Peringatan Keamanan

Tolfenamic acid has a relatively low acute toxicity with LD50 values in 200-1000 mg/kg. The metabolites of tolfenamic acid are reported to have an even less important toxicity. Some of the expected toxicity is related to the presence of gastrointestinal effects such as gut ulceration and renal papillitis.L1303

Tolfenamic acid

DB09216

small molecule approved investigational

Deskripsi

Tolfenamic acid, with the formula N-(2-methyl-3-chlorphenyl)-anthranilic acid, is a nonsteroidal anti-inflammatory agent.A31824 It was discovered by scientists at Medica Pharmaceutical Company in Finland. It is used in the UK as a treatment for migraine under the name of Clotam.L1292 In the US, it presents a Status class I by the FDA. By the European Medicine Agency, it was granted in 2016 with the status of orphan for the treatment of supranuclear palsy.L1291

Struktur Molekul 2D

Berat 261.704
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The estimated half-life of tolfenamic acid is 8.01-13.50 hours.[A31842] When tested intravenously, the reported half-life was 6.1h.[A31849]
Volume Distribusi The volume of distribution is of 1.79-3.2 L/kg.[A31842] When tested intravenously, the reported steady-state volume of distribution was 0.33 L/kg.[A31849]
Klirens (Clearance) The estimated clearance rate of tolfenamic acid is 0.142-0.175 L.h/kg.[A31842] When tested intravenously, the reported clearance rate was 72.4 ml.h/kg.[A31849]

Absorpsi

Tolfenamic acid pharmacokinetic is marked by a short tmax of 0.94-2.04 h.A31842 It also presented a linear pharmacokinetic profile with an AUC from 13-50 mcg/ml.h if administered in a dose of 2-8 mg/kg respectively.A31843 The oral absorption is delayed and it gives a mean lag-time to absorption of 32 min. The peak plasma concentration of 11.1 mcg/ml.A31849 The bioavailability of tolfenamic acid is around 75%.A31851

Metabolisme

The first pass metabolism accounts for 20% of the administered dose of tolfenamic acid.A31851 Urine metabolite studies have demonstrated the identification of five metabolites from which three of them are monohydroxylated, one is monohydroxylated and hydroxylated and one last metabolite that presented and oxidized methyl group to form a carboxyl group.A31851 Two of these hydroxylated metabolites are N-(2-hydroxymethyl-3-chlorophenyl)-anthranilic acid and N-(2-hydroxymethyl-3-chloro-4-hydroxyphenyl)-anthranilic acid.L1303

Rute Eliminasi

Tolfenamic acid is cleared relatively fast and it undergoes by hepatic metabolism where the produced metabolites are renally cleared as glucuronic acid conjugates.A31851 Most of the elimination occurs by extrarenal mechanisms in which the unchanged drug together with its glucuronide in urine accounts for only 8.8% of the administered dose.A7838

