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BETA
BLOCKERS
DR.RESHMI.T.R
FIGHT OR FLIGHT
SYMPATHETIC RECEPTORS
β1 β2 β3
BETA
RECEPTORS
BETA 1 HEART
BETA 2 BRONCHUS
GIT
BLADDER
UTERUS
LIVER
BLOOD VESSELS
BETA 3 ADIPOSE TISSUE
BETA BLOCKERS
Beta adrenergic receptor antagonists act on
Β1 or β2 receptors or on both
SIR JAMES
BLACK
DEVELOPED BETA
BLOCKER
PROPRANOL IN 1958
AWARDED NOBEL
PRIZE FOR MEDICINE
IN 1988
NON
SELECTIVE
BLOCKERS
SELECTIVE
BLOCKERS
MIXED
BLOCKERS
CLASSIFICATION OF BETA BLOCKERS
PROPRANOLOL
TIMOLOL
SOTALOL
NADOLOL
PINDOLOL
OXPRENOLOL
NON SELECTIVE BETA BLOCKERS
METOPROLOL
ATENOLOL
ESMOLOL
ACEBUTOLOL
CELIPROLOL
BETAXOLOL
BISOPROLOL
NEBIVOLOL
SELECTIVE β1 BLOCKERS
BUTOXAMINE
SELECTIVE β2 BLOCKERS
LABETOLOL
CARVEDILOL
MIXED BLOCKERS---α+β BLOCKERS
NON SELECTIVE BLOCKERS
• Blocks both β1 and β2 receptors
• Eg:Propranolol
CARDIOVASCULAR
USES
BLOCK CARDIAC β1
RECEPTORS
HEART RATE
MYOCARDIAL
CONTRACTILITY
CARDIAC OUTPUT
BP
CARDIOVASCULAR USES
• ESSENTIAL HYPERTENSION
• CONGESTIVE HEART FAILURE
• ANGINA PECTORIS
• CARDIAC ARRHYTHMIAS
• MYOCARDIAL INFARCTION
ESSENTIAL HYPERTENSION
• Alone or in combination with
diuretics
• Rationale
– Decrease in HR,CO
,myocardial contractility.
– Decrease renin release
Dose:
20-40mg TDS
Congestive heart
failure
Useful in mild to moderate heart
failure
Introduced gradually
Can antagonise damaging effect due
to β1 overactivity
CI in severe heart failure
CANNOT PUMP
SUFFICIENT BLOOD
ANGINA PECTORIS
DECREASES OXYGEN DEMAND
INCREASES EXERCISE
TOLERANCE
CI:PRINZMETAL’S ANGINASENSATION OF CHEST PAIN
IMBALANCE BTW OXYGEN
DEMAND AND SUPPLY
CARDIAC ARRHYTHMIAS
• Used in SVT associated with thyrotoxicosis,
• Digitalis toxicity
Mechanism:
• Membrane stabilising effect
IRREGULAR
HEARTBEAT
TACHYCARDIA
PALPITATIONS
MYOCARDIAL INFARCTION
Decrease incidence,recurrence,mortality
Prevent VF at the
second attack of MI
Dose:
40-80 mg tds orally
NON CARDIOVASCULAR
USES
• Migraine
Anxiety provoking situations
• Glaucoma
• Hyperthyroidism
• Pheochromocytoma
• Alcohol withdrawal
• Oesophageal varices
NON CARDIOVASCULAR
USES
• MIGRAINE
• Prophylaxis
• Not for acute attack
• Dose:20mg tds orally
ANXIETY
Reduce anxiety
Block peripheral
manifestations of
anxiety:tremors, sweating
DOSE:10-20 MG TDS
GLAUCOMA
Decrease intraocular
pressure
Propranolol not used
Eg:Timolol topically
HYPERTHYROIDISM
Reduces symptoms like
tremor,sweating
DOSE:20MG BD ORALLY
PHEOCHROMOCYTOMA
GIVEN IN COMBINATION WITH α
BLOCKER
control tachycardia and
arrythmia
DOSE:20MG TDS FOR 3 DAYS
BEFORE SURGERY
ALCOHOL WITHDRAWAL
Reduces sympathetic
overactivity during
phase of withdrawal
Dose:20 mg BD orally
ADVERSE EFFECTS
• BRONCHOCONSTRICTION
• BRADYCARDIA
• COLD EXTREMITIES
• CNS SIDE EFFECTS
• HEART FAILURE
• HYPOGLYCEMIA
• REBOUND HYPERTENSION
• ADVERSE LIPID PROFILE
BRONCHOCONSTRICTION
Contra indicated
In
ASTHMATICS
COPD
BRADYCARDIA
Can lower HR to 55
bpm

