Peringatan Keamanan

The oral TDLo in humans 5.71 mg/kg.L7610

It is not advisable to administer celecoxib in patients with renal impairment or advanced hepatic impairment, as this may lead to increased serum concentrations, causing toxicity.L7646 Symptoms of overdose may include breathing difficulties, coma, drowsiness, gastrointestinal bleeding, high blood pressure, kidney failure, nausea, sluggishness, stomach pain, and vomiting.L3293 Because serious gastrointestinal tract ulceration and bleeding can occur without preceding symptoms, patients should be monitored for signs/symptoms of gastrointestinal bleeding. Symptomatic and supportive measures should be taken in a celecoxib overdose. The induction of emesis or administration of active charcoal should take place if the patient is seen within 4 hours of celecoxib ingestion. Diuresis, urinary alkalinization, hemodialysis, or hemoperfusion may not be useful in a celecoxib overdose due to its high level of protein binding.L7646

Celecoxib

DB00482

small molecule approved investigational

Deskripsi

Celecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, is a nonsteroidal anti-inflammatory drug (NSAID) which is known for its decreased risk of causing gastrointestinal bleeding compared to other NSAIDS.A181544 It is used to manage symptoms of various types of arthritis pain and in familial adenomatous polyposis (FAP) to reduce precancerous polyps in the colon.A181532 It is marketed by Pfizer under the brand name Celebrex, and was initially granted FDA approval in 1998.L7604

Interestingly, selective COX-2 inhibitors (especially celecoxib), have been evaluated as potential cancer chemopreventive and therapeutic drugs in clinical trials for a variety of malignancies.A34124

Struktur Molekul 2D

Berat 381.372
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The effective half-life of celecoxib is approximately 11 hours when a single 200 mg dose is given to healthy subjects.[L3296,L7646] The terminal half-life of celecoxib varies because of its low solubility, which prolongs absorption.[L7646]
Volume Distribusi The apparent volume of distribution of celecoxib at steady state (Vss/F) is about 429 L[L3296], which suggests wide distribution into various tissues. Celecoxib is not preferentially bound to red blood cells.[L7646] Another resource reports a volume of distribution of 455 ± 166L.[A4983]
Klirens (Clearance) Apparent clearance (CL/F), single oral 200 mg dose, healthy subjects = 27.7 L/hr.[L7646] Clearance may be decreased by about 47% in patients with chronic renal insufficiency, according to a pharmacokinetic study. Studies have not been performed in patients with severe renal impairment.[L7646]

Absorpsi

Celecoxib is absorbed rapidly in the gastrointestinal tract.A34124 When a single oral dose of 200 mg was given to healthy research subjects, the peak plasma levels of celecoxib occurred within 3 hours.A34124,L7646 The Cmax is 705 ng/mL.L3296 When multiple doses are given, steady-state concentrations are reached on or before day 5. When taken with a high-fat meal, peak plasma levels are delayed for about 1 to 2 hours with an increase in total absorption (AUC) of 10% to 20%.L7646 The AUC of celecoxib has been shown to be significantly lower in patients with chronic renal impairment.A4983,L7646 A meta-analysis of pharmacokinetic studies has suggested an approximately 40% higher AUC (area under the curve) of celecoxib in black patients compared to Caucasians for unknown reasons.L3296

Metabolisme

A large part of celecoxib metabolism is mediated by cytochrome P450 2C9 in the liver with some contribution from CYP3A4 and CYP2C8 and possible contributions from CYP2D6.A34124,A181379,A38563,T647 It is metabolized by biotransformation to carboxylic acid and glucuronide metabolites.A4983 Three metabolites, a primary alcohol, a carboxylic acid, and a glucuronide conjugate, have been found in human plasma after celecoxib administration.A34124 These are considered inactive metabolites in regards to COX enzyme inhibition. Patients who are known or suspected to have decreased cytochrome P450 2C9 activity or function, based on their previous history, should be administered celecoxib with caution as they may have abnormally high serum concentrations resulting from decreased metabolism celecoxib.L7646

Rute Eliminasi

Celecoxib is primarily eliminated by hepatic metabolism with small amounts (<3%) of the unchanged drug found in both the urine and feces.A4983 About 57% of an oral dose of celecoxib is excreted in the feces and 27% is found to be excreted into the urine in the form of metabolites. The main metabolite in urine and feces is identified as the carboxylic acid metabolite (73%). The amount of glucuronide in the urine is reported to be low.L7646

Farmakogenomik

1 Varian
CYP2C9 (rs1057910)

Patients with this genotype have reduced metabolism of celecoxib.

