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1、1,Chapter 11,肾上腺素受体阻断药,Adrenoceptor blocking drugs,2,Teaching goals,1、简述酚妥拉明的作用、用途、不良反应。2、简述普萘洛尔的作用、用途、禁忌症。3、解释：内在拟交感活性。,3,【Classification】,Adrenoceptor blocking drugs,According to the selectivity to the receptors,1)-adrenoceptor blocking drugs,2)-adrenoceptor blocking drugs,3)、-adrenoceptor drugs,4
2、,1 肾上腺素受体阻断药-adrenoceptor blocking drugs,短效类(short-acting),非选择性nonselective,选择性selective,(-)1-R:哌唑嗪 prazosin,长效类(long-acting),酚妥拉明 phentolamine,酚苄明 phenoxybenzamine,(-)2-R:育亨宾 yohimbine,5,酚妥拉明 phentolamine,可使 R激动剂量效曲线 平行右移，最大效应不变。,regitine 立其丁、瑞支亭,(-)1、2-R reversibly(可逆地),【Actions Uses】,Competitive
3、antagonist,1、心血管（cardiovascular system）,6,phentolamine,(-)-R,血管扩张,外周阻力,BP,外周血管痉挛性疾病,静滴NA外漏,抗休克,心衰(heart failure),诊治嗜铬细胞瘤,心脏（+），心律失常,体位性低血压,减压反射,能否用Adr升压？,(-)2-R,NA,(+)1-R,7,酚妥拉明,Adr,Adrenaline reversal(肾上腺素作用的翻转),Adr,8,1)（+）M-R（+）smooth muscle of gastrointestinal tract.,2、others（其他）：,2)（+）histamine（
4、组胺）receptors secretion of gastric acid(胃酸),(组胺样作用 胃酸分泌 诱发溃疡),(腹痛、腹泻),9,雷诺病又称“肢端动脉痉挛病”,发作时指端苍白，继而发紫，伴局部冷感、麻木、疼痛，数分钟后缓解，局部皮肤转为潮红伴有烧灼、刺痛感，然后恢复正常。病情严重者，长期发作可致皮肤萎缩、增厚、溃疡，甚至指端坏死。,10,1.（-）-R 作用与酚妥拉明相似而弱；2.主要用于血管痉挛性疾病、新生儿持续性肺动脉高压症。,妥拉唑啉（苄唑啉）Tolazoline,酚苄明 phenoxybenzamine,1.可使-R激动剂量效曲线右移，Emax。,Competitive a
5、ntagonist,2.Its clinical uses are similar to phentolamine.,指出生后肺血管阻力持续性增高，肺动脉压超过体循环动脉压，使由胎儿型循环过渡至正常“成人”型循环发生障碍，引起的心房及(或)动脉导管水平血液的右向左分流，临床出现严重低氧血症等症状。多见于足月儿或过期产儿。,11,【Classification】,nonselective：,selective：,普萘 洛尔 propranolol,阿替洛尔atenolol美多洛尔metoprolol,（-）1、2-R,（-）1-R,2-adrenoceptor blocking drugs,12
6、,propranolol(普萘洛尔、心得安),【Pharmacological action】,1、(-)-R,1）cardiovascular system,(-)1-R,heart(-),force,HR,conduction,CO,oxygen consumption 耗氧量,13,（-）2-R constrict the blood vessel of skeletal muscle and coronary artery decrease the blood flow 冠脉和骨骼肌血管收缩，血流减少。,2）bronchia,（-）2-R bronchoconstriction（支气管
7、收缩）particularly in patients with asthma（哮喘）,3）renin,（-）1-R release of renin BP,14,2、,Intrinsic sympathomimetic activity,ISA,有些-R 阻断药与-R 结合后，除能阻断受体外，对-R 具有部分激动作用。,Some-adrenergic antagonists,after combining with and blocking-receptors,may have partial agonistic action.,具ISA的药，-R阻断作用弱于无ISA药。,内在拟交感活性,普
8、萘洛尔无此作用。,15,3、Membrane stabilizing action（膜稳定作用）,Some-adrenergic antagonists have local anesthetic(麻醉)effects.They decrease the membrane ion channel permeability(通透性).,细胞膜对离子的通透性,4、other effects,1)antiplatelet aggregating(抗血小板聚集),2)Some-blockers may decrease intraocular pressure(眼内压).,16,1、tachycard
9、iac arrhythmia（心律失常）2、angina pectoris（心绞痛）3、hypertension（高血压）4、others：hyperthyroidism（甲亢）偏头痛等,【Clinical uses】,17,【Contraindication】禁忌症,【Adverse reactions】,1.Inhibition of cardiac function2.Inducement or exacerbation of asthma 诱发加重哮喘3.Withdrawal(rebound)action 反跳现象,Severe heart failure（严重心衰）sinus bra
10、dycardia(窦性心动过缓)serious atria-ventricular blockade 重度房室传导阻滞 bronchial asthma（支气管哮喘）,18,3、-adrenoceptor blocker,Labetalol 拉贝洛尔,1.(-)-R(-)-RClinical use:,(1)hypertension 高血压,hypertension crisis(高血压危象)iv,(2)angina pectoris(心绞痛),19,20,拟胆碱药,M-R 激动药,抗ChE药,pilocarpine,neostigmine,抗胆碱药,M-R 阻断药,N-R 阻断药,atropine,拟肾上腺素药,-R激动药,、-R激动药,-R激动药,NA,Adr,DA,Isop,抗肾上腺素药,-R阻断药,-R阻断药,phentolamine,propranolol,d-tubocuraine,21,good bye,22,Thank you,23,