BRADYARRHYTHMIA
HEART BLOCK
COLD EXTREMITIES
Loss of β2 receptor
mediated cutaneous
vasodilataton in extremities

CONTRA INDICATED
IN
REYNAUD’S
DISEASE
BLOOD VESSELS IN EXTREMITIES
CONSTRICT IN RESPONSE TO
TEMPERATURE:
TURN BLUE OR WHITE
CNS SIDE EFFECTS
SLEEP DISTURBANCES
DEPRESSION
NIGHTMARES
HEART FAILURE
Cardiac patients need
sympathetic drive to support
heart to maintain proper
cardiac output
Beta blockers block this
support

Contraindicated in
SEVERE HEART FAILURE
HYPOGLYCEMIA
Beta blockers mask the
symptoms of
hypoglycemia like tremors
,sweating and tachycardia

CONTRAINDICATED IN
PATIENTS ON INSULIN AND
OHA
REBOUND HYPERTENSION
CHRONIC THERAPY OF BETA BLOCKERS

UPREGULATION IN NUMBER OF RECEPTORS

NEWLY FORMED RECEPTORS ARE HYPER
RESPONSIVE TO CATECHOLAMINES

REBOUND HYPERTENSION ON STOPPING THE
DRUG
DOSE SHOULD BE GRADUALLY TAPERED
ADVERSE LIPID PROFILE
TOTAL TG 
LDL
HDL 
• TIMOLOL:USED IN GLAUCOMA
• SOTALOL: K CHANNEL BLOCKING AND
ANTIARRHYTHMIC PROPERTY
• NADOLOL:LONG HALF LIFE,LEAST FIRST PASS
METABOLISM
CARDIOSELECTIVE
BLOCKERS
• BLOCKS β1 RECEPTORS
• METOPROLOL
• ATENOLOL
• BISOPROLOL
• NEBIVOLOL
• ESMOLOL
• BETAXOLOL
Advantages over non-selective
blockers
• Safer in asthmatics
• Safer in diabetes
• Safer in Reynaud’s disease
• Less deleterious effect on lipid profile
• Metaprolol:
• Completely absorbed orally
• BA less due to first pass metabolism
Atenolol:Does not cross BBB
Bisoprolol:Used in hypertension and angina
NEBIVOLOL
New highly selective beta1 blocker
Rapid onset action
Less deleterious effect on lipids
• ESMOLOL:
• Ultra short acting beta 1 antagonist
• Given IV in urgent settings when beta1
blockade of short duration is desired.
• Eg:
• SVT,AF
• completely withdrawn
if adverse effects like bradycardia
or heart failure occur
• BETAXOLOL
• Used as eye drops in glaucoma
• Less efficacious than Timolol
• Safer in asthmatics and diabetics
NON SELECTIVE BLOCKERS WITH ISA
PINDOLOL
OXPRENOLOL
ADVANTAGES:
Lesser bradycardia and myocardial
depression
SELECTIVE BLOCKERS WITH ISA
• ACEBUTOLOL
• CELIPROLOL
• Celiprolol:
• Partial agonist at beta 2 receptors
• Used in hypertensives with asthma
Mixed antagonists
• LABETALOL
• CARVEDILOL
LABETELOL
• Blocks alpha1 and beta receptors
• Fall in BP due to alpha 1 and beta1
blockade
• Uses:
• Pheochromocytoma
• Rebound hypertension after clonidne
withdrawal
Carvedilol
• Blocks alpha and beta receptors
• USES:
• Essential hypertension
• CHF
• Reduces mortality in MI
Selective β2 blockers
• BUTOXAMINE
• EXPERIMENTAL
• NO CLINICAL UTILITY
