-chuan-chu-shen-jing-xi-tong-yao-wu-zhi-dan-jian-shou-ti.html 32 KB

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  166. <h1 id="seo-header">【迁移】药理一:传出神经系统药物之胆碱受体</h1>
  167. <p id="updated-time" class="note note-info" style="">
  168. Last updated on March 19, 2024 pm
  169. </p>
  170. <div class="markdown-body">
  171. <p>传出神经分植物神经和运动神经,前者支配心肌、平滑肌和腺体等,后者支配骨骼肌。植物神经分交感和副交感(副交感节前纤维常在迷走神经内走行),交感兴奋时效应器表现为应急时的状态,副交感兴奋时效应器表现为睡眠时的状态。</p>
  172. <p><img src="https://img.limour.top/2023/09/01/64f1a938bbb3e.webp" srcset="https://jscdn.limour.top/gh/Limour-dev/Sakurairo_Vision/load_svg/inload.svg" lazyload alt=""></p>
  173. <h2 id="ACh、AChE相关药">ACh、AChE相关药</h2>
  174. <p>拟胆碱药分两类,兴奋受体抑制酶<br>
  175. 匹罗卡品作用眼,外用治疗青光眼<br>
  176. 阿托交替芸香碱,防止虹膜晶状粘<br>
  177. 贝胆碱、腹气胀,兴奋泌尿和胃肠<br>
  178. 新斯地明抗酯酶,主治重症肌无力<br>
  179. 术后腹胀尿潴留,小心胆碱能危象<br>
  180. 毒扁豆碱毒性大,作用眼科降眼压<br>
  181. 解磷定解N症状,百虫遇碱敌敌畏,乐果中毒碘无效</p>
  182. <p>M样作用<br>
  183. 扩张血管降血压,负性三连心动缓<br>
  184. 兴奋膀胱逼尿肌,括约舒张胃肠蠕<br>
  185. 缩瞳降压调痉挛,泪腺唾液汗泌增</p>
  186. <p>N样作用<br>
  187. 骨骼肌,神经节,N样受体有烟碱</p>
  188. <p>毛果芸香碱(匹罗卡品)毛开头,所以是M受体激动剂,具有副交感样作用,一般用于滴眼。放松时,看近物比较多,比如刷手机,需要避免近处亮光刺激眼睛,因此瞳孔括约肌上的M受体激动时瞳孔会收缩,此时前房角会开大,有利于房水从内部的小梁网排出,降低眼内压,常用1%滴眼液来治疗青光眼。同时看近物需要更高的晶状体屈光度,所以会调节痉挛,睫状肌上的M受体激动、睫状肌收缩,悬韧带两端靠近而松弛,让晶状体回弹。由于所有腺体上都长M受体,所有毛果芸香碱不小心通过内眦的鼻泪管进入鼻腔、然后进入口腔时,会有大量鼻涕和唾液分泌,所以也能用来治疗口腔干燥,不过如果是治疗青光眼,则需要压迫内眦,避免此副作用。如果全身给药,肠道、支气管等内脏平滑肌上也长M受体,会促进胃肠蠕动引起痉挛、诱发哮喘,心肌上长M受体,会降低心率和血压,中枢神经长M受体,会激活和维持皮层觉醒。</p>
  189. <p>阿毛是一对,所以阿托品是M受体拮抗剂,可以起到与毛果芸香碱相反的作用,交替使用可以瞳孔扩缩交替,让虹膜保持运动状态,避免虹膜与晶状体粘连。如果阿托品中毒,则用毛果芸香碱来解毒。</p>
  190. <p>氯贝胆碱为M胆碱受体激动剂,对胃肠道和膀胱平滑肌的选择性较高,对心血管系统影响小,所以常用于术后腹气胀,胃张力缺乏症及胃潴留等的治疗。</p>
