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Which of the following is a pro-drug and related to indomethacin?(a) Piroxicam(b) Phenylbutazone(c) Sulindac(d) IndomethacinI have been asked this question in exam.My query is from Drug Addiction and Abuse in chapter Local & General Anesthetics, Opioid Analgesics, Drug Addiction and Drug Abuse of Drug Biotechnology

Answer»

Correct option is (c) Sulindac

Best explanation: Sulindac is an inactive pro-drug closely RELATED to indomethacin. It must be metabolized by hepatic MICROSOMAL enzymes to an active form. It has a long duration of action (half-life = 8h). The ADVERSE effects are less severe than other NSAIDs (ex. GI and renal). Indomethacin is an indole derivative more potent than ASA but INFERIOR at doses tolerated by rheumatoid arthritis patients, QUITE toxic.



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