Ketoprofen

Ketoprofen belongs to the propionic acid class of non-steroidal anti-inflammatory drugs (NSAIDs) with analgesic and antipyretic effects. Ketoprofen is generally prescribed for arthritis-related inflammatory pain or severe toothache leading to inflammation of the gums. Ketoprofen in topical patches is used to treat musculoskeletal pain. Ketoprofen may also be used to treat some pain, especially nerve pain such as sciatica, post-herpetic neuralgia, and referring pain from radiculopathy, in the form of a cream, ointment, liquid, spray, or gel.

Pharmacodynamics

The anti-inflammatory effect of ketoprofen is thought to be due to inhibition of cyclooxygenase-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.

Pharmacokinetics

Ketoprofen is rapidly and well absorbed orally, with maximum plasma levels reached within 0.5 to 2 hours. It is 99% bound to plasma proteins, primarily albumin. It is rapidly and extensively metabolized in the liver, mainly by conjugation to glucuronic acid and by the CYP3A4 and CYP2C9 enzymes. No active metabolites have been identified. Over a 24-hour period, approximately 80% of an administered dose of ketoprofen is excreted in the urine, primarily as a glucuronide metabolite. The half-life is approximately 1-4 hours.

Side Effects

Adverse effects include:

• Nausea
• Dyspepsia
• Diarrhea
• constipation
• gastrointestinal ulceration/bleeding
• headache
• Dizziness
• Skin rash
• salt and fluid retention
• high blood pressure

Rare adverse effects include esophageal ulcers, heart failure, high blood potassium levels, kidney dysfunction, confusion, and bronchospasm. Ketoprofen may exacerbate asthma, so use is contraindicated in asthmatics.

Toxicological Data

LD50 (rat, oral): 62.4 mg-kg-1