Tìm theo
Tolmetin
Các tên gọi khác (8 ) :
  • 1-Methyl-5-(4-methylbenzoyl)-pyrrole-2-acetic acid
  • 1-Methyl-5-P-toluoylpyrrole-2-acetic acid
  • 5-(P-Toluoyl)-1-methylpyrrole-2-acetic acid
  • Tolmetin
  • Tolmetina
  • Tolmétine
  • Tolmetino
  • Tolmetinum
anti inflammatory agents non steroidal, cyclooxygenase inhibitors
Thuốc Gốc
Small Molecule
CAS: 26171-23-3
ATC: M01AB03, M02AA21
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C15H15NO3
PTK: 257.2845
A non-steroidal anti-inflammatory agent (anti-inflammatory agents, NON-steroidal) similar in mode of action to indomethacin. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H15NO3
Phân tử khối
257.2845
Monoisotopic mass
257.105193351
InChI
InChI=1S/C15H15NO3/c1-10-3-5-11(6-4-10)15(19)13-8-7-12(16(13)2)9-14(17)18/h3-8H,9H2,1-2H3,(H,17,18)
InChI Key
InChIKey=UPSPUYADGBWSHF-UHFFFAOYSA-N
IUPAC Name
2-{1-methyl-5-[(4-methylphenyl)carbonyl]-1H-pyrrol-2-yl}acetic acid
Traditional IUPAC Name
tolmetin
SMILES
CN1C(CC(O)=O)=CC=C1C(=O)C1=CC=C(C)C=C1
Độ tan chảy
156 dec °C
Độ hòa tan
222 mg/L
logP
2.79
logS
-3.3
pKa (strongest acidic)
3.96
pKa (Strongest Basic)
-7.8
PSA
59.3 Å2
Refractivity
72.39 m3·mol-1
Polarizability
27.67 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
-1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
3.5
Dược Lực Học : Tolmetin is a nonsteroidal anti-inflammatory agent. Studies in animals have shown tolmetin to possess anti-inflammatory, analgesic and antipyretic activity. In the rat, tolmetin prevents the development of experimentally induced polyarthritis and also decreases established inflammation. In patients with either rheumatoid arthritis or osteaoarthritis, tolmetin is as effective as aspirin and indomethacin in controlling disease activity, but the frequency of the milder gastrointestinal adverse effects and tinnitus was less than in aspirin-treated patients, and the incidence of central nervous system adverse effects was less than in indomethacin-treated patients. In patients with juvenile rheumatoid arthritis, tolmetin is as effective as aspirin in controlling disease activity, with a similar incidence of adverse reactions. tolmetin has produced additional therapeutic benefit when added to a regimen of gold salts and, to a lesser extent, with corticosteroids. Tolmetin should not be used in conjunction with salicylates since greater benefit from the combination is not likely, but the potential for adverse reactions is increased.
Cơ Chế Tác Dụng : A non-steroidal anti-inflammatory agent (anti-inflammatory agents, NON-steroidal) similar in mode of action to indomethacin. [PubChem] The mode of action of tolmetin is not known. However, studies in laboratory animals and man have demonstrated that the anti-inflammatory action of tolmetin is not due to pituitary-adrenal stimulation. Tolmetin inhibits prostaglandin synthetase in vitro and lowers the plasma level of prostaglandin E in man. This reduction in prostaglandin synthesis may be responsible for the anti-inflammatory action. Tolmetin does not appear to alter the course of the underlying disease in man.
Dược Động Học :
▧ Absorption :
Rapidly and almost completely absorbed with peak plasma levels being reached within 30-60 minutes after an oral therapeutic dose.
▧ Metabolism :
Essentially all of the administered dose is recovered in the urine in 24 hours either as an inactive oxidative metabolite or as conjugates of tolmetin.
▧ Half Life :
Biphasic elimination from the plasma consisting of a rapid phase with a half-life of one to 2 hours followed by a slower phase with a half-life of about 5 hours.
Độc Tính : Symptoms of overdose include lethargy, drowsiness, nausea, vomiting, and epigastric pain.
Chỉ Định : For the relief of signs and symptoms of rheumatoid arthritis and osteoarthritis, including the treatment of acute flares long-term management. Also for treatment of juvenile rheumatoid arthritis.
Tương Tác Thuốc :
  • Acenocoumarol Increased risk of bleeding. Monitor for signs and symptoms of bleeding.
  • Acetylsalicylic acid Additive adverse effects increase the risk of gastrointestinal bleeding. Possible decrease in the cardioprotective effect of acetylsalicylic acid. Monitor for increased bleeding risk during concomitant therapy.
  • Aminosalicylic Acid Additive effects increase the risk of GI bleeding. Monitor for increased bleeding risk during concomitant therapy.
