Peringatan Keamanan

No overdoses of rofecoxib were reported during clinical trials. Administration of single doses of rofecoxib 1000 mg to 6 healthy volunteers and multiple doses of 250 mg/day for 14 days to 75 healthy volunteers did not result in serious toxicity.

Rofecoxib

DB00533

small molecule approved investigational withdrawn

Deskripsi

Rofecoxib is used for the treatment of osteoarthritis, rheumatoid arthritis, acute pain in adults, and primary dysmenorrhea, as well as acute treatment of migraine attacks with or without auras. Rofecoxib is a solid. This compound belongs to the stilbenes. These are organic compounds containing a 1,2-diphenylethylene moiety. Stilbenes (C6-C2-C6 ) are derived from the common phenylpropene (C6-C3) skeleton building block. The introduction of one or more hydroxyl groups to a phenyl ring lead to stilbenoids. Rofecoxib has a half-life of 17 hours and its mean oral bioavailability at therapeutically recommended doses of 125, 25, and 50 mg is approximately 93%. The proteins that rofecoxib target include elastin and prostaglandin G/H synthase 2. Cytochrome P450 1A2, Cytochrome P450 3A4, Cytochrome P450 2C9, Cytochrome P450 2C8, and Prostaglandin G/H synthase 1 are known to metabolize rofecoxib. On September 30, 2004, Merck voluntarily withdrew rofecoxib from the market because of concerns about increased risk of heart attack and stroke associated with long-term, high-dosage use.

Struktur Molekul 2D

Berat 314.356
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 17 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

The mean oral bioavailability of rofecoxib at therapeutically recommended doses of 12.5, 25, and 50 mg is approximately 93%.

Metabolisme

Hepatic. Metabolism of rofecoxib is primarily mediated through reduction by cytosolic enzymes. The principal metabolic products are the cis-dihydro and trans-dihydro derivatives of rofecoxib, which account for nearly 56% of recovered radioactivity in the urine. An additional 8.8% of the dose was recovered as the glucuronide of the hydroxy derivative, a product of oxidative metabolism. The biotransformation of rofecoxib and this metabolite is reversible in humans to a limited extent (< 5%). These metabolites are inactive as COX-1 or COX-2 inhibitors. Cytochrome P450 plays a minor role in metabolism of rofecoxib.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

2 Data
  • 1. Take separate from antacids. Taking rofecoxib with antacids can reduce the AUC and Cmax of rofecoxib, therefore consider separating their administration for optimal efficacy.
  • 2. Take with or without food. The AUC and Cmax of rofecoxib tablets are not impacted by administration with food, however, the Tmax may be delayed. The food effect on the absorption of rofecoxib suspension formulation has not been studied according to the official product labeling.

