Ketoprofen

Indications

Ketoprofen is indicated for the symptomatic management of both acute and chronic rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis. Additionally, it is prescribed for the treatment of primary dysmenorrhea and for alleviating mild to moderate pain resulting from musculotendinous injuries such as sprains and strains. It is also effective in managing postoperative, including dental surgery-related discomfort, as well as postpartum pain.

Pharmacodynamics

Ketoprofen is classified as a nonsteroidal anti-inflammatory agent (NSAID) possessing both analgesic and antipyretic properties. Its pharmacological activity is akin to other standard NSAIDs, functioning primarily through the inhibition of prostaglandin synthesis. This mechanism underlies its efficacy in treating conditions like rheumatoid arthritis, osteoarthritis, and dysmenorrhea, as well as in the relief of moderate pain.

Absorption

When administered orally, ketoprofen is characterized by rapid and efficient absorption. Peak plasma concentrations are typically achieved within 0.5 to 2 hours post-ingestion, reflecting its prompt systemic availability.

Metabolism

Ketoprofen undergoes rapid and extensive metabolism in the liver, predominantly through conjugation with glucuronic acid. Notably, no active metabolites have been identified, indicating that its pharmacological effects are primarily exerted by the parent compound.

Mechanism of Action

Ketoprofen functions primarily through the inhibition of cyclooxygenase-2 (COX-2), an enzyme critical to the synthesis of prostaglandins via the arachidonic acid pathway. This action results in reduced prostaglandin levels, which diminishes pain, fever, and inflammation. As a non-selective cyclooxygenase inhibitor, Ketoprofen also affects COX-1, leading to potential side effects like gastrointestinal disturbances and ulceration. Additionally, it exhibits anti-bradykinin activity and stabilizes lysosomal membranes. Its antipyretic effects are attributed to its action on the hypothalamus, enhancing peripheral blood flow and vasodilation, which facilitates heat dissipation.