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Desflurane

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Chemistry

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Also known as: 57041-67-5, Suprane, 2-(difluoromethoxy)-1,1,1,2-tetrafluoroethane, Desflurano [inn-spanish], Difluoromethyl 1,2,2,2-tetrafluoroethyl ether, Desfluranum [inn-latin]

Molecular Formula

C₃H₂F₆O

Molecular Weight

168.04 g/mol

InChI Key

DPYMFVXJLLWWEU-UHFFFAOYSA-N

FDA UNII

CRS35BZ94Q

A fluorinated ether that is used as a volatile anesthetic for maintenance of general anesthesia.

Desflurane is a General Anesthetic. The physiologic effect of desflurane is by means of General Anesthesia.

1 2D Structure

Desflurane

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

2-(difluoromethoxy)-1,1,1,2-tetrafluoroethane

2.1.2 InChI

InChI=1S/C3H2F6O/c4-1(3(7,8)9)10-2(5)6/h1-2H

2.1.3 InChI Key

DPYMFVXJLLWWEU-UHFFFAOYSA-N

2.1.4 Canonical SMILES

C(C(F)(F)F)(OC(F)F)F

2.2 Other Identifiers

2.2.1 UNII

CRS35BZ94Q

2.3 Synonyms

2.3.1 MeSH Synonyms

1. 1,2,2,2-tetrafluoroethyl Difluoromethyl Ether

2. I 653

3. I-653

4. I653

5. Suprane

2.3.2 Depositor-Supplied Synonyms

1. 57041-67-5

2. Suprane

3. 2-(difluoromethoxy)-1,1,1,2-tetrafluoroethane

4. Desflurano [inn-spanish]

5. Difluoromethyl 1,2,2,2-tetrafluoroethyl Ether

6. Desfluranum [inn-latin]

7. I-653

8. 1,2,2,2-tetrafluoroethyl Difluoromethyl Ether

9. (+-)-2-difluoromethyl 1,2,2,2-tetrafluoroethyl Ether

10. Crs35bz94q

11. Chebi:4445

12. 1,1,1,2-tetrafluoro-2-(difluoromethoxy)ethane

13. Desfluranum

14. Desflurano

15. Ethane, 2-(difluoromethoxy)-1,1,1,2-tetrafluoro-, (+-)-

16. (+/-)-2-difluoromethyl 1,2,2,2-tetrafluoroethyl Ether

17. I 653

18. Suprane (tn)

19. Unii-crs35bz94q

20. Desflurane (jan/usp/inn)

21. Desfluran-o

22. Hsdb 8058

23. Desflurane [usan:usp:inn:ban]

24. Ethane, 2-(difluoromethoxy)-1,1,1,2-tetrafluoro-

25. Chf2ochfcf3

26. Desflurane [mi]

27. Desflurane [inn]

28. Desflurane [jan]

29. Desflurane [usan]

30. Desflurane [vandf]

31. Desflurane [mart.]

32. Desflurane [usp-rs]

33. Desflurane [who-dd]

34. Schembl62917

35. Ethane,2-(difluoromethoxy)-1,1,1,2-tetrafluoro-

36. Gtpl7156

37. Chembl1200733

38. Desflurane [orange Book]

39. Desflurane [ep Monograph]

40. Dtxsid80866606

41. Desflurane [usp Monograph]

42. Mfcd00236716

43. Akos006228397

44. Db01189

45. Db-053001

46. Difluoromethyl1,2,2,2-tetrafluoroethylether

47. Ft-0624525

48. C07519

49. D00546

50. Q419383

51. Ethane, 2-(difluoromethoxy)-1,1,1,2-tetrafluoro-, (+/-)-

52. 1351959-69-7

2.4 Create Date

2005-06-24

3 Chemical and Physical Properties

Molecular Formula	C₃H₂F₆O
Molecular Weight	168.04 g/mol
XLogP3	2.6
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	2
Exact Mass	168.00098366 g/mol
Monoisotopic Mass	168.00098366 g/mol
Topological Polar Surface Area	9.2 Å²
Heavy Atom Count	10
Formal Charge	0
Complexity	97.7
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	1
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Information

1 of 2
Drug Name	Suprane
PubMed Health	Desflurane (By breathing)
Drug Classes	Volatile Liquid
Drug Label	SUPRANE (desflurane, USP), a nonflammable liquid administered via vaporizer, is a general inhalation anesthetic. It is ()1,2,2,2-tetrafluoroethyl difluoromethyl ether:Some physical constants are:Molecular weight168.04Specific gravity (at 20C/4C...
Active Ingredient	Desflurane
Dosage Form	Liquid
Route	Inhalation
Strength	99.9%
Market Status	Prescription
Company	Baxter Hlthcare

