Articles: oxycodone-pharmacokinetics.
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J Pain Palliat Care Pharmacother · Dec 2014
Multicenter Study Clinical TrialPharmacokinetics of oxycodone after intravenous and subcutaneous administration in Japanese patients with cancer pain.
ABSTRACT In Japan, Oxycodone hydrochloride injection formulation has been approved in 2012. However, its pharmacokinetics has been poorly studied. The aim of this study is to evaluate the pharmacokinetics of oxycodone after intravenous and subcutaneous administration of oxycodone hydrochloride injection in Japanese patients with cancer pain. ⋯ The estimated geometric mean clearance (CL) of oxycodone was 24.3 L per hour after constant intravenous infusion and 29.5 L per hour after constant subcutaneous infusion, respectively. Population pharmacokinetic analysis indicated that body surface area was the influencing factor on CL and there were no pharmacokinetic differences for CL between intravenous and subcutaneous infusion. These results provide important information for the clinical use of oxycodone injection.
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Eur Rev Med Pharmacol Sci · Oct 2014
The pharmacokinetics of oral oxycodone in patients after total gastric resection.
Oxycodone is a semi-synthetic opioid with a stronger analgesic effect than morphine and codeine. The efficacy of this opioid in the treatment of postoperative pain has been proved in different groups of patients. The drug has a favourable adverse reaction profile, which encourages doctors and patients to use it more and more widely. The drug is also used in the patients who underwent an abdominal surgery, e.g. stomach resection. Gastrectomy leads to pathophysiological changes within the gastrointestinal tract, which may cause changes in the drug absorption. In consequence this leads to a change in the pharmacokinetics and effect of the drug. The aim of the research was an analysis of the pharmacokinetics of oxycodone from prolonged release tablet in patients after total gastrectomy. ⋯ Total gastrectomy did not affect the pharmacokinetics of oxycodone administered in prolonged release tablets, but the exposure to the drug was significantly lower in women.
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We hypothesize that oxycodone (OC) recycling promotes sustained synaptic OC content, which prolongs OC's exposure to local μ-opioid receptors (μORs). In that way, OC recycling gives rise to OC tolerance in humans. To pilot test our hypothesis, we developed a whole-body OC mass transport tolerance recovery model. ⋯ This reflects that OC stimulated endocytosis of μORs was accompanied by a reduction in the availability OC responsive neuroeffector cell surface μOR binding sites. We conclude that our hypothesis extends current concepts of opioid tolerance development to include OC recycling. OC recycling is a novel hypothesis of OC tolerance development in humans.
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Randomized Controlled Trial
Impact of physical manipulation on in vitro and in vivo release profiles of oxycodone DETERx®: an extended-release, abuse-deterrent formulation.
In vitro: To assess the effect of common crushing techniques on particle size reduction (PSR) and in vitro drug-release kinetics of oxycodone DETERx® (herein DETERx) and of a commercially available oxycodone extended-release (ER) tablet. In vivo: To evaluate the impact of the most effective manipulation method identified in the in vitro study and the effect of chewing on the pharmacokinetics (PK) of DETERx relative to oxycodone solution. ⋯ These mechanical manipulation and PK studies demonstrated that DETERx beads retained their ER properties after mechanical tampering and chewing by study subjects.