NSAIDS

Information about NSAIDS

The nonsteroidal antiinflammatory drugs (NSAIDs) are a group of chemically heterogenous medications used widely in the therapy of mild-to-moderate pain and inflammation. 

Mechanism of action of NSAIDS

NSAIDs act through inhibition of intracellular cyclo-oxygenase enzymes (Cox-1 and Cox-2), which cause a decrease in synthesis of the proinflammatory prostaglandins that are potent mediators of pain and inflammation.  Most NSAIDs are nonselective and inhibit both Cox-1 and Cox-2.  Recently, several selective inhibitors of Cox-2 have been developed that have the antiinflammatory and analgesic efficacy of other NSAIDs, but lack the effects on gastric and renal tissue that account for a majority of their adverse events (gastrointestinal bleeding and renal insufficiency).  NSAIDS are among the most frequently prescribed drugs worldwide and rarely cause drug induced liver disease. 

Liver safety of NSAIDS

An estimated 30 million Americans take NSAIDs every year, so that despite the overall low incidence of NSAID induced hepatotoxicity, their widescale use makes them an important cause of drug induced liver injury.

NSAIDS are indicated in the treatment of various acute and chronic inflammatory conditions, headaches, and fever.  The pharmacologic properties of the various NSAIDS are related to their molecular structure, which can be categorized into the five classes (Table).  Not all of these agents are currently available either in the United States or elsewhere.  Only ibuprofen and naproxen are available over-the-counter (in the United States); the rest are by prescription only.  Carprofen and phenylbutazone are available in the United States as veterinary medications.  NSAIDs withdrawn from use or testing because of hepatotoxicity or other serious adverse events include benoxaprofen, sudoxicam, isoxicam, fluproquazone, bromfenac, oxyphenbutazone and phenylbutazone (aplastic anemia), indoprofen (gastrointestinal bleeding), suprofen and zomepirac (anaphylaxis). 

NSAIDs in use in other countries of the world include acemetacin, azaproprazone, fenbufen, feprazone, floctafenine, flufenamic acid, nimesulide, pirprofen, and tiaprofenic acid.

PROPIONIC ACIDS	ACETIC ACIDS	FENAMIC ACIDS	PYRAZALONES	OXICAMS
Carprofen Benoxaprofen Fenbufen Fenoprofen* Flurbiprofen* Ibuprofen* Indoprofen Ketoprofen*  Loxoprofen Oxaprozin* Naproxen* Pirprofen Tiaprofenic acid	Aceclofenac* Acemetacin Bromfenac Diclofenac*  Etodolac*  Indomethacin*  Ketorolac* Nabumetone* Sulindac* Tolmetin* Zomepirac	Floctafenine Flufenamic Meclofenamate* Mefenamic acid*	Azapropazone Feprazone Oxyphenbutazone Phenylbutazone	Isoxicam Lornoxicam  Meloxicam* Piroxicam* Sudoxicam

 * Currently available for human use in the United States.

• Dailymed label info on NSAIDS
• FDA NSAIDS

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