Indication |
Used to relieve the inflammation, swelling, stiffness, and joint pain associated with rheumatoid arthritis and osteoarthritis. |
Pharmacodynamics |
Oxaprozin is a nonsteroidal anti-inflammatory drug (NSAID) with
analgesic and antipyretic properties. Oxaprozin is used to treat
rheumatoid arthritis, osteoarthritis, dysmenorrhea, and to alleviate
moderate pain. |
Mechanism of action |
Anti-inflammatory effects of Oxaprozin are believed to be due to
inhibition of cylooxygenase in platelets which leads to the blockage of
prostaglandin synthesis. Antipyretic effects may be due to action on the
hypothalamus, resulting in an increased peripheral blood flow,
vasodilation, and subsequent heat dissipation. Oxaprozin is a
non-selective NSAID, with a cell assay system showing lower COX-2
selectivity implying higher COX-1 selectivity. |
Absorption |
Oxaprozin is 95% absorbed after oral administration. Food may
reduce the rate of absorption of oxaprozin, but the extent of absorption
is unchanged. Antacids do not significantly affect the extent and rate
of oxaprozin absorption. |
Volume of distribution |
|
Protein binding |
>99.5% bound to albumin |
Metabolism |
Hepatic. Ester and ether glucuronide are the major conjugated
metabolites of oxaprozin, and do not have significant pharmacologic
activity. |
Route of elimination |
Oxaprozin is expected to be excreted in human milk based on its
physical-chemical properties; however, the amount of oxaprozin excreted
in breast milk has not been evaluated. Approximately 95% of oxaprozin is
metabolized by the liver. Approximately 5% of the oxaprozin dose is
excreted unchanged in the urine. Sixty-five percent (65%) of the dose is
excreted in the urine and 35% in the feces as metabolite.
Biliary excretion of unchanged oxaprozin is a minor pathway. Several
oxaprozin metabolites have been identified in human urine or feces. |
Half life |
54.9 hours |
Clearance |
Not Available |
Toxicity |
Oral, mouse: LD50 = 1210 mg/kg; Oral, rabbit: LD50 = 172 mg/kg; Oral, rat: LD50 = 4470 mg/kg |