Nimesulide

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Nimesulide
Systematic (IUPAC) name
N-(4-Nitro-2-phenoxyphenyl)methanesulfonamide
Identifiers
CAS number	51803-78-2
ATC code	M01AX17[1]
PubChem	4495
Chemical data
Formula	C₁₃H₁₂N₂O₅S
Mol. mass	308.311
Pharmacokinetic data
Bioavailability	?
Protein binding	>97.5%
Metabolism	Hepatic
Half life	1.8-4.7h
Excretion	Renal(50%) Fecal(29%)
Therapeutic considerations
Pregnancy cat.	?
Legal status	Prescription only Drug
Routes	oral, rectal, topical

Nimesulide is a prescription non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties and its approved indications are the treatment of acute pain, the symptomatic treatment of osteoarthrosis and primary dysmenorrhoea in adolescents and adults above 12 years old. Nimesulide is among the top 5 non-steroidal anti-inflammatory drugs worldwide.

1 History
2 Availability
- 2.1 Trade names
3 Pharmacokinetics
4 Side effects
5 References
6 External links

[edit] History

It was launched in Italy for the first time as Aulin and Mesulid in 1985 and is presently available in more than 50 countries worldwide, among others France, Portugal, Greece, Switzerland, Belgium, Ireland, Mexico, Brazil.

Alembic Ltd. issued a circular asking wholesalers and retailers to withdraw all stocks of Nimegesic Drops (a pediatric dosage form of nimesulide) in 2003.^[1]

[edit] Availability

It is available in a variety of forms: tablets, powder for dissolution in water, suppositories and topical gel. A recent evaluation from EMEA (the European Medicines Agency) concluded that the overall benefit/risk profile of nimesulide is favourable and in line with that of the other NSAIDs (such as for example, diclofenac, ibuprofen, naproxen).

[edit] Trade names

Nimesulide is available through the world as original product with the following trademarks: Aulin, Ainex, Donulide, Edrigyl, Eskaflam, Heugan, Mesulid, Nexen, Nimed, Nimedex, Nisulid, Scaflam, Scaflan. Sulidene and Zolan for veterinary use. Many generic and copy-products also exist (Coxtral, Lusemin, Medicox, Nidol, Nimalox, Nimesil, Nimulid, Ventor, Willgo among others).

[edit] Pharmacokinetics

Nimesulide is rapidly absorbed following oral administration.^{[citation needed]} Nimesulide undergoes extensive biotransformation, mainly to 4-hydroxynimesulide (which also appears to be biologically active).^{[citation needed]} Food, gender and advanced age have negligible effects on nimesulide pharmacokinetics.^{[citation needed]} Moderate renal impairment does not necessitate dosage adjustment while patients with severe renal impairment or hepatic insufficiency should be treated with a lower dose.^{[citation needed]}

In terms of onset of clinical effect, nimesulide has a relatively onset of action, with meaningful reductions in pain and inflammation observed in less than one hour.^{[citation needed]}

As many as almost 480 million patients have been treated with nimesulide from its launch until today.^{[citation needed]}

The therapeutic effects of Nimesulide are the result of its complete mode of action which targets a number of key mediators of the inflammatory process such as: COX-2 mediated prostaglandins, free radicals, proteolytic enzymes and histamine.^{[citation needed]}

Clinical evidence are available to support a particularly good profile in terms of gastrointestinal tolerability.^{[citation needed]} As all anti-inflammatory drugs, it should be taken in compliance with the recommendations included in the patient leaflet.

[edit] Side effects

Like most drugs in NSAID category, nimesulide is known to be hepatotoxic (damaging to the liver) in rare but unpredictable cases and should be taken with care. It did not achieve Food and Drug Administration (FDA) approval in the USA, and is banned in many countries due to cases of jaundice and hepatitis induced by its use. Italy was the first country to allow the drug in 1985. The European Medicine Evaluation Agency has prohibited the use of nimesulide for children under the age of 2.