Articles: opioid.
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Drug metabolism reviews · Nov 2016
Review Comparative StudyComparative metabolism of tramadol and tapentadol: a toxicological perspective.
Tramadol and tapentadol are centrally acting, synthetic opioid analgesics used in the treatment of moderate to severe pain. Main metabolic patterns for these drugs in humans are well characterized. Tramadol is mainly metabolized by cytochrome P450 CYP2D6 to O-desmethyltramadol (M1), its main active metabolite. ⋯ This review aims to comparatively discuss the metabolomics of tramadol and tapentadol, namely by presenting all their known metabolites. An exhaustive literature search was performed using textual and structural queries for tramadol and tapentadol, and associated known metabolizing enzymes and metabolites. A thorough knowledge about tramadol and tapentadol metabolomics is expected to provide additional insights to better understand the interindividual variability in their pharmacokinetics and dose-responsiveness, and contribute to the establishment of personalized therapeutic approaches, minimizing side effects and optimizing analgesic efficacy.
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To examine laxative use by individuals in hospice who were taking opioids during the last week of life. ⋯ In 2007, slightly more than half of older adults in hospice who were taking opioids used laxatives during the last week of life. Recent quality indicators from the Centers for Medicare and Medicaid Services recommend laxative treatment when opioid therapy is initiated to prevent opioid-induced constipation and are intended to improve laxative use in individuals in hospice treated with opioids.
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Opioids are the mainstay of pain control for patients with chronic pain. Often, opioids with reported active metabolites, such as morphine and hydromorphone, are thought to increase the risk of neurotoxicity in renal impairment. ⋯ Although morphine and hydromorphone use may be associated with neurotoxic effects in patients with renal impairment, current evidence consists of very low-quality studies with conflicting findings. Clinicians may consider using either morphine or hydromorphone in mild-to-moderate renal impairment, while closely monitoring for neurotoxic effects, particularly when used in high doses and for extended duration.