Beta Blockers

Dr. SHUBHAM JAJU

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Before you proceed on this section,
brush up where β receptors located
and what are their effects…..

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ISA : Intrinsic Sympathomimetic Activity
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 PHARMACOLOGICAL ACTIONS
• HEART :
– Decrease in ….
• Automaticity & HR
• Cardiac output
• Oxygen consumption
• AV conduction
– These effects are mediated by β1 receptors

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• BLOOD VESSELS :
– Initially increase in total peripheral resistance followed
by fall.
– Promotes PG synthesis in several vascular beds 
vasodilatation.
– Reduces portal venous pressure in cirrhosis.
– Blocks cerebral vasodilatation  used in migraine

• These effects are mediated by β 2 receptors

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• CNS :
– Forgetfulness
– Increased dreaming
– Nightmares
– Diminish libido.
– Suppresses anxiety  by peripheral action.
• RESPIRATORY TRACT :
– Bronchospasm with nonselective agents.
– These effects are mediated by β2 receptors

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• METABOLIC :
– FAT METABOLISM:
• Adrenergic system produces lipolysis
• So BB increases TG and LDL/HDL ratio.
– CARBOHYDRATE METABOLISM :
• Normally…….
• HYPOGLYCEMIA  RELEASE OF NA  GLYCOGENOLYSIS AND
NEOGLUCOGENESIS (by β2 receptors) NORMOGLYCEMIA
• BB block this
• So prolonged recovery from hypoglycemia.
• Prolonged therapy may cause decrease in insulin levels .
• These effects are medicated by β2 receptors

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These effects are medicated by β2
receptors

Reduce exercise capacity

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• EYES :
– Reduces aqueous humor formation
– Reduces IOP.
– These effects are medicated by β2 receptors
• BLOOD :
– Inhibits platelet aggregation and promotes
fibrinolysis
– Used in MI.

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These effects are very important….
Answer to yourself……..
• What are the effects of BB on heart ?
• What is effect of BB on various blood vessels?
• What is effect of BB on CNS function ?
• What is effect of BB on respiratory tract ?
• What is effect of BB on lipid metabolism ?
• What is effect of BB on carbohydrate metabolism ?
• What is effect of BB on skeletal muscles ?
• What is effect of BB on eye ?

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 ADVERSE REACTIONS
• ADRS RELATED TO HEART :

– Bradycardia, AV block and cardiac arrest in pt’ s with lower HR.

– Withdrawal symptoms : precipitation of MI due to upregulation &

super sensitivity of receptors.
– Aggravation of CHF

– These effects are mediated by β1 receptors

– Aggravation of variant angina due to β2 block which is coronary

vasodilator( with nonselective blockers only)

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• ADRS RELATED TO BLOOD VESSELS :

– Tiredness due to blockade of blood vessels β2 receptors in muscles,

because of loss of muscle perfusion and reduced cardiac output
– Cold hands and feet due to blockade of blood vessels β2 receptors in
skin
– Worsening of PVD due to blockade of blood vessels β2 receptors in
peripheral blood vessels which are vasodilator.
– These effects are medicated by β2 receptors

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• COPD & bronchial asthma  life threatening bronchoconstriction

– These effects are medicated by β2 receptors

• CNS : sleep disturbances, bad dreams, depression, loss of libido

• METABOLIC EFFECTS :
• Delayed recovery from hypoglycemia inhibits adrenergically induced
glycogenolysis and neoglucogenesis in response to hypoglycemia .(β2 )

• Inhibits adrenergically induced lipolysis  Dyslipidemia

• These effects are mediated by β2 receptors

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Contraindications of non-selective
β Blockers
• A- Asthma
• B - Block (AV)
• C - CHF
• D - Diabetes

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 These ADRs are very important,
answer to your self…..
• BB produce which cardiac ADRs ?
• BB produce which vascular ADRS ?
• BB produce which ADRs related to respiratory
tract ?
• BB produce which ADRs related to CNS ?
• BB produce which metabolic ADRs ?

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 Class specific effects
• Cardioselective BB :(β1 selective)
• This selectivity is relative , at higher doses, it blocks beta 2 receptors
as well……
– Less aggravation of bronchial asthma.
– Less worsening of glycemic control
– Less worsening of PVD
– Less dyslipidemia
– Do not block essential tremors
– Less impairment of exercise capacity due to action of energy
metabolism and blood flow to skeletal muscles.
• Because these effects are mediated by β2 receptors.

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• BB WITH Intrinsic Sympathomimetic Activity:
– No Bradycardia & -ve inotropic effect
– Less rebound hypertension.
– Less dyslipidemia
– Not effective in migraine
– Not effective for prophylaxis of MI.
– Pindolol, acebutolol.

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• BB WITH Membrane Stabilizing Activity :
– They have additional antiarrhythmic action.
– Propranolol, oxprenolol, acebutolol.

