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QuickView for Diclofenac (compound)

Name: Diclofenac
PubChem Compound ID: 152165
Description: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.
Molecular formula: C12H12N4O
Molecular weight: 228.25 g/mol
98046-72-1; Hydroxylamine, N-(4,6-dimethyldipyrido(1,2-a:3',2'-d)imidazol-3-yl)-; SR 38; N-(4,6-Dimethyldipyrido(1,2-a:3',2'-d)imidazol-3-yl)hydroxylamine; 3-Hydroxyimino-4,6-dimethyldipyrido(1,2-a:3',2'-d)imidazole; CCRIS 6135; 3-Hydroxyamino-4,6-dimethyldipyrido(1,2-a:3',2'-d)imidazole; Dipyrido(1,2-a:3',2'-d)imidazol-3-imine, N-hydroxy-4,6-dimethyl-
Name: Diclofenac
Name (isomeric): DB00586
Drug Type: small molecule
Description: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.
Diclofenac Acid; Diclofenac Potassium; ISV-205; Diclofenac Sodium
Brand: Voltaren Ophtha, Voltaren Ophthalmic, Rhumalgan, Benfofen, Prophenatin, Apo-Diclo, Novapirina, Tsudohmin, Dicloreum, Voldal, Effekton, Pennsaid, Dolobasan, Novo-Difenac, Valetan, Cataflam, Voltaren SR, Neriodin, Nu-Diclo, Solaraze T, Primofenac, Assaren, Diclord, Delphimix, Ecofenac, Dichlofenac, Duravolten, Kriplex, Xenid, Voltaren Rapide, Diclo-Phlogont, Diclo-Puren, Dichronic, Allvoran, Novo-Difenac SR, Voltaren, ProSorb-D, Voltarol, Dyloject, Solaraze, Voltaren-XR, Diclobenin
Category: Cyclooxygenase Inhibitors, Nonsteroidal Anti-inflammatory Agents (NSAIAs)
CAS number: 15307-86-5
Indication: For the acute and chronic treatment of signs and symptoms of osteoarthritis and rheumatoid arthritis.
Pharmacology: 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....
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Absorption: Completely absorbed from the gastrointestinal tract.
Protein binding: More than 99%
Biotransformation: Hepatic
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
Food interaction:
Avoid alcohol.
Take with food to reduce irritation.
Drug interaction:
DicumarolThe NSAID, diclofenac, may increase the anticoagulant effect of dicumarol.
TacrineThe 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.
TimololThe NSAID, Diclofenac, may antagonize the antihypertensive effect of Timolol.
TreprostinilThe prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Diclofenac. Monitor for increased bleeding during concomitant thearpy.
VoriconazoleVoriconazole, 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.
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