Flurofen - General Information
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. [PubChem]
Pharmacology of Flurofen
Flurofen, a nonsteroidal antiinflammatory drug (NSAID) of the propionic acid class, is used for the relief of pain and inflammation associated with rheumatoid arthritis and osteoarthritis and for the inhibition of intraoperative miosis. Flurofen exhibits antiinflammatory, analgesic, and antipyretic activities.
Flurofen for patients
Flurbiprofen, like other drugs of its' class, is not free of side effects. The side effects of these drugs can cause discomfort and rarely, there are more serious side effects, such as gastrointestinal bleeding, which may result in hospitalization and even fatal outcomes. Nonsteroidal anti-inflammatory drugs are often essential agents in the management of arthritis, but they also may be commonly employed for conditions which are less serious. Physicians may w.s. to discuss with their patients the potential risks and likely benefits of nonsteroidal anti-inflammatory drug treatment, particularly when the drugs are used for less serious conditions where treatment without such agents may represent an acceptable alternative to both the patient and the physician.
Antacids: Administration of flurbiprofen to volunteers under fasting conditions, or with antacid suspension yielded similar serum flurbiprofen time profiles in young subjects (n=12). In geriatric subjects (n=7) there was a reduction in the rate but not the extent of flurbiprofen absorption.
Anticoagulants: Flurbiprofen like other nonsteroidal anti-inflammatory drugs, has been shown to affect bleeding parameters in patients receiving anti-coagulants, and serious clinical bleeding has been reported. The physician should be cautious when administering flurbiprofen to patients taking anticoagulants.
Aspirin: Concurrent administration of aspirin and flurbiprofen resulted in 50% lower serum flurbiprofen concentrations. This effect of aspirin (which also lowers serum concentrations of other nonsteroidal anti-inflammatory drugs given with it) has been demonstrated in patients with rheumatoid arthritis (n= 15) as well as normal volunteers (n= 16). Concurrent use of flurbiprofen and aspirin is therefore not recommended.
Beta-adrenergic Blocking Agents: The effect of flurbiprofen on blood pressure response to propranolol and atenolol was evaluated in men with mild uncomplicated hypertension (n = 10). Flurbiprofen pretreatment attenuated the hypotensive effect of a single dose of propranolol but not atenolol. Flurbiprofen did not appear to affect the beta-blocker-mediated reduction in heart rate. Flurbiprofen did not affect the pharmacokinetic profile of either drug, and the mechanism under lying the interference with propranolol's hypotensive effect is unknown. Patients taking both flurbiprofen and a beta-blocker should be monitored to ensure that a satisfactory hypotensive effect is achieved.
Cimetidine, Ranitidine: In normal volunteers (n=9), pretreatment with cimetidine or ranitidine did not affect flurbiprofen pharmacokinetics except that a small (13 %) but statistically significant increase in the area under the serum concentration curve of flurbiprofen resulted with cimetidine.
Digoxin: Studies of concomitant administration of flurbiprofen and digoxin to healthy men (n= 14) did not show a change in the steady state serum levels of either drug.
Diuretics: Studies in normal volunteers have shown that flurbiprofen like other nonsteroidal anti-inflammatory drugs, can interfere with the effects of furosemide. Although results have varied from study to study, effects have been shown on furosemide-stimulated diuresis, natriuresis, and kaliuresis. Other nonsteroidal anti-inflammatory drugs that inhibit prostaglandin synthesis have been shown to interfere with thiazide diuretics in some studies and with potassium-sparing diuretics. Patients receiving flurbiprofen and furosemide or other diuretics should be observed closely to determine if the desired effect is obtained.
Oral Hypoglycemic Agents: In one study, flurbiprofen was given to adult diabetics who were already receiving glyburide (n=4), metformin (n=2) chlorpropamide with phenformin (n= 3) or glyburide with phenformin (n=6). Although there was a slight reduction in blood sugar concentrations during concomitant administration of flurbiprofen and hypoglycemic agents, there were no signs or symptoms of hypoglycemia.
Flurbiprofen tablets are contraindicated in patients who have previously demonstrated hypersensitivity to the product flurbiprofen should not be given to patients in whom flurbiprofen, aspirin, or other nonsteroidal anti-inflammatory drugs induce asthma urticaria or other allergic-type reactions. Fatal asthmatic reactions have been reported in such patients receiving this type of drug.
Additional information about Flurofen
Flurofen Indication: Flurofen tablets are indicated for the acute or long-term treatment of the signs and symptoms of rheumatoid arthritis and osteorarthritis.
Mechanism Of Action: The antiinflammatory effect of flurbiprofen may result from the reversible inhibition of cyclooxygenase, causing the peripheral inhibition of prostaglandin synthesis. Flurofen also inhibits the migration of leukocytes into sites of inflammation and prevents the formation of thromboxane A2, an aggregating agent, by the platelets.
Drug Interactions: Alendronate Increased risk of gastric toxicity
Methotrexate The NSAID increases the effect and toxicity of methotrexate
Anisindione The NSAID increases the anticoagulant effect
Dicumarol The NSAID increases the anticoagulant effect
Acenocoumarol The NSAID increases the anticoagulant effect
Warfarin The NSAID increases the anticoagulant effect
Cyclosporine Monitor for nephrotoxicity
Food Interactions: Take with food to reduce irritation.
Generic Name: Flurbiprofen
Synonyms: FLP; Flurbiprofen Sodium; Flurbiprofene [Inn-French]; Flurbiprofeno [Inn-Spanish]; Flurbiprofenum [Inn-Latin]
Drug Category: Anti-inflammatory Agents; Analgesics; Nonsteroidal Antiinflammatory Agents (NSAIDs); Carbonic Anhydrase Inhibitors; Cyclooxygenase Inhibitors
Drug Type: Small Molecule; Approved
Absorption: The mean oral bioavailability of flurbiprofen from tablets is 96% relative to an oral solution.
Toxicity (Overdose): LD50=10 mg/kg (orally in dogs).
Protein Binding: > 99%
Biotransformation: 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.
Half Life: 4.7-5.7 hours
Dosage Forms of Flurofen: Tablet Oral
Capsule, extended release Oral
Chemical IUPAC Name: 2-(3-fluoro-4-phenylphenyl)propanoic acid
Chemical Formula: C15H13FO2
Flurbiprofen on Wikipedia: https://en.wikipedia.org/wiki/Flurbiprofen
Organisms Affected: Humans and other mammals