Peringatan Keamanan

Patients experiencing a desflurane overdose may experience deepening anesthesia, cardiac or respiratory depression.L30285 In the event of an overdose, patients may require symptomatic and supportive treatment to maintain airway, breathing, and circulation.L30285 Discontinue desflurane.L30285

Desflurane

DB01189

small molecule approved

Deskripsi

Desflurane, or I-653, a a volatile anesthetic that is more rapidly cleared and less metabolized than previous inhaled anesthetics such as methoxyflurane, sevoflurane, enflurane, or isoflurane.A226390,A39015,A226893. It was developed in the late 1980s out of a need for a more rapidly acting and rapidly cleared inhaled anesthetic.A226883,A226888

Desflurane was granted FDA approval on 18 September 1992.L30285

Struktur Molekul 2D

Berat 168.0378
Wujud liquid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Desflurane has a terminal elimination half life of 8.16 ± 3.15 minutes.[A226525]
Volume Distribusi Desflurane has a median volume of distribution of 612 mL/kg.[A226540]
Klirens (Clearance) A 26 g dose of desflurane is 90% eliminated from the brain after 33 hours.[A226380] The metabolite trifluoroacetic acid has a urinary clearance rate of 0.169 ± 0.107 µmol/L.[A226390]

Absorpsi

Data regarding the Cmax, Tmax, and AUC of desflurane are not readily available.L30285

Metabolisme

Desflurane is minimally defluorinated by CYP2E1,A39015 to the extent that serum fluoride levels do not increase above baseline levels.A226390

Rute Eliminasi

Initially, desflurane is rapidly eliminated from the lungs.A226530 A small amount of the metabolite trifluoroacetic acid is eliminated in the urineA226385 and only 0.02% of an inhaled dose is recovered as urinary metabolites.L30285

