Peringatan Keamanan

Symptoms of overdose include lethargy, drowsiness, nausea, vomiting, and epigastric pain, and gastrointestinal bleeding.label Hypertension, acute renal failure, respiratory depression and coma occur rarely. In case of overdose, provide supportive care and consider inducing emesis and administering activated charcoal if overdose occurred less than 4 hours prior.

Diclofenac

DB00586

small molecule approved vet_approved

Deskripsi

Diclofenac is a phenylacetic acid derivative and non-steroidal anti-inflammatory drug (NSAID).label NSAIDs inhibit cyclooxygenase (COX)-1 and-2 which are the enzyme responsible for producing prostaglandins (PGs). PGs contribute to inflammation and pain signalling. Diclofenac, like other NSAIDs, is often used as first line therapy for acute and chronic pain and inflammation from a variety of causes. Diclofenac was the product of rational drug design based on the structures of phenylbutazone, mefenamic acid, and indomethacin.A180796 The addition of two chlorine groups in the ortho position of the phenyl ring locks the ring in maximal torsion which appears to be related to increased potency. It is often used in combination with misoprostol to prevent NSAID-induced gastric ulcers. Diclofenac was first approved by the FDA in July 1988 under the trade name Voltaren, marketed by Novartis (previously Ciba-Geigy).L7360

Struktur Molekul 2D

Berat 296.149
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal half-life of diclofenac is approximately 2 h, however the apparent half-life including all metabolites is 25.8-33 h.[label,A180694]
Volume Distribusi Diclofenac has a total volume of distribution of 5-10 L or 0.1-0.2 L/kg.[A178633] The volume of the central compartment is 0.04 L/kg.[A180694] Diclofenac distributes to the synovial fluid reaching peak concentration 2-4h after administration.[A178633] There is limited crossing of the blood brain barrier and cerebrospinal fluid concentrations only reach 8.22% of plasma concentrations. Doses of 50 mg delivered via intramuscular injection produced no detectable diclofenac concentrations in breast milk, however metabolite concentrations were not investigated. Diclofenac has been shown to cross the placenta in mice and rats but human data is unavailable.[A180694]
Klirens (Clearance) Diclofenac has a plasma clearance 16 L/h.[A180694]

Absorpsi

Diclofenac is completely absorbed from the GI tract but likely undergoes significant first pass metabolism with only 60% of the drug reaching systemic circulation unchanged label,A178633,A180694. Many topical formulations are absorbed percutaneous and produce clinically significant plasma concentrations. Absorption is dose proportional over the range of 25-150 mg.A178633 Tmax varies between formulations with the oral solution reaching peak plasma concentrations in 10-40min, the enteric coated tablet in 1.5-2h, and the sustained- and extended-release formulations prolonging Tmax even further. Administration with food has no significant effects on AUC but does delay Tmax to 2.5-12h.A178633,A180694

Metabolisme

Diclofenac undergoes oxidative metabolism to hydroxy metabolites as well as conjugation to glucuronic acid, sulfate, and taurine.label,A178633 The primary metabolite is 4'-hydroxy diclofenac which is generated by CYP2C9. This metabolite is very weakly active with one thirtieth the activity of diclofenac. Other metabolites include 3'-hydroxy diclofenac, 3'-hydroxy-4'methoxy diclofenac, 4',5-dihydroxy diclofenac, an acylglucuronide conjugate, and other conjugate metabolites.

Rute Eliminasi

Diclofenac is mainly eliminated via metabolism.A178633,A180694 Of the total dose, 60-70% is eliminated in the urine and 30% is eliminated in the feces. No significant enterohepatic recycling occurs.

Interaksi Makanan

2 Data
  • 1. Avoid excessive or chronic alcohol consumption. Co-administration with alcohol may increase the risk of gastrointestinal side effects, such as ulceration.
  • 2. Take with food. Food reduces gastric irritation.

