Successfully reported this slideshow.
We use your LinkedIn profile and activity data to personalize ads and to show you more relevant ads. You can change your ad preferences anytime.
BETA BLOCKERS
Dr. RENJU.S.RAVI MD
OVERVIEW
Introduction
MOA
Classification
Actions
Adverse effects
Drug interactions
Uses
Contraindications
Overdose
BETA BLOCKERS
Drugs which inhibit adrenergic
response mediated by beta receptors
BETA RECEPTORS
Receptors Sites actions
β1 Heart
JG cells-kidney
Posterior pituitary
Adipose tissue
stimulatory
Renin relea...
Professor Raymond P Ahlquist
Classified adrenoreceptors.
(1948)
HISTORY
1st β blocker –DICHLORO
ISOPROTERENOL-1958
PRONETHALOL---1962
PROPRANOLOL--1963
NEWER β BLOCKERS
James Black
MOA
Ac
PKA
α
GTP
ATP
cAMP
+
GDP
α βγ
MECHANISM OF ACTION
Via GPCR
Antagonist binding to receptor
No stimulation of G protein
No change in cAMP conc
No EFFECT
PROPERTIES
Receptor Blockade
Nonselective β blockade
Selective β1 blockade
Β+α blockade
Intrinsic sympathomimetic pro...
CLASSIFICATION
Beta blockers
1st
generation
Classical
Non
selective
2nd
generation
Classical
Beta 1
selective
3rd generati...
1ST GENERATION – NON SELECTIVE
With ISA only
Penbutolol
With MSA only
Propranolol
With ISA & MSA
Pindolol
Without ISA ...
2ND GENERATION – SELECTIVE Β1
AGENTS
With MSA only
Metoprolol
With ISA & MSA
Acebutolol
Without ISA &MSA
Atenolol
Bisop...
3RD GENERATION
Non-selective Selective
With ISA
Carteolol
With ISA
Celiprolol
With MSA
Betaxolol
With MSA
Carvedilol
With ...
Β BLOCKERS
With ISA
Penbutolol
Carteolol
Celiprolol
Both
Pindolol
Acebutolol
Labetalol
With MSA
Propranolol
Metoprolol
Bet...
PROPERTIES OF Β1 SELECTIVITY
Less broncho constriction
Less interference with CHO metabolism less
hypoglycemia  prefer...
PROPERTIES OF ISA
Less bradycardia
Less rebound effect on withdrawal
Less deleterious effect on blood lipid
profile
No...
ACTIONS
On CVS
Heart
 Negative
Ionotropy
Chronotropy
Dromotropy
Bathmotropy
ACTIONS….
On CVS
Blood vessel
Vasoconstriction in prone
individuals  Direct
Vasodilatation  due to
additional proper...
ACTIONS….
On CVS
Antihypertensive action
Decreased CO
Decreased TPR on long term
administration
Decreased renin relea...
BETABLOCKERS WITH
VASODILATOR PROPERTY
Alpha blockade
Labetalol
Carvedilol
Bucindolol
Bevantolol
Nipradilol
Beta2 agonism
...
ACTIONS -CNS
Anti anxiety
Behaviour changes
Forgetfulness
Night mares
Increased dreaming
Non-selective
lipid soluble
ACTIONS -METABOLIC
CHO metabolism
Hypoglycemia
Inhibits muscle glycogenolysis
Hypoglycemic unawareness
Lipid
Increas...
ACTIONS - EYE
Decrease secretion
of aqueous
Decrease IOT
No effect on pupil size or
accommodation
Ciliary
body
ACTIONS- BRONCHUS
Increases airway
resistance
Less with
beta 1 selective
agents
SKELETAL MUSCLES
o Decrease exercise capacity
By decreasing blood flow
Inhibit glycogenolysis and
lipolysis.
MISCELLANEOUS
o Antagonise catecholamine
induced
Tremor
Inhibition of mast cell
degranulation
o Prevent platelet aggrega...
Water soluble
Lipid solubleBy Liver
By Kidney
100% 80 60 40 20 0
0 20 40 60 80 100%
PROPRANOLOL TIMOLOL PINDOLOL BISOPROLO...
ADVERSE EFFECTS - CVS
Bradycardia
Exacerbation of
angina
Precipitation of CHF
ADVERSE EFFECTS…
Increased air way
resistance
worsening of
bronchial asthma
ADVERSE REACTIONS
Impairment of carbohydrate tolerance
Alteration of lipid profile
Rebound hypertension on withdrawal
...
ADVERSE EFFECTS…
Nightmares
Decreased exercise capacity
Tiredness
Lack of drive
DRUG INTERACTIONS
PHARMACOKINETIC
• Al salts, Cholestyramine
Decrease absorption
• Enzyme inducers
Decrease plasma conc.
