We have synthesized a novel derivative of oxymorphone, oxymorphone-6 alpha-spirohydantoin. The derivative was less toxic in mice than the parent compound and it showed a significant anticonvulsive activity. It exerted agonist effects in doses lower than those of morphine and its agonist effects were longer lasting. Furthermore, both oxymorphone and the 6-spirohydantoin showed definite antagonist properties 48 hr later: they prevented analgesic effects of morphine. The antagonist effects of the derivative persisted for a week.
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http://dx.doi.org/10.1016/0091-3057(89)90062-2 | DOI Listing |
Rev Cardiovasc Med
January 2024
The Second Clinical College, Shandong University of Traditional Chinese Medicine, 250014 Jinan, Shandong, China.
Background: Atrial fibrillation is the most common tachyarrhythmia, while catheter ablation is an effective therapy for atrial fibrillation. However, pain and nervousness may occur during the procedure. Moreover, a consensus has still not been reached on which is the best kind of analgesic and sedative to use in these procedures.
View Article and Find Full Text PDFJ Anal Toxicol
October 2022
9-Delta Analytical LLC, 4365 E. Lowell Street, Suite E, Ontario, CA 91761, USA.
A rapid, simple extraction method followed by qualitative screening using liquid chromatography-tandem mass spectrometry (LC-MS-MS) for drugs in oral fluid is presented. The decision points were selected to be at, or lower, than those recommended as Tier I compounds by the National Safety Council's Alcohol, Drugs and Impairment Division for toxicological investigation of driving under the influence of drug (DUID) cases and were also at, or lower, than those recommended by Substance Abuse and Mental Health Service Administration and the Department of Transportation for Federal workplace drug testing programs. The method included 30 drugs: delta-9-tetrahydrocannabinol, amphetamine, methamphetamine, 3,4-methylenedioxymethamphetamine, 3,4-methylenedioxyamphetamine, cocaine, benzoylecgonine, carisoprodol, meprobamate, zolpidem, alprazolam, clonazepam, 7-aminoclonazepam, diazepam, nordiazepam, lorazepam, oxazepam, temazepam, codeine, morphine, 6-acetylmorphine, buprenorphine, fentanyl, hydrocodone, hydromorphone, oxycodone, oxymorphone, methadone, tramadol and phencyclidine.
View Article and Find Full Text PDFMolecules
September 2021
Department of Pharmaceutical Chemistry, Institute of Pharmacy and Center for Molecular Biosciences Innsbruck (CMBI), University of Innsbruck, Innrain 80-82, 6020 Innsbruck, Austria.
Adequate pain management, particularly chronic pain, remains a major challenge associated with modern-day medicine. Current pharmacotherapy offers unsatisfactory long-term solutions due to serious side effects related to the chronic administration of analgesic drugs. Morphine and structurally related derivatives (e.
View Article and Find Full Text PDFNeuropharmacology
September 2021
Medical College of Wisconsin, USA. Electronic address:
There is a need to develop a novel analgesic for pain associated with interstitial cystitis/painful bladder syndrome (IC/PBS). The use of the conventional μ-opioid receptor agonists to manage IC/PBS pain is controversial due to adverse CNS effects. These effects are attenuated in benzylideneoxymorphone (BOM), a low-efficacy μ-opioid receptor agonist/δ-opioid receptor antagonist that attenuates thermal pain and is devoid of reinforcing effects.
View Article and Find Full Text PDFJ Pharm Biomed Anal
September 2021
UniSA: Clinical and Health Sciences, University of South Australia, Adelaide, Australia; Health and Biomedical Innovation, University of South Australia, Adelaide, Australia.
Introduction: A range of opioids are commonly prescribed to manage chronic pain, but individual patient responses vary greatly, especially in older populations. One source of that variability are differences in absorption, metabolism and excretion, i.e.
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