Peringatan Keamanan

Adverse effects include anorexia, nausea, vomiting, bleeding, anemia, diarrhea, and constipation.L1235 Loxoprofen toxicity may lead to gastrointestinal disturbance (including flatulence, dyspepsia and gastritis) and renal failure.L1268

Loxoprofen

DB09212

small molecule approved

Deskripsi

Loxoprofen is a propionic acid derivative non-steroidal anti-inflammatory drug. It is marketed under the trade name Loxonin in Brazil, Mexico and Japan by Sankyo, as Loxomac in India, and as Oxeno in Argentina. A transdermal preparation was approved for use in Japan in January 2006.

Struktur Molekul 2D

Berat 246.3016
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of Loxoprofen is approximately 15 hours.[L1268] Steady concentration is achieved after 2-3 doses.[L1268]
Volume Distribusi Loxoprofen has a volume of distribution of 0.16 L/kg.[L1268]
Klirens (Clearance) Most of the drug as unchanged loxoprofen, 6-0-desmethyl loxoprofen (less than 1%) and glucuronide or other conjugates (66-92%).[L1235] In patients with renal failure, metabolites may accumulate.[L1268]

Absorpsi

Loxoprofen is rapidly and completely absorbed from the GI tract with a bioavailability of 95%.L1268 The absorption phase of the medication occurs in the first 4-6 hours after ingestion. Food ingestion with the medication causes a slight decrease in the rate of loxoprofen absorption.L1268

Metabolisme

Loxoprofen is a prodrug that is rapidly converted to its active trans-alcohol metabolite by carbonyl reductase in the liver.A187934 This same process also results in a cis-alcohol metabolite, though this isomer carries little pharmacological activity.A187931,A27797 The parent drug has also been observed to undergo oxidation via CYP3A4/5 to two hydroxylated metabolites (M3 and M4) and glucuronidation by UGT2B7 to two glucuronide metabolites (M5 and M6).A187931 The alcohol metabolites of loxoprofen also undergo glucuronide conjugation via UGT2B7 to two glucuronide metabolites (M7 and M8) prior to excretion.A187931 When applied in topical formulations, loxoprofen is metabolized to its active trans-alcohol form by carbonyl reductase in the skin.A187937

Rute Eliminasi

50% renal excretion.L1235 This drug is 20% - 30% excreted in the stool.L1231,L1235

Interaksi Makanan

3 Data
  • 1. Exercise caution with grapefruit products. Loxoprofen is metabolized by CYP3A4 to an inactive metabolite and grapefruit is a CYP3A4 inhibitor.
  • 2. Exercise caution with St. John's Wort. Loxoprofen is metabolized by CYP3A4 to an inactive metabolite and St. Johns Wort is a CYP3A4 inducer.
  • 3. Take with food. Taking loxoprofen with food may reduce the risk of gastrointestinal upset.

