Peringatan Keamanan

Some common adverse effects include gastro-intestinal disorders (dyspepsia, abdominal pain, nausea), rash, ruber, urticaria, symptoms of enuresis, headache, dizziness, and drowsiness L869. Oral LD50 value in rats is 130 mg/kg MSDS.

Aceclofenac

DB06736

small molecule approved investigational

Deskripsi

Aceclofenac is an oral non-steroidal anti-inflammatory drug (NSAID) with marked anti-inflammatory and analgesic properties used to treat osteoarthritis, rheumatoid arthritis and ankylosing spondylitis. It is reported to have a higher anti-inflammatory action or at least comparable effects than conventional NSAIDs in double-blind studies A19667, A19668, A19670. Aceclofenac potently inhibits the cyclo-oxygenase enzyme (COX) that is involved in the synthesis of prostaglandins, which are inflammatory mediators that cause pain, swelling, inflammation, and fever. Aceclofenac belongs to BCS Class II as it possesses poor aqueous solubility A19667. It displays high permeability to penetrate into synovial joints where in patients with osteoarthritis and related conditions, the loss of articular cartilage in the area causes joint pain, tenderness, stiffness, crepitus, and local inflammation A19666. Aceclofenac is also reported to be effective in other painful conditions such as dental and gynaecological conditions A19672. In 1991, aceclofenac was developed as an analog of a commonly prescribed NSAID, DB00586, via chemical modification in effort to improve the gastrointestinal tolerability of the drug. It is a more commonly prescribed drug in Europe.

Struktur Molekul 2D

Berat 354.18
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean plasma elimination half-life is approximately 4 hours [L868].
Volume Distribusi The volume of distribution is approximately 25 L [L868].
Klirens (Clearance) The mean clearance rate is approximately 5 L/h [A19674].

Absorpsi

Aceclofenac is rapidly and completely absorbed from the gastrointestinal tract and circulates mainly as unchanged drug following oral administration. Peak plasma concentrations are reached around 1.25 to 3 hours post-ingestion, and the drug penetrates into the synovial fluid where the concentration may reach up to 60% of that in the plasma L868. There is no accumulation in regular dosing, with similar maximum plasma concentration (Cmax) and time to reach peak plasma concentration (Tmax) after single and multiple doses A19667.

Metabolisme

4'-hydroxyaceclofenac is the main metabolite detected in plasma however other minor metabolites include diclofenac, 5-hydroxyaceclofenac, 5-hydroxydiclofenac, and 4'-hydroxydiclofenac A19667. It is probable that the metabolism of aceclofenac is mediated by CYP2C9 A19674.

Rute Eliminasi

The main route of elimination is via the urine where the elimination accounts for 70-80% of clearance of the drug A19667. Approximately two thirds of the administered dose is excreted via the urine, mainly as glucuronidated and hydroxylated forms of aceclofenac L868. About 20% of the dose is excreted into feces A19671.

