrate metabolism
• Lower incidence of colder hands and feet
• Less effect on lipid profile
• Less liable to impair exercise capacity
Partial agonistic beta blockers
Pindolol, Celiprolol, Acebutolol
• Activates β1 and/or β2 receptors sub-
maximally
• Bradycardia and depression of contractility:
• Not prominent at rest
• Exercise tachycardia blocked
• Prevents development of super-sensitivity
• No/less effect on plasma lipid profile
• Not suitable for prophylaxis in MI, migraine
Beta blockers: Additional Properties
Membrane stabilizing activity of
beta blockers Lipid insoluble beta blockers
Propanolol, Atenolol, Celiprolol,
Oxprenolol, Bisoprolol, Sotalol
acebutolol • Less likely to produce
• Contributes to the sleep disturbances and
nightmares
anti arrhythmic
action • Incomplete absorption, no
first pass metabolism,
• Significant only at high excreted unchanged in
doses urine
• Longer acting (6-20 hrs)
• Effective in narrow dose
range
Beta adrenergic blocking drugs:Uses
• Hypertension • Dissecting aortic
• Stable Angina aneurysm
• Cardiac arrhythmias • Pheochromocytoma
• Myocardial infarction • Thyrotoxicosis
• Congestive heart • Migraine
failure • Anxiety
• Hypertrophic • Essential tremor
obstructive • Glaucoma
cardiomyopathy
 Beta blockers: Adverse effects

Can accentuate myocardial insufficiency and precipitate

CHF/edema
Bradycardia
Exacerbates variant angina
mpaired Carbohydrate tolerance
Altered plasma lipid profile
Tiredness and reduced exercise capacity
Cold hands and feet
Others: G.I. upset, lack of drive, nightmares,
orgetfulness, hallucinations, sexual distress in male
 Beta blockers: Warnings and
Contraindications

• Sudden withdrawal : rebound hypertension,

worsening of angina, sudden death
• Worsens COPD; can produce acute Bronchial
asthma: Contraindicated
• Partial or complete heart block: Contraindicated
α + β adrenergicblockers
Labetalol, Carvedilol
• β1+ β2 + α1 blocking property; weak β2 agonistic
activity
• 5 times more potent in blocking β receptors
•• Fall
Uses:in BP • Side
• Pheochromocytoma •effects:
Postural
• Clonidine withdrawal Hypotension
• Essential
• Rashes, liver
Hypertension
damage
That would be all for thistopic.

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