  191. <p>新斯的明能抑制AChE,同时还具有直接激动骨骼肌上的N2受体的作用,因此主要用于治疗重症肌无力,同时也能用于治疗抑制N2受体的非去极化肌松药中毒和筒箭毒中毒。如果过量,则产生胆碱能危象,持续激活化学门控离子通道N2受体,肌束震颤,较长时间后,其他电压门控离子通道由于不能复极化而无法复活,当失活数量太多时,将产生肌麻痹,而呼吸肌麻痹后果严重。此外因为抑制AChE、激动M受体,胃肠道、支气管、膀胱、心脏、腺体、眼睛,所以可以治疗术后肠胀气、尿潴留、阵发性室上性心动过速、青光眼、解救阿托品中毒,同时机械性肠/尿路梗阻、支气管哮喘禁用。季铵类化合物,脂溶性差,不易穿过血脑屏障。依酚氯胺常用于诊断。多奈哌齐常用于中枢阿尔兹海默症。</p>
  192. <p>毒扁豆碱具有与新斯的明相似的可逆性抑制胆碱酯酶的作用,同时易于通过血脑屏障,对中枢神经系统,小剂量兴奋,大剂量抑制。因此毒性大,只外用来降低眼压。</p>
  193. <p>有机磷酸酯类急性中毒,除了M样症状和N样症状外,还有中枢症状,早期兴奋中枢,表现为躁动不安、幻觉、谵妄、惊厥,后期抑制,头晕、乏力、嗜睡、昏迷,晚期呼吸循环衰竭,呼吸中枢和心血管中枢抑制</p>
  194. <p>有机磷酸酯类治疗,首先清除尚未吸收的药物,生理盐水或小苏打洗胃、但是敌百虫(美曲膦酯)遇碱会水解成敌敌畏、对硫磷遇高锰酸钾会氧化成对氧磷,用肥皂水清洗皮肤,然后解毒,联用阿托品和解磷定,由于解磷定的半衰期非常短,需要重复给药,同时维持气道通畅、给氧、抗休克。注意事项 阿托品给药需要一直到阿托品化,瞳孔扩大、面色潮红、皮肤干燥、口干、心率加快;复活剂在碱性溶液中会水解成氰化物,不能与碱性药物并用,且对中毒超3d的老化AChE无效。</p>
  195. <p>M样作用的扩血管主要来自激动血管内皮细胞上的M3受体,其释放NO,从而使周围平滑肌舒张,血压下降,此时会有短暂的反射性心率增加,之后作用于心肌M受体,负性三连。</p>
  196. <h2 id="胆碱受体阻断药">胆碱受体阻断药</h2>
  197. <p>阿托品<br>
  198. 莨菪碱类阿托品,抑制腺体平滑肌<br>
  199. 瞳孔扩大眼压升,调节麻痹心率快<br>
  200. 大量改善微循环,中枢兴奋须防范<br>
  201. 作用广泛有利弊,应用注意心血管<br>
  202. 临床用途有奇效,胃肠绞痛立即缓<br>
  203. 抑制分泌麻醉前,虹膜睫状体发炎,散瞳配镜眼底检<br>
  204. 防止虹晶粘,能治心动缓<br>
  205. 感染休克解痉挛,有机磷中毒它首选<br>
  206. 禁用前列青光眼,幽门梗阻也禁选<br>
  207. 阿托中毒解救药,毒扁豆碱地西泮</p>
  208. <p>莨菪碱类<br>
  209. 莨菪碱类阿托品,阻断M–抗胆碱<br>
  210. 尿不出去和便秘,老年痴呆青光眼<br>
  211. 作用广泛有利弊,最好不用老年人<br>
  212. 镇静显著东莨碱,能抗晕动是特点<br>
  213. 帕金森病麻醉前,只是不用它点眼<br>
  214. 感染休克山莨碱,内脏平滑肌绞痛</p>
  215. <p>N受体<br>
  216. 美卡拉明神经节,两类骨骼肌松弛<br>
  217. 琥珀胆、肌束颤,没有神经节阻断<br>
  218. 除极化、N结合,烧伤高钾心脏停<br>
  219. 碱分解、勿硫喷,呼吸麻痹抗生素<br>
  220. 筒箭毒碱正相反,缓慢持久组胺释</p>
  221. <p>阿托品可以抑制腺体M受体,胃酸分泌影响不明显,汗腺、唾液腺支气管腺分泌减少,可以用来治疗流涎、盗汗和麻醉前给药防止支气管痰液阻塞。正在发热的患者使用会降低出汗散热的能力,导致高热。</p>
  222. <p>阿托品散瞳,眼压升高,阻断睫状肌,调节麻痹,因此可以阿毛一起用于虹膜炎,但阿托品常用的还是眼底检查和验光配镜。散瞳和调节麻痹的效果可以持续一周,所以验光后会长时间视力模糊。解除迷走神经对心脏的抑制作用,可以正性三变。因此首选用于治疗各种缓慢性心律失常,如窦性心动过缓、房室传导阻滞。会用心悸的副作用、可能诱发心梗。低剂量会心率短暂性轻度减慢。</p>
  223. <p>能解除内脏平滑肌痉挛状态,因此和阿片类(中枢止痛但会加剧外周平滑肌痉挛,阿托品解除痉挛)合用可以治疗胃肠道、膀胱、肾、胆的绞痛。禁用于便秘、肠胀气、尿潴留、前列腺肥大。</p>
