Peringatan Keamanan

When orally administered, oxetacaine presents a good tolerance. However, following intravenous injection, oxetacaine toxicity is high and it is presented as a depression in myocardial contractility and impaired conduction.A33107

Oxetacaine

DB12532

small molecule approved investigational

Deskripsi

Oxetacaine, also called oxethazaince, is a potent surface analgesic with the molecular formula N, N-bis-(N-methyl-N-phenyl-t-butyl-acetamide)-beta-hydroxyethylamine that conserves its unionized form at low pH levels. Its actions have shown to relieve dysphagia, relieve pain due to reflux, chronic gastritis, and duodenal ulcer.A33104 Oxetacaine is approved by Health Canada since 1995 for its use as an antacid combination in over-the-counter preparations.L1113 It is also in the list of approved derivatives of herbal products by the EMA.L2816

Struktur Molekul 2D

Berat 467.654
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Oxetacaine presents a very short half-life of approximately one hour.[T213]
Volume Distribusi This pharmacokinetic property has not been studied.
Klirens (Clearance) This pharmacokinetic property has not been studied.

Absorpsi

A peak plasma concentration of oxetacaine of approximately 20 ng/ml is attained about one hour after oral administration.T213 LEss than 1/3 of the administered dose is absorbed as it undergoes extensive metabolism.T214

Metabolisme

Oxetacaine is rapidly and extensively metabolized hepatically. After metabolism, there is a formation of primary metabolites such as beta-hydroxy-mephentermine and beta-hydroxy-phentermine. The major metabolites are found in the plasma in insignificant amounts.T213

Rute Eliminasi

Less than 0.1% of the amdinistered dose is recovered in urine within 24 hours in the form of unchanged oxetacaine or its metabolites.T213

