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药品详细

Ondansetron(昂丹司琼)

化学结构式图
中文名
昂丹司琼
英文名
Ondansetron
分子式
C18H19N3O
化学名
9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-2,3,4,9-tetrahydro-1H-carbazol-4-one
分子量
Average: 293.363
Monoisotopic: 293.152812245
CAS号
99614-02-5
ATC分类
A04A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

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]

生产厂家
  • Akorn strides llc
  • Apotex inc
  • Apotex inc richmond hill
  • App pharmaceuticals llc
  • Aurobindo pharma ltd
  • Barr laboratories inc
  • Baxter healthcare corp
  • Baxter healthcare corp anesthesia and critical care
  • Bedford laboratories
  • Bedford laboratories div ben venue laboratories inc
  • Claris lifesciences ltd
  • Dr reddys laboratories ltd
  • Emcure pharmaceuticals ltd
  • Gland pharma ltd
  • Glaxosmithkline
  • Glenmark generics ltd
  • Hikma farmaceutica (portugal) sa
  • Hospira inc
  • Kv pharmaceutical co
  • Lannett holdings inc
  • Luitpold pharmaceuticals inc
  • Mylan pharmaceuticals inc
  • Natco pharma ltd
  • Par pharmaceutical
  • Par pharmaceutical inc
  • Pharmaforce inc
  • Pliva hrvatska doo
  • Roxane laboratories inc
  • Sandoz canada inc
  • Sandoz inc
  • Spectrum pharmaceuticals
  • Sun pharmaceutical industries ltd
  • Taro pharmaceutical industries ltd
  • Taro pharmaceuticals ireland ltd
  • Teva parenteral medicines inc
  • Teva pharmaceuticals usa inc
  • West ward pharmaceutical corp
  • Wockhardt ltd
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Ramsook C, Sahagun-Carreon I, Kozinetz CA, Moro-Sutherland D: A randomized clinical trial comparing oral ondansetron with placebo in children with vomiting from acute gastroenteritis. Ann Emerg Med. 2002 Apr;39(4):397-403. Pubmed
  2. Yilmaz HL, Yildizdas RD, Sertdemir Y: Clinical trial: oral ondansetron for reducing vomiting secondary to acute gastroenteritis in children—a double-blind randomized study. Aliment Pharmacol Ther. 2010 Jan;31(1):82-91. Epub . Pubmed
  3. Gregory RE, Ettinger DS: 5-HT3 receptor antagonists for the prevention of chemotherapy-induced nausea and vomiting. A comparison of their pharmacology and clinical efficacy. Drugs. 1998 Feb;55(2):173-89. Pubmed
  4. Gan TJ: Selective serotonin 5-HT3 receptor antagonists for postoperative nausea and vomiting: are they all the same? CNS Drugs. 2005;19(3):225-38. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Carbazoles
  • Tryptamines and Derivatives
Substructures
  • Indoles and Indole Derivatives
  • Carbazoles
  • Pyrroles
  • Benzene and Derivatives
  • Tryptamines and Derivatives
  • Imidazoles
  • Heterocyclic compounds
  • Aromatic compounds
  • Imines
  • Cyanamides
  • Cyclohexenes and Derivatives
  • Ketones
适应症
药理
Indication 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.
Pharmacodynamics 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.
Mechanism of action 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.
Absorption Ondansetron is well absorbed after oral administration and undergoes limited first-pass metabolism.
Volume of distribution Not Available
Protein binding 70%-76% (Plasma protein binding)
Metabolism
Hepatic
Route of elimination Not Available
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)]
Toxicity Low blood pressure and fainting, sudden blindness, severe constipation
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
logP 2.4 Not Available
Predicted Properties
Property Value Source
water solubility 2.48e-01 g/l ALOGPS
logP 2.56 ALOGPS
logP 2.35 ChemAxon
logS -3.1 ALOGPS
pKa (strongest acidic) 15.39 ChemAxon
pKa (strongest basic) 7.34 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 39.82 ChemAxon
rotatable bond count 2 ChemAxon
refractivity 86.78 ChemAxon
polarizability 33.16 ChemAxon
药物相互作用
Drug Interaction
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.
食物相互作用
  • Take without regard to meals.

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