Definition
An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.
Description
Flurbiprofen, a propionic acid derivative, is a nonsteroidal anti-inflammatory agent (NSAIA) with antipyretic and analgesic activity. Oral formulations of flurbiprofen may be used for the symptomatic treatment of rheumatoid arthritis, osteoarthritis and anklylosing spondylitis. Flurbiprofen may also be used topically prior to ocular surgery to prevent or reduce intraoperative miosis. Flurbiprofen is structurally and pharmacologically related to fenoprofen, ibuprofen, and ketoprofen.
Top Gene Interactions
Related Pathways
General Information
- Metabolism: Hepatic. Cytochrome P450 2C9 plays an important role in the metabolism of flurbiprofen to its major metabolite, 4’-hydroxy-flurbiprofen. The 4’-hydroxy-flurbiprofen metabolite showed little anti-inflammatory activity in animal models of inflammation. Route of Elimination: Flurbiprofen is poorly excreted into human milk. Following dosing with flurbiprofen, less than 3% of flurbiprofen is excreted unchanged in the urine, with about 70% of the dose eliminated in the urine as parent drug and metabolites. Renal elimination is a significant pathway of elimination of flurbiprofen metabolites. Half Life: R-flurbiprofen, 4.7 hours; S-flurbiprofen, 5.7 hours
- Uses/Sources: Flurbiprofen tablets are indicated for the acute or long-term symptomatic treatment of rheumatoid arthritis, osteorarthritis and anklosing spondylitis. It may also be used to treat pain associated with dysmenorrhea and mild to moderate pain accompanied by inflammation (e.g. bursitis, tendonitis, soft tissue trauma). Topical ophthalmic formulations may be used pre-operatively to prevent intraoperative miosis.
- Symptoms: Symptoms of a flurbiprofen overdose may include nausea, vomiting, stomach pain, dizziness, drowsiness, black or bloody stools, coughing up blood, urinating less than usual or not at all, shallow breathing, fainting, or coma.
- Treatment: Patients should be managed by symptomatic and supportive care following overdose with a nonsteroidal anti-inflammatory drug. There are no specific antidotes. Emesis and/or activated charcoal (60 to 100 g in adults, 1 to 2 g/kg in children) and/or osmotic cathartic may be indicated in patients seen within 4 hours of ingestion with symptoms, or following a large overdose (5 to 10 times the usual dose). Forced diuresis, alkalization of urine, hemodialysis, or hemoperfusion may not be useful due to high protein binding. (L1712)
- Route of Exposure: Fluribiprofen is rapidly and almost completely absorbed following oral administration. Peak plasma concentrations are reached 0.5 - 4 hours after oral administration.
Toxicity
- Carcinogenicity: No indication of carcinogenicity to humans (not listed by IARC).
- Toxicity: LD50: 10 mg/kg (Oral, Dog) (A308)
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
Aldo-keto reductase family 1 member C3 Solute carrier family 22 member 6 Cytochrome P450 2C9 Aldo-keto reductase family 1 member C1 Fatty acid-binding protein, intestinal Aldo-keto reductase family 1 member C4 Aldo-keto reductase family 1 member C2 Fas-binding factor 1 |
21053930 18533710 9353694 22877157 10991954 |
|
Serum albumin Prostaglandin G/H synthase 1 Prostaglandin G/H synthase 2 |
The antiinflammatory effect of flurbiprofen may result from the reversible inhibition of cyclooxygenase, causing the peripheral inhibition of prostaglandin synthesis. Flurbiprofen also inhibits the migration of leukocytes into sites of inflammation and prevents the formation of thromboxane A2, an aggregating agent, by the platelets. |
11811354 2867185 10091674 11006278 9626023 10358065 10977131 16867708 2514947 2294437 12711844 11405284 17341061 16134939 12392782 11698048 10594327 10773011 3420949 |