Nabumetone and medical uses

Nabumetone is a nonsteroidal anti-inflammatory drug (NSAID).Nabumetone was developed by Beecham and first received regulatory approval in 1991.It has many brand names such as Relafen, Relifex, and Gambaran.Nabumetone is a nonacidic NSAID prodrug that is rapidly metabolized in the liver to the active metabolite 6-methoxy-2-naphthylacetic acid.As previously discovered with NSAIDs, the active metabolite of nabumetone inhibits cyclooxygenase and preferentially blocks COX-2 activity (which indirectly contributes to inflammation and pain during arthritis). The active metabolite of nabumetone is believed to be the compound primarily responsible for the therapeutic effect.In contrast, the parent drug is a less effective inhibitor of COX-2 byproducts, especially prostaglandins.It may be less nephrotoxic than indomethacin.This compound has two known polymorphs.Nabumetone had minimal effects on renal prostaglandin secretion and a lesser association with heart failure than other conventional drugs in its class.Nabumetone is also effective in controlling blood pressure in hypertensive patients taking ACE inhibitors,is equivalent to paracetamol.

Medical uses 

Similar in action to other NSAIDs, Nabumetone is used to treat pain and inflammation.

Side effects

It has been shown to have a slightly lower risk of gastrointestinal side effects than most other nonselective NSAIDs because it is a nonacidic prodrug that is metabolized to its active 6-MNA (6-methoxy-2-naphthaleneacetic acid) form.Side effects include bloody or black tarry stools; changes in color, frequency, or amount of urine; chest pain; shortness of breath; coughing up blood; pale stools; numbness; weakness; flu-like symptoms; leg pain; vision problems; speech problems; difficulty walking; weight increased; stomach pain; cold sweat; rash; blisters; headache; swelling; bleeding; bruising; vomiting blood; jaundice; diarrhea; constipation; dizziness; indigestion; gas; nausea; and ringing in the ears.In October 2020, the U.S. Food and Drug Administration (FDA) required updates to drug labels on all NSAIDs to describe the risk of kidney problems in an unborn baby resulting in low amniotic fluid.They advise pregnant women at 20 weeks or later to avoid NSAIDs.