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药品详细

Pramipexole(普拉克索)

化学结构式图
中文名
普拉克索
英文名
Pramipexole
分子式
C10H17N3S
化学名
(6S)-6-N-propyl-4,5,6,7-tetrahydro-1,3-benzothiazole-2,6-diamine
分子量
Average: 211.327
Monoisotopic: 211.114318249
CAS号
104632-26-0
ATC分类
N04B 未知
药物类型
small molecule
阶段
approved
商品名
Mirapex (Boehringer Ingelheim);
同义名
Furfuryl Acetate;Pramipexol;Pramipexol [Spanish];pramipexole;Pramipexole 2HCl Monohydrate;Pramipexole hydrochloride;Pramipexolum [Latin];
基本介绍

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.

生产厂家
  • Boehringer ingelheim
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Mierau J, Schneider FJ, Ensinger HA, Chio CL, Lajiness ME, Huff RM: Pramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors. Eur J Pharmacol. 1995 Jun 23;290(1):29-36. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes Not Available
Substructures Not Available
适应症
PARKINSON 帕金森氏症;
药理
Indication For the treatment of signs and symptoms of idiopathic Parkinson's disease
Pharmacodynamics 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.
Mechanism of action 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.
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
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
logP 0.4 Not Available
Predicted Properties
Property Value Source
water solubility 1.40e-01 g/l ALOGPS
logP 2.18 ALOGPS
logP 1.76 ChemAxon
logS -3.2 ALOGPS
pKa (strongest acidic) 17.66 ChemAxon
pKa (strongest basic) 10.31 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 3 ChemAxon
hydrogen donor count 2 ChemAxon
polar surface area 50.94 ChemAxon
rotatable bond count 3 ChemAxon
refractivity 59.77 ChemAxon
polarizability 24.47 ChemAxon
药物相互作用
Drug Interaction
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.
食物相互作用
  • Take without regard to meals, however if nausea is a problem, taking the product with food may reduce its incidence.

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