•...
USES
CARDIOVASCULAR
Hypertension
Angina
Myocardial infarction
Arrhythmia
Cardiomyopathy
CCF
Dissecting aneurysm of
...
HYPERTENSION
Cardioselective beta blockers
Rationale
Decrease in HR,CO,
myocardial contractility.
Decrease renin relea...
ANGINA
Metoprolol
Atenolol
Bisoprolol
ProphylaxisTreatment
Contraindication
•Variant angina
ANGINA - RATIONALE
Decrease HR & contractility
Decrease myocardial oxygen demand
Antianginal action
MI
o Prophylaxiso Treatment
 Anti anginal action
 Reduce infarct size
 Prevents arrhythmia
 Prevents reinfarction
 Pr...
ARRYTHMIAS
Propranolol
Esmolol
Acebutolol
Sotalol
Decreases AV conduction
Inhibits impulses from
atria to ventricle 
...
ARRHYTHMIA
Control ventricular rate in atrial flutter and
fibrillation.
Suppress extrasystole and tachycardia especially...
HOCM
↓ contractility
↓ LV outflow obstruction
Improve cardiac output in
exercise
CHF
ONLY in compensated CHF
Antagonise sympathetic overactivity
on myocardium
Prevents myocyte apoptosis
↓ cardiac remo...
DISSECTING AORTIC ANEURYSM
↓ cardiac contractility, and aortic
pulsation.
NON - CARDIAC USES
o Pheochromocytoma
Used after an α blocker
To control tachycardia and arrhythmia
Suppress cardiomyop...
MIGRAINE PROPHYLAXIS
Propranolol
Nadolol
Metoprolol
PORTAL HYPERTENSION
To Decrease Portal Vein
Pressure in Patients with
Cirrhosis
Decrease variceal bleeding
Propranolol
GLAUCOMA
Decrease aqueous
humour secretion
Attenuating neuronal Ca
and Na influx 
Protection to retinal
neurons
Inhibi...
CNS
Anxiety
Essential tremor
Akathisia induced by
antipsychotics
Alcohol withdrawal
3RD GENERATION AGENTS
Drug MSA ISA Beta blockade Other properties
Labetalol + + Non selective α1 blockade
Carvedilol + Non...
CONTRAINDICATIONS
Absolute
1. Severe Bradycardia
2. Pre-existing High Grade Heart Block
3. Overt Untreated Heart Failure
4...
CONTRAINDICATIONS
Relative
1. Prinzmetals Angina
2. Concomitant Use Of :Verapamil/
Diltiazam/Digoxin
3. Mild Asthma
4. Ins...
OVERDOSAGE
Manifestations  extension of pharmacological
properties
Hypotension
Bradycardia
Prolonged Conduction Times
Wid...
SIGNS AND SYMPTOMS
Seizures
Depression
Hypoglycemia
Bronchospasm
TREATMENT
Atropine Initially
Cardiac Pacemakers Required
Large amt of Isoproterenol /  Agonist
Glucagon
B blockers
Upcoming SlideShare
Loading in …5
×

B blockers

CLASS FOR UNDER GRADUATES

  • Login to see the comments

B blockers

  1. 1. BETA BLOCKERS Dr. RENJU.S.RAVI MD
  2. 2. OVERVIEW Introduction MOA Classification Actions Adverse effects Drug interactions Uses Contraindications Overdose
  3. 3. BETA BLOCKERS Drugs which inhibit adrenergic response mediated by beta receptors
  4. 4. BETA RECEPTORS Receptors Sites actions β1 Heart JG cells-kidney Posterior pituitary Adipose tissue stimulatory Renin release ADH release lipolysis β2 Bronchi Blood vessels of skeletal muscle Smooth muscle (Uterus ,intestine , detrusor) Liver, Muscle Adipose tissue Eye Bronchodilation Vasodilatation Relaxation Glycogenolysis Lipolysis Enhanced aqueous secretion β3 Adipose tissue Lipolysis
  5. 5. Professor Raymond P Ahlquist Classified adrenoreceptors. (1948)
  6. 6. HISTORY 1st β blocker –DICHLORO ISOPROTERENOL-1958 PRONETHALOL---1962 PROPRANOLOL--1963 NEWER β BLOCKERS James Black
