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Oxycodone is a semisynthetic opioid with agonistic properties on mu, kappa, and delta-type opioid receptors, with the strongest affinity for mu-type receptors. Upon binding to these G-protein–coupled receptors, oxycodone stimulates the exchange of guanosine diphosphate (GDP) on the G-alpha subunit for guanosine triphosphate (GTP), inhibiting adenylate cyclase and decreasing intracellular cyclic adenosine monophosphate (cAMP). This signal cascade leads to a consequent inhibition of the nociceptive neurotransmitters acetylcholine, dopamine, gamma-aminobutyric acid (GABA), noradrenaline, and substance P and the hormones glucagon, insulin, somatostatin, and vasopressin.As with other opioids, oxycodone causes hyperpolarization and reduced excitability of neurons in the central nervous system (CNS). This generalized CNS depression results from the agonistic effect on kappa-type receptors, leading to N-type voltage-gated calcium channel closure. In contrast, stimulation of the mu and delta-type receptors opens calcium-dependent inward-rectifying potassium channels.The onset of action is 10 to 30 minutes for the immediate-release formulation and about 1 hour for the controlled release. The plasma half-life is 3 to 5 hours, and stable plasma levels are reached within 24 to 36 hours. The duration ranges from 3 to 6 hours for immediate release or 12 hours for controlled-release formulations.Oxycodone therapy is contraindicated in patients with respiratory depression, acute bronchospasm, hypercarbia, hypersensitivity to oxycodone, and known or suspected ileus or gastrointestinal obstruction.If limited information exists involving studies of allergenic cross-reactivity in opioid medications, the possibility of cross-sensitivity cannot be fully excluded. For patients with an opioid allergy, a clear description of the allergic reaction should be explored and documented adequately before considering oxycodone. Patients who have a true allergic reaction to other opioid medications should avoid oxycodone therapy when possible.Signs and symptoms of an oxycodone overdose include bradycardia, hypotension, miosis, respiratory depression, somnolence, muscle flaccidity, cold and clammy skin, and death. The use is also linked with acute hepatic injury, especially in higher doses and in combination with high acetaminophen doses. When a person overdoses on oxycodone, an opioid antagonist such as naloxone should be administered. Clinicians should not give opioid antagonists such as naloxone in the absence of clinically significant respiratory or circulatory depression. Repeat dosing may be necessary as the duration of action of these drugs can vary from 30 to 120 minutes. The FDA has recently approved a 4 mg naloxone hydrochloride nasal spray for over-the-counter usage, the first naloxone product sanctioned for nonprescription useWhen a person overdoses on oxycodone, an opioid antagonist such as naloxone should be administered. Clinicians should not give opioid antagonists such as naloxone in the absence of clinically significant respiratory or circulatory depression. Repeat dosing may be necessary as the duration of action of these drugs can vary from 30 to 120 minutes. Order oxycodone Online .The FDA has recently approved a 4 mg naloxone hydrochloride nasal spray for over-the-counter usage, the first naloxone product sanctioned for nonprescription use.
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