Peringatan Keamanan

The symptoms of overdose are presented in individuals that consumed more than 99 mg/kg. Most common symptoms of overdose are abdominal pain, nausea, vomiting, lethargy, vertigo, drowsiness (somnolence), dizziness and insomnia. Other symptoms of overdose include headache, loss of consciousness, tinnitus, CNS depression, convulsions and seizures. May rarely cause metabolic acidosis, abnormal hepatic function, hyperkalemia, renal failure, dyspnea, respiratory depression, coma, acute renal failure, and apnea (primarily in very young pediatric patients).A39200

The reported LD50 of ibuprofen is of 636 mg/kg in rat, 740 mg/kg in mouse and 495 mg/kg in guinea pig.MSDS

Ibuprofen

DB01050

small molecule approved

Deskripsi

Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) derived from propionic acid and it is considered the first of the propionics.A39074 The formula of ibuprofen is 2-(4-isobutylphenyl) propionic acid and its initial development was in 1960 while researching for a safer alternative for aspirin.A39075 Ibuprofen was finally patented in 1961 and this drug was first launched against rheumatoid arthritis in the UK in 1969 and USA in 1974. It was the first available over-the-counter NSAID.A39076

On the available products, ibuprofen is administered as a racemic mixture. Once administered, the R-enantiomer undergoes extensive interconversion to the S-enantiomer in vivo by the activity of the alpha-methylacyl-CoA racemase. In particular, it is generally proposed that the S-enantiomer is capable of eliciting stronger pharmacological activity than the R-enantiomer.A39194

Struktur Molekul 2D

Berat 206.2808
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The serum half-life of ibuprofen is 1.2-2 hours.[A39092] In patients with a compromised liver function, the half-life can be prolonged to 3.1-3.4 hours.[A39190]
Volume Distribusi The apparent volume of distribution of ibuprofen is of 0.1 L/kg.[A39195]
Klirens (Clearance) The clearance rate ranges between 3-13 L/h depending on the route of administration, enantiomer type and dosage.[A39190]

Absorpsi

It is very well absorbed orally and the peak serum concentration can be attained in 1 to 2 hours after extravascular administration. When ibuprofen is administered immediately after a meal there is a slight reduction in the absorption rate but there is no change in the extent of the absorption.A39092 When orally administered, the absorption of ibuprofen in adults is very rapidly done in the upper GI tract.A39190 The average Cmax, Tmax and AUC ranges around 20 mcg/ml, 2 h and 70 mcg.h/ml. These parameters can vary depending on the enantiomer form, route, and dose of administration.A39190

Metabolisme

Ibuprofen is rapidly metabolized and biotransformed in the liver to the formation of major metabolites which are the hydroxylated and carboxylated derivatives.A39092 As soon as it is absorbed, the R-enantiomer undergoes extensive enantiomeric conversion (53-65%) to the more active S-enantiomer in vivo by the activity of alpha-methylacyl-CoA racemase.A39194 Ibuprofen metabolism can be divided in phase I which is represented by the hydroxylation of the isobutyl chains for the formation of 2 or 3-hydroxy derivatives followed by oxidation to 2-carboxy-ibuprofen and p-carboxy-2-propionate. These oxidative reactions are performed by the activity of the cytochrome P450 isoforms CYP 2C9, CYP 2C19 and CYP 2C8. Therefore, these enzymes participate in the oxidation of the alkyl side chain to hydroxyl and carboxyl derivatives. From this enzymes, the major catalyst in the formation of oxidative metabolites is the isoform CYP 2C9.A39190 The metabolic phase I is followed by a phase II in which the oxidative metabolites may be conjugated to glucuronide prior to excretion. This activity forms phenolic and acyl glucuronides.A39190

Rute Eliminasi

Ibuprofen is rapidly metabolized and eliminated in the urine thus, this via accounts for more than 90% of the administered dose. It is completely eliminated in 24 hours after the last dose and almost all the administered dose goes through metabolism, representing about 99% of the eliminated dose.A39092 The biliary excretion of unchanged drug and active phase II metabolites represents 1% of the administered dose.A39190 In summary, ibuprofen is excreted as metabolites or their conjugates. The elimination of ibuprofen is not impaired by old age or the presence of renal impairment.A39092

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with food. Food reduces irritation.

