Tìm theo
Salsalate
Các tên gọi khác (15 ) :
  • 2-Carboxyphenyl salicylate
  • Disalcid
  • Disalicylic acid
  • Disalicylsaeure
  • O-Salicylcylsalicylsaeure
  • O-Salicylsalicylic acid
  • Salicylic acid bimolecular ester
  • Salicyloxysalicylic acid
  • Salicyloylsalicylic acid
  • salicylsalicylic acid
  • Salsalato
  • Salsalatum
  • Sasapyrin
  • Sasapyrine
  • Sasapyrinum
anti inflammatory agents non steroidal
Thuốc Gốc
Small Molecule
CAS: 552-94-3
ATC: N02BA06
ĐG : 3M Health Care , http://www.3m.com
CTHH: C14H10O5
PTK: 258.2262
Salsalate is a nonsteroidal anti-inflammatory agent for oral administration. Salsalate's mode of action as an anti-inflammatory and antirheumatic agent may be due to inhibition of synthesis and release of prostaglandins. The usefulness of salicylic acid, the active in vivo product of salsalate, in the treatment of arthritic disorders has been established. In contrast to aspirin, salsalate causes no greater fecal gastrointestinal blood loss than placebo. Salsalate is readily soluble in the small intestine where it is partially hydrolyzed to two molecules of salicylic acid. A significant portion of the parent compound is absorbed unchanged and undergoes rapid esterase hydrolysis in the body. The parent compound has an elimination half-life of about 1 hour. Salicylic acid (the active metabolite) biotransformation is saturated at anti-inflammatory doses of salsalate. Such capacity limited biotransformation results in an increase in the half-life of salicylic acid from 3.5 to 16 or more hours.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C14H10O5
Phân tử khối
258.2262
Monoisotopic mass
258.05282343
InChI
InChI=1S/C14H10O5/c15-11-7-3-1-5-9(11)14(18)19-12-8-4-2-6-10(12)13(16)17/h1-8,15H,(H,16,17)
InChI Key
InChIKey=WVYADZUPLLSGPU-UHFFFAOYSA-N
IUPAC Name
2-[(2-hydroxyphenyl)carbonyloxy]benzoic acid
Traditional IUPAC Name
salsalate
SMILES
OC(=O)C1=CC=CC=C1OC(=O)C1=CC=CC=C1O
Độ tan chảy
147 °C
Độ hòa tan
2.46e-01 g/l
logP
3.64
logS
-3
pKa (strongest acidic)
3.4
pKa (Strongest Basic)
-4.3
PSA
83.83 Å2
Refractivity
67.1 m3·mol-1
Polarizability
24.92 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Salsalate is a nonsteroidal anti-inflammatory agent for oral administration. Salsalate's mode of action as an anti-inflammatory and antirheumatic agent may be due to inhibition of synthesis and release of prostaglandins. The usefulness of salicylic acid, the active in vivo product of salsalate, in the treatment of arthritic disorders has been established. In contrast to aspirin, salsalate causes no greater fecal gastrointestinal blood loss than placebo.
Cơ Chế Tác Dụng : Salsalate is a nonsteroidal anti-inflammatory agent for oral administration. Salsalate's mode of action as an anti-inflammatory and antirheumatic agent may be due to inhibition of synthesis and release of prostaglandins. The usefulness of salicylic acid, the active in vivo product of salsalate, in the treatment of arthritic disorders has been established. In contrast to aspirin, salsalate causes no greater fecal gastrointestinal blood loss than placebo. Salsalate is readily soluble in the small intestine where it is partially hydrolyzed to two molecules of salicylic acid. A significant portion of the parent compound is absorbed unchanged and undergoes rapid esterase hydrolysis in the body. The parent compound has an elimination half-life of about 1 hour. Salicylic acid (the active metabolite) biotransformation is saturated at anti-inflammatory doses of salsalate. Such capacity limited biotransformation results in an increase in the half-life of salicylic acid from 3.5 to 16 or more hours. The mode of anti-inflammatory action of salsalate and other nonsteroidal anti-inflammatory drugs is not fully defined, but appears to be primarily associated with inhibition of prostaglandin synthesis. This inhibition of prostaglandin synthesis is done through the inactivation of cyclooxygenase-1 (COX-1) and COX-2, which are reponsible for catalyzing the formation of prostaglandins in the arachidonic acid pathway. Although salicylic acid (the primary metabolite of salsalate) is a weak inhibitor of prostaglandin synthesis in vitro, salsalate appears to selectively inhibit prostaglandin synthesis in vivo, providing anti-inflammatory activity equivalent to aspirin and indomethacin. Unlike aspirin, salsalate does not inhibit platelet aggregation.
