ADRENERGIC RECEPTORS Dr. S. Parthasarathy MD., DA., DNB, MD (Acu), Dip. Diab.DCA, Dip. Software statistics- Ph d Mahatma Gandhi Medical college and research institute , puducherry , India AHLQUIST – 1948 PROGRESS ADRENERGIC RECEPTORS WHAT IS THIS ?? Two transmitters Adrenaline Acetyl choline Its noradrenaline CLASSIFICATION α α1 α2 β β1 β2 β3 MOST OF THE DRUGS ACT ON SOME OTHER RECEPTORS ALSO Dopamine DA 1 DA 2 ALPHA RECEPTORS ALPHA RECEPTORS Vasoconstriction Metabolism Conscious status Nociception ALPHA RECEPTORS α1 Smooth vessels of blood vessels Vasoconstriction Liver – glycogenolysis Intestine – contraction ALPHA 1 AGONISTS – MINOR mydriasis (pupillary dilation due to contraction of the radial eye muscles), broncho constriction, uterine contracture, contraction of sphincters in the gastrointestinal and genitourinary tracts. α 1-Stimulation also inhibits insulin secretion and lipolysis. α 1-receptors that have slightly positive inotropic and negative chronotropic effects ALPHA 2 Platelet aggregation Sympathetic nerve endings Decrease norad release Pancreatic beta cell Decrease insulin release BETA BETA 1 Heart – force , rate, excitability increased Renal JG apparatus - ↑ rennin release BETA 2 Smooth muscle of bronchi, blood vessel, uterus bladder- vasodilation and relaxation Heart – force, rate increased Skeletal muscle – hypokalemia Beta cell pancreas- ↑ insulin BETA 3 Fat – thermogenesis Subcutaneous tissue Lipolysis DOPAMINE Dopamine-1: vascular smooth muscle (renal, mesentery, coronary causing vasodilation),renal tubules (natriuresis, diuresis), juxtaglomerular cells (increased renin release). Dopamine-2: postganglionic sympathetic nerves (inhibits NE release), smooth muscle constriction). (renal, mesenteric causing possible ALPHA RECEPTORS Noradrenaline > adrenaline > > isoprenaline beta receptors Isoprenaline > adrenaline > noradrenaline PHARMACOLOGICAL DYNAMISM After stoppage of beta blockers , there is sudden increase of beta receptors ADRENERGIC AGONISTS Dopamine Phenyleph Dopamine Clonidine Dobutamine Isoprenaline Oxymetazoline Noradrenaline Terbutalin norad Adrenaline Alpha Alpha 1 Ephedrine Beta Alpha 2 Beta 1 Beta 2 Ephedrine Beta 3 DIFFERENCES Adrenaline , noradrenaline and dopamine – Natural catecholamines Direct acting and indirect acting SUMMARY Alpha 1 Alpha 2 Beta 1 Beta 2 ANAPHYLAXIS alpha-adrenergic receptors, _____lessens the vasodilation and increased vascular permeability. action on beta- receptors, ________causes bronchial smooth muscle relaxation that helps alleviate bronchospasm, wheezing, and dyspnoea Adrenaline WHY WE SHOULD USE ADRENALINE Additives CPR EPHEDRINE Direct B1 and B 2 and indirect alpha 1 May cause tachycardia and hypertension Ideal for spinal epidural hypotension especially in pregnant patients- should not cross placenta CARDIOGENIC SHOCK. Dobutamine Acts on b1 and b2, with minimal action on a1 receptors. It increases cardiac output and reduces afterload (b2effects on skeletal muscle). SEPTIC SHOCK Vasodilation is predominant pathology Inotrope with minimal beta 2 action Use noradrenaline Sys, dias, MAP increase without CO increase No chronotropic effects ISOPRENALINE Complete heart block, overdose of beta blocker or severe bradycardia unresponsive to atropine Acts on b1 and b2 receptors Isoprenaline CARDIOGENIC SHOCK WITH OLIGURIA Beta 1, alpha 1 and DA 1 and DA 2 Dopamine 2 µg / kg 5 µg / kg 10 µg / kg DOBUTAMINE Alpha and beta Inotropy with minimal vasodilation at low doses But alpha vasoconstriction predominates in higher doses Increases myocardial oxygen consumption – stress testing Use in patients where myocardial O2 consumption ?? Sudden hypotension and aortic stenosis obstructive hypertrophic cardiomyopathy, Phenylephrine Nitrates and viagra induced BP fall ACUTE MI Dopamine and dobutamine individual or combination Vasopressin RV infarct – IV fluids and dobutamine POST CARDIAC SURGERY STATUS Correction of the cause with dobutamine Adrenaline Isoprenaline where we need the highest kick and not bother about tachycardia BRONCHIAL ASTHMA We want only beta 2 agonists Terbutaline and others CLONIDINE Adrenergic receptor agonist But hypotension Analgesia Sedation Alpha 2 agonist RITODRINE , ISOXSUPRINE Preterm labour Beta 2 agonist Not much tachycardia not much hypotension ADRENERGIC AGONISTS Dopamine Phenyleph Dopamine Clonidine Dobutamine Isoprenaline Oxymetazoline Noradrenaline Terbutalin norad Adrenaline Alpha Alpha 1 Ephedrine Beta Alpha 2 Beta 1 Beta 2 Ephedrine Beta 3 BLOCKERS Beta Alpha Alpha 1 Alpha 2 labetolol Tamsulo sin Beta 2 labetolol Phent, phenoxy Prazosin Beta 1 Yohimbine propranolol Aten Butoxami Beta 3 THANK YOU