-zhong-shu-shen-jing-xi-tong-yao-wu-zhi-kang-dian-xian-he-kang-jing-jue.html 29 KB

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  166. <h1 id="seo-header">【迁移】药理四:中枢神经系统药物之抗癫痫和抗惊厥</h1>
  167. <p id="updated-time" class="note note-info" style="">
  168. Last updated on March 19, 2024 pm
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  173. </div>
  174. <p>癫痫是一种突然发生的、阵发性、短暂性、反复发作的大脑功能障碍,发作时常伴有脑电的异常。惊厥是中枢神经系统过度兴奋的一种症状,表现为突发性的全身性或局限性肌群强直性或阵挛性抽搐。常用的抗惊厥药物包括巴比妥类、苯二氮䓬类中的部分药物、水合氯醛及硫酸镁。</p>
  175. <p>癫痫小发作,首选乙琥胺,抑T钙通道<br>
  176. 局限发作大发作,卡马西平加二苯<br>
  177. 皮质激素肌阵挛,持续状态用安定<br>
  178. 慢加剂量停药渐,坚持用药防骤停<br>
  179. 苯妥英钠<br>
  180. 大仑丁,小无效,三坐舌咽室性常<br>
  181. 膜稳定,阻钠钙,口慢不肌静脉给,小十一级大零级<br>
  182. 碱刺激,齿龈增,低钙贫血男女症,补D补钙补叶酸<br>
  183. 卡马西平<br>
  184. 单局性,三舌咽,锂盐无效躁狂症<br>
  185. 阻滞钠,升GABA,骨髓抑制肝损伤<br>
  186. 丙戊酸钠<br>
  187. 大小并,顽固性,GABA生成代谢少<br>
  188. 抑制钠T钙通道,广谱抗癫痫病药<br>
  189. 硫酸镁<br>
  190. 效用主要看途径,泻下利胆用口服<br>
  191. 消炎去肿外热敷,注射用药抑中枢<br>
  192. 高压危象急救用,子痫抽搐破伤风</p>
  193. <h2 id="乙琥胺">乙琥胺</h2>
  194. <p>口服吸收完全,血浆蛋白结合率低,儿童半衰期30小时,成人半衰期40~50小时</p>
  195. <p>抑制丘脑T型钙通道,抑制3Hz异常放电,高浓度可抑制钠钾泵和GABA转氨酶</p>
  196. <p>治疗小发作的首选药(对其他类型无效),抗戊四氮引起的阵挛性惊厥,提高电惊厥阈值</p>
  197. <p>毒性低,但可引起肠胃道反应、中枢神经系统症状(精神病患者慎用)</p>
  198. <p>偶见粒细胞缺乏症,严重者发生再生障碍性贫血。</p>
  199. <h2 id="苯妥英钠(大仑丁)">苯妥英钠(大仑丁)</h2>
  200. <p>口服吸收不规则,起效慢,不宜作肌内注射。静脉注射用于治疗癫痫的持续状态。药物消除速率与血药浓度密切相关,<10μg/mg按一级动力学消除,半衰期为20小时;大于10μg/mg按零级动力学消除,半衰期>60小时。有条件监测血药浓度,调整剂量。</p>
  201. <p>具有膜稳定作用,阻止病灶放电向正常组织扩散,主要通过:阻断电压依赖性Na+通道,阻断电压依赖性Ca2+通道,影响钙调素激酶系统。</p>
  202. <p>抗癫痫 抗大发作、局限性发作首选,但对小发作无效,甚至会增加发作次数</p>
  203. <p>治疗中枢性疼痛综合征及外周神经痛:三叉神经、坐骨神经、舌咽神经痛</p>
  204. <p>抗心律失常 室性,特别是强心苷中毒</p>
  205. <p>局部刺激、齿龈增生</p>
  206. <p>神经系统反应 20 共济失调,40 精神错乱, 50 昏迷</p>
  207. <p>血液系统反应 巨幼红细胞性贫血</p>
  208. <p>骨骼系统反应 低钙血症</p>
  209. <p>过敏反应</p>
  210. <p>其他反应 男性乳房增大、女性多毛症、淋巴结肿大、致畸,久用突然停药可致癫痫发作加剧</p>
  211. <p>药物相互作用 肝药酶诱导剂、血浆蛋白</p>
  212. <h2 id="卡马西平(酰胺咪嗪)">卡马西平(酰胺咪嗪)</h2>
  213. <p>口服吸收缓慢、不规则,血浆蛋白质结合率为75%~80%,单次给药半衰期为15~20小时。</p>
  214. <p>与苯妥英钠相似,治疗浓度阻滞Na+通道,阻止放电扩散,并可提高脑内GABA浓度,增强其中枢抑制作用。</p>
  215. <p>抗癫痫 为有效的广谱抗癫痫药,治疗单纯性局限性发作和大发作的首选之一,还可抗复合性局限性发作和小发作</p>
  216. <p>对中枢性疼痛(三叉、舌咽)的疗效优于苯妥英钠</p>
  217. <p>对锂盐无效的躁狂症有效</p>
  218. <p>常见眩晕、视物模糊、恶心、呕吐、共济失调、手指震颤、水钠潴留等不良反应</p>
  219. <p>严重不良反应有骨髓抑制、过敏反应(肝损伤)、心律失常等</p>
  220. <p>药物相互作用 肝药酶诱导剂</p>