Interaksi Obat

1852 Data
Reserpine Reserpine may decrease the excretion rate of Diclofenac which could result in a higher serum level.
Progesterone Progesterone may decrease the excretion rate of Diclofenac which could result in a higher serum level.
Chlorpromazine Chlorpromazine may decrease the excretion rate of Diclofenac which could result in a higher serum level.
Cimetidine Cimetidine may decrease the excretion rate of Diclofenac which could result in a higher serum level.
Bosentan Bosentan may decrease the excretion rate of Diclofenac which could result in a higher serum level.
Glyburide Glyburide may decrease the excretion rate of Diclofenac which could result in a higher serum level.
Ursodeoxycholic acid Ursodeoxycholic acid may decrease the excretion rate of Diclofenac which could result in a higher serum level.
Cholic Acid Cholic Acid may decrease the excretion rate of Diclofenac which could result in a higher serum level.
Fusidic acid Fusidic acid may decrease the excretion rate of Diclofenac which could result in a higher serum level.
Simeprevir Simeprevir may decrease the excretion rate of Diclofenac which could result in a higher serum level.
Lenvatinib Lenvatinib may decrease the excretion rate of Diclofenac which could result in a higher serum level.
Letermovir The metabolism of Diclofenac can be decreased when combined with Letermovir.
Valinomycin Valinomycin may decrease the excretion rate of Diclofenac which could result in a higher serum level.
Erythromycin The serum concentration of Diclofenac can be increased when it is combined with Erythromycin.
Pralsetinib Pralsetinib may decrease the excretion rate of Diclofenac which could result in a higher serum level.
Peginterferon alfa-2b The serum concentration of Diclofenac can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Diclofenac can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Diclofenac can be decreased when it is combined with Teriflunomide.
Amlodipine The metabolism of Diclofenac can be decreased when combined with Amlodipine.
Midodrine The risk or severity of hypertension can be increased when Midodrine is combined with Diclofenac.
Isoetharine The risk or severity of hypertension can be increased when Isoetharine is combined with Diclofenac.
Norepinephrine The risk or severity of hypertension can be increased when Norepinephrine is combined with Diclofenac.
Phenylpropanolamine The risk or severity of hypertension can be increased when Phenylpropanolamine is combined with Diclofenac.
Droperidol The risk or severity of hypertension can be increased when Droperidol is combined with Diclofenac.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Diclofenac.
Linezolid The risk or severity of hypertension can be increased when Diclofenac is combined with Linezolid.
Metaraminol The risk or severity of hypertension can be increased when Diclofenac is combined with Metaraminol.
Furazolidone The risk or severity of hypertension can be increased when Diclofenac is combined with Furazolidone.
Nicergoline The risk or severity of hypertension can be increased when Diclofenac is combined with Nicergoline.
Methoxamine The risk or severity of hypertension can be increased when Diclofenac is combined with Methoxamine.
Propiomazine The risk or severity of hypertension can be increased when Diclofenac is combined with Propiomazine.
Minaprine The risk or severity of hypertension can be increased when Diclofenac is combined with Minaprine.
Orciprenaline The risk or severity of hypertension can be increased when Diclofenac is combined with Orciprenaline.
Phenmetrazine The risk or severity of hypertension can be increased when Diclofenac is combined with Phenmetrazine.
Pseudoephedrine The risk or severity of hypertension can be increased when Diclofenac is combined with Pseudoephedrine.
Ritodrine The risk or severity of hypertension can be increased when Diclofenac is combined with Ritodrine.
Remifentanil The risk or severity of hypertension can be increased when Diclofenac is combined with Remifentanil.
Bitolterol The risk or severity of hypertension can be increased when Diclofenac is combined with Bitolterol.
Oxymetazoline The risk or severity of hypertension can be increased when Diclofenac is combined with Oxymetazoline.
Diethylpropion The risk or severity of hypertension can be increased when Diclofenac is combined with Diethylpropion.
Naratriptan The risk or severity of hypertension can be increased when Diclofenac is combined with Naratriptan.
Isoprenaline The risk or severity of hypertension can be increased when Diclofenac is combined with Isoprenaline.
Arbutamine The risk or severity of hypertension can be increased when Diclofenac is combined with Arbutamine.
Desflurane The risk or severity of hypertension can be increased when Diclofenac is combined with Desflurane.
Isocarboxazid The risk or severity of hypertension can be increased when Diclofenac is combined with Isocarboxazid.
Lisdexamfetamine The risk or severity of hypertension can be increased when Diclofenac is combined with Lisdexamfetamine.
Fenoterol The risk or severity of hypertension can be increased when Diclofenac is combined with Fenoterol.
Pirbuterol The risk or severity of hypertension can be increased when Diclofenac is combined with Pirbuterol.
Ephedra sinica root The risk or severity of hypertension can be increased when Diclofenac is combined with Ephedra sinica root.
Ephedrine The risk or severity of hypertension can be increased when Diclofenac is combined with Ephedrine.
Mephentermine The risk or severity of hypertension can be increased when Diclofenac is combined with Mephentermine.