Interaksi Obat

1672 Data
Amlodipine The metabolism of Ibuprofen can be decreased when combined with Amlodipine.
Midodrine The risk or severity of hypertension can be increased when Midodrine is combined with Ibuprofen.
Isoetharine The risk or severity of hypertension can be increased when Isoetharine is combined with Ibuprofen.
Zolmitriptan The risk or severity of hypertension can be increased when Zolmitriptan is combined with Ibuprofen.
Norepinephrine The risk or severity of hypertension can be increased when Norepinephrine is combined with Ibuprofen.
Droperidol The risk or severity of hypertension can be increased when Droperidol is combined with Ibuprofen.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Ibuprofen.
Atropine The risk or severity of hypertension can be increased when Atropine is combined with Ibuprofen.
Linezolid The risk or severity of hypertension can be increased when Linezolid is combined with Ibuprofen.
Metaraminol The risk or severity of hypertension can be increased when Metaraminol is combined with Ibuprofen.
Furazolidone The risk or severity of hypertension can be increased when Furazolidone is combined with Ibuprofen.
Nicergoline The risk or severity of hypertension can be increased when Nicergoline is combined with Ibuprofen.
Methoxamine The risk or severity of hypertension can be increased when Methoxamine is combined with Ibuprofen.
Isoflurane The risk or severity of hypertension can be increased when Isoflurane is combined with Ibuprofen.
Propiomazine The risk or severity of hypertension can be increased when Propiomazine is combined with Ibuprofen.
Minaprine The risk or severity of hypertension can be increased when Minaprine is combined with Ibuprofen.
Orciprenaline The risk or severity of hypertension can be increased when Orciprenaline is combined with Ibuprofen.
Phenmetrazine The risk or severity of hypertension can be increased when Phenmetrazine is combined with Ibuprofen.
Ritodrine The risk or severity of hypertension can be increased when Ritodrine is combined with Ibuprofen.
Bitolterol The risk or severity of hypertension can be increased when Bitolterol is combined with Ibuprofen.
Oxymetazoline The risk or severity of hypertension can be increased when Oxymetazoline is combined with Ibuprofen.
Naratriptan The risk or severity of hypertension can be increased when Naratriptan is combined with Ibuprofen.
Frovatriptan The risk or severity of hypertension can be increased when Frovatriptan is combined with Ibuprofen.
Isoprenaline The risk or severity of hypertension can be increased when Ibuprofen is combined with Isoprenaline.
Arbutamine The risk or severity of hypertension can be increased when Ibuprofen is combined with Arbutamine.
Dutasteride The risk or severity of hypertension can be increased when Ibuprofen is combined with Dutasteride.
Desflurane The risk or severity of hypertension can be increased when Ibuprofen is combined with Desflurane.
Isocarboxazid The risk or severity of hypertension can be increased when Ibuprofen is combined with Isocarboxazid.
Fenoterol The risk or severity of hypertension can be increased when Ibuprofen is combined with Fenoterol.
Pirbuterol The risk or severity of hypertension can be increased when Ibuprofen is combined with Pirbuterol.
Ephedra sinica root The risk or severity of hypertension can be increased when Ibuprofen is combined with Ephedra sinica root.
Ephedrine The risk or severity of hypertension can be increased when Ibuprofen is combined with Ephedrine.
Procaterol The risk or severity of hypertension can be increased when Ibuprofen is combined with Procaterol.
Clenbuterol The risk or severity of hypertension can be increased when Ibuprofen is combined with Clenbuterol.
Bambuterol The risk or severity of hypertension can be increased when Ibuprofen is combined with Bambuterol.
4-Methoxyamphetamine The risk or severity of hypertension can be increased when Ibuprofen is combined with 4-Methoxyamphetamine.
Phendimetrazine The risk or severity of hypertension can be increased when Ibuprofen is combined with Phendimetrazine.
Epicaptopril The risk or severity of hypertension can be increased when Ibuprofen is combined with Epicaptopril.
Clorgiline The risk or severity of hypertension can be increased when Ibuprofen is combined with Clorgiline.
1-benzylimidazole The risk or severity of hypertension can be increased when Ibuprofen is combined with 1-benzylimidazole.
Nialamide The risk or severity of hypertension can be increased when Ibuprofen is combined with Nialamide.
Amibegron The risk or severity of hypertension can be increased when Ibuprofen is combined with Amibegron.
Naluzotan The risk or severity of hypertension can be increased when Ibuprofen is combined with Naluzotan.
Pizotifen The risk or severity of hypertension can be increased when Ibuprofen is combined with Pizotifen.
Solabegron The risk or severity of hypertension can be increased when Ibuprofen is combined with Solabegron.
Esmirtazapine The risk or severity of hypertension can be increased when Ibuprofen is combined with Esmirtazapine.
Nitrous oxide The risk or severity of hypertension can be increased when Ibuprofen is combined with Nitrous oxide.
Xylometazoline The risk or severity of hypertension can be increased when Ibuprofen is combined with Xylometazoline.
Dexmethylphenidate The risk or severity of hypertension can be increased when Ibuprofen is combined with Dexmethylphenidate.
Isometheptene The risk or severity of hypertension can be increased when Ibuprofen is combined with Isometheptene.
