物质信息

ID:469

名称和标识
商标名
Novo-Difenac SRPennsaidTsudohminVoltaren RapideVoltaren SRApo-DicloDiclo-PhlogontDiclobeninDolobasanEcofenacKriplexAllvoranRhumalganSolarazeVoldalVoltarolDylojectDicloreumNeriodinNovo-DifenacProphenatinDichronicEffektonPrimofenacVoltaren OphthaVoltaren-XRXenidVoltaren OphthalmicProSorb-DCataflamDichlofenacDuravoltenNovapirinaNu-DicloSolaraze TValetanVoltarenAssarenBenfofenDelphimixDiclo-PurenDiclord
IUPAC标准名
2-{2-[(2,6-dichlorophenyl)amino]phenyl}acetic acid
IUPAC传统名
diclofenac
别名
Diclofenac PotassiumISV-205DiclofenacDiclofenac SodiumDiclofenac Acid
数据登录号
PubChem CID
PubChem SID
化合物性质
理化性质
疏水性(logP)
3.9
溶解度
50 mg/mL (sodium salt) [Sigma Aldrich]
描述信息
Drug Groups
approved
Description
A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt. [PubChem]
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
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
Biotransformation
Hepatic
Absorption
Completely absorbed from the gastrointestinal tract.
Half Life
2 hours
Protein Binding
More than 99%
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.
Distribution
* 1.3 L/kg
Clearance
* oral cl=622 mL/min [healthy]
* renal cl <1 mL/min [healthy]
References
• 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]
External Links
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参考文献
• 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
• Gan TJ: Diclofenac: an update on its mechanism of action and safety profile. Curr Med Res Opin. 2010 Jul;26(7):1715-31. 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
• FitzGerald GA, Patrono C: The coxibs, selective inhibitors of cyclooxygenase-2. N Engl J Med. 2001 Aug 9;345(6):433-42. 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