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Beta blockers
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- 3. SYMPATHETIC RECEPTORS β1 β2β3 BETA RECEPTORS
- 4. BETA 1 HEART BETA2 BRONCHUS GIT BLADDER UTERUS LIVER BLOOD VESSELS BETA 3 ADIPOSE TISSUE
- 5. BETA BLOCKERS Beta adrenergicreceptor antagonists act on Β1 or β2 receptors or on both
- 6. SIR JAMES BLACK DEVELOPED BETA BLOCKER PROPRANOLIN 1958 AWARDED NOBEL PRIZE FOR MEDICINE IN 1988
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- 12. NON SELECTIVE BLOCKERS •Blocks both β1 and β2 receptors • Eg:Propranolol
- 14. CARDIOVASCULAR USES BLOCK CARDIAC β1 RECEPTORS HEARTRATE MYOCARDIAL CONTRACTILITY CARDIAC OUTPUT BP
- 15. CARDIOVASCULAR USES • ESSENTIALHYPERTENSION • CONGESTIVE HEART FAILURE • ANGINA PECTORIS • CARDIAC ARRHYTHMIAS • MYOCARDIAL INFARCTION
- 16. ESSENTIAL HYPERTENSION • Aloneor in combination with diuretics • Rationale – Decrease in HR,CO ,myocardial contractility. – Decrease renin release Dose: 20-40mg TDS
- 17. Congestive heart failure Useful inmild 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 OXYGENDEMAND INCREASES EXERCISE TOLERANCE CI:PRINZMETAL’S ANGINASENSATION OF CHEST PAIN IMBALANCE BTW OXYGEN DEMAND AND SUPPLY
- 19. CARDIAC ARRHYTHMIAS • Usedin SVT associated with thyrotoxicosis, • Digitalis toxicity Mechanism: • Membrane stabilising effect IRREGULAR HEARTBEAT TACHYCARDIA PALPITATIONS
- 20. MYOCARDIAL INFARCTION Decrease incidence,recurrence,mortality PreventVF at the second attack of MI Dose: 40-80 mg tds orally
- 21. NON CARDIOVASCULAR USES • Migraine Anxietyprovoking 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 manifestationsof anxiety:tremors, sweating DOSE:10-20 MG TDS
- 24. GLAUCOMA Decrease intraocular pressure Propranolol notused Eg:Timolol topically
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- 26. PHEOCHROMOCYTOMA GIVEN IN COMBINATIONWITH α BLOCKER control tachycardia and arrythmia DOSE:20MG TDS FOR 3 DAYS BEFORE SURGERY
- 27. ALCOHOL WITHDRAWAL Reduces sympathetic overactivityduring 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
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- 30. BRADYCARDIA Can lower HRto 55 bpm BRADYARRHYTHMIA HEART BLOCK
- 31. COLD EXTREMITIES Loss ofβ2 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 SLEEPDISTURBANCES DEPRESSION NIGHTMARES
- 33. HEART FAILURE Cardiac patientsneed sympathetic drive to support heart to maintain proper cardiac output Beta blockers block this support Contraindicated in SEVERE HEART FAILURE
- 34. HYPOGLYCEMIA Beta blockers maskthe symptoms of hypoglycemia like tremors ,sweating and tachycardia CONTRAINDICATED IN PATIENTS ON INSULIN AND OHA
- 35. REBOUND HYPERTENSION CHRONIC THERAPYOF 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 TOTALTG LDL HDL
- 37. • TIMOLOL:USED INGLAUCOMA • SOTALOL: K CHANNEL BLOCKING AND ANTIARRHYTHMIC PROPERTY • NADOLOL:LONG HALF LIFE,LEAST FIRST PASS METABOLISM
- 38. CARDIOSELECTIVE BLOCKERS • BLOCKS β1RECEPTORS • 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: • Completelyabsorbed orally • BA less due to first pass metabolism Atenolol:Does not cross BBB Bisoprolol:Used in hypertension and angina
- 41. NEBIVOLOL New highly selectivebeta1 blocker Rapid onset action Less deleterious effect on lipids
- 42. • ESMOLOL: • Ultrashort 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 • Usedas eye drops in glaucoma • Less efficacious than Timolol • Safer in asthmatics and diabetics
- 44. NON SELECTIVE BLOCKERSWITH ISA PINDOLOL OXPRENOLOL ADVANTAGES: Lesser bradycardia and myocardial depression
- 45. SELECTIVE BLOCKERS WITHISA • ACEBUTOLOL • CELIPROLOL • Celiprolol: • Partial agonist at beta 2 receptors • Used in hypertensives with asthma
- 46. Mixed antagonists • LABETALOL •CARVEDILOL
- 47. LABETELOL • Blocks alpha1and beta receptors • Fall in BP due to alpha 1 and beta1 blockade • Uses: • Pheochromocytoma • Rebound hypertension after clonidne withdrawal
- 48. Carvedilol • Blocks alphaand 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
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- 52. ADVERSE EFFECTS ANDCI • 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 WITHISA • CELIPROLOL,OXPRENOLOL • PINDOLOL,PENBUTOLOL • ACEBUTOLOL • ALPRENOLOL CONTAIN PARTIAL AGONISTIC ACTIVITY
- 55. BETA BLOCKERS WITHMSA • PROPRANOLOL • METOPROLOL • LABETALOL • ACEBUTOLOL • PINDOLOL POSSESSES MEMBRANE STABILISING LOCAL ANAESTHETIC PROPERTY
- 56. LIPID INSOLUBLE BETABLOCKERS • EXCRETED BY KIDNEY • LONG DOA • CI IN RF • NADOLOL • SOTALOL • ATENOLOL,ACEBUTOLOL • BETAXOLOL,BISOPROLOL • CELIPROLOL • NOT SOLUBLE ABC
- 57. • Longest actingbeta 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 nonselective beta blockers except: a)Propranolol b)Timolol c)Sotalol d)Carvedilol Ans: d Carvedilol alpha +beta blocker
- 59. All are cardioselectivebeta blockers except: a)Atenolol b)Esmolol c)Bisoprolol d)Labetalol Ans:d NEW BETA BLOCKERS ACTING EXCLUSIVELY AT MYO CARDIUM
- 60. Combined alpha andbeta blockers are: a)Labetalol b)Prazocin c)Tamsulosin d)Milrinone Ans:a
- 61. Contraindication of betablockers are: a)Asthma b)Angina c)Hypertension d)Arrhythmia Ans: a
- 62. Beta blockers withISA are: a)Propranolol b)Oxprenolol c)Esmolol d)Butoxamine Ans: b
- 63. Beta blocker withcardioselectivity,membrane stabilsing property and ISA: a)Carvedilol b)Atenolol c)Acebutolol d)Metoprolol Ans: c
- 64. Propranolol can beused in all except: a)Hyperthyroidism b)Prinzmetal angina c)Migraine d)Hypertension Ans: b
- 65. Beta blockers areCI in Diabetes as it : a)Causes hyperglycemia b)Causes seizure c)Masks symptoms of hypoglycemia d)Causes hypotension Ans: c
- 66. An ultra shortacting beta blocker: a)Esmolol b)Timolol c)Atenolol d)Pindolol Ans: a
- 67. Adverse effects ofbeta blockers include: a)Compensated heart failure b)Masking the features of hypoglycemia c)Bronchial asthma d)All the above Ans: d