Peringatan Keamanan

In the event of sevoflurane overdosage (or what may appear to be overdosage) discontinue administration, maintain a patent airway, initiate assisted or controlled ventilation with oxygen, and maintain adequate cardiovascular function.L42340 Patients experiencing an overdose may be at an increased risk of severe adverse effects such as renal injury, respiratory depression, severe bradycardia and cardiac arrest. Fatalities due to sevoflurane abuse have been reported as well.A249900 Symptomatic and supportive measures are recommended. Animal studies have shown that the use of anesthetic agents during periods of rapid brain growth or synaptogenesis results in alterations in synaptic morphology and neurogenesis. In primates, anesthetic regimens of up to 3 hours did not increase neuronal cell loss, but regimens of 5 hours or longer did have a significant effect.L42340 The oral LD50 of sevoflurane is 10.8 g/kg in rats and 18.2 g/kg in mice.L42345

Sevoflurane

DB01236

small molecule approved vet_approved

Deskripsi

Sevoflurane is an ether inhalation anesthetic agent used to induce and maintain general anesthesia.L42340 It is a volatile, non-flammable compound with a low solubility profile and blood/gas partition coefficient.L42340 Sevoflurane was patented in 1972, was approved for clinical use in Japan in 1990, and approved by the FDA in 1996.A249885 Sevoflurane is three times more potent than desflurane, but has lower potency compared to halothane and isoflurane. Unlike other volatile anesthetics, sevoflurane has a pleasant odor and does not irritate the airway. The hemodynamic and respiratory depressive effects of sevoflurane are well tolerated, and most patients receiving this anesthetic agent present little toxicity.A249910 Therefore, it can be used for inhalational induction in adults and children for a wide variety of anesthetic procedures.A249885

Struktur Molekul 2D

Berat 200.0548
Wujud liquid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal elimination half-life of sevoflurane from the peripheral fat compartment is approximately 20 hours.[A249885]
Volume Distribusi Patients given low-flow sevoflurane anesthesia during maxillofacial surgery (n=16) had a peripheral volume of distribution of 1634 ml<sub>vapour</sub>/kg<sub>bw</sub> and a total volume of distribution of 1748 ml<sub>vapour</sub>/kg<sub>bw</sub>.[A226540]
Klirens (Clearance) In patients given low-flow sevoflurane anaesthesia during maxillofacial surgery (n=16), the transport clearance from the central to the peripheral compartment was 13.0 ml<sub>vapour</sub>/kg<sub>bw</sub>?min.[A226540]

Absorpsi

Sevoflurane is rapidly absorbed into circulation through the lungs; however, solubility in the blood is low (blood/gas partition coefficient at 37°C ranges from 0.63 to 0.69).L42340 Therefore, a minimal amount of sevoflurane needs to be dissolved in blood in order to induce anesthesia.A249885

Metabolisme

Sevoflurane is metabolized to hexafluoroisopropanol by cytochrome P450 2E1 in a reaction that promotes the release of inorganic fluoride and carbon dioxide. Hexafluoroisopropanol is rapidly conjugated with glucuronic acid and eliminated in urine. In vivo metabolism studies suggest that approximately 5% of the sevoflurane dose may be metabolized.L42340 In most cases, inorganic fluoride reaches its highest concentration within 2 hours of the end of sevoflurane anesthesia, and returns to baseline levels within 48 hours. Sevoflurane metabolism may be induced by chronic exposure to isoniazid and ethanol, and it has been shown that barbiturates do not affect it.L42340

Rute Eliminasi

The low solubility of sevoflurane facilitates its rapid elimination through the lungs, where 95% to 98% of this anesthetic is eliminated.A249885,L42340 Up to 3.5% of the sevoflurane dose appears in urine as inorganic fluoride, and as much as 50% of fluoride clearance is nonrenal (fluoride taken up into bone).L42340