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

1429 Data
Amlodipine Aceclofenac may decrease the antihypertensive activities of Amlodipine.
Phentermine The risk or severity of hypertension can be increased when Phentermine is combined with Aceclofenac.
Midodrine The risk or severity of hypertension can be increased when Midodrine is combined with Aceclofenac.
Isoetharine The risk or severity of hypertension can be increased when Isoetharine is combined with Aceclofenac.
Ziprasidone The risk or severity of hypertension can be increased when Ziprasidone is combined with Aceclofenac.
Methysergide The risk or severity of hypertension can be increased when Methysergide is combined with Aceclofenac.
Cabergoline The risk or severity of hypertension can be increased when Cabergoline is combined with Aceclofenac.
Zolmitriptan The risk or severity of hypertension can be increased when Zolmitriptan is combined with Aceclofenac.
Dihydroergotamine The risk or severity of hypertension can be increased when Dihydroergotamine is combined with Aceclofenac.
Methylergometrine The risk or severity of hypertension can be increased when Methylergometrine is combined with Aceclofenac.
Norepinephrine The risk or severity of hypertension can be increased when Norepinephrine is combined with Aceclofenac.
Mirtazapine The risk or severity of hypertension can be increased when Mirtazapine is combined with Aceclofenac.
Phenylephrine The risk or severity of hypertension can be increased when Phenylephrine is combined with Aceclofenac.
Phenylpropanolamine The risk or severity of hypertension can be increased when Phenylpropanolamine is combined with Aceclofenac.
Droperidol The risk or severity of hypertension can be increased when Droperidol is combined with Aceclofenac.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Aceclofenac.
Atropine The risk or severity of hypertension can be increased when Atropine is combined with Aceclofenac.
Lisuride The risk or severity of hypertension can be increased when Lisuride is combined with Aceclofenac.
Linezolid The risk or severity of hypertension can be increased when Linezolid is combined with Aceclofenac.
Metaraminol The risk or severity of hypertension can be increased when Metaraminol is combined with Aceclofenac.
Furazolidone The risk or severity of hypertension can be increased when Furazolidone is combined with Aceclofenac.
Thioridazine The risk or severity of hypertension can be increased when Thioridazine is combined with Aceclofenac.
Ergotamine The risk or severity of hypertension can be increased when Ergotamine is combined with Aceclofenac.
Nicergoline The risk or severity of hypertension can be increased when Nicergoline is combined with Aceclofenac.
Sufentanil The risk or severity of hypertension can be increased when Sufentanil is combined with Aceclofenac.
Methoxamine The risk or severity of hypertension can be increased when Methoxamine is combined with Aceclofenac.
Risperidone The risk or severity of hypertension can be increased when Risperidone is combined with Aceclofenac.
Isoflurane The risk or severity of hypertension can be increased when Isoflurane is combined with Aceclofenac.
Propiomazine The risk or severity of hypertension can be increased when Propiomazine is combined with Aceclofenac.
Alfentanil The risk or severity of hypertension can be increased when Alfentanil is combined with Aceclofenac.
Minaprine The risk or severity of hypertension can be increased when Minaprine is combined with Aceclofenac.
Orciprenaline The risk or severity of hypertension can be increased when Orciprenaline is combined with Aceclofenac.
Phenmetrazine The risk or severity of hypertension can be increased when Phenmetrazine is combined with Aceclofenac.
Trifluoperazine The risk or severity of hypertension can be increased when Trifluoperazine is combined with Aceclofenac.
Pseudoephedrine The risk or severity of hypertension can be increased when Pseudoephedrine is combined with Aceclofenac.
Benzphetamine The risk or severity of hypertension can be increased when Benzphetamine is combined with Aceclofenac.
Ritodrine The risk or severity of hypertension can be increased when Ritodrine is combined with Aceclofenac.
Flupentixol The risk or severity of hypertension can be increased when Flupentixol is combined with Aceclofenac.
Remifentanil The risk or severity of hypertension can be increased when Remifentanil is combined with Aceclofenac.
Bitolterol The risk or severity of hypertension can be increased when Bitolterol is combined with Aceclofenac.
Oxymetazoline The risk or severity of hypertension can be increased when Oxymetazoline is combined with Aceclofenac.
Diethylpropion The risk or severity of hypertension can be increased when Diethylpropion is combined with Aceclofenac.
Salmeterol The risk or severity of hypertension can be increased when Salmeterol is combined with Aceclofenac.
Naratriptan The risk or severity of hypertension can be increased when Naratriptan is combined with Aceclofenac.
Frovatriptan The risk or severity of hypertension can be increased when Frovatriptan is combined with Aceclofenac.
Ergoloid mesylate The risk or severity of hypertension can be increased when Ergoloid mesylate is combined with Aceclofenac.
Isoprenaline The risk or severity of hypertension can be increased when Isoprenaline is combined with Aceclofenac.
Arbutamine The risk or severity of hypertension can be increased when Arbutamine is combined with Aceclofenac.
Dutasteride The risk or severity of hypertension can be increased when Dutasteride is combined with Aceclofenac.
Pergolide The risk or severity of hypertension can be increased when Pergolide is combined with Aceclofenac.
