Sulindac

Sulindac (中文: 舒林酸) 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.

Drug name

Generic Name 藥名	HA Code 藥物代碼	Classification藥物分類
Sulindac Tablet 100mg	SULI01	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

NSAIDs in general

Common Side Effects	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.
Adverse Side Effects	Depression, drowsiness, tinnitus, confusion, insomnia, psychiatric disturbances, convulsion.

Blood	Localized spontaneous bleeding, bruising and prolonged bleeding time have been reported.
Asthma	Can be worsen.
Cardiovascular risk	Chronic ibuprofen 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 have 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.

Drug Management

Sulindac is much more likely than other NSAIDs to cause damage to the liver or pancreas, though it is less likely to cause kidney damage than other NSAIDs.

Monitoring

• Regular physical examination to detect edema and signs of central nervous side effects.
• Blood pressure checks will reveal development of hypertension.
• Periodic serum electrolyte (sodium, potassium, chloride) measurements,
• Complete blood counts, and
• Assessment of liver enzymes as well as creatinine (renal function) should be performed.

This is particularly important if Indomethacin is given together with an ACE inhibitor or with potassium-sparing diuretic (e.g. spironolactone), because these combinations can lead to hyperkalemia and/or serious kidney failure.

Drug Interaction

• Increases the blood thinning effects of warfarin because it displaces them from their plasma protein binding and increases their free concentrations in the bloodstream.
• Increase the risk of adverse effects of lithium, methotrexate and cardiac glycosides by lowering their excretion via the kidneys.
• Risk of nephrotoxicity may be increased if given with ACE inhibitors, ciclosporin, tacrolimus or diuretics.
• Combination with antihypertensive drugs such as ACE inhibitors, sartans and diuretics can decrease their effectiveness as well as increase the risk for kidney toxicity.
• Antihypertensive effects of ACEIs, beta blockers and diuretics may be reduced.
• Use of more than one NSAID together (including aspirin) should be avoided because of the increased risk of adverse effects.
• It adds to the risk of gastrointestinal bleeding and ulceration when used with steroids, the SSRIs, the SNRI venlafaxaine, the antiplatelet clopidogrel, bisphosphonates or pentoxifylline.

Many NSAIDs, but particularly indomethacin, cause lithium retention by reducing its excretion by the kidney. Thus, indomethacin users have an elevated risk of lithium toxicity. For patients taking lithium (e.g. for treatment of bipolar disorder), less toxic NSAIDs such as sulindac is preferred. All NSAIDs, including indomethacin, also increase plasma renin activity and aldosterone levels, and increase sodium and potassium retention. Vasopressin activity is also enhanced. Together these may lead to:

• Edema (swelling due to fluid retention),
• Hyperkaelemia (high potassium levels),
• Hypernatremia (high sodium levels),
• Hypertension.

Contraindication

• Allergy to indomethacin, aspirin or other NSAIDs.
• History of allergic reactions (bronchospasm, rhinitis, urticaria) following the use of other NSAIDs such as aspirin.
• Third-trimester pregnancy.
• Active stomach and/or duodenal ulceration or gastrointestinal bleeding, or history of peptic ulcer disease.
• Inflammatory bowel disease such as Crohn’s disease or ulcerative colitis.
• Severe congestive heart failure (NYHA III/IV).
• Severe pre-existing liver damage.
• Severe chronic kidney disease (creatinine clearance <30 mi/min).
• Caution in patients with pre-existing hepatic porphyria, as diclofenac may trigger attacks.
• Caution in patients with severe, active bleeding such as cerebral hemorrhage.
• Caution in patients with fluid retention or heart failure.
• Caution in patients with Parkinson’s disease, epilepsy, psychotic disorders (sulindac may worsen these conditions).
• Concurrent with potassium sparing diuretics.
• Can lead to onset of new hypertension or worsening of pre-existing hypertension.

Precautions

Rectal use should be avoided in patients with a history of proctitis, haemorrhoids, or rectal bleeding.

FAQ

How should I take the tablet?

Should always be taken with food. Nearly all patients benefit from an ulcer protective drug (e.g. antacids, or famotidine 20mg or omeprazole 20mg at bedtime).

What should I avoid while taking?

Avoid alcohol consumption.

What happen if I overdose?

Contact your primary care doctor. If emergency situation, call 999

What happen if I miss a dose?

Take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.