Products
Oxycodone is commercially available in the form of sustained-release tablets, capsules, melting tablets, as an injectable, and drops (including Oxycontin, Oxynorm, and generics). It has been used medicinally for decades. In the U.S., it is also used as a fix in combination with other analgesics such as acetaminophen (e.g., Percocet). Oxycodone is also available as a fixed combination with naloxone to counteract the development of constipation; see oxycodone and naloxone (Targin).
Structure and properties
Oxycodone(C18H21NO4, Mr = 315.4 g/mol) is present in the drug as oxycodone hydrochloride, a white, odorless, hygroscopic, and crystalline powder with a salty and bitter taste that is readily soluble in water. It is semisynthetically derived from thebaine, an ingredient in opium.
Effects
Oxycodone (ATC N02AA05) has analgesic, depressant, antianxiety, and psychotropic properties. The effects are due to binding to μ-opioid receptors. Oxycodone is a pure agonist with no antagonistic properties. It has a short half-life of approximately 4.5 hours.
Indications
For the treatment of moderate to severe, persistent pain.
Dosage
According to the prescribing information. Both sustained-release and non-retarded dosage forms are available. Discontinuation should be gradual to avoid withdrawal symptoms.
Abuse
Like other opioids, oxycodone can be abused as a narcotic and become addictive because of its depressant, antianxiety, relaxant, and euphoric effects.
Contraindications
For complete precautions, see the drug label.
Interactions
Oxycodone is metabolized by CYP2D6 and CYP3A4. Corresponding interactions are possible. Other drug-drug interactions have been described with central depressant drugs, alcohol, MAO inhibitors (contraindicated), muscle relaxants, and vitamin K antagonists, among others.
Adverse effects
The most common potential adverse effects include central disturbances such as fatigue, dizziness, and headache; blood pressure changes; bronchospasm; respiratory disturbances; digestive symptoms such as nausea and constipation; skin rash; pruritus; and sweating. Like other opioids, oxycodone can be addictive, and withdrawal symptoms may occur upon discontinuation. An overdose can lead to respiratory depression, low blood pressure, and coma and is life-threatening. Opioid antagonists are used as antidotes.
