Tìm theo
Ondansetron
Các tên gọi khác (1) :
  • Zofran odt
Thuốc đường tiêu hóa
Thuốc Gốc
Small Molecule
CAS: 99614-02-5
ATC: A04AA01
ĐG : Aceto Pharma Inc. , http://www.aceto.com
CTHH: C18H19N3O
PTK: 293.363
A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H19N3O
Phân tử khối
293.363
Monoisotopic mass
293.152812245
InChI
InChI=1S/C18H19N3O/c1-12-19-9-10-21(12)11-13-7-8-16-17(18(13)22)14-5-3-4-6-15(14)20(16)2/h3-6,9-10,13H,7-8,11H2,1-2H3
InChI Key
InChIKey=FELGMEQIXOGIFQ-UHFFFAOYSA-N
IUPAC Name
9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-2,3,4,9-tetrahydro-1H-carbazol-4-one
Traditional IUPAC Name
ondansetron
SMILES
CN1C2=C(C3=CC=CC=C13)C(=O)C(CN1C=CN=C1C)CC2
Độ hòa tan
2.48e-01 g/l
logP
2.4
logS
-3.1
pKa (strongest acidic)
15.39
pKa (Strongest Basic)
7.34
PSA
39.82 Å2
Refractivity
86.78 m3·mol-1
Polarizability
33.16 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist, not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors. The serontonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery, and centrally in the chemoreceptor trigger zone of the area postrema. The temporal relationship between the emetogenic action of emetogenic drugs and the release of serotonin, as well as the efficacy of antiemetic agents suggest that chemotherapeutic agents release serotonin from the enterochromaffin cells of the small intestine by causing degenerative changes in the GI tract. The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT3 receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting.
Cơ Chế Tác Dụng : A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties. [PubChem] Ondansetron is a selective serotonin 5-HT3 receptor antagonist. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone.
Dược Động Học :
▧ Absorption :
Ondansetron is well absorbed after oral administration and undergoes limited first-pass metabolism.
▧ Protein binding :
70%-76% (Plasma protein binding)
▧ Metabolism :
Hepatic
▧ Half Life :
5.7 hours
▧ Clearance :
* 0.38 L/h/kg [Normal Adult Volunteers (19-40 yrs)] * 0.32 L/h/kg [Normal Adult Volunteers (61-74 yrs)] * 0.26 L/h/kg [Normal Adult Volunteers (>=75 yrs)]
Độc Tính : Low blood pressure and fainting, sudden blindness, severe constipation
Chỉ Định : For the prevention of nausea and vomiting associated with emetogenic cancer chemotherapy, postoperation, and radiation. Also used for the treatment of postoperative nausea and vomiting.
Tương Tác Thuốc :
  • Asenapine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Crizotinib Concurrent use with crizotinib may decrease QTc interval. Consider alternative therapy.
  • Ezogabine Concurrent use of ezogabine and ondansetron can increase QTc interval. Consider alternate therapy.
  • Indacaterol Both indacaterol and ondansetron prolong the QT interval. Consider alternate therapy.
  • Pazopanib Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Telavancin Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Liều Lượng & Cách Dùng : Liquid - Intravenous
Liquid - Oral
Solution - Intravenous
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Zofran
  • Công ty :
    Sản phẩm biệt dược : Zofran ODT
  • Công ty :
    Sản phẩm biệt dược : Zophren
  • Công ty :
    Sản phẩm biệt dược : Zuplenz
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00904
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4595
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504819
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07325
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00456
ChemSpider
http://www.chemspider.com/Chemical-Structure.4434.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50000493
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0338-1762-41
PharmGKB
http://www.pharmgkb.org/drug/PA450705
Wikipedia
http://en.wikipedia.org/wiki/Ondansetron
RxList
http://www.rxlist.com/cgi/generic/ondansetron.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/zof1501.shtml
Drugs.com
http://www.drugs.com/cdi/ondansetron.html
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