Interaksi Obat

1475 Data
Ceritinib Tolfenamic acid may increase the bradycardic activities of Ceritinib.
Ivabradine Tolfenamic acid may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Tolfenamic acid.
Amlodipine Tolfenamic acid may decrease the antihypertensive activities of Amlodipine.
Isoetharine The risk or severity of hypertension can be increased when Isoetharine is combined with Tolfenamic acid.
Zolmitriptan The risk or severity of hypertension can be increased when Zolmitriptan is combined with Tolfenamic acid.
Norepinephrine The risk or severity of hypertension can be increased when Norepinephrine is combined with Tolfenamic acid.
Phenylpropanolamine The risk or severity of hypertension can be increased when Phenylpropanolamine is combined with Tolfenamic acid.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Tolfenamic acid.
Linezolid The risk or severity of hypertension can be increased when Linezolid is combined with Tolfenamic acid.
Metaraminol The risk or severity of hypertension can be increased when Metaraminol is combined with Tolfenamic acid.
Furazolidone The risk or severity of hypertension can be increased when Furazolidone is combined with Tolfenamic acid.
Methoxamine The risk or severity of hypertension can be increased when Methoxamine is combined with Tolfenamic acid.
Isoflurane The risk or severity of hypertension can be increased when Isoflurane is combined with Tolfenamic acid.
Minaprine The risk or severity of hypertension can be increased when Minaprine is combined with Tolfenamic acid.
Orciprenaline The risk or severity of hypertension can be increased when Orciprenaline is combined with Tolfenamic acid.
Propofol The risk or severity of hypertension can be increased when Propofol is combined with Tolfenamic acid.
Phenmetrazine The risk or severity of hypertension can be increased when Phenmetrazine is combined with Tolfenamic acid.
Pseudoephedrine The risk or severity of hypertension can be increased when Pseudoephedrine is combined with Tolfenamic acid.
Ritodrine The risk or severity of hypertension can be increased when Ritodrine is combined with Tolfenamic acid.
Bitolterol The risk or severity of hypertension can be increased when Bitolterol is combined with Tolfenamic acid.
Oxymetazoline The risk or severity of hypertension can be increased when Oxymetazoline is combined with Tolfenamic acid.
Diethylpropion The risk or severity of hypertension can be increased when Diethylpropion is combined with Tolfenamic acid.
Naratriptan The risk or severity of hypertension can be increased when Naratriptan is combined with Tolfenamic acid.
Formoterol The risk or severity of hypertension can be increased when Formoterol is combined with Tolfenamic acid.
Frovatriptan The risk or severity of hypertension can be increased when Frovatriptan is combined with Tolfenamic acid.
Isoprenaline The risk or severity of hypertension can be increased when Isoprenaline is combined with Tolfenamic acid.
Arbutamine The risk or severity of hypertension can be increased when Arbutamine is combined with Tolfenamic acid.
Moclobemide The risk or severity of hypertension can be increased when Moclobemide is combined with Tolfenamic acid.
Desflurane The risk or severity of hypertension can be increased when Desflurane is combined with Tolfenamic acid.
Isocarboxazid The risk or severity of hypertension can be increased when Isocarboxazid is combined with Tolfenamic acid.
Lisdexamfetamine The risk or severity of hypertension can be increased when Lisdexamfetamine is combined with Tolfenamic acid.
Fenoterol The risk or severity of hypertension can be increased when Fenoterol is combined with Tolfenamic acid.
Pirbuterol The risk or severity of hypertension can be increased when Pirbuterol is combined with Tolfenamic acid.
Ephedra sinica root The risk or severity of hypertension can be increased when Ephedra sinica root is combined with Tolfenamic acid.
Ephedrine The risk or severity of hypertension can be increased when Ephedrine is combined with Tolfenamic acid.
Mephentermine The risk or severity of hypertension can be increased when Mephentermine is combined with Tolfenamic acid.
Procaterol The risk or severity of hypertension can be increased when Procaterol is combined with Tolfenamic acid.
Clenbuterol The risk or severity of hypertension can be increased when Clenbuterol is combined with Tolfenamic acid.
Bambuterol The risk or severity of hypertension can be increased when Bambuterol is combined with Tolfenamic acid.
MMDA The risk or severity of hypertension can be increased when MMDA is combined with Tolfenamic acid.
Midomafetamine The risk or severity of hypertension can be increased when Midomafetamine is combined with Tolfenamic acid.
2,5-Dimethoxy-4-ethylamphetamine The risk or severity of hypertension can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Tolfenamic acid.
4-Methoxyamphetamine The risk or severity of hypertension can be increased when 4-Methoxyamphetamine is combined with Tolfenamic acid.
4-Bromo-2,5-dimethoxyamphetamine The risk or severity of hypertension can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Tolfenamic acid.
Tenamfetamine The risk or severity of hypertension can be increased when Tenamfetamine is combined with Tolfenamic acid.
Chlorphentermine The risk or severity of hypertension can be increased when Chlorphentermine is combined with Tolfenamic acid.
Dextroamphetamine The risk or severity of hypertension can be increased when Dextroamphetamine is combined with Tolfenamic acid.
Phendimetrazine The risk or severity of hypertension can be increased when Phendimetrazine is combined with Tolfenamic acid.
Epicaptopril The risk or severity of hypertension can be increased when Epicaptopril is combined with Tolfenamic acid.
Clorgiline The risk or severity of hypertension can be increased when Clorgiline is combined with Tolfenamic acid.
1-benzylimidazole The risk or severity of hypertension can be increased when 1-benzylimidazole is combined with Tolfenamic acid.
Iproniazid The risk or severity of hypertension can be increased when Iproniazid is combined with Tolfenamic acid.
Nialamide The risk or severity of hypertension can be increased when Nialamide is combined with Tolfenamic acid.
Amibegron The risk or severity of hypertension can be increased when Amibegron is combined with Tolfenamic acid.
Naluzotan The risk or severity of hypertension can be increased when Naluzotan is combined with Tolfenamic acid.
Solabegron The risk or severity of hypertension can be increased when Solabegron is combined with Tolfenamic acid.
Esmirtazapine The risk or severity of hypertension can be increased when Esmirtazapine is combined with Tolfenamic acid.
Nitrous oxide The risk or severity of hypertension can be increased when Nitrous oxide is combined with Tolfenamic acid.
Dexmethylphenidate The risk or severity of hypertension can be increased when Dexmethylphenidate is combined with Tolfenamic acid.
Isometheptene The risk or severity of hypertension can be increased when Isometheptene is combined with Tolfenamic acid.
Levonordefrin The risk or severity of hypertension can be increased when Levonordefrin is combined with Tolfenamic acid.
Naphazoline The risk or severity of hypertension can be increased when Naphazoline is combined with Tolfenamic acid.
Tetryzoline The risk or severity of hypertension can be increased when Tetryzoline is combined with Tolfenamic acid.
Cinitapride The risk or severity of hypertension can be increased when Cinitapride is combined with Tolfenamic acid.
Tyramine The risk or severity of hypertension can be increased when Tyramine is combined with Tolfenamic acid.
Adrafinil The risk or severity of hypertension can be increased when Adrafinil is combined with Tolfenamic acid.
Isoxsuprine The risk or severity of hypertension can be increased when Isoxsuprine is combined with Tolfenamic acid.
Ifenprodil The risk or severity of hypertension can be increased when Ifenprodil is combined with Tolfenamic acid.
Hexoprenaline The risk or severity of hypertension can be increased when Hexoprenaline is combined with Tolfenamic acid.
Etilefrine The risk or severity of hypertension can be increased when Etilefrine is combined with Tolfenamic acid.
Olodaterol The risk or severity of hypertension can be increased when Olodaterol is combined with Tolfenamic acid.
Cirazoline The risk or severity of hypertension can be increased when Cirazoline is combined with Tolfenamic acid.
Synephrine The risk or severity of hypertension can be increased when Synephrine is combined with Tolfenamic acid.
Hydracarbazine The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Hydracarbazine.
Benmoxin The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Benmoxin.
Mebanazine The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Mebanazine.
Octamoxin The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Octamoxin.
Pheniprazine The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Pheniprazine.
Phenoxypropazine The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Phenoxypropazine.
Pivhydrazine The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Pivhydrazine.
Safrazine The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Safrazine.
Caroxazone The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Caroxazone.
Doxofylline The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Doxofylline.
Iofetamine I-123 The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Iofetamine I-123.
Racepinephrine The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Racepinephrine.
Amitraz The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Amitraz.
Medetomidine The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Medetomidine.
Xylazine The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Xylazine.
Atipamezole The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Atipamezole.
Ractopamine The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Ractopamine.
Romifidine The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Romifidine.
Detomidine The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Detomidine.
Tetrahydrocannabivarin The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Tetrahydrocannabivarin.
PF-00610355 The risk or severity of hypertension can be increased when Tolfenamic acid is combined with PF-00610355.
Ritobegron The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Ritobegron.
Abediterol The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Abediterol.
Tulobuterol The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Tulobuterol.
Dopexamine The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Dopexamine.
Piclozotan The risk or severity of hypertension can be increased when Tolfenamic acid is combined with Piclozotan.