2 of 2
Drug Name	Suprane
PubMed Health	Desflurane (By breathing)
Drug Classes	Volatile Liquid
Drug Label	SUPRANE (desflurane, USP), a nonflammable liquid administered via vaporizer, is a general inhalation anesthetic. It is ()1,2,2,2-tetrafluoroethyl difluoromethyl ether:Some physical constants are:Molecular weight168.04Specific gravity (at 20C/4C...
Active Ingredient	Desflurane
Dosage Form	Liquid
Route	Inhalation
Strength	99.9%
Market Status	Prescription
Company	Baxter Hlthcare

4.2 Therapeutic Uses

SUPRANE (desflurane, USP) is indicated as an inhalation agent for induction and/or maintenance of anesthesia for inpatient and outpatient surgery in adults. SUPRANE (desflurane, USP) is not recommended for induction of anesthesia in pediatric patients because of a high incidence of moderate to severe upper airway adverse events (see WARNINGS). After induction of anesthesia with agents other than SUPRANE, and tracheal intubation, SUPRANE is indicated for maintenance of anesthesia in infants and children. /Included in US product label/

US Natl Inst Health; DailyMed. Current Medication Information for Suprane (desflurane) liquid (April 2011). Available from, as of July 20, 2012: https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=bf4d8d29-852d-4281-b732-4af0eca019e1

4.3 Drug Warning

Anesthetics, Inhalation

National Library of Medicine's Medical Subject Headings online file (MeSH, 2009) https://www.nlm.nih.gov/cgi/mesh/2012/MB_cgi?mode=&term=desflurane

SUPRANE (desflurane, USP) may produce a dose-dependent increase in cerebrospinal fluid pressure (CSFP) when administered to patients with intracranial space occupying lesions. Desflurane should be administered at 0.8 MAC or less, and in conjunction with a barbiturate induction and hyperventilation (hypocapnia) until cerebral decompression in patients with known or suspected increases in CSFP. Appropriate attention must be paid to maintain cerebral perfusion pressure.

The concentrations of desflurane in milk are probably of no clinical importance 24 hours after anesthesia. Because of rapid washout, desflurane concentrations in milk are predicted to be below those found with other volatile potent anesthetics.

SUPRANE (desflurane, USP) should be administered only by persons trained in the administration of general anesthesia, using a vaporizer specifically designed and designated for use with desflurane. Facilities for maintenance of a patent airway, artificial ventilation, oxygen enrichment, and circulatory resuscitation must be immediately available. Hypotension and respiratory depression increase as anesthesia is deepened.

For more Drug Warnings (Complete) data for Desflurane (22 total), please visit the HSDB record page.

4.4 Drug Indication

Desflurane is indicated for the induction and maintenance of anesthesia in adults, as well as the maintenance of anesthesia in pediatric patients.

FDA Label

5 Pharmacology and Biochemistry

5.1 Pharmacology

Desflurane is a general inhalation anesthetic. It has a short duration of action as it is rapidly cleared. Patients should be counselled regarding the risks of malignant hyperthermia, perioperative hyperkalemia, respiratory adverse reactions in pediatric patients, QTc prolongation, hepatobiliary disorders, pediatric neurotoxicity, and postoperative agitation in children.

5.2 MeSH Pharmacological Classification

Anesthetics, Inhalation

Gases or volatile liquids that vary in the rate at which they induce anesthesia; potency; the degree of circulation, respiratory, or neuromuscular depression they produce; and analgesic effects. Inhalation anesthetics have advantages over intravenous agents in that the depth of anesthesia can be changed rapidly by altering the inhaled concentration. Because of their rapid elimination, any postoperative respiratory depression is of relatively short duration. (From AMA Drug Evaluations Annual, 1994, p173) (See all compounds classified as Anesthetics, Inhalation.)

5.3 FDA Pharmacological Classification

5.3.1 Active Moiety

DESFLURANE

5.3.2 FDA UNII

CRS35BZ94Q

5.3.3 Pharmacological Classes

General Anesthetic [EPC]; General Anesthesia [PE]

5.4 ATC Code

N01AB07

S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355

N - Nervous system

N01 - Anesthetics

N01A - Anesthetics, general

N01AB - Halogenated hydrocarbons

N01AB07 - Desflurane

5.5 Absorption, Distribution and Excretion

Absorption

Data regarding the C_max, T_max, and AUC of desflurane are not readily available.

