Methoxyflurane

Identification

Generic Name
Methoxyflurane
DrugBank Accession Number
DB01028
Background

An inhalation anesthetic. Currently, methoxyflurane is rarely used for surgical, obstetric, or dental anesthesia. If so employed, it should be administered with nitrous oxide to achieve a relatively light level of anesthesia, and a neuromuscular blocking agent given concurrently to obtain the desired degree of muscular relaxation. (From AMA Drug Evaluations Annual, 1994, p180)

In the US, methoxyflurane is one of the products that have been withdrawn or removed from the market for reasons of safety or effectiveness.1

Type
Small Molecule
Groups
Approved, Investigational, Vet approved, Withdrawn
Structure
Weight
Average: 164.966
Monoisotopic: 163.960726574
Chemical Formula
C3H4Cl2F2O
Synonyms
  • Methoflurane
  • Methoxyfluoran
  • Methoxyfluran
  • Methoxyflurane
  • Methoxyfluranum
  • Methyl 1,1-difluoro-2,2-dichloroethyl ether
  • Metoxiflurano
External IDs
  • DA-759
  • NSC-110432

Pharmacology

Indication

For use in the induction and maintenance of general anesthesia

Reduce drug development failure rates
Build, train, & validate machine-learning models
with evidence-based and structured datasets.
See how
Build, train, & validate predictive machine-learning models with structured datasets.
See how
Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Management ofSevere pain••••••••••••••••••••••••••
Management ofModerate pain••••••••••••••••••••••••••
Contraindications & Blackbox Warnings
Prevent Adverse Drug Events Today
Tap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.
Learn more
Avoid life-threatening adverse drug events with our Clinical API
Learn more
Pharmacodynamics

Methoxyflurane is a general inhalation anesthetic used for induction and maintenance of general anesthesia. It induces muscle relaxation and reduces pains sensitivity by altering tissue excitability. It does so by decreasing the extent of gap junction mediated cell-cell coupling and altering the activity of the channels that underlie the action potential.

Mechanism of action

Methoxyflurane induces a reduction in junctional conductance by decreasing gap junction channel opening times and increasing gap junction channel closing times. Methoxyflurane also activates calcium dependent ATPase in the sarcoplasmic reticulum by increasing the fluidity of the lipid membrane. It also appears to bind the D subunit of ATP synthase and NADH dehydogenase. Methoxyflurane also binds to the GABA receptor, the large conductance Ca2+ activated potassium channel, the glutamate receptor and the glycine receptor.

TargetActionsOrganism
AGamma-aminobutyric acid receptor subunit alpha-1
agonist
Humans
AGlutamate receptor 1
antagonist
Humans
AGlycine receptor subunit alpha-1
agonist
Humans
APotassium voltage-gated channel subfamily A member 1
inducer
Humans
AGABA(A) Receptor
positive allosteric modulator
Humans
UCalcium-transporting ATPase type 2C member 1
inhibitor
Humans
UNADH-ubiquinone oxidoreductase chain 1
unknown
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Hepatic.

Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
Improve decision support & research outcomes
With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!
See the data
Improve decision support & research outcomes with our structured adverse effects data.
See a data sample
Toxicity

LD50=3600 mg/kg (Orally in rats). Symptoms of overexposure include eye irritation, CNS depression, analgesia, anesthesia, seizures, respiratory depression, and liver and kidney damage.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
1,2-BenzodiazepineThe risk or severity of CNS depression can be increased when Methoxyflurane is combined with 1,2-Benzodiazepine.
AbametapirThe serum concentration of Methoxyflurane can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Methoxyflurane can be increased when combined with Abatacept.
AbirateroneThe metabolism of Methoxyflurane can be decreased when combined with Abiraterone.
AbrocitinibThe metabolism of Abrocitinib can be decreased when combined with Methoxyflurane.
Food Interactions
  • Avoid alcohol. Ingesting alcohol may increase the CNS depressant effects of methoxyflurane.