  7. 7. MOA Ac PKA α GTP ATP cAMP + GDP α βγ
  8. 8. MECHANISM OF ACTION Via GPCR Antagonist binding to receptor No stimulation of G protein No change in cAMP conc No EFFECT
  9. 9. PROPERTIES Receptor Blockade Nonselective β blockade Selective β1 blockade Β+α blockade Intrinsic sympathomimetic property-ISA (partial agonistic action) Membrane stabilising action-MSA (Local anaesthetic action-Na channel block)
  10. 10. CLASSIFICATION Beta blockers 1st generation Classical Non selective 2nd generation Classical Beta 1 selective 3rd generation Newer Non selective & beta1 selective + Add. properties
  11. 11. 1ST GENERATION – NON SELECTIVE With ISA only Penbutolol With MSA only Propranolol With ISA & MSA Pindolol Without ISA &MSA Timolol Nadolol Sotalol
  12. 12. 2ND GENERATION – SELECTIVE Β1 AGENTS With MSA only Metoprolol With ISA & MSA Acebutolol Without ISA &MSA Atenolol Bisoprolol Esmolol
  13. 13. 3RD GENERATION Non-selective Selective With ISA Carteolol With ISA Celiprolol With MSA Betaxolol With MSA Carvedilol With MSA & ISA Labetalol
  14. 14. Β BLOCKERS With ISA Penbutolol Carteolol Celiprolol Both Pindolol Acebutolol Labetalol With MSA Propranolol Metoprolol Betaxolol Carvedilol Without ISA & MSA Timolol, Sotalol, Nadolol Atenolol, Bisoprolol, Esmolol
  15. 15. PROPERTIES OF Β1 SELECTIVITY Less broncho constriction Less interference with CHO metabolism less hypoglycemia  preferred in diabetics Less chances of Raynaud's phenomenon Less deleterious effect on blood lipid profile Less impairment of exercise capacity Less effect on tremor
  16. 16. PROPERTIES OF ISA Less bradycardia Less rebound effect on withdrawal Less deleterious effect on blood lipid profile Not effective in migraine prophylaxis Not suitable for secondary prophylaxis of MI
  17. 17. ACTIONS On CVS Heart  Negative Ionotropy Chronotropy Dromotropy Bathmotropy
  18. 18. ACTIONS…. On CVS Blood vessel Vasoconstriction in prone individuals  Direct Vasodilatation  due to additional properties Precipitates Reynaud's disease •α1 blockade •β2 agonism •Ca ++ channel block •K+ channel opening •NO production
  19. 19. ACTIONS…. On CVS Antihypertensive action Decreased CO Decreased TPR on long term administration Decreased renin release
  20. 20. BETABLOCKERS WITH VASODILATOR PROPERTY Alpha blockade Labetalol Carvedilol Bucindolol Bevantolol Nipradilol Beta2 agonism Celiprolol Carteolol Bopindolol CCB action Betaxolol Bevantolol Carvedilol K+ Channel opening Tilisolol NO production Celiprolol Carteolol Bopindolol Nipradilol Nebivolol Anti oxidant Carvedilol
  21. 21. ACTIONS -CNS Anti anxiety Behaviour changes Forgetfulness Night mares Increased dreaming Non-selective lipid soluble
  22. 22. ACTIONS -METABOLIC CHO metabolism Hypoglycemia Inhibits muscle glycogenolysis Hypoglycemic unawareness Lipid Increases VLDL(TG) levels Alters HDL/LDL ratio Less with β 1 selective agents
  23. 23. ACTIONS - EYE Decrease secretion of aqueous Decrease IOT No effect on pupil size or accommodation Ciliary body
  24. 24. ACTIONS- BRONCHUS Increases airway resistance Less with beta 1 selective agents
  25. 25. SKELETAL MUSCLES o Decrease exercise capacity By decreasing blood flow Inhibit glycogenolysis and lipolysis.
