神经系统药理2胆碱能神经系统知识介绍.ppt

Norepinephrine, Noradrenaline (去甲肾上腺素): DIRECT Pharmacological effect ?1, ?2 receptor agonists (1) Vascular effects： ?1：vasoconstriction (skin, renal, brain, hepatic, mesenteric, etc.), blood flow ? ?2：inhibiting NE release Actions of norepinephrine on post-synaptic (?1) and pre-synaptic (?2 ) receptors (2) Blood pressure： Systolic BP ?, Diastolic BP ?(especially at larger doses) (3) Cardiac effects： Weak direct stimulation (?1); inhibition via reflex (in vivo) Net result: little cardiac stimulates Coronary artery dilation Norepinephrine, Noradrenaline Effects of catecholamines（therapeutic doses） Predominant Effects: NE : ? ?1 effects EPI : ?1, ? 2 then at higher concentrations ? effects predominate ISO: ?1 and ? 2 Clinical uses (limited therapeutic value) (1) Shock used in early phase of some types of shock: small doses and shorter duration (dopamine is better; replaced by Metaraminol间羟胺) (2) Hypotension due to drug poisoning especially for chlorpromazine (氯丙嗪) (3) Hemorrhage in upper alimentary tract orally given after dilution Norepinephrine, Noradrenaline Adverse effects (1) Ischemia and necrosis at the site of iv administration relieved by filtrating the area with phentolamine (? receptor antagonist) (2) Acute renal failure avoiding larger doses and longer duration; monitoring urinary volume (3) Contraindication hypertension, arteriosclerosis, heart diseases, severe urinary volume ?, microcirculation disorders Norepinephrine, Noradrenaline Acting on ? receptors directly, promoting NE release indirectly； Weaker effects and longer duration than NE, Weak effects on renal vessels; Used in early phase of shock, hypotension Metaraminol 间羟胺 Induces reflex bradycardia, used in hypotension, paroxysmal supraventricular tachycardia ； Activate ? receptor at normal dose Block ? receptor at high dose Phenylephrine: Mydriasis, pupillary dilator muscles, no or less effect on intraocular pressure, short