| 词条 | Enflurane | ||||||||||||
| 释义 |
| verifiedrevid = 461093677 | IUPAC_name = (RS)-2-chloro-1-(difluoromethoxy)-1,1,2-trifluoro-ethane | image = Enflurane.svg | image2 = Enflurane-3D-balls.png | tradename = | Drugs.com = {{drugs.com|CONS|enflurane}} | pregnancy_category = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = 97% | metabolism = | elimination_half-life = | IUPHAR_ligand = 7175 | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 13838-16-9 | ATC_prefix = N01 | ATC_suffix = AB04 | ATC_supplemental = | PubChem = 3226 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB00228 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 3113 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 91I69L5AY5 | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D00543 | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 4792 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 1257 | C=3 | H=2 | Cl=1 | F=5 | O=1 | molecular_weight = 184.492 g/mol | smiles = FC(Cl)C(F)(F)OC(F)F | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C3H2ClF5O/c4-1(5)3(8,9)10-2(6)7/h1-2H | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = JPGQOUSTVILISH-UHFFFAOYSA-N }} Enflurane (2-chloro-1,1,2,-trifluoroethyl-difluoromethyl ether) is a halogenated ether. Developed by Ross Terrell in 1963, it was first used clinically in 1966. It was increasingly used for inhalational anesthesia during the 1970s and 1980s[1] but is no longer in common use. Enflurane is a structural isomer of isoflurane. It vaporizes readily, but is a liquid at room temperature. Physical properties
Side effectsClinically, enflurane produces a dose-related depression of myocardial contractility with an associated decrease in myocardial oxygen consumption. Between 2% and 5% of the inhaled dose is oxidised in the liver, producing fluoride ions and difluoromethoxy-difluoroacetic acid. This is significantly higher than the metabolism of its structural isomer isoflurane. Enflurane also lowers the threshold for seizures, and should especially not be used on people with epilepsy.[2] Like all potent inhalation anaesthetic agents it is a known trigger of malignant hyperthermia. Like the other potent inhalation agents it relaxes the uterus in pregnant women which is associated with more blood loss at delivery or other procedures on the gravid uterus. The obsolete (as an anaesthetic) agent methoxyflurane had a nephrotoxic effect and caused acute renal failure, usually attributed to the liberation of fluoride ions from its metabolism. Enflurane is similarly metabolised but the liberation of fluoride results in a lower plasma level and enflurane related renal failure seemed unusual if seen at all.[3] PharmacologyThe exact mechanism of the action of general anaesthetics have not been delineated.[4] Enflurane acts as a positive allosteric modulator of the GABAA,[5][6][7][8] glycine, and 5-HT3 receptors,[9][10] and as a negative allosteric modulator of the AMPA, kainate, and NMDA receptors,[10][11][12] as well as of nicotinic acetylcholine receptors.[9] Occupational safetyIn the workplace, people may be exposed to enflurane by breathing it in as a waste anaesthetic gas, swallowing it, eye contact, or skin contact. The National Institute for Occupational Safety and Health (NIOSH) has set a recommended exposure limit (REL) for exposure to waste anaesthetic gas of 2 ppm (15.1 mg/m3) over a 60-minute period. Symptoms of occupational exposure to enflurane include eye irritation, central nervous system depression, analgesia, anesthesia, convulsions, and respiratory depression.[13] References1. ^{{cite book|last1=Niedermeyer|first1=Ernst|last2=Silva|first2=F. H. Lopes da|title=Electroencephalography: Basic Principles, Clinical Applications, and Related Fields|url=https://books.google.com/books?id=tndqYGPHQdEC&pg=PA1156|year=2005|publisher=Lippincott Williams & Wilkins|isbn=978-0-7817-5126-1|page=1156}} {{General anesthetics}}{{Navboxes2. ^{{Cite journal|url=https://thinklab.com/discussion/prediction-in-epilepsy/224#6|title=Enflurane has established ictogenic properties?