Interaksi Obat

1858 Data
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Rofecoxib.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Rofecoxib.
Peginterferon alfa-2b The serum concentration of Rofecoxib can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Rofecoxib can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Rofecoxib can be decreased when it is combined with Teriflunomide.
Midodrine The risk or severity of hypertension can be increased when Midodrine is combined with Rofecoxib.
Isoetharine The risk or severity of hypertension can be increased when Isoetharine is combined with Rofecoxib.
Norepinephrine The risk or severity of hypertension can be increased when Norepinephrine is combined with Rofecoxib.
Phenylpropanolamine The risk or severity of hypertension can be increased when Phenylpropanolamine is combined with Rofecoxib.
Droperidol The risk or severity of hypertension can be increased when Droperidol is combined with Rofecoxib.
Doxapram The risk or severity of hypertension can be increased when Rofecoxib is combined with Doxapram.
Atropine The risk or severity of hypertension can be increased when Rofecoxib is combined with Atropine.
Linezolid The risk or severity of hypertension can be increased when Rofecoxib is combined with Linezolid.
Metaraminol The risk or severity of hypertension can be increased when Rofecoxib is combined with Metaraminol.
Furazolidone The risk or severity of hypertension can be increased when Rofecoxib is combined with Furazolidone.
Thioridazine The risk or severity of hypertension can be increased when Rofecoxib is combined with Thioridazine.
Nicergoline The risk or severity of hypertension can be increased when Rofecoxib is combined with Nicergoline.
Methoxamine The risk or severity of hypertension can be increased when Rofecoxib is combined with Methoxamine.
Isoflurane The risk or severity of hypertension can be increased when Rofecoxib is combined with Isoflurane.
Propiomazine The risk or severity of hypertension can be increased when Rofecoxib is combined with Propiomazine.
Minaprine The risk or severity of hypertension can be increased when Rofecoxib is combined with Minaprine.
Orciprenaline The risk or severity of hypertension can be increased when Rofecoxib is combined with Orciprenaline.
Phenmetrazine The risk or severity of hypertension can be increased when Rofecoxib is combined with Phenmetrazine.
Pseudoephedrine The risk or severity of hypertension can be increased when Rofecoxib is combined with Pseudoephedrine.
Ritodrine The risk or severity of hypertension can be increased when Rofecoxib is combined with Ritodrine.
Flupentixol The risk or severity of hypertension can be increased when Rofecoxib is combined with Flupentixol.
Remifentanil The risk or severity of hypertension can be increased when Rofecoxib is combined with Remifentanil.
Bitolterol The risk or severity of hypertension can be increased when Rofecoxib is combined with Bitolterol.
Oxymetazoline The risk or severity of hypertension can be increased when Rofecoxib is combined with Oxymetazoline.
Diethylpropion The risk or severity of hypertension can be increased when Rofecoxib is combined with Diethylpropion.
Naratriptan The risk or severity of hypertension can be increased when Rofecoxib is combined with Naratriptan.
Isoprenaline The risk or severity of hypertension can be increased when Rofecoxib is combined with Isoprenaline.
Arbutamine The risk or severity of hypertension can be increased when Rofecoxib is combined with Arbutamine.
Desflurane The risk or severity of hypertension can be increased when Rofecoxib is combined with Desflurane.
Isocarboxazid The risk or severity of hypertension can be increased when Rofecoxib is combined with Isocarboxazid.
Lisdexamfetamine The risk or severity of hypertension can be increased when Rofecoxib is combined with Lisdexamfetamine.
Fenoterol The risk or severity of hypertension can be increased when Rofecoxib is combined with Fenoterol.
Pirbuterol The risk or severity of hypertension can be increased when Rofecoxib is combined with Pirbuterol.
Ephedra sinica root The risk or severity of hypertension can be increased when Rofecoxib is combined with Ephedra sinica root.
Ephedrine The risk or severity of hypertension can be increased when Rofecoxib is combined with Ephedrine.
Mephentermine The risk or severity of hypertension can be increased when Rofecoxib is combined with Mephentermine.
Procaterol The risk or severity of hypertension can be increased when Rofecoxib is combined with Procaterol.
Methotrimeprazine The risk or severity of hypertension can be increased when Rofecoxib is combined with Methotrimeprazine.
Clenbuterol The risk or severity of hypertension can be increased when Rofecoxib is combined with Clenbuterol.
Bambuterol The risk or severity of hypertension can be increased when Rofecoxib is combined with Bambuterol.
MMDA The risk or severity of hypertension can be increased when Rofecoxib is combined with MMDA.
Midomafetamine The risk or severity of hypertension can be increased when Rofecoxib is combined with Midomafetamine.
2,5-Dimethoxy-4-ethylamphetamine The risk or severity of hypertension can be increased when Rofecoxib is combined with 2,5-Dimethoxy-4-ethylamphetamine.
4-Methoxyamphetamine The risk or severity of hypertension can be increased when Rofecoxib is combined with 4-Methoxyamphetamine.
4-Bromo-2,5-dimethoxyamphetamine The risk or severity of hypertension can be increased when Rofecoxib is combined with 4-Bromo-2,5-dimethoxyamphetamine.
