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Chapter 19 Adrenoceptor agonists

Chapter 19 Adrenoceptor agonists. 1. ,  receptor agonists 2.  receptor agonists 3.  receptor agonists. Catechol. dopamine 多巴胺. norepinephrine 去甲肾上腺素. epinephrine 肾上腺素. Structure-activity relationship of catecholamines and related compounds

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Chapter 19 Adrenoceptor agonists

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  1. Chapter 19Adrenoceptor agonists • 1. ,  receptor agonists • 2.  receptor agonists • 3.  receptor agonists

  2. Catechol dopamine 多巴胺 norepinephrine 去甲肾上腺素 epinephrine 肾上腺素

  3. Structure-activity relationship of catecholamines and related compounds Substitution on the aromatic nucleus COMT, central activity Substitution on the -carbon atom MAO, uptake-1, NE release Substitution on the amino group sensitivity to the subunits of receptors

  4. Metabolism of catecholamines

  5. Overview of catecholamines

  6. Effect patterns of sympathomimetics

  7. Subtypes of adrenoceptors

  8. Effects of catecholamines（therapeutic doses）

  9. Effects of catacholamines and non-catecholamines

  10. epinephrine  antagonist epinephrine BP Epinephrine reversal （adrenaline reversal）

  11. 1. ,  receptor agonists Epinephrine 肾上腺素, Adrenaline

  12. 1. ,  receptor agonists • 1.1 Pharmacological effects • (1) Cardiac effects • 1: HR , output , • oxygen consumption , inducing arrhythmia • (2) Vascular effects • 1：vasoconstriction, especially at larger doses • 2：vasodilatation of skeletal muscles and coronary vessels

  13. 1. ,  receptor agonists • (3) Blood pressure • SP , DP  (at therapeutic doses) • (4) Bronchodilatation • 2：dilatation of bronchial smooth muscles • 1：reducing congestion and edema of bronchial mucosa • (5) Metabolic effects • blood glucose ; free fatty acids 

  14. 1. ,  receptor agonists • 1.2 Clinical uses • (1) Cardiac arrest • (2) Anaphylactic shock • (3) Acute bronchial asthma • (4) Local uses • adjuvant for local anesthetics; control of bleeding

  15. Systmatic uses: Cardiac arrest Anaphylactic shock Acute bronchial asthma Topical uses: Adjuvant of local anesthesia Bleeding Clinical uses of epinephrine

  16. 1. ,  receptor agonists • 1.3 Adverse effects • (1) Cardiac arrhythmia: BP , arrhythmia • (2) Excesive rise of BP: cerebral or subarachnoid hemorrhage • (3) Central excitation：anxiety • (4) Contraindications: heart diseases, hypertension, coronary arterial disease, arteriosclerosis, hyperthyroidism

  17. 1. ,  receptor agonists Ephedrine 麻黄碱 Ephedrine 麻黄碱 Epinephrine 肾上腺素

  18. 1. ,  receptor agonists • 1.1 Pharmacological effects • Promoting release of NE, weak agonist effectson 1、2、1、2 receptors • Properties： • chemically stable, orally effective； • less potent and longer action duration; • central stimulating； • tachyphylaxis.

  19. 1. ,  receptor agonists • 1.2 Clinical uses • (1) Prevention of hypotension: anesthetics • (2) Nasal decongestion: nasal drop • (3) Bronchial asthma: mild, chronic cases • (4) Relieving allergic disorders: urticaria, angioneurotic edema

  20. 1. ,  receptor agonists • 1.3 Adverse effects • (1) Central stimulation • (2) CVS effects • (3) Dependence

  21. 1. ,  receptor agonists Dopamine 多巴胺

  22. 1. ,  receptor agonists • 1.1 Pharmacological effects • (1) Cardiac effects：1 receptor, weak • (2) Vascular effects and blood pressure： • DA receptor：dilatation of renal and mesenteric arteries , blood flow (small doses); • 1 receptor：vasoconstriction of skin, mesenteric vessels (larger doses) • (3) Renal effects：renal vasodilatation; natriuretic effects

