Nimesulide
Nimesulide is a nonsteroidal anti-inflammatory drug, an NSAID, a selective inhibitor of cyclo-oxygenase-2 (COX-2). As an NSAID, sulindac is an analgesic, anti-inflammatory and antipyretic.
Nimesulide is not recommended long-term, as for chronic conditions such as arthritis. This is due to its association with an increased risk of liver toxicity, including liver failure.
It is useful in the treatment of acute pain, the symptomatic treatment of osteoarthritis, and primay dysmenorrhoea.
Drug name
| 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) selective COX-2 inhibitor
Dosage
| acute pain | Oral : 100 mg twice daily |
|---|---|
| Acute gout | Oral : 150 to 200 mg in divided doses until all symptoms and signs subsided |
| Dysmenorrhea | Oral : 75 mg daily |
In the treatment of acute pain and dysmenorrhiea
Oral: 100 mg twice daily.
In the symptomatic treatment of sprains and tendinitis nimesulide has been applied topically as a 3% gel.
Side Effects
Due to concerns about the risk of liver toxicity, nimesulide has been withdrawn from market in several countries (Spain, Finland, Belgium, Ireland and United States). Liver problems have resulted in both deaths and the need for transplantation. This may occur in as little as three days after starting the medication.
Continuous use of nimesulide (more than 15 days) may cause the following side effects:
- Diarrhea
- Vomiting
- Skin rash
- Itchiness
- Dizziness
- Bitterness in mouth
Pharmacokinetics
Nimesulide is absorbed rapidly following oral administration. It has a rapid onset of action, with reductions in pain and inflammation observed within 15 minutes from drug intake.
Drug Management
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
- it should be avoided by children under 12
- people with liver problems
- Allergy to aspirin or other NSAIDs
- History of allergic reactions (bronchospasm, rhinitis, urticaria) following the use of other NSAIDs such as aspirin
- Contraindicated during pregnancy and in lactating women.
- 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 chronic kidney disease (creatinine clearance <30 mi/min)
- 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 20 mg 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.
