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地氟醚

地氟醚
临床资料
商品名英语Drug nomenclatureSUPRANE
给药途径吸入
ATC码
法律规范状态
法律规范
  • 处方药物
药物动力学数据
药物代谢不参与代谢
生物半衰期视乎每分钟换气次数
识别信息
  • 2-(二氟甲氧基)-1,1,1,2-四氟乙烷
CAS号57041-67-5  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.214.382 编辑维基数据链接
化学信息
化学式C3H2F6O
摩尔质量168.038 克/摩尔
3D模型(JSmol英语JSmol
  • FC(F)(F)C(F)OC(F)F
  • InChI=1S/C3H2F6O/c4-1(3(7,8)9)10-2(5)6/h1-2H checkY
  • Key:DPYMFVXJLLWWEU-UHFFFAOYSA-N checkY

地氟醚(英语:Desflurane),又称地氟烷,是卤代醚麻醉药之一,常用于维持麻醉状态。和其他卤代醚麻醉药一样,地氟醚是外消旋体。地氟醚和七氟醚正逐步取代异氟醚成为人用全身麻醉药的首选。由于地氟醚在血液的溶解度低,地氟醚在挥发性麻醉药之中起效最快,药力也最快散去。地氟醚的缺点包括药效较弱、气味刺鼻及成本较高。在经济欠发达地区,地氟醚碍于成本而未能推广。但对于低通气量的应用情景,地氟醚和异氟醚的成本差异似乎微不足道[1]。当以大于体积分数10%的剂量施用时,地氟醚有可能引致心跳过速和刺激呼吸道,故地氟醚甚少用于诱导麻醉。

地氟醚的挥发性很强,但在室温下仍然是种液体。兼容地氟醚的麻醉机一般都装有专门的加热器,确保地氟醚处于恒温状态,避免环境温度变化而影响输出浓度。地氟醚和恩氟醚(某程度上异氟醚)已知和麻醉机内的二氧化碳吸收剂反应分解,放出微量但可被侦测的一氧化碳。高风险量等情况下二氧化碳吸收剂较容易失水,这会加剧地氟醚的分解和一氧化碳的生成,尤其是对于二氧化碳吸收剂巴拉林(Baralyme)[2]

药理学

地氟醚是种已知的γ-氨基丁酸A型受体(GABAA受体)和甘氨酸受体别构激活剂[3][4],与及烟碱型乙酰胆碱受体别构抑制剂[5][6]。地氟醚对其他配体门控离子通道也有影响[7][8]

特性

地氟烷是外消旋体,即以下两种对映异构体的1:1混合物:[9]

对映体
Structural Formula of (R)-Desfluran Structural Formula of (S)-Desfluran
临床用的地氟醚,瓶颈标识为银色(最右)。由于其室温下蒸气压较高,药瓶需要配备阀门而非普通瓶盖。
分子质量 168 克/摩尔
沸点[注 1] 23.5°C
密度(20°C) 1.465 克/毫升
蒸气压(20°C) 88.5 kPa (672 mmHg)
蒸气压(24°C) 107 kPa (804 mmHg)
血气分配系数 0.42
油气分配系数 19
最低气泡浓度英语Minimum alveolar concentration[注 2] 1.17%

环境影响

地氟醚蒸气是种强大的温室气体,二十年期的全球暖化潜势达3,714之高[10],也就是说,每排放一公吨地氟醚的影响相当于排放3,714吨二氧化碳。这数值要比七氟醚异氟醚远高得多。为了比较临床应用上不同麻醉气体对环境的实质影响,除了全球暖化潜势,药性的强烈程度和鲜风量也应一并考虑。通常的假设是地氟醚和异氟醚在最低气泡浓度下,每分钟需要鲜风1升;而七氟醚则需要2升。按照每小时最低气泡浓度测算和比较,地氟醚的全生命周期温室效应影响为异氟醚和七氟醚的20倍[11]

有文献推断,全球的挥发性麻醉剂的排放的影响相当于1百万辆汽车行驶的排放[12]。这个估算结果常常被麻醉科医生拿来当作工作时无需顾及环境保护的借口。然而,本结果的推算过程被后来的文献抨击。首先,该结果只是从美国其中一所医疗机构的数据推算而来,但该机构完全没有使用地氟醚。其次,研究人员忽视了笑气的全球暖化潜势。该推算是基于在部分麻醉使用地氟醚的医疗机构并修正了笑气的影响,每次麻醉的排放大概为175-220公斤二氧化碳当量。这意味着,1百万辆汽车行驶的排放这估算相当可能被低估。尽管如此,该文献作者依然呼吁采取措施来避免向大气排放麻醉气体[13]