Interaksi Obat

1480 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Sevoflurane is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Sevoflurane is combined with Levodopa.
Risperidone Sevoflurane may increase the hypotensive activities of Risperidone.
Dasatinib The risk or severity of QTc prolongation can be increased when Sevoflurane is combined with Dasatinib.
Obinutuzumab The risk or severity of adverse effects can be increased when Sevoflurane is combined with Obinutuzumab.
Furosemide Sevoflurane may decrease the antihypertensive activities of Furosemide.
Valsartan Sevoflurane may decrease the antihypertensive activities of Valsartan.
Ramipril Sevoflurane may decrease the antihypertensive activities of Ramipril.
Remikiren Sevoflurane may decrease the antihypertensive activities of Remikiren.
Torasemide Sevoflurane may decrease the antihypertensive activities of Torasemide.
Bethanidine Sevoflurane may decrease the antihypertensive activities of Bethanidine.
Guanadrel Sevoflurane may decrease the antihypertensive activities of Guanadrel.
Olmesartan Sevoflurane may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Sevoflurane may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Sevoflurane may decrease the antihypertensive activities of Nitroprusside.
Atenolol Sevoflurane may decrease the antihypertensive activities of Atenolol.
Minoxidil Sevoflurane may decrease the antihypertensive activities of Minoxidil.
Bendroflumethiazide Sevoflurane may decrease the antihypertensive activities of Bendroflumethiazide.
Prazosin Sevoflurane may decrease the antihypertensive activities of Prazosin.
Fosinopril Sevoflurane may decrease the antihypertensive activities of Fosinopril.
Trandolapril Sevoflurane may decrease the antihypertensive activities of Trandolapril.
Metolazone Sevoflurane may decrease the antihypertensive activities of Metolazone.
Benazepril Sevoflurane may decrease the antihypertensive activities of Benazepril.
Enalapril Sevoflurane may decrease the antihypertensive activities of Enalapril.
Labetalol Sevoflurane may decrease the antihypertensive activities of Labetalol.
Cyclothiazide Sevoflurane may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Sevoflurane may decrease the antihypertensive activities of Candoxatril.
Guanabenz Sevoflurane may decrease the antihypertensive activities of Guanabenz.
Mecamylamine Sevoflurane may decrease the antihypertensive activities of Mecamylamine.
Phentolamine Sevoflurane may decrease the antihypertensive activities of Phentolamine.
Lisinopril Sevoflurane may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Sevoflurane may decrease the antihypertensive activities of Nitroglycerin.
Hydroflumethiazide Sevoflurane may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Sevoflurane may decrease the antihypertensive activities of Cryptenamine.
Perindopril Sevoflurane may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Sevoflurane may decrease the antihypertensive activities of Candesartan cilexetil.
Tolazoline Sevoflurane may decrease the antihypertensive activities of Tolazoline.
Fenoldopam Sevoflurane may decrease the antihypertensive activities of Fenoldopam.
Eprosartan Sevoflurane may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Sevoflurane may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Sevoflurane may decrease the antihypertensive activities of Quinapril.
Omapatrilat Sevoflurane may decrease the antihypertensive activities of Omapatrilat.
Phenoxybenzamine Sevoflurane may decrease the antihypertensive activities of Phenoxybenzamine.
Telmisartan Sevoflurane may decrease the antihypertensive activities of Telmisartan.
Methyldopa Sevoflurane may decrease the antihypertensive activities of Methyldopa.
Trichlormethiazide Sevoflurane may decrease the antihypertensive activities of Trichlormethiazide.
Deserpidine Sevoflurane may decrease the antihypertensive activities of Deserpidine.
Pentolinium Sevoflurane may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Sevoflurane may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Sevoflurane may decrease the antihypertensive activities of Diazoxide.
Terazosin Sevoflurane may decrease the antihypertensive activities of Terazosin.
Rescinnamine Sevoflurane may decrease the antihypertensive activities of Rescinnamine.
Captopril Sevoflurane may decrease the antihypertensive activities of Captopril.
Nadolol Sevoflurane may decrease the antihypertensive activities of Nadolol.
Bevantolol Sevoflurane may decrease the antihypertensive activities of Bevantolol.
Practolol Sevoflurane may decrease the antihypertensive activities of Practolol.
Polythiazide Sevoflurane may decrease the antihypertensive activities of Polythiazide.
Cilazapril Sevoflurane may decrease the antihypertensive activities of Cilazapril.
Saprisartan Sevoflurane may decrease the antihypertensive activities of Saprisartan.
Spirapril Sevoflurane may decrease the antihypertensive activities of Spirapril.
Dexpropranolol Sevoflurane may decrease the antihypertensive activities of Dexpropranolol.
Tienilic acid Sevoflurane may decrease the antihypertensive activities of Tienilic acid.
Debrisoquine Sevoflurane may decrease the antihypertensive activities of Debrisoquine.
Diethylnorspermine Sevoflurane may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Sevoflurane may decrease the antihypertensive activities of Temocapril.
Indoramin Sevoflurane may decrease the antihypertensive activities of Indoramin.
Trimazosin Sevoflurane may decrease the antihypertensive activities of Trimazosin.
Moxonidine Sevoflurane may decrease the antihypertensive activities of Moxonidine.
Rauwolfia serpentina root Sevoflurane may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Sevoflurane may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Sevoflurane may decrease the antihypertensive activities of Angiotensin 1-7.
Rilmenidine Sevoflurane may decrease the antihypertensive activities of Rilmenidine.
Imidapril Sevoflurane may decrease the antihypertensive activities of Imidapril.
BQ-123 Sevoflurane may decrease the antihypertensive activities of BQ-123.
Landiolol Sevoflurane may decrease the antihypertensive activities of Landiolol.
Dihydralazine Sevoflurane may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Sevoflurane may decrease the antihypertensive activities of Zofenopril.
Guanoxan Sevoflurane may decrease the antihypertensive activities of Guanoxan.
Delapril Sevoflurane may decrease the antihypertensive activities of Delapril.
Vincamine Sevoflurane may decrease the antihypertensive activities of Vincamine.
Guanoxabenz Sevoflurane may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Sevoflurane may decrease the antihypertensive activities of Tolonidine.
Endralazine Sevoflurane may decrease the antihypertensive activities of Endralazine.
Esatenolol Sevoflurane may decrease the antihypertensive activities of Esatenolol.
Cadralazine Sevoflurane may decrease the antihypertensive activities of Cadralazine.
Cloranolol Sevoflurane may decrease the antihypertensive activities of Cloranolol.
Cyclopenthiazide Sevoflurane may decrease the antihypertensive activities of Cyclopenthiazide.
Bietaserpine Sevoflurane may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Sevoflurane may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Sevoflurane may decrease the antihypertensive activities of Methoserpidine.
Epanolol Sevoflurane may decrease the antihypertensive activities of Epanolol.
Guanoclor Sevoflurane may decrease the antihypertensive activities of Guanoclor.
Muzolimine Sevoflurane may decrease the antihypertensive activities of Muzolimine.
Xipamide Sevoflurane may decrease the antihypertensive activities of Xipamide.
Candesartan Sevoflurane may decrease the antihypertensive activities of Candesartan.
Benazeprilat Sevoflurane may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Sevoflurane may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Sevoflurane may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Sevoflurane may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Sevoflurane may decrease the antihypertensive activities of Quinaprilat.