Interaksi Makanan

3 Data
  • 1. Avoid alcohol. Alcohol increases the risk of gastrointestinal irritation.
  • 2. Avoid multivalent ions. Separate the administration of aluminum and magnesium containing drugs by several hours.
  • 3. Take with or without food. Doses up to 200 mg can be taken without regard to food, but doses of 400mg or higher should be taken with food.

Interaksi Obat

1885 Data
Pravastatin Celecoxib may decrease the excretion rate of Pravastatin which could result in a higher serum level.
Atropine Celecoxib may decrease the excretion rate of Atropine which could result in a higher serum level.
Fluorescein Celecoxib may decrease the excretion rate of Fluorescein which could result in a higher serum level.
Disulfiram Celecoxib may decrease the excretion rate of Disulfiram which could result in a higher serum level.
Ezetimibe Celecoxib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Ofloxacin Celecoxib may decrease the excretion rate of Ofloxacin which could result in a higher serum level.
Glycochenodeoxycholic Acid Celecoxib may decrease the excretion rate of Glycochenodeoxycholic Acid which could result in a higher serum level.
Prasterone sulfate Celecoxib may decrease the excretion rate of Prasterone sulfate which could result in a higher serum level.
Indocyanine green acid form Celecoxib may decrease the excretion rate of Indocyanine green acid form which could result in a higher serum level.
Pilsicainide Celecoxib may decrease the excretion rate of Pilsicainide which could result in a higher serum level.
Dihydroergocristine Celecoxib may decrease the excretion rate of Dihydroergocristine which could result in a higher serum level.
Glycyrrhizic acid Celecoxib may decrease the excretion rate of Glycyrrhizic acid which could result in a higher serum level.
Cefaclor Celecoxib may decrease the excretion rate of Cefaclor which could result in a higher serum level.
Tinidazole Celecoxib may decrease the excretion rate of Tinidazole which could result in a higher serum level.
Fenofibrate Celecoxib may decrease the excretion rate of Fenofibrate which could result in a higher serum level.
Rosuvastatin Celecoxib may decrease the excretion rate of Rosuvastatin which could result in a higher serum level.
Flucloxacillin Celecoxib may decrease the excretion rate of Flucloxacillin which could result in a higher serum level.
Atorvastatin Celecoxib may decrease the excretion rate of Atorvastatin which could result in a higher serum level.
Belantamab mafodotin Celecoxib may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Celecoxib.
Eliglustat The metabolism of Celecoxib can be decreased when combined with Eliglustat.
Isoetharine The risk or severity of hypertension can be increased when Isoetharine is combined with Celecoxib.
Zolmitriptan The risk or severity of hypertension can be increased when Zolmitriptan is combined with Celecoxib.
Norepinephrine The risk or severity of hypertension can be increased when Norepinephrine is combined with Celecoxib.
Phenylephrine The risk or severity of hypertension can be increased when Phenylephrine is combined with Celecoxib.
Phenylpropanolamine The risk or severity of hypertension can be increased when Phenylpropanolamine is combined with Celecoxib.
Droperidol The risk or severity of hypertension can be increased when Droperidol is combined with Celecoxib.
Doxapram The risk or severity of hypertension can be increased when Celecoxib is combined with Doxapram.
Linezolid The risk or severity of hypertension can be increased when Celecoxib is combined with Linezolid.
Metaraminol The risk or severity of hypertension can be increased when Celecoxib is combined with Metaraminol.
Furazolidone The risk or severity of hypertension can be increased when Celecoxib is combined with Furazolidone.
Methoxamine The risk or severity of hypertension can be increased when Celecoxib is combined with Methoxamine.