Desflurane The risk or severity of hypertension can be increased when Desflurane is combined with Aceclofenac.
Bromocriptine The risk or severity of hypertension can be increased when Bromocriptine is combined with Aceclofenac.
Finasteride The risk or severity of hypertension can be increased when Finasteride is combined with Aceclofenac.
Aripiprazole The risk or severity of hypertension can be increased when Aripiprazole is combined with Aceclofenac.
Isocarboxazid The risk or severity of hypertension can be increased when Isocarboxazid is combined with Aceclofenac.
Ergometrine The risk or severity of hypertension can be increased when Ergometrine is combined with Aceclofenac.
Lisdexamfetamine The risk or severity of hypertension can be increased when Lisdexamfetamine is combined with Aceclofenac.
Fenoterol The risk or severity of hypertension can be increased when Fenoterol is combined with Aceclofenac.
Pirbuterol The risk or severity of hypertension can be increased when Pirbuterol is combined with Aceclofenac.
Ephedra sinica root The risk or severity of hypertension can be increased when Ephedra sinica root is combined with Aceclofenac.
Ephedrine The risk or severity of hypertension can be increased when Ephedrine is combined with Aceclofenac.
Mephentermine The risk or severity of hypertension can be increased when Mephentermine is combined with Aceclofenac.
Procaterol The risk or severity of hypertension can be increased when Procaterol is combined with Aceclofenac.
Yohimbine The risk or severity of hypertension can be increased when Yohimbine is combined with Aceclofenac.
Methotrimeprazine The risk or severity of hypertension can be increased when Methotrimeprazine is combined with Aceclofenac.
Clenbuterol The risk or severity of hypertension can be increased when Clenbuterol is combined with Aceclofenac.
Bambuterol The risk or severity of hypertension can be increased when Bambuterol is combined with Aceclofenac.
MMDA The risk or severity of hypertension can be increased when MMDA is combined with Aceclofenac.
Midomafetamine The risk or severity of hypertension can be increased when Midomafetamine is combined with Aceclofenac.
2,5-Dimethoxy-4-ethylamphetamine The risk or severity of hypertension can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Aceclofenac.
4-Methoxyamphetamine The risk or severity of hypertension can be increased when 4-Methoxyamphetamine is combined with Aceclofenac.
4-Bromo-2,5-dimethoxyamphetamine The risk or severity of hypertension can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Aceclofenac.
Tenamfetamine The risk or severity of hypertension can be increased when Tenamfetamine is combined with Aceclofenac.
Chlorphentermine The risk or severity of hypertension can be increased when Chlorphentermine is combined with Aceclofenac.
Dextroamphetamine The risk or severity of hypertension can be increased when Dextroamphetamine is combined with Aceclofenac.
Phendimetrazine The risk or severity of hypertension can be increased when Phendimetrazine is combined with Aceclofenac.
Solifenacin The risk or severity of hypertension can be increased when Solifenacin is combined with Aceclofenac.
Periciazine The risk or severity of hypertension can be increased when Periciazine is combined with Aceclofenac.
Acepromazine The risk or severity of hypertension can be increased when Acepromazine is combined with Aceclofenac.
Thioproperazine The risk or severity of hypertension can be increased when Thioproperazine is combined with Aceclofenac.
Zuclopenthixol The risk or severity of hypertension can be increased when Zuclopenthixol is combined with Aceclofenac.
Epicaptopril The risk or severity of hypertension can be increased when Epicaptopril is combined with Aceclofenac.
Clorgiline The risk or severity of hypertension can be increased when Clorgiline is combined with Aceclofenac.
1-benzylimidazole The risk or severity of hypertension can be increased when 1-benzylimidazole is combined with Aceclofenac.
Nialamide The risk or severity of hypertension can be increased when Nialamide is combined with Aceclofenac.
Lysergic acid diethylamide The risk or severity of hypertension can be increased when Lysergic acid diethylamide is combined with Aceclofenac.
Dronedarone The risk or severity of hypertension can be increased when Dronedarone is combined with Aceclofenac.
Flibanserin The risk or severity of hypertension can be increased when Flibanserin is combined with Aceclofenac.
Iloperidone The risk or severity of hypertension can be increased when Iloperidone is combined with Aceclofenac.
Indacaterol The risk or severity of hypertension can be increased when Indacaterol is combined with Aceclofenac.
Rotigotine The risk or severity of hypertension can be increased when Rotigotine is combined with Aceclofenac.
Amibegron The risk or severity of hypertension can be increased when Amibegron is combined with Aceclofenac.
Naluzotan The risk or severity of hypertension can be increased when Naluzotan is combined with Aceclofenac.
Cariprazine The risk or severity of hypertension can be increased when Cariprazine is combined with Aceclofenac.
Mianserin The risk or severity of hypertension can be increased when Mianserin is combined with Aceclofenac.
Pizotifen The risk or severity of hypertension can be increased when Pizotifen is combined with Aceclofenac.
Solabegron The risk or severity of hypertension can be increased when Solabegron is combined with Aceclofenac.
Asenapine The risk or severity of hypertension can be increased when Asenapine is combined with Aceclofenac.
Esmirtazapine The risk or severity of hypertension can be increased when Esmirtazapine is combined with Aceclofenac.
Vilazodone The risk or severity of hypertension can be increased when Vilazodone is combined with Aceclofenac.

