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药品详细

Sertindole(舍吲哚)

化学结构式图
中文名
舍吲哚
英文名
Sertindole
分子式
C24H26ClFN4O
化学名
1-(2-{4-[5-chloro-1-(4-fluorophenyl)-1H-indol-3-yl]piperidin-1-yl}ethyl)imidazolidin-2-one
分子量
Average: 440.941
Monoisotopic: 440.177917386
CAS号
106516-24-9
ATC分类
N05A 未知
药物类型
small molecule
阶段
approved, withdrawn
商品名
同义名
基本介绍

Sertindole, a neuroleptic, is one of the newer antipsychotic medications available. Serdolect is developed by the Danish pharmaceutical company H. Lundbeck. Like the other atypical antipsychotics, it has activity at dopamine and serotonin receptors in the brain. It is used in the treatment of schizophrenia. It is classified chemically as a phenylindole derivative. It was first marketed in 1996 in several European countries before being withdrawn two years later because of numerous cardiac adverse effects. It has once again been approved and should soon be available on the French and Australian market.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Kane JM, Tamminga CA: Sertindole (Serdolect): preclinical and clinical findings of a new atypical antipsychotic. Expert Opin Investig Drugs. 1997 Nov;6(11):1729-41. Pubmed
    2. Lewis R, Bagnall AM, Leitner M: Sertindole for schizophrenia. Cochrane Database Syst Rev. 2005 Jul 20;(3):CD001715. Pubmed
    3. Perquin LN: Treatment with the new antipsychotic sertindole for late-occurring undesirable movement effects. Int Clin Psychopharmacol. 2005 Nov;20(6):335-8. Pubmed
    4. Murdoch D, Keating GM: Sertindole : a review of its use in schizophrenia. CNS Drugs. 2006;20(3):233-55. Pubmed
    5. Sertindole: new drug. Another “atypical” neuroleptic; QT prolongation. Prescrire Int. 2007 Apr;16(88):59-62. Pubmed
    6. Lindstrom E, Levander S: Sertindole: efficacy and safety in schizophrenia. Expert Opin Pharmacother. 2006 Sep;7(13):1825-34. Pubmed
    7. Hertel P: Comparing sertindole to other new generation antipsychotics on preferential dopamine output in limbic versus striatal projection regions: mechanism of action. Synapse. 2006 Dec 1;60(7):543-52. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes Not Available
    Substructures Not Available
    适应症
    药理
    Indication Used in the treatment of schizophrenia.
    Pharmacodynamics Sertindole is an atypical antipsychotic at least as effective as haloperidol and risperidone in the treatment of neuroleptic-responsive schizophrenia. Sertindole improves negative symptoms, and is also effective for the treatment of neuroleptic-resistant schizophrenia. Sertindole is generally well tolerated and is associated with a low rate of extrapyramidal symptoms (EPS).
    Mechanism of action Sertindole is an antipsychotic drug with affinity for dopamine D2, serotonin 5-HT2A and 5-HT2C, and alpha1-adrenoreceptors. Preclinical studies suggest that sertindole acts preferentially on limbic and cortical dopaminergic neurons and clinical trials have confirmed that sertindole is effective at a low dopamine D2 occupancy level.
    Absorption Orally available.
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Hepatic. Sertindole is metabolized by cytochrome P450 isoenzymes CYP 2D6 and CYP 3A4.
    Route of elimination Not Available
    Half life 3 days
    Clearance Not Available
    Toxicity Not Available
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties Not Available
    Predicted Properties
    Property Value Source
    water solubility 9.63e-03 g/l ALOGPS
    logP 4.29 ALOGPS
    logP 3.77 ChemAxon
    logS -4.7 ALOGPS
    pKa (strongest acidic) 14.36 ChemAxon
    pKa (strongest basic) 8.59 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 2 ChemAxon
    hydrogen donor count 1 ChemAxon
    polar surface area 40.51 ChemAxon
    rotatable bond count 5 ChemAxon
    refractivity 131.77 ChemAxon
    polarizability 47.17 ChemAxon
    药物相互作用
    Drug Interaction
    Mesoridazine Increased risk of cardiotoxicity and arrhythmias
    Thioridazine Increased risk of cardiotoxicity and arrhythmias
    食物相互作用
    Not Available

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