Isoflurane The risk or severity of hypertension can be increased when Celecoxib is combined with Isoflurane.
Propiomazine The risk or severity of hypertension can be increased when Celecoxib is combined with Propiomazine.
Orciprenaline The risk or severity of hypertension can be increased when Celecoxib is combined with Orciprenaline.
Phenmetrazine The risk or severity of hypertension can be increased when Celecoxib is combined with Phenmetrazine.
Pseudoephedrine The risk or severity of hypertension can be increased when Celecoxib is combined with Pseudoephedrine.
Ritodrine The risk or severity of hypertension can be increased when Celecoxib is combined with Ritodrine.
Remifentanil The risk or severity of hypertension can be increased when Celecoxib is combined with Remifentanil.
Bitolterol The risk or severity of hypertension can be increased when Celecoxib is combined with Bitolterol.
Oxymetazoline The risk or severity of hypertension can be increased when Celecoxib is combined with Oxymetazoline.
Diethylpropion The risk or severity of hypertension can be increased when Celecoxib is combined with Diethylpropion.
Naratriptan The risk or severity of hypertension can be increased when Celecoxib is combined with Naratriptan.
Frovatriptan The risk or severity of hypertension can be increased when Celecoxib is combined with Frovatriptan.
Isoprenaline The risk or severity of hypertension can be increased when Celecoxib is combined with Isoprenaline.
Arbutamine The risk or severity of hypertension can be increased when Celecoxib is combined with Arbutamine.
Desflurane The risk or severity of hypertension can be increased when Celecoxib is combined with Desflurane.
Isocarboxazid The risk or severity of hypertension can be increased when Celecoxib is combined with Isocarboxazid.
Fenoterol The risk or severity of hypertension can be increased when Celecoxib is combined with Fenoterol.
Pirbuterol The risk or severity of hypertension can be increased when Celecoxib is combined with Pirbuterol.
Ephedra sinica root The risk or severity of hypertension can be increased when Celecoxib is combined with Ephedra sinica root.
Ephedrine The risk or severity of hypertension can be increased when Celecoxib is combined with Ephedrine.
Mephentermine The risk or severity of hypertension can be increased when Celecoxib is combined with Mephentermine.
Procaterol The risk or severity of hypertension can be increased when Celecoxib is combined with Procaterol.
Clenbuterol The risk or severity of hypertension can be increased when Celecoxib is combined with Clenbuterol.
Bambuterol The risk or severity of hypertension can be increased when Celecoxib is combined with Bambuterol.
MMDA The risk or severity of hypertension can be increased when Celecoxib is combined with MMDA.
2,5-Dimethoxy-4-ethylamphetamine The risk or severity of hypertension can be increased when Celecoxib is combined with 2,5-Dimethoxy-4-ethylamphetamine.
4-Bromo-2,5-dimethoxyamphetamine The risk or severity of hypertension can be increased when Celecoxib is combined with 4-Bromo-2,5-dimethoxyamphetamine.
Tenamfetamine The risk or severity of hypertension can be increased when Celecoxib is combined with Tenamfetamine.
Chlorphentermine The risk or severity of hypertension can be increased when Celecoxib is combined with Chlorphentermine.
Phendimetrazine The risk or severity of hypertension can be increased when Celecoxib is combined with Phendimetrazine.
Periciazine The risk or severity of hypertension can be increased when Celecoxib is combined with Periciazine.
Acepromazine The risk or severity of hypertension can be increased when Celecoxib is combined with Acepromazine.
Thioproperazine The risk or severity of hypertension can be increased when Celecoxib is combined with Thioproperazine.
