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Oxycodone is a potent opioid analgesic that plays a critical role in the management of moderate to severe pain. As a full opioid agonist, it lacks antagonist properties, meaning it does not block the effects of opioids but rather enhances them by binding to the kappa, mu, and delta opioid receptors located in the brain and spinal cord. This binding mimics the action of endogenous pain-relief mechanisms, leading to its primary therapeutic effects: analgesia (pain relief), anxiolysis (anxiety reduction), antitussive (cough suppression), and sedation.
Chemically and pharmacologically similar to morphine, oxycodone distinguishes itself by its superior oral bioavailability, which is up to 87%, significantly higher than morphine's approximate 30% bioavailability. This high bioavailability is a testament to oxycodone's efficient absorption and systemic utilization following oral administration, making it a preferred choice for pain management.
Oxycodone is metabolized primarily into noroxycodone and oxymorphone, with oxymorphone possessing analgesic activity. However, oxymorphone's low plasma concentration suggests a minimal contribution to the overall pharmacological effects of oxycodone. The elimination half-life of oxycodone is approximately 3-4 hours, and both the active drug and its metabolites are predominantly excreted through the urine, indicating the need for cautious administration in patients with renal impairments.
Clinical studies have...
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