Anti

Adrenergi
c Drugs
Introductio
n
• 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
 Anti Adrenergic 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 Generation Second Third Generation (with additional
(Older, Generation (β1 alpha blocking and/or
nonselective) selective) vasodilator property)

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
General Effects of beta
blockers
System Effects
Respiratory Increase bronchial resistance (β blockade)
2

CNS Subtle behaviour changes, forgetfulness, increased dreaming and

nightmares
Anti-anxiety effect (peripheral action of propranolol)
Metabolic Blocks adrenergically mediated lipolysis
Inhibits glygenolysis in heart, skeletal muscles, liver
May reduce carbohydrate tolerance (decreased insulin release)
Skeleta Inhibits adrenergically provoked tremor (β2 blockade)
l Attenuate exercise capacity
muscle
Eye Reduced secretion of aqueous humour and intra ocular tension
Uterus Relaxant activity of β agonists blocked
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
Propanolol, Oxprenolol,
acebutolol
• Contributes to the anti
arrhythmic action
• Significant only at high
doses
Lipid insoluble beta blockers
Atenolol, Celiprolol, Bisoprolol,
Sotalol
• Less likely to produce sleep
disturbances and nightmares
• Incomplete absorption, no first
pass metabolism, excreted
unchanged in urine
• Longer acting (6-20 hrs)
• Effective in narrow dose range
Beta adrenergic blocking drugs:
Uses
• Hypertension • Dissecting aortic aneurysm
• Stable Angina • Pheochromocytoma
• Cardiac arrhythmias • Thyrotoxicosis
• Myocardial infarction • Migraine
• Congestive heart failure • Anxiety
• Hypertrophic obstructive • Essential tremor
cardiomyopathy • Glaucoma
 Beta blockers: Adverse
effects
• Can accentuate myocardial insufficiency and precipitate CHF/edema
• Bradycardia
• Exacerbates variant angina
• Impaired Carbohydrate tolerance
• Altered plasma lipid profile
• Tiredness and reduced exercise capacity
• Cold hands and feet
• Others: G.I. upset, lack of drive, nightmares, forgetfulness,
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 adrenergic
blockers
Labetalol, Carvedilol
• β1+ β2 + α1 blocking property; weak β2 agonistic activity
• 5 times more potent in blocking β receptors
• Fall in BP
• Uses: • Side effects:
• Pheochromocytoma • Postural Hypotension
• Clonidine withdrawal • Rashes, liver damage
• Essential Hypertension
That would be all for this
topic.

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