Sulindac

Introduction

Sulindac, is a nonsteroidal anti-inflammatory drug, an NSAID. As an NSAID, meloxicam is an analgesic, anti-inflammatory and antipyretic. It is useful in the treatment of acute or chronic inflammatory conditions.

Sulindac is used in musculoskeletal and joint disorders such as ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis, and also in the short-term management of acute gout and peri-articular conditions such as bursitis and tendinitis. It has also bben sued to reduce fever.

Generic Name 藥名	HA Code 藥物代碼	Classification藥物分類
Sulindac Tablet 100mg		P1S1S3

Mechanism of Action

Anti-inflammatory agent, Non-steroidal anti-inflammatory drug (NSAID) Non-selective COX inhibitor

Dosage

In the treatment of rheumatoid arthritis and ankylosing spondylitis:

Oral: 150 or 200 mg twice daily, the maximum recommended daily dose is 400 mg.

Those with an increased risk of adverse reactions should be started on 7.5 mg daily. A dose of 7.5 mg daily is recommended for long-term treatment in the elderly.

The treatment of peri-articular disorders should be limited to 7 to 14 days; for acute gout, 7 days of therapy is usually adequate.

Sulindac sodium has been given by rectal suppository

Side Effects

As for NSAIDs in general.

Sulindac can result in gastrointestinal toxicity and bleeding, headaches, rash and very dark or black stool (a sign of intestinal bleeding). Like other NSAIDs, its use is associated with an increased risk of cardiovascular events such as heart attack and stroke.

Other adverse effects include depression, drowsiness, tinnitus, confusion, insomnia, psychiatric disturbances, convulsion.

Effects on the blood: localized spontaneous bleeding, bruising and prolonged bleeding time have been reported. It also increases the risk of heart attack, stroke, kidney failure and liver failure.

NSAID can also worsen asthma.

Cardiovascular risk

Chronic use has been found correlated with risk of progression to hypertension and myocardial infarction (heart attack). Both the U.S. Food and Drug Administration (FDA) and The European Medicines Agency (EMA) issues warnings of increased heart attack and stroke risk.

Skin

NSAIDs has been associated with the onset of bullous pemphigoid. It can also cause serious skin adverse events such as exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis which can be fatal.

Geriatrics

Use of sulindac is not recommended in people with peptic ulcer disease or increased gastrointestinal bleed risk, including those over 75 years of age, or those taking medications associated with bleeding risk. Adverse events have been found to be dose-dependent and associated with length of treatment.

Pharmacokinetics

Sulindac is a prodrug, that is converted by liver enzymes to a sulfide, which is the active NSAID. Peak plasma concentrations of active metabolite occur in about 2 hours. Sulindac and its metabolites are over 90% bound to plasma proteins. About 50% is excreted in the urine, 25% appears in the feaces. Sulindac and its metabolites are also excreted in bile and then reabsorbed from the intestine. The mean elimination half-life is about 7.8 hours and of the sulfide metabolite about 16.4 hours.