药品详细

Regadenoson(的regadenoson)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

的regadenoson

英文名

Regadenoson

分子式

C₁₅H₁₈N₈O₅

化学名

1-{6-amino-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-9H-purin-2-yl}-N-methyl-1H-pyrazole-4-carboxamide

分子量

Average: 390.354
Monoisotopic: 390.140015726

CAS号

313348-27-5

ATC分类

C01E 未知

药物类型

small molecule

阶段

approved

商品名

同义名

基本介绍

Regadenoson is an A2A adenosine receptor agonist that causes coronary vasodilation and used for myocardial perfusion imagining. Manufactured by Astellas and FDA approved April 10, 2008.

生产厂家

Astellas pharma us inc

封装厂家

参考

Synthesis Reference

Not Available

General Reference

Mitka M: New stress test agents reduce adverse effects. JAMA. 2008 May 14;299(18):2140. Pubmed
Lieu HD, Shryock JC, von Mering GO, Gordi T, Blackburn B, Olmsted AW, Belardinelli L, Kerensky RA: Regadenoson, a selective A2A adenosine receptor agonist, causes dose-dependent increases in coronary blood flow velocity in humans. J Nucl Cardiol. 2007 Jul;14(4):514-20. Pubmed
Zoghbi GJ, Iskandrian AE: Selective adenosine agonists and myocardial perfusion imaging. J Nucl Cardiol. 2012 Feb;19(1):126-41. doi: 10.1007/s12350-011-9474-9. Pubmed
FDA label

剂型

规格

化合物类型

Type	small molecule

Classes

Not Available

Substructures

Not Available

适应症

药理

Indication	Diagnostic agent for radionuclide myocardial perfusion imaging (MPI)
Pharmacodynamics	Regadenoson rapidly increases coronary blood flow (CBF) which is sustained for a short duration. Mean average peak velocity increased to greater than twice baseline by 30 seconds and decreased to less than twice the baseline level within 10 minutes. Myocardial uptake of the radiopharmaceutical is proportional to (CBF). Regadenoson increases blood flow in normal coronary arteries but not in stenotic (blocked) arteries. The significance of this finding is that stenotic arteries will take up less of the radiopharmaceutical than normal coronary arteries, resulting in a signal that is less intense in these areas.
Mechanism of action	Regadenoson is an selective low-affinity (Ki= 1.3 µM) A2A receptor agonist that mimics the effects of adenosine in causing coronary vasodilatation and increasing myocardial blood flow. It is a very weak agonist of the A1 adenosine receptor (Ki > 16.5 µM). Furthermore, it has negligible affinity to A2B and A3 adenosine receptors. Regadenoson is undergoing trials for use in pharmacological stress tests. Adenosine slows conduction time through the A-V node, can interrupt the reentry pathways through the A-V node, and can restore normal sinus rhythm in patients with paroxysmal supraventricular tachycardia (PSVT), including PSVT associated with Wolff-Parkinson-White Syndrome.
Absorption	The pharmacokinetic profile of regadenoson is best described by a 3-compartment model. T max, injection = 1 to 3 minutes; Onset of pharmacodynamic response = 1 to 3 minutes; E max 12.3 ng/mL
Volume of distribution	Central compartment: 11.5 L; Steady state: 78.7 L
Protein binding	Not Available
Metabolism	The metabolism of regadenoson is unknown in humans. The cytochrome P450 enzyme system is not likely to be involved with the metabolism of regadenoson.
Route of elimination	58% of total regadenoson eliminate is via renal excretion
Half life	Initial phase: 2-4 minutes; Intermediate phase: 30 minutes (this phase coincides with a loss of the pharmacodynamic effect); Terminal phase: 2 hours
Clearance	Average plasma renal clearance = 450 mL/min. As this value is larger than the glomerular filtration rate, this suggests occurrence of renal tubular secretion.
Toxicity	The most common (incidence ≥ 5%) adverse reactions to regadenoson are dyspnea, headache, flushing, chest discomfort, dizziness, angina pectoris, chest pain, and nausea. MTD (male, supine position): 20 µg/kg; MTD (male, standing position): 10 µg/kg;
Affected organisms	Humans and other mammals
Pathways	Not Available

理化性质

Properties

State

liquid

Experimental Properties

Not Available

Predicted Properties

Property	Value	Source
water solubility	4.85e+00 g/l	ALOGPS
logP	-0.89	ALOGPS
logP	-2.3	ChemAxon
logS	-1.9	ALOGPS
pKa (strongest acidic)	12.37	ChemAxon
pKa (strongest basic)	1.63	ChemAxon
physiological charge	0	ChemAxon
hydrogen acceptor count	10	ChemAxon
hydrogen donor count	5	ChemAxon
polar surface area	186.46	ChemAxon
rotatable bond count	4	ChemAxon
refractivity	95.48	ChemAxon
polarizability	37.48	ChemAxon

药物相互作用

Drug	Interaction
Aminophylline	Reduces duration of >2-fold increase in peak flow velocity. No effect on heart rate increase.
Caffeine	Caffeine may diminish the vasodilatory effect of Regadenoson. Regadenoson prescribing information recommends avoiding using caffeine or other methylxanthine containing products (e.g., theophylline) for at least 12 hours prior the the administration of regadenoson. The impact of low doses of caffeine-containing products such as coffee, tea, and colas is unclear.
Dipyridamole	Dipyridamole may change the effects of regadenoson. When possible, withhold dipyridamole for at least two days prior to regadenoson administration.
Theophylline	Non-specific adenosine receptor antagonist may interfere with the vasodilation activity of regadenoson. Avoid methylxanthines for at least 12 hours before administration of regadenoson.

食物相互作用

Not Available

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