NON SELECTIVE BETA
BLOCKERS
• CARDIOVASCULAR USES
• 2H 2A MI
• Hypertension
• Heart failure
• Angina
• Arrhythmia
• Myocardial Infarction
NON CARDIOVASCULAR USES
MIGRAINE
ANXIETY
GLAUCOMA
HYPERTHYROIDISM
PHEOCHROMOCYTOMA
ALCOHOL WITHDRAWAL
MAGH PAW
ADVERSE EFFECTS AND CI
• BRONCHOCONSTRICTION
• BRADYCARDIA
• COLD EXTREMITIES
• CNS SIDE EFFECTS
• HEART FAILURE
• HYPOGLYCEMIA
• REBOUND HYPERTENSION
• ADVERSE LIPID PROFILE
• 2(BCH) RHAL
CARDIOSELECTIVE BETA
BLOCKERS
• NEBIVOLOL
• BETAXOLOL
• BISOPROLOL
• ACEBUTOLOL
• ESMOLOL
• ATENOLOL
• METOPROLOL
• CELIPROLOL
NEW
BETA
BLOCKERS
ACTING
EXCLUSIVELY
AT
MYO
CARDIUM
BETA BLOCKERS WITH ISA
• CELIPROLOL,OXPRENOLOL
• PINDOLOL,PENBUTOLOL
• ACEBUTOLOL
• ALPRENOLOL
CONTAIN
PARTIAL
AGONISTIC
ACTIVITY
BETA BLOCKERS WITH MSA
• PROPRANOLOL
• METOPROLOL
• LABETALOL
• ACEBUTOLOL
• PINDOLOL
POSSESSES
MEMBRANE STABILISING
LOCAL
ANAESTHETIC
PROPERTY
LIPID INSOLUBLE BETA BLOCKERS
• EXCRETED BY KIDNEY
• LONG DOA
• CI IN RF
• NADOLOL
• SOTALOL
• ATENOLOL,ACEBUTOLOL
• BETAXOLOL,BISOPROLOL
• CELIPROLOL
• NOT SOLUBLE ABC
• Longest acting beta blocker: NADOLOL
• Shortest acting: ESMOLOL
• Beta blocker with cardioselectivity, ISA, MSA and lipid
solubility: ACEBUTOLOL
• Most commonly used beta blocker in chronic CHF:
CARVEDILOL(has antioxidant and antimitogenic
property)
All are non selective beta blockers
except:
a)Propranolol
b)Timolol
c)Sotalol
d)Carvedilol
Ans: d
Carvedilol alpha +beta blocker
All are cardioselective beta blockers except:
a)Atenolol
b)Esmolol
c)Bisoprolol
d)Labetalol
Ans:d
NEW
BETA
BLOCKERS
ACTING
EXCLUSIVELY
AT
MYO
CARDIUM
Combined alpha and beta blockers are:
a)Labetalol
b)Prazocin
c)Tamsulosin
d)Milrinone
Ans:a
Contraindication of beta blockers are:
a)Asthma
b)Angina
c)Hypertension
d)Arrhythmia
Ans: a
Beta blockers with ISA are:
a)Propranolol
b)Oxprenolol
c)Esmolol
d)Butoxamine
Ans: b
Beta blocker with cardioselectivity,membrane stabilsing
property and ISA:
a)Carvedilol
b)Atenolol
c)Acebutolol
d)Metoprolol
Ans: c
Propranolol can be used in all except:
a)Hyperthyroidism
b)Prinzmetal angina
c)Migraine
d)Hypertension
Ans: b
Beta blockers are CI in Diabetes as it :
a)Causes hyperglycemia
b)Causes seizure
c)Masks symptoms of hypoglycemia
d)Causes hypotension
Ans: c
An ultra short acting beta blocker:
a)Esmolol
b)Timolol
c)Atenolol
d)Pindolol
Ans: a
Adverse effects of beta blockers include:
a)Compensated heart failure
b)Masking the features of hypoglycemia
c)Bronchial asthma
d)All the above
Ans: d
Beta blockers

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