  26. 26. MISCELLANEOUS o Antagonise catecholamine induced Tremor Inhibition of mast cell degranulation o Prevent platelet aggregation and promote fibrinolysis
  27. 27. Water soluble Lipid solubleBy Liver By Kidney 100% 80 60 40 20 0 0 20 40 60 80 100% PROPRANOLOL TIMOLOL PINDOLOL BISOPROLOL ACEBUTOLOL ATENOLOL CARVEDILOL NADOLOL METOPROLOL SOTALOL LABETALOL CARTEOLOL PENBUTOLOL Pharmacokinetics
  28. 28. ADVERSE EFFECTS - CVS Bradycardia Exacerbation of angina Precipitation of CHF
  29. 29. ADVERSE EFFECTS… Increased air way resistance worsening of bronchial asthma
  30. 30. ADVERSE REACTIONS Impairment of carbohydrate tolerance Alteration of lipid profile Rebound hypertension on withdrawal Cold hands and feet, worsening of PVD
  31. 31. ADVERSE EFFECTS… Nightmares Decreased exercise capacity Tiredness Lack of drive
  32. 32. DRUG INTERACTIONS PHARMACOKINETIC • Al salts, Cholestyramine Decrease absorption • Enzyme inducers Decrease plasma conc. • Cimitidine, Hydralazine Increase BA • They impair clearance of lidocaine PHARMACODYNAMIC Digoxin CCB (Verapamil) CCB (DHP) NSAIDs Adrenaline & other α agonists
  33. 33. USES CARDIOVASCULAR Hypertension Angina Myocardial infarction Arrhythmia Cardiomyopathy CCF Dissecting aneurysm of aorta NON - CARDIOVASCULAR Thyrotoxicosis Pheochromocytoma Migraine prophylaxis Essential tremor Glaucoma Anxiety Portal hypertension Anti psychotic induced akathesia
  34. 34. HYPERTENSION Cardioselective beta blockers Rationale Decrease in HR,CO, myocardial contractility. Decrease renin release Decrease central sympathetic out flow
  35. 35. ANGINA Metoprolol Atenolol Bisoprolol ProphylaxisTreatment Contraindication •Variant angina
  36. 36. ANGINA - RATIONALE Decrease HR & contractility Decrease myocardial oxygen demand Antianginal action
  37. 37. MI o Prophylaxiso Treatment  Anti anginal action  Reduce infarct size  Prevents arrhythmia  Prevents reinfarction  Prevents arrhythmia Metoprolol Esmolol Timolol
  38. 38. ARRYTHMIAS Propranolol Esmolol Acebutolol Sotalol Decreases AV conduction Inhibits impulses from atria to ventricle  controls ventricular rate Mainly effective in Arrhythmias precipitated by catecholamines Sotalol K+ channel block class3 anti arrhythmic Esmolol ultra short acting supraventricular tachycardia
  39. 39. ARRHYTHMIA Control ventricular rate in atrial flutter and fibrillation. Suppress extrasystole and tachycardia especially mediated adrenergically .
  40. 40. HOCM ↓ contractility ↓ LV outflow obstruction Improve cardiac output in exercise
  41. 41. CHF ONLY in compensated CHF Antagonise sympathetic overactivity on myocardium Prevents myocyte apoptosis ↓ cardiac remodelling Retard progression of CHF Metoprolol Bisoprolol Carvedilol
  42. 42. DISSECTING AORTIC ANEURYSM ↓ cardiac contractility, and aortic pulsation.
  43. 43. NON - CARDIAC USES o Pheochromocytoma Used after an α blocker To control tachycardia and arrhythmia Suppress cardiomyopathy due to excess catecholamines o Thyrotoxicosis Control sympathetic symptoms Inhibit peripheral conversion of T4 to T3 Preoperative use
  44. 44. MIGRAINE PROPHYLAXIS Propranolol Nadolol Metoprolol
  45. 45. PORTAL HYPERTENSION To Decrease Portal Vein Pressure in Patients with Cirrhosis Decrease variceal bleeding Propranolol
  46. 46. GLAUCOMA Decrease aqueous humour secretion Attenuating neuronal Ca and Na influx  Protection to retinal neurons Inhibit ganglion cell death Timolol Carteolol Betaxolol Levobetaxolol Levobunolol Metipranolol
  47. 47. CNS Anxiety Essential tremor Akathisia induced by antipsychotics Alcohol withdrawal
  48. 48. 3RD GENERATION AGENTS Drug MSA ISA Beta blockade Other properties Labetalol + + Non selective α1 blockade Carvedilol + Non selective α1 blockade,CCB Antioxidant Bucindolol + Non selective α1 blockade,β2,β3 agonism Increases HDL cholesterol Celiprolol + β1 selective β2 agonism NO release Nebivolol β1 selective •NO release •Inhibits platelet aggregation Bevantolol Nonselective α1 blockade CCB
  49. 49. CONTRAINDICATIONS Absolute 1. Severe Bradycardia 2. Pre-existing High Grade Heart Block 3. Overt Untreated Heart Failure 4. Cardiogenic Shock 5. Severe Bronchospasm 6. Severe Depression 7. Active Raynaud’s Phenomenon
  50. 50. CONTRAINDICATIONS Relative 1. Prinzmetals Angina 2. Concomitant Use Of :Verapamil/ Diltiazam/Digoxin 3. Mild Asthma 4. Insulin Requiring DM
  51. 51. OVERDOSAGE Manifestations  extension of pharmacological properties Hypotension Bradycardia Prolonged Conduction Times Widened QRS Complexes
  52. 52. SIGNS AND SYMPTOMS Seizures Depression Hypoglycemia Bronchospasm
  53. 53. TREATMENT Atropine Initially Cardiac Pacemakers Required Large amt of Isoproterenol /  Agonist Glucagon

×