Tìm theo
Sucralfate
Các tên gọi khác (5 ) :
  • Hexadeca-μ-hydroxytetracosahydroxy[μ8-[1,3,4,6-tetra-O-sulfo-β-Dfructofuranosyl-α-D-glucopyranoside tetrakis(hydrogen sulfato)8-)]]hexadecaaluminum
  • Sucralfat
  • Sucralfate
  • Sucralfato
  • Sucralfatum
Thuốc Gốc
Small Molecule
CAS: 54182-58-0
ATC: A02BX02
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C11H28Al8O51S8
PTK: 1448.682
A basic aluminum complex of sulfated sucrose. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C11H28Al8O51S8
Phân tử khối
1448.682
Monoisotopic mass
1447.588619666
InChI
InChI=1S/C11H20O35S8.8Al.16H2O/c12-47(13,14)36-1-3-4(41-49(18,19)20)5(42-50(21,22)23)6(43-51(24,25)26)9(38-3)39-11(2-37-48(15,16)17)8(45-53(30,31)32)7(44-52(27,28)29)10(40-11)46-54(33,34)35;;;;;;;;;;;;;;;;;;;;;;;;/h3-10H,1-2H2,(H,12,13,14)(H,15,16,17)(H,18,19,20)(H,21,22,23)(H,24,25,26)(H,27,28,29)(H,30,31,32)(H,33,34,35);;;;;;;;;16*1H2/q;8*+3;;;;;;;;;;;;;;;;/p-24/t3-,4-,5+,6-,7+,8+,9+,10-,11-;;;;;;;;;;;;;;;;;;;;;;;;/m1......................../s1
InChI Key
InChIKey=MNQYNQBOVCBZIQ-JQOFMKNESA-A
IUPAC Name
[({[(2S,3R,4S,5R,6R)-4,5-bis({[(dihydroxyalumanyl)oxy]sulfonyl}oxy)-6-[({[(dihydroxyalumanyl)oxy]sulfonyl}oxy)methyl]-2-{[(2R,3S,4S,5R)-3,4,5-tris({[(dihydroxyalumanyl)oxy]sulfonyl}oxy)-2-[({[(dihydroxyalumanyl)oxy]sulfonyl}oxy)methyl]oxolan-2-yl]oxy}oxan-3-yl]oxy}sulfonyl)oxy]alumanediol
Traditional IUPAC Name
({[(2S,3R,4S,5R,6R)-4,5-di{[(dihydroxyalumanyl)oxysulfonyl]oxy}-6-({[(dihydroxyalumanyl)oxysulfonyl]oxy}methyl)-2-{[(2R,3S,4S,5R)-3,4,5-tri{[(dihydroxyalumanyl)oxysulfonyl]oxy}-2-({[(dihydroxyalumanyl)oxysulfonyl]oxy}methyl)oxolan-2-yl]oxy}oxan-3-yl]oxysulfonyl}oxy)alumanediol
SMILES
O[Al](O)OS(=O)(=O)OC[[email protected]]1O[[email protected]@H](O[[email protected]]2(COS(=O)(=O)O[Al](O)O)O[[email protected]](OS(=O)(=O)O[Al](O)O)[[email protected]@H](OS(=O)(=O)O[Al](O)O)[[email protected]@H]2OS(=O)(=O)O[Al](O)O)[[email protected]](OS(=O)(=O)O[Al](O)O)[[email protected]@H](OS(=O)(=O)O[Al](O)O)[[email protected]@H]1OS(=O)(=O)O[Al](O)O
Độ hòa tan
Insoluble in cold water
logP
-5.6
logS
-3.3
pKa (strongest acidic)
13.53
pKa (Strongest Basic)
-3
PSA
772.17 Å2
Refractivity
175.09 m3·mol-1
Polarizability
105.22 Å3
Rotatable Bond Count
36
H Bond Acceptor Count
35
H Bond Donor Count
16
Physiological Charge
0
Number of Rings
2
Bioavailability
0
Dược Lực Học : Sucralfate is a prescription medication used to treat peptic ulcers. The current clinical uses of sucralfate are limited. It is effective for the healing of duodenal ulcers, but it is not frequently used for this since more effective drugs (e.g. proton pump inhibitors) have been developed. Although the mechanism of sucralfate's ability to accelerate healing of duodenal ulcers remains to be fully defined, it is known that it exerts its effect through a local, rather than systemic, action. Chemically, sucralfate is a complex of the disaccharide sugar, sucrose, combined with sulfate and aluminum. In acidic solutions (e.g. gastric acid) it forms a thick paste that has a strong negative charge.
Cơ Chế Tác Dụng : A basic aluminum complex of sulfated sucrose. [PubChem] Although sucralfate's mechanism is not entirely understood, there are several factors that most likely contribute to its action. Sucralfate, with its strong negative charge, binds to exposed positively-charged proteins at the base of ulcers. In this way, it coats the ulcer and forms a physical barrier that protects the ulcer surface from further injury by acid and pepsin. It directly inhibits pepsin (an enzyme that breaks apart proteins) in the presence of stomach acid and binds bile salts coming from the liver via the bile thus protecting the stomach lining from injury caused by the bile acids. Sucralfate may increase prostaglandin production. Prostaglandins are known to protect the lining of the stomach and may also bind epithelial growth factor and fibroblast growth factor, both of which enhance the growth and repair mechanism of the stomach lining.
Dược Động Học :
▧ Absorption :
Minimally absorbed from the gastrointestinal tract (up to 5% of the disaccharide component and less than 0.02% of aluminum).
▧ Route of Elimination :
The small amounts of the sulfated disaccharide that are absorbed are excreted primarily in the urine.
▧ Half Life :
Not known.
Độc Tính : Acute oral toxicity (LD50) in mice is >8000 mg/kg. There is limited experience in humans with overdosage of sucralfate. Sucralfate is only minimally absorbed from the gastrointestinal tract and thus risks associated with acute overdosage should be minimal. In rare reports describing sucralfate overdose, most patients remained asymptomatic.
Chỉ Định : For the short-term treatment (up to 8 weeks) of active duodenal ulcer, as well as maintenance therapy for duodenal ulcer patients at reduced dosage (1 gram twice a day) after healing of acute ulcers. Also used for the short-term treatment of gastric ulcer.
Tương Tác Thuốc :
  • Calcipotriol Vitamin D Analogs may increase the serum concentration of Sucralfate. Specifically, the absorption of aluminum from sucralfate may be increased, leading to an increase in the serum aluminum concentration. Avoid chronic and/or excessive use of aluminum and aluminum-containing products (such as sucralfate) in patients who are also taking vitamin D analogs. Any patients consuming such a combination should be monitored closely for aluminum status and signs/symptoms of aluminum-related toxicities.
  • Cholecalciferol Vitamin D analogs such as cholecalciferol may increase the serum concentration of sucralfate. Specifically, the absorption of aluminum from sucralfate may be increased, leading to an increase in the serum aluminum concentration. Avoid chronic and/or excessive use of aluminum and aluminum-containing products (such as sucralfate) in patients who are also taking vitamin D analogs. Any patients consuming such a combination should be monitored closely for aluminum status and signs/symptoms of aluminum-related toxicities.
  • Ciprofloxacin Formation of non-absorbable complexes
  • Clodronate Formation of non-absorbable complexes
  • Etidronic acid Formation of non-absorbable complexes
  • Fosphenytoin Sucralfate decreases the effect of hydantoin
  • Gatifloxacin Formation of non-absorbable complexes
  • Gemifloxacin Formation of non-absorbable complexes
  • Grepafloxacin Formation of non-absorbable complexes
  • Ibandronate Formation of non absorbable complexes
  • Itraconazole Sucralfate may decrease the absorption of itraconazole.
  • Ketoconazole Sucralfate may decrease the absorption of ketoconazole.
  • Lansoprazole Sucralfate decreases the effect of lansoprazole
  • Levofloxacin Formation of non-absorbable complexes
  • Levothyroxine Sucralfate decreases the effect of levothyroxine
  • Moxifloxacin Formation of non-absorbable complexes
  • Norfloxacin Formation of non-absorbable complexes
  • Ofloxacin Formation of non-absorbable complexes
  • Phenytoin Sucralfate decreases the effect of hydantoin
  • Trovafloxacin Sucralfate may decrease the absorption of orally administered Trovafloxacin. The Sucralfate formulation contains aluminum ions that may intefere with Trovafloxacin absorption. Administer Trovafloxacin 2 hours before or 6 hours after the Sucralfate dose to minimize the interaction.
  • Warfarin Sucralfate may reduce the absorption of warfarin. Warfarin should be administered at least 2 hours before or 6 hours after sucralfate administration. Monitor for changes in prothrombin time if sucralfate is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Suspension - Oral
Tablet - Oral
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