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药品详细

Ropinirole(罗匹尼罗)

化学结构式图
中文名
罗匹尼罗
英文名
Ropinirole
分子式
C16H24N2O
化学名
4-[2-(dipropylamino)ethyl]-2,3-dihydro-1H-indol-2-one
分子量
Average: 260.3746
Monoisotopic: 260.1888634
CAS号
91374-21-9
ATC分类
N04B 未知
药物类型
small molecule
阶段
approved
商品名
Requip (GlaxoSmithKline);ReQuip CR (GlaxoSmithKline);ReQuip XL (GlaxoSmithKline);
同义名
Ropinirol [INN-Spanish];ropinirole;Ropinirole HCl;Ropinirole hydrochloride;Ropinirolum [INN-Latin];
基本介绍

Ropinirole is a non-ergoline dopamine agonist, manufactured by GlaxoSmithKline. It is used in the treatment of Parkinson’s disease, and is also one of two medications in the United States with an FDA-approved indication for the treatment of restless legs syndrome (the other being Pramipexole). [Wikipedia]

生产厂家
  • Alembic ltd
  • Corepharma llc
  • Glaxosmithkline
  • Glenmark generics ltd
  • Huahai us inc
  • Mylan pharmaceuticals inc
  • Roxane laboratories inc
  • Smithkline beecham corp dba glaxosmithkline
  • Teva pharmaceuticals usa inc
  • Wockhardt ltd
  • Zydus pharmaceuticals usa inc
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes
  • Indoles and Indole Derivatives
  • Phenethylamines
  • Lactams
Substructures
  • Indoles and Indole Derivatives
  • Amino Ketones
  • Benzene and Derivatives
  • Carboxylic Acids and Derivatives
  • Aliphatic and Aryl Amines
  • Phenethylamines
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamides and Derivatives
  • Lactams
  • Anilines
  • Pyrrolines
适应症
PARKINSON 帕金森氏症;
药理
Indication For the treatment of the signs and symptoms of idiopathic Parkinson's disease. Also used for the treatment of restless legs syndrome.
Pharmacodynamics Ropinirole is a nonergot dopamine agonist with high relative in vitro specificity and full intrinsic activity at the D2 subfamily of dopamine receptors, binding with higher affinity to D3 than to D2 or D4 receptor subtypes. The relevance of D3 receptor binding in Parkinson's disease is unknown. The mechanism of ropinirole-induced postural hypotension is presumed to be due to a D2 -mediated blunting of the noradrenergic response to standing and subsequent decrease in peripheral vascular resistance.
Mechanism of action Ropinirole binds the dopamine receptors D3 and D2. Although the precise mechanism of action of ropinirole as a treatment for Parkinson's disease is unknown, it is believed to be related to its ability to stimulate these receptors in the striatum. This conclusion is supported by electrophysiologic studies in animals that have demonstrated that ropinirole influences striatal neuronal firing rates via activation of dopamine receptors in the striatum and the substantia nigra, the site of neurons that send projections to the striatum.
Absorption Absolute bioavailability is 55%, indicating a first pass effect. Food does not affect the extent of absorption.
Volume of distribution
  • 7.5 L/kg
  • 525 L
Protein binding 40% bound to plasma proteins with a blood-to-plasma ratio of 1:1.
Metabolism
Hepatic. Ropinirole is extensively metabolized to inactive metabolites via N -despropylation and hydroxylation pathways, largely by the P450 isoenzyme CYP1A2. N-despropyl ropinirole is the predominant metabolite found in urine (40%), followed by the carboxylic acid metabolite (10%), and the glucuronide of the hydroxy metabolite (10%).

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Ropinirole
    		N-despropyl ropinirole Details
    Route of elimination Ropinirole is extensively metabolized by the liver to inactive metabolites, and less than 10% of the administered dose is excreted as unchanged drug in urine.
    Half life 6 hours
    Clearance
    • 47 L/hr [after oral administration to Parkinson’s disease patients and patients with Restless Legs Syndrome]
    Toxicity Symptoms of overdose include agitation, chest pain, confusion, drowsiness, facial muscle movements, grogginess, increased jerkiness of movement, symptoms of low blood pressure (dizziness, light-headedness)upon standing, nausea, and vomiting.
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 243-250 °C Not Available
    water solubility 133 mg/mL Not Available
    logP 2.70 ADLARD,M ET AL. (1995)
    Predicted Properties
    Property Value Source
    water solubility 3.53e-01 g/l ALOGPS
    logP 3.16 ALOGPS
    logP 3.06 ChemAxon
    logS -2.9 ALOGPS
    pKa (strongest acidic) 13.24 ChemAxon
    pKa (strongest basic) 10.17 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 2 ChemAxon
    hydrogen donor count 1 ChemAxon
    polar surface area 32.34 ChemAxon
    rotatable bond count 7 ChemAxon
    refractivity 81.43 ChemAxon
    polarizability 31.19 ChemAxon
    药物相互作用
    Drug Interaction
    Ciprofloxacin Ciprofloxacin may increase the effect and toxicity of ropinirole.
    Dihydrocodeine Dihydrocodeine may enhance the sedative effect of ropinirole. It is recommended to monitor therapy
    Fluvoxamine Increases the effect and toxicity of ropinirole
    Paliperidone The atypical antipsychotic agent, paliperidone, may decrease the therapeutic effect of the anti-Parkinson's agent, ropinirole. This interaction may be due to the dopamine antagonist properties of paliperidone. Consider an alternate antipsychotic in those with Parkinson's disease or consider using clozapine or quetiapine if an atypical antipsychotic is necessary.
    Thiothixene Thiothixene may antaonize the effects of the anti-Parkinsonian agent, Ropinirole. Consider alternate therapy or monitor for decreased effects of both agents.
    Ziprasidone The atypical antipsychotic, ziprasidone, may antagonize the effect of the dopamine agonist, ropinirole. Consider alternate therapy or monitor for worsening of movement disorder.
    Zuclopenthixol Antagonism may occur between zuclopenthixol, a dopamine D2 receptor antagonist, and ropinirole, a dopamine agonist. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of both agents if concurrent therapy is initiated, discontinued or dose(s) changed.
    食物相互作用
    Not Available

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