OXYCODONE HYDROCHLORIDE

Description

Oxycodone (hydrochloride) (Item No. 26513) is an analytical reference standard categorized as an opioid. Oxycodone is regulated as a Schedule II compound in the United States. This product is intended for research and forensic applications.

Chemical Properties

White Solid

Originator

Oxyfast,Purdue Pharma, L.P.

Uses

Controlled substance (opiate). Analgesic (narcotic)

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

Biological Activity

Potent and selective μ -opioid receptor agonist (K i values are 16 and >1000 nM for hMOR1 and hKOR1 respectively).

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.