Interaksi Obat

1386 Data
Amlodipine Loxoprofen may decrease the antihypertensive activities of Amlodipine.
Phentermine The risk or severity of hypertension can be increased when Phentermine is combined with Loxoprofen.
Midodrine The risk or severity of hypertension can be increased when Midodrine is combined with Loxoprofen.
Eletriptan The risk or severity of hypertension can be increased when Eletriptan is combined with Loxoprofen.
Isoetharine The risk or severity of hypertension can be increased when Isoetharine is combined with Loxoprofen.
Ziprasidone The risk or severity of hypertension can be increased when Ziprasidone is combined with Loxoprofen.
Methysergide The risk or severity of hypertension can be increased when Methysergide is combined with Loxoprofen.
Cabergoline The risk or severity of hypertension can be increased when Cabergoline is combined with Loxoprofen.
Zolmitriptan The risk or severity of hypertension can be increased when Zolmitriptan is combined with Loxoprofen.
Dihydroergotamine The risk or severity of hypertension can be increased when Dihydroergotamine is combined with Loxoprofen.
Methylergometrine The risk or severity of hypertension can be increased when Methylergometrine is combined with Loxoprofen.
Norepinephrine The risk or severity of hypertension can be increased when Norepinephrine is combined with Loxoprofen.
Mirtazapine The risk or severity of hypertension can be increased when Mirtazapine is combined with Loxoprofen.
Phenylephrine The risk or severity of hypertension can be increased when Phenylephrine is combined with Loxoprofen.
Phenylpropanolamine The risk or severity of hypertension can be increased when Phenylpropanolamine is combined with Loxoprofen.
Promazine The risk or severity of hypertension can be increased when Promazine is combined with Loxoprofen.
Droperidol The risk or severity of hypertension can be increased when Droperidol is combined with Loxoprofen.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Loxoprofen.
Atropine The risk or severity of hypertension can be increased when Atropine is combined with Loxoprofen.
Lisuride The risk or severity of hypertension can be increased when Lisuride is combined with Loxoprofen.
Linezolid The risk or severity of hypertension can be increased when Linezolid is combined with Loxoprofen.
Metaraminol The risk or severity of hypertension can be increased when Metaraminol is combined with Loxoprofen.
Furazolidone The risk or severity of hypertension can be increased when Furazolidone is combined with Loxoprofen.
Epinephrine The risk or severity of hypertension can be increased when Epinephrine is combined with Loxoprofen.
Thioridazine The risk or severity of hypertension can be increased when Thioridazine is combined with Loxoprofen.
Ergotamine The risk or severity of hypertension can be increased when Ergotamine is combined with Loxoprofen.
Nicergoline The risk or severity of hypertension can be increased when Nicergoline is combined with Loxoprofen.
Sufentanil The risk or severity of hypertension can be increased when Sufentanil is combined with Loxoprofen.
Methoxamine The risk or severity of hypertension can be increased when Methoxamine is combined with Loxoprofen.
Risperidone The risk or severity of hypertension can be increased when Risperidone is combined with Loxoprofen.
Tranylcypromine The risk or severity of hypertension can be increased when Tranylcypromine is combined with Loxoprofen.
Isoflurane The risk or severity of hypertension can be increased when Isoflurane is combined with Loxoprofen.
Propiomazine The risk or severity of hypertension can be increased when Propiomazine is combined with Loxoprofen.
Alfentanil The risk or severity of hypertension can be increased when Alfentanil is combined with Loxoprofen.
Minaprine The risk or severity of hypertension can be increased when Minaprine is combined with Loxoprofen.
Orciprenaline The risk or severity of hypertension can be increased when Orciprenaline is combined with Loxoprofen.
Propofol The risk or severity of hypertension can be increased when Propofol is combined with Loxoprofen.
Phenmetrazine The risk or severity of hypertension can be increased when Phenmetrazine is combined with Loxoprofen.
Trifluoperazine The risk or severity of hypertension can be increased when Trifluoperazine is combined with Loxoprofen.
Pseudoephedrine The risk or severity of hypertension can be increased when Pseudoephedrine is combined with Loxoprofen.
Benzphetamine The risk or severity of hypertension can be increased when Benzphetamine is combined with Loxoprofen.
Ritodrine The risk or severity of hypertension can be increased when Ritodrine is combined with Loxoprofen.
Flupentixol The risk or severity of hypertension can be increased when Flupentixol is combined with Loxoprofen.
Remifentanil The risk or severity of hypertension can be increased when Remifentanil is combined with Loxoprofen.
Bitolterol The risk or severity of hypertension can be increased when Bitolterol is combined with Loxoprofen.
Oxymetazoline The risk or severity of hypertension can be increased when Oxymetazoline is combined with Loxoprofen.
Diethylpropion The risk or severity of hypertension can be increased when Diethylpropion is combined with Loxoprofen.
Salmeterol The risk or severity of hypertension can be increased when Salmeterol is combined with Loxoprofen.
Naratriptan The risk or severity of hypertension can be increased when Naratriptan is combined with Loxoprofen.
Formoterol The risk or severity of hypertension can be increased when Formoterol is combined with Loxoprofen.
Frovatriptan The risk or severity of hypertension can be increased when Frovatriptan is combined with Loxoprofen.
Methoxyflurane The risk or severity of hypertension can be increased when Methoxyflurane is combined with Loxoprofen.
Selegiline The risk or severity of hypertension can be increased when Selegiline is combined with Loxoprofen.
Ergoloid mesylate The risk or severity of hypertension can be increased when Ergoloid mesylate is combined with Loxoprofen.
Isoprenaline The risk or severity of hypertension can be increased when Isoprenaline is combined with Loxoprofen.
Arbutamine The risk or severity of hypertension can be increased when Arbutamine is combined with Loxoprofen.
Dutasteride The risk or severity of hypertension can be increased when Dutasteride is combined with Loxoprofen.
Halothane The risk or severity of hypertension can be increased when Halothane is combined with Loxoprofen.
Moclobemide The risk or severity of hypertension can be increased when Moclobemide is combined with Loxoprofen.
Pergolide The risk or severity of hypertension can be increased when Pergolide is combined with Loxoprofen.
Desflurane The risk or severity of hypertension can be increased when Desflurane is combined with Loxoprofen.
Bromocriptine The risk or severity of hypertension can be increased when Bromocriptine is combined with Loxoprofen.
Finasteride The risk or severity of hypertension can be increased when Finasteride is combined with Loxoprofen.
Aripiprazole The risk or severity of hypertension can be increased when Aripiprazole is combined with Loxoprofen.
Isocarboxazid The risk or severity of hypertension can be increased when Isocarboxazid is combined with Loxoprofen.
Ergometrine The risk or severity of hypertension can be increased when Ergometrine is combined with Loxoprofen.
Lisdexamfetamine The risk or severity of hypertension can be increased when Lisdexamfetamine is combined with Loxoprofen.
Fenoterol The risk or severity of hypertension can be increased when Fenoterol is combined with Loxoprofen.
Pirbuterol The risk or severity of hypertension can be increased when Pirbuterol is combined with Loxoprofen.
Ephedra sinica root The risk or severity of hypertension can be increased when Ephedra sinica root is combined with Loxoprofen.
Ephedrine The risk or severity of hypertension can be increased when Ephedrine is combined with Loxoprofen.
Mephentermine The risk or severity of hypertension can be increased when Mephentermine is combined with Loxoprofen.
Procaterol The risk or severity of hypertension can be increased when Procaterol is combined with Loxoprofen.
Yohimbine The risk or severity of hypertension can be increased when Yohimbine is combined with Loxoprofen.
Methotrimeprazine The risk or severity of hypertension can be increased when Methotrimeprazine is combined with Loxoprofen.
Clenbuterol The risk or severity of hypertension can be increased when Clenbuterol is combined with Loxoprofen.
Bambuterol The risk or severity of hypertension can be increased when Bambuterol is combined with Loxoprofen.
MMDA The risk or severity of hypertension can be increased when MMDA is combined with Loxoprofen.
Midomafetamine The risk or severity of hypertension can be increased when Midomafetamine is combined with Loxoprofen.
2,5-Dimethoxy-4-ethylamphetamine The risk or severity of hypertension can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Loxoprofen.
4-Methoxyamphetamine The risk or severity of hypertension can be increased when 4-Methoxyamphetamine is combined with Loxoprofen.
4-Bromo-2,5-dimethoxyamphetamine The risk or severity of hypertension can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Loxoprofen.
Tenamfetamine The risk or severity of hypertension can be increased when Tenamfetamine is combined with Loxoprofen.
Chlorphentermine The risk or severity of hypertension can be increased when Chlorphentermine is combined with Loxoprofen.
Dextroamphetamine The risk or severity of hypertension can be increased when Dextroamphetamine is combined with Loxoprofen.
Phendimetrazine The risk or severity of hypertension can be increased when Phendimetrazine is combined with Loxoprofen.
Solifenacin The risk or severity of hypertension can be increased when Solifenacin is combined with Loxoprofen.
Periciazine The risk or severity of hypertension can be increased when Periciazine is combined with Loxoprofen.
Acepromazine The risk or severity of hypertension can be increased when Acepromazine is combined with Loxoprofen.
Thioproperazine The risk or severity of hypertension can be increased when Thioproperazine is combined with Loxoprofen.
Zuclopenthixol The risk or severity of hypertension can be increased when Zuclopenthixol is combined with Loxoprofen.
Epicaptopril The risk or severity of hypertension can be increased when Epicaptopril is combined with Loxoprofen.
Clorgiline The risk or severity of hypertension can be increased when Clorgiline is combined with Loxoprofen.
1-benzylimidazole The risk or severity of hypertension can be increased when 1-benzylimidazole is combined with Loxoprofen.
Iproniazid The risk or severity of hypertension can be increased when Iproniazid is combined with Loxoprofen.
Nialamide The risk or severity of hypertension can be increased when Nialamide is combined with Loxoprofen.
Lysergic acid diethylamide The risk or severity of hypertension can be increased when Lysergic acid diethylamide is combined with Loxoprofen.
Dronedarone The risk or severity of hypertension can be increased when Dronedarone is combined with Loxoprofen.
Flibanserin The risk or severity of hypertension can be increased when Flibanserin is combined with Loxoprofen.
Iloperidone The risk or severity of hypertension can be increased when Iloperidone is combined with Loxoprofen.

