肾上腺能受体激动剂——山东大学药理学英文课件.ppt

Mephentermine(美芬丁胺,wyamine,恢压敏) Similar to ephedrine (direct, indirect) central excitation Used to prevent hypotension state Used to treat nasal congestion section 3 α-R agonists α-R agonists α1、α2-R agonists α1-R agonists α2-R agonists  ?1, ?2 Agonists noradrenaline(去甲肾上腺素，norepinephrine，NA，NE) [source and chemistry] NA pharmacokinetics pharmacological actions strongly activate α1, α2 -R slightly activate β1-R. pharmacological actions 1.vessels: contraction(α-R) coronary vessels :dilation (similar to AD) presynaptic adrenergic terminals (α2-R):NE ↓ negative feedback 2.heart: excitation(β1-R) 3.BP: small dose: SBP↑ DBP→ large dose: SBP↑ DBP↑ 4.others: weaker than AD clinical uses 1.shock：early 2.hypotension caused by drugs’ intoxication 3.upper digestive tract hemorrhage adverse reactions 1.local ischemia and necrosis 2.acute renal failure metaraminol (间羟胺, aramine, 阿拉明) [Mechanisms]1.direct actions 2.indirect actions [Characteristics] 1. weaker and longer than NA 2.little adverse reactions: renal failure, arrhythmias 3.tachyphylaxis [Uses] substitute for NA in treatment of shock ?1-R Agonists Phenylephrine(去氧肾上腺素) Methoxamine(甲氧明) Phenylephrine and methoxamine 1.selective α1-R agonists: shock, hypotension 2. renal vasoconstriction: significant 3. paroxysmal supraventricular tachycardia 4.phenylephrine→mydriasis(rapid, weak, short) ?2-R Agonists Peripheral ?2-R Agonists: oxymetazoline(羟甲唑啉)： nasal congestion apraclonidine(阿可乐定): Glaucoma Central ?2-R Agonists：HBP clonidine(可乐定)， methyldopa （甲基多巴） Section4 β-R agonists β1、 β2-R agonist β1-R agonists β2-R agonists β1、 β2-R agonist Isoprenaline (Isop,异丙肾上腺素) pharmacological actions: strongly activate β1、 β2-R pharmacological actions 1.heart: excitation (β1-R) positive inotropic effect positive chronotropic effect positive dromotropic effect pharmacological actions 2.vessels: Skeleta