Nimesulide

BRAND NAMES:

Nimprex-P – It is a combinational medicine of Nimesulide 100mg and paracetamol 325mg available as Nimprex – P used in the treatment of relieving pain.

100 Mg Nise Nimesulide Tablets – Nimesulide is the main active ingredient available on the market, as it is available in Nise 100mg tablets.

MECHANISM OF ACTION:

Its principal mode of action is the specific suppression of the enzyme cyclooxygenase-2 (COX-2). Cyclooxygenase enzymes are essential for turning arachidonic acid into prostaglandins, lipid molecules involved in inflammation and pain signaling. This enzyme has two primary isoforms: COX-1 and COX-2. COX-1 is expressed constitutively in most tissues and plays a role in maintaining normal physiological activities such as gastrointestinal lining protection and platelet function. COX-2, on the other hand, is inducible and is found largely in inflammatory areas.

PHARMACOKINETICS:

Absorption: The medication is promptly and thoroughly absorbed upon oral administration. 

Distribution: It is quickly disseminated, substantially bound to albumin, and removed with a terminal half-life of approximately 4 hours. 

Metabolism: Metabolism involves extensive biotransformation, mostly to 4-hydroxynimesulide, which appears to be physiologically active. 

Excretion: The amount of unaltered medication in urine and feces is minimal.

PHARMACODYNAMICS:

Nimesulide acts specifically as a relatively selective cyclooxygenase -2 inhibitor. It is peculiar, that additional and unknown mechanisms appear to be involved. It has been implicated in its action in the ecto-5-nucleotidase receptor pathway.

DOSAGE AND ADMINISTRATION:

Nimesulide is available in various formulations, including pills, syrups, capsules, DT tablets, injectables, oral drops, solutions, and gels. The doctor will recommend a dosage based on the patient's condition.

• 100mg tablets are the recommended dose for every 12 hours. It can be taken orally at 50 mg twice a day or 100mg once a day.

• Solutions in drops of 50mg/ml are recommended dose 1 drop for every kg of body weight for every 12 hours.

• If the patient is available in the hospital the doctor may recommend nimesulide injections.

• A thin layer of ointment is applied on the skin over the affected area twice a day for 7 to 15 days.

• Nimesulide capsules 200mg are recommended to take 1 capsule orally once a day.

• 100mg suppository is the recommended dose and should be taken rectally every 12 hours.

CONTRAINDICATIONS:

Nimeslide should avoided by patients with liver problems and also those under the age of 12 years.

DRUG INTERACTIONS:

Generally, few drugs taken along with nimesulide can cause adverse side effects or it may decrease the functioning of the drug. To avoid such type of drug interactions in the body the patient needs to discuss with the doctor before taking the nimesulide. Below are some medications that may interact with the nimesulide.

• Respiratory medicines -  Theophylline

• Blood thinners – Warfarin

• Antidiabetics - Insulin

• Anti epileptics – Phenytoin

• Anti-cancer agent – Methotrexate

• Immune system medicines – Cyclosporine

• Anti HIV – Didanosine

FOOD INTERACTIONS:

Nimesulide should be taken with dairy products like milk, yogurt, or calcium-fortified juices.

ADVERSE EFFECTS:

Common adverse effects of Nimesulide are

• Elevated liver enzymes.

• Blood clotting disorders

• Dizziness

• Nausea

• Vomiting

• Diarrhea

• Acidity 

• Stomach cramps

• Skin rashes

• Pain at the injection site

TOXICITY:

 If the patient has taken more than the prescribed drug there is a chance of getting harmful effects on the body functions. Taking nimesulide may cause some toxic effects as below.

• Drowsiness

• Nausea

• Abdominal pain

• Vomitings