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Dr Venkatesh Karthikeyan
Intern
VMCH & RI
Email : 4852012@gmail.com
13/09/2019
ANS
 Sympathetic (Adrenergic)
 Parasympathetic (Cholinergic)
Cholinergic
 Muscarinic (M1, M2, M3)
 Nicotinic (Nm, Nn)
Adrenergic
 Alpha (1 and 2)
 Beta (1,2,3)
Beta 1 receptors
 In heart, JG cells of kidney
 Selective agonist - Dobutamine
 Selective antagonist – Metoprolol, Atenolol
Beta 2 receptors
 In Bronchi, blood vessels, uterus, liver, GIT, GUT, Eye
 Selective agonist – Salbutamol, terbutalin
 Selective antagonist – Alpha methyl propanolol
Beta 3 receptors
 In adipose tissue
Classification
 First generation (Older, non selective)
 Second generation (Beta 1 selective)
 Third generation (with additional alpha blocking
and/or vasodilator property)
First generation
Propanalol
Timolol
Sotalol
Pindolol
Second generation
Metaprolol
Atenolol
Acebutolol
Bisoprolol
Esmolol
Third generation
Labetolol
Carvedilol
Celiprolol
Nebivolol
Betaxolol
Pharmacological actions
 CVS
 Respiratory tract
 CNS
 Local Anaesthetic
 Metabolic
 Skeletal muscle
 Eye
 Uterus
CVS - Heart
 Decreases heart rate
 Decreases force of contraction
 Decreases cardiac output
 Effects are prominent under sympathetic overactivity
 CHF may be aggravated
 In angina patients, improvement of oxygen
supply/demand status, exercise tolerance is increased.
CVS – Blood vessels
 On prolonged administration, propanolol causes
gradual fall in BP in hypertensive patients.
Respiratory tract
 Increases bronchial resistance
 Asthma may be precipitated
CNS
 Subtle behavioural changes
 Forgetfulness
 Increased dreaming
 Nightmares
 Suppresses anxiety
Local anaesthesia
 Proponolol – Potent local anaesthetic
 Causes irritation at injected site
Metabolic
 Blocks adrenergically induced lipolysis
 Causes increase in plasma free fatty acid level
 Plasma triglyceride level increases
 LDL/HDL ratio is increased
Skeletal muscle
 Inhibits adrenergically provoked tremor
 Reduce exercise capacity
Eye
 Reduces secretion of aqueous humor
 IOT is lowered
Uterus
 Relaxation of uterus in response to Beta 2 agonists is
blocked
Uses
 Hypertension
 Angina pectoris
 Cardiac arrhythmias
 Myocardial infarction
 Congestive heart failure
 Dissecting aortic aneurysm
Uses
 Pheochromocytoma
 Thyrotoxicosis
 Migraine
 Anxiety
 Essential tremor
 Glaucoma
 HOCM
Hypertension
 First line
 Good patient acceptability
 Cardioprotective
Angina Pectoris
 Decreases frequency of attacks
 Increases exercise tolerance
 Not suitable in vasospastic angina
Cardiac arrythymias
 Supresses extrasystoles and tachycardias, especially
those mediated adrenergically – during anaesthesia/
digitalis induced
 Controls ventricular rate in AF and atrial flutter
 Esmolol - PSVT
Myocardial infarction
 Secondary prophylaxis of MI
 Myocardial salvage during evolution of MI
Secondary prophylaxis of MI
 Prevents reinfarction
 Prevents sudden ventricular fibrillation at subsequent
attack of MI
Myocardial salvage during MI
 Limit infarction size by reducing O2 consumption
 Prevents arrhythmias
 Can be administered only those who are not in
shock/cardiac failure/ bradycardia
Congestive heart failure
 Useful in selected patients with DCM
 Prevents deleterious effects of sympathetic overactivity
invoked reflexly by heart failure
Dissecting aortic aneurysm
 Reduces cardiac contractile force
 Decreases aortic pulsation
Pheochromocytoma
 Used to control tachycardia and arrhythmias
 Never administer unless an alpha blocker is given
– otherwise dangerous rise in BP can occur.
Thyrotoxicosis
 Rapidly controls sympathetic symptoms
 Inhibits peripheral conversion of T4 to T3
Migraine
 Most effective for chronic prophylaxis
Anxiety
 Blocks peripheral manifestations of anxiety
Essential tremor
 Does not benefit parkinsonian tremor (resting)
Hypertrophic obstructive
cardiomyopathy
 Beta blockers reduce left ventricular outflow
obstruction
 Improves cardiac output in these patients during
exercise
Glaucoma
 Timolol
 Betaxolol
 Levobunolol
 Advantages over miotics
 No change in pupil size
 No diminution of vision in dim light/cataract patients
 Does not induced myopia
 No persistant spasm of iris and ciliary muscles/ No
headache and brow pain
 No IOT fluctuation
Perioperative Cardiovascular death
 Increased sympathetic response
 Imbalance in oxygen supply and demand
 Plaque rupture
 Thrombosis
 Occlusion
Cardioprotective effects in
perioperative patients
 Decreased oxygen demand
 Increased systolic perfusion time
 Suppresses arrhythmia
 Stabilizes plaque
 Anti inflammatory response
 Inhibits apoptosis
In Non Cardiac surgery
 Beta blockers should be titrated against
hemodynamics over a period of days before surgery
 Protective against MI and have preventive/therapeutic
benefits in arrhythmias
 Decreases incidence of mortality due to cardiac cause
In Cardiac surgery
 Prevent and treat perioperative arrhythmia in CABG
and valvular disease
 Beneficial in MI (age<75 years, EF >30%)
 Mortality benefits of beta blockers have been
conclusively proven in large studies
Individual drugs
 Sotalol – Class III antiarrhythmic activity
 Timolol – glaucoma
 Pindolol – Antihypertensive used in patients who
develop bradycardia with propanolol
 Metoprolol – prefered in diabetics
 Atenolol – MC used in hypertension and angina / once
daily dose/ does not derange lipid profile
 Acebutolol - once daily dose
 Bisoprolol – once daily dose in angina/CHF/SHT
 Esmolol
 Ultrashort acting (T1/2 – 10 mins)
 Terminates SVT
 Useful in AF/flutter
 Useful in arrythmia during anaesthesia
 Reduces HR and BP during and after cardiac surgery
 In early treatment of MI
 Celiprolol – safe in asthmatics
 Nebivolol – delays atherosclerosis
 Labetolol – alpha + beta blocker / potent hypotensive
(20-40 mg IV every 10 mins in hypertensive
emergencies)
 Carvedilol
 Alpha 1 + Beta 1 + Beta 2 blocker
 Antioxidant property
 Cardioprotective
Interactions
 Delays recovery from hypoglycemia due to
antidiabetics
 Warning signs of hypoglycemia masked
 Retards lignocaine metabolism
 Increases bioavailability of chlorpromazine
ADR
 Can precipitate CHF/edema
 Bradycardia (sick sinus patients are more prone)
 Contraindicated in asthmatics
 Exacerbates vasospastic angina
 Plasma lipid profile altered
 Enhances risk of of CAD
 Sudden withdrawal of propanolol – rebound
hypertension / worsening of angina / death
 Contraindicated in heart block
 Tiredness and decreased exercise capacity
 Worsening of peripheral vascular disease
 Sexual distress
 GI upset
Thank you 

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Beta adrenergic blocking drugs

Editor's Notes

  1. Perioperative use of beta blockers? Recent advances