Interaksi Obat

1074 Data
Eliglustat The metabolism of Eliglustat can be decreased when combined with Oxetacaine.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Oxetacaine.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Oxetacaine.
Colchicine The metabolism of Colchicine can be decreased when combined with Oxetacaine.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Oxetacaine.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Oxetacaine.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Oxetacaine.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Oxetacaine.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Oxetacaine.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Oxetacaine.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Oxetacaine.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Oxetacaine.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Oxetacaine.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Oxetacaine.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Oxetacaine.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Oxetacaine.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Oxetacaine.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Oxetacaine.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Oxetacaine.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Oxetacaine.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Oxetacaine.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Oxetacaine.
Technetium Tc-99m tilmanocept Oxetacaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Aripiprazole The metabolism of Aripiprazole can be decreased when combined with Oxetacaine.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be decreased when combined with Oxetacaine.
Prucalopride The metabolism of Prucalopride can be decreased when combined with Oxetacaine.
Voxelotor The serum concentration of Voxelotor can be increased when it is combined with Oxetacaine.
Levamlodipine The serum concentration of Levamlodipine can be increased when it is combined with Oxetacaine.
Tramadol The metabolism of Tramadol can be decreased when combined with Oxetacaine.
Haloperidol The serum concentration of Haloperidol can be increased when it is combined with Oxetacaine.
Finerenone The serum concentration of Finerenone can be increased when it is combined with Oxetacaine.
Roflumilast The serum concentration of Roflumilast can be increased when it is combined with Oxetacaine.
Enzalutamide The serum concentration of Enzalutamide can be increased when it is combined with Oxetacaine.
Chloroprocaine The risk or severity of adverse effects can be increased when Oxetacaine is combined with Chloroprocaine.
Lidocaine The risk or severity of methemoglobinemia can be increased when Lidocaine is combined with Oxetacaine.
Ropivacaine The risk or severity of methemoglobinemia can be increased when Ropivacaine is combined with Oxetacaine.
Bupivacaine The risk or severity of methemoglobinemia can be increased when Bupivacaine is combined with Oxetacaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Cinchocaine is combined with Oxetacaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when Dyclonine is combined with Oxetacaine.
Procaine The risk or severity of methemoglobinemia can be increased when Procaine is combined with Oxetacaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when Prilocaine is combined with Oxetacaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when Proparacaine is combined with Oxetacaine.
Meloxicam The risk or severity of methemoglobinemia can be increased when Meloxicam is combined with Oxetacaine.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Oxybuprocaine is combined with Oxetacaine.
Cocaine The risk or severity of methemoglobinemia can be increased when Cocaine is combined with Oxetacaine.
Mepivacaine The risk or severity of methemoglobinemia can be increased when Mepivacaine is combined with Oxetacaine.
Levobupivacaine The risk or severity of methemoglobinemia can be increased when Levobupivacaine is combined with Oxetacaine.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when Diphenhydramine is combined with Oxetacaine.
Benzocaine The risk or severity of methemoglobinemia can be increased when Benzocaine is combined with Oxetacaine.
Phenol The risk or severity of methemoglobinemia can be increased when Phenol is combined with Oxetacaine.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when Tetrodotoxin is combined with Oxetacaine.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Benzyl alcohol is combined with Oxetacaine.
Capsaicin The risk or severity of methemoglobinemia can be increased when Capsaicin is combined with Oxetacaine.
Etidocaine The risk or severity of methemoglobinemia can be increased when Etidocaine is combined with Oxetacaine.
Articaine The risk or severity of methemoglobinemia can be increased when Articaine is combined with Oxetacaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when Tetracaine is combined with Oxetacaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when Propoxycaine is combined with Oxetacaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when Pramocaine is combined with Oxetacaine.
Butamben The risk or severity of methemoglobinemia can be increased when Butamben is combined with Oxetacaine.
Butacaine The risk or severity of methemoglobinemia can be increased when Butacaine is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when Oxetacaine is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when Oxetacaine is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when Oxetacaine is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when Oxetacaine is combined with Quinisocaine.
Cetuximab The risk or severity of methemoglobinemia can be increased when Cetuximab is combined with Oxetacaine.
Denileukin diftitox The risk or severity of methemoglobinemia can be increased when Denileukin diftitox is combined with Oxetacaine.
Leuprolide The risk or severity of methemoglobinemia can be increased when Leuprolide is combined with Oxetacaine.
Peginterferon alfa-2a The risk or severity of methemoglobinemia can be increased when Peginterferon alfa-2a is combined with Oxetacaine.
Goserelin The risk or severity of methemoglobinemia can be increased when Goserelin is combined with Oxetacaine.
Asparaginase Escherichia coli The risk or severity of methemoglobinemia can be increased when Asparaginase Escherichia coli is combined with Oxetacaine.
Interferon alfa-2a The risk or severity of methemoglobinemia can be increased when Interferon alfa-2a is combined with Oxetacaine.
Aldesleukin The risk or severity of methemoglobinemia can be increased when Aldesleukin is combined with Oxetacaine.
Gemtuzumab ozogamicin The risk or severity of methemoglobinemia can be increased when Gemtuzumab ozogamicin is combined with Oxetacaine.
Pegaspargase The risk or severity of methemoglobinemia can be increased when Pegaspargase is combined with Oxetacaine.
Trastuzumab The risk or severity of methemoglobinemia can be increased when Trastuzumab is combined with Oxetacaine.
Rituximab The risk or severity of methemoglobinemia can be increased when Rituximab is combined with Oxetacaine.
Tositumomab The risk or severity of methemoglobinemia can be increased when Tositumomab is combined with Oxetacaine.
Alemtuzumab The risk or severity of methemoglobinemia can be increased when Alemtuzumab is combined with Oxetacaine.
Octreotide The risk or severity of methemoglobinemia can be increased when Octreotide is combined with Oxetacaine.
Interferon alfa-2b The risk or severity of methemoglobinemia can be increased when Interferon alfa-2b is combined with Oxetacaine.
Bevacizumab The risk or severity of methemoglobinemia can be increased when Bevacizumab is combined with Oxetacaine.
Masoprocol The risk or severity of methemoglobinemia can be increased when Masoprocol is combined with Oxetacaine.
Bortezomib The risk or severity of methemoglobinemia can be increased when Bortezomib is combined with Oxetacaine.
Pipobroman The risk or severity of methemoglobinemia can be increased when Pipobroman is combined with Oxetacaine.
Cladribine The risk or severity of methemoglobinemia can be increased when Cladribine is combined with Oxetacaine.
Cabergoline The risk or severity of methemoglobinemia can be increased when Cabergoline is combined with Oxetacaine.
Anagrelide The risk or severity of methemoglobinemia can be increased when Anagrelide is combined with Oxetacaine.
Carmustine The risk or severity of methemoglobinemia can be increased when Carmustine is combined with Oxetacaine.
Chlorotrianisene The risk or severity of methemoglobinemia can be increased when Chlorotrianisene is combined with Oxetacaine.
Amsacrine The risk or severity of methemoglobinemia can be increased when Amsacrine is combined with Oxetacaine.
Pamidronic acid The risk or severity of methemoglobinemia can be increased when Pamidronic acid is combined with Oxetacaine.
Bleomycin The risk or severity of methemoglobinemia can be increased when Bleomycin is combined with Oxetacaine.
Chlorambucil The risk or severity of methemoglobinemia can be increased when Chlorambucil is combined with Oxetacaine.
Raltitrexed The risk or severity of methemoglobinemia can be increased when Raltitrexed is combined with Oxetacaine.
Mitomycin The risk or severity of methemoglobinemia can be increased when Mitomycin is combined with Oxetacaine.
Bexarotene The risk or severity of methemoglobinemia can be increased when Bexarotene is combined with Oxetacaine.
Vindesine The risk or severity of methemoglobinemia can be increased when Vindesine is combined with Oxetacaine.
Valproic acid The risk or severity of methemoglobinemia can be increased when Valproic acid is combined with Oxetacaine.
Gefitinib The risk or severity of methemoglobinemia can be increased when Gefitinib is combined with Oxetacaine.
Floxuridine The risk or severity of methemoglobinemia can be increased when Floxuridine is combined with Oxetacaine.

Target Protein

Gastrin GAST

Referensi & Sumber

Artikel (PubMed)
  • PMID: 14079039
    BALMFORTH GV, SAMUEL RK: CONTROLLED TRIAL OF OXETHAZAINE AS AN ANALGESIC IN DUODENAL ULCER. Br Med J. 1964 Feb 8;1(5379):355-6.
  • PMID: 8935718
    Masuda Y, Yoshizawa T, Ozaki M, Tanaka T: The metabolic and hemodynamic effects of oxethazaine in the perfused rat liver. Jpn J Pharmacol. 1996 Mar;70(3):243-52.
  • PMID: 28867721
    Namba H, Nishimura Y, Kurata N, Iwase M, Hirai T, Kiuchi Y: Inhibitory Effect of Oxethazaine on Midazolam Metabolism in Rats. Biol Pharm Bull. 2017;40(9):1361-1365. doi: 10.1248/bpb.b16-01016.
Textbook
  • Parakh R. and Patil N. (2017). International Journal of Research in Medical Sciences. MSJ Online.
  • ISBN: 978-93-5090-655-2
    Kapoor A. and Raju S. (2013). Ilustrated Medical Pharmacology. Jaypee Brothers.

Contoh Produk & Brand

Produk: 1 • International brands: 0
Produk
  • Mucaine - Sus
    Suspension • - • Oral • Canada • OTC • Approved

Sekuens Gen/Protein (FASTA)

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