Procaterol The risk or severity of hypertension can be increased when Diclofenac is combined with Procaterol.
Methotrimeprazine The risk or severity of hypertension can be increased when Diclofenac is combined with Methotrimeprazine.
Clenbuterol The risk or severity of hypertension can be increased when Diclofenac is combined with Clenbuterol.
Bambuterol The risk or severity of hypertension can be increased when Diclofenac is combined with Bambuterol.
MMDA The risk or severity of hypertension can be increased when Diclofenac is combined with MMDA.
Midomafetamine The risk or severity of hypertension can be increased when Diclofenac is combined with Midomafetamine.
2,5-Dimethoxy-4-ethylamphetamine The risk or severity of hypertension can be increased when Diclofenac is combined with 2,5-Dimethoxy-4-ethylamphetamine.
4-Methoxyamphetamine The risk or severity of hypertension can be increased when Diclofenac is combined with 4-Methoxyamphetamine.
4-Bromo-2,5-dimethoxyamphetamine The risk or severity of hypertension can be increased when Diclofenac is combined with 4-Bromo-2,5-dimethoxyamphetamine.
Tenamfetamine The risk or severity of hypertension can be increased when Diclofenac is combined with Tenamfetamine.
Chlorphentermine The risk or severity of hypertension can be increased when Diclofenac is combined with Chlorphentermine.
Dextroamphetamine The risk or severity of hypertension can be increased when Diclofenac is combined with Dextroamphetamine.
Phendimetrazine The risk or severity of hypertension can be increased when Diclofenac is combined with Phendimetrazine.
Periciazine The risk or severity of hypertension can be increased when Diclofenac is combined with Periciazine.
Acepromazine The risk or severity of hypertension can be increased when Diclofenac is combined with Acepromazine.
Thioproperazine The risk or severity of hypertension can be increased when Diclofenac is combined with Thioproperazine.
Epicaptopril The risk or severity of hypertension can be increased when Diclofenac is combined with Epicaptopril.
Clorgiline The risk or severity of hypertension can be increased when Diclofenac is combined with Clorgiline.
1-benzylimidazole The risk or severity of hypertension can be increased when Diclofenac is combined with 1-benzylimidazole.
Nialamide The risk or severity of hypertension can be increased when Diclofenac is combined with Nialamide.
Amibegron The risk or severity of hypertension can be increased when Diclofenac is combined with Amibegron.
Naluzotan The risk or severity of hypertension can be increased when Diclofenac is combined with Naluzotan.
Pizotifen The risk or severity of hypertension can be increased when Diclofenac is combined with Pizotifen.
Solabegron The risk or severity of hypertension can be increased when Diclofenac is combined with Solabegron.
Esmirtazapine The risk or severity of hypertension can be increased when Diclofenac is combined with Esmirtazapine.
Nitrous oxide The risk or severity of hypertension can be increased when Diclofenac is combined with Nitrous oxide.
Xylometazoline The risk or severity of hypertension can be increased when Diclofenac is combined with Xylometazoline.
Dexmethylphenidate The risk or severity of hypertension can be increased when Diclofenac is combined with Dexmethylphenidate.
Isometheptene The risk or severity of hypertension can be increased when Diclofenac is combined with Isometheptene.
Levonordefrin The risk or severity of hypertension can be increased when Diclofenac is combined with Levonordefrin.
Naphazoline The risk or severity of hypertension can be increased when Diclofenac is combined with Naphazoline.
Tetryzoline The risk or severity of hypertension can be increased when Diclofenac is combined with Tetryzoline.
Cinitapride The risk or severity of hypertension can be increased when Diclofenac is combined with Cinitapride.
Tyramine The risk or severity of hypertension can be increased when Diclofenac is combined with Tyramine.
Adrafinil The risk or severity of hypertension can be increased when Diclofenac is combined with Adrafinil.
Isoxsuprine The risk or severity of hypertension can be increased when Diclofenac is combined with Isoxsuprine.
Ifenprodil The risk or severity of hypertension can be increased when Diclofenac is combined with Ifenprodil.
Hexoprenaline The risk or severity of hypertension can be increased when Diclofenac is combined with Hexoprenaline.
Etilefrine The risk or severity of hypertension can be increased when Diclofenac is combined with Etilefrine.
Cirazoline The risk or severity of hypertension can be increased when Diclofenac is combined with Cirazoline.
Synephrine The risk or severity of hypertension can be increased when Diclofenac is combined with Synephrine.
Hydracarbazine The risk or severity of hypertension can be increased when Diclofenac is combined with Hydracarbazine.
Benmoxin The risk or severity of hypertension can be increased when Diclofenac is combined with Benmoxin.
Mebanazine The risk or severity of hypertension can be increased when Diclofenac is combined with Mebanazine.
Octamoxin The risk or severity of hypertension can be increased when Diclofenac is combined with Octamoxin.
Pheniprazine The risk or severity of hypertension can be increased when Diclofenac is combined with Pheniprazine.
Phenoxypropazine The risk or severity of hypertension can be increased when Diclofenac is combined with Phenoxypropazine.
Pivhydrazine The risk or severity of hypertension can be increased when Diclofenac is combined with Pivhydrazine.
Safrazine The risk or severity of hypertension can be increased when Diclofenac is combined with Safrazine.

