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头孢曲松 vs 头孢他啶、头孢哌酮，三代头孢用药有何不同？

2022-03-29 药圈网 药圈网

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第三代头孢菌素自20世纪80年代起逐步进入临床并得到广泛应用。与其他头孢菌素相比，具有抗菌活性强、抗菌谱广、高度耐酶、对细菌外膜穿透力强、对组织穿透力强、血清和组织药物浓度高、有效浓度维持时间长、

第三代头孢菌素自20世纪80年代起逐步进入临床并得到广泛应用。与其他头孢菌素相比，具有抗菌活性强、抗菌谱广、高度耐酶、对细菌外膜穿透力强、对组织穿透力强、血清和组织药物浓度高、有效浓度维持时间长、对人体毒性低等优点。

 

临床常用的品种有头孢他啶、头孢哌酮、头孢曲松、头孢噻肟等，今天界小药就来为大家汇总这4种常用头孢菌素的异同点。

| 抗菌活性 |
第三代头孢菌素对革兰阴性杆菌的抗菌作用强，明显超过第一代和第二代头孢菌素，并且对革兰阴性杆菌产生的广谱β内酰胺酶高度稳定[对超广谱β内酰胺酶（ESBLS）无效]。
第三代头孢菌素的抗菌谱广，部分药物对铜绿假单胞菌和厌氧菌有不同程度的抗菌作用，而头孢曲松与头孢噻肟则对肺炎链球菌具有较强的抗菌活性，但对铜绿假单胞菌无效，见表1。
表1 四种头孢菌素的抗菌活性[1]

| 药物在体内的特点 |

第三代头孢菌素在组织分布广，除头孢哌酮不易透过血脑屏障外，其余药物均能透过。头孢哌酮与头孢曲松在胆道中有较高浓度，头孢曲松具有较长半衰期，可一天给药一次，见表2。
表2  四种头孢菌素在体内特点[1]

| 临床应用 |
由于每种头孢菌素的抗菌活性及体内特点不同，因此在临床选择用药侧重点也所不同。
头孢曲松与头孢噻肟可用于常见病原菌为青霉素耐药肺炎链球菌的感染性疾病及社区获得性感染的经验治疗，头孢他啶与头孢哌酮则用于常见病原菌为敏感铜绿假单胞菌的感染性疾病及医院获得性感染的经验治疗。4种药物在国内批准的适应症见表3。
表3  四种头孢菌素在国内批准适应症[2]
| 不良反应与注意事项 |

过敏试验

2021年4月，国家卫生健康委发布《β内酰胺类抗菌药物皮肤试验指导原则（2021版）》中指出，头孢类抗菌药物在以下两种情况下需要做皮试：

  • 既往明确的青霉素或头孢菌素（速发型）过敏史患者；

  • 药品说明书中规定需进行皮试的。

头孢噻肟部分厂家说明书中明确提示“用药前需进行过敏试验”，因此在应用该药时应引起注意。

双硫仑样反应

头孢菌素类抗菌药以母核7-氨基头孢烯酸（7-ACA）为基础，若7-ACA环的3位上有甲硫四氮唑侧链，如头孢哌酮钠，可与辅酶I（NAD）竞争乙醛脱氢酶的活性中心，从而抑制乙醛脱氢酶的活性，使酒精初步代谢生成的乙醛积聚而引起“双硫仑样反应”。
此外若含有相似的结构，如：含有甲硫三嗪侧链的头孢曲松钠、含有氨基噻唑侧链的头孢噻肟钠等，也可能发生双硫仑样反应。因此，使用头孢菌素类抗菌药时应避免饮酒，并注意与含有乙醇的药物（如藿香正气水）合用。

出血风险

头孢哌酮，可致低凝血酶原血症或出血。其机制可能与合成维生素K的肠道菌群受到抑制有关，营养不良者、吸收不良者（如肺囊性纤维化者）、酒精中毒者和长期静脉输注高营养制剂者均存在上述危险。此外，甲硫四氮唑侧链可干扰维生素K循环，阻碍凝血酶原的合成，致维生素K依赖性凝血因子合成受阻。7位碳原子的取代基为-COOH的头孢菌素类可抑制血小板聚集，使出血倾向加重。

胆囊假性结石

头孢曲松钠的钙盐易沉淀于胆囊中，形成头孢曲松钠相关性胆囊假性结石，停药后可自行消退，也称可逆性结石或假结石症。其机制主要是头孢曲松钠在体内不被分解，而以原形经胆囊、肾排出，故在胆汁及尿液中的药物浓度高。头孢曲松钠解离后的阴离子与钙离子亲和力较高，易在胆囊及肾集合系统内形成不溶性头孢曲松钙盐沉淀物而形成结石。
头孢曲松钠制剂不能加入哈特曼氏及林格氏等含有钙的溶液中使用。其与含钙剂或含钙产品合并用药有可能导致致死性结局的不良事件。

