Peringatan Keamanan

The LD50 of enflurane in rats is 14000 ppm/3 hour(s) when inhaled.L13871
There is limited information in the literature about enflurane overdose. Hepatotoxicity, cardiotoxicity, nephrotoxicity, and neurotoxicity are expected.L13646 One report in the literature of an enflurane overdose describes an accidental fatal overdose in a 21-year-old male.A203174 About 72 hours after death, high amounts of enflurane were found in the brain, blood, and subcutaneous fat. Gas chromatographic studies revealed enflurane concentrations of 350 mg/l-1 in the brain, 130 mg/l-1 in the blood, and 100 mg/l-1 in the subcutaneous fat.A203174

In the event of an enflurane overdose, immediately stop the administration of enflurane, establish a patent airway, and administer pure oxygen by assisted or controlled ventilation.L13646

Enflurane

DB00228

small molecule approved investigational vet_approved

Deskripsi

Enflurane is a halogenated inhalational anesthetic initially approved by the FDA in 1972. Since this date, it has been withdrawn from the US market.L13646,L13649 Unlike its other inhalational anesthetic counterparts including isoflurane and halothane, enflurane is known to induce seizure activity. In addition, it is known to cause increased cardio depressant effects when compared to other inhaled anesthetics.A202022

Struktur Molekul 2D

Berat 184.492
Wujud liquid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi Enflurane distributes to the brain, blood, and subcutaneous fat.[A203174]
Klirens (Clearance) -

Absorpsi

Enflurane is rapidly absorbed into the circulation through the lungs.A203216,L13646 The minimum alveolar concentration is oxygen is 1.68%.A202022

Metabolisme

Enflurane is metabolized by the CYP2E1 enzyme in the liver to produce inorganic fluoride ions, the major metabolite of enflurane metabolism.A202118 One reference indicates that enflurane is only 2-5% eliminated after oxidative metabolism in the liver, however more recent evidence suggests that about 9% is eliminated via hepatic oxidation.A202022

Rute Eliminasi

Metabolism accounts for 5-9% of enflurane elimination, sometimes causing nephrotoxicity. Excretion through the skin is believed to be minimal.A202022