Epicaptopril The risk or severity of hypertension can be increased when Celecoxib is combined with Epicaptopril.
Clorgiline The risk or severity of hypertension can be increased when Celecoxib is combined with Clorgiline.
1-benzylimidazole The risk or severity of hypertension can be increased when Celecoxib is combined with 1-benzylimidazole.
Nialamide The risk or severity of hypertension can be increased when Celecoxib is combined with Nialamide.
Amibegron The risk or severity of hypertension can be increased when Celecoxib is combined with Amibegron.
Naluzotan The risk or severity of hypertension can be increased when Celecoxib is combined with Naluzotan.
Pizotifen The risk or severity of hypertension can be increased when Celecoxib is combined with Pizotifen.
Solabegron The risk or severity of hypertension can be increased when Celecoxib is combined with Solabegron.
Xylometazoline The risk or severity of hypertension can be increased when Celecoxib is combined with Xylometazoline.
Dexmethylphenidate The risk or severity of hypertension can be increased when Celecoxib is combined with Dexmethylphenidate.
Levonordefrin The risk or severity of hypertension can be increased when Celecoxib is combined with Levonordefrin.
Naphazoline The risk or severity of hypertension can be increased when Celecoxib is combined with Naphazoline.
Tetryzoline The risk or severity of hypertension can be increased when Celecoxib is combined with Tetryzoline.
Cinitapride The risk or severity of hypertension can be increased when Celecoxib is combined with Cinitapride.
Tyramine The risk or severity of hypertension can be increased when Celecoxib is combined with Tyramine.
Adrafinil The risk or severity of hypertension can be increased when Celecoxib is combined with Adrafinil.
Isoxsuprine The risk or severity of hypertension can be increased when Celecoxib is combined with Isoxsuprine.
Ifenprodil The risk or severity of hypertension can be increased when Celecoxib is combined with Ifenprodil.
Hexoprenaline The risk or severity of hypertension can be increased when Celecoxib is combined with Hexoprenaline.
Etilefrine The risk or severity of hypertension can be increased when Celecoxib is combined with Etilefrine.
Cirazoline The risk or severity of hypertension can be increased when Celecoxib is combined with Cirazoline.
Synephrine The risk or severity of hypertension can be increased when Celecoxib is combined with Synephrine.
Hydracarbazine The risk or severity of hypertension can be increased when Celecoxib is combined with Hydracarbazine.
Benmoxin The risk or severity of hypertension can be increased when Celecoxib is combined with Benmoxin.
Mebanazine The risk or severity of hypertension can be increased when Celecoxib is combined with Mebanazine.
Octamoxin The risk or severity of hypertension can be increased when Celecoxib is combined with Octamoxin.
Pheniprazine The risk or severity of hypertension can be increased when Celecoxib is combined with Pheniprazine.
Phenoxypropazine The risk or severity of hypertension can be increased when Celecoxib is combined with Phenoxypropazine.
Pivhydrazine The risk or severity of hypertension can be increased when Celecoxib is combined with Pivhydrazine.
Safrazine The risk or severity of hypertension can be increased when Celecoxib is combined with Safrazine.
Caroxazone The risk or severity of hypertension can be increased when Celecoxib is combined with Caroxazone.
Doxofylline The risk or severity of hypertension can be increased when Celecoxib is combined with Doxofylline.
Iofetamine I-123 The risk or severity of hypertension can be increased when Celecoxib is combined with Iofetamine I-123.
Racepinephrine The risk or severity of hypertension can be increased when Celecoxib is combined with Racepinephrine.
Amitraz The risk or severity of hypertension can be increased when Celecoxib is combined with Amitraz.

