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Beta blockers
- 3. SYMPATHETIC RECEPTORS β1 β2 β3 BETA RECEPTORS
- 4. BETA 1 HEART BETA 2 BRONCHUS GIT BLADDER UTERUS LIVER BLOOD VESSELS BETA 3 ADIPOSE TISSUE
- 5. BETA BLOCKERS Beta adrenergic receptor antagonists act on Β1 or β2 receptors or on both
- 6. SIR JAMES BLACK DEVELOPED BETA BLOCKER PROPRANOL IN 1958 AWARDED NOBEL PRIZE FOR MEDICINE IN 1988
- 12. NON SELECTIVE BLOCKERS • Blocks both β1 and β2 receptors • Eg:Propranolol
- 14. CARDIOVASCULAR USES BLOCK CARDIAC β1 RECEPTORS HEART RATE MYOCARDIAL CONTRACTILITY CARDIAC OUTPUT BP
- 15. CARDIOVASCULAR USES • ESSENTIAL HYPERTENSION • CONGESTIVE HEART FAILURE • ANGINA PECTORIS • CARDIAC ARRHYTHMIAS • MYOCARDIAL INFARCTION
- 16. ESSENTIAL HYPERTENSION • Alone or in combination with diuretics • Rationale – Decrease in HR,CO ,myocardial contractility. – Decrease renin release Dose: 20-40mg TDS
- 17. 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
- 18. ANGINA PECTORIS DECREASES OXYGEN DEMAND INCREASES EXERCISE TOLERANCE CI:PRINZMETAL’S ANGINASENSATION OF CHEST PAIN IMBALANCE BTW OXYGEN DEMAND AND SUPPLY
- 19. CARDIAC ARRHYTHMIAS • Used in SVT associated with thyrotoxicosis, • Digitalis toxicity Mechanism: • Membrane stabilising effect IRREGULAR HEARTBEAT TACHYCARDIA PALPITATIONS
- 20. MYOCARDIAL INFARCTION Decrease incidence,recurrence,mortality Prevent VF at the second attack of MI Dose: 40-80 mg tds orally
- 21. NON CARDIOVASCULAR USES • Migraine Anxiety provoking situations • Glaucoma • Hyperthyroidism • Pheochromocytoma • Alcohol withdrawal • Oesophageal varices
- 22. NON CARDIOVASCULAR USES • MIGRAINE • Prophylaxis • Not for acute attack • Dose:20mg tds orally
- 23. ANXIETY Reduce anxiety Block peripheral manifestations of anxiety:tremors, sweating DOSE:10-20 MG TDS
- 24. GLAUCOMA Decrease intraocular pressure Propranolol not used Eg:Timolol topically
- 26. PHEOCHROMOCYTOMA GIVEN IN COMBINATION WITH α BLOCKER control tachycardia and arrythmia DOSE:20MG TDS FOR 3 DAYS BEFORE SURGERY
- 27. ALCOHOL WITHDRAWAL Reduces sympathetic overactivity during phase of withdrawal Dose:20 mg BD orally
- 28. ADVERSE EFFECTS • BRONCHOCONSTRICTION • BRADYCARDIA • COLD EXTREMITIES • CNS SIDE EFFECTS • HEART FAILURE • HYPOGLYCEMIA • REBOUND HYPERTENSION • ADVERSE LIPID PROFILE
- 30. BRADYCARDIA Can lower HR to 55 bpm BRADYARRHYTHMIA HEART BLOCK
- 31. 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
- 32. CNS SIDE EFFECTS SLEEP DISTURBANCES DEPRESSION NIGHTMARES
- 33. 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
- 34. HYPOGLYCEMIA Beta blockers mask the symptoms of hypoglycemia like tremors ,sweating and tachycardia CONTRAINDICATED IN PATIENTS ON INSULIN AND OHA
- 35. 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
- 36. ADVERSE LIPID PROFILE TOTAL TG LDL HDL
- 37. • TIMOLOL:USED IN GLAUCOMA • SOTALOL: K CHANNEL BLOCKING AND ANTIARRHYTHMIC PROPERTY • NADOLOL:LONG HALF LIFE,LEAST FIRST PASS METABOLISM
- 38. CARDIOSELECTIVE BLOCKERS • BLOCKS β1 RECEPTORS • METOPROLOL • ATENOLOL • BISOPROLOL • NEBIVOLOL • ESMOLOL • BETAXOLOL
- 39. Advantages over non-selective blockers • Safer in asthmatics • Safer in diabetes • Safer in Reynaud’s disease • Less deleterious effect on lipid profile
- 40. • Metaprolol: • Completely absorbed orally • BA less due to first pass metabolism Atenolol:Does not cross BBB Bisoprolol:Used in hypertension and angina