  224. <p>当大剂量使用阿托品时(与阻断M受体无关),也能解除血管平滑肌痉挛,扩张血管(直接和间接两种方式,间接的比如汗腺分泌减少后,散热需要通过皮肤血管扩张来代偿),改善微循环,增加重要脏器的血供,适用于感染性休克。休克时皮肤苍白湿冷、而阿托品可以使面色潮红、手脚温暖。也会使中枢先兴奋后抑制,先多言、谵妄、幻觉、惊厥,然后呼吸抑制。</p>
  225. <ul>
  226. <li>唯有阿托品,可解除迷走对心脏的抑制而治疗缓慢型心律失常</li>
  227. <li>利多卡因、苯妥英钠,可用于治疗强心苷中毒时的快速型心律失常</li>
  228. <li>普萘洛尔,首选用于窦性心动过速</li>
  229. <li>奎尼丁,可将地高辛从组织中置换出来,升高其血药浓度而加重中毒</li>
  230. </ul>
  231. <p>东莨菪碱容易穿过血脑屏障,对中枢的作用强,有中枢抗胆碱作用和中枢镇静作用,可以抑制前庭神经,治疗帕金森和晕动病。对腺体的抑制作用比阿托品强,加上具有中枢镇静的效果,所以常用于麻醉前给药。容易出现中枢不良反应、谵妄、幻觉、欣快,进而导致滥用。对心血管、眼的作用弱。</p>
  232. <p>山莨菪碱(6542)很难穿过血脑屏障,对眼、腺体、中枢作用弱,主要具有强大的血管平滑肌和内脏平滑肌的痉挛作用,主治感染性休克、内脏绞痛,补足血容量的前提下,可用于其他休克。有面色潮红、便秘、肠胀气、尿潴留的副作用。</p>
  233. <p>阿托品的徒子徒孙(合成代用品)有合成扩瞳药,后马托品、托吡卡胺、环喷托酯、尤卡托品,较阿托品起效快,持续时间短,名字都带托,起效一点不托;合成解痉药,异丙托溴铵、溴丙胺太林(普鲁本辛)、贝那替嗪(胃复康)。另,各种西平,如派仑西平,可以选择阻断胃壁细胞上的M1受体,抑制胃酸分泌。</p>
  234. <p><img src="https://img.limour.top/2023/09/01/64f1a94b9d91f.webp" srcset="https://jscdn.limour.top/gh/Limour-dev/Sakurairo_Vision/load_svg/inload.svg" lazyload alt=""></p>
  235. <p>N1受体主要在神经节上,阻断剂有经典的美卡拉明,六甲双铵,速效短效的樟磺咪芬,既阻断交感,又阻断副交感。美卡拉明阻断交感,血压下降,麻醉时用来控制血压。阻断副交感,阻断M样症状,口干、视力模糊、便秘、肠胀气、尿潴留。</p>
  236. <p>去打老虎,因此琥珀胆碱事去极化型肌松药,激动N2受体,持久去极化,使骨骼肌长期处于不应期状态。因此短暂肌束颤动后起效快,时间短,易于控制。静注用于短时操作,如气管插管、消化道镜检,静滴用于较长的手术。不能用新斯的明解救,因为琥珀年代久远,不新了。由于持续去极化,肌肉钾离子流出,血钾会升高。呼吸肌麻痹可能窒息、肌束震颤会疼、血钾升高抑制心脏。禁用于白内障、青光眼(眼外骨骼肌短暂收缩,升高眼压)、晶体摘除手术和血钾升高的烧伤、脑血管意外、恶性高热等。与氨基糖苷类抗生素或多黏菌素B合用,后者阻断神经肌肉接头,协同易致呼吸肌麻痹。</p>
  237. <p>而捡裤子穿的筒箭毒碱阻断N2受体,竞争性抑制受体,使骨骼肌不能收缩。肌松作用慢而持久,先松弛眼部和头部的小肌肉,然后是颈部,到四肢、躯干,再面、舌、咽喉和咀嚼肌,最后是肋间肌、膈肌,另,对喉头、气管作用强。用于大手术的辅助麻醉。用新斯的明解救。此外,还具有促组胺释放和神经节阻滞的作用,诱发皮疹、支气管痉挛、血压下降。</p>
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  249. <div>【迁移】药理一:传出神经系统药物之胆碱受体</div>
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  263. <div>March 19, 2024</div>
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