Mechanism of Action
Oxycodone is a semisynthetic opioid with agonistic properties on mu, kappa, and delta-type opioid receptors, with the strongest affinity being for mu-type receptors. Upon binding to these G-protein coupled receptors, oxycodone stimulates the exchange of GDP on the G-alpha subunit for GTP, resulting in the inhibition of adenylate cyclase and a decrease in intracellular cAMP. This signal cascade leads to a consequent inhibition of the nociceptive neurotransmitters acetylcholine, dopamine, GABA, noradrenaline, and substance P and the hormones glucagon, insulin, somatostatin, and vasopressin. Buy OxyNorm online in Australia – OxyNorm for sale Australia
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, which leads to a closure of N-type voltage-gated calcium channels, while stimulation of the mu and delta-type receptors opens calcium-dependent inward-rectifying potassium channels. Buy OxyNorm online in Australia – OxyNorm for sale Australia
Oxycodone is metabolized by the hepatic enzymes CYP3A4 and CYP2D6, producing the metabolites noroxycodone and oxymorphone, respectively. These metabolites get excreted from the body via the kidneys.
Administration
Oxycodone is widely available in tablet, capsule, and oral solutions. It is currently available in 10-mg, 20-mg, 40-mg, or 80-mg pills. Manufacturers discontinued the 160-mg dose in May 2001 due to the high misuse potential. Oxycodone is available in combination with other analgesics, including acetaminophen, aspirin, or ibuprofen. In select countries, oxycodone may be available in intramuscular and/or intravenous forms as well. Buy OxyNorm online in Australia – OxyNorm for sale Australia
- Initial recommended doses of oxycodone are in the 5 to 15 mg range, every 4 to 6 hours as needed for adequate analgesia of acute pain. Further dosing should titrate upwards as required for pain control, with attention and monitoring for potential side effects.
- For patients with chronic pain, it is recommended to titrate dosage in the same manner. However, the medication should be taken at regularly scheduled intervals to prevent the reoccurrence of pain as opposed to treating the pain after it has started. Buy OxyNorm online in Australia – OxyNorm for sale Australia
- Tablets are intended to be taken the whole and must not be broken, chewed, crushed, or dissolved in liquid.
- Dose reduction may be necessary for the elderly and patients with hepatic or renal failure. Initiating a starting dose at one-third to one-half the usual doses and close monitoring is recommended. Titration upwards should proceed at a careful rate.
- The onset of action is 10 to 30 minutes for the immediate-release formulation and about 1 hour for controlled-release.
- Duration range is from 3 to 6 hours for immediate-release or 12 hours in controlled-release formulations.
- The plasma half-life is 3 to 5 hours, and stable plasma levels are reached within 24 to 36 hours.
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