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Active ingredient: Flurbiprofen - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Anti-inflammatory Agents
  • Analgesics
  • Nonsteroidal Antiinflammatory Agents (NSAIDs)
  • Carbonic Anhydrase Inhibitors
  • Cyclooxygenase Inhibitors

Dosage Forms

  • Capsule (sustained-release)
  • Liquid
  • Tablet

Brands / Synonyms

Adfeed; Ansaid; Antadys; Apo-Flurbiprofen; Cebutid; FLP; Flurbiprofen; Flurbiprofen Axetil; Flurbiprofen Sodium; Flurbiprofene [Inn-French]; Flurbiprofeno [Inn-Spanish]; Flurbiprofenum [Inn-Latin]; Flurofen; Froben; Froben Sr; Novo-Flurprofen; Nu-Flurbiprofen; Ocufen; Stayban; Zepolas

Indications

Flurbiprofen tablets are indicated for the acute or long-term treatment of the signs and symptoms of rheumatoid arthritis and osteorarthritis.

Pharmacology

Flurbiprofen, 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. Flurbiprofen exhibits antiinflammatory, analgesic, and antipyretic activities.

Mechanism of Action

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.

Absorption

The mean oral bioavailability of flurbiprofen from tablets is 96% relative to an oral solution.

Toxicity

LD50=10 mg/kg (orally in dogs).

Biotrnasformation / Drug 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.

Contraindications

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.

Drug Interactions

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.

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