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Chapter: Modern Pharmacology with Clinical Applications: Opioid and Nonopioid Analgesics

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Indoles (indomethacin) and Related Compounds

Indomethacin (Indocin) is an acetic acid derivative re-lated functionally to sulindac (Clinoril), a prodrug with a long half-life, and etodolac (Lodine).

Indoles (indomethacin) and Related Compounds

Chemistry and Mechanism of Action

Indomethacin (Indocin) is an acetic acid derivative re-lated functionally to sulindac (Clinoril), a prodrug with a long half-life, and etodolac (Lodine). They are metab-olized in the liver and excreted as metabolites in the bile and via the kidney. They are potent inhibitors of COX and thus extremely effective antiinflammatory agents .

Clinical Uses, Adverse Effects, and Contraindications

All of these drugs produce analgesic effects, antipyresis, and antiinflammatory effects. Due to the high incidence of gastric irritation, headache, nausea, and other side ef-fects, including hematological effects and coronary vasoconstriction, they are not useful as an initial treat-ment for pain. GI irritation and ulceration occur to a lesser extent with etodolac. Indomethacin is useful in the treatment of acute gout, osteoarthritis, ankylosing spondylitis, and acceleration of the closure of the ductus arteriosus in premature infants. The tocolytic effects of indomethacin to prevent preterm labor are the result of its effects on prostaglandin synthesis. However, the tox-icity of the drug limits such application, since it in-creases fetal morbidity. Indomethacin is contraindicated in pregnancy, in asthmatics, and in those with gastric ul-cers or other ulceration of the GI tract. Indomethacin may increase the symptoms associated with depression or other psychiatric disturbances and those associated with epilepsy and Parkinson’s disease. The drug should be used with caution in such patients.

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