Indications
Sulindac is indicated for both acute and long-term management of symptoms associated with several conditions. It is prescribed for the relief of signs and symptoms of osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis. Additionally, it is utilized in treating acute painful shoulder conditions such as acute subacromial bursitis and supraspinatus tendinitis, as well as acute gouty arthritis.
Pharmacodynamics
As a non-steroidal anti-inflammatory drug (NSAID) with indene derivative properties, Sulindac exhibits analgesic and antipyretic effects. These properties make it effective in reducing inflammation and pain, contributing to its therapeutic use in managing the aforementioned conditions.
Absorption
Following oral administration, Sulindac is efficiently absorbed in humans, with approximately 90% of the dose being absorbed. This high absorption rate supports its efficacy in providing therapeutic relief to patients with the targeted inflammatory conditions.
Metabolism
Sulindac undergoes two primary metabolic transformations. It is subject to reversible reduction to form a sulfide metabolite and irreversible oxidation to form a sulfone metabolite. Extensive enterohepatic circulation involves Sulindac and its metabolites. The sulfide metabolite is primarily responsible for the drug's biological activity. Additional metabolic pathways include side chain hydroxylation and hydration of the double bond.
Mechanism of Action
Sulindac exerts its therapeutic effects through mechanisms that are yet to be fully elucidated. It is widely believed that the drug's anti-inflammatory properties arise from the inhibition of the cyclooxygenase enzymes COX-1 and COX-2, which leads to a reduction in prostaglandin synthesis. These compounds are pivotal in mediating inflammation and pain. Additionally, the antipyretic effects of Sulindac may stem from its action on the hypothalamus, leading to an increase in peripheral blood flow and vasodilation, which facilitates heat dissipation and helps reduce fever.
