Diflunisal
Diflunisal Uses, Dosage, Side Effects, Food Interaction and all others data.
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.
Diflunisal is a nonsteroidal drug with analgesic, anti-inflammatory and antipyretic properties. It is a peripherally-acting non-narcotic analgesic drug. Habituation, tolerance and addiction have not been reported. Diflunisal is a difluorophenyl derivative of salicylic acid. Chemically, diflunisal differs from aspirin (acetylsalicylic acid) in two respects. The first of these two is the presence of a difluorophenyl substituent at carbon 1. The second difference is the removal of the 0-acetyl group from the carbon 4 position. Diflunisal is not metabolized to salicylic acid, and the fluorine atoms are not displaced from the difluorophenyl ring structure.
| Trade Name | Diflunisal |
| Availability | Prescription only |
| Generic | Diflunisal |
| Diflunisal Other Names | Diflunisal, Diflunisalum |
| Related Drugs | Humira, Buprenex, aspirin, prednisone, ibuprofen, acetaminophen, tramadol, meloxicam, naproxen, Tylenol |
| Weight | 500mg |
| Type | Oral tablet |
| Formula | C13H8F2O3 |
| Weight | Average: 250.1976 Monoisotopic: 250.044150532 |
| Protein binding | At least 98 to 99% of diflunisal in plasma is bound to proteins. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Diflunisal is an NSAID used to treat mild to moderate pain, inflammation, osteoarthritis, and rheumatoid arthritis.
For symptomatic treatment of mild to moderate pain accompanied by inflammation (e.g. musculoskeletal trauma, post-dental extraction, post-episiotomy), osteoarthritis, and rheumatoid arthritis.
Diflunisal is also used to associated treatment for these conditions: Mild pain, Osteoarthritis (OA), Rheumatoid Arthritis, Moderate Pain
How Diflunisal works
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.
Toxicity
Oral LD50 in rat, mouse, and rabbit is 392 mg/kg, 439 mg/kg, and 603 mg/kg, respectively. Symptoms of overdose include drowsiness, nausea, vomiting, diarrhea, hyperventilation, tachycardia, sweating, tinnitus, disorientation, stupor, and coma. As a monotherapy, the smallest dosage capable of causing death was reported as 15 grams.
Selective COX-2 inhibitors have been associated with increased risk of serious cardiovascular events (e.g. myocardial infarction, stroke) in some patients. Current data is insufficient to assess the cardiovascular risk of diflunisal. Short-term use does not appear to be associated with increased cardiovascular risk (except when used immediately following coronary artery bypass graft (CABG) surgery). Risk of GI toxicity including bleeding, ulceration and perforation. Risk of direct renal injury, including renal papillary necrosis. Severe hepatic reactions, including cholestasis and/or jaundice, have been reported. May cause rash or hypersensitivity syndrome.
Food Interaction
- Avoid alcohol.
- Take with food. Food reduces irritation.
Diflunisal Hypertension interaction
[Major] Fluid retention and edema have been reported in association with the use of nonsteroidal anti-inflammatory drugs (NSAIDs).
Therapy with NSAIDs should be administered cautiously in patients with preexisting fluid retention, hypertension, or a history of heart failure.
Blood pressure and cardiovascular status should be monitored closely during the initiation of NSAID treatment and throughout the course of therapy.
Diflunisal Drug Interaction
Moderate: aspirin, aspirin, duloxetine, duloxetine, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acidsUnknown: cyclobenzaprine, cyclobenzaprine, pregabalin, pregabalin, gabapentin, gabapentin, levothyroxine, levothyroxine, cyanocobalamin, cyanocobalamin, ergocalciferol, ergocalciferol, cholecalciferol, cholecalciferol
Diflunisal Disease Interaction
Major: asthma, fluid retention, GI toxicity, renal toxicities, Reye's syndromeModerate: anemia, hepatotoxicity, platelet aggregation inhibition
Elimination Route
Rapidly and completely absorbed following oral administration, with a bioavailability of 80-90%. Peak plasma concentrations are achieved 2 - 3 hours following oral administration.
Half Life
8 to 12 hours
Elimination Route
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.
Innovators Monograph
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