  • Azilsartan medoxomil Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
  • Cholestyramine Cholestyramine may decrease the absorption of Tolmetin. Monitor for changes in the therapeutic and adverse effects of Tolmetin if Cholestyramine is initiated, discontinued or dose changed. Spacing administration by at least 2 hours may reduce the risk of interaction.
  • Citalopram Increased antiplatelet effects may enhance the risk of bleeding. Alternate therapy may be considered or monitor for inreased bleeding during concomitant therapy.
  • Colesevelam Colesevelam may decrease the absorption of Tolmetin. Monitor for changes in the therapeutic and adverse effects of Tolmetin if Colesevelam is initiated, discontinued or dose changed. Spacing administration by at least 2 hours may reduce the risk of interaction.
  • Colestipol Colestipol may decrease the absorption of Tolmetin. Monitor for changes in the therapeutic and adverse effects of Tolmetin if Colestipol is initiated, discontinued or dose changed. Spacing administration by at least 2 hours may reduce the risk of interaction.
  • Cyclosporine Tolmetin may increase the serum concentration of cyclosporine and/or increase the nephrotoxicity of cyclosporine. Consider alternate therapy or monitor for increased cyclosporine serum concentration and nephrotoxicity during concomitant therapy.
  • Drotrecogin alfa Increased risk of bleeding. Monitor for increased bleeding during concomitant therapy.
  • Escitalopram Increased antiplatelet effects may enhance the risk of bleeding. Alternate therapy may be considered or monitor for inreased bleeding during concomitant therapy.
  • Fluoxetine Increased antiplatelet effects may enhance the risk of bleeding. Alternate therapy may be considered or monitor for inreased bleeding during concomitant therapy.
  • Fluvoxamine Increased antiplatelet effects may enhance the risk of bleeding. Alternate therapy may be considered or monitor for inreased bleeding during concomitant therapy.
  • Ginkgo biloba Increased risk of bleeding due to additive antiplatelet properties of the two agents. Concomitant therapy should be avoided or monitored carefully for bleeding, bruising and altered mental status, which may be caused by CNS bleeds.
  • Ginseng Increased risk of bleeding due to additive antiplatelet properties of the two agents. Concomitant therapy should be avoided or monitored carefully for bleeding, bruising and altered mental status, which may be caused by CNS bleeds.
  • Ketorolac Risk of adverse NSAID toxic effects (e.g. GI bleeding, renal dysfunction). Concomitant therapy is contraindicated.
  • Lithium Tolmetin may increase the risk of Lithium toxicity by decreasing the renal elminiation of Lithium. A dose adjustment of Lithium may be required. Monitor for changes in Lithium therapeutic and adverse effects if Tolmetin is initiated, discontinued or dose changed.
  • Methotrexate Tolmetin may decrease the renal excretion of Methotrexate. Alternate therapy should be considered. Otherwise, monitor for hemotologic and renal toxicities.
  • Paroxetine Increased antiplatelet effects may enhance the risk of bleeding. Alternate therapy may be considered or monitor for inreased bleeding during concomitant therapy.
  • Pemetrexed Tolmetin may decrease the renal excretion of Pemetrexed in patients with decreased creatinine clearance. Tolmetin may be withheld in these patients from 2 days before to 2 days after Pemetrexed administration.
  • 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.
  • Salsalate Additive effects increase the risk of GI bleeding. Monitor for increased bleeding risk during concomitant therapy.
  • Sertraline Increased antiplatelet effects may enhance the risk of bleeding. Alternate therapy may be considered or monitor for inreased bleeding during concomitant therapy.
  • Telmisartan Concomitant use of Telmisartan and Tolmetin may increase the risk of acute renal failure and hyperkalemia. Monitor renal function at the beginning and during treatment.
  • Timolol The NSAID, Tolmetin, may antagonize the antihypertensive effect of Timolol.
  • Trandolapril The NSAID, Tolmetin, may reduce the antihypertensive effect of Trandolapril. Consider alternate therapy or monitor for changes in Trandolapril efficacy if Tolmetin is initiated, discontinued or dose changed.
  • Treprostinil The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Tolmetin. Monitor for increased bleeding during concomitant thearpy.
  • Warfarin The antiplatelet effects of tolmetin 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 : Capsule - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Teva
    Sản phẩm biệt dược : Tolectin
  • Công ty : Teva
    Sản phẩm biệt dược : Tolectin DS
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00500
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5509
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507060
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C02328
ChemSpider
http://www.chemspider.com/Chemical-Structure.5308.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0093-8815-01
PharmGKB
http://www.pharmgkb.org/drug/PA451721
Wikipedia
http://en.wikipedia.org/wiki/Tolmetin
RxList
http://www.rxlist.com/cgi/generic2/tolmetin.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/tol1449.shtml
Drugs.com
http://www.drugs.com/cdi/tolmetin.html
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