Target Protein

GABA(A) Receptor GABRA1
Glycine receptor subunit alpha-1 GLRA1
Glutamate receptor 1 GRIA1
Calcium transporting ATPases ATP2C1
Mitochondrial potassium channel CCDC51
NADH-ubiquinone oxidoreductase chain 1 MT-ND1

Referensi & Sumber

Synthesis reference: Terrell, RC., et al. (1999) Method for the preparation of sevoflurane (U.S. Patent US 5,969,193). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/76/64/1d/83a9d1ed707307/US5969193.pdf
Artikel (PubMed)
  • PMID: 9989340
    Behne M, Wilke HJ, Harder S: Clinical pharmacokinetics of sevoflurane. Clin Pharmacokinet. 1999 Jan;36(1):13-26. doi: 10.2165/00003088-199936010-00002.
  • PMID: 10823093
    Wissing H, Kuhn I, Rietbrock S, Fuhr U: Pharmacokinetics of inhaled anaesthetics in a clinical setting: comparison of desflurane, isoflurane and sevoflurane. Br J Anaesth. 2000 Apr;84(4):443-9. doi: 10.1093/oxfordjournals.bja.a013467.
  • PMID: 12761368
    Campagna JA, Miller KW, Forman SA: Mechanisms of actions of inhaled anesthetics. N Engl J Med. 2003 May 22;348(21):2110-24. doi: 10.1056/NEJMra021261.
  • PMID: 28800884
    Kojima A, Matsuura H: Ionic mechanisms of the action of anaesthetics on sinoatrial node automaticity. Eur J Pharmacol. 2017 Nov 5;814:63-72. doi: 10.1016/j.ejphar.2017.08.006. Epub 2017 Aug 9.
  • PMID: 17988469
    Levine B, Cox D, Jufer-Phipps RA, Li L, Jacobs A, Fowler D: A fatality from sevoflurane abuse. J Anal Toxicol. 2007 Oct;31(8):534-6. doi: 10.1093/jat/31.8.534.
  • PMID: 14980913
    Masaki E, Kawamura M, Kato F: Attenuation of gap-junction-mediated signaling facilitated anesthetic effect of sevoflurane in the central nervous system of rats. Anesth Analg. 2004 Mar;98(3):647-52, table of contents. doi: 10.1213/01.ane.0000103259.72635.72.
  • PMID: 19351234
    Michel F, Constantin JM: Sevoflurane inside and outside the operating room. Expert Opin Pharmacother. 2009 Apr;10(5):861-73. doi: 10.1517/14656560902798752.

Contoh Produk & Brand

Produk: 20 • International brands: 2
Produk
  • Sevoflurane
    Liquid • 250 mL/250mL • Respiratory (inhalation) • US • Generic • Approved
  • Sevoflurane
    Liquid • 1 mL/1mL • Respiratory (inhalation) • US • Generic • Approved
  • Sevoflurane
    Liquid • 1 mL/1mL • Respiratory (inhalation) • US • Generic • Approved
  • Sevoflurane
    Liquid • 250 mL/250mL • Respiratory (inhalation) • US • Generic • Approved
  • Sevoflurane
    Liquid • 250 mL/250mL • Respiratory (inhalation) • US • Generic • Approved
  • Sevoflurane
    Liquid • 1 mL/1mL • Respiratory (inhalation) • US • Generic • Approved
  • Sevoflurane
    Liquid • 99.97 % • Respiratory (inhalation) • Canada • Approved
  • Sevoflurane
    Liquid • 99.97 % • Respiratory (inhalation) • Canada • Approved
Menampilkan 8 dari 20 produk.
International Brands
  • Sevorane — AbbVie
  • Ultane — AbbVie

Sekuens Gen/Protein (FASTA)

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