Indomethacin

2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetic_acid_200

Indomethacin_sticks-model

Indomethacin (IN-doh-MEH-thuh-sin) is renowned for its prowess in alleviating pain, fever, swelling, and redness. More recently, it has found utility in curtailing tumor-induced immune suppression, enhancing the efficiency of antineoplastic agents. This potent medication is a member of the nonsteroidal anti-inflammatory drug (NSAID) family.

Pharmacological Attributes

At its core, Indomethacin serves as a potent NSAID and is often the drug of choice for chronic inflammatory arthritis. Its power in treating pain and inflammation, combined with its affordability and accessibility, makes it a staple in many therapeutic regimens.

Mechanism of Action

Chemically, Indomethacin is characterized as a methylated indole, fitting into the acetic acid derivative subclass of NSAIDs. Like its NSAID counterparts, it showcases antipyretic, analgesic, and anti-inflammatory properties. The mechanism underlying these effects is attributed to the inhibition of intracellular cyclooxygenases, namely Cox-1 and Cox-2. This inhibition leads to a diminished synthesis of prostaglandins, which are integral mediators of pain and inflammation.

Liver Safety and Considerations

Though rare, there have been associations between Indomethacin and idiosyncratic drug-induced liver disease. It's imperative for patients and healthcare providers to be vigilant for signs of hepatic dysfunction during treatment.

FDA Approval and Indications

The U.S. Food and Drug Administration (FDA) conferred its approval for Indomethacin back in 1965. Despite being in use for decades, it remains in demand with over 2.5 million prescriptions dispensed annually. Its therapeutic indications span various chronic arthritic conditions including osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and gouty arthritis. Additionally, it is employed in the management of acute shoulder pain and dysmenorrhea. A specialized intravenous formulation is also available specifically for sealing the patent ductus arteriosus in premature infants.

Dosage and Administration

Available by prescription, Indomethacin can be procured as capsules in strengths of 25, 50, and 75 mg. Additionally, sustained-release forms, suppositories, and oral suspensions are also available, marketed under several commercial labels including Indocin, Indochron, Indolar, Indo-Lemmon, and Zendole, among others. The typical adult dosing for chronic arthritis ranges from 25 to 50 mg, administered orally two to three times daily. This can be titrated up based on symptom control, up to a ceiling dose of 200 mg daily. A specialized injectable version is also available in 1 mg vials, specifically designed for intravenous use in premature neonates with patent ductus arteriosus.

Potential Side Effects

Indomethacin, like all medications, carries the potential for adverse effects. Commonly reported side effects encompass:

• Headache
• Dizziness
• Somnolence
• Dyspepsia
• Abdominal discomfort
• Diarrhea
• Peripheral swelling (peripheral edema)
• Allergic (hypersensitivity) reactions

Patients and healthcare professionals should collaborate closely to ensure that any emerging side effects are addressed promptly.

See Also

• NSAIDs
• Cyclooxygenases
• Prostaglandins
• Nonsteroidal anti-inflammatory drug

Nonsteroidal Antiinflammatory Drugs (NSAIDs)

Acetaminophen, Celecoxib, Diclofenac, Diflunisal, Etodolac, Fenoprofen, Flurbiprofen, Ibuprofen, Indomethacin, Ketoprofen, Ketorolac, Mefenamic Acid, Meloxicam, Nabumetone, Naproxen, Nimesulide, Oxaprozin, Phenylbutazone, Piroxicam, Rofecoxib, Sulindac, Tolmetin

• Dailymed label info on Indomethacin
• FDA Indomethacin

Indomethacin Resources
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