  23. Effects of dopamine on CVS Vasodilatation Vasoconstriction

  24. 1. ,  receptor agonists • 1.2 Clinical uses • (1) Shock • cardiac and septic shock: low output, urinary volume , fully adequate replacement of intravascular fluid • (2) Acute renal failure • combined with furosemide • 1.3 Adverse effects • tachycardia, arrhythmia, renal vasoconstriction

  25. 2.  receptor agonists • 2-1 1, 2 receptor agonists Norepinephrine 去甲肾上腺素, noradrenaline

  26. 2.  receptor agonists • 2.1 Pharmacological effects • (1) Vascular effects： • 1：vasoconstriction (skin, renal, brain, hepatic, mesenteric, etc.) • vasodilatation of coronary arteries • 2：inhibiting NE release

  27. 2.  receptor agonists • (2) Cardiac effects： • weak direct stimulation (1); • inhibition via reflex • (3) Blood pressure： • SP , DP (especially at larger doses), • larger doses:pulse pressure , blood flow 

  28. Actions of norepinephrine on post-synaptic (1) and pre-synaptic (2 ) receptors

  29. 2.  receptor agonists • 2.2 Clinical uses • (1) Shock • BP , blood flow , tissue damage • used in early phase of some types of shock or BP rise too slow after treatment: small doses and shorter duration

  30. 2.  receptor agonists • (2) Hypotension due to drug poisoning • especially for chlorpromazine • (3) Hemorrhage in upper alimentary tract • orally given after dilution

  31. 2.  receptor agonists • 2.3 Adverse effects • (1) Ischemia and necrosis at the site of iv administrationrelieved by filtration with procaine or phentolamine • (2) Acute renal failure avoiding larger doses and longer duration; monitoring urinary volume • (3) Contraindication hypertension, arteriosclerosis, heart diseases, severe urinary volume , microcirculation disorders

  32. 2.  receptor agonists Metaraminol 间羟胺, Aramine • Acting on  receptors directly, promoting NE release indirectly； • Weaker effects and longer duration than NE, • weak for renal vessels; • Used in early phase of shock, hypotension

  33. 2.  receptor agonists • 2-2 1 receptor agonists • used in hypotension, paroxysmal supraventricular tachycardia (by reflex)； • Mydriasis (phenylephrine): pupillary dilator muscles, no or less effect on intraocular pressure, short-acting (for several hours) Phenylephrine 去氧肾上腺素 Methoxamien 甲氧明

  34. 3.  receptor agonists • 3-1 1, 2 receptor agonists Isoproterenol 异丙肾上腺素, Isoprenaline

  35. 3.  receptor agonists • 3.1 Pharmacological effects • (1) Cardiac effects • 1 receptor stimulation • (2) Vascular effects and blood pressure • 2 receptor: dilatation of skeletal muscles and coronary vessels； • SP ，DP  or ，pulse pressure 

  36. 3.  receptor agonists • (3) Bronchodilatation • 2 receptor，no effect on edema of mucosa • (4) Metabolism • Promoting effects as epinephrine

  37. Effects of isoproterenol

  38. 3.  receptor agonists 3.2 Clinical uses • (1) Cardiac arrest • (2) A-V block • (3) Septic shock：low-output • (4) Bronchial asthma： • usually 2 receptor agonists

  39. 3.  receptor agonists 3.3 Adverse effects • (1) Heart stimulation, arrtythmia • (2) Contraindications: • coronary heart disease, myocarditis, hyperthyroidism

  40. 3.  receptor agonists • 3-2 1 receptor agonists • Heart failure • Cardiac stimulation Dobutamine 多巴酚丁胺

  41. 3.  receptor agonists • 3-3 2 receptor agonists • Bronchial asthma Salbutemol 沙丁胺醇

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