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药品详细

Reboxetine(瑞波西汀)

化学结构式图
中文名
瑞波西汀
英文名
Reboxetine
分子式
C19H23NO3
化学名
(2S)-2-[(S)-2-ethoxyphenoxy(phenyl)methyl]morpholine
分子量
Average: 313.3908
Monoisotopic: 313.167793607
CAS号
98769-81-4
ATC分类
N06A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Reboxetine is an antidepressant drug used in the treatment of clinical depression, panic disorder and ADD/ADHD. Its mesylate (i.e. methanesulfonate) salt is sold under tradenames including Edronax, Norebox, Prolift, Solvex, Davedax or Vestra. Reboxetine has two chiral centers, but it only exists as two enantiomers, (R,R)-(-)- and (S,S)-(+)-reboxetine.

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    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Fleishaker JC: Clinical pharmacokinetics of reboxetine, a selective norepinephrine reuptake inhibitor for the treatment of patients with depression. Clin Pharmacokinet. 2000 Dec;39(6):413-27. Pubmed
    2. Edwards DM, Pellizzoni C, Breuel HP, Berardi A, Castelli MG, Frigerio E, Poggesi I, Rocchetti M, Dubini A, Strolin Benedetti M: Pharmacokinetics of reboxetine in healthy volunteers. Single oral doses, linearity and plasma protein binding. Biopharm Drug Dispos. 1995 Aug;16(6):443-60. Pubmed
    3. Wienkers LC, Allievi C, Hauer MJ, Wynalda MA: Cytochrome P-450-mediated metabolism of the individual enantiomers of the antidepressant agent reboxetine in human liver microsomes. Drug Metab Dispos. 1999 Nov;27(11):1334-40. Pubmed
    4. Kasper S, el Giamal N, Hilger E: Reboxetine: the first selective noradrenaline re-uptake inhibitor. Expert Opin Pharmacother. 2000 May;1(4):771-82. Pubmed
    5. Fleishaker JC: Clinical pharmacokinetics of reboxetine, a selective norepinephrine reuptake inhibitor for the treatment of patients with depression. Clin Pharmacokinet. 2000 Dec;39(6):413-27. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Phenylpropylamines
    Substructures
    • Benzyl Alcohols and Derivatives
    • Aliphatic and Aryl Amines
    • Phenols and Derivatives
    • Ethers
    • Benzene and Derivatives
    • Catechols
    • Heterocyclic compounds
    • Aromatic compounds
    • Anisoles
    • Phenylpropylamines
    • Morpholines
    • Phenyl Esters
    适应症
    药理
    Indication For the treatment of clinical depression.
    Pharmacodynamics Reboxetine is a selective noradrenaline reuptake inhibitor (NaRI), the first drug of new antidepressant class. Reboxetine is an a-ariloxybenzyl derivative of morpholine. Reboxetine is primarily used to treat depression but has also been found useful in the treatment of narcolepsy and panic disorders.
    Mechanism of action Reboxetine is a selective inhibitor of noradrenaline reuptake. It inhibits noradrenaline reuptake in vitro to a similar extent to the tricyclic antidepressant desmethylimipramine. Reboxetine does not affect dopamine or serotonin reuptake and it has low in vivo and in vitro affinity for adrenergic, cholinergic, histaminergic, dopaminergic and serotonergic receptors.
    Absorption Reboxetine is rapidly and extensively absorbed following oral administration.
    Volume of distribution Not Available
    Protein binding 98%
    Metabolism
    Reboxetine is metabolized by dealkylation, hydroxylation and oxidation followed by glucuronide or sulphate conjugation. It is metabolized by the cytochrome P450 CYP isoenzyme 3A4.
    Route of elimination Not Available
    Half life 12.5 hours
    Clearance Not Available
    Toxicity Reports of seizures (rare) have been reported
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 170-171 °C (Mesylate salt) Not Available
    water solubility 8 mg/mL (Mesylate salt) Not Available
    logP 3.1 Not Available
    Predicted Properties
    Property Value Source
    water solubility 2.23e-02 g/l ALOGPS
    logP 3.06 ALOGPS
    logP 3.28 ChemAxon
    logS -4.2 ALOGPS
    pKa (strongest basic) 7.91 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 4 ChemAxon
    hydrogen donor count 1 ChemAxon
    polar surface area 39.72 ChemAxon
    rotatable bond count 6 ChemAxon
    refractivity 89.48 ChemAxon
    polarizability 34.17 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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