Interaksi Obat

1334 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Desflurane is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Desflurane is combined with Levodopa.
Risperidone Desflurane may increase the hypotensive activities of Risperidone.
Furosemide Desflurane may decrease the antihypertensive activities of Furosemide.
Valsartan Desflurane may decrease the antihypertensive activities of Valsartan.
Ramipril Desflurane may decrease the antihypertensive activities of Ramipril.
Remikiren Desflurane may decrease the antihypertensive activities of Remikiren.
Torasemide Desflurane may decrease the antihypertensive activities of Torasemide.
Bethanidine Desflurane may decrease the antihypertensive activities of Bethanidine.
Guanadrel Desflurane may decrease the antihypertensive activities of Guanadrel.
Metoprolol Desflurane may decrease the antihypertensive activities of Metoprolol.
Olmesartan Desflurane may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Desflurane may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Desflurane may decrease the antihypertensive activities of Nitroprusside.
Atenolol Desflurane may decrease the antihypertensive activities of Atenolol.
Minoxidil Desflurane may decrease the antihypertensive activities of Minoxidil.
Nisoldipine Desflurane may decrease the antihypertensive activities of Nisoldipine.
Bendroflumethiazide Desflurane may decrease the antihypertensive activities of Bendroflumethiazide.
Prazosin Desflurane may decrease the antihypertensive activities of Prazosin.
Fosinopril Desflurane may decrease the antihypertensive activities of Fosinopril.
Trandolapril Desflurane may decrease the antihypertensive activities of Trandolapril.
Metolazone Desflurane may decrease the antihypertensive activities of Metolazone.
Lercanidipine Desflurane may decrease the antihypertensive activities of Lercanidipine.
Benazepril Desflurane may decrease the antihypertensive activities of Benazepril.
Bosentan Desflurane may decrease the antihypertensive activities of Bosentan.
Enalapril Desflurane may decrease the antihypertensive activities of Enalapril.
Doxazosin Desflurane may decrease the antihypertensive activities of Doxazosin.
Labetalol Desflurane may decrease the antihypertensive activities of Labetalol.
Cyclothiazide Desflurane may decrease the antihypertensive activities of Cyclothiazide.
Bisoprolol Desflurane may decrease the antihypertensive activities of Bisoprolol.
Candoxatril Desflurane may decrease the antihypertensive activities of Candoxatril.
Guanabenz Desflurane may decrease the antihypertensive activities of Guanabenz.
Mecamylamine Desflurane may decrease the antihypertensive activities of Mecamylamine.
Phentolamine Desflurane may decrease the antihypertensive activities of Phentolamine.
Eplerenone Desflurane may decrease the antihypertensive activities of Eplerenone.
Lisinopril Desflurane may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Desflurane may decrease the antihypertensive activities of Nitroglycerin.
Hydroflumethiazide Desflurane may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Desflurane may decrease the antihypertensive activities of Cryptenamine.
Perindopril Desflurane may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Desflurane may decrease the antihypertensive activities of Candesartan cilexetil.
Tolazoline Desflurane may decrease the antihypertensive activities of Tolazoline.
Fenoldopam Desflurane may decrease the antihypertensive activities of Fenoldopam.
Tadalafil Desflurane may decrease the antihypertensive activities of Tadalafil.
Eprosartan Desflurane may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Desflurane may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Desflurane may decrease the antihypertensive activities of Quinapril.
Omapatrilat Desflurane may decrease the antihypertensive activities of Omapatrilat.
Phenoxybenzamine Desflurane may decrease the antihypertensive activities of Phenoxybenzamine.
Telmisartan Desflurane may decrease the antihypertensive activities of Telmisartan.
Methyldopa Desflurane may decrease the antihypertensive activities of Methyldopa.
Trichlormethiazide Desflurane may decrease the antihypertensive activities of Trichlormethiazide.
Irbesartan Desflurane may decrease the antihypertensive activities of Irbesartan.
Deserpidine Desflurane may decrease the antihypertensive activities of Deserpidine.
Pentolinium Desflurane may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Desflurane may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Desflurane may decrease the antihypertensive activities of Diazoxide.
Carvedilol Desflurane may decrease the antihypertensive activities of Carvedilol.
Terazosin Desflurane may decrease the antihypertensive activities of Terazosin.
Guanethidine Desflurane may decrease the antihypertensive activities of Guanethidine.
Rescinnamine Desflurane may decrease the antihypertensive activities of Rescinnamine.
Captopril Desflurane may decrease the antihypertensive activities of Captopril.
Nadolol Desflurane may decrease the antihypertensive activities of Nadolol.
Epoprostenol Desflurane may decrease the antihypertensive activities of Epoprostenol.
Hydralazine Desflurane may decrease the antihypertensive activities of Hydralazine.
Bevantolol Desflurane may decrease the antihypertensive activities of Bevantolol.
Practolol Desflurane may decrease the antihypertensive activities of Practolol.
Polythiazide Desflurane may decrease the antihypertensive activities of Polythiazide.
Cilazapril Desflurane may decrease the antihypertensive activities of Cilazapril.
Saprisartan Desflurane may decrease the antihypertensive activities of Saprisartan.
Spirapril Desflurane may decrease the antihypertensive activities of Spirapril.
Dexpropranolol Desflurane may decrease the antihypertensive activities of Dexpropranolol.
Tienilic acid Desflurane may decrease the antihypertensive activities of Tienilic acid.
Debrisoquine Desflurane may decrease the antihypertensive activities of Debrisoquine.
Nebivolol Desflurane may decrease the antihypertensive activities of Nebivolol.
Sitaxentan Desflurane may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Desflurane may decrease the antihypertensive activities of Ambrisentan.
Diethylnorspermine Desflurane may decrease the antihypertensive activities of Diethylnorspermine.
Pinacidil Desflurane may decrease the antihypertensive activities of Pinacidil.
Temocapril Desflurane may decrease the antihypertensive activities of Temocapril.
Riociguat Desflurane may decrease the antihypertensive activities of Riociguat.
Macitentan Desflurane may decrease the antihypertensive activities of Macitentan.
Indoramin Desflurane may decrease the antihypertensive activities of Indoramin.
Aliskiren Desflurane may decrease the antihypertensive activities of Aliskiren.
Trimazosin Desflurane may decrease the antihypertensive activities of Trimazosin.
Manidipine Desflurane may decrease the antihypertensive activities of Manidipine.
Moxonidine Desflurane may decrease the antihypertensive activities of Moxonidine.
Rauwolfia serpentina root Desflurane may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Desflurane may decrease the antihypertensive activities of Enalaprilat.
Selexipag Desflurane may decrease the antihypertensive activities of Selexipag.
Angiotensin 1-7 Desflurane may decrease the antihypertensive activities of Angiotensin 1-7.
Rilmenidine Desflurane may decrease the antihypertensive activities of Rilmenidine.
Imidapril Desflurane may decrease the antihypertensive activities of Imidapril.
BQ-123 Desflurane may decrease the antihypertensive activities of BQ-123.
Naftopidil Desflurane may decrease the antihypertensive activities of Naftopidil.
Landiolol Desflurane may decrease the antihypertensive activities of Landiolol.
Dihydralazine Desflurane may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Desflurane may decrease the antihypertensive activities of Zofenopril.
Guanoxan Desflurane may decrease the antihypertensive activities of Guanoxan.
Delapril Desflurane may decrease the antihypertensive activities of Delapril.

