Allvoran;Apo-Diclo;Assaren;Benfofen;Cataflam;Delphimix;Dichlofenac;Dichronic;Diclo-Phlogont;Diclo-Puren;Diclobenin;Diclord;Dicloreum;Dolobasan;Duravolten;Dyloject;Ecofenac;Effekton;Kriplex;Neriodin;Novapirina;Novo-Difenac;Novo-Difenac SR;Nu-Diclo;Pennsaid;Primofenac;Prophenatin;ProSorb-D;Rhumalgan;Solaraze;Solaraze T;Tsudohmin;Valetan;Voldal;Voltaren;Voltaren Ophtha;Voltaren Ophthalmic;Voltaren Rapide;Voltaren SR;Voltaren-XR;Voltarol;Xenid;

Diclofenac Acid;Diclofenac Potassium;Diclofenac Sodium;ISV-205;

A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt. [PubChem]

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Synthesis Reference

Not Available

General Reference

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. Pubmed 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. Pubmed FitzGerald GA, Patrono C: The coxibs, selective inhibitors of cyclooxygenase-2. N Engl J Med. 2001 Aug 9;345(6):433-42. Pubmed 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. Pubmed Brater DC: Renal effects of cyclooxygyenase-2-selective inhibitors. J Pain Symptom Manage. 2002 Apr;23(4 Suppl):S15-20; discussion S21-3. Pubmed Sigma Aldrich Link Gan TJ: Diclofenac: an update on its mechanism of action and safety profile. Curr Med Res Opin. 2010 Jul;26(7):1715-31. Pubmed

Form	Route	Strength
Solution	Ophthalmic
Solution	Topical
Suppository	Rectal
Tablet	Oral
Tablet, coated	Oral
Tablet, extended release	Oral

Unit description	Cost	Unit
Voltaren Ophtha 0.1 % Solution	2.73 USD	ml
Voltaren 100 mg Suppository	1.88 USD	suppository
Voltaren Sr 100 mg Sustained-Release Tablet	1.86 USD	tablet
Voltaren 50 mg Suppository	1.4 USD	suppository
Voltaren Sr 75 mg Sustained-Release Tablet	1.31 USD	tablet
Voltaren 50 mg Enteric-Coated Tablet	0.93 USD	tablet
Pms-Diclofenac 100 mg Suppository	0.88 USD	suppository
Sandoz Diclofenac 100 mg Suppository	0.88 USD	suppository
Novo-Difenac Sr 100 mg Sustained-Release Tablet	0.8 USD	tablet
Pms-Diclofenac-Sr 100 mg Sustained-Release Tablet	0.8 USD	tablet
Sandoz Diclofenac Sr 100 mg Sustained-Release Tablet	0.8 USD	tablet
Pms-Diclofenac 50 mg Suppository	0.65 USD	suppository
Sandoz Diclofenac 50 mg Suppository	0.65 USD	suppository
Novo-Difenac Sr 75 mg Sustained-Release Tablet	0.6 USD	tablet
Pms-Diclofenac-Sr 75 mg Sustained-Release Tablet	0.6 USD	tablet
Sandoz Diclofenac Sr 75 mg Sustained-Release Tablet	0.6 USD	tablet
Apo-Diclo 50 mg Enteric-Coated Tablet	0.4 USD	tablet
Novo-Difenac 50 mg Enteric-Coated Tablet	0.4 USD	tablet
Pms-Diclofenac 50 mg Enteric-Coated Tablet	0.4 USD	tablet
Sandoz Diclofenac 50 mg Enteric-Coated Tablet	0.4 USD	tablet
Apo-Diclo 25 mg Enteric-Coated Tablet	0.2 USD	tablet
Novo-Difenac 25 mg Enteric-Coated Tablet	0.2 USD	tablet
Nu-Diclo 25 mg Enteric-Coated Tablet	0.2 USD	tablet
Pms-Diclofenac 25 mg Enteric-Coated Tablet	0.2 USD	tablet
Sandoz Diclofenac 25 mg Enteric-Coated Tablet	0.2 USD	tablet

Type	small molecule

Classes

Aminobenzoates Phenylacetates

Substructures

Aminobenzoates Hydroxy Compounds Acetates Aliphatic and Aryl Amines Carboxylic Acids and Derivatives Phenylacetates Benzene and Derivatives Aryl Halides Halobenzenes Aromatic compounds Anilines

ANTIINFLAMMATORY AND ANTIRHEUMATIC 消炎抗风湿;