Tenamfetamine The risk or severity of hypertension can be increased when Rofecoxib is combined with Tenamfetamine.
Chlorphentermine The risk or severity of hypertension can be increased when Rofecoxib is combined with Chlorphentermine.
Dextroamphetamine The risk or severity of hypertension can be increased when Rofecoxib is combined with Dextroamphetamine.
Phendimetrazine The risk or severity of hypertension can be increased when Rofecoxib is combined with Phendimetrazine.
Periciazine The risk or severity of hypertension can be increased when Rofecoxib is combined with Periciazine.
Acepromazine The risk or severity of hypertension can be increased when Rofecoxib is combined with Acepromazine.
Thioproperazine The risk or severity of hypertension can be increased when Rofecoxib is combined with Thioproperazine.
Epicaptopril The risk or severity of hypertension can be increased when Rofecoxib is combined with Epicaptopril.
Clorgiline The risk or severity of hypertension can be increased when Rofecoxib is combined with Clorgiline.
1-benzylimidazole The risk or severity of hypertension can be increased when Rofecoxib is combined with 1-benzylimidazole.
Nialamide The risk or severity of hypertension can be increased when Rofecoxib is combined with Nialamide.
Amibegron The risk or severity of hypertension can be increased when Rofecoxib is combined with Amibegron.
Naluzotan The risk or severity of hypertension can be increased when Rofecoxib is combined with Naluzotan.
Pizotifen The risk or severity of hypertension can be increased when Rofecoxib is combined with Pizotifen.
Solabegron The risk or severity of hypertension can be increased when Rofecoxib is combined with Solabegron.
Esmirtazapine The risk or severity of hypertension can be increased when Rofecoxib is combined with Esmirtazapine.
Nitrous oxide The risk or severity of hypertension can be increased when Rofecoxib is combined with Nitrous oxide.
Xylometazoline The risk or severity of hypertension can be increased when Rofecoxib is combined with Xylometazoline.
Dexmethylphenidate The risk or severity of hypertension can be increased when Rofecoxib is combined with Dexmethylphenidate.
Isometheptene The risk or severity of hypertension can be increased when Rofecoxib is combined with Isometheptene.
Levonordefrin The risk or severity of hypertension can be increased when Rofecoxib is combined with Levonordefrin.
Naphazoline The risk or severity of hypertension can be increased when Rofecoxib is combined with Naphazoline.
Tetryzoline The risk or severity of hypertension can be increased when Rofecoxib is combined with Tetryzoline.
Cinitapride The risk or severity of hypertension can be increased when Rofecoxib is combined with Cinitapride.
Tyramine The risk or severity of hypertension can be increased when Rofecoxib is combined with Tyramine.
Adrafinil The risk or severity of hypertension can be increased when Rofecoxib is combined with Adrafinil.
Isoxsuprine The risk or severity of hypertension can be increased when Rofecoxib is combined with Isoxsuprine.
Ifenprodil The risk or severity of hypertension can be increased when Rofecoxib is combined with Ifenprodil.
Hexoprenaline The risk or severity of hypertension can be increased when Rofecoxib is combined with Hexoprenaline.
Etilefrine The risk or severity of hypertension can be increased when Rofecoxib is combined with Etilefrine.
Cirazoline The risk or severity of hypertension can be increased when Rofecoxib is combined with Cirazoline.
Synephrine The risk or severity of hypertension can be increased when Rofecoxib is combined with Synephrine.
Hydracarbazine The risk or severity of hypertension can be increased when Rofecoxib is combined with Hydracarbazine.
Benmoxin The risk or severity of hypertension can be increased when Rofecoxib is combined with Benmoxin.
Mebanazine The risk or severity of hypertension can be increased when Rofecoxib is combined with Mebanazine.
Octamoxin The risk or severity of hypertension can be increased when Rofecoxib is combined with Octamoxin.
Pheniprazine The risk or severity of hypertension can be increased when Rofecoxib is combined with Pheniprazine.
Phenoxypropazine The risk or severity of hypertension can be increased when Rofecoxib is combined with Phenoxypropazine.
Pivhydrazine The risk or severity of hypertension can be increased when Rofecoxib is combined with Pivhydrazine.
Safrazine The risk or severity of hypertension can be increased when Rofecoxib is combined with Safrazine.
Caroxazone The risk or severity of hypertension can be increased when Rofecoxib is combined with Caroxazone.
Iofetamine I-123 The risk or severity of hypertension can be increased when Rofecoxib is combined with Iofetamine I-123.
Racepinephrine The risk or severity of hypertension can be increased when Rofecoxib is combined with Racepinephrine.
Amitraz The risk or severity of hypertension can be increased when Rofecoxib is combined with Amitraz.
Medetomidine The risk or severity of hypertension can be increased when Rofecoxib is combined with Medetomidine.
Xylazine The risk or severity of hypertension can be increased when Rofecoxib is combined with Xylazine.
Atipamezole The risk or severity of hypertension can be increased when Rofecoxib is combined with Atipamezole.
Ractopamine The risk or severity of hypertension can be increased when Rofecoxib is combined with Ractopamine.
Romifidine The risk or severity of hypertension can be increased when Rofecoxib is combined with Romifidine.
Detomidine The risk or severity of hypertension can be increased when Rofecoxib is combined with Detomidine.

