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Concentration – Efficacy Relationships Studies in normal volunteers and patients reveal predictable relationships between oxycodone dosage and plasma oxycodone concentrations, as well as between concentration and certain expected opioid effects, such as pupillary constriction, sedation, overall "drug effect", analgesia and feelings of "relaxation". As with all opioids, the minimum effective plasma concentration for analgesia will vary widely among patients, especially among patients who have been previously treated with potent agonist opioids. As a result, patients must be treated with individualized titration of dosage to the desired effect. The minimum effective analgesic concentration of oxycodone for any individual patient may increase over time due to an increase in pain, the development of a new pain syndrome and/ or the development of analgesic tolerance. Concentration – Adverse Experience Relationships OxyContin ® Tablets are associated with typical opioid-related adverse experiences. There is a general relationship between increasing oxycodone plasma concentration and increasing frequency of dose-related opioid adverse experiences such as nausea, vomiting, CNS effects, and respiratory depression. In opioid-tolerant patients, the situation is altered by the development of tolerance to opioid-related side effects, and the relationship is not clinically relevant. As with all opioids, the dose must be individualized (see DOSAGE AND ADMINISTRATION), because the effective analgesic dose for some patients will be too high to be tolerated by other patients. PHARMACOKINETICS AND METABOLISM The activity of OxyContin Tablets is primarily due to the parent drug oxycodone. OxyContin Tablets are designed to provide controlled delivery of oxycodone over 12 hours. Breaking, chewing or crushing OxyContin Tablets eliminates the controlled delivery mechanism and results in the rapid release and absorption of a potentially fatal dose of oxycodone. Page: << Prev | 1 | 2 | 3 | 4 | 5 | Next >>
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