Indomethacin is an non-steroidal anti-inflammatory drug (NSAID) that has anti-inflammatory, analgesic, and antipyretic activity. It belongs to the acetic acid class of NSAIDs and works by inhibiting the cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes. These enzymes are required for the synthesis of prostaglandins, which are hormone-like molecules that regulate the body’s inflammatory response to injury.1 The anti-inflammatory and analgesic properties of indomethacin also derive from its ability to uncouple oxidative phosphorylation in mitochondria and inhibit the motility of polymorphonuclear leukocytes.2 Indomethacin is primarily used to treat moderate to severe pain and inflammation.
Indomethacin has been approved to treat3:
Common side effects of indomethacin include4:
Patients should contact a doctor immediately if they experience uncommon but serious side effects, including:
In some cases, prolonged indomethacin use can cause peptic ulcers or severe liver disease, and it can worsen the symptoms of Parkinson’s disease, epilepsy, and psychotic disorders. Indomethacin also puts patients at significantly higher cardiovascular risk than other NSAIDs.5
Indomethacin is known to interact with ACE-inhibitors and angiotensin II antagonists, aspirin, beta-adrenoceptor blocking agents, cyclosporine, diflunisal, digoxin, lithium, methotrexate, and probenecid. It may also reduce the effectiveness of potassium-sparing and thiazide diuretics. It should not be taken in conjunction with other NSAIDs.6
Indomethacin was discovered in 1963 and approved for use by the FDA in 1965. Because it was one of the first NSAIDs to be discovered, indomethacin was used in the early biochemical research that revealed the mechanisms of NSAID action and the physiological importance of prostaglandins.7
There is ongoing research into how indomethacin can be used to treat more conditions.
One recent study suggests that NSAID-metal ion complexes may be toxic to cancer cells that resist chemotherapy treatment. The combination of indomethacin with ruthenium and osmium ions was found to be more effective against ovarian cancer cells than cisplatin.8 Other studies seek to optimize the use of indomethacin as a tocolytic agent. The drug has been shown to effectively delay preterm labor, but it can cross the placental barrier and cause heart problems in the fetus. Some researchers are seeking to use nanoparticles to target indomethacin to the uterus in order to eliminate this risk.9
Safety concerns about indomethacin also continue to generate research. Indomethacin has a wide range of side effects and recent research highlights the drug’s ability to alter the activity of cell membrane proteins as a possible cause.10 Another study suggests that indomethacin could alter the composition of the gut microbiome, which can contribute to a wide range of health conditions, including metabolic disorders and depression.11
Many compound pharmacists prefer other NSAIDs, including Diclofenac Sodium, Flurbiprofen, Ketoprofen, Meloxicam, and Piroxicam, which can treat similar conditions but have less serious side effects. Please find more information about our Bulk APIs here.