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 INDIVIDUAL BB
• Sotalol :
– Antiarrhythmic
• Timolol :
– Glaucoma
– Just like…. betoxolol, levobunolol, cartiolol, metipranolol.
• Pindolol :
– Intrinsic sympathomimetic activity
• Metoprolol :
– β1 selective
• Atenolol :
– β1 selective
• Acebutolol :
– ISA + MSA.
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• Esmolol :
– Shortest acting BB.
– Used in hypertensive emergency.
– 0.5 mg/kg infusion
– 0.02-0.5 mg/kg/min infusion.
• Celiprolol :
– β1 blocker + β2 agonist
– Safe in asthmatics
– Non adrenoceptor mediated vasodilatation due to NO release.
• Nebivolol :
– NO donor
– Improve endothelial function
– Delay atherosclerosis.
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 USES
1.Hypertension
2. Angina pectoris
3. Cardiac arrhythmias
4.MI
 During MI
 After MI
5.CHF
6.Thyrotoxicosis
7.Migraine
8.Anxiety
9.Tremors
10.Glaucoma
11.Treatment of withdrawal symptoms

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• 1.HYPERTENSION
HEART BLOOD PERIPHER
VESSELS CNS AL KIDNEY
NERVES

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• NEED A REVISION ?

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• ANGINA PECTORIS :
– It reduces myocardial oxygen consumption
– It reduces the frequency of anginal attack and improve exercise
tolerance.
• Antiarrhythmics :
– Retard post MI arrhythmias
– Control ventricular rate in Afi/Afl.
– Used in supraventricular and ventricular arrhythmias.
• MYOCARDIAL INFARCTION :
– During MI :
• Salvage myocardium, retards the progression of infarct by
decreasing oxygen consumption.
• Prevent arrhythmias
– After MI :
• Prevent post MI arrhythmias.
• Prevent second MI. 25
• Heart failure :
– Initially decrease cardiac out put  later increases it.
– CHF Sympathetical over activity myocardial remodelling and
myocardial apoptosis.
– To be avoided in severe heart failure
• Obstructive cardiomyopathy :
– Slow HR and improve ventricular ejection
• Dissecting aortic aneurysm :
– Decreases systolic BP
• Thyrotoxicosis :
– Reduce the extra sympathetic activity and control the
cardiovascular effects of raised thyroid hormone levels
• Migraine :
– Used for prophylaxis

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• Glaucoma :
– Reduces aqueous humor formation
• Essential Tremors :
– They reduce tremors
• Treatment of withdrawal symptoms :
– Alcohol and opioid withdrawl symptoms manifested by sympathetic
overactivity are treated by BB
• Cirrhosis:
– Reduce the portal venous pressure
– Reduce the bleeding for oesophageal varices
• Pheochromocytoma :
– Only after prior alpha blocker administration BB is administered.
– Other unopposed alpha action will produce severe increase in BP.
• Anxiety :
– Suppresses the peripheral manifestation of anxiety.
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 α+β blockers
• LABETOLOL :
– α1+β1+β2 blocking action
– Weak β2 agonists
– Fall in BP
– Uses :
• Pheochromocytoma
• Clonidine withdrawl
– ADR :
• Postural hypotension
• Failure of ejaculation
• Liver damage
• rashes
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• Carvedilol :
– β1+β2+α1 blocking action
– Calcium channel blocking
– Antioxidant activity
– HT
– Angina pectoris
– CHF.

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• Now it is time for self assessment…..

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• What are the effects of BB on heart ?
• What is effect of BB on various blood vessels?
• What is effect of BB on CNS function ?
• What is effect of BB on respiratory tract ?
• What is effect of BB on lipid metabolism ?
• What is effect of BB on carbohydrate metabolism ?
• What is effect of BB on skeletal muscles ?
• What is effect of BB on eye ?
• Which are the ADRs seen with BB ?
• Which are the uses of BB ?

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 Question 1
• A β-blocker was prescribed for hypertension in a female
asthma patient. After about a week of treatment, the
asthma attacks got worse, and the patient was asked to
stop taking the β-blocker. Which of the following β-
blockers would you suggest as an alternative in this
patient that is less likely to worsen her asthma?
A. Propranolol.
B. Metoprolol.
C. Labetalol.
D. Carvedilol.

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• Correct answer = B.
• The patient was most likely given a nonselective β-
blocker (antagonizes both β1 and β2 receptors) that
made her asthma worse due to β2 antagonism.
• An alternative is to prescribe a cardio selective
(antagonizes only β1) β-blocker that does not
antagonize β2 receptors in the bronchioles.
• Metoprolol is a cardio selective β-blocker.
• Propranolol, labetalol, and carvedilol are nonselective
β-blockers and could worsen the asthma.

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THANK YOU
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