Nimesulide Gel

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Created On: 27/09/2019

Nimesulide transdermal gel is a COX-2 selective, Non-Steroidal Anti-inflammatory Drug (NSAID) with analgesic properties. It is used to reduce pain and improve musculoskeletal conditions such as soft tissue injuries or non-articular rheumatic disorders.

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Introduction

Nimesulide transdermal gel is a COX-2 selective, non-steroidal anti-inflammatory drug (NSAID) with analgesic properties. It is used to reduce pain and improve musculoskeletal conditions such as soft tissue injuries or non-articular rheumatic disorders, including discomfort in the muscles, tendonitis, back pain, arthritis, tenosynovitis, sprains, or strains. The onset of pain relief is normally observed within 15-60 minutes.

Indications

Acute pain
Primary dysmenorrhea
Thrombophlebitis
Dental pain
Headache
ENT inflammation
Phlebitis/thrombosis
Post-operative pain states
Sports injuries

Pharmachologic action

Nimesulide 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, it has less potential for gastric injury and intolerance. Apart from its novel pharmacological features of pain control and inflammation reduction, it is also a free radical scavenger, and helps to protect against the tissue damage that occurs during inflammation.

Dosage

Apply three or four times per day

Pharmacokinetics

Nimesulide gel is rapidly absorbed, C_max (Maximum Peak Concentration) is reached rapidly within 120 minutes after application. Its effective concentration occurs in blood within 30 minutes after treatment and can persist for 8 hours post treatment.

Contraindications

Use in the following conditions is contraindicated:

Active peptic ulcer
Moderate to severe hepatic disease
Pregnancy
Gastrointestinal bleeding
Severe kidney
Bleeding disorders
Hypersensitivity

Drug interaction

Cyclosporine, digitalis glycosides, lithium, methotrexate, phenytoin
Nimesulide may displace salicylic acid and furosemide (but not warfarin) from plasma proteins

Side effects

Common (affecting between 1 in 10 to 1 in 100 people)

Skin rash
Burning sensation on the skin

Uncommon (affecting between 1 in 100 to 1 in 1000 people)

Dizziness
Pruritis

Precautions

History of alcohol abuse, colitis, crohn's disease, diverticulitis, gastric ulcer, diabetes mellitus, hemorrhoids, hepatitis, renal disease, rectal irritation or bleeding, burning sensation and tobacco abuse may increase chance of adverse effects.

Clinical evidence

Nimesulide gel is effective and much safer for the treatment of osteoarthritis. Treatment group received topical nimesulide gel 1% on the knee 3 times a day whereas placebo group received an identical-appearing gel for 30 days. The overall WOMAC (Western Ontario and McMaster Universities Osteoarthritis Index) scores was significantly better than placebo (P = 0.03), but physical functioning, stiffness, and pain scales did not reach statistical significance. For the NHP (Nottingham Health Profile) scores there was an improvement at "energy level," "pain," "physical motion," and " Nottingham Health Profile distress" scores in the treatment group whereas no improvement was found in the placebo group. Both patient and physician satisfaction scores were significantly better in the treatment group. So it is concluded that topical nimesulide gel can have beneficial effects and can improve quality of life in patients with knee Osteoarthritis¹.
Nimesulide exhibits better efficacy than diclofenac and piroxicam. The superior analgesic activity of nimesulide gel, correlating with its pharmacokinetic profile indicates that the topical route of administration is safe and effective alternative to the oral and rectal routes².