Levonordefrin The risk or severity of hypertension can be increased when Ibuprofen is combined with Levonordefrin.
Tetryzoline The risk or severity of hypertension can be increased when Ibuprofen is combined with Tetryzoline.
Cinitapride The risk or severity of hypertension can be increased when Ibuprofen is combined with Cinitapride.
Tyramine The risk or severity of hypertension can be increased when Ibuprofen is combined with Tyramine.
Adrafinil The risk or severity of hypertension can be increased when Ibuprofen is combined with Adrafinil.
Isoxsuprine The risk or severity of hypertension can be increased when Ibuprofen is combined with Isoxsuprine.
Ifenprodil The risk or severity of hypertension can be increased when Ibuprofen is combined with Ifenprodil.
Hexoprenaline The risk or severity of hypertension can be increased when Ibuprofen is combined with Hexoprenaline.
Etilefrine The risk or severity of hypertension can be increased when Ibuprofen is combined with Etilefrine.
Cirazoline The risk or severity of hypertension can be increased when Ibuprofen is combined with Cirazoline.
Synephrine The risk or severity of hypertension can be increased when Ibuprofen is combined with Synephrine.
Hydracarbazine The risk or severity of hypertension can be increased when Ibuprofen is combined with Hydracarbazine.
Benmoxin The risk or severity of hypertension can be increased when Ibuprofen is combined with Benmoxin.
Mebanazine The risk or severity of hypertension can be increased when Ibuprofen is combined with Mebanazine.
Octamoxin The risk or severity of hypertension can be increased when Ibuprofen is combined with Octamoxin.
Pheniprazine The risk or severity of hypertension can be increased when Ibuprofen is combined with Pheniprazine.
Phenoxypropazine The risk or severity of hypertension can be increased when Ibuprofen is combined with Phenoxypropazine.
Pivhydrazine The risk or severity of hypertension can be increased when Ibuprofen is combined with Pivhydrazine.
Safrazine The risk or severity of hypertension can be increased when Ibuprofen is combined with Safrazine.
Caroxazone The risk or severity of hypertension can be increased when Ibuprofen is combined with Caroxazone.
Doxofylline The risk or severity of hypertension can be increased when Ibuprofen is combined with Doxofylline.
Racepinephrine The risk or severity of hypertension can be increased when Ibuprofen is combined with Racepinephrine.
Amitraz The risk or severity of hypertension can be increased when Ibuprofen is combined with Amitraz.
Medetomidine The risk or severity of hypertension can be increased when Ibuprofen is combined with Medetomidine.
Atipamezole The risk or severity of hypertension can be increased when Ibuprofen is combined with Atipamezole.
Ractopamine The risk or severity of hypertension can be increased when Ibuprofen is combined with Ractopamine.
Romifidine The risk or severity of hypertension can be increased when Ibuprofen is combined with Romifidine.
Detomidine The risk or severity of hypertension can be increased when Ibuprofen is combined with Detomidine.
Tetrahydrocannabivarin The risk or severity of hypertension can be increased when Ibuprofen is combined with Tetrahydrocannabivarin.
PF-00610355 The risk or severity of hypertension can be increased when Ibuprofen is combined with PF-00610355.
Abediterol The risk or severity of hypertension can be increased when Ibuprofen is combined with Abediterol.
Tulobuterol The risk or severity of hypertension can be increased when Ibuprofen is combined with Tulobuterol.
Dopexamine The risk or severity of hypertension can be increased when Ibuprofen is combined with Dopexamine.
Piclozotan The risk or severity of hypertension can be increased when Ibuprofen is combined with Piclozotan.
Idazoxan The risk or severity of hypertension can be increased when Ibuprofen is combined with Idazoxan.
Higenamine The risk or severity of hypertension can be increased when Ibuprofen is combined with Higenamine.
Reproterol The risk or severity of hypertension can be increased when Ibuprofen is combined with Reproterol.
Theodrenaline The risk or severity of hypertension can be increased when Ibuprofen is combined with Theodrenaline.
Tramazoline The risk or severity of hypertension can be increased when Ibuprofen is combined with Tramazoline.
Octopamine The risk or severity of hypertension can be increased when Ibuprofen is combined with Octopamine.
Trichloroethylene The risk or severity of hypertension can be increased when Ibuprofen is combined with Trichloroethylene.
Fenozolone The risk or severity of hypertension can be increased when Ibuprofen is combined with Fenozolone.
Norfenefrine The risk or severity of hypertension can be increased when Ibuprofen is combined with Norfenefrine.
Oxyfedrine The risk or severity of hypertension can be increased when Ibuprofen is combined with Oxyfedrine.
Xenon The risk or severity of hypertension can be increased when Ibuprofen is combined with Xenon.
Metergoline The risk or severity of hypertension can be increased when Ibuprofen is combined with Metergoline.
Rimiterol The risk or severity of hypertension can be increased when Ibuprofen is combined with Rimiterol.
Tretoquinol The risk or severity of hypertension can be increased when Ibuprofen is combined with Tretoquinol.
Prenalterol The risk or severity of hypertension can be increased when Ibuprofen is combined with Prenalterol.
Xamoterol The risk or severity of hypertension can be increased when Ibuprofen is combined with Xamoterol.