Interaksi Obat

780 Data
Buprenorphine Enflurane may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Enflurane.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Enflurane.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Enflurane.
Hydrocodone Enflurane may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Enflurane.
Magnesium sulfate The therapeutic efficacy of Enflurane can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Enflurane may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Enflurane may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Enflurane.
Mirtazapine Enflurane may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Enflurane.
Orphenadrine Enflurane may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Enflurane may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Enflurane.
Pramipexole Enflurane may increase the sedative activities of Pramipexole.
Ropinirole Enflurane may increase the sedative activities of Ropinirole.
Rotigotine Enflurane may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Enflurane.
Sodium oxybate Enflurane may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Enflurane may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Enflurane.
Thalidomide Enflurane may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Enflurane may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Enflurane.
Dopamine Enflurane may increase the arrhythmogenic activities of Dopamine.
Ephedra sinica root Enflurane may increase the arrhythmogenic activities of Ephedra sinica root.
Formoterol Enflurane may increase the arrhythmogenic activities of Formoterol.
Methylphenidate Methylphenidate may increase the hypertensive activities of Enflurane.
Dexmethylphenidate Dexmethylphenidate may increase the hypertensive activities of Enflurane.
Norepinephrine Enflurane may increase the arrhythmogenic activities of Norepinephrine.
Isoprenaline Enflurane may increase the arrhythmogenic activities of Isoprenaline.
Ethanol Enflurane may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Enflurane may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Enflurane.
Fluvoxamine The risk or severity of adverse effects can be increased when Enflurane is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Enflurane is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Enflurane is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Enflurane is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Enflurane is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Enflurane is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Enflurane is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Enflurane is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Enflurane is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Enflurane is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Enflurane is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Enflurane is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Enflurane is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Enflurane is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Enflurane is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Enflurane is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Enflurane is combined with Alaproclate.
Ephedrine Ephedrine may increase the arrhythmogenic activities of Enflurane.
Epinephrine Enflurane may increase the arrhythmogenic activities of Epinephrine.
Amitriptyline The risk or severity of CNS depression can be increased when Enflurane is combined with Amitriptyline.
Cyproheptadine The risk or severity of CNS depression can be increased when Enflurane is combined with Cyproheptadine.
Imipramine The risk or severity of CNS depression can be increased when Enflurane is combined with Imipramine.
Nortriptyline The risk or severity of CNS depression can be increased when Enflurane is combined with Nortriptyline.
Amoxapine The risk or severity of CNS depression can be increased when Enflurane is combined with Amoxapine.
Propiomazine The risk or severity of CNS depression can be increased when Enflurane is combined with Propiomazine.
Maprotiline The risk or severity of CNS depression can be increased when Enflurane is combined with Maprotiline.
Doxepin The risk or severity of CNS depression can be increased when Enflurane is combined with Doxepin.
Desipramine The risk or severity of CNS depression can be increased when Enflurane is combined with Desipramine.
Pizotifen The risk or severity of CNS depression can be increased when Enflurane is combined with Pizotifen.
Dosulepin The risk or severity of CNS depression can be increased when Enflurane is combined with Dosulepin.
Zopiclone The risk or severity of adverse effects can be increased when Enflurane is combined with Zopiclone.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Enflurane.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Enflurane.
Tryptophan The risk or severity of CNS depression can be increased when Tryptophan is combined with Enflurane.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Enflurane.
Lorazepam The risk or severity of CNS depression can be increased when Lorazepam is combined with Enflurane.
Ethchlorvynol The risk or severity of CNS depression can be increased when Ethchlorvynol is combined with Enflurane.
Succinylcholine The risk or severity of CNS depression can be increased when Succinylcholine is combined with Enflurane.
Reserpine The risk or severity of CNS depression can be increased when Reserpine is combined with Enflurane.
Eletriptan The risk or severity of CNS depression can be increased when Eletriptan is combined with Enflurane.
Temazepam The risk or severity of CNS depression can be increased when Enflurane is combined with Temazepam.
Reboxetine The risk or severity of CNS depression can be increased when Enflurane is combined with Reboxetine.
Butabarbital The risk or severity of CNS depression can be increased when Enflurane is combined with Butabarbital.
Butalbital The risk or severity of CNS depression can be increased when Enflurane is combined with Butalbital.
Methysergide The risk or severity of CNS depression can be increased when Enflurane is combined with Methysergide.
Cabergoline The risk or severity of CNS depression can be increased when Enflurane is combined with Cabergoline.
Phenytoin The risk or severity of CNS depression can be increased when Enflurane is combined with Phenytoin.
Topiramate The risk or severity of CNS depression can be increased when Enflurane is combined with Topiramate.
Clemastine The risk or severity of CNS depression can be increased when Enflurane is combined with Clemastine.
Venlafaxine The risk or severity of CNS depression can be increased when Enflurane is combined with Venlafaxine.
Etomidate The risk or severity of CNS depression can be increased when Enflurane is combined with Etomidate.
Morphine The risk or severity of CNS depression can be increased when Enflurane is combined with Morphine.
Talbutal The risk or severity of CNS depression can be increased when Enflurane is combined with Talbutal.
Pentobarbital The risk or severity of CNS depression can be increased when Enflurane is combined with Pentobarbital.
Valproic acid The risk or severity of CNS depression can be increased when Enflurane is combined with Valproic acid.
Zolmitriptan The risk or severity of CNS depression can be increased when Enflurane is combined with Zolmitriptan.
Codeine The risk or severity of CNS depression can be increased when Enflurane is combined with Codeine.
Dihydroergotamine The risk or severity of CNS depression can be increased when Enflurane is combined with Dihydroergotamine.
Tolcapone The risk or severity of CNS depression can be increased when Enflurane is combined with Tolcapone.
Hydromorphone The risk or severity of CNS depression can be increased when Enflurane is combined with Hydromorphone.
Olanzapine The risk or severity of CNS depression can be increased when Enflurane is combined with Olanzapine.
Cetirizine The risk or severity of CNS depression can be increased when Enflurane is combined with Cetirizine.
Protriptyline The risk or severity of CNS depression can be increased when Enflurane is combined with Protriptyline.
Trimethadione The risk or severity of CNS depression can be increased when Enflurane is combined with Trimethadione.
Clobazam The risk or severity of sedation, somnolence, and CNS depression can be increased when Clobazam is combined with Enflurane.