Target Protein

Prostaglandin G/H synthase 2 PTGS2
Prostaglandin G/H synthase 1 PTGS1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 30072626
    Shrestha R, Cho PJ, Paudel S, Shrestha A, Kang MJ, Jeong TC, Lee ES, Lee S: Exploring the Metabolism of Loxoprofen in Liver Microsomes: The Role of Cytochrome P450 and UDP-Glucuronosyltransferase in Its Biotransformation. Pharmaceutics. 2018 Aug 2;10(3). pii: pharmaceutics10030112. doi: 10.3390/pharmaceutics10030112.
  • PMID: 29851133
    Quinones-Lombrana A, Li N, Del Solar V, Atilla-Gokcumen GE, Blanco JG: CBR1 rs9024 genotype status impacts the bioactivation of loxoprofen in human liver. Biopharm Drug Dispos. 2018 Jun;39(6):315-318. doi: 10.1002/bdd.2135.
  • PMID: 14980665
    Riendeau D, Salem M, Styhler A, Ouellet M, Mancini JA, Li CS: Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2. Bioorg Med Chem Lett. 2004 Mar 8;14(5):1201-3.
  • PMID: 25765700
    Sawamura R, Sakurai H, Wada N, Nishiya Y, Honda T, Kazui M, Kurihara A, Shinagawa A, Izumi T: Bioactivation of loxoprofen to a pharmacologically active metabolite and its disposition kinetics in human skin. Biopharm Drug Dispos. 2015 Sep;36(6):352-363. doi: 10.1002/bdd.1945. Epub 2015 Apr 21.

Contoh Produk & Brand

Produk: 0 • International brands: 3
International Brands
  • Loxomac
  • Loxonin
  • Oxeno

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