Oxycodone (OxyContin)
Mechanism of action
- Opioid analgesic (strong)
- Analgesic properties are based mostly on its selective agonism to the μ-opioid receptor (MOR) which is crucial for transmission of information about pain throughout the central nervous system. These receptors are located mostly in brainstem and thalamus.
Indications and dose
Pharmacokinetics
Onset of action:
- 2–3 minutes (intravenous)
- 10–30 minutes (immediate release tablets)
- 1 hour (prolonged release tablets)
Duration of action:
- 3–6 hours (immediate release tablets)
- 12 hours (prolonged release tablets)
Half-life of elimination: 4.5 hours
Metabolism: Hepatic (CYP 3A4, 3A5)
Elimination: Kidneys
Directions for administration
Lowest effective dose for shortest time possible is recommended.
Switching
- parenteral morphine → parenteral oxycodone: 1:1 dose ratio
- peroral morphine → paroral oxycodone: 20 mg morphine ~ 10-13 mg oxycodone
- oral oxycodone → parenteral oxycodone: 2:1 dose ratio
Medicinal forms
Prolonged-release tablets – 5 mg, 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 60 mg, 80 mg,
Solution for injection/infusion (10 mg/ml)
Side-effects
Acute:
Drowsiness
Respiratory depression
Nausea, vomiting
Dysphoria
Delirium
Seizures
Bradycardia
Hypotension
Urinary retention
Constipation
Urticaria
Pruritus
Chronic:
Tolerance, addiction
Withdrawal effects
Hyperalgesia
Hypogonadism
Immunosuppression
Reversal
Rapid reversal may be achieved with Naloxone.
See more about it in Naloxone list.
References