其他

头孢曲松不得用于新生儿高胆红素血症治疗。体外研究表明头孢曲松能取代胆红素与血清白蛋白结合，导致这些患者可能发生胆红素脑病的风险。有黄疸的新生儿或有黄疸严重倾向的新生儿应慎用或避免使用本品。
第三代头孢菌素抗菌药物由于抗菌谱广，可致二重感染，如假膜性肠炎、念珠菌感染等。
| 小结 |
第三代头孢菌素类抗菌药物均有抗菌谱广、抗菌活性强、低致敏性等优点，在临床上广泛应用。只有正确认识药物特点，正确掌握应用药物指征，才能保持抗菌药物的持久抗菌活性，避免细菌耐药率快速增长。
参考文献：
[1]药物比较与临床合理选择（呼吸科疾病分册），人民卫生出版社，2014.
[2]MCDEX合理用药信息支持系统。
[3]头孢噻肟、头孢曲松、头孢他啶、头孢哌酮药品说明书。

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    2023-08-10 西红柿炒鸡蛋（Mary） 来自湖北省

    学习

    0

  2. [GetPortalCommentsPageByObjectIdResponse(id=2152109, encodeId=8c0a21521091e, content=学习, beContent=null, objectType=article, channel=null, level=null, likeNumber=22, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=8eab5296526, createdName=西红柿炒鸡蛋（Mary）, createdTime=Thu Aug 10 15:27:25 CST 2023, time=2023-08-10, status=1, ipAttribution=湖北省), GetPortalCommentsPageByObjectIdResponse(id=1238616, encodeId=3ce212386166f, content=分析的真好！老师在注射用阿莫西林钠克拉维酸钾会出现双硫仑反应吗？, beContent=null, objectType=article, channel=null, level=null, likeNumber=27, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=80216408729, createdName=ms7000001405050111, createdTime=Sun Aug 14 13:52:14 CST 2022, time=2022-08-14, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1207630, encodeId=8c7a120e630f2, content=学习到了, beContent=null, objectType=article, channel=null, level=null, likeNumber=29, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=62342839718, createdName=188927378, createdTime=Thu Mar 31 19:03:48 CST 2022, time=2022-03-31, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1379575, encodeId=eede13e9575e2, content=<a href='/topic/show?id=d9694434815' target=_blank style='color:#2F92EE;'>#头孢曲松#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=29, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=44348, encryptionId=d9694434815, topicName=头孢曲松)], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=37d0457, createdName=yhj-time, createdTime=Thu Mar 31 05:42:54 CST 2022, time=2022-03-31, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1459584, encodeId=89f81459584d6, content=<a href='/topic/show?id=82a24434020' target=_blank style='color:#2F92EE;'>#头孢#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=57, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=44340, encryptionId=82a24434020, topicName=头孢)], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=acae6165124, createdName=jj000003, createdTime=Thu Mar 31 05:42:54 CST 2022, time=2022-03-31, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1207045, encodeId=31dd120e045a9, content=解释明白，简单明了, beContent=null, objectType=article, channel=null, level=null, likeNumber=45, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=da5e5589925, createdName=ms9000001320509575, createdTime=Tue Mar 29 22:57:58 CST 2022, time=2022-03-29, status=1, ipAttribution=)]
    2022-08-14 ms7000001405050111

    分析的真好！老师在注射用阿莫西林钠克拉维酸钾会出现双硫仑反应吗？

    0

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    2022-03-31 188927378

    学习到了

    0

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    2022-03-31 yhj-time

    #头孢曲松#

    0

  5. [GetPortalCommentsPageByObjectIdResponse(id=2152109, encodeId=8c0a21521091e, content=学习, beContent=null, objectType=article, channel=null, level=null, likeNumber=22, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=8eab5296526, createdName=西红柿炒鸡蛋（Mary）, createdTime=Thu Aug 10 15:27:25 CST 2023, time=2023-08-10, status=1, ipAttribution=湖北省), GetPortalCommentsPageByObjectIdResponse(id=1238616, encodeId=3ce212386166f, content=分析的真好！老师在注射用阿莫西林钠克拉维酸钾会出现双硫仑反应吗？, beContent=null, objectType=article, channel=null, level=null, likeNumber=27, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=80216408729, createdName=ms7000001405050111, createdTime=Sun Aug 14 13:52:14 CST 2022, time=2022-08-14, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1207630, encodeId=8c7a120e630f2, content=学习到了, beContent=null, objectType=article, channel=null, level=null, likeNumber=29, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=62342839718, createdName=188927378, createdTime=Thu Mar 31 19:03:48 CST 2022, time=2022-03-31, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1379575, encodeId=eede13e9575e2, content=<a href='/topic/show?id=d9694434815' target=_blank style='color:#2F92EE;'>#头孢曲松#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=29, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=44348, encryptionId=d9694434815, topicName=头孢曲松)], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=37d0457, createdName=yhj-time, createdTime=Thu Mar 31 05:42:54 CST 2022, time=2022-03-31, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1459584, encodeId=89f81459584d6, content=<a href='/topic/show?id=82a24434020' target=_blank style='color:#2F92EE;'>#头孢#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=57, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=44340, encryptionId=82a24434020, topicName=头孢)], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=acae6165124, createdName=jj000003, createdTime=Thu Mar 31 05:42:54 CST 2022, time=2022-03-31, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1207045, encodeId=31dd120e045a9, content=解释明白，简单明了, beContent=null, objectType=article, channel=null, level=null, likeNumber=45, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=da5e5589925, createdName=ms9000001320509575, createdTime=Tue Mar 29 22:57:58 CST 2022, time=2022-03-29, status=1, ipAttribution=)]
    2022-03-31 jj000003

    #头孢#

    0

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    2022-03-29 ms9000001320509575

    解释明白，简单明了

    0