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Sulindac
Systematic (IUPAC) name
{(1Z)-5-fluoro-2-methyl-1-[4-(methylsulfinyl)benzylidene]-1H-indene-3-yl}acetic acid
Identifiers
CAS number 38194-50-2
ATC code M01AB02
PubChem 5352
DrugBank APRD01243
Chemical data
Formula C 20H17FO3S 
Mol. mass 356.412 g/mol
Pharmacokinetic data
Bioavailability Approximately 90% (Oral)
Metabolism  ?
Half life 7.8 hours, metabolites up to 16.4 hours
Excretion Renal (50%) and fecal (25%)
Therapeutic considerations
Pregnancy cat. C(AU) C(US)
Legal status POM (UK) -only (US)
Routes Oral
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Sulindac is a non-steroidal anti-inflammatory drug of the arylalkanoic acid class that is marketed in the UK & U.S. by Merck as Clinoril.

Uses

Like other NSAIDs, it is useful in the treatment of acute or chronic inflammatory conditions. Sulindac is a prodrug, derived from sulfinylindene, that is converted in the body to the active NSAID. More specifically, the agent is converted by liver enzymes to a sulfide that is excreted in the bile and then reabsorbed from the intestine. This is thought to help maintain constant blood levels with reduced gastrointestinal side effects. Some studies have shown sulindac to be relatively less irritating to the stomach than other NSAID's except for drugs of the COX-2 inhibitor class. The exact mechanism of its NSAID properties is unknown, but it is thought to act on enzymes COX-1 and COX-2, inhibiting prostaglandin synthesis.

Its usual dosage is 150-200 milligrams twice per day, with food. It should not be used by persons with a history of major allergic reactions (urticaria or anaphylaxis) to aspirin or other NSAIDs, and should be used with caution by persons having pre-existing peptic ulcer disease. Sulindac is much more likely than other NSAIDs to cause damage to the liver or pancreas.

Sulindac seems to have a property, independent of COX-inhibition, of reducing the growth of polyps and precancerous lesions in the colon, especially in association with familial adenomatous polyposis, and may have other anti-cancer properties.[1]

Sulindac is an effective tocolytic and may be used in the treatment of preterm labour. In common with other NSAIDs, sulindac is currently being investigated for its role in the treatment of Alzheimer's disease.

Since it was found that the sulfoxide functional group can be reduced by methionine sulfoxide reductase A (MsrA), a possible anti-oxidative capability is being discussed.

Sulindac Inhibits Canonical Wnt Signaling by Blocking the PDZ Domain of the Protein Dishevelled.

References

  1. ^ Scheper MA, Nikitakis NG, Chaisuparat R, Montaner S, Sauk JJ (March 2007). "Sulindac induces apoptosis and inhibits tumor growth in vivo in head and neck squamous cell carcinoma". Neoplasia 9 (3): 192–9. PMID 17401459. PMC 1838577. http://www.neoplasia.com/abstract.php?msid=1062.  

Sulindac Inhibits Canonical Wnt Signaling by Blocking the PDZ Domain of the Protein Dishevelled.

Lee HJ, Wang NX, Shi DL, Zheng JJ.

Department of Structural Biology,Stop 311, St. Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105-3678 (USA), Fax: (+1) 901-595-3168 http://www.stjude.org/zheng.

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