Target Protein

GABA(A) Receptor GABRA1
Voltage-dependent calcium channel CACNG1
Glycine receptor subunit alpha-1 GLRA1
Voltage-gated Potassium Channels KCND1
Calcium-transporting ATPase type 2C member 1 ATP2C1
Glutamate (NMDA) receptor GRIN1
Sarcoplasmic/endoplasmic reticulum calcium ATPase 1 ATP2A1

Referensi & Sumber

Synthesis reference: Terrell, R.C.; U.S. Patents 3,469,011; September 23,1969 and 3,527,813; September 8, 1970; both assigned to Air Reduction Company, Incorporated.
Artikel (PubMed)
  • PMID: 2657350
    Quail AW: Modern inhalational anaesthetic agents. A review of halothane, isoflurane and enflurane. Med J Aust. 1989 Jan 16;150(2):95-102.
  • PMID: 16973644
    Grasshoff C, Antkowiak B: Effects of isoflurane and enflurane on GABAA and glycine receptors contribute equally to depressant actions on spinal ventral horn neurones in rats. Br J Anaesth. 2006 Nov;97(5):687-94. doi: 10.1093/bja/ael239. Epub 2006 Sep 13.
  • PMID: 31643793
    Authors unspecified: Enflurane .
  • PMID: 6869859
    Berger JM, Stirt JA, Sullivan SF: Enflurane, halothane, and aminophylline--uptake and pharmacokinetics. Anesth Analg. 1983 Aug;62(8):733-7.
  • PMID: 3555939
    Dale O, Brown BR Jr: Clinical pharmacokinetics of the inhalational anaesthetics. Clin Pharmacokinet. 1987 Mar;12(3):145-67. doi: 10.2165/00003088-198712030-00001.
  • PMID: 19762755
    Sleigh JW, Vizuete JA, Voss L, Steyn-Ross A, Steyn-Ross M, Marcuccilli CJ, Hudetz AG: The electrocortical effects of enflurane: experiment and theory. Anesth Analg. 2009 Oct;109(4):1253-62. doi: 10.1213/ANE.0b013e3181add06b.
  • PMID: 8053596
    Connelly TJ, Coronado R: Activation of the Ca2+ release channel of cardiac sarcoplasmic reticulum by volatile anesthetics. Anesthesiology. 1994 Aug;81(2):459-69. doi: 10.1097/00000542-199408000-00025.
  • PMID: 1850580
    Eskinder H, Rusch NJ, Supan FD, Kampine JP, Bosnjak ZJ: The effects of volatile anesthetics on L- and T-type calcium channel currents in canine cardiac Purkinje cells. Anesthesiology. 1991 May;74(5):919-26. doi: 10.1097/00000542-199105000-00018.
Menampilkan 8 dari 15 artikel.
Textbook
  • John D. Current M.D. (n/A). Pharmacology for Anesthetists: anesthesia and adjuvants. N/A.

Contoh Produk & Brand

Produk: 5 • International brands: 4
Produk
  • Enflurane
    Liquid • 1 mL/1mL • Respiratory (inhalation) • US • Generic • Approved
  • Enflurane
    Liquid • 99.9 % • Respiratory (inhalation) • Canada • Approved
  • Ethrane
    Liquid • 125 mL/125mL • Respiratory (inhalation) • US • Approved
  • Ethrane Liq Inh
    Liquid • 100 % • Respiratory (inhalation) • Canada • Approved
  • Ethrane Liquid Inh
    Liquid • 100 % • Respiratory (inhalation) • Canada • Approved
International Brands
  • Alyrane — Baxter
  • Compound 347 — Dexa Medica
  • Endurane — Singapore Pharmawealth Lifesciences
  • Enfluran — Cristália

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