Tìm theo
Pramipexole
Các tên gọi khác (6 ) :
  • (-)-Pramipexole
  • (S)-N  6-propyl-4,5,6,7-tetrahydro-1,3-benzothiazole-2,6-diamine
  • 2,6-Benzothiazolediamine, 4,5,6,7-tetrahydro-N(sup 6)-propyl-, (S)-
  • Pramipexol
  • Pramipexole
  • Pramipexolum
Thực phẩm tăng cường hệ miễn dịch
Thuốc Gốc
Small Molecule
CAS: 104632-26-0
ATC: N04BC05
ĐG : Barr Pharmaceuticals
CTHH: C10H17N3S
PTK: 211.327
Pramipexole is a medication indicated for treating Parkinson's disease and restless legs syndrome (RLS). It is also sometimes used off-label as a treatment for cluster headache or to counteract the problems with low libido experienced by some users of SSRI antidepressant drugs. Pramipexole has shown robust effects on pilot studies in bipolar disorder. Pramipexole is classified as a non-ergoline dopamine agonist.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H17N3S
Phân tử khối
211.327
Monoisotopic mass
211.114318249
InChI
InChI=1S/C10H17N3S/c1-2-5-12-7-3-4-8-9(6-7)14-10(11)13-8/h7,12H,2-6H2,1H3,(H2,11,13)/t7-/m0/s1
InChI Key
InChIKey=FASDKYOPVNHBLU-ZETCQYMHSA-N
IUPAC Name
(6S)-6-N-propyl-4,5,6,7-tetrahydro-1,3-benzothiazole-2,6-diamine
Traditional IUPAC Name
(-)-pramipexole
SMILES
CCCN[C@H]1CCC2=C(C1)SC(N)=N2
Độ hòa tan
1.40e-01 g/l
logP
0.4
logS
-3.2
pKa (strongest acidic)
17.66
pKa (Strongest Basic)
10.31
PSA
50.94 Å2
Refractivity
59.77 m3·mol-1
Polarizability
24.47 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Pramipexole 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 precise mechanism of action of Pramipexole as a treatment for Parkinson's disease is unknown, although it is believed to be related to its ability to stimulate dopamine receptors in the striatum. This conclusion is supported by electrophysiologic studies in animals that have demonstrated that Pramipexole 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.
Cơ Chế Tác Dụng : Pramipexole is a medication indicated for treating Parkinson's disease and restless legs syndrome (RLS). It is also sometimes used off-label as a treatment for cluster headache or to counteract the problems with low libido experienced by some users of SSRI antidepressant drugs. Pramipexole has shown robust effects on pilot studies in bipolar disorder. Pramipexole is classified as a non-ergoline dopamine agonist. The precise mechanism of action of Pramipexole as a treatment for Parkinson's disease is unknown, although it is believed to be related to its ability to stimulate dopamine receptors in the striatum.
Dược Động Học :
▧ Absorption :
Rapid. Absolute bioavailability is greater than 90%, indicating that pramipexole is well absorbed and undergoes little presystemic metabolism. Food does not affect the extent of absorption.
▧ Volume of Distribution :
* 500 L
▧ Protein binding :
About 15% bound to plasma proteins.
▧ Metabolism :
No metabolites have been identified in plasma or urine.
▧ Route of Elimination :
Urinary excretion is the major route of pramipexole elimination, with 90% of a pramipexole dose recovered in urine, almost all as unchanged drug. Nonrenal routes may contribute to a small extent to pramipexole elimination, although no metabolites have been identified in plasma or urine.
▧ Half Life :
8 hours
▧ Clearance :
* renal cl=400 mL/min
Chỉ Định : For the treatment of signs and symptoms of idiopathic Parkinson's disease
Tương Tác Thuốc :
  • Cimetidine Cimetidine may increase the effect and toxicity of pramipexole.
  • Dihydrocodeine Dihydrocodeine may enhance the sedative effect of pramipexole. It is recommended to monitor therapy
  • Paliperidone The atypical antipsychotic agent, paliperidone, may decrease the therapeutic effect of the anti-Parkinson's agent, pramipexole. 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, Pramipexole. Consider alternate therapy or monitor for decreased effects of both agents.
  • Triprolidine The CNS depressants, Triprolidine and Pramipexole, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Ziprasidone The atypical antipsychotic, ziprasidone, may antagonize the effect of the dopamine agonist, pramipexole. Consider alternate therapy or monitor for worsening of movement disorder.
  • Zuclopenthixol Antagonism may occur between zuclopenthixol, a dopamine D2 receptor antagonist, and pramipexole, 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 - Oral - 0.125 mg
Tablet - Oral - 0.25 mg
Tablet - Oral - 0.5 mg
Tablet - Oral - 1 mg
Tablet - Oral - 1.5 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00413
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00559
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50226040
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0597-0183-90
PharmGKB
http://www.pharmgkb.org/drug/PA164742949
Wikipedia
http://en.wikipedia.org/wiki/Pramipexole
RxList
http://www.rxlist.com/cgi/generic/prampex.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/mir1271.shtml
Drugs.com
http://www.drugs.com/cdi/pramipexole.html
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