adrenergicantiadrenergicdrugsbymr-200330145102 (1).pptx

Adrengic Drugs

1. Adrenergic and Anti- adrengics Drugs

2. Human Nervous system Central Nervous System Peripheral Nervous System Autonomic Nervous System 3 / 3 / 2 020

3. With neurotransmitters norepinephrine and acetylcholine *Either “ fight and f li g h t ” m o d e o r “ r e st and diges t” Includes neurons and ganglia outside of the brain and spinal cord P eri p her a l Nervous System *Autonomic Nervous System (involuntary) Sympathetic Nervous System (adrenergic) P a r as y mpa th et i c Nervous System (cholinergic) Somatic Nervous System (voluntary) 3 / 3 / 2 020

4. Fight or flight response results in: Increased BP I n crea s ed b l o o d f lo w t o b ra i n , h eart a n d sk e l e t a l muscles Increased muscle glycogen for energy Increased rate of coagulation Pupil dilation 3 / 3 / 2 020

5. A lph a — A 1 a n d A 2 Beta—B1, B2, B3 Dopamine—subsets D1-5 3 / 3 / 2 020

6. Alpha 1—smooth muscle contraction Alpha 2-negative feedback causes norepinephrine to be released so BP is reduced Beta 1—increased heart rate Beta 2—bronchodilation Beta 3—actual site for lipolysis l e ss 3 / 3 / 2 020

7. Direct adrenergic drug action A f fec t s p o s t s y n a p ti c a l p h a 1 a n d b e t a rec e p t o rs on target effector organs E x a m pl e s : e pi n e ph r in e , phenylephrine I s u p re l , n o re p in e ph r in e , 3 / 3 / 2 020

8. 2. Indirect adrenergic drug action occurs by stimulation o f p o s ts y n a p t i c receptors.Cause a l p h a release 1 , b e t a 1 a n d of norepinephrine reuptake b e t a 2 i n t o the of s y n a p se o f n e r v e e n d i n g s o r p r e v e n t norepinephrine. Examples include cocaine and TCAs 3 / 3 / 2 020

9. 3 . m ix ed ac t i o n . C o m bin a t i o n o f di rect a n d i n d i re c t receptor stimulation Examples are ephedrine and pseudoephedrine 3 / 3 / 2 020

10. St i m ul a ti o n o f a l ph a 2 rece p to r s i n C N S i s us e f u l in decreasing BP Most body tissues have both alpha and beta receptors Effect occurs 2ndary to receptor activated and number of receptors in the particular body tissue 3 / 3 / 2 020

11. Some drugs act on both receptors--dopamine Some are selective--Isuprel 3 / 3 / 2 020

12. Emergency drugs in treatment of acute cardiovascular, respiratory and allergic disorders In c h i l d re n , e pi n e ph r in e m a y b e us e d to bronchospasm due to asthma or allergic reactions t reat Phenylephrine may be used to treat sinus congestion 3 / 3 / 2 020

13. St o k es A d a m s Shock Inhibition of uterine contractions For vasoconstrictive and hemostatic purposes 3 / 3 / 2 020

14. Cardiac dysrhythmias, angina pectoris Hypertension Hyperthyroidism Cerebrovascular disease Distal areas with a single blood supply such as fingers, toes, nose and ears Renal impairment use caution 3 / 3 / 2 020

15. Increased glucose, lactate, and fatty acids in the blood due to metabolic effects Increased leukocyte and increased coagulation Inhibition of insulin secretion 3 / 3 / 2 020

16. Affects both alpha and beta receptors Usual doses, beta adenergic effects on heart and vascular smooth muscle will predominate, high doses, alpha adrenergic effects will predominate Drug of choice for bronchospasm and laryngeal edema of anaphylaxis 3 / 3 / 2 020

17. E x ce ll e n t f o r ca r di ac s ti m ul a n t a n d v a s o c o n s t r i c t i v e effects in cardiac arrest Added to local anesthetic May be given IV, inhalation, topically Not PO 3 / 3 / 2 020

18. Physiologic antagonist to histamine Those on beta blockers may need larger doses D r u g o f c h oi ce i n P E A . V a s op re s s i n h as no w b ec o m e drug of choice in ventricular tachycardia Single dose of Vasopressin, 40 units IV 3 / 3 / 2 020

19. Ephedrine is a mixed acting adrenergic drug. Stimulates alpha and beta receptors. Longer lasting than epinephrine. See in Primatene mist 3 / 3 / 2 020

20. Used for bronchodilating and nasal decongestant effects 3 / 3 / 2 020

21. S y nth e t i c c a t ec ho l a m in e t h at a c t s o n b e t a 1 a n d 2 receptors S t i m ul a t es h ea r t , d il a t es b l o o d v e sse l s i n s k e l e t a l muscle and causes bronchodilation No alpha stimulation U s ed i n h ea r t b l o c k s ( w h e n p ace m a k er n o t a v a i l a b l e ) and as a bronchodilator 3 / 3 / 2 020

22. Pure alpha Decreases CO and renal perfusion No B1 or B2 effects Longer lasting than epinephrine Can cause a reflex bradycardia Useful as a mydriatic 3 / 3 / 2 020

23. Affects renal perfusion Can induce cardiac dysrhythmias Increases myocardial oxygen consumption May decrease perfusion of liver Tissue necrosis with extravasation 3 / 3 / 2 020

24. Do not give epinephrine and Isuprel at same time or within 4 hours of each other. Could result in serious dysrhythmias. 3 / 3 / 2 020

25. Sympatholytic Block or decrease the effects of sympathetic nerve stimulation, endogenous catecholamines and adrenergic drugs 3 / 3 / 2 020

