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b-blockers.pptx
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- 3. BETA BLOCKERS ⯈Drugs whichinhibit adrenergic response mediated by beta receptors
- 4. BETA RECEPTORS Receptors Sites β1Heart JG cells-kidney Posterior pituitary Adipose tissue β2 Bronchi Blood vessels of skeletal muscle Smooth muscle (Uterus ,intestine , detrusor) Liver, Muscle Adipose tissue Eye actions stimulatory Renin release ADH release lipolysis Bronchodilation Vasodilatation Relaxation Glycogenolysis Lipolysis Enhanced aqueous secretion β3 Adipose tissue Lipolysis
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- 6. MECHANISM OF ACTION ⯈ViaGPCR Antagonist binding to receptor No stimulation of G protein No change in cAMP conc No EFFECT
- 7. PROPERTIES Receptor Blockade Nonselective βblockade Selective β1 blockade Β+α blockade Intrinsic sympathomimetic property- ISA (partial agonistic action) Membrane stabilising action-MSA (Local anaesthetic action-Na channel block)
- 8. Classification on thebasis of receptors selectivity Non selective (β1 and β2 blockers) Without intrinsic sympathomimetic activity Propanolol Timolol Sotalol With intrinsic sympathomimetic activity Celiprolol Oxprenolol Pindolol Alprenolol
- 9. Selective β1 blockers(Cardioselective) Bisoprolol Betaxalol Atenolol Esmolol Acebutalol Metoprolol
- 10. Selective β2 blocker Butoxamine Mixedα and β blockers Labetalol Carvedilol Nebivolol
- 11. CLASSIFICATION Beta blockers 1st generation Classical Non selective 2nd generation Classical Beta 1 selective 3rdgeneration Newer Non selective & beta1 selective + Add. properties
- 12. 1ST GENERATION –NON SELECTIVE Propanolol Pindolol Nadolol Tilmolol
- 13. 2ND GENERATION –SELECTIVE Β1 AGENTS Acebutalol Atenolol Betaxolol Bisoprolol Celiprolol Metoprolol
- 14. 3rd GENERATION BETABLOCKERS (VASODILATORPROPERTY) 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
- 15. Β BLOCKERS With ISA Penbutolol Carteolol Celiprolol Both Pindolol Acebutolol Labetalol WithMSA Propranolol Metoprolol
- 16. PROPERTIES OF Β1SELECTIVITY (Advantages of cardioselective beta blockers) •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
- 17. PROPERTIES OF ISA •Lessbradycardia •Less rebound effect on withdrawal • Less deleterious effect on blood lipid profile •Not effective in migraine prophylaxis • Not suitable for secondary prophylaxis of MI
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- 19. 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
- 20. ACTIONS…. •CVS •Antihypertensive action •Decreased CO •Decreased TPR on long term administration •Decreased renin release •Blockade of presynaptic beta 1 receptor result in decreased peripheral and central sympathetic outflow.
- 21. ACTIONS -CNS •Anti anxiety •Behaviourchanges •Forgetfulness •Night mares •Increased dreaming Non-selective lipid soluble
- 22. ACTIONS -METABOLIC •CHO metabolism •Hypoglycemia •Inhibitsmuscle 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 Lesswith beta 1 selective agents
- 25. SKELETAL MUSCLES o Decreaseexercise capacity By decreasing blood flow Inhibit glycogenolysis and lipolysis.
- 26. MISCELLANEOUS o Antagonise catecholamine induced •Tremor oPrevent platelet aggregation and promote fibrinolysis
- 27. ADVERSE EFFECTS -CVS •Bradycardia • Exacerbation of variant angina •Precipitation of CHF
- 28. ADVERSE EFFECTS… • Increasedair way resistance worsening of bronchial asthma
- 29. ADVERSE REACTIONS •Impairment ofcarbohydrate tolerance •Alteration of lipid profile •Rebound hypertension on withdrawal •Cold hands and feet, worsening of PVD
- 30. ADVERSE EFFECTS… Nightmares Decreased exercisecapacity Tiredness Lack of drive
- 31. USES CARDIOVASCULAR •Hypertension •Angina •Myocardial infarction •Arrhythmia •Cardiomyopathy •CCF •Dissecting aneurysmof aorta NON - CARDIOVASCULAR •Thyrotoxicosis •Pheochromocytoma •Migraine prophylaxis •Essential tremor •Glaucoma •Anxiety •Portal hypertension •Anti psychotic induced akathesia
- 32. HYPERTENSION •Cardioselective beta blockers •Rationale •Decrease in HR,CO, myocardial contractility. •Decrease renin release • Decrease central sympathetic out flow
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- 34. ANGINA - RATIONALE DecreaseHR & contractility Decrease myocardial oxygen demand Antianginal action
- 35. MI o Prophylaxis o Treatment Anti anginal action Reduce infarct size Prevents arrhythmia Prevents reinfarction Prevents arrhythmia Metoprolol Esmolol Timolol
- 36. ARRYTHMIAS •Propranolol •Esmolol •Acebutolol •Sotalol Decreases AV conduction Inhibitsimpulses from atria to ventricle controls ventricular rate Mainly effective in Arrhythmias precipitated by catecholamines Sotalol K+ channel opener class3 anti arrhythmic Esmolol ultra short acting supraventricular tachycardia
- 37. ARRHYTHMIA • Control ventricularrate in atrial flutter and fibrillation. • Suppress extrasystole and tachycardia especially mediated adrenergically .
- 38. HOCM •↓ contractility •↓ LVoutflow obstruction • Improve cardiac output in exercise
- 39. CHF ONLY in compensatedCHF • Antagonise sympathetic overactivity on myocardium •Prevents myocyte apoptosis •↓ cardiac remodelling Retard progression of CHF Metoprolol Bisoprolol Carvedilol
- 40. DISSECTING AORTIC ANEURYSM ↓cardiac contractility, and aortic pulsation.
- 41. NON - CARDIACUSES 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
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- 43. PORTAL HYPERTENSION • ToDecrease Portal Vein Pressure in Patients with Cirrhosis •Decrease variceal bleeding Propranolol Nadolol
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- 45. CNS •Anxiety •Essential tremor • Akathisiainduced by antipsychotics •Alcohol withdrawal
- 46. CONTRAINDICATIONS Absolute 1. Severe Bradycardia 2.Heart Block 3. Overt Untreated Heart Failure 4. Cardiogenic Shock 5. Severe Bronchospasm 6. Severe Depression 7. Active Raynaud’s Phenomenon
- 47. CONTRAINDICATIONS Relative 1. Prinzmetals Angina 2.Concomitant Use Of :Verapamil/ Diltiazam/Digoxin 3. Mild Asthma 4. Insulin Requiring DM
- 48. OVERDOSAGE Manifestations extensionof pharmacological properties Hypotension Bradycardia Prolonged Conduction Times Widened QRS Complexes
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- 50. TREATMENT •Atropine Initially •Cardiac PacemakersRequired •Large amt of Isoproterenol / Agonist •Glucagon