Oxycodone
 NAME OF DRUG: Oxycodone (Oxycontin, Roxicodone, Percodan, Percoset, and Tylox) |
| PHYSICAL CHARACTERISTICS: Oxycodone is 14-hydroxydihydrocdeinone which is a white odorless crystalline powder derived from the opium alkaloid, thebaine. |
| DOSAGE/OCCURRENCE/USAGE: Oxycodone is an ingredient of Percodan, Percocet, Roxicet, and Tylox. It is a semisynthetic narcotic analgesic that is derived from thebaine. Available in oral formulations often in combination with aspirin, phenacetin and caffeine. Typical adult dose is 2.5 – 5 mg as the hydrochloride or terephthalate salt every 6 hours. Although it is typically used for the relief of moderate to moderately severe pain, it can also produce drug dependence of the morphine type. The main actions of therapeutic value are analgesia and sedation. |
| BLOOD CONCENTRATIONS VS. DOSAGE: Therapeutic plasma concentration is 10–100 ng/mL and the toxic plasma concentration is greater than 200 ng/mL. After 6 subjects were given 4.5 mg of hydrochloride plus 0.38 mg of terephthalate, the plasma concentrations averaged 0.018 mg/L (range0.009 – 0.037) at 1 hour, 0.016 mg/L at 2 hours, 0.009 mg/L at 4 hours, and 0.005 mg/L at 8 hours. |
| URINE EXCRETION RATE: Oxycodone is metabolized by N- and O-demethylation. Between 33 – 61% of a single dose of oxycodone is excreted in a 24 hour urine collection and consists of 13 – 19% free oxycodone, 7 – 29% conjugated oxycodone, 13 – 14% conjugated oxymorphone and an unknown amount of noroxycodone. After a single oral dose, free oxycodone concentrations in urine don’t usually exceed 1 mg/L. |
| METABOLITES: Free oxycodone, conjugated oxycodone, conjugated oxymorphone, and noroxycodone. |
| TOXICITY: In overdosage, oxycodone can produce stupor, coma, muscle flaccidity, severe respiratory depression, hypotension, and cardiac arrest. |
| REFERENCES:Baselt, R C. Disposition of Toxic Drugs and
Chemicals in Man, Second Edition. Davis, Calif.: Biomedical Publications, 1982. Physicians’ Desk Reference, Forty-Eight Edition. Montvale, NJ: Medical Economics Data Production Company, 1994. Goldberger, Bruce A. Opiates Abused Drugs Monograph Series. Ed. Caplan, Yale H. Irving, TX: Abbott Laboratories, 1994. |