Target Protein

Prostaglandin G/H synthase 2 PTGS2
C-X-C chemokine receptor type 2 CXCR2
Interleukin-8 CXCL8
C-X-C chemokine receptor type 1 CXCR1
Prostaglandin G/H synthase 1 PTGS1
Apoptosis regulator Bcl-2 BCL2
Thrombomodulin THBD
Fatty acid-binding protein, intestinal FABP2
Peroxisome proliferator-activated receptor gamma PPARG
Cystic fibrosis transmembrane conductance regulator CFTR
Peroxisome proliferator-activated receptor alpha PPARA
Platelet glycoprotein Ib alpha chain GP1BA
Protein S100-A7 S100A7

Referensi & Sumber

Artikel (PubMed)
  • PMID: 7041104
    Zawada ET Jr: Renal consequences of nonsteroidal antiinflammatory drugs. Postgrad Med. 1982 May;71(5):223-30.
  • PMID: 16195368
    Townsend KP, Pratico D: Novel therapeutic opportunities for Alzheimer's disease: focus on nonsteroidal anti-inflammatory drugs. FASEB J. 2005 Oct;19(12):1592-601.
  • PMID: 16240369
    Chen H, Jacobs E, Schwarzschild MA, McCullough ML, Calle EE, Thun MJ, Ascherio A: Nonsteroidal antiinflammatory drug use and the risk for Parkinson's disease. Ann Neurol. 2005 Dec;58(6):963-7.
  • PMID: 2777420
    Geisslinger G, Dietzel K, Bezler H, Nuernberg B, Brune K: Therapeutically relevant differences in the pharmacokinetical and pharmaceutical behavior of ibuprofen lysinate as compared to ibuprofen acid. Int J Clin Pharmacol Ther Toxicol. 1989 Jul;27(7):324-8.
  • PMID: 1531054
    Bergner T, Przybilla B: Photosensitization caused by ibuprofen. J Am Acad Dermatol. 1992 Jan;26(1):114-6.
  • PMID: 20089905
    Dill J, Patel AR, Yang XL, Bachoo R, Powell CM, Li S: A molecular mechanism for ibuprofen-mediated RhoA inhibition in neurons. J Neurosci. 2010 Jan 20;30(3):963-72. doi: 10.1523/JNEUROSCI.5045-09.2010.
  • PMID: 1569234
    Adams SS: The propionic acids: a personal perspective. J Clin Pharmacol. 1992 Apr;32(4):317-23.
  • PMID: 12723739
    Rainsford KD: Discovery, mechanisms of action and safety of ibuprofen. Int J Clin Pract Suppl. 2003 Apr;(135):3-8.
Menampilkan 8 dari 26 artikel.

Contoh Produk & Brand

Produk: 3002 • International brands: 89
Produk
  • 10 Person ANSI
    Kit • - • Ophthalmic; Oral; Topical • US • OTC
  • 24/7 Life IBUPROFEN
    Tablet, film coated • 200 mg/1 • Oral • US • Generic • OTC • Approved
  • 25 Person ANSI
    Kit • - • Ophthalmic; Oral; Topical • US • OTC
  • 365 Everyday Value Ibuprofen
    Tablet, film coated • 200 mg/1 • Oral • US • Generic • OTC • Approved
  • 365 Whole Foods Market Ibuprofen
    Tablet, film coated • 200 mg/1 • Oral • US • Generic • OTC • Approved
  • 4389 First Aid Kit
    Kit • - • Ophthalmic; Oral; Respiratory (inhalation); Topical • US • OTC
  • 4390 First Aid Kit
    Kit • - • Ophthalmic; Oral; Respiratory (inhalation); Topical • US • OTC
  • 4392 First Aid Kit
    Kit • - • Ophthalmic; Oral; Respiratory (inhalation); Topical • US • OTC
Menampilkan 8 dari 3002 produk.
International Brands
  • Act-3 — Healthcare Logistics
  • Actiprofen — Sterling Health
  • Adex — Dexxon
  • Aktren — Bayer
  • Alges-X — Axapharm
  • Algoflex — Chinoin
  • Algofren — Intermed
  • Alivium — Bristol-Myers Squibb
  • Artofen — Teva
  • Betagesic — Adcock Ingram Pharmaceuticals

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