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Sulindac

 

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Sulindac



 
 
Sulindac is a non-steroidal anti-inflammatory drug
Non-steroidal anti-inflammatory drug

Non-steroidal anti-inflammatory drugs, usually abbreviated to NSAIDs or NAIDs, are Medications with analgesic, antipyretic and, in higher doses, with anti-inflammatory effects ....
 of the arylalkanoic acid class that is marketed in the UK & U.S. by Merck
Merck & Co.

Merck & Co., Inc. , also known as Merck Sharp & Dohme or MSD outside the USA and Canada, is one of the largest pharmaceutical companies in the world....
 as Clinoril.

other NSAIDs, it is useful in the treatment of acute or chronic
Chronic (medicine)

In medicine, a chronic disease is a disease that is long-lasting or recurrent. The term chronic describes the Course of the disease, or its rate of onset and development....
 inflammatory conditions. Sulindac is a prodrug
Prodrug

A prodrug is a Pharmacology substance that is administered in an inactive form. Once administered, the prodrug is drug metabolism in vivo into an active metabolite....
, 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.






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Sulindac is a non-steroidal anti-inflammatory drug
Non-steroidal anti-inflammatory drug

Non-steroidal anti-inflammatory drugs, usually abbreviated to NSAIDs or NAIDs, are Medications with analgesic, antipyretic and, in higher doses, with anti-inflammatory effects ....
 of the arylalkanoic acid class that is marketed in the UK & U.S. by Merck
Merck & Co.

Merck & Co., Inc. , also known as Merck Sharp & Dohme or MSD outside the USA and Canada, is one of the largest pharmaceutical companies in the world....
 as Clinoril.

Uses

Like other NSAIDs, it is useful in the treatment of acute or chronic
Chronic (medicine)

In medicine, a chronic disease is a disease that is long-lasting or recurrent. The term chronic describes the Course of the disease, or its rate of onset and development....
 inflammatory conditions. Sulindac is a prodrug
Prodrug

A prodrug is a Pharmacology substance that is administered in an inactive form. Once administered, the prodrug is drug metabolism in vivo into an active metabolite....
, 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
COX-2 inhibitor

COX-2 selective inhibitor is a form of Non-steroidal anti-inflammatory drug that directly targets COX-2, an enzyme responsible for inflammation and pain....
 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
Effective dose

An effective dose in pharmacology is the amount of medication that produces a therapeutic response in 50% of the people taking it, sometimes also called ED-50....
 is 150-200 milligrams twice per day, with food. It should not be used by persons with a history of major allergic reactions (urticaria
Urticaria

Urticaria are a kind of skin rash notable for dark red, raised, itchy bumps. Hives are frequently caused by allergic reactions, however there are many non-allergic causes....
 or anaphylaxis
Anaphylaxis

Anaphylaxis is an acute Circulatory system and very severe Type I hypersensitivity allergy reaction in humans and other mammals. The term comes from the Greek words a?a ana and f??a??? phylaxis ....
) to aspirin
Aspirin

Aspirin , also known as acetylsalicylic acid , is a salicylate medication, often used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication....
 or other NSAIDs, and should be used with caution by persons having pre-existing peptic ulcer
Peptic ulcer

A peptic ulcer, also known as ulcus pepticum, PUD or peptic ulcer disease, is an ulcer of an area of the gastrointestinal tract that is usually acidic and thus extremely painful....
 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
Familial adenomatous polyposis

Familial adenomatous polyposis is an inherited condition in which numerous Polyp s form mainly in the epithelium of the colon . While these polyps start out benign, malignant into colorectal cancer occurs when not treated....
, and may have other anti-cancer properties.

Sulindac is an effective tocolytic
Tocolytic

Tocolytics are medications used to suppress premature labor . They are given when delivery would result in premature birth. The therapy also buys time for the administration of betamethasone, a glucocorticoid drug which greatly accelerates fetal lung maturity, but takes one to two days to work....
 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
Alzheimer's disease

Alzheimer's disease , also called Alzheimer disease, Senile Dementia of the Alzheimer Type or simply Alzheimer's, is the most common form of dementia....
.

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.

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