Target Protein

Prostaglandin G/H synthase 2 PTGS2
Elastin ELN

Referensi & Sumber

Artikel (PubMed)
  • PMID: 11087881
    Bombardier C, Laine L, Reicin A, Shapiro D, Burgos-Vargas R, Davis B, Day R, Ferraz MB, Hawkey CJ, Hochberg MC, Kvien TK, Schnitzer TJ: Comparison of upper gastrointestinal toxicity of rofecoxib and naproxen in patients with rheumatoid arthritis. VIGOR Study Group. N Engl J Med. 2000 Nov 23;343(21):1520-8, 2 p following 1528.
  • PMID: 15713943
    Bresalier RS, Sandler RS, Quan H, Bolognese JA, Oxenius B, Horgan K, Lines C, Riddell R, Morton D, Lanas A, Konstam MA, Baron JA: Cardiovascular events associated with rofecoxib in a colorectal adenoma chemoprevention trial. N Engl J Med. 2005 Mar 17;352(11):1092-102. Epub 2005 Feb 15.
  • PMID: 16495386
    Curfman GD, Morrissey S, Drazen JM: Expression of concern reaffirmed. N Engl J Med. 2006 Mar 16;354(11):1193. Epub 2006 Feb 22.
  • PMID: 15470192
    Fitzgerald GA: Coxibs and cardiovascular disease. N Engl J Med. 2004 Oct 21;351(17):1709-11. Epub 2004 Oct 6.
  • PMID: 15641522
    Karha J, Topol EJ: The sad story of Vioxx, and what we should learn from it. Cleve Clin J Med. 2004 Dec;71(12):933-4, 936, 938-9.
  • PMID: 18922570
    Baron JA, Sandler RS, Bresalier RS, Lanas A, Morton DG, Riddell R, Iverson ER, Demets DL: Cardiovascular events associated with rofecoxib: final analysis of the APPROVe trial. Lancet. 2008 Nov 15;372(9651):1756-64. doi: 10.1016/S0140-6736(08)61490-7. Epub 2008 Oct 14.
  • PMID: 11398914
    Matheson AJ, Figgitt DP: Rofecoxib: a review of its use in the management of osteoarthritis, acute pain and rheumatoid arthritis. Drugs. 2001;61(6):833-65.
  • PMID: 11249495
    Hillson JL, Furst DE: Rofecoxib. Expert Opin Pharmacother. 2000 Jul;1(5):1053-66.

Contoh Produk & Brand

Produk: 3 • International brands: 1
Produk
  • Vioxx Suspension 12.5mg/5ml
    Suspension • 12.5 mg / 5 mL • Oral • Canada • Approved
  • Vioxx Tab 12.5mg
    Tablet • 12.5 mg / tab • Oral • Canada • Approved
  • Vioxx Tab 25mg
    Tablet • 25 mg / tab • Oral • Canada • Approved
International Brands
  • Vioxx

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