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Methods and compositions for increasing patient tolerance during myocardial imaging methods

一种组合物、耐受性的技术，应用在腺苷A2A受体激动剂领域，能够解决限制应用、腺苷半衰期短等问题

Inactive Publication Date: 2011-12-28
GILEAD PALO ALTO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the short half-life of adenosine requires multiple treatments during the process, further limiting its application

Method used

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  • Methods and compositions for increasing patient tolerance during myocardial imaging methods
  • Methods and compositions for increasing patient tolerance during myocardial imaging methods
  • Methods and compositions for increasing patient tolerance during myocardial imaging methods

Examples

Experimental program
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Embodiment 1

[0211] The effect of caffeine on coronary artery dilation (1-10 mg / kg) and the hemodynamic changes of regadenosine (5 μg / kg, IV) were determined in conscious dogs. Caffeine dose-dependently reduces coronary dilation periods but does not affect the peak increase in coronary hyperemia induced by regadenosine. Caffeine (4 and 10 mg / kg) greatly reduced the effect of regadenosine on mean arterial pressure and heart rate. The results show that immediately using an A 2A Adenosine receptor agonists prior to pharmacological stress testing, caffeine administration can reduce the duration of drug-induced coronary dilation.

[0212] List of abbreviations:

[0213] CBF: coronary blood flow

[0214] MAP: mean arterial pressure

[0215] HR: heart rate

[0216] LVSP: left ventricular systolic pressure

[0217] method

[0218] Sixteen long-term measured male mongrel dogs weighing 22-30 kg were used in this study. Animal experiments were approved by the New York Medical College Animal C...

Embodiment 2

[0278] Purpose:

[0279] The primary objective was to evaluate the effect of a 200 mg oral dose of caffeine on regadenoson-induced increases in myocardial blood flow (MBF), measured approximately 2 hours after caffeine ingestion. The second purpose includes the following:

[0280] Response of regadenosine-induced heart rhythm (HR) with and without caffeine was evaluated.

[0281] The relationship between regadenosine-induced increases in MBF and changes in HR and whether it was modified by oral caffeine was evaluated.

[0282] Regadenosine-induced blood pressure (BP) responses were evaluated with and without caffeine.

[0283] To assess the safety and tolerability of regadenosine with and without caffeine.

[0284] To assess whether the effect of prior caffeine on regadenosine-induced MBF responses differs between male and female volunteers

[0285] Methodology:

[0286] This was a double-blind, crossover study of regadenosine with or without caffeine in randomized normal...

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Abstract

The present application discloses methods and compositions for increasing patient tolerance during myocardial imaging comprising administering multiple times of caffeine and one or more adenosine A2A receptor agonists to a mammal undergoing myocardial imaging.

Description

technical field [0001] The present invention relates to methods and compositions for increasing patient tolerance during myocardial imaging comprising administering multiple times of caffeine and one or more adenosine A to a mammal undergoing myocardial imaging 2A receptor agonist. Background technique [0002] Myocardial perfusion imaging (MPI) is a useful diagnostic technique for the detection and identification of coronary artery disease. Perfusion imaging uses, for example, radionuclide substances to identify areas of insufficient blood flow. In MPI, blood flow is measured at rest and the results are compared to blood flow measured during exercise on a treadmill (cardiac stress test), the exertion necessary to stimulate blood flow. Unfortunately, many patients are unable to exercise to the extent necessary to provide adequate blood flow due to conditions such as peripheral vascular disease, arthritis, and the like. [0003] Thus, a pharmacological agent that increases...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/52A61K31/7076A61K49/00
CPCA61K31/7076A61K31/52A61P43/00A61P9/00A61P9/08
Inventor 刘晓悌布伦特·布莱克本路易斯·贝拉尔迪内利
Owner GILEAD PALO ALTO
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