Description

Simple

An opioid medication used to treat moderate to severe pain.

Clinical

An opioid used in the management of moderate to severe pain.

Overview

Oxycodone is a semisynthetic opioid analgesic derived from thebaine in Germany in 1917.[3] It is currently indicated as an immediate release product for moderate to severe pain and as an extended release product for chronic moderate to severe pain requiring continuous opioid analgesics for an extended period.[Label] The first oxycodone containing product, Percodan, was approved by the FDA on April 12, 1950.[5]

Pharmacology

Indication

Oxycodone is indicated for the treatment of moderate to severe pain.[Label] There is also an extended release formulation indicated for chronic moderate to severe pain requiring continuous opioid analgesics for an extended period.[Label]

Pharmacodynamic

Oxycodone acts directly on a number of tissues not related to its analgesic effect. These tissues include the respiratory centre in the brain stem, the cough centre in the medulla, muscles of the pupils, gastrointestinal tract, cardiovascular system, endocrine system, and immune system.[Label] Oxyco... Read more

Mechanism of action

The full mechanism of oxycodone is not known.[Label] Under conditions of inflammation or hyperalgesia, opioid receptors in the heart, lungs, liver, gastrointestinal tract, and reproductive system are upregulated and transported to nerve terminals.[ Read more

Absorption

Oxycodone has an oral bioavailability of 60% to 87% that is unaffected by food.[Label]

The area under the curve is 135ng/mL\*hr, maximum plasma concentration is 11.5ng/mL, and time to maximum concentration is 5.11hr in patients given a 10mg oral immediate release dose of oxycodone.[Label]

Protein binding

45%.[Label] Oxycodone is primarily bound to serum albumin and to a lesser degree alpha1-acid glycoprotein.[ Read more

Volume of distribution

2.6L/kg.[Label]

Clearance

Total plasma clearance is 1.4L/min in adults.[Label]

Half life

The apparent elimination half life of oxycodone is 3.2 hours for immediate release formulations and 4.5 hours for extended release formulations.[Label] Noroxycodone has a half life of 5.8 hours, oxymorphone has a half life of 8.8 hours, noroxymorphone has a half life of 9 hours.[ Read more

Route of elimination

Oxycodone is mainly eliminated in the urine.[Label] Unbound noroxycodone makes up 23% of the dose recovered in urine and oxymorphone makes up Read more

Toxicity

Patients experiencing an overdose may present with respiratory depression, sleepiness, stupor, coma, skeletal muscle flaccidity, cold sweat, constricted pupils, bradycardia, hypotension, partial or complete airway obstruction, atypical snoring, and death.[Label] Overdose should be treated by maintai... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Nausea US
  • Kind: experimental
    • Percent: 23%
  • Kind: placebo
    • Percent: 11%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 23%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 23%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Pruritis US
  • Kind: experimental
    • Percent: 13%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 13%
  • Kind: placebo
    • Percent: 9%
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 12%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Postural Hypotension US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Dyspnea US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Thought abnormalities US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Hiccups US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Nervousness US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Confusion US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Euphoria US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Dysphoria US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Abnormal dreams US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Twitching US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Anorexia US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Fever US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Gastritis US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Chills US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Dyspepsia US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Sweating US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Exfoliative dermatitis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Dry Skin US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Voice Alteration US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Cough increased US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Impotence US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Urinary Retention US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Polyuria US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Hematuria US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Dysuria US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Hallucination US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Emotional Lability US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Depersonalization US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Agitation US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Depression US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Speech Disorder US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Stupor US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Tremor US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Vertigo US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Taste perversion US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Abnormal Gait US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Amnesia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Hyperkinesia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial

    Contraindications

    • Hypersensitivity:
      • true
    • Sex Group: all
    • Regions: US
    • Route:
      • Oral
    • Regions: US
    • Patient Conditions:
        • Name: Intestinal Obstruction
        • Drugbank Id: DBCOND0031423
    • Route:
      • Oral
    • Regions: US
    • Patient Conditions:
        • Name: Suspected intestinal obstruction
        • Drugbank Id: DBCOND0107799
    • Route:
      • Oral
    • Regions: US
    • Patient Conditions:
        • Name: Paralytic Ileus
        • Drugbank Id: DBCOND0047064
    • Route:
      • Oral
    • Regions: US
    • Patient Conditions:
        • Name: Suspected paralytic ileus
        • Drugbank Id: DBCOND0107798
    • Route:
      • Oral
    • Regions: US
    • Patient Conditions:
        • Name: Significant respiratory depression
        • Drugbank Id: DBCOND0107580
    • Route:
      • Oral
    • Regions: US
    • Patient Conditions:
        • Name: Acute or severe bronchial asthma
        • Drugbank Id: DBCOND0107797

    Food Interactions

    Avoid alcohol.

    Take with or without food. Food does not significantly affect absorption.