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Pharmacology of Ketoprofen (Ketofen) ; Mechanism of action, Pharmacokinetics, Uses, Effects
Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory, and antipyretic properties. Here’s a breakdown of its pharmacology:
Mechanism of Action
Ketoprofen works by inhibiting the enzyme cyclooxygenase (COX), which is involved in the synthesis of prostaglandins. Prostaglandins are mediators of inflammation, pain, and fever. By inhibiting COX, ketoprofen reduces the production of prostaglandins, thereby alleviating inflammation and pain.
Pharmacokinetics
Absorption: Ketoprofen is rapidly absorbed following oral administration, with peak plasma concentrations reached within 0.5 to 2 hours.
Distribution: It is widely distributed throughout the body and binds extensively to plasma proteins (approximately 99%).
Metabolism: Ketoprofen is metabolized primarily in the liver by the enzymes CYP2C8 and CYP2C9, and is conjugated with glucuronic acid by UGT2B7.
Excretion: The metabolites are excreted mainly through urine. The elimination half-life of ketoprofen is approximately 0.9 to 3.3 hours.
Therapeutic Uses
Ketoprofen is used to treat a variety of conditions, including:
Rheumatoid arthritis
Osteoarthritis
Ankylosing spondylitis
Acute gouty arthritis
Tendinitis
Bursitis
Headache
Postoperative dental pain
Primary dysmenorrhea1.
Side Effects
Common side effects include:
Gastrointestinal discomfort (e.g., nausea, vomiting, diarrhea)
Headache
Dizziness
Rash
Edema.
Warnings and Precautions
Cardiovascular Risk: Ketoprofen may increase the risk of serious cardiovascular events, such as heart attack and stroke.
Gastrointestinal Risk: It may cause gastrointestinal bleeding, ulceration, and perforation.
Renal Risk: Use with caution in patients with renal impairment, as it may worsen renal function
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