Target Protein

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

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25045671
    Raza K, Kumar M, Kumar P, Malik R, Sharma G, Kaur M, Katare OP: Topical delivery of aceclofenac: challenges and promises of novel drug delivery systems. Biomed Res Int. 2014;2014:406731. doi: 10.1155/2014/406731. Epub 2014 Jun 18.
  • PMID: 15163279
    Legrand E: Aceclofenac in the management of inflammatory pain. Expert Opin Pharmacother. 2004 Jun;5(6):1347-57.
  • PMID: 23581533
    Pareek A, Chandurkar N: Comparison of gastrointestinal safety and tolerability of aceclofenac with diclofenac: a multicenter, randomized, double-blind study in patients with knee osteoarthritis. Curr Med Res Opin. 2013 Jul;29(7):849-59. doi: 10.1185/03007995.2013.795139. Epub 2013 Apr 30.
  • PMID: 19588436
    Moore RA, Derry S, McQuay HJ: Single dose oral aceclofenac for postoperative pain in adults. Cochrane Database Syst Rev. 2009 Jul 8;(3):CD007588. doi: 10.1002/14651858.CD007588.pub2.
  • PMID: 21277837
    Pareek A, Chandurkar N, Gupta A, Sirsikar A, Dalal B, Jesalpura B, Mehrotra A, Mukherjee A: Efficacy and safety of aceclofenac-cr and aceclofenac in the treatment of knee osteoarthritis: a 6-week, comparative, randomized, multicentric, double-blind study. J Pain. 2011 May;12(5):546-53. doi: 10.1016/j.jpain.2010.10.013. Epub 2011 Feb 1.
  • PMID: 8799688
    Brogden RN, Wiseman LR: Aceclofenac. A review of its pharmacodynamic properties and therapeutic potential in the treatment of rheumatic disorders and in pain management. Drugs. 1996 Jul;52(1):113-24. doi: 10.2165/00003495-199652010-00008.
  • PMID: 11511027
    Dooley M, Spencer CM, Dunn CJ: Aceclofenac: a reappraisal of its use in the management of pain and rheumatic disease. Drugs. 2001;61(9):1351-78.
  • PMID: 8730134
    Gonzalez-Alvaro I, Carmona L, Diaz-Gonzalez F, Gonzalez-Amaro R, Mollinedo F, Sanchez-Madrid F, Laffon A, Garcia-Vicuna R: Aceclofenac, a new nonsteroidal antiinflammatory drug, decreases the expression and function of some adhesion molecules on human neutrophils. J Rheumatol. 1996 Apr;23(4):723-9.
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Contoh Produk & Brand

Produk: 1 • International brands: 3
Produk
  • Clanza CR
    Tablet, film coated • 200 mg/1 • Oral • US
International Brands
  • Cincofen
  • Clanza
  • Hifenac

Sekuens Gen/Protein (FASTA)

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