Flurbiprofen

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[edit] BRAND NAMES

[edit] STRUCTURE

Flurbiprofen.jpg

[edit] MECHANISM OF ACTION

Flurbiprofen is a nonsteroidal antiinflammatory drug (NSAID) with analgesic and antipyretic properties.

Flurbiprofen inhibits the enzyme, cyclooxygenase (COX), an early component of the arachidonic acid cascade, resulting in the reduced formation of prostaglandins and thromboxanes. Prostaglandins act as messenger molecules in the process of inflammation.

[edit] INDICATIONS

  • Flurbiprofen is indicated for the relief of the signs and symptoms of rheumatoid arthritis, osteoarthritis, low back pain, gout, migraine, dysmenorrhoea, musculoskeletal pain and postoperative pain
  • The 8,75 mg lozenges are indicated for the symptomatic relief of sore throat.

[edit] DOSAGE

  • 100 mg, 2-3 times a day. The largest recommended single dose in a multiple-dose daily regimen is 100 mg.
  • 8,75mg lozenges: Adults and children over the age of 12 years, one lozenge dissolved slowlyin the mouth every 3-6 hoursas required. Maximum 5 lozenges in a 24 hours period.

[edit] CONTRAINDICATIONS

  • Known hypersensitivity to Flurbiprofen
  • History of asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDs
  • Use during the perioperative period in the setting of coronary artery bypass graft (CABG) surgery
  • Active gastrointestinal bleeding

[edit] WARNINGS AND PRECAUTIONS

  • Cardiovascular Thrombotic Events: Clinical trials of several COX-2 selective and nonselective NSAIDs of up to three years duration have shown an increased risk of serious cardiovascular (CV) thrombotic events, myocardial infarction, and stroke, which can be fatal. All nonsteroidal anti-inflammatory drugs (NSAIDs) may have a similar risk. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk. To minimize the potential risk for an adverse cardiovascular event, the lowest effective dose should be used for the shortest duration consistent with individual patient treatment goals.
  • Hypertension: NSAIDs can lead to onset of new hypertension or worsening of preexisting hypertension, either of which may contribute to the increased incidence of cardiovascular events. Patients taking thiazides (Hydrochlorothiazide) or loop diuretics (Bumetanide, Etacrynic acid, Furosemide, Torasemide) may have impaired response to these therapies when taking NSAIDs. NSAIDs, including diclofenac, should be used with caution in patients with hypertension. Blood pressure (BP) should be monitored closely during the initiation of NSAID treatment and throughout the course of therapy.
  • Heart failure and edema: Fluid retention and edema have been observed in some patients taking NSAIDs. Therefore caution is advised in patients with fluid retention or heart failure.
  • Gastrointestinal effects: NSAIDs can cause serious gastrointestinal events including bleeding, ulceration, and perforation of the stomach, small intestine or large intestine, which can be fatal. The risk is greater in patients with a prior history of ulcer disease or GI bleeding, and in patients at high risk for GI events, especially the elderly. Flurbiprofen should be used with caution in these patients.
  • Renal Effects: Long-term administration of NSAIDs has resulted in renal papillary necrosis and other renal injury. Use Flurbiprofen with caution in the elderly, those with impaired renal function, heart failure, liver dysfunction, and those taking diuretics and ACE inhibitors.
  • Anaphylactoid Reactions: Do not use Flurbiprofen in patients with the aspirin triad (nasal polyps, asthma and aspirin intolerance).
  • Skin Reactions: Rare cases of serious skin adverse events such as exfoliative dermatitis, Stevens-Johnson syndrome (SJS), and toxic epidermal necrolysis (TEN), which can be fatal and can occur without warning, have been reported in patients receiving NSAIDs, including Flurbiprofen. Discontinue Flurbiprofen at first appearance of rash or skin reactions.
  • Hepatic Effects: Elevated liver enzymes (ALT or AST) and, rarely, severe hepatic reactions have been reported with NSAISs including Flurbiprofen. Discontinue use of Flurbiprofen immediately if abnormal liver enzymes persist or worsen.
  • Vision changes: Blurred and/or diminished vision has been reported with the use of Flurbiprofen and other nonsteroidal anti-inflammatory drugs. Patients experiencing eye complaints should have ophthalmologic examinations.

[edit] INTERACTIONS

  • Warfarin: increased risk of bleeding complications.
  • Lithium carbonate: NSAIDs have produced an elevation of plasma lithium levels and a reduction in renal lithium clearance
  • ACE Inhibitors: Flurbiprofen may reduce the antihypertensive effect of ACE-inhibitors.
  • The concurrent use of aspirin and Flurbiprofen increase the risk of serious GI events

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). Flurbiprofen should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus.In late pregnancy, as with other NSAIDs, Flurbiprofen should be avoided because it may cause premature closure of the ductus arteriosus.
  • Nursing mothers: a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother

[edit] SIDE EFFECTS

Common adverse reactions (incidence of 1% or greater) include: edema, abdominal pain, constipation, diarrhea, dyspepsia/heartburn, elevated liver enzymes, flatulence, GI bleeding, nausea, vomiting, body weight changes, headache, nervousnes, rhinitis, rash, tinnitus, dizziness/vertigo and changes in vision .

[edit] RELATED LINKS

NSAIDs: MOAs and Clinical Considerations...

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Non-steroidal anti-inflammatory drugs (NSAIDs)
Non-selective (COX-1 and COX-2 inhibitors) Aceclofenac   Acetylsalicylic acid   Benzydamine   Diclofenac   Flurbiprofen   Ibuprofen   Indometacin   Ketoprofen   Ketorolac   Ketorolac   Lornoxicam   Mefenamic acid   Morniflumate   Nabumetone   Naproxen   Niflumic acid   Piroxicam   Tenoxicam
Relatively COX-2 selective Meloxicam   Nimesulide
COX-2 selective inhibitors (Coxibs) Celecoxib   Etoricoxib   Parecoxib
Ophthalmic NSAIDs Bromfenac (ophthalmic)   Diclofenac (ophthalmic)   Flurbiprofen (ophthalmic)   Ketorolac (ophthalmic)   Nepafenac (ophthalmic)
Veterinary use Carprofen   Deracoxib   Firocoxib   Mavacoxib   Robenacoxib