Tìm theo
Olsalazine
Các tên gọi khác (2) :
  • Dipentum
  • SID50125747
Thuốc Gốc
Small Molecule
CAS: 15722-48-2
ATC: A07EC03
ĐG : Alaven Pharmaceutical , http://www.alavenpharm.com
CTHH: C14H10N2O6
PTK: 302.239
Olsalazine is an anti-inflammatory drug used in the treatment of Inflammatory Bowel Disease and Ulcerative Colitis. Olsalazine is a derivative of salicylic acid. Inactive by itself (it is a prodrug), it is converted by the bacteria in the colon to mesalamine. Mesalamine works as an anti-inflammatory agent in treating inflammatory diseases of the intestines.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C14H10N2O6
Phân tử khối
302.239
Monoisotopic mass
302.053886062
InChI
InChI=1S/C14H10N2O6/c17-11-3-1-7(5-9(11)13(19)20)15-16-8-2-4-12(18)10(6-8)14(21)22/h1-6,17-18H,(H,19,20)(H,21,22)/b16-15+
InChI Key
InChIKey=QQBDLJCYGRGAKP-FOCLMDBBSA-N
IUPAC Name
5-[(E)-2-(3-carboxy-4-hydroxyphenyl)diazen-1-yl]-2-hydroxybenzoic acid
Traditional IUPAC Name
olsalazine
SMILES
OC(=O)C1=CC(=CC=C1O)\N=N\C1=CC=C(O)C(=C1)C(O)=O
Độ tan chảy
Sodium salt decomposes at 240 °C
Độ hòa tan
7.81e-02 g/l
logP
2.3
logS
-3.6
pKa (strongest acidic)
2.93
pKa (Strongest Basic)
-0.019
PSA
139.78 Å2
Refractivity
78.85 m3·mol-1
Polarizability
28.61 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
8
H Bond Donor Count
4
Physiological Charge
-2
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
caco2 Permeability
-6.96
Dược Lực Học : Olsalazine is an anti-inflammatory drug used in the treatment of Inflammatory Bowel Disease and Ulcerative Colitis. Olsalazine reduces the bowel inflammation, diarrhea (stool frequency), rectal bleeding, and abdominal pain. Like Balsalazide, Olsalazine is believed to deliver Mesalazine, or 5-aminosalicylic acid (5-ASA), past the small intestine, directly to the large intestine, which is that active site of disease in ulcerative colitis.
Cơ Chế Tác Dụng : Olsalazine is an anti-inflammatory drug used in the treatment of Inflammatory Bowel Disease and Ulcerative Colitis. Olsalazine is a derivative of salicylic acid. Inactive by itself (it is a prodrug), it is converted by the bacteria in the colon to mesalamine. Mesalamine works as an anti-inflammatory agent in treating inflammatory diseases of the intestines. Orally administered olsalazine is converted to mesalamine which is thought to be the therapeutically active agent in the treatment of ulcerative colitis. The mechanism of action of mesalamine (and sulfasalazine) is unknown, but appears to be topical rather than systemic. Mucosal production of arachidonic acid (AA) metabolites, both through the cyclooxygenase pathways, i.e., prostanoids, and through the lipoxygenase pathways, i.e., leukotrienes (LTs) and hydroxyelcosatetraenoic acids (HETEs) is increased in patients with chronic inflammatory bowel disease, and it is possible that mesalamine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin (PG) production in the colon.
Dược Động Học :
▧ Absorption :
After oral administration, olsalazine, has limited systemic bioavailability. 98-99% of the dose is converted to mesalamine (5-ASA) in the colon, which is absorbed slowly resulting in very high local concentrations in the colon.
▧ Protein binding :
Olsalazine and olsalazine-S are more than 99% bound to plasma proteins. Mesalamine (5-ASA) is 74% bound to plasma proteins.
▧ Metabolism :
Most (98 to 99%) of an oral dose is rapidly converted into two molecules of 5-aminosalicylic acid (5-ASA) by colonic bacteria and the low prevailing redox potential found in this environment. The conversion of olsalazine to mesalamine in the colon is similar to that of sulfasalazine, which is converted into sulfapyridine and mesalamine. Approximately 0.1% of an oral dose of olsalazine is metabolized in the liver to olsalazine-O-sulfate (olsalazine-S)
▧ Route of Elimination :
Approximately 0.1% of an oral dose of olsalazine is metabolized in the liver to olsalazine-O-sulfate (olsalazine-S).The remaining 5-ASA is partially acetylated and is excreted in the feces.
▧ Half Life :
Olsalazine has an elimination half-life of 0.9 hours, however, olsalazine-S has a half-life of 7 days.
Độc Tính : Maximum single oral doses of 5g/kg in mice and rats and 2 g/kg in dogs were not lethal.
Chỉ Định : For the treatment of Inflammatory Bowel Disease and Ulcerative Colitis.
Tương Tác Thuốc :
  • Azathioprine Olsalazine may increase the toxicity of thiopurine, azathioprine.
  • Mercaptopurine Olsalazine may increase the toxicity of thiopurine, mercaptopurine.
  • Tioguanine Olsalazine may increase the toxicity of thiopurine, thioguanine.
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
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Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01250
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=6003770
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506356
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07323
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00727
ChemSpider
http://www.chemspider.com/Chemical-Structure.4777171.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/53014-726-71
PharmGKB
http://www.pharmgkb.org/drug/PA450700
Wikipedia
http://en.wikipedia.org/wiki/Olsalazine
RxList
http://www.rxlist.com/cgi/cgi/generic/olsal.htm
Drugs.com
http://www.drugs.com/cdi/olsalazine.html
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