Target Protein

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

Referensi & Sumber

Artikel (PubMed)
  • PMID: 7238564
    Pentikainen PJ, Neuvonen PJ, Backman C: Human pharmacokinetics of tolfenamic acid, a new anti-inflammatory agent. Eur J Clin Pharmacol. 1981;19(5):359-65.
  • PMID: 6691890
    Tokola RA, Neuvonen PJ: Effects of migraine attack and metoclopramide on the absorption of tolfenamic acid. Br J Clin Pharmacol. 1984 Jan;17(1):67-75.
  • PMID: 9638074
    Lees P, McKellar QA, Foot R, Gettinby G: Pharmacodynamics and pharmacokinetics of tolfenamic acid in ruminating calves: evaluation in models of acute inflammation. Vet J. 1998 May;155(3):275-88.
  • PMID: 8200415
    McKellar QA, Lees P, Gettinby G: Pharmacodynamics of tolfenamic acid in dogs. Evaluation of dose response relationships. Eur J Pharmacol. 1994 Mar 3;253(3):191-200.
  • PMID: 1649132
    Kankaanranta H, Moilanen E, Vapaatalo H: Tolfenamic acid inhibits leukotriene B4-induced chemotaxis of polymorphonuclear leukocytes in vitro. Inflammation. 1991 Apr;15(2):137-43.
  • PMID: 9109966
    Jaussaud P, Guieu D, Bellon C, Barbier B, Lhopital MC, Sechet R, Courtot D, Toutain PL: Pharmacokinetics of tolfenamic acid in the horse. Equine Vet J Suppl. 1992 Feb;(11):69-72.
  • PMID: 3758148
    Laznicek M, Senius KE: Protein binding of tolfenamic acid in the plasma from patients with renal and hepatic disease. Eur J Clin Pharmacol. 1986;30(5):591-6.
  • PMID: 7816776
    Pedersen SB: Biopharmaceutical aspects of tolfenamic acid. Pharmacol Toxicol. 1994;75 Suppl 2:22-32.

Contoh Produk & Brand

Produk: 0 • International brands: 1
International Brands
  • Clotam — GEA Farmaceutisk Fabrik

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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