Target Protein

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

Referensi & Sumber

Synthesis reference: Takuzo Kamishita, "Gel preparations for topical application of diclofenac sodium." U.S. Patent US4670254, issued October, 1983.
Artikel (PubMed)
  • PMID: 16740558
    Kearney PM, Baigent C, Godwin J, Halls H, Emberson JR, Patrono C: Do selective cyclo-oxygenase-2 inhibitors and traditional non-steroidal anti-inflammatory drugs increase the risk of atherothrombosis? Meta-analysis of randomised trials. BMJ. 2006 Jun 3;332(7553):1302-8.
  • PMID: 16645966
    Solomon DH, Avorn J, Sturmer T, Glynn RJ, Mogun H, Schneeweiss S: Cardiovascular outcomes in new users of coxibs and nonsteroidal antiinflammatory drugs: high-risk subgroups and time course of risk. Arthritis Rheum. 2006 May;54(5):1378-89.
  • PMID: 11496855
    FitzGerald GA, Patrono C: The coxibs, selective inhibitors of cyclooxygenase-2. N Engl J Med. 2001 Aug 9;345(6):433-42.
  • PMID: 16968830
    Graham DJ: COX-2 inhibitors, other NSAIDs, and cardiovascular risk: the seduction of common sense. JAMA. 2006 Oct 4;296(13):1653-6. Epub 2006 Sep 12.
  • PMID: 11992745
    Brater DC: Renal effects of cyclooxygyenase-2-selective inhibitors. J Pain Symptom Manage. 2002 Apr;23(4 Suppl):S15-20; discussion S21-3.
  • PMID: 20470236
    Gan TJ: Diclofenac: an update on its mechanism of action and safety profile. Curr Med Res Opin. 2010 Jul;26(7):1715-31. doi: 10.1185/03007995.2010.486301.
  • PMID: 9314611
    Davies NM, Anderson KE: Clinical pharmacokinetics of diclofenac. Therapeutic insights and pitfalls. Clin Pharmacokinet. 1997 Sep;33(3):184-213. doi: 10.2165/00003088-199733030-00003.
  • PMID: 3286213
    Todd PA, Sorkin EM: Diclofenac sodium. A reappraisal of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy. Drugs. 1988 Mar;35(3):244-85. doi: 10.2165/00003495-198835030-00004.
Menampilkan 8 dari 16 artikel.
Textbook
  • ISBN: 978-1-25-958473-2
    Brunton LL, Hilal-Dandan R, Knollmann BC. eds (2018). Goodman & Gilman's: The Pharmacological Basis of Therapeutics (13th ed.). McGraw-Hill Education.

Contoh Produk & Brand

Produk: 1054 • International brands: 9
Produk
  • Act Diclo-miso
    Tablet, delayed release • - • Oral • Canada • Approved
  • Act Diclo-miso
    Tablet, delayed release • - • Oral • Canada • Approved
  • Aleve Arthritis Pain Gel
    Gel • 1 mg/1g • Topical • US • Generic • OTC • Approved
  • Amazon Basic Care Arthritis Pain
    Gel • 10 mg/1g • Topical • US • Generic • OTC • Approved
  • Ambator Diclofenac Patch
    Patch • 1 g/10mL • Topical • US
  • Apo-diclo
    Tablet, delayed release • 25 mg • Oral • Canada • Generic • Approved
  • Apo-diclo
    Tablet, delayed release • 50 mg • Oral • Canada • Generic • Approved
  • Apo-diclo Rapide 50 Mg Tablets
    Tablet • 50 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 1054 produk.
International Brands
  • Aclonac
  • Allvoran
  • Ecofenac
  • Effekton
  • Nu-Diclo
  • Primofenac
  • Prophenatin
  • Rhumalgan
  • Voltarol

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