Route of Elimination

Initially, desflurane is rapidly eliminated from the lungs. A small amount of the metabolite trifluoroacetic acid is eliminated in the urine and only 0.02% of an inhaled dose is recovered as urinary metabolites.

Volume of Distribution

Desflurane has a median volume of distribution of 612 mL/kg.

Clearance

A 26 g dose of desflurane is 90% eliminated from the brain after 33 hours. The metabolite trifluoroacetic acid has a urinary clearance rate of 0.169 0.107 mol/L.

The concentrations of desflurane in milk are probably of no clinical importance 24 hours after anesthesia.

Due to the volatile nature of desflurane in plasma samples, the washin-washout profile of desflurane was used as a surrogate of plasma pharmacokinetics. Eight healthy male volunteers first breathed 70% N2O/30% O2 for 30 minutes and then a mixture of SUPRANE (desflurane, USP) 2.0%, isoflurane 0.4%, and halothane 0.2% for another 30 minutes. During this time, inspired and endtidal concentrations (FI and FA) were measured. The FA/FI (washin) value at 30 minutes for desflurane was 0.91, compared to 1.00 for N2O, 0.74 for isoflurane, and 0.58 for halothane. The washin rates for halothane and isoflurane were similar to literature values. The washin was faster for desflurane than for isoflurane and halothane at all time points. The FA/FAO (washout) value at 5 minutes was 0.12 for desflurane, 0.22 for isoflurane, and 0.25 for halothane. The washout for SUPRANE was more rapid than that for isoflurane and halothane at all elimination time points. By 5 days, the FA/FAO for desflurane is 1/20th of that for halothane or isoflurane.

5.6 Metabolism/Metabolites

Desflurane is minimally defluorinated by CYP2E1, to the extent that serum fluoride levels do not increase above baseline levels.

Renal and hepatic toxicity of the fluorinated ether volatile anesthetics is caused by biotransformation to toxic metabolites. Metabolism also contributes significantly to the elimination pharmacokinetics of some volatile agents. Although innumerable studies have explored anesthetic metabolism in animals, there is little information on human volatile anesthetic metabolism with respect to comparative rates or the identity of the enzymes responsible for defluorination. The first purpose of this investigation was to compare the metabolism of the fluorinated ether anesthetics by human liver microsomes. The second purpose was to test the hypothesis that cytochrome P450 2E1 is the specific P450 isoform responsible for volatile anesthetic defluorination in humans. Microsomes were prepared from human livers. Anesthetic metabolism in microsomal incubations was measured by fluoride production. The strategy for evaluating the role of P450 2E1 in anesthetic defluorination involved three approaches: for a series of 12 human livers, correlation of microsomal defluorination rate with microsomal P450 2E1 content (measured by Western blot analysis), correlation of defluorination rate with microsomal P450 2E1 catalytic activity using marker substrates (para-nitrophenol hydroxylation and chlorzoxazone 6-hydroxylation), and chemical inhibition by P450 isoform-selective inhibitors. The rank order of anesthetic metabolism, assessed by fluoride production at saturating substrate concentrations, was methoxyflurane > sevoflurane > enflurane > isoflurane > desflurane > 0. There was a significant linear correlation of sevoflurane and methoxyflurane defluorination with antigenic P450 2E1 content (r = 0.98 and r = 0.72, respectively), but not with either P450 1A2 or P450 3A3/4. Comparison of anesthetic defluorination with either para-nitrophenol or chlorzoxazone hydroxylation showed a significant correlation for sevoflurane (r = 0.93, r = 0.95) and methoxyflurane (r = 0.78, r = 0.66). Sevoflurane defluorination was also highly correlated with that of enflurane (r = 0.93), which is known to be metabolized by human P450 2E1. Diethyldithiocarbamate, a selective inhibitor of P450 2E1, produced a concentration-dependent inhibition of sevoflurane, methoxyflurane, and isoflurane defluorination. No other isoform-selective inhibitor diminished the defluorination of sevoflurane, whereas methoxyflurane defluorination was inhibited by the selective P450 inhibitors furafylline (P450 1A2), sulfaphenazole (P450 2C9/10), and quinidine (P450 2D6) but to a much lesser extent than by diethyldithiocarbamate. These results demonstrate that cytochrome P450 2E1 is the principal, if not sole human liver microsomal enzyme catalyzing the defluorination of sevoflurane. P450 2E1 is the principal, but not exclusive enzyme responsible for the metabolism of methoxyflurane, which also appears to be catalyzed by P450s 1A2, 2C9/10, and 2D6. The data also suggest that P450 2E1 is responsible for a significant fraction of isoflurane metabolism. Identification of P450 2E1 as the major anesthetic metabolizing enzyme in humans provides a mechanistic understanding of clinical fluorinated ether anesthetic metabolism and toxicity.

