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地氟醚

地氟醚
臨床資料
商品名英语Drug nomenclatureSUPRANE
给药途径吸入
ATC碼
法律規範狀態
法律規範
  • 處方藥物
藥物動力學數據
药物代谢不參與代謝
生物半衰期視乎每分鐘換氣次數
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 編輯維基數據鏈接
化学信息
化学式C3H2F6O
摩尔质量168.038 克/摩爾
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(英語:Desflurane),又稱地氟烷,是鹵代醚麻醉藥之一,常用於維持麻醉狀態。和其他鹵代醚麻醉藥一樣,地氟醚是外消旋體。地氟醚和七氟醚正逐步取代異氟醚成為人用全身麻醉藥的首選。由於地氟醚在血液的溶解度低,地氟醚在揮發性麻醉藥之中起效最快,藥力也最快散去。地氟醚的缺點包括藥效較弱、氣味刺鼻及成本較高。在經濟欠發達地區,地氟醚礙於成本而未能推廣。但對於低通氣量的應用情景,地氟醚和異氟醚的成本差異似乎微不足道[1]。當以大於體積分數10%的劑量施用時,地氟醚有可能引致心跳過速和刺激呼吸道,故地氟醚甚少用於誘導麻醉。

地氟醚的揮發性很強,但在室溫下仍然是種液體。兼容地氟醚的麻醉機一般都裝有專門的加熱器,確保地氟醚處於恆溫狀態,避免環境溫度變化而影響輸出濃度。地氟醚和恩氟醚(某程度上異氟醚)已知和麻醉機內的二氧化碳吸收劑反應分解,放出微量但可被偵測的一氧化碳。高風險量等情況下二氧化碳吸收劑較容易失水,這會加劇地氟醚的分解和一氧化碳的生成,尤其是對於二氧化碳吸收劑巴拉林(Baralyme)[2]

藥理學

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地氟醚是種已知的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],與及烟碱型乙酰胆碱受体别构抑制剂[5][6]。地氟醚對其他配体门控離子通道也有影響[7][8]

特性

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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
臨床用的地氟醚,瓶頸標識為銀色(最右)。由於其室溫下蒸氣壓較高,藥瓶需要配備閥門而非普通瓶蓋。
分子質量 168 克/摩爾
沸點[註 1] 23.5°C
密度(20°C) 1.465 克/毫升
蒸氣壓(20°C) 88.5 kPa (672 mmHg)
蒸氣壓(24°C) 107 kPa (804 mmHg)
血氣分配係數 0.42
油氣分配係數 19
最低氣泡濃度英语Minimum alveolar concentration[註 2] 1.17%

環境影響

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地氟醚蒸氣是種強大的温室气体,二十年期的全球暖化潛勢達3,714之高[10],也就是說,每排放一公噸地氟醚的影響相當於排放3,714噸二氧化碳。這數值要比七氟醚異氟醚遠高得多。為了比較臨床應用上不同麻醉氣體對環境的實質影響,除了全球暖化潛勢,藥性的強烈程度和鮮風量也應一併考慮。通常的假設是地氟醚和異氟醚在最低氣泡濃度下,每分鐘需要鮮風1公升;而七氟醚則需要2公升。按照每小時最低氣泡濃度測算和比較,地氟醚的全生命週期溫室效應影響為異氟醚和七氟醚的20倍[11]

有文獻推斷,全球的揮發性麻醉劑的排放的影響相當於1百萬輛汽車行駛的排放[12]。這個估算結果常常被麻醉科醫生拿來當作工作時無需顧及環境保護的藉口。然而,本結果的推算過程被後來的文獻抨擊。首先,該結果只是從美國其中一所醫療機構的數據推算而來,但該機構完全沒有使用地氟醚。其次,研究人員忽視了笑氣的全球暖化潛勢。該推算是基於在部分麻醉使用地氟醚的醫療機構並修正了笑氣的影響,每次麻醉的排放大概為175-220公斤二氧化碳當量。這意味著,1百萬輛汽車行駛的排放這估算相當可能被低估。儘管如此,該文獻作者依然呼籲採取措施來避免向大氣排放麻醉氣體[13]

備註

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  1. ^ 大氣壓力下
  2. ^ 體積分數

參考文獻

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  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]. 

延伸閱讀

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  • 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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