Nabumetone

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DRUGS
Nabumetone

Nabumetone belongs to a class of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