Oxycodone: a pharmacological and clinical review

摘要: Oxycodone is a semi-synthetic opioid with an agonist activity on mu, kappa and delta receptors. Equivalence regard to morphine 1:2. Its effect commences one hour after administration lasts for 12 h in the controlled-release formulation. Plasma half-life 3–5 (half that of morphine) stable plasma levels are reached within 24 (2–7 days morphine). Oral bioavailability ranges from 60 87%, protein binding 45%. Most drug metabolised liver, while rest excreted by kidney along its metabolites. The two main metabolites oxymorphone — which also very potent analgesic noroxycodone, weak analgesic. metabolism more predictable than morphine, therefore titration easier. has same mechanism action as other opioids: receptor, inhibition adenylyl-cyclase hyperpolarisation neurons, decreased excitability. These mechanisms play part onset dependence tolerance. clinical efficacy oxycodone similar ratio 1/1.5–2 treatment cancer pain. Long-term may be associated less toxicity comparison morphine. In future, both opioids could used simultaneously at low doses reduce toxicity. It does not appear there any differences between immediate slow-release oxycodone, except their 3–4 h, respectively. Spain, (OxyContin®) marketed 10-, 20-, 40-or 80-mg tablets b.i.d. administration. Tablets must taken whole broken, chewed or crushed. There no food interference. initial dose 10 mg new treatments reduction needed elderly cases moderate hepatic renal failure. Immediate-release (OxyNorm®) available capsules oral solution. Side effects those common mainly nausea, constipation drowsiness. Vomiting, pruritus dizziness common. intensity these side tends decrease over course time. causes somewhat hallucinations