Nimesulide

Nimesulide is a Cyclooxygenase-2 (COX-2) inhibitor / non-steroidal anti-inflammatory drugs (NSAIDs) belonging to Analgesic class.

Nimesulide is used to treat acute pain and primary dysmenorrhea.

Nimesulide is Well absorbed from GI tract following oral administration. The peak plasma concentration is achieved within 1-3 hours. Nimesulide is 99% bound to plasma protein.

It undergoes Hepatic biotransformation principal metabolite is 4-hydroxy-nimesulide and excreted as Metabolites in urine 80% and in feces: 20% of the administered dose.

Nimesulide shows side effects like Acid or sour stomach, Stomach discomfort and cramps, Dizziness, Skin rash, Nausea and vomiting, Pain at the injection site, Nervousness, Loss of appetite.

Nimesulide is available in the form of Oral Tablet and Topical gel.

Nimesulide is available in India, Austria, Belgium, Finland, France, Greece, Ireland, Italy, Luxembourg, Portugal and Spain.

Nimesulide is an Analgesic a belonging to the class Cyclooxygenase-2 (COX-2) inhibitor / non-steroidal anti-inflammatory drugs (NSAIDs).

Nimesulide is cyclooxygenase inhibiting potency, is intermediate but is relatively selective for the cyclo-oxygenase-2 (COX-2) thus the potential for gastric injury and intolerance is less. It is also a free radical scavenger and helps protect against the tissue damage that occurs during inflammation.

The onset and duration of action for Nimesulide is not known.

The Tmax of Nimesulide is about 1-3 hours.

Nimesulide is available in the form of Oral Tablet and Topical gel.

Nimesulide tablet is taken orally while Gel is applied topically twice or thrice a day.

Nimesulide is a painkiller used in the treatment of pain. It provides relief from mild to moderate pain due to menstrual cramps and osteoarthritis (occurs when flexible tissue at the ends of your bones wears down). Nimesulide decreases the intensity of pain signals to the brain and prevents the release of substances called prostaglandins in the brain that cause pain and fever.

Nimesulide is a Cyclooxygenase-2 (COX-2) inhibitor / non-steroidal anti-inflammatory drugs (NSAIDs) belonging to Analgesic class.

Nimesulide is cyclooxygenase inhibiting potency is intermediate but is relatively selective for the cyclo-oxygenase-2 (COX-2) thus the potential for gastric injury and intolerance is less. It is also a free radical scavenger and helps protect against the tissue damage that occurs during inflammation.

Nimesulide is approved for use in the following clinical indications

• Osteoarthritis
• Postoperative pain
• Acute pain
• Dysmenorrhoea
• Sprains
• Acute traumatic tendinitis

• Osteoarthritis

Adult Oral: 100 mg twice a day.

Adult Rectal: 200 mg twice a day.

• Postoperative pain

Adult Oral: 100 mg twice a day.

• Acute pain

Adult Oral: 100 mg twice a day.

Adult Rectal: 200 mg twice a day.

• Dysmenorrhoea

Adult Oral: 100 mg twice a day.

Adult Rectal: 200 mg twice a day.

• Sprains

Adult Topical/Cutaneous: 3% gel/cream: Apply thin layer to affected area twice or thrice a day.

Duration: 7-15 days.

• Acute traumatic tendinitis

Adult Topical/Cutaneous: 3% gel/cream: Apply thin layer to affected area twice or thrice a day.

Duration: 7-15 days.

Nimesulide is available in various strengths as 100mg, 200mg and 3%.

Nimesulide is available in the form of Oral Tablet and Topical gel.

• Dosage Adjustment in Kidney Patient

Nimesulide to be taken with caution, especially if you have a history of kidney diseases/conditions. The dose adjustment may be required.

• Dosage Adjustment in Hepatic impairment Patient

Nimesulide can cause hepatotoxicity (liver damage). So, it is not recommended for people with liver disease/impairment.

Nimesulide is contraindicated in patients with

• Hypersensitivity
• GI bleeding
• Active peptic ulcer disease
• Severe renal and heart failure
• Hepatic impairment or known liver disease.
• Coagulation disorders
• Pregnancy
• Children <12 year.

• Caution should be exercised in patients with a history of stomach problem, high blood pressure, fluid retention, elderly, during pregnancy and breast-feeding.

Consumption of alcohol is not recommended while treatment with Nimesulide due to the risk of stomach bleeding, drowsiness, and lack of concentration.

Use of Nimesulide during breastfeeding is not recommended as it may pass through the milk and harm the baby.

Nimesulide is not recommended for use in pregnancy especially during 1st trimester, as it has been reported to cause birth defects in the newborn baby.

• Common

Epigastric discomfort, heartburn or abdominal cramps, nausea, vomiting and diarrhea, skin rash, pruritus, oedema, headache, dizziness, drowsiness, hypersensitivity reactions (e.g. bronchospasm, rhinitis, angioedema urticaria), GI haemorrhage/perforation, bullous/erosive stomatitis, purpura, thrombocytopenia, toxic epidermal necrolysis, haematuria, oliguria, and renal failure; increases in liver enzymes.

• Rare

Fatal hepatitis, Stevens Johnson syndrome.

• Nimesulide may interact with respiratory medicines (theophylline), blood thinners (warfarin), antidiabetics (insulin), anti-epileptics (phenytoin), anti-cancer agents (methotrexate), immune system affecting medicines (cyclosporine), antacids, and anti-HIV (didanosine).

The common side effects of Nimesulide include the following

• Common side effects

Acid or sour stomach, Stomach discomfort and cramps, Dizziness, Skin rash, Nausea and vomiting, Pain at the injection site, Nervousness, Loss of appetite.

• Pregnancy

Pregnancy Category

Nimesulide is not recommended for use in pregnancy especially during 1st trimester, as it has been reported to cause birth defects in the newborn baby

• Nursing Mothers

Use of Nimesulide during breastfeeding is not recommended as it may pass through the milk and harm the baby.

• Pediatric Use

Nimesulide is contraindicated in children below 12 years of age. It may cause kidney problems in children and adolescents who are dehydrated.

• Geriatric Use

Nimesulide should be used with caution in the elderly population due to an increase in the risk of undesired side effects.

Epigastric pain, nausea, vomiting, drowsiness, lethargy, GI haemorrhage, seizures, hypertension, apnoea, coma, anaphylactic reactions and renal failure.

• Pharmacodynamic

Nimesulide is a nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, anti-pyretic, and analgesic properties. It inhibits prostaglandin synthetase/cyclooxygenase, which limits prostaglandin production. Its cyclooxygenase inhibiting potency is intermediate but is relatively selective for the cyclo-oxygenase-2 (COX-2) thus the potential for gastric injury and intolerance is less. It is also a free radical scavenger and helps protect against the tissue damage that occurs during inflammation.

• Pharmacokinetics

Absorption

Nimesulide is Well absorbed from GI tract following oral administration. Peak plasma concentration is achieved within 1-3 hr.

Distribution

Nimesulide is 99% bound to plasma protein.

Metabolism and Excretion

Nimesulide undergoes Hepatic biotransformation principal metabolite is 4-hydroxy-nimesulide. Nimesulide is excreted as Metabolites in urine 80% and in feces: 20% of the administered dose.

• https://go.drugbank.com/drugs/DB04743
• https://www.apollopharmacy.in/salt/NIMESULIDE
• https://www.medindia.net/doctors/drug_information/nimesulide.htm#Warning
• https://www.vademecum.es/principios-activos-nimesulida-m01ax17-us
• https://www.drugs.com/medical-answers/nimesulide-3571533/