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). 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 .
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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