2960 Diflunisal Diflunisal, a salicylate derivative, is a nonsteroidal anti-inflammatory agent (NSAIA) with pharmacologic actions similar to other prototypical NSAIAs. Diflunisal possesses anti-inflammatory, analgesic and antipyretic activity. Though its mechanism of action has not been clearly established, most of its actions appear to be associated with inhibition of prostaglandin synthesis via the arachidonic acid pathway. Diflunisal is used to relieve pain accompanied with inflammation and in the symptomatic treatment of rheumatoid arthritis and osteoarthritis. 22494-42-4 3059 C13H8F2O3 250.044150 White powder. 210-211°C Practically insoluble (14.5 mg/L) at neutral or acidic pH. Rapidly and completely absorbed following oral administration, with a bioavailability of 80-90%. Peak plasma concentrations are achieved 2 - 3 hours following oral administration. The precise mechanism of the analgesic and anti-inflammatory actions of diflunisal is not known. Diflunisal is a prostaglandin synthetase inhibitor. In animals, prostaglandins sensitize afferent nerves and potentiate the action of bradykinin in inducing pain. Since prostaglandins are known to be among the mediators of pain and inflammation, the mode of action of diflunisal may be due to a decrease of prostaglandins in peripheral tissues. Hepatic, primarily via glucuronide conjugation (90% of administered dose). Route of Elimination: The drug is excreted in the urine as two soluble glucuronide conjugates accounting for about 90% of the administered dose. Little or no diflunisal is excreted in the feces. Half Life: 8 to 12 hours LD50: 392 mg/kg (Oral, Rat) (A308) LD50: 439 mg/kg (Oral, Mouse) (A308) LD50: 603 mg/kg (Oral, Rabbit) (A308) The lowest dose without the presence of other medicines which caused death was 15 grams. No indication of carcinogenicity to humans (not listed by IARC). Used to relieve pain, tenderness, swelling and stiffness caused by osteoarthritis (arthritis caused by a breakdown of the lining of the joints) and rheumatoid arthritis (arthritis caused by swelling of the lining of the joints). [L1869] Symptoms of overdose include coma, tachycardia, stupor, and vomiting. In the event of overdosage, the stomach should be emptied by inducing vomiting or by gastric lavage, and the patient carefully observed and given symptomatic and supportive treatment. Because of the high degree of protein binding, hemodialysis may not be effective. (L1712) 2009-07-21T20:27:51Z 2026-05-14T16:51:00Z Diflunisal C01691 39669 Diflunisal DB00861 1FL true OC(=O)C1=C(O)C=CC(=C1)C1=C(F)C=C(F)C=C1 C13H8F2O3 InChI=1S/C13H8F2O3/c14-8-2-3-9(11(15)6-8)7-1-4-12(16)10(5-7)13(17)18/h1-6,16H,(H,17,18) HUPFGZXOMWLGNK-UHFFFAOYSA-N 250.1976 250.044150532 Exogenous Solid 4.44 HMDB14999 CHEMBL898 2951 <p>Ruyle, W.V., Jarett, L.H. and Matzuk, A.R. ; U S . Patent 3,714,226; January 30, 1973; assigned to Merck &amp; Co., Inc.</p> CHEM002292 DTXSID5022932 NS00009099 2',4'-difluoro-4-hydroxy-[1,1'-biphenyl]-3-carboxylic acid 57.53 60.86410000000001 22.288758065174765 2 3 2 2.690490099742292 -6.306963933716664 -1 2 3.11 -3.55 7.11e-02 g/l