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1、Chapter9 Adrenoceptoragonists 肾上腺素受体激动药 1 Introduction basic chemical structure 苯乙胺 catecholamines CA类 儿茶酚胺类 adrenaline 肾上腺素 noradrenaline 去甲肾上腺素 isoprenaline 异丙肾上腺素 dopamine 多巴胺 非CA类 ephedrine 麻黄碱 metaraminol 间羟胺 Classification 一 according to the structure mainly R noradrenaline 去甲肾上腺素 mainly R iso
2、prenaline 异丙肾上腺素 R adrenaline 肾上腺素 二 according to the receptor 2 R agonists noradrenaline NA norepinephrine NE 去甲肾上腺素 1 chemical characteristic is unstable ineffective when given orally should be given intravenous infusion 2 the effect is quick strong and short metabolism mainly in the liver COMT MA
3、O characteristics R 1 R cannot stimulate 2 R mechanism Pharmacological effect 1 Blood vessel 1 R constrict the vessel of the skin mucous membrane viscus increase the peripheral resistance 外阻 1 R heart dilation 扩张 of coronary blood vessels 2 Heart 1 R Force HR conduction cardiac output CO In intact 整
4、体 animal or human being NA 1 R peripheral resistance HR NA 1 R peripheral resistance CO is unchangeable or degressive 下降 窦弓反射 3 blood pressure BP heart CO systolic blood pressure SBP收缩压 constriction of blood vessel peripheral resistance diastolic blood pressure DBP舒张压 low dosage 血管收缩不剧烈 外阻略 DBP略 inc
5、rease the pulse pressure 脉压 larger dosage 血管剧烈收缩 外阻 DBP decrease the pulse pressure 脉压 1 Early phase of shock 休克早期 2 Hypotension 低血压 induced by drug toxication 3 Upper gastrointestinal tract bleeding PO 粘膜血管收缩 止血 clinical use 2 acute renal failure too long and too large dose 用药间尿量应 25ml h 1 local ne
6、crosis 坏死 静滴过久 药浓过高 外漏 Side effects Contraindications 高血压 动脉硬化症 器质性心脏病 少尿 无尿 严重微 循环障碍病人 防治 1 局部热敷 2 普鲁卡因局部浸润注射 3 R阻断剂 酚妥拉明 1 R effect is similar to NA but weak and long 2 stimulates the release of NA can cause tachyphylaxis 快速耐受性 3 升压作用久 可靠 不易引起肾衰 Metaraminol 间羟胺 Aramine阿拉明 Clinical Use 各种休克早期 术后或脊椎
7、麻醉后休克 NA代用品 缩血管药中首选 characteristics Phenylephrine 去氧肾上腺素又名 新福林 苯肾上腺素 1 1 R 反射性HR下降 paroxysmal supraventricular tachycardia 阵发性室 上性心动过速 constrict smooth muscle of vessel antishock 2 1 R 瞳孔开大肌 扩瞳 无调节麻痹 作用快 短 检查眼底 3 R agonists 1 heart 1 R force HR conduction overdose 心肌兴奋性提高 心肌耗氧 arrhythmia 可致室颤 adrena
8、line Adr epinephrine 肾上腺素 mechanism 1 2 R Pharmachological action blood vessel 2 R dilate the blood vessel of skeletal muscle and coronary artery R constrict the blood vessel of skin mucous membrane and viscus 2 blood vessel and Bp Blood pressure Therapeutic dose R 皮肤 粘膜 内脏血管收缩 Adr 1 R heart CO SBP
9、2 R 骨骼肌血管 舒张 1 R heart CO SBP R 皮肤 粘膜 内脏血管收缩 Large dose SBP DBP R 皮肤 粘膜 内脏血管收缩 1 R heart CO SBP 占优势 占优势 DBP不变 或略 SBP 2 R 骨骼肌血管 舒张 2 R 骨骼肌血管 舒张 给较大剂量Adr 随时间推移 血 压发生什么变化 Adr R 2 R 3 smooth muscle bronchia 2 R dilate the SM R 支气管粘膜血管收缩 消除粘膜水肿 GI relaxation bladder relaxation dysuria排尿困难 retention of ur
10、ine尿潴留 4 metabolism 血糖 脂肪分解 可能与 1 2 R 有关 1 Cardiac arrest 心跳骤停 induced by drowning 溺死 toxication of CNS inhibitors anesthesia and acute infectious disease Clinical Use ABC approach A airway B breath C circulation Adr R 血管收缩 毛细血管通透性 R 改善心功 扩张冠脉 缓解支气管痉挛 减少过敏介质释放 消除支气管粘膜水肿 2 Allergic shock 过敏性休克 3 Bron
11、chial asthma 皮下 或肌肉注射 用于急性发作 4 Local usage adrenaline procaine普鲁卡因 局麻药中加Adr 收缩血管 延缓局麻药吸收 降低毒性 局麻药麻醉时间 心悸 烦躁 头痛 BP 心律失常 重者室颤 心肌缺血等 Side reaction 高血压 脑动脉硬化 器质心脏病 糖尿病 甲亢 contraindication dopamine DA 多巴胺 mechanism DA R 1 PO destroyed easily 2 metabolized by MAO and COMT easily 维时短 3 cannot pass BBB 外源性D
12、A无中枢作用 pharmacokinetics 1 Cardiovascular system low concentration 肾 肠系膜血管 DA R 血管舒张 high concentration R 心脏 对 R作用弱 舒张压无明显影响 Higher concentration R 血管收缩 BP 2 kidney DA R 肾血管扩张 肾血流 注意 低浓度时出现 pharmacological action 1 various shock cardiogenic and septicemic 败血病的 shock hemorrhagic 出血 shock especially wi
13、th cardiac dysfunction oliguria 尿少 or anuria 无尿 2 Acute renal failure particularly in patients with oliguria 3 acute heart failure Clinical Use Ephedrine 麻黄碱 1 action is similar to Adr R but slow weak long po 2 also has indirect effect 可促递质释放 tachyphylaxis 快速耐受性 3 CNS characteristics Clinical Uses 1
14、 Prevention of the asthma 哮喘 and treatment of the moderate asthma 2 Nasal decongestion 减轻鼻充血 3 Prevention and treatment of some hypotension 低血压 such as hypotention by spinal anesthesia 腰 麻 4 treatment of urticaria 荨麻疹 angioneurotic edema 血管神经性水肿 4 R agonists 1 heart 1 R force HR conduction 特点 1 作用强于
15、肾上腺素 2 也可引起心律失常 较少产生室颤 Isoprenaline 异丙肾上腺素 mechanism 1 2 R Pharmachological action 3 bronchial SM 2 R 平滑肌舒张 特点 1 作用略强于Adr 2 也可抑制过敏介质释放 3 久用可产生耐受性 2 blood vessel and blood pressure 2 R dilatation of blood vessel BP SBP DBP 略 4 others 不透BBB 中枢作用弱 R 心脏 组织耗氧 1 Bronchial asthma for controlling the attack
16、 2 A V conduction blockade II III 3 Hear arrest 适用于心脏自身原因引起的骤停 4 Septicemic 败血症的 shock suitable for high central vein pressure 中心静脉压 and lower cardiac output 低排高阻型 Clinical Uses 心悸 头晕 心律失常 adverse action 冠心病 心肌炎 甲亢等 contraindication 1 Stimulate 1 receptor selectively positive inotropic 变力的 effect HR 不明显 心肌耗氧增加不明显 2 clinical uses cardiogenic shock and congestive 充血 heart failure Dobutamine 多巴酚丁胺
