Chemical Properties
White Solid
Uses
Controlled substance (opiate). Analgesic (narcotic)
Biological Activity
Potent and selective μ -opioid receptor agonist (K i values are 16 and >1000 nM for hMOR1 and hKOR1 respectively).
Description
Oxycodone (hydrochloride) (Item No. 26513) is an analytical reference standard categorized as an opioid.
1 Oxycodone is regulated as a Schedule II compound in the United States. This product is intended for research and forensic applications.
Originator
Oxyfast,Purdue Pharma, L.P.
Definition
ChEBI: Oxycodone hydrochloride is a hydrochloride obtained by reaction of oxycodone with one molar equivalent of hydrochloric acid. It is a moderately potent opioid analgesic, generally used for relief of moderate to severe pain. It has a role as a mu-opioid receptor agonist, an antitussive and an opioid analgesic. It contains an oxycodone(1+).
Brand name
Oxycontin (Purdue); Roxicodone (Roxane); Roxicodone (Xanodyne).
Therapeutic Function
Narcotic analgesic
Clinical Use
Oxycodone is about equipotent with morphine, but because of the 3-OCH group, it has a much
lower oral:parenteral dose ratio. Thus, oxycodone is used orally to treat severe to moderate pain. It
is a drug as a single agent and when combined in strong analgesic mixtures.
Oxycodone has a plasma half-life of approximately 4 hours and requires dosing every 4 to 6 hours.
Drug interactions
Potentially hazardous interactions with other drugs
Analgesics: possible opioid withdrawal with
buprenorphine and pentazocine.
Antibacterials: metabolism possibly increased by
rifampicin; metabolism inhibited by telithromycin.
Antidepressants: CNS excitation or depression
with MAOIs - avoid; possible CNS excitation or
depression with moclobemide; increased sedative
effects with tricyclics.
Antifungals: concentration increased by voriconazole.
Antihistamines: increased sedative effects with
sedating antihistamines.
Antipsychotics: enhanced hypotensive and sedative
effects.
Antivirals: concentration possibly increased by
ritonavir.
Dopaminergics: avoid with selegiline.
Nalmefene: avoid concomitant use.
Sodium oxybate: enhanced effect of sodium oxybate
- avoid.
Metabolism
Oxycodone is metabolised in the liver to produce
noroxycodone via the CYP3A system, oxymorphone via
the CYP2D6 system and various conjugated glucuronides.
The analgesic effects of the metabolites are clinically
insignificant. Both metabolites undergo glucuronidation
and are excreted with unchanged drug in urine.
