INT230829
From wiki-pain
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Sentences Mentioned In
Key: | Protein | Mutation | Event | Anatomy | Negation | Speculation | Pain term | Disease term |
Many other opioids, including oxycodone, codeine, dihydrocodeine, hydrocodone, and tramadol, are primarily metabolized by the cytochrome P450 (CYP) enzymes CYP2D6 or CYP3A4.46 Mutations in the CYP2D6 gene, which occur in approximately 1% to 7% of the Caucasian population, can either decrease or increase enzyme activity, leading to alterations in opioid analgesia.47 The analgesic effects of codeine are highly dependent on conversion of codeine to morphine by CYP2D6; a poor CYP2D6 metabolic phenotype can suppress codeine analgesia, and an ultra-rapid CYP2D6 metabolic phenotype can lead to increased opioid effects, such as euphoria, dizziness, and visual disturbances.47 | |||||||||||||||
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Drugs metabolized by CYP2D6 | |||||||||||||||
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Many other opioids, including oxycodone, codeine, dihydrocodeine, hydrocodone, and tramadol, are primarily metabolized by the cytochrome P450 (CYP) enzymes CYP2D6 or CYP3A4.46 Mutations in the CYP2D6 gene, which occur in approximately 1% to 7% of the Caucasian population, can either decrease or increase enzyme activity, leading to alterations in opioid analgesia.47 The analgesic effects of codeine are highly dependent on conversion of codeine to morphine by CYP2D6; a poor CYP2D6 metabolic phenotype can suppress codeine analgesia, and an ultra-rapid CYP2D6 metabolic phenotype can lead to increased opioid effects, such as euphoria, dizziness, and visual disturbances.47 | |||||||||||||||
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The pharmacokinetics of lasofoxifene are linear over a wide dose-range (0.01 to 100 mg)57 and are not significantly affected by age, ethnicity, weight, moderately impaired hepatic or renal function, or medications such as warfarin, ketoconazole, and digoxin.6063 In a study of lasofoxifene disposition in healthy male subjects, it was eliminated by phase I oxidative metabolism (largely mediated by CYP2D6 and CYP3A4) and phase II conjugation.64
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General Comments
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