Target Protein

GABA(A) Receptor GABRA1
Glycine receptor subunit alpha-1 GLRA1
Glutamate receptor 1 GRIA1
Potassium voltage-gated channel subfamily A member 1 KCNA1
NADH-ubiquinone oxidoreductase chain 1 MT-ND1
Calcium transporting ATPases ATP2C1
ATP synthase subunit delta, mitochondrial ATP5F1D

Referensi & Sumber

Synthesis reference: Leonid A. Rozov, Chialang Huang, Gerald G. Vernice, "Synthesis of desflurane." U.S. Patent US5205914, issued June, 1991.
Artikel (PubMed)
  • PMID: 20233751
    Lockwood G: Theoretical context-sensitive elimination times for inhalation anaesthetics. Br J Anaesth. 2010 May;104(5):648-55. doi: 10.1093/bja/aeq051. Epub 2010 Mar 16.
  • PMID: 8214760
    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.
  • PMID: 1524235
    Koblin DD: Characteristics and implications of desflurane metabolism and toxicity. Anesth Analg. 1992 Oct;75(4 Suppl):S10-6.
  • PMID: 1854033
    Sutton TS, Koblin DD, Gruenke LD, Weiskopf RB, Rampil IJ, Waskell L, Eger EI 2nd: Fluoride metabolites after prolonged exposure of volunteers and patients to desflurane. Anesth Analg. 1991 Aug;73(2):180-5. doi: 10.1213/00000539-199108000-00011.
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    Khan J, Liu M: Desflurane .
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    Tu K, Tarek M, Klein ML, Scharf D: Effects of anesthetics on the structure of a phospholipid bilayer: molecular dynamics investigation of halothane in the hydrated liquid crystal phase of dipalmitoylphosphatidylcholine. Biophys J. 1998 Nov;75(5):2123-34. doi: 10.1016/S0006-3495(98)77655-6.
  • PMID: 17494361
    Krasowski MD: Contradicting a unitary theory of general anesthetic action: a history of three compounds from 1901 to 2001. Bull Anesth Hist. 2003 Jul;21(3):1, 4-8, 21 passim. doi: 10.1016/s1522-8649(03)50031-2.
  • PMID: 28265069
    Herold KF, Sanford RL, Lee W, Andersen OS, Hemmings HC Jr: Clinical concentrations of chemically diverse general anesthetics minimally affect lipid bilayer properties. Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3109-3114. doi: 10.1073/pnas.1611717114. Epub 2017 Mar 6.
Menampilkan 8 dari 21 artikel.

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