Drug intelligence / Profile preview

aspirin + oxycodone hydrochloride + oxycodone terephthalate

Development stage
Discontinued
Lead developer
Endo International
Modality
Small Molecules
Administration
Oral
01

Overview

Aspirin + oxycodone hydrochloride + oxycodone terephthalate is an oral small-molecule analgesic combination historically marketed as **Percodan** by Endo Pharmaceuticals for the treatment of moderate to moderately severe pain. The specific legacy formulation contains 325 mg aspirin together with oxycodone provided as two salts, 4.5 mg oxycodone hydrochloride and 0.38 mg oxycodone terephthalate, in a tablet dosage form. Its analgesic effect combines the central opioid activity of oxycodone, a semisynthetic opioid agonist acting primarily at mu-opioid receptors and also kappa-opioid receptors in the central nervous system, with the peripheral anti-inflammatory and analgesic activity of aspirin, which inhibits prostaglandin synthesis through cyclooxygenase inhibition. This exact two-salt oxycodone formulation was later reformulated, with the oxycodone terephthalate component removed from newer Percodan products.

Brand names
Percodan
Other names
aspirin + oxycodone hydrochloride + oxycodone terephthalateoxycodone + aspirin
02

Targets

KOR (Kappa opioid receptor)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)MOR (Mu opioid receptor)PGHS-1 (Prostaglandin G/H Synthase 1)

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