Recommended
More Related Content
What's hot
What's hot (20)
Similar to B blockers
Similar to B blockers (20)
More from Dr Renju Ravi
More from Dr Renju Ravi (20)
Recently uploaded
Recently uploaded (20)
B blockers
- 3. BETA BLOCKERS Drugs which inhibit adrenergic response mediated by beta receptors
- 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. Professor Raymond P Ahlquist Classified adrenoreceptors. (1948)
- 6. HISTORY 1st β blocker –DICHLORO ISOPROTERENOL-1958 PRONETHALOL---1962 PROPRANOLOL--1963 NEWER β BLOCKERS James Black
- 8. MECHANISM OF ACTION Via GPCR Antagonist binding to receptor No stimulation of G protein No change in cAMP conc No EFFECT
- 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. CLASSIFICATION Beta blockers 1st generation Classical Non selective 2nd generation Classical Beta 1 selective 3rd generation Newer Non selective & beta1 selective + Add. properties
- 11. 1ST GENERATION – NON SELECTIVE With ISA only Penbutolol With MSA only Propranolol With ISA & MSA Pindolol Without ISA &MSA Timolol Nadolol Sotalol
- 12. 2ND GENERATION – SELECTIVE Β1 AGENTS With MSA only Metoprolol With ISA & MSA Acebutolol Without ISA &MSA Atenolol Bisoprolol Esmolol
- 13. 3RD GENERATION Non-selective Selective With ISA Carteolol With ISA Celiprolol With MSA Betaxolol With MSA Carvedilol With MSA & ISA Labetalol
- 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. 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. 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
- 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. ACTIONS…. On CVS Antihypertensive action Decreased CO Decreased TPR on long term administration Decreased renin release
- 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. ACTIONS -CNS Anti anxiety Behaviour changes Forgetfulness Night mares Increased dreaming Non-selective lipid soluble
- 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. ACTIONS - EYE Decrease secretion of aqueous Decrease IOT No effect on pupil size or accommodation Ciliary body
- 24. ACTIONS- BRONCHUS Increases airway resistance Less with beta 1 selective agents
- 25. SKELETAL MUSCLES o Decrease exercise capacity By decreasing blood flow Inhibit glycogenolysis and lipolysis.
- 26. MISCELLANEOUS o Antagonise catecholamine induced Tremor Inhibition of mast cell degranulation o Prevent platelet aggregation and promote fibrinolysis
- 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. ADVERSE EFFECTS - CVS Bradycardia Exacerbation of angina Precipitation of CHF
- 29. ADVERSE EFFECTS… Increased air way resistance worsening of bronchial asthma
- 30. ADVERSE REACTIONS Impairment of carbohydrate tolerance Alteration of lipid profile Rebound hypertension on withdrawal Cold hands and feet, worsening of PVD
- 31. ADVERSE EFFECTS… Nightmares Decreased exercise capacity Tiredness Lack of drive
- 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. 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. HYPERTENSION Cardioselective beta blockers Rationale Decrease in HR,CO, myocardial contractility. Decrease renin release Decrease central sympathetic out flow
- 36. ANGINA - RATIONALE Decrease HR & contractility Decrease myocardial oxygen demand Antianginal action
- 37. MI o Prophylaxiso Treatment Anti anginal action Reduce infarct size Prevents arrhythmia Prevents reinfarction Prevents arrhythmia Metoprolol Esmolol Timolol
- 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. ARRHYTHMIA Control ventricular rate in atrial flutter and fibrillation. Suppress extrasystole and tachycardia especially mediated adrenergically .
- 40. HOCM ↓ contractility ↓ LV outflow obstruction Improve cardiac output in exercise
- 41. CHF ONLY in compensated CHF Antagonise sympathetic overactivity on myocardium Prevents myocyte apoptosis ↓ cardiac remodelling Retard progression of CHF Metoprolol Bisoprolol Carvedilol
- 42. DISSECTING AORTIC ANEURYSM ↓ cardiac contractility, and aortic pulsation.
- 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
- 45. PORTAL HYPERTENSION To Decrease Portal Vein Pressure in Patients with Cirrhosis Decrease variceal bleeding Propranolol
- 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. CNS Anxiety Essential tremor Akathisia induced by antipsychotics Alcohol withdrawal
- 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. 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. CONTRAINDICATIONS Relative 1. Prinzmetals Angina 2. Concomitant Use Of :Verapamil/ Diltiazam/Digoxin 3. Mild Asthma 4. Insulin Requiring DM
- 51. OVERDOSAGE Manifestations extension of pharmacological properties Hypotension Bradycardia Prolonged Conduction Times Widened QRS Complexes
- 53. TREATMENT Atropine Initially Cardiac Pacemakers Required Large amt of Isoproterenol / Agonist Glucagon