胺碘酮为什么禁用生理盐水?临床应用还有这7个问题,太关键了!

2021-12-22 中国医学论坛报今日循环 网络

胺碘酮为什么禁用生理盐水?临床应用还有这7个问题,太关键了!

孙志军副主任医师

首都医科大学附属北京友谊医院

胺碘酮是临床中常用的抗心律失常药物,广泛应用于房性心律失常和室性心律失常的治疗,尤其对一些合并有心功能不全的房颤患者适用。

对于房颤的药物复律,心功能不全合并室性心律失常的治疗、频发室早以及一些致命室速等情况的处理中,胺碘酮都是相对安全的药物。

在临床使用过程中,胺碘酮配伍时要注意只能用葡萄糖溶液溶解而不能用生理盐水。这与胺碘酮是苯环上二碘取代物这一分子结构特点有关。

首先,一般含碘物质化学性质不太稳定,在碱性环境中易发生降解,而偏酸性的环境可以在一定程度上抑制胺碘酮上二碘取代物降解。

葡萄糖溶液和生理盐水之间pH值略有不同,葡萄糖溶液是偏酸性的,生理盐水是中性或者是中性偏碱性的溶液。因此葡萄糖溶液能够抑制胺碘酮分子上二碘取代物的降解。

其次,生理盐水的溶质主要是氯化钠,氯化钠中的氯离子可以与胺碘酮苯环上的碘产生化合反应,导致碘在液体中形成一些沉淀聚集,液体中的沉淀物输到体内有可能会产生不良反应。

所以,胺碘酮说明书也有提到胺碘酮需要用葡萄糖溶液溶解而不能用生理盐水。

虽然有些情况可能错用生理盐水溶解胺碘酮并使用后没有发生严重后果。但是,临床用药一定要谨慎,注意溶解胺碘酮一定要用葡萄糖溶液,不能使用生理盐水。

随着我国人口老龄化问题日益显著,许多与老龄化相关的慢性疾病,尤其是心血管疾病发病率是越来越高,患病人数越来越多。

其中,房颤的危险因素中非常重要的一项就是年龄,房颤患者人数增加,临床使用胺碘酮的机会也非常多。

下面简单总结胺碘酮使用中几个需要注意的问题。

第一点,胺碘酮是多离子通道的抑制剂,而不是单纯的钾离子通道抑制剂,胺碘酮在一定程度上还具有钙离子通道、钠离子通道抑制剂以及β受体阻滞剂的作用。

虽然胺碘酮对于血压及心功能的影响比Ⅰ类抗心律失常药物及β受体阻滞剂小,但是仍然不能忽略胺碘酮对血流动力学的影响以及胺碘酮降低血压、抑制心肌收缩力的作用。因此,对于老年人,尤其是低血压或者合并心功能不全的患者,在使用胺碘酮时一定要注意患者血压和射血分数的情况。

第二点,刚才已经提到胺碘酮是多离子通道抑制剂,对于基础心率偏慢的患者,比如说有房室传导阻滞、窦性心动过缓甚至窦性停搏的患者,使用胺碘酮要谨慎。

另外,要特别注意老年人,受患者肝功能、肾功能代谢的影响,老年人更容易发生胺碘酮的蓄积,导致已有合并缓慢性心律失常的患者,发生更严重的心动过缓。

第三点,胺碘酮是一种钾离子通道抑制剂,可以使QT间期延长。应用时应注意患者血钾情况及其他同时使用的药物。尤其是老年人容易发生胃肠功能紊乱、肠炎,患者呕吐、腹泻造成严重低钾。临床上有些药物会延长QT间期,比如常用的喹诺酮类抗生素,左氧氟沙星、莫西沙星等。

如果低钾的患者同时使用了胺碘酮和喹诺酮等使QT间期延长的抗生素,就很容易发生尖端扭转型室速,甚至诱发室颤,导致患者猝死。

第四点,胺碘酮与他汀类等(阿托伐他汀等)临床上常用的一些心血管药物之间存在互相影响的作用。

比如胺碘酮与常用的抗凝药华法林、降脂药他汀类等都是在肝脏内经细胞色素P450系统3A4同工酶参与代谢,因此使用胺碘酮会增加华法林的蓄积作用,使华法林的血药浓度成倍增加,产生过抗凝作用,增加出血风险。

所以,胺碘酮与华法林合用,需要更加密切监测INR的变化。同理,胺碘酮也可能增加他汀类肌病和肝功能异常等副作用发生的概率。

第五点,胺碘酮可能引起甲状腺功能异常,虽然发生率并不是非常高,但是在胺碘酮使用的初期,要密切监测患者的甲状腺功能。

建议患者初次使用胺碘酮一个月时复查甲状腺功能,明确患者是否有甲状腺功能亢进(甲亢)或者甲状腺功能减退的情况,其中甲亢更为常见。

第六点,胺碘酮还有可能引起肺间质纤维化。虽然这种情况并不多见,但是一旦发生肺间质纤维化,患者肺部的病变就是不可逆的。肺间质纤维化对患者的肺功能以及全身状态的影响都是非常大的,甚至是致命的。

所以,临床上一定要重视这个情况,密切关注患者肺部情况,至少在患者使用胺碘酮的前3个月安排患者复查一次胸部低剂量CT或者是胸片,排除肺纤维化的情况。

第七点,刚才提到过,胺碘酮通过肝脏代谢,所以有引起肝功能异常的可能。患者尤其是老年患者使用胺碘酮时必须定期监测肝功能。如果患者合用上面提到的他汀类以及其他有肝脏毒性的药物时,要更加注意密切监测肝功能。

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    2022-01-16 胡国宏
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    2022-01-03 ms5000000518050841

    学习了

    0

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胺碘酮规范应用专家建议

胺碘酮是临床常用抗心律失常药。随着心律失常治疗理念的不断更新,胺碘酮的临床地位在不断变化。临床实践中也有诸多不规范应用的情况。本专家建议从适应证、药理学与临床、使用剂量、随访和副作用等方面介绍了胺碘酮,重在规范应用。同时对一些有争议的问题也表达了专家组的观点。 

NEJM:胺碘酮引起的皮肤变色-病例报道

皮肤变色是胺碘酮罕见的不良反应,可能会随着药物的停用而减轻。跌倒可归因于体位性低血压。在住院期间,对患者的药物进行了调整,包括停用胺碘酮。

Circulation:静脉或骨内给药对院外心脏骤停患者预后的影响

抗心律失常药物还没有被证明能显著提高由休克难治性心室颤动/无脉性室性心动过速引起的院外心脏骤停的总生存率。而且给药途径如何影响这一点也尚不清楚。在一项随机化、安慰剂为对照的临床试验的判断分析中,研究人员对比了在ALPS试验中由急救医疗人员随机分配抗心律失常药物vs安慰剂的休克难治性室颤/无脉性室速患者的生存期和出院期的差异,并根据静脉和骨内给药分层。共3019位被随机分配的患者,2358例经静脉通

氢氯噻嗪、胺碘酮、环丙沙星、萘普生等可引发光敏性反应,造成皮肤损伤

晒晒太阳是好事,但有时候就会发生严重晒伤,皮肤出现灼热和瘙痒感、发红、肿胀及起疱等。这里值得注意的是,也许是因为服用的某种药物让你对阳光更敏感。

服用胺碘酮,这8点一定要注意!

胺碘酮不是谁想用就能用的!