Tìm theo
Ropinirole
Các tên gọi khác (3) :
  • Ropinirol
  • Ropinirole
  • Ropinirolum
Thuốc chống Parkinson
Thuốc Gốc
Small Molecule
CAS: 91374-21-9
ATC: N04BC04
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C16H24N2O
PTK: 260.3746
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]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H24N2O
Phân tử khối
260.3746
Monoisotopic mass
260.1888634
InChI
InChI=1S/C16H24N2O/c1-3-9-18(10-4-2)11-8-13-6-5-7-15-14(13)12-16(19)17-15/h5-7H,3-4,8-12H2,1-2H3,(H,17,19)
InChI Key
InChIKey=UHSKFQJFRQCDBE-UHFFFAOYSA-N
IUPAC Name
4-[2-(dipropylamino)ethyl]-2,3-dihydro-1H-indol-2-one
Traditional IUPAC Name
ropinirole
SMILES
CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
Độ tan chảy
243-250 °C
Độ hòa tan
133 mg/mL
logP
2.70
logS
-2.9
pKa (strongest acidic)
13.24
pKa (Strongest Basic)
10.17
PSA
32.34 Å2
Refractivity
81.43 m3·mol-1
Polarizability
31.19 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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] 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.
Dược Động Học :
▧ 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%).
▧ 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]
Độc Tính : 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.
Chỉ Định : For the treatment of the signs and symptoms of idiopathic Parkinson's disease. Also used for the treatment of restless legs syndrome.
Tương Tác Thuốc :
  • 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.
Liều Lượng & Cách Dùng : Tablet, film coated - Oral - 0.25 mg
Tablet, film coated - Oral - 1 mg
Tablet, film coated - Oral - 2 mg
Tablet, film coated - Oral - 3 mg
Tablet, film coated - Oral - 4 mg
Tablet, film coated - Oral - 5 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Adartrel
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : ReQuip
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : ReQuip CR
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : ReQuip XL
  • Công ty :
    Sản phẩm biệt dược : Ronirol
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00268
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5095
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507918
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07564
ChemSpider
http://www.chemspider.com/Chemical-Structure.4916.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0007-4890-20
PharmGKB
http://www.pharmgkb.org/drug/PA164749035
Wikipedia
http://en.wikipedia.org/wiki/Ropinirole
RxList
http://www.rxlist.com/cgi/generic/ropinirole.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/req1372.shtml
Drugs.com
http://www.drugs.com/cdi/ropinirole.html
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