Products

Drug product information from 10+ global regions
Our datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.
Access now
Access drug product information from over 10 global regions.
Access now
International/Other Brands
Penthrane (Abbott Laboratories)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
PenthroxSolution99.9 %Respiratory (inhalation)Endo Ventures Ltd.2018-06-13Not applicableCanada flag
PenthroxKit; Solution99.9 %Respiratory (inhalation)Endo Ventures Ltd.2018-06-12Not applicableCanada flag

Categories

ATC Codes
N02BG09 — Methoxyflurane
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as dialkyl ethers. These are organic compounds containing the dialkyl ether functional group, with the formula ROR', where R and R' are alkyl groups.
Kingdom
Organic compounds
Super Class
Organic oxygen compounds
Class
Organooxygen compounds
Sub Class
Ethers
Direct Parent
Dialkyl ethers
Alternative Parents
Organofluorides / Organochlorides / Hydrocarbon derivatives / Alkyl fluorides / Alkyl chlorides
Substituents
Aliphatic acyclic compound / Alkyl chloride / Alkyl fluoride / Alkyl halide / Dialkyl ether / Hydrocarbon derivative / Organochloride / Organofluoride / Organohalogen compound
Molecular Framework
Aliphatic acyclic compounds
External Descriptors
organofluorine compound, organochlorine compound, ether (CHEBI:6843)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
30905R8O7B
CAS number
76-38-0
InChI Key
RFKMCNOHBTXSMU-UHFFFAOYSA-N
InChI
InChI=1S/C3H4Cl2F2O/c1-8-3(6,7)2(4)5/h2H,1H3
IUPAC Name
2,2-dichloro-1,1-difluoro-1-methoxyethane
SMILES
COC(F)(F)C(Cl)Cl

References

General References
  1. Code of Federal Regulations 216.24: Drug products withdrawn or removed from the market for reasons of safety or effectiveness. [Link]
Human Metabolome Database
HMDB0015162
KEGG Drug
D00544
KEGG Compound
C07517
PubChem Compound
4116
PubChem Substance
46508879
ChemSpider
3973
RxNav
6857
ChEBI
6843
ChEMBL
CHEMBL1341
ZINC
ZINC000000896988
Therapeutic Targets Database
DAP000682
PharmGKB
PA450434
Wikipedia
Methoxyflurane
MSDS
Download (52.9 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedOtherAcute Pain / Trauma1
4CompletedPreventionBenign Prostatic Hypertrophy / Pain1
4CompletedTreatmentAcute Pain3
4CompletedTreatmentAcute Pain / Hypovolaemia / Trauma1
4CompletedTreatmentPain Measurement1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Medical Development Int Ltd.
Dosage Forms
FormRouteStrength
SolutionOral99.90 %
Aerosol, meteredRespiratory (inhalation)99.9 %
Kit; solutionRespiratory (inhalation)99.9 %
SolutionRespiratory (inhalation)99.9 %
InhalantRespiratory (inhalation)99.9 %
SolutionOral; Respiratory (inhalation)999 mg
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)-35 °CPhysProp
boiling point (°C)105 °CPhysProp
water solubility2.83E+004 mg/L (at 37 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.21HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility6.46 mg/mLALOGPS
logP2.01ALOGPS
logP2.31Chemaxon
logS-1.4ALOGPS
pKa (Strongest Basic)-4.5Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count1Chemaxon
Hydrogen Donor Count0Chemaxon
Polar Surface Area9.23 Å2Chemaxon
Rotatable Bond Count2Chemaxon
Refractivity27.98 m3·mol-1Chemaxon
Polarizability11.46 Å3Chemaxon
Number of Rings0Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterNoChemaxon
Veber's RuleYesChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9921
Caco-2 permeable+0.6119
P-glycoprotein substrateNon-substrate0.8535
P-glycoprotein inhibitor INon-inhibitor0.9588
P-glycoprotein inhibitor IINon-inhibitor0.9203
Renal organic cation transporterNon-inhibitor0.9227
CYP450 2C9 substrateNon-substrate0.7959
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.6542
CYP450 1A2 substrateNon-inhibitor0.6508
CYP450 2C9 inhibitorNon-inhibitor0.8587
CYP450 2D6 inhibitorNon-inhibitor0.9407
CYP450 2C19 inhibitorNon-inhibitor0.6081
CYP450 3A4 inhibitorNon-inhibitor0.9753
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8956
Ames testNon AMES toxic0.9132
CarcinogenicityCarcinogens 0.7261
BiodegradationNot ready biodegradable0.9737
Rat acute toxicity1.6296 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9515
hERG inhibition (predictor II)Non-inhibitor0.9016
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (7.12 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-001i-9300000000-2b014e075c584d7d00e8
Mass Spectrum (Electron Ionization)MSsplash10-001i-9100000000-e9387eb71a01da84865e
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-03di-0900000000-4104c395105297b2ec0f
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-001i-9100000000-f5410d6333596bec3893
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-03di-0900000000-c49ca1565d57c9eaf7df
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-01q9-9500000000-f7e49fd52820cf710a91
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-001i-9600000000-b2b1433660cff9693318
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-03di-1900000000-9072c4f4a264dccb8a97
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-104.2173284
predicted
DarkChem Lite v0.1.0
[M-H]-126.78183
predicted
DeepCCS 1.0 (2019)
[M+H]+105.3408284
predicted
DarkChem Lite v0.1.0
[M+H]+129.0424
predicted
DeepCCS 1.0 (2019)
[M+Na]+104.6475284
predicted
DarkChem Lite v0.1.0
[M+Na]+137.81529
predicted
DeepCCS 1.0 (2019)

