Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1   Pharmacodynamic properties
Pharmacotherapeutic group: Natural opium alkaloids
ATC code: N02A A05
Oxycodone is a full opioid agonist with no antagonist properties. It has an affinity for kappa, mu and delta opiate receptors in the brain and spinal cord. The therapeutic effect is mainly analgesic, anxiolytic and sedative.


Gastrointestinal System
Opioids may induce spasm of the sphincter of Oddi.

Endocrine system
See section 4.4.
Other pharmacological effects
In vitro and animal studies indicate various effects of natural opioids, such as morphine, on components of the immune system; the clinical significance of these findings is unknown. Whether oxycodone, a semisynthetic opioid, has immunological effects similar to morphine is unknown.

Pharmacokinetic Properties

5.2    Pharmacokinetic properties
Pharmacokinetic studies in healthy subjects demonstrated an equivalent availability of oxycodone from Oxycod injection when administered by the intravenous and subcutaneous routes, as a single bolus dose or a continuous infusion over 8 hours.
Following absorption, oxycodone is distributed throughout the entire body. Approximately 45% is bound to plasma protein. It is metabolised in the liver to produce noroxycodone, oxymorphone and various conjugated glucuronides. The analgesic effects of the metabolites are clinically insignificant.
The active drug and its metabolites are excreted in both urine and faeces.
The plasma concentrations of oxycodone are only minimally affected by age, being 15% greater in elderly as compared to young subjects.
Female subjects have, on average, plasma oxycodone concentrations up to 25% higher than males on a body weight adjusted basis.
The drug penetrates the placenta and can be found in breast milk.
When compared to normal subjects, patients with mild to severe hepatic dysfunction may have higher plasma concentrations of oxycodone and noroxycodone, and lower plasma concentrations of oxymorphone. There may be an increase in the elimination half-life of oxycodone and this may be accompanied by an increase in drug effects.
When compared to normal subjects, patients with mild to severe renal dysfunction may have higher plasma concentrations of oxycodone and its metabolites. There may be an increase in the elimination half-life of oxycodone and this may be accompanied by an increase in drug effects.