Tìm theo
Alosetron
Các tên gọi khác (1) :
  • 2,3,4,5-Tetrahydro-5-methyl-2-((5-methyl-1H-imidazol-4-yl)methyl)-1H-pyrido(4,3-b)indol-1-one
Thuốc đường tiêu hóa
Thuốc Gốc
Small Molecule
CAS: 122852-42-0
ATC: A03AE01
ĐG : GlaxoSmithKline Inc. , http://www.gsk.com
CTHH: C17H18N4O
PTK: 294.351
Alosetron is a 5-HT3 antagonist used only for the management of severe diarrhoea-predominant irritable bowel syndrome (IBS) in women. Alosetron has an antagonist action on the 5-HT3 receptors and thus may modulate serotonin-sensitive gastrointestinal (GI) processes. Alosetron was voluntarily withdrawn from the US market in November 2000 by the manufacturer due to numerous reports of severe adverse effects including ischemic colitis, severely obstructed or ruptured bowel, and death. In June 2002, the FDA approved a supplemental new drug application allowing the remarketing of the drug under restricted conditions of use.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H18N4O
Phân tử khối
294.351
Monoisotopic mass
294.148061218
InChI
InChI=1S/C17H18N4O/c1-11-13(19-10-18-11)9-21-8-7-15-16(17(21)22)12-5-3-4-6-14(12)20(15)2/h3-6,10H,7-9H2,1-2H3,(H,18,19)
InChI Key
InChIKey=JSWZEAMFRNKZNL-UHFFFAOYSA-N
IUPAC Name
5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-1H,2H,3H,4H,5H-pyrido[4,3-b]indol-1-one
Traditional IUPAC Name
alosetron
SMILES
CN1C2=C(C3=CC=CC=C13)C(=O)N(CC1=C(C)NC=N1)CC2
Độ hòa tan
4.38e-01 g/l
logP
2
logS
-2.8
pKa (strongest acidic)
13.32
pKa (Strongest Basic)
6.81
PSA
53.92 Å2
Refractivity
86.41 m3·mol-1
Polarizability
32.52 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Alosetron is a potent and selective antagonist of the serotonin 5-HT3 receptor type. Activation of these receptors and the resulting neuronal depolarization affects the regulation of visceral pain, colonic transit, and GI secretions processes that are related to IBS. By blocking these receptors, alosetron is able to effectively control IBS.
Cơ Chế Tác Dụng : Alosetron is a 5-HT3 antagonist used only for the management of severe diarrhoea-predominant irritable bowel syndrome (IBS) in women. Alosetron has an antagonist action on the 5-HT3 receptors and thus may modulate serotonin-sensitive gastrointestinal (GI) processes. Alosetron was voluntarily withdrawn from the US market in November 2000 by the manufacturer due to numerous reports of severe adverse effects including ischemic colitis, severely obstructed or ruptured bowel, and death. In June 2002, the FDA approved a supplemental new drug application allowing the remarketing of the drug under restricted conditions of use. Alosetron is a potent and selective 5-HT3 receptor antagonist. 5-HT3 receptors are nonselective cation channels that are extensively distributed on enteric neurons in the human gastrointestinal tract, as well as other peripheral and central locations. Activation of these channels and the resulting neuronal depolarization affect the regulation of visceral pain, colonic transit and gastrointestinal secretions, processes that relate to the pathophysiology of irritable bowel syndrome (IBS). 5-HT3 receptor antagonists such as alosetron inhibit activation of non-selective cation channels which results in the modulation of serotonin-sensitive GI motor and sensory processes.
Dược Động Học :
▧ Absorption :
50-60 %
▧ Volume of Distribution :
* 65 to 95 L
▧ Protein binding :
82%
▧ Metabolism :
Hepatic, via microsomal cytochrome P450 (CYP)
▧ Route of Elimination :
Renal elimination of unchanged alosetron accounts for only 6% of the dose. Alosetron is extensively metabolized in humans.
▧ Half Life :
1.5 hours
▧ Clearance :
* 600 mL/min
Chỉ Định : Only for the treatment of symptoms of severe diarrhea-predominant irritable bowel syndrome (IBS) in women with chronic symptoms (generally lasting greater than 6 months) who does not present with anatomic or biochemical GI abnormalities and have not responded to conventional therapy.
Tương Tác Thuốc :
  • Thiabendazole The strong CYP1A2 inhibitor, Thiabendazole, may increase the effects and toxicity of Alosetron by decreasing Alosetron metabolism and clearance. Monitor for changes in the therapeutic and adverse effects of Alosetron if Thiabendazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Lotronex 0.5 mg tablet
    Giá bán buôn : USD >14.3
    Đơn vị tính : tablet
  • Biệt dược thương mại : Lotronex 1 mg tablet
    Giá bán buôn : USD >19.47
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Lotronex
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00969
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2099
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506274
ChemSpider
http://www.chemspider.com/Chemical-Structure.2015.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50131429
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0173-0738-00
PharmGKB
http://www.pharmgkb.org/drug/PA164745502
Wikipedia
http://en.wikipedia.org/wiki/Alosetron
RxList
http://www.rxlist.com/cgi/generic3/alosetron.htm
Drugs.com
http://www.drugs.com/cdi/alosetron.html
... loading
... loading