Targets

Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
Learn more
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRA1
Uniprot ID
P14867
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-1
Molecular Weight
51801.395 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Moody EJ, Suzdak PD, Paul SM, Skolnick P: Modulation of the benzodiazepine/gamma-aminobutyric acid receptor chloride channel complex by inhalation anesthetics. J Neurochem. 1988 Nov;51(5):1386-93. [Article]
  4. Moody EJ, Skolnick P: The imidazobenzodiazepine Ro 15-4513 antagonizes methoxyflurane anesthesia. Life Sci. 1988;43(16):1269-76. [Article]
  5. Krasowski MD, Harrison NL: The actions of ether, alcohol and alkane general anaesthetics on GABAA and glycine receptors and the effects of TM2 and TM3 mutations. Br J Pharmacol. 2000 Feb;129(4):731-43. [Article]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Pdz domain binding
Specific Function
Ionotropic glutamate receptor. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a co...
Gene Name
GRIA1
Uniprot ID
P42261
Uniprot Name
Glutamate receptor 1
Molecular Weight
101505.245 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Martin DC, Plagenhoef M, Abraham J, Dennison RL, Aronstam RS: Volatile anesthetics and glutamate activation of N-methyl-D-aspartate receptors. Biochem Pharmacol. 1995 Mar 15;49(6):809-17. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Transmitter-gated ion channel activity
Specific Function
The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing).
Gene Name
GLRA1
Uniprot ID
P23415
Uniprot Name
Glycine receptor subunit alpha-1
Molecular Weight
52623.35 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Krasowski MD, Harrison NL: The actions of ether, alcohol and alkane general anaesthetics on GABAA and glycine receptors and the effects of TM2 and TM3 mutations. Br J Pharmacol. 2000 Feb;129(4):731-43. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inducer
General Function
Voltage-gated potassium channel activity
Specific Function
Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes, primarily in the brain and the central nervous system, but also in the kidney (PubMed:1990381...
Gene Name
KCNA1
Uniprot ID
Q09470
Uniprot Name
Potassium voltage-gated channel subfamily A member 1
Molecular Weight
56465.01 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Elliott JR, Elliott AA, Harper AA, Winpenny JP: Effects of general anaesthetics on neuronal sodium and potassium channels. Gen Pharmacol. 1992 Nov;23(6):1005-11. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Signal transducer activity
Specific Function
This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of the calcium.
Gene Name
ATP2C1
Uniprot ID
P98194
Uniprot Name
Calcium-transporting ATPase type 2C member 1
Molecular Weight
100576.42 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Lopez MM, Kosk-Kosicka D: How do volatile anesthetics inhibit Ca(2+)-ATPases? J Biol Chem. 1995 Nov 24;270(47):28239-45. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Unknown
General Function
Nadh dehydrogenase (ubiquinone) activity
Specific Function