备注

  1. ^ 大气压力下
  2. ^ 体积分数

参考文献

  1. ^ John Varkey. Cost Analysis of Desflurane and Sevoflurane: An Integrative Review and Implementation Project Introducing the Volatile Anesthetic Cost Calculator (PDF). 2012. 
  2. ^ Fang; et al. Carbon Monoxide Production from Degradation of Desflurane (PDF). Anesthesia and Analgesia. 1995. 
  3. ^ Hugh C. Hemmings; Philip M. Hopkins. Foundations of Anesthesia: Basic Sciences for Clinical Practice. Elsevier Health Sciences. 2006: 290–291 [2017-07-10]. ISBN 0-323-03707-0. (原始内容存档于2016-05-13). 
  4. ^ Ronald D. Miller; Lars I. Eriksson; Lee A Fleisher; Jeanine P. Wiener-Kronish; Neal H Cohen; William L. Young. Miller's Anesthesia. Elsevier Health Sciences. 20 October 2014: 624– [2017-07-10]. ISBN 978-0-323-28011-2. (原始内容存档于2016-05-03). 
  5. ^ Allan P. Reed; Francine S. Yudkowitz. Clinical Cases in Anesthesia. Elsevier Health Sciences. 2 December 2013: 101– [2017-07-10]. ISBN 978-0-323-18654-4. (原始内容存档于2016-06-23). 
  6. ^ Paul Barash; Bruce F. Cullen; Robert K. Stoelting; Michael Cahalan; Christine M. Stock; Rafael Ortega. Clinical Anesthesia, 7e: Print + Ebook with Multimedia. Lippincott Williams & Wilkins. 7 February 2013: 470– [2017-07-10]. ISBN 978-1-4698-3027-8. (原始内容存档于2016-05-11). 
  7. ^ Charles J. Coté; Jerrold Lerman; Brian J. Anderson. A Practice of Anesthesia for Infants and Children: Expert Consult - Online and Print. Elsevier Health Sciences. 2013: 499– [2017-07-10]. ISBN 1-4377-2792-1. (原始内容存档于2016-05-02). 
  8. ^ Linda S. Aglio; Robert W. Lekowski; Richard D. Urman. Essential Clinical Anesthesia Review: Keywords, Questions and Answers for the Boards. Cambridge University Press. 8 January 2015: 128– [2017-07-10]. ISBN 978-1-107-68130-9. (原始内容存档于2016-05-11). 
  9. ^ Rote Liste Service GmbH (Hrsg.): Rote Liste 2017 - Arzneimittelverzeichnis für Deutschland (einschließlich EU-Zulassungen und bestimmter Medizinprodukte). Rote Liste Service GmbH, Frankfurt/Main, 2017, Aufl. 57, ISBN 978-3-946057-10-9, S. 175.
  10. ^ Ryan, Susan M.; Nielsen, Claus J. Global Warming Potential of Inhaled Anesthetics: Application to Clinical Use. Anesthesia & Analgesia (San Francisco, CA: International Anesthesia Research Society). July 2010, 111 (1): 92–98 [9 September 2011]. doi:10.1213/ane.0b013e3181e058d7. 
  11. ^ Sherman J, Le C, Lamers V, Eckelman M. Life Cycle Greenhouse Gas Emissions of Anesthetic Drugs. Anesthesia and Analgesia. May 2012, 114 (5): 1086–1090 [2017-07-10]. doi:10.1213/ANE.0b013e31824f6940. (原始内容存档于2017-05-29). 
  12. ^ Sulbaek Andersen MP, Sander SP, Nielsen OJ, Wagner DS, Sanford Jr TJ, Wallington TJ. Inhalation anaesthetics and climate change. British Journal of Anaesthesia. July 2010, 105 (6  ): 760–766 [2017-07-10]. doi:10.1093/bja/aeq259. (原始内容存档于2011-09-05). 
  13. ^ Sherman, J. Estimate of Carbon Dioxide Equivalents of Inhaled Anesthetics in the United States. American Society of Anesthesiologists. American Society of Anesthesiologists. [June 3, 2015]. 

延伸阅读

  • Eger, Eisenkraft, Weiskopf. The Pharmacology of Inhaled Anesthetics. 2003.
  • Rang, Dale, Ritter, Moore. Pharmacology 5th Edition. 2003.
  • Martin Bellgardt: Evaluation der Sedierungstiefe und der Aufwachzeiten frisch operierter Patienten mit neurophysiologischem Monitoring im Rahmen der Studie: Desfluran versus Propofol zur Sedierung beatmeter Patienten. Bochum, Dissertation, 2005 (pdf)
  • Susanne Lohmann: Verträglichkeit, Nebenwirkungen und Hämodynamik der inhalativen Sedierung mit Desfluran im Rahmen der Studie: Desfluran versus Propofol zur Sedierung beatmeter Patienten. Bochum, Dissertation, 2006 (pdf)
  • Patel SS, Goa KL. (1995) "Desflurane. A review of its pharmacodynamic and pharmacokinetic properties and its efficacy in general anaesthesia." Drugs Oct;50(4):742-67. PMID 8536556
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地氟醚
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