Ketoprofen

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DRUGS
Ketoprofen

Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID), which is widely used in the treatment of patients with rheumatic diseases. It is known to reduce fever, inflammation or swelling and relieves pain. In case of arthritis, it is used to treat pain, swelling and associated stiffness. It inhibits cyclooxygenase actvity with reduction in production of prostaglandins such as PGE-2 and PGF-2a. It is also used to treat headaches, muscle aches and dental pain.

Introduction

Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID), which is widely used in the treatment of patients with rheumatic diseases. It is known to reduce fever, inflammation or swelling and relieves pain. In case of arthritis, it is used to treat pain, swelling and associated stiffness. It inhibits cyclooxygenase actvity with reduction in production of prostaglandins such as PGE-2 and PGF-2a. It is also used to treat headaches, muscle aches and dental pain.

Pharmacological Class: NSAID

Indications

  • Rheumatoid arthritis
  • Ankylosing spondylitis
  • Osteoarthritis
  • Musculo-Tendonitis
  • Synovitis
  • Dysmenorrhoea
  • Gout
  • Musculoskeletal disorders
  • Mild to moderate pain

Pharamcological Action

Ketoprofen is a non-steroidal anti-inflammatory of the propionics group, derivative of aryl-carboxylic acid. It shows anti-inflammatory effects by inhibition of cylooxygenase-2 (COX-2), an enzyme involved in prostaglandin synthesis via the arachidonic acid pathway. This results in decreased levels of prostaglandins that mediate pain, fever and inflammation. Ketoprofen is a non-specific cyclooxygenase inhibitor and inhibition of COX-1 is thought to confer some of its side effects, such as GI upset and ulceration. Ketoprofen also have anti-bradykinin activity as well as lysosomal membrane-stabilizing action. 

Dosage

Adult dose for

  • Osteoarthritis: 75 mg orally 3 times a day or 50 mg orally 4 times a day
  • Rheumatoid arthritis: 75 mg orally 3 times a day or 50 mg orally 4 times a day
  • Dysmenorrhea: 5 to 50 mg orally every 6 to 8 hours as needed for pain relief
  • Mild to moderate pain: 25 to 50 mg orally every 6 to 8 hours
  • Gout: 100 mg orally one time, followed by 50 mg every 6 hours until the acute gouty attack has resolved, usually 2 to 3 days.

Note: Not for use by children

Pharmacokinetics

Oral absorption of Ketoprofen has been found to be 94% ±4, volume of distribution as 0.11 l/kg and plasma protein binding as 95%. Presystemic metabolism is noted to be 45.5% ±4.5 and metabolism is reported to occur extensively by liver. Renal excretion accounts for 1% (unchanged) and its plasma half life is 1.5-4 hr.

Contraindications

In patients with established:

  • Peptic ulcers
  • Bronchospasms
  • Rhinitis
  • Renal insufficiency

Drug Interactions

  • Concurrent administration of aspirin decreased ketoprofen protein binding and increased ketoprofen plasma clearance, from 0.07 L/kg/h without aspirin to 0.11 L/kg/h with aspirin. Therefore, concurrent use of aspirin and ketoprofen is not recommended.
  • Patients taking diuretics are at a greater risk of developing renal failure secondary to a decrease in renal blood flow caused by prostaglandin inhibition.
  • Probenecid increases both free and bound ketoprofen by reducing the plasma clearance of ketoprofen to about one-third and decreasing its protein binding.
  • Ketoprofen, like other NSAIDs, may cause changes in the elimination of methotrexate leading to elevated serum levels of the drug and increased toxicity.
  • NSAIDs have been reported to increase steady state plasma lithium levels. It is recommended that plasma lithium levels be monitored when ketoprofen is co administered with lithium.

Side effects

Common (affecting between 1 in10 to 1 in 100)

  • Dizziness
  • Headache
  • Nervousness
  • Mild heartburn or Stomach pain
  • Diarrhea
  • Constipation
  • Bloating

Uncommon (affecting 1 in 100 to 1 in 1000)

  • Dry mouth
  • Increase sweating
  • Runny nose
  • Blurred vision
  • Ringing in ears
  • Skin itching or rash

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

  • Chest pain
  • Shortness of breath
  • Black, bloody or tarry Stools
  • Coughing up blood or vomit
  • Confusion, tremors or shaking
  • Bruising
  • Muscle weakness

Precautions

  • Caution should be taken in patients with intrinsic coagulation defects and those on anticoagulant therapy.
  • Caution should be taken in patients with compromised cardiac function, hypertension other conditions predisposing to fluid retention.
  • It should be used with extra care in the presence of existing controlled infection. Perform periodic auditory (hearing) function test during chronic therapy.
  • Not recommended in patients who have experienced severe aspirin hypersensitivity reactions. 

Clinic Evidence

  • Ketoprofen is used in treating acute and chronic pain, both rheumatic and traumatic origin, and postoperative pain. It has shown to be an excellent choice of drug for treating chronic pain in osteoarthritis, rheumatoid arthritis or gout, demonstrating a high level of efficacy with good tolerability, also in elderly patients. 1
  • Ketoprofen is effective in the treatment of migraine attacks. Relief was reported for 62.6% of headaches treated with ketoprofen 75 mg, 61.6% with ketoprofen 150 mg, and 66.8% with zolmitriptan. The difference between three active treatments and placebo (27.8% relief) was highly significant, but the tolerance of ketoprofen was good than zolmitriptan. Oral ketoprofen (75 mg or 150 mg) is an effective and well-tolerated drug in the acute treatment of migraine attacks. 2
  • Ketoprofen treated patients shows more rapid and sustained improvement in overall assessments of symptoms, based on rating scale scores for pain, duration of morning stiffness and inflammation. Measurements of inflamed joint size and grip strength also improved more with ketoprofen than with ibuprofen. 3

References

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