期刊
REGULATORY TOXICOLOGY AND PHARMACOLOGY
卷 59, 期 3, 页码 385-390出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.yrtph.2010.12.007
关键词
Opioids; Receptor; Mu; Binding; K-i
The safe disposal of unused opioid drugs is an area of regulatory concern. While toilet flushing is recommended for some drugs to prevent accidental exposure, there is a need for data that can support a more consistent disposal policy based on an assessment of relative risk. For drugs acting at the Mu-opioid receptor (MOR), published measurements of binding affinity (K-i) are incomplete and inconsistent due to differences in methodology and assay system, leading to a wide range of values for the same drug thus precluding a simple and meaningful relative ranking of drug potency. Experiments were conducted to obtain K-i's for 19 approved opioid drugs using a single binding assay in a cell membrane preparation expressing recombinant human MOR. The K-i values obtained ranged from 0.1380 (sufentanil) to 12.486 mu M (tramadol). The drugs were separated into three categories based upon their K-i values: K-i > 100 nM (tramadol, codeine, meperidine, propoxyphene and pentazocine), K-i =1-100 nM (hydrocodone, oxycodone, diphenoxylate, alfentanil, methadone, nalbuphine, fentanyl and morphine) and K-i < 1 nM (butorphanol, levorphanol, oxymorphone, hydromorphone, buprenorphine and sufentanil). These data add to the understanding of the pharmacology of opioid drugs and support the development of a more consistent labeling policies regarding safe disposal. Published by Elsevier Inc.
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