26. Can occur by blocking alpha 1 receptors postsynaptically Or by stimulation presynaptic alpha 2 receptors. Results in return of norepineprhine to presynaptic site. Activates alpha 2 resulting in negative feedback. Decreases release of additional norepinephrine. 3 / 3 / 2 020

27. A lph a 2 a g o n i s t s in h i b i t r e l ea s e o f no re p in e ph r in e in brain; thus, decrease effects on entire body Results in decrease of BP A l so a f fe c t s p a n crea t i c i s l e t c e ll s , t h u s s o m e suppression of insulin secretion 3 / 3 / 2 020

28. Act on skin, mucosa, intestines, lungs and kidneys to prevent vasoconstriction Effects: dilation of arterioles and veins, decreased blood pressure, pupillary constriction, and increased motility of GI tract 3 / 3 / 2 020

29. May ac tiv a t e ref l e x es th a t o p p os e fa l l i n B P su c h as fluid retention and increased heart rate Can p r e v e n t a l ph a m e di ca t ed c o n t rac t i o n o f s m oot h muscle in nonvascular tissues T hus , us e f u l i n t r ea ti n g BP H as in hi b i t c o n t rac t i o n of muscles in prostate and bladder 3 / 3 / 2 020

30. Minipress (prazosin)—prototype. Hytrin (terazosin) and Cardura (doxazosin)—both are longer acting than Minipress. 3 / 3 / 2 020

31. Flomax (tamsulosin). Used in BPH. Produces smooth muscle relaxation of prostate gland and bladder neck. Minimal orthostatic hypotension. Priscoline (tolaxoline) used for vasospastic disorders. Pulmonary hypertension in newborns. Can be given sub Q, IM or IV. 3 / 3 / 2 020

32. Catapres (clonidine). PO or patch. Tenex (guanfacine) Aldomet (methyldopa). Can give IV. Caution in renal and hepatic impairment. 3 / 3 / 2 020

33. Prevent receptors from responding to sympathetic nerve impulses, catecholamines and beta adrenergic drugs. 3 / 3 / 2 020

34. Decreased heart rate Decreased force of contraction Decreased CO Slow cardiac conduction Decreased automaticity of ectopic pacemakers 3 / 3 / 2 020

35. Decreased renin secretion from kidneys Decreased BP Bronchoconstriction Less effective metabolism of glucose. May result in more pronounced hypoglycemia and early s/s of hypoglycemia may be blocker (tachycardia) 3 / 3 / 2 020

36. Decreased production of aqueous humor in eye May increase VLDL and decrease HDL Diminished portal pressure in clients with cirrhosis 3 / 3 / 2 020

37. Alpha 1 blocking agents are used for tx of hypertension, BPH, in vasospastic disorders, and in persistent pulmonary hypertension in the newborn May be useful in treating pheochromocytoma May be used in Raynaud’s or frostbite to enhance blood flow 3 / 3 / 2 020

38. U s ed f o r e x t ra v a s a t i o n o f p ot e n t v a s o c o n s t r i c to r s (dopamine, norepinephrine) into subcutaneous tissues. 3 / 3 / 2 020

39. Alpha 2 agonists are used for hypertension—Catapres Epidural route for severe pain in cancer Investigationally for anger management, alcohol withdrawal, postmenopausal hot flashes, ADHD, in opioid withdrawal and as adjunct in anesthesia 3 / 3 / 2 020

40. Mainly for cardiovascular disorders (angina, dysrhythmias, hypertension, MI and glaucoma) In angina, beta blockers decrease myocardial oxygen consumption by decreasing rate, BP and contractility. Slow conduction both in SA node and AV node . 3 / 3 / 2 020

41. Possibly work by inhibition of renin, decreasing cardiac output and by decreasing sympathetic stimulation May worsen condition of heart failure as are negative inotropes May reduce risk of “sudden death” 3 / 3 / 2 020

42. Decrease remodeling seen in heart failure In glaucoma, reduce intraocular pressur by binding to beta-adrenergic receptors in ciliary body, thus decrease formation of aqueous humor 3 / 3 / 2 020

43. Inderal (propranolol) is prototype U s ef u l i n t re a t m e n t o f h y p er t e n si on , angina pectoris, MI dysrhythmias, Useful in pheochromocytoma in conjunction with alpha blockers (counter catecholamine release) migraines 3 / 3 / 2 020

44. In cirrhosis, Inderal may decrease the incidence of bleeding esophageal varices Used to be contraindicated in heart failure, now are standard Known to reduce sudden death O f t en giv en w it h A C E Is Indications include: htn, angina, prevention of MI 3 / 3 / 2 020

45. H a v e c h e m i cal st r u c t u re s i m il ar t o th a t of catecholamines Block some beta receptors and stimulate others Cause less bradycardia A g e nt s i n c l ud e : Sectral (ac e bu t o l o l ) , Ca r t r o l (carteolol), Levatol (penbutolol) and Visken (pindolol) 3 / 3 / 2 020

46. In tx for BPH, patient should be evaluated for prostate cancer With alpha 2 agonists, sudden cessation can cause rebound BP elevation With alpha 1 blockers, first dose syncope may occurr from hypotension. Give low starting dose and at hs. May also cause reflex tachycardia and fluid retention . 3 / 3 / 2 020

47. W it h s i g ni f i ca n t b ra d y car di a , m a y n eed m ed w it h ISA such as pindolol and penbutolol Patient with asthma, cardioselectivity is preferred F or MI, s t art as s o o n as p a ti e n t i s h e m od y n a m i ca ll y stable 3 / 3 / 2 020

48. Should be discontinued gradually. Long term blockade results in increase receptor sensitivity to epinephrine and norepinephrine. Can result in severe hypertension. Taper 1-2 weeks. 3 / 3 / 2 020

49. THANK YOU….! 3 / 3 / 2 020