Oxycodone/aspirin

Oxycodone/aspirin (trade name Percodan) is a combination drug marketed by Endo Pharmaceuticals. It is a tablet containing a mixture of 325 mg (5 grains) of aspirin and 4.8355 mg of oxycodone HCl (equivalent to 4.3346 mg of oxycodone as the free base); it is used to treat moderate to moderately severe pain.^[1] The safety of the combination during pregnancy has not been established, although aspirin is generally contraindicated during pregnancy, and the drug has been placed in pregnancy category D.^[2] Inactive ingredients include D&C Yellow 10, FD&C Yellow 6, microcrystalline cellulose, and corn starch.^[2] Percodan was first marketed by DuPont Pharmaceuticals and prescribed in the United States in 1950. At one time one of the most widely prescribed painkillers, it has largely been replaced by alternative oxycodone compounds containing paracetamol (acetaminophen) instead of aspirin, such as Percocet.

Pharmacology

The oxycodone component in the combination is technically 14-hydroxy-7,8-dihydrocodein-6-one, a white odorless, crystalline powder which is synthesized from the opium alkaloid thebaine. Thebaine by itself has no therapeutic value. Oxycodone is metabolized into oxymorphone. Unlike morphine and like codeine, oxycodone has a good oral potency. Prior to the introduction of paracetamol, Percodan was the mainstay in post-operative oral pain treatment due to the potency and long half-life of oxycodone. It originally contained a small amount of caffeine.

The usual dose is one tablet every six hours as needed for pain. The maximum daily dose should not exceed 12 tablets.

Reformulation

Percodan was reformulated in 2005; prior to 2005, it contained two oxycodone salts—4.62 mg of oxycodone hydrochloride and 0.38 mg of oxycodone terephthalate. Since the latter salt is unusual in the pharmacopeia, the manufacturer increased the amount of oxycodone hydrochloride to 4.8355 and discontinued the oxycodone terephthalate.

Decline of use

Percodan has largely been replaced by Percocet (which is a compound of oxycodone and paracetamol, instead of Percodan's aspirin) and other oxycodone-containing compounds for post-operative pain, since aspirin and other anti-inflammatory drugs increase prothrombin time and thus inhibit the blood from clotting, which can result in post-operative complications, such as excessive bleeding. Norco and Vicodin, which contain hydrocodone and paracetamol, have also gained favor over Percodan for post-operative pain because hydrocodone is nearly as potent as oxycodone, and it is not as highly regulated. In the United States, Percodan is regulated as a Schedule II controlled substance under the Uniform Controlled Substances Act of 1970, along with cocaine, morphine and raw (unprocessed) opium. Schedule II prescriptions may not be filled by telephone (except in an emergency), and no refills are allowed. As of October 6th 2014, Vicodin, Norco, and other hydrocodone-containing compounds are NOW SCHEDULE II. Percodan is becoming something of a relic in the United States, at least, as the number of prescriptions has fallen precipitously since the 1960s in light of the alternate drugs available containing oxycodone (Percocet, Tylox, OxyContin, Roxicodone).

Miscellaneous

The combination oxycodone/aspirin is also sold under the brand name Endodan. All products containing oxycodone (including Percodan, Percocet, OxyContin) have the potential to be habit-forming. Oxycodone can produce drug dependence of the morphine type and, therefore, has the potential for being addictive.

See also

• Vicodin
• Vicoprofen
• Percocet
• Targin
• Embeda
• Hypnorm

References

External links

• Percodan Prescribing Information from Endo Pharmaceuticals.
• Search "Percodan" in FDA Archives; shows approval in 1950.