API: Nabumetone

What Is Nabumetone and How Does It Work?

Nabumetone is a naphthyl alkanone nonsteroidal anti-inflammatory drug (NSAID) that works by blocking the effect of cyclooxygenase (COX) enzymes, but preferentially blocking COX-2 enzymes. COX enzymes are associated with the production of prostaglandins at the injury site, which cause both pain and inflammation. Blocking COX enzymes decreases prostaglandin production, thereby lowering pain and inflammation. This drug belongs to a new class of NSAIDs that are absorbed well in the gastrointestinal tract and therefore have a better chance of not irritating gastrointestinal mucosa.1 Nabumetone is used to treat reduce pain, swelling, and joint stiffness from chronic conditions such as arthritis.

Approved Indications

  • Osteoarthritis: Nabumetone can be used orally to relieve pain from osteoarthritis, a type of arthritis caused by a breakdown of lining in the joint. Joints that are typically affected include those in the knee, ankle, foot, elbow, wrist, and hand. Used as a topical liquid, diclofenac sodium can relieve osteoarthritis pain in the knees by reducing muscle contraction in the area.
  • Rheumatoid Arthritis: Oral formulations of nabumetone are also used to manage symptoms of rheumatoid arthritis, a chronic, autoimmune inflammatory disorder that typically affects the small joints in the hands and feet.
  • Psoriasis and psoriatic arthritis: Nabumetone may help reduce inflammation and pain due to psoriasis and psoriatic arthritis.2
  • Other: Off-label topical preparations of nabumetone have shown some promise for lowering pain.3

Side Effects and Drug Interactions

Common side effects in patients taking oral nabumetone include4:

  • Upset stomach or stomach pain
  • Bloating or gas
  • Diarrhea or constipation
  • Mild heartburn
  • Dizziness
  • Anxiety
  • Headache
  • Skin itch or rash
  • Tinnitus

Patients who suffer from severity of these common side effects should contact their pharmacist or physician right away. Patients who experience an allergic reaction (hives, trouble breathing, swelling of the face, lips, tongue, or throat) or chest pain, weakness, shortness of breath, problems with vision or balance, slurred speech, bloody, tarry, or black stools, unusual weight gain, swelling, lack of or less urination, nausea, loss of appetite, clay-colored stools, fever, jaundice, headache with a severe blistering or peeling skin rash, bruising, tingling or numbness, or muscle weakness should contact their physician immediately.

Patients who are allergic to nabumetone should not take this drug. This drug may interact with aspirin, some diuretics, ACE-inhibitors, lithium, methotrexate, and warfarin. Use of nabumetone has not been studied well in pregnant or nursing patients; however, general NSAIDs should be avoided during late pregnancy. Patients who have or have had asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs should advise their physician before taking this drug. Nabumetone is contraindicated for the treatment of peri-operative pain associated with  coronary artery bypass graft surgery.

Commercial preparations of nabumetone as a topical gel or cream are not currently available, thus the side effects of such are not well known.

Latest News and Research

Nabumetone is a unique type of drug because of its safety profile, especially in terms of how well it is absorbed in the gastrointestinal tract. Much of the literature reporting on this drug continues to examine its safety and efficacy profile, alone but perhaps more significantly, with other medications.5 One promising study looks at how a suppository containing a combination of diclofenac and nabumetone may help provide pain relief in arthritic patients who cannot take oral pills.6

Another promising area in nabumetone research is for the treatment of Duchenne muscular dystrophy, a traumatic disease caused by mutations in one of the body’s muscle cytoskeletal protein. Upregulation, or cellular increase, of utrophin, a homologue of dystrophin, may provide an effective treatment strategy—cellular studies of nabumetone shows promising results in this area.7

Studies evaluating the use of nabumetone as a topical gel are also in the works. Stable topical preparations of the drug are currently being developed so that safety and efficacy profiles can be evaluated.8

Buying Guide

Many compound pharmacists prefer Diclofenac sodium as a more well-studied alternative, especially for topical delivery. Please find more information about our Bulk APIs here.

Show 8 footnotes

  1. “Nabumetone,” September 16, 2013, http://www.drugbank.ca/drugs/DB00461
  2. “Nabumetone,” 2016, http://www.papaa.org/non-steroidal-anti-inflammatory-drugs-nsaids/nabumetone
  3. “Development of nabumetone topical gels: effect of formulation variables on the release of nabumetone,” 2012, http://www.wjpr.net/dashboard/abstract_id/120
  4. “Relafen,” May 15, 2015, http://www.rxlist.com/relafen-side-effects-drug-center.htm
  5. “A Controlled Study Comparing the Effects of Nabumetone, Ibuprofen, and Ibuprofen Plus Misoprostol on the Upper Gastrointestinal Tract Mucosa”, November 22, 1993, http://www.ncbi.nlm.nih.gov/pubmed/8239849
  6. “A diclofenac suppository–nabumetone combination therapy for arthritic pain relief and a monitoring method for the diclofenac binding capacity of HSA site II in rheumatoid arthritis,” March 2013, http://onlinelibrary.wiley.com/doi/10.1002/bdd.1829/abstract?userIsAuthenticated=false&deniedAccessCustomisedMessage=
  7. “Drug Discovery for Duchenne Muscular Dystrophy via Utrophin Promoter Activation Screening,” October 20, 2011, http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0026169
  8. “Development and Evaluation of Solid Dispersion Incorporated Topical Gel of Nabumetone,” July 2014, http://www.indianjournals.com/ijor.aspx?target=ijor:rjpt&volume=7&issue=12&article=011