PMID:8214760 Kharasch ED, Thummel KE; Anesthesiology 79 (4): 795-807 (1993)

SUPRANE (desflurane, USP) is a volatile liquid inhalation anesthetic minimally biotransformed in the liver in humans.

Biotransformation and hepatotoxicity of desflurane were evaluated in the guinea pig liver slice culture system. Liver slices (250-300 microns) were prepared from 600-650-g male Hartley guinea pigs. The slices were incubated in sealed vials in a Krebs-Henseleit buffer at 37 degrees C under 95% O2. Desflurane was vaporized to produce media concentrations of 0.7-2.3 mM. After incubation (3-24 hr) viability of the slices was determined (K+ content; protein synthesis secretion) along with the biotransformation of desflurane (F-). Isoflurane (2.3 mM) was included in the studies for comparative purposes. Although desflurane caused a mild concentration-related reduction in slice K+ content (1.1-2.2 mM; 20%-40% of control), the effects were less than those produced by 2.3 mM isoflurane (50% of control). High concentrations of desflurane decreased protein synthesis at the first 9 hr of incubation, and isoflurane decreased protein synthesis throughout the incubation period. Neither anesthetic affected protein secretion. The biotransformation of desflurane was minimal with threefold less F- produced from desflurane than isoflurane.

PMID:2035863 Ghantous HN et al; Anesth Analg 72 (6): 796-800 (1991)

The metabolism of desflurane has been assessed both in animals and humans by measuring the appearance of fluoride metabolites (fluoride ion, nonvolatile organic fluoride, trifluoroacetic acid) in blood and urine. Desflurane administered to rats (either pretreated or not pretreated with phenobarbital or ethanol) for 3.2 MAC-hours and to swine for 5.5 MAC-hours produced fluoride ion levels in blood that were almost indistinguishable from values measured in control animals. In contrast, a significant 17% increase in plasma fluoride ion concentration in swine was detected 4 hr after exposure to desflurane. In human studies, desflurane administered to patients (3.1 MAC-hours) and volunteers (7.35 MAC-hours) resulted in postanesthesia serum fluoride in concentrations that did not differ from background fluoride ion concentrations. Similarly, postanesthetic urinary excretion of fluoride ion and organic fluoride in volunteers was comparable to preanesthetic excretion rates. Small but statistically significant levels of trifluoroacetic acid were found in both serum and urine from volunteers after exposure to desflurane. Peak serum concentrations averaging 0.38 +/- 0.17 uM trifluoroacetic acid (mean +/- SD) and peak urinary excretion rates averaging 0.169 +/- 0.107 umol/hr were detected in volunteers 24 hr after desflurane exposure. Although these increases in trifluoroacetic acid after exposure to desflurane were statistically significant, they are approximately 10-fold less than levels seen after exposure to isoflurane. Desflurane strongly resists biodegradation, and only a small amount is metabolized in animals and humans.

PMID:1524235 Koblin DD; Anesth Analg 75 (4 Suppl): S10-6 (1992)

5.7 Biological Half-Life

Desflurane has a terminal elimination half life of 8.16 3.15 minutes.

5.8 Mechanism of Action

The mechanism of inhalational anesthetics is still not fully understood. They can block excitatory ion channels and increase the activity of inhibitory ion channels. The most notable agonism is at the GABA_A channel. Desflurane is also an agonist of glycine receptors, antagonist of glutamate receptors, inducer of potassium voltage gated channels, and inhibits both NADH-ubiquinone oxioreductase chain 1 and calcium transporting ATPases. An older school of thought is the unitary theory of general anesthetic action, suggesting that desflurane affects the lipid bilayer of cells. Studies of other halogenated inhalational anesthetics have shown that the lipid bilayer spreads out more thinly as the anesthetic incorporates into the bilayer. However, the anesthetic does not bind to lipid heads or acyl chains of hydrocarbons in the bilayer. The effect of incorporating into the lipid bilayer is not well described. By incorporating into the lipid bilayer, anesthetics may introduce disorder in the lipids, leading to some indirect effect on ion channels. However, this theory remains controversial.

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