Core subunit of the mitochondrial membrane respiratory chain NADH dehydrogenase (Complex I) that is believed to belong to the minimal assembly required for catalysis. Complex I functions in the tra...
Gene Name
MT-ND1
Uniprot ID
P03886
Uniprot Name
NADH-ubiquinone oxidoreductase chain 1
Molecular Weight
35660.055 Da
References
  1. Britt BA, Kalow W, Endrenyi L: Effects of halothane and methoxyflurane on rat skeletal muscle mitochondria. Biochem Pharmacol. 1972 Apr 15;21(8):1159-69. doi: 10.1016/0006-2952(72)90110-4. [Article]
  2. Hall GM, Kirtland SJ, Baum H: The inhibition of mitochondrial respiration by inhalational anaesthetic agents. Br J Anaesth. 1973 Oct;45(10):1005-9. doi: 10.1093/bja/45.10.1005. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
Data supporting this enzyme action are limited to an in vitro study.
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Kharasch ED, Thummel KE: Identification of cytochrome P450 2E1 as the predominant enzyme catalyzing human liver microsomal defluorination of sevoflurane, isoflurane, and methoxyflurane. Anesthesiology. 1993 Oct;79(4):795-807. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 Da
References
  1. Liu J, Flockhart PJ, Lu D, Lv W, Lu WJ, Han X, Cushman M, Flockhart DA: Inhibition of cytochrome p450 enzymes by the e- and z-isomers of norendoxifen. Drug Metab Dispos. 2013 Sep;41(9):1715-20. doi: 10.1124/dmd.113.052506. Epub 2013 Jul 3. [Article]
  2. Kharasch ED, Hankins DC, Thummel KE: Human kidney methoxyflurane and sevoflurane metabolism. Intrarenal fluoride production as a possible mechanism of methoxyflurane nephrotoxicity. Anesthesiology. 1995 Mar;82(3):689-99. doi: 10.1097/00000542-199503000-00011. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Kharasch ED, Thummel KE: Identification of cytochrome P450 2E1 as the predominant enzyme catalyzing human liver microsomal defluorination of sevoflurane, isoflurane, and methoxyflurane. Anesthesiology. 1993 Oct;79(4):795-807. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Kharasch ED, Thummel KE: Identification of cytochrome P450 2E1 as the predominant enzyme catalyzing human liver microsomal defluorination of sevoflurane, isoflurane, and methoxyflurane. Anesthesiology. 1993 Oct;79(4):795-807. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Kharasch ED, Hankins DC, Thummel KE: Human kidney methoxyflurane and sevoflurane metabolism. Intrarenal fluoride production as a possible mechanism of methoxyflurane nephrotoxicity. Anesthesiology. 1995 Mar;82(3):689-99. doi: 10.1097/00000542-199503000-00011. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 Da
References
  1. Kharasch ED, Thummel KE: Identification of cytochrome P450 2E1 as the predominant enzyme catalyzing human liver microsomal defluorination of sevoflurane, isoflurane, and methoxyflurane. Anesthesiology. 1993 Oct;79(4):795-807. [Article]
  2. Chang GW, Kam PC: The physiological and pharmacological roles of cytochrome P450 isoenzymes. Anaesthesia. 1999 Jan;54(1):42-50. doi: 10.1046/j.1365-2044.1999.00602.x. [Article]
  3. Flockhart Table of Drug Interactions [Link]

Drug created at June 13, 2005 13:24 / Updated at February 02, 2024 22:47