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Adrenomimetic drugs adrenoceptor agonists

Adrenomimetic drugs adrenoceptor agonists. Department of pharmacology Zhu ling ( 朱玲 ) 2010.3. Adrenomimetic drugs adrenoceptor agonists.

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Adrenomimetic drugs adrenoceptor agonists

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  1. Adrenomimetic drugs adrenoceptor agonists Department of pharmacology Zhu ling (朱玲) 2010.3

  2. Adrenomimetic drugs adrenoceptor agonists • A kind of drugs that mimic the actions and the chemistry structure (amine) of epinephrine or norepinephrine. • Because the action similar to sympathetic effects that stimulation are mediated by release of norepinephrine sympathomimetic drugs

  3. Adrenomimetic drugsadrenoceptor agonists

  4. αreceptor: blood vessels of skin, gut contracts β1receptor:heart function enhancement β2receptor: bronchial smooth muscles: relaxation skeletal muscle vessels: relaxation coronary artery: relaxation

  5. Adrenomimetic drugsadrenoceptor agonists Commonness 1 Basic structure :β--phenylethylamine 2 main effects in the cadiovascular systerm 3 elimination from uptake, MAO, COMT 4 main application: shock

  6. Noradrenaline synthesize and elimination

  7. Adrenomimetic drugsadrenoceptor agonists • individuality 1 structure: different substituted groups 2 different of receptor selectivity 3 different effects mostly on the systolic and diastolic blood pressure (pulse pressure)

  8. αβreceptor agonist Adrenaline Ad 肾上腺素 Epinephrine E • Rooted in adrenal gland medulla,instability • Pharmacokinetics: absorption : is poor with oral administration , sc or i.m injection . distrbution: the area of noradrenergic nerve domination; elimilation: uptake,or inactivation by MAO, COMT

  9. αβreceptor agonist --adrenaline Effects a very potentαβreceptor agitated action 1 heart : β1receptor excitement 2 blood vessels: α1 and β2 receptor skin vessels, mucous membrane vessels, viscus vessels contraction; brain, pulmonary blood vessels feeble vasoconstriction; skeletal muscle vessels ,coronary artery dilation

  10. αβreceptor agonist --adrenaline β2 receptor agitate blood pressure coronary artery perfusion pressure flux adenosine increase • 3 blood pressure systolic blood pressure increase, diastolic pressure steadiness or slightly fall pulse pressure

  11. αβreceptor agonist --adrenaline 4 bronchia smooth muscle relaxation 5 metabolism: activates fat lipolysis, blood glucose↑ 6 CNS application 1 anaphylactic shock first choose drug 2 bronchial asthma( urgent outbreak) 3 sudden cardiac arrest 4 local application local anesthetics and rhinorrhagia

  12. αβreceptor agonist --adrenaline Adverse reaction heart-throb, headache, arrhythmia (extensions of their receptor effects in the cardiovascular ) Contraindication hypertension , hyperthyroid etc

  13. αβreceptor agonist --ephedrine pharmacokinetics: substitution on benzene ring(Absence of ring-OH groups) and substitution on alpha carbon preferably lipid-soluble, stabilization, orally active, increase the distribution, prolong the action(resistant to COMT,MAO) effects: Agitate, accelerate NA release 1 peripheral effects like Ad but the function is slow, feeble, long duration 2 CNS effects elevation of mood

  14. Methyl-benzedrine甲基苯丙胺(冰毒)

  15. αβreceptor agonist --ephedrine application : • bronchial asthma • congestive snuffle (as a nasal decongestant ) • Prevent some hypotension (as a pressor agent) arachnoid below cavity and outside putamen anesthesia, local anesthetics poisoning • Some disease induced by allergic reaction Adverse reaction: like Ad, further insomnia (CNS effects)

  16. αreceptor agonist --noradrenaline Pharmacokinetics chemical quality like Ad, orally taking easily be destroyed, maybe ischemia or putrescence with sc or im , only can be applied by iv

  17. αreceptor agonist --noradrenaline Effect mostly agitateαβ1 receptor 1 heart positive klinotropic effect, positive chronotropic effect positive inotropic effects 2 blood vessel vasoconstriction except coronary artery peripheral resistance 3 blood pressure both diastolic and systolic blood pressure

  18. αreceptor agonist --noradrenaline Clinical uses: ① shock and hypotension ② hemorrhage of the upper alimentary tract oral administration (local application) Adverse reaction: marked vasoconstriction , arrhythmia ① local tissues necrosis ② acute kidney failure

  19. αreceptor agonist • metaraminal direct and indirect action weak, long-duration substitute of NA • Phenylephrine and methoxamine kidney blood vessels contract >NA treatmemt of paroxysmal atrial tachycardia and effictive mydriatic agent (Phenylephrine)

  20. βreceptor agonist Isoproterenol (Isoprenaline 异丙肾上腺素) • Isoproterenol (Isoprenaline) 1 pharmacokinetics: absorption: low bioavailability of oral administration,usually iv, sublingua administration, aerosol inhalation (through capillary vessel , rapid absorption ) biotransformation: main metabolized by COMT,some by MAO,some by uptake

  21. βreceptor agonist Isoproterenol (Isoprenaline 异丙肾上腺素) effects:more active βreceptor agonist ① heart exciting ② blood vessels potent vasodilator ③ blood pressure systolic pressure slightly increased, diastolic pressure decreased • bronchia smooth muscle: relaxation • metabolism glycogenolysis and lipolysis ↑ increased oxygen consumption

  22. βreceptor agonist Isoproterenol (Isoprenaline 异丙肾上腺素) Therapeutic application: ① Sudden cardiac arrest: (cause: ventricular automaticity slowness, severity atrioventricular block and SA nodes function failure) ② atrioventricular block ③ bronchial asthma acute outbreak ④ Infected shock Adverse reaction: heart-throb, arrhythmia etc

  23. β1 receptor agonist Dobutamine 多巴酚丁胺 • effects: relatively β1 selective synthetic catecholamine, positive inotropic effects characteristic: in low to moderate doses, it can increase, constriction and cardiac output , but slightly influence on the heart rate, cause relatively little peripheral vasoconstriction and little increase oxygen consumption

  24. β1 receptor agonist Therapeutic application: 1 shock well curative effect when companying with weak contract or renal failure 2 congestive heart failure 3 acute renal failure always with diuretic Adverse reaction: tachycardia, hypertension, angina, inducing tolerance

  25. αβDA receptor agonist – Dopamine多巴胺 Dopamine( DA 多巴胺) • the immediate metabolic precursor of norepinephrine • Exist in peripheral nerve, ganglion and central nerve pharmacokinetics: absorption: low bioavailability of oral administration,usually iv distribution: difficult pass through blood-brain barrier

  26. αβDA receptor agonist – Dopamine多巴胺 effect:agitate αβDA receptor 1 heart β1 R 2 blood vessel and blood pressure • low doses activate D1 receptor in several vascular beds vasodilation, reduce peripheral resistance • moderate doses β1R systolic pressure↑ diastolic pressure -unchanged • higher doses α β1R systolic pressure ↑ diastolic pressure ↑ 3 kidney renal vascular dilation blood flow↑ (raise glomerulus filtration rate) (clinical value)

  27. αβDA receptor agonist – Dopamine多巴胺 Therapeutic application: 1 shock especially oliguria 2 congestive heart failure 3 acute renal failure (with diuretic) Ibopamine (异波帕胺) heart failure (difficult controlling)

  28. Sympathomimetic drugs

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