|date=April 2004|website=Thinklab|publisher=|access-date=October 17, 2016|doi=10.15363/thinklab.d224|last1=Khankhanian|first1=Pouya|last2=Himmelstein|first2=Daniel}} 3. ^By G. Edward Morgan, Maged S. Mikhail, Michael J. Murray, C. Philip Larson; Clinical Anaesthesiology third edition,142. 4. ^{{cite web | url=http://www.scientificamerican.com/article/how-does-anesthesia-work/ | title=How does anesthesia work?}} 5. ^{{Cite journal | author = M. Wakamori, Y. Ikemoto & N. Akaike | title = Effects of two volatile anesthetics and a volatile convulsant on the excitatory and inhibitory amino acid responses in dissociated CNS neurons of the rat | journal = Journal of Neurophysiology | volume = 66 | issue = 6 | pages = 2014–2021 | year = 1991 | doi = 10.1152/jn.1991.66.6.2014 | pmid = 1667416}} 6. ^{{Cite journal | author = M. V. Jones, P. A. Brooks & N. L. Harrison | title = Enhancement of gamma-aminobutyric acid-activated Cl- currents in cultured rat hippocampal neurones by three volatile anaesthetics | journal = The Journal of Physiology | volume = 449 | pages = 279–293 | year = 1992 | pmid = 1326046| pmc = 1176079 }} 7. ^{{Cite journal | author = M. D. Krasowski & N. L. Harrison | title = The actions of ether, alcohol and alkane general anaesthetics on GABAA and glycine receptors and the effects of TM2 and TM3 mutations | journal = British Journal of Pharmacology | volume = 129 | issue = 4 | pages = 731–743 | year = 2000 | doi = 10.1038/sj.bjp.0703087 | pmid = 10683198| pmc = 1571881 }} 8. ^{{Cite journal | author = L. H. Lin, L. L. Chen, J. A. Zirrolli & R. A. Harris | title = General anesthetics potentiate gamma-aminobutyric acid actions on gamma-aminobutyric acidA receptors expressed by Xenopus oocytes: lack of involvement of intracellular calcium | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 263 | issue = 2 | pages = 569–578 | year = 1992 | pmid = 1331405}} 9. ^1 {{cite book|author1=Elaine K. Perry|author2=Heather Ashton|author3=Allan H. Young|title=Neurochemistry of Consciousness: Neurotransmitters in Mind|url=https://books.google.com/books?id=3o2fCDDoSuUC&pg=PA154|year=2002|publisher=John Benjamins Publishing|isbn=978-1-58811-124-1|pages=154–}} 10. ^1 {{cite book|author1=Charles J. Cote|author2=Jerrold Lerman|author3=Brian J. Anderson|title=A Practice of Anesthesia for Infants and Children: Expert Consult - Online and Print|url=https://books.google.com/books?id=MAXTnQStL0cC&pg=PA499|year=2013|publisher=Elsevier Health Sciences|isbn=978-1-4377-2792-0|pages=499–}} 11. ^{{cite book|author1=Paul Barash|author2=Bruce F. Cullen|author3=Robert K. Stoelting |author4=Michael Cahalan |author5=Christine M. Stock |author6=Rafael Ortega|title=Clinical Anesthesia, 7e: Print + Ebook with Multimedia|url=https://books.google.com/books?id=exygUxEuxnIC&pg=PA116|date=7 February 2013|publisher=Lippincott Williams & Wilkins|isbn=978-1-4698-3027-8|pages=116–}} 12. ^{{cite journal | vauthors = Lin LH, Chen LL, Harris RA | title = Enflurane inhibits NMDA, AMPA, and kainate-induced currents in Xenopus oocytes expressing mouse and human brain mRNA | journal = FASEB J. | volume = 7 | issue = 5 | pages = 479–85 | year = 1993 | pmid = 7681790 | doi = | url = http://www.fasebj.org/cgi/pmidlookup?view=long&pmid=7681790}} 13. ^{{Cite web|title = CDC - NIOSH Pocket Guide to Chemical Hazards - Enflurane|url = https://www.cdc.gov/niosh/npg/npgd0253.html|website = www.cdc.gov|accessdate = 2015-10-01}} | title = Pharmacodynamics | titlestyle = background:#ccccff | list1 ={{GABAA receptor positive modulators}}{{Glycine receptor modulators}}{{Ionotropic glutamate receptor modulators}}{{Nicotinic acetylcholine receptor modulators}}{{Serotonin receptor modulators}} }} 12 : 5-HT3 agonists|AMPA receptor antagonists|NMDA receptor antagonists|Kainate receptor antagonists|General anesthetics|Ethers|Organochlorides|Organofluorides|GABAA receptor positive allosteric modulators|Nicotinic antagonists|Glycine receptor agonists|Fluranes |
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