Nabumetone is a non-steroidal anti-inflammatory drug

Non-steroidal anti-inflammatory drug

Nonsteroidal anti-inflammatory drugs, usually abbreviated to NSAIDs or NAIDs, but also referred to as nonsteroidal anti-inflammatory agents/analgesics or nonsteroidal Anti-inflammatory medicines , are drugs with analgesic and antipyretic effects and which have, in higher doses, anti-inflammatory...

 (NSAID), the only 1-naphthaleneacetic acid

1-Naphthaleneacetic acid

1-Naphthaleneacetic acid, commonly abbreviated NAA, is an organic compound with the formula C10H7CH2CO2H. This colourless solid is soluble in organic solvents...

 derivative. Nabumetone has been developed by Beecham

Beecham (pharmaceutical company)

Beecham was a British pharmaceutical company. It was once a constituent of the FTSE 100 Index. Beecham, after having merged with SmithKline Beckman, merged with GlaxoWellcome to become GlaxoSmithKline .-History:...

. It is available under numerous brand names, such as Relafen, Relifex and Gambaran.

Introduction

Nabumetone is a non acidic NSAID (Non-steroidal anti-inflammatory drug) that is rapidly metabolized in the liver to a major active metabolite, 6-methoxy-2-naphthyl acetic acid. As found with previous NSAIDs, nabumetone's active metabolite inhibits the cyclooxygenase enzyme preferentially blocks cyclo-oxygenase-2 activity which is indirectly responsible for the production of inflammation and pain during arthritis by way of enhancing the production of endoperoxides and prostaglandins E2 and I2 (prostacyclin). The active metabolite of nabumetone is felt to be the compound primarily responsible for therapeutic effect. Comparatively, the parent drug is a poor inhibitor of prostaglandin synthesis. It may be less nephrotoxic than indomethacin which decreases the excretion of 6-oxo-PGF1a by inhibition of cyclooxygenase- 1 or by inhibition of specific exercise-induced activation of cyclo-oxygenase-2, or both . Nabumetone belongs to a new class of NSAID with a low potential for causing gastrointestinal mucosal irritancy and inhibition of platelet function and has little effect on renal prostaglandin secretion and had less of an association with CHF (congestive heart failure) than other traditional drugs of the class . Effects of nabumetone on blood pressure control in hypertensive patients on ACE inhibitors is also good i.e. equivalent to paracetamol .

Uses

It is used to treat pain or inflammation caused by arthritis. Nabumetone works by reducing the effects of hormones that cause pain and inflammation.

Side effects

It has been shown to have a slightly lower risk of gastrointestinal side effects than most other non-selective NSAIDs since it is a non-acidic prodrug which is then metabolized to its active 6MNA (6-methoxy-2-naphthylacetic acid) form.

Assay of Nabumetone

There are few papers published reporting analytical methods for nabumetone. Two of them employed HPLC with UV-detection . One HPLC method using direct injection on restricted access media columns . Flow injection analysis (FIA) with UV-detection was also reported for the determination of nabumetone in pharmaceutical preparations . Methods using HPLC with fluorescence detection were reported. M. Nobilis et al. carried out biotransformation and disposition studies in humans and minipigs using HPLC with UV, fluorescence and mass spectrometric detection. The interactions with gamma-cyclodextrin were also studied by fluorescence measurements13. Assay methods employed HPLC using UV detection, photodiode array (PDA) detector and mass spectrometric detection for the determination of nabumetone and its metabolites. Murillo Pulgarín et al. reported three analytical methods using different techniques along with phosphorescence. Liquid chromatography methods using different techniques of mass spectrometry were also reported . The electrochemical behavior of nabumetone by a voltammetric technique and a novel colorimetric method based on chemical derivatization were also published.