Dược Động Học :
▧ Absorption :
Salsalate is insoluble in acid gastric fluids (< 0.1 mg/ml at pH 1.0), but readily soluble in the small intestine where it is partially hydrolyzed to two molecules of salicylic acid. A significant portion of the parent compound is absorbed unchanged. The amount of salicylic acid available from salsalate is about 15% less than from aspirin, when the two drugs are administered on a salicylic acid molar equivalent basis (3.6 g salsalate/5 g aspirin). Food slows the absorption of all salicylates including salsalate.
▧ Protein binding :
Salicylate: 90-95% bound at plasma salicylate concentrations <100 mcg/mL; 70-85% bound at concentrations of 100-400 mcg/mL; 25-60% bound at concentrations >400 mcg/mL.
▧ Metabolism :
Salsalate is readily soluble in the small intestine where it is partially hydrolyzed to two molecules of salicylic acid. A significant portion of the parent compound is absorbed unchanged and undergoes rapid esterase hydrolysis in the body.
▧ Half Life :
The parent compound has an elimination half-life of about 1 hour. Salicylic acid (the active metabolite) biotransformation is saturated at anti-inflammatory doses of salsalate. Such capacity limited biotransformation results in an increase in the half-life of salicylic acid from 3.5 to 16 or more hours.
Độc Tính : Death has followed ingestion of 10 to 30 g of salicylates in adults, but much larger amounts have been ingested without fatal outcome.
Chỉ Định : For relief of the signs and symptoms of rheumatoid arthritis, osteoarthritis and related rheumatic disorders.
Tương Tác Thuốc :
  • Betamethasone The corticosteroid, betamethasone, may decrease the effect of the salicylate, salsalate.
  • Chlorpropamide The salicylate, salsalate, increases the effect of the sulfonylurea, chlorpropamide.
  • Dexamethasone The corticosteroid, dexamethasone, may decrease the effect of the salicylate, salsalate.
  • Fludrocortisone The corticosteroid, fludrocortisone, may decrease the effect of the salicylate, salsalate.
  • Gliclazide The salicylate, salsalate, increases the effect of the sulfonylurea, gliclazide.
  • Glyburide The salicylate, salsalate, increases the effect of the sulfonylurea, glibenclamide.
  • Hydrocortisone The corticosteroid, hydrocortisone, may decrease the effect of the salicylate, salsalate.
  • Methazolamide The salicylate, salsalate, at high dose increases the effect of the carbonic anhydrase inhibitor, methazolamide.
  • Methotrexate The salicylate, salsalate, increases the effect and toxicity of methotrexate.
  • Prednisolone The corticosteroid, prednisolone, may decrease the effect of the salicylate, salsalate.
  • Prednisone The corticosteroid, prednisone, may decrease the effect of the salicylate, salsalate.
  • Probenecid The salicylate, salsalate, decreases the uricosuric effect of probenecid.
  • Sulindac Risk of additive toxicity (e.g. bleed risk). Salsalate may decrease the serum concentration of sulindac. Consider alternate therapy or monitor for changes in the therapeutic effects of sulindac and adverse effects of both agents if the interacting agent is initiated, discontinued or dose changed.
  • Tiaprofenic acid Increased risk of gastrointestinal bleeding.
  • Tolmetin Additive effects increase the risk of GI bleeding. Monitor for increased bleeding risk during concomitant therapy.
  • Trandolapril The salicylate, Salsalate, may reduce the efficacy of Trandolapril. Monitor for changes in Trandolapril efficacy if Salsalate is initiated, discontinued or dose changed.
  • Treprostinil The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the salicylate, Salsalate. Monitor for increased bleeding during concomitant thearpy.
  • Triamcinolone The corticosteroid, triamcinolone, may decrease the effect of the salicylate, salsalate.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Salsalate powder
    Giá bán buôn : USD >16.8
    Đơn vị tính : g
  • Biệt dược thương mại : Salsalate 500 mg tablet
    Giá bán buôn : USD >0.26
    Đơn vị tính : tablet
  • Biệt dược thương mại : Salflex-500 tablet
    Giá bán buôn : USD >0.37
    Đơn vị tính : tablet
  • Biệt dược thương mại : Salflex-750 tablet
    Giá bán buôn : USD >0.5
    Đơn vị tính : tablet
  • Biệt dược thương mại : Salsalate 750 mg tablet
    Giá bán buôn : USD >0.55
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Disalcid
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01399
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5161
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506882
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00428
ChemSpider
http://www.chemspider.com/Chemical-Structure.4977.html
PharmGKB
http://www.pharmgkb.org/drug/PA164745462
RxList
http://www.rxlist.com/cgi/generic/salsalate.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/dis1142.shtml
Drugs.com
http://www.drugs.com/cdi/salsalate.html
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