Tìm theo
Diclofenac
Các tên gọi khác (7 ) :
  • [2-(2,6-Dichloroanilino)phenyl]acetic acid
  • 2-((2,6-Dichlorophenyl)amino)benzeneacetic acid
  • Diclofenac
  • Diclofenac Acid
  • Diclofenaco
  • Diclofenacum
  • ISV-205
Thuốc giảm đau, hạ sốt, chống viêm không steroid, điều trị Gút và các bệnh xương khớp
Thuốc Gốc
Small Molecule
CAS: 15307-86-5
ATC: M01AB05, M02AA15, S01BC03, D11AX18
ĐG : 4uOrtho LLC , http://www.4udr.com
CTHH: C14H11Cl2NO2
PTK: 296.149
A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C14H11Cl2NO2
Phân tử khối
296.149
Monoisotopic mass
295.016684015
InChI
InChI=1S/C14H11Cl2NO2/c15-10-5-3-6-11(16)14(10)17-12-7-2-1-4-9(12)8-13(18)19/h1-7,17H,8H2,(H,18,19)
InChI Key
InChIKey=DCOPUUMXTXDBNB-UHFFFAOYSA-N
IUPAC Name
2-{2-[(2,6-dichlorophenyl)amino]phenyl}acetic acid
Traditional IUPAC Name
diclofenac
SMILES
OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl
Độ tan chảy
283-285 °C
Độ hòa tan
2.37 mg/L (at 25 °C)
logP
4.51
logS
-4.8
pKa (strongest acidic)
4
pKa (Strongest Basic)
-2.1
PSA
49.33 Å2
Refractivity
75.46 m3·mol-1
Polarizability
27.93 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
4.15
Dược Lực Học : 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
Cơ Chế Tác Dụng : A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt. [PubChem] 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.
Dược Động Học :
▧ Absorption :
Completely absorbed from the gastrointestinal tract.
▧ Volume of Distribution :
* 1.3 L/kg
▧ Protein binding :
More than 99%
▧ Metabolism :
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]
Độc Tính : Symptoms of overdose include loss of consciousness, increased intracranial pressure, and aspiration pneumonitis. LD50=390mg/kg (orally in mice)
Chỉ Định : For the acute and chronic treatment of signs and symptoms of osteoarthritis and rheumatoid arthritis.
Tương Tác Thuốc :
  • Alendronate Increased risk of gastric toxicity
  • Anisindione The NSAID, diclofenac, may increase the anticoagulant effect of anisindione.
  • Azilsartan medoxomil Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Colesevelam Bile acid sequestrants may decrease the absorption of Nonsteroidal Anti-Inflammatory Agents. Monitor for decreased serum concentrations/therapeutic effects of nonsteroidal anti-inflammatory agents (NSAID) if coadministered with bile acid sequestrants. Separating the administration of doses by 2 or more hours may reduce (but not eliminate) the risk of interaction. The manufacturer of colesevelam recommends that drugs should be administered at least 1 hour before or 4 hours after colesevelam.
  • Cyclosporine Monitor for nephrotoxicity
  • Dicoumarol The NSAID, diclofenac, may increase the anticoagulant effect of dicumarol.
  • Difluprednate NSAIDs may slow healing.
  • Eltrombopag Eltrombopag increases levels of Diclofenac via metabolism decrease. UDP-glucuronosyltransferase inhibition.
  • 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.
  • Pralatrexate NSAIDs increase the risk of toxicity due to impairment of renal clearance of pralatrexate thus increasing exposure. Monitor for adverse effects or adjust dose of pralatrexate.
  • Rifampicin 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.
  • Vilazodone Increased risk of bleeding with concomitant use of NSAIDs with vilazodone.
  • 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.
Liều Lượng & Cách Dùng : Solution - Ophthalmic
Solution - Topical
Suppository - Rectal
Tablet - Oral
Tablet, coated - Oral
Tablet, extended release - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Aclonac
  • Công ty :
    Sản phẩm biệt dược : Allvoran
  • Công ty :
    Sản phẩm biệt dược : CAMBIA
  • Công ty :
    Sản phẩm biệt dược : Cataflam
  • Công ty : Hospira
    Sản phẩm biệt dược : Dyloject
  • Công ty :
    Sản phẩm biệt dược : Ecofenac
  • Công ty :
    Sản phẩm biệt dược : Effekton
  • Công ty :
    Sản phẩm biệt dược : Flector
  • Công ty :
    Sản phẩm biệt dược : Nu-Diclo
  • Công ty :
    Sản phẩm biệt dược : Pennsaid
  • Công ty :
    Sản phẩm biệt dược : Primofenac
  • Công ty :
    Sản phẩm biệt dược : Prophenatin
  • Công ty :
    Sản phẩm biệt dược : Rhumalgan
  • Công ty :
    Sản phẩm biệt dược : Solaraze
  • Công ty :
    Sản phẩm biệt dược : Voltaren
  • Công ty :
    Sản phẩm biệt dược : Voltaren Emulgel
  • Công ty :
    Sản phẩm biệt dược : Voltarol
  • Công ty :
    Sản phẩm biệt dược : Zipsor
  • Công ty :
    Sản phẩm biệt dược : Zorvolex
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00586
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3033
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504644
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C01690
ChemSpider
http://www.chemspider.com/Chemical-Structure.2925.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=13066
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0781-5017-01
PharmGKB
http://www.pharmgkb.org/drug/PA449293
Wikipedia
http://en.wikipedia.org/wiki/Diclofenac
RxList
http://www.rxlist.com/cgi/generic/diclofen.htm
Drugs.com
http://www.drugs.com/cdi/diclofenac-drops.html
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