- 41. NEBIVOLOL New highly selective beta1 blocker Rapid onset action Less deleterious effect on lipids
- 42. • 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
- 43. • BETAXOLOL • Used as eye drops in glaucoma • Less efficacious than Timolol • Safer in asthmatics and diabetics
- 44. NON SELECTIVE BLOCKERS WITH ISA PINDOLOL OXPRENOLOL ADVANTAGES: Lesser bradycardia and myocardial depression
- 45. SELECTIVE BLOCKERS WITH ISA • ACEBUTOLOL • CELIPROLOL • Celiprolol: • Partial agonist at beta 2 receptors • Used in hypertensives with asthma
- 46. Mixed antagonists • LABETALOL • CARVEDILOL
- 47. LABETELOL • Blocks alpha1 and beta receptors • Fall in BP due to alpha 1 and beta1 blockade • Uses: • Pheochromocytoma • Rebound hypertension after clonidne withdrawal
- 48. Carvedilol • Blocks alpha and beta receptors • USES: • Essential hypertension • CHF • Reduces mortality in MI
- 49. Selective β2 blockers • BUTOXAMINE • EXPERIMENTAL • NO CLINICAL UTILITY
- 50. NON SELECTIVE BETA BLOCKERS • CARDIOVASCULAR USES • 2H 2A MI • Hypertension • Heart failure • Angina • Arrhythmia • Myocardial Infarction
- 51. NON CARDIOVASCULAR USES MIGRAINE ANXIETY GLAUCOMA HYPERTHYROIDISM PHEOCHROMOCYTOMA ALCOHOL WITHDRAWAL MAGH PAW
- 52. ADVERSE EFFECTS AND CI • BRONCHOCONSTRICTION • BRADYCARDIA • COLD EXTREMITIES • CNS SIDE EFFECTS • HEART FAILURE • HYPOGLYCEMIA • REBOUND HYPERTENSION • ADVERSE LIPID PROFILE • 2(BCH) RHAL
- 53. CARDIOSELECTIVE BETA BLOCKERS • NEBIVOLOL • BETAXOLOL • BISOPROLOL • ACEBUTOLOL • ESMOLOL • ATENOLOL • METOPROLOL • CELIPROLOL NEW BETA BLOCKERS ACTING EXCLUSIVELY AT MYO CARDIUM
- 54. BETA BLOCKERS WITH ISA • CELIPROLOL,OXPRENOLOL • PINDOLOL,PENBUTOLOL • ACEBUTOLOL • ALPRENOLOL CONTAIN PARTIAL AGONISTIC ACTIVITY
- 55. BETA BLOCKERS WITH MSA • PROPRANOLOL • METOPROLOL • LABETALOL • ACEBUTOLOL • PINDOLOL POSSESSES MEMBRANE STABILISING LOCAL ANAESTHETIC PROPERTY
- 56. LIPID INSOLUBLE BETA BLOCKERS • EXCRETED BY KIDNEY • LONG DOA • CI IN RF • NADOLOL • SOTALOL • ATENOLOL,ACEBUTOLOL • BETAXOLOL,BISOPROLOL • CELIPROLOL • NOT SOLUBLE ABC
- 57. • 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)
- 58. All are non selective beta blockers except: a)Propranolol b)Timolol c)Sotalol d)Carvedilol Ans: d Carvedilol alpha +beta blocker
- 59. All are cardioselective beta blockers except: a)Atenolol b)Esmolol c)Bisoprolol d)Labetalol Ans:d NEW BETA BLOCKERS ACTING EXCLUSIVELY AT MYO CARDIUM
- 60. Combined alpha and beta blockers are: a)Labetalol b)Prazocin c)Tamsulosin d)Milrinone Ans:a
- 61. Contraindication of beta blockers are: a)Asthma b)Angina c)Hypertension d)Arrhythmia Ans: a
- 62. Beta blockers with ISA are: a)Propranolol b)Oxprenolol c)Esmolol d)Butoxamine Ans: b
- 63. Beta blocker with cardioselectivity,membrane stabilsing property and ISA: a)Carvedilol b)Atenolol c)Acebutolol d)Metoprolol Ans: c
- 64. Propranolol can be used in all except: a)Hyperthyroidism b)Prinzmetal angina c)Migraine d)Hypertension Ans: b
- 65. Beta blockers are CI in Diabetes as it : a)Causes hyperglycemia b)Causes seizure c)Masks symptoms of hypoglycemia d)Causes hypotension Ans: c
- 66. An ultra short acting beta blocker: a)Esmolol b)Timolol c)Atenolol d)Pindolol Ans: a
- 67. 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