Indication	For the acute and chronic treatment of signs and symptoms of osteoarthritis and rheumatoid arthritis.
Pharmacodynamics	Diclofenac is an acetic acid nonsteroidal antiinflammatory drug (NSAID) with analgesic and antipyretic properties. Diclofenac is used to treat pain, dysmenorrhea, ocular inflammation, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and actinic keratosis
Mechanism of action	The antiinflammatory effects of diclofenac are believed to be due to inhibition of both leukocyte migration and the enzyme cylooxygenase (COX-1 and COX-2), leading to the peripheral inhibition of prostaglandin synthesis. As prostaglandins sensitize pain receptors, inhibition of their synthesis is responsible for the analgesic effects of diclofenac. Antipyretic effects may be due to action on the hypothalamus, resulting in peripheral dilation, increased cutaneous blood flow, and subsequent heat dissipation.
Absorption	Completely absorbed from the gastrointestinal tract.
Volume of distribution	1.3 L/kg
Protein binding	More than 99%
Metabolism	Hepatic Enzyme Metabolite Reaction Km Vmax Prostaglandin G/H synthase 1 3'-Hydroxydiclofenac 3'-hydroxylation Cytochrome P450 3A4 5-Hydroxydiclofenac 5-hydroxylation Cytochrome P450 2C9 4'-Hydroxydiclofenac 4'-hydroxylation 3.1 1.01 UDP-glucuronosyltransferase 1-1 Diclofenac acyl glucuronide glucuronidation UDP-glucuronosyltransferase 2B7 Diclofenac acyl glucuronide glucuronidation
Route of elimination	Diclofenac is eliminated through metabolism and subsequent urinary and biliary excretion of the glucuronide and the sulfate conjugates of the metabolites. Little or no free unchanged diclofenac is excreted in the urine. Approximately 65% of the dose is excreted in the urine and approximately 35% in the bile as conjugates of unchanged diclofenac plus metabolites.
Half life	2 hours
Clearance	oral cl=622 mL/min [healthy] renal cl <1 mL/min [healthy]
Toxicity	Symptoms of overdose include loss of consciousness, increased intracranial pressure, and aspiration pneumonitis. LD50=390mg/kg (orally in mice)
Affected organisms	Humans and other mammals
Pathways	Pathway Name SMPDB ID Diclofenac Pathway SMP00093

Properties
State	solid
Melting point	283-285oC
Experimental Properties	Property Value Source water solubility 50 mg/mL (sodium salt) [Sigma Aldrich] PhysProp logP 3.9 PhysProp pKa 4.15 Various sources
Predicted Properties	Property Value Source water solubility 4.47e-03 g/l ALOGPS logP 4.98 ALOGPS logP 4.26 ChemAxon Molconvert logS -4.82 ALOGPS pKa 16.40 ChemAxon Molconvert hydrogen acceptor count 3 ChemAxon Molconvert hydrogen donor count 2 ChemAxon Molconvert polar surface area 49.33 ChemAxon Molconvert rotatable bond count 4 ChemAxon Molconvert refractivity 75.46 ChemAxon Molconvert polarizability 27.93 ChemAxon Molconvert

Drug	Interaction
Alendronate	Increased risk of gastric toxicity
Anisindione	The NSAID, diclofenac, may increase the anticoagulant effect of anisindione.
Cyclosporine	Monitor for nephrotoxicity
Dicumarol	The NSAID, diclofenac, may increase the anticoagulant effect of dicumarol.
Ginkgo biloba	Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
Lithium	The NSAID, diclofenac, may decrease the renal excretion of lithium. Increased risk of lithium toxicity.
Methotrexate	The NSAID, diclofenac, may decrease the renal excretion of methotrexate. Increased risk of methotrexate toxicity.
Rifampin	Rifampin, a CYP2C9 inducer, may increase the metabolism of diclofenac.
Tacrine	The metabolism of Tacrine, a CYP1A2 substrate, may be reduced by Diclofenac, a CYP1A2 inhibitors. Monitor the efficacy and toxicity of Tacrine if Diclofenac is initiated, discontinued or if the dose is changed.
Telmisartan	Concomitant use of Telmisartan and Diclofenac may increase the risk of acute renal failure and hyperkalemia. Monitor renal function at the beginning and during treatment.
Timolol	The NSAID, Diclofenac, may antagonize the antihypertensive effect of Timolol.
Tizanidine	Diclofenac may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration.
Trandolapril	The NSAID, Diclofenac, may reduce the antihypertensive effect of Trandolapril. Consider alternate therapy or monitor for changes in Trandolapril efficacy if Diclofenac is initiated, discontinued or dose changed.
Treprostinil	The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Diclofenac. Monitor for increased bleeding during concomitant thearpy.
Voriconazole	Voriconazole, a strong CYP2C9 inhibitor, may increase the serum concentration of diclofenac by decreasing its metabolism. Renal impairment may increase the risk of diclofenac adverse effects. Monitor for changes in therapeutic and adverse effects of diclofenac if voriconazole is initiated, discontinued or dose changed.
Warfarin	The antiplatelet effects of oral diclofenac may increase the bleed risk associated with warfarin. Consider alternate therapy or monitor for signs and symptoms of bleeding during concomitant therapy.

• Avoid alcohol.
• Take with food to reduce irritation.