Tìm theo
Roxatidine acetate
Các tên gọi khác (4 ) :
  • Aceroxatidine
  • Roxatidina
  • Roxatidine
  • Roxatidine acetate
anti ulcer agents, histamine h2 antagonists
Thuốc Gốc
Small Molecule
CAS: 78628-28-1
ATC: A02BA06
CTHH: C19H28N2O4
PTK: 348.4366
Roxatidine acetate is a specific and competitive H2 receptor antagonist. It is currently approved in South Africa under the tradename Roxit.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H28N2O4
Phân tử khối
348.4366
Monoisotopic mass
348.204907394
InChI
InChI=1S/C19H28N2O4/c1-16(22)25-15-19(23)20-9-6-12-24-18-8-5-7-17(13-18)14-21-10-3-2-4-11-21/h5,7-8,13H,2-4,6,9-12,14-15H2,1H3,(H,20,23)
InChI Key
InChIKey=SMTZFNFIKUPEJC-UHFFFAOYSA-N
IUPAC Name
({3-[3-(piperidin-1-ylmethyl)phenoxy]propyl}carbamoyl)methyl acetate
Traditional IUPAC Name
roxatidine
SMILES
CC(=O)OCC(=O)NCCCOC1=CC=CC(CN2CCCCC2)=C1
Độ tan chảy
145-146 for HCl salt
Độ hòa tan
6.12e-02 g/l
logP
1.31
logS
-3.8
pKa (strongest acidic)
14.88
pKa (Strongest Basic)
8.83
PSA
67.87 Å2
Refractivity
96.32 m3·mol-1
Polarizability
39.26 Å3
Rotatable Bond Count
10
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Roxatidine acetate suppresses the effect of histamine on the parietal cells of the stomach (H2-receptor antagonist). This suppressive action is dose-dependent. As a result, the production and secretion, particularly of gastric acid, are reduced. Roxatidine acetate has no antiandrogenic effects and does not influence drug-metabolizing enzymes in the liver.
Cơ Chế Tác Dụng : Roxatidine acetate is a specific and competitive H2 receptor antagonist. It is currently approved in South Africa under the tradename Roxit. The H2 antagonists are competitive inhibitors of histamine at the parietal cell H2 receptor. They suppress the normal secretion of acid by parietal cells and the meal-stimulated secretion of acid. They accomplish this by two mechanisms: histamine released by ECL cells in the stomach is blocked from binding on parietal cell H2 receptors which stimulate acid secretion, and other substances that promote acid secretion (such as gastrin and acetylcholine) have a reduced effect on parietal cells when the H2 receptors are blocked.
Dược Động Học :
▧ Absorption :
Well absorbed orally (80–90% bioavailability).
▧ Protein binding :
5-7%
▧ Metabolism :
Roxatidine acetate is rapidly metabolised to the primary, active desacetyl metabolite.
▧ Half Life :
5-6 hours
Độc Tính : Oral, mouse LD50: 1000 mg/kg
Chỉ Định : For the treatment of disorders of the upper gastro-intestinal region that are due to an excess of hydrochloric acid in the gastric juice, i.e. duodenal ulcers, benign gastric ulcers. Also for prophylaxis of recurrent gastric and duodenal ulcers
Liều Lượng & Cách Dùng : Tablet, film coated - Oral - 150 mg
Tablet, film coated - Oral - 75 mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Roxit
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08806
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08495
ChemSpider
http://www.chemspider.com/Chemical-Structure.4926.html
PharmGKB
http://www.pharmgkb.org/drug/PA165958424
Wikipedia
http://en.wikipedia.org/wiki/Roxatidine
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