Flurbiprofen

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DRUGS
Flurbiprofen

Flurbiprofen is a member of the phenylalkanoic acid derivative family of non-steroidal anti-inflammatory drugs (NSAIDs). It is used for the symptomatic treatment of rheumatoid arthritis, osteoarthritis and ankylosing spondylitis, ocular surgery to prevent or reduce intraoperative miosis, to treat pain associated with dysmenorrhea and inflammatory pain. 

Introduction

Flurbiprofen is a member of the phenylalkanoic acid derivative family of non-steroidal anti-inflammatory drugs (NSAIDs). It is used for the symptomatic treatment of rheumatoid arthritis, osteoarthritis and ankylosing spondylitis, ocular surgery to prevent or reduce intraoperative miosis, to treat pain associated with dysmenorrhea and inflammatory pain.

 Pharmacological class: NSAID

Indications

  • Rheumatoid arthritis
  • Osteoarthritis
  • Pain and inflammation
  • Dysmenorrhea

Pharamcological Action

The mechanism of flurbiprofen involves reversible inhibition of cyclooxygenase (COX), the enzyme that converts arachidonic acid to prostaglandin G2 (PGG2) and PGG2 to prostaglandin H2 (PGH2) in the prostaglandin synthesis pathway. Flurbiprofen is a non-selective COX inhibitor and inhibits the activity of both COX-1 and COX-2. This decreases the concentration of inflammation, pain, swelling and fever causing prostaglandins. It is one of the most potent prostaglandin inhibitory agent.

Dosage

Osteoarthritis: 50 mg orally 4 times a day or 100 mg orally 3 times a day

Rheumatoid Arthritis: 50 mg orally 4 times a day or 100 mg orally 3 times a day

Pain: 50 mg orally every 6 to 8 hours as needed

Dysmenorrhea: 50 mg orally 4 times a day

Pharmacokinetics

Flurbiprofen is rapidly and almost completely absorbed following oral administration. Peak plasma concentrations are reached 0.5 - 4 hours after oral administration. Cytochrome P450 2C9 plays an important role in metabolism of flurbiprofen to its major metabolite, 4’-hydroxy-flurbiprofen. It is poorly excreted into human milk, and less than 3% is excreted unchanged in urine, with about 70% of the dose eliminated in the urine as parent drug and metabolites. Renal elimination is a significant pathway of elimination of flurbiprofen metabolites.

Contraindications

  • Contraindicated in patients with known hypersensitivity to flurbiprofen.
  • For treating perioperative pain in the setting of coronary artery bypass graft surgery.
  • In patients who have experienced asthma, utricaria, or allergic-type reactions as severe, rarely fatal, anaphylactic-like reactions may occur.

Drug Interactions

  • Flurbiprofen when given with abciximab, may increase its anticoagulant activities.
  • Flurbiprofen with aspirin lowers serum flurbiprofen concentrations up to 50%.
  • If taken with lithium, it decreases renal clearance of lithium and causes lithium toxicity.
  • When taken along with beta-adrenergic blockers may reduce hypotensive effect of propranolol.

Side effects

Common (affecting between 1 in10 to 1 in 100)

  • Constipation
  • Diarrhea
  • Dizziness
  • Drowsiness
  • Headache
  • Heartburn
  • Nausea
  • Stomach upset
  • Stuffy nose

Uncommon (affecting 1 in 100 to 1 in 1000)

  • Memory loss
  • Blood in bowel
  • Involuntary quivering
  • Abnormal heart rhythm
  • Pink eye

Very rare (affecting less than 1 in 10,000)

  • Anemia
  • Life-threatening skin reactions
  • Life-threatening allergic reactions
  • Liver problems including liver failure
  • Asthma attacks

Precautions

  • Avoid in patients with pre-existing asthma or aspirin sensitivity.
  • Avoid in patients having coagulation disorders or patients receiving anticoagulants.
  • Avoid in patients who have eye complaints as it may cause blurred vision.
  • Avoid in patients with abnormal liver functions as they may get severe hepatic reactions.

Clinic Evidence

  • Flurbiprofen and ibuprofen, two propionic acid derivatives with anti-inflammatory and analgesic activity, were compared in a double-blind multiclinic study in 195 patients with osteoarthritis of the peripheral joints. The patients were given 80 mg/day flurbiprofen or 1600 mg/day ibuprofen for six weeks. Pain, subjective evaluation and functional tests improved significantly in both groups. There were no statistically significant differences between the two treatments in any of the response.1
  • Efficacy of flurbiprofen for dysmenorrhea was studied and 59 dysmenorrhea patients were given flurbiprofen (50 mg), aspirin (650 mg), or placebo. Results showed that flurbiprofen was more effective in pain relief and in reducing the need for additional analgesics. Except in patient preference, aspirin was only marginally superior to placebo. Results indicate therapeutic utility for flurbiprofen in dysmenorrhea.2

 

References

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