  221. <h2 id="苯巴比妥(鲁米那)">苯巴比妥(鲁米那)</h2>
  222. <p>既能抑制病灶的异常放电又能阻止放电扩散,主要通过:促进GABA与GABAA受体结合,延长Cl-通道开放时间,产生中枢抑制作用;阻断突触前膜Ca2+摄取,减少Ca2+依赖性神经递质的释放;较高浓度可阻断Na+和Ca2+通道。</p>
  223. <p>可用于癫痫的大发作和持续状态,对单纯的局限性发作和精神运动性发作也有效,但对小发作效果差</p>
  224. <p>中枢抑制作用强,不作为长期维持用药</p>
  225. <p>用药初期易出现嗜睡、精神萎靡</p>
  226. <p>长期使用产生耐受性</p>
  227. <p>药物相互作用 肝药酶诱导剂</p>
  228. <p>药物相互作用 肝药酶诱导剂</p>
  229. <h2 id="扑米酮(去氧苯巴比妥)">扑米酮(去氧苯巴比妥)</h2>
  230. <p>体内代谢为苯巴比妥和苯乙基丙二酰胺</p>
  231. <p>对部分性发作和大发作疗效好(不能耐受二苯的大发作),对小发作无效</p>
  232. <p>常见的不良反应包括中枢症状和血液系统毒性</p>
  233. <h2 id="丙戊酸钠">丙戊酸钠</h2>
  234. <p>口服吸收完全迅速,血浆蛋白质结合率高,半衰期约为15小时</p>
  235. <p>阻止放电扩散,使GABA生成增加、代谢减少,增加GABA能神经突触后抑制作用,抑制Na+通道和T型Ca2+通道,抑制3Hz异常放电</p>
  236. <p>广谱抗癫痫药,尤其对小发作效果好,但有肝毒性,不作为小发作的首选药</p>
  237. <p>是大发作合并小发作时的首选药,对其他药物不能控制的顽固性癫痫也有效</p>
  238. <p>消化系统症状 恶心、呕吐、腹痛等</p>
  239. <p>肝毒性</p>
  240. <p>偶见皮疹、脱发、血小板减少及聚集障碍</p>
  241. <h2 id="苯二氮䓬类">苯二氮䓬类</h2>
  242. <p>可以阻止放电扩散,但不能消除病灶的异常放电</p>
  243. <p>地西泮首选用于癫痫持续状态,静脉注射起效快,但需要注意其对呼吸的抑制作用</p>
  244. <p>硝西泮主要用于癫痫的小发作,肌阵挛性发作、婴儿痉挛</p>
  245. <p>氯硝西泮抗癫痫谱广,但易耐受,久用突然停药会加剧癫痫发作</p>
  246. <h2 id="氟桂利嗪">氟桂利嗪</h2>
  247. <p>口服易吸收,半衰期19~22天,血浆蛋白质结合率高(99%)</p>
  248. <p>可以阻断T型和L型Ca2+通道及电压依赖性Na+通道</p>
  249. <p>对局限性发作、大发作效果好</p>
  250. <p>常见不良反应是困倦、体重增加。</p>
  251. <h2 id="拉莫三嗪">拉莫三嗪</h2>
  252. <p>口服吸收完全,生物利用度98%,血浆蛋白质结合率55%,半衰期12.6小时</p>
  253. <p>阻断电压依赖性Na+通道,阻止病灶的异常放电</p>
  254. <p>多与其他抗癫痫药合用,治疗难治性癫痫</p>
  255. <p>中枢系统反应 头痛、头晕、嗜睡、视物模糊、复视、共济失调</p>
  256. <p>胃肠道反应 恶性、呕吐、便秘</p>
  257. <p>偶见皮肤水肿及弥散性血管内凝血</p>
  258. <h2 id="托吡酯">托吡酯</h2>
  259. <p>可以阻断电压依赖性Na+通道,增强GABA活性,并抑制谷氨酸介导的兴奋作用</p>
  260. <p>主要用于局限性发作和大发作,特别是辅助治疗难治性癫痫</p>
  261. <p>常见的不良反应是中枢系统反应,孕妇慎用</p>
  262. <h2 id="硫酸镁">硫酸镁</h2>
  263. <p>不同给药途径产生不同的药理作用,口服泻下和利胆作用,外用热敷消炎去肿,注射产生全身作用</p>
  264. <p>可能是由于Mg2+可以特异性地与Ca2+竞争Ca2+受体,拮抗Ca2+作用,从而发挥肌松及降压作用,而Mg2+作用于中枢神经系统,则引起感觉及意识丧失。</p>
  265. <p>主要用于子痫、破伤风等惊厥,也常用于高血压危象。</p>
  266. <p>注射给药的安全范围窄,血镁过高会引发呼吸抑制、血压骤降和心搏骤停</p>
  267. <p>肌腱反射消失是呼吸抑制的先兆,连续注射需监测</p>
  268. <p>急性中毒时应立即进行人工呼吸,注射氯化钙和葡萄糖酸钙解毒</p>
  269. </div>
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  280. <div>【迁移】药理四:中枢神经系统药物之抗癫痫和抗惊厥</div>
  281. <div>https://hexo.limour.top/-zhong-shu-shen-jing-xi-tong-yao-wu-zhi-kang-dian-xian-he-kang-jing-jue</div>
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