Target Protein

Prostaglandin G/H synthase 2 PTGS2
Signal transducer and activator of transcription 3 STAT3
Sialidase-1 NEU1
Carbonic anhydrase 2 CA2
Carbonic anhydrase 3 CA3
Cadherin-11 CDH11
3-phosphoinositide-dependent protein kinase 1 PDPK1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 15208519
    Malhotra S, Shafiq N, Pandhi P: COX-2 inhibitors: a CLASS act or Just VIGORously promoted. MedGenMed. 2004 Mar 23;6(1):6.
  • PMID: 10979111
    Silverstein FE, Faich G, Goldstein JL, Simon LS, Pincus T, Whelton A, Makuch R, Eisen G, Agrawal NM, Stenson WF, Burr AM, Zhao WW, Kent JD, Lefkowith JB, Verburg KM, Geis GS: Gastrointestinal toxicity with celecoxib vs nonsteroidal anti-inflammatory drugs for osteoarthritis and rheumatoid arthritis: the CLASS study: A randomized controlled trial. Celecoxib Long-term Arthritis Safety Study. JAMA. 2000 Sep 13;284(10):1247-55.
  • PMID: 15713944
    Solomon SD, McMurray JJ, Pfeffer MA, Wittes J, Fowler R, Finn P, Anderson WF, Zauber A, Hawk E, Bertagnolli M: Cardiovascular risk associated with celecoxib in a clinical trial for colorectal adenoma prevention. N Engl J Med. 2005 Mar 17;352(11):1071-80. Epub 2005 Feb 15.
  • PMID: 16777855
    Yelland MJ, Nikles CJ, McNairn N, Del Mar CB, Schluter PJ, Brown RM: Celecoxib compared with sustained-release paracetamol for osteoarthritis: a series of n-of-1 trials. Rheumatology (Oxford). 2007 Jan;46(1):135-40. Epub 2006 Jun 15.
  • PMID: 16943400
    Bertagnolli MM, Eagle CJ, Zauber AG, Redston M, Solomon SD, Kim K, Tang J, Rosenstein RB, Wittes J, Corle D, Hess TM, Woloj GM, Boisserie F, Anderson WF, Viner JL, Bagheri D, Burn J, Chung DC, Dewar T, Foley TR, Hoffman N, Macrae F, Pruitt RE, Saltzman JR, Salzberg B, Sylwestrowicz T, Gordon GB, Hawk ET: Celecoxib for the prevention of sporadic colorectal adenomas. N Engl J Med. 2006 Aug 31;355(9):873-84.
  • PMID: 12392591
    Sandberg M, Yasar U, Stromberg P, Hoog JO, Eliasson E: Oxidation of celecoxib by polymorphic cytochrome P450 2C9 and alcohol dehydrogenase. Br J Clin Pharmacol. 2002 Oct;54(4):423-9.
  • PMID: 22336956
    Gong L, Thorn CF, Bertagnolli MM, Grosser T, Altman RB, Klein TE: Celecoxib pathways: pharmacokinetics and pharmacodynamics. Pharmacogenet Genomics. 2012 Apr;22(4):310-8. doi: 10.1097/FPC.0b013e32834f94cb.
  • PMID: 11566042
    Hawkey CJ: COX-1 and COX-2 inhibitors. Best Pract Res Clin Gastroenterol. 2001 Oct;15(5):801-20. doi: 10.1053/bega.2001.0236.
Menampilkan 8 dari 21 artikel.
Textbook
  • Brandon Cohen; Charles V. Preuss (2019). Celecoxib, NIH StatPearls. StatPearls.

Contoh Produk & Brand

Produk: 510 • International brands: 12
Produk
  • Accel-celecoxib
    Capsule • 100 mg • Oral • Canada • Generic • Approved
  • Accel-celecoxib
    Capsule • 200 mg • Oral • Canada • Generic • Approved
  • Act Celecoxib
    Capsule • 100 mg • Oral • Canada • Approved
  • Act Celecoxib
    Capsule • 200 mg • Oral • Canada • Approved
  • Ag-celecoxib
    Capsule • 100 mg • Oral • Canada • Generic • Approved
  • Ag-celecoxib
    Capsule • 200 mg • Oral • Canada • Generic • Approved
  • Apo-celecoxib
    Capsule • 100 mg • Oral • Canada • Generic • Approved
  • Apo-celecoxib
    Capsule • 200 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 510 produk.
International Brands
  • Articox — Keyfarm
  • Articoxib — Nabiqasim
  • Artiflex — Standpharm
  • Artilog — Pfizer
  • Artix — Pharmalab
  • Artrixib — Intipharma
  • Blockten — Infarmasa
  • Caditar — Farmindustria
  • Cefinix — Farmacoop
  • Celact — Sun

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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