Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Traditional IUPAC Name
Độ hòa tan
0.84 g/L at 20°C
pKa (strongest acidic)
pKa (Strongest Basic)
Dược Lực Học :
Mesalazine (INN, BAN), also known as Mesalamine (USAN) or 5-aminosalicylic acid (5-ASA), is an anti-inflammatory drug used to treat inflammation of the digestive tract (Crohn's disease) and mild to moderate ulcerative colitis. Mesalazine is a bowel-specific aminosalicylate drug that is metabolized in the gut and has its predominant actions there, thereby having fewer systemic side effects. As a derivative of salicylic acid, 5-ASA is also an antioxidant that traps free radicals, which are potentially damaging by-products of metabolism.
Cơ Chế Tác Dụng :
An anti-inflammatory agent, structurally related to the salicylates, which is active in inflammatory bowel disease. It is considered to be the active moiety of sulphasalazine. (From Martindale, The Extra Pharmacopoeia, 30th ed)
Although the mechanism of action of mesalazine is not fully understood, it appears to be topical rather than systemic. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, i.e., prostanoids, and through the lipoxygenase pathways, i.e., leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with chronic inflammatory bowel disease, and it is possible that mesalazine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin production in the colon.
Dược Động Học :
▧ Absorption :
20 to 30% absorbed following oral administration. 10 to 35% absorbed from the colon (rectal suppository) - extent of absorption is determined by the length of time the drug is retained in the colon.
▧ Protein binding :
About 80% of N-Ac-5-ASA is bound to plasma proteins, whereas 40% of mesalamine is protein bound.
▧ Metabolism :
Rapidly and extensively metabolized, mainly to N-acetyl-5-ASA (Ac-5-ASA) in the intestinal mucosal wall and the liver. Ac-5-ASA is further acetylated (deactivated) in at least 2 sites, the colonic epithelium and the liver.
▧ Route of Elimination :
Approximately 28% of the mesalamine in Asacol tablets is absorbed after oral ingestion, leaving the remainder available for topical action and excretion in the feces.
It is excreted mainly by the kidney as N-acetyl-5-aminosalicylic acid.
▧ Half Life :
The mean elimination half-life was 5 hours for 5-ASA and six hours for N-acetyl-5-ASA following the initial dose. At steady state, the mean elimination half-life was seven hours for both 5-ASA and N-acetyl-5-ASA.
Độc Tính :
Oral, mouse: LD50 = 3370 mg/kg; Oral, rat: LD50 = 2800 mg/kg; Skin, rabbit: LD50 = >5 gm/kg. There have been no documented reports of serious toxicity in man resulting from massive overdosing with mesalamine. Under ordinary circumstances, mesalazine absorption from the colon is limited.
Chỉ Định :
For the treatment of active ulcerative proctitis.
Tương Tác Thuốc :
Mesalazine may increase the toxicity of thiopurine, azathioprine.
Mesalazine may increase the toxicity of thiopurine, mercaptopurine.
Mesalazine may increase the toxicity of thiopurine, thioguanine.
Liều Lượng & Cách Dùng :
Enema - Rectal
Suppository - Rectal
Suspension - Rectal
Tablet, coated - Oral
Tablet, delayed release - Oral
Tablet, extended release - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
Sản phẩm biệt dược : APRISO
Sản phẩm biệt dược : Asacol
Sản phẩm biệt dược : Asacolitin
Sản phẩm biệt dược : Canasa
Sản phẩm biệt dược : Claversal
Sản phẩm biệt dược : Delzicol
Sản phẩm biệt dược : Fisalamine
Sản phẩm biệt dược : Lixacol
Sản phẩm biệt dược : Mesasal
Sản phẩm biệt dược : Pentasa
Sản phẩm biệt dược : Rowasa
Sản phẩm biệt dược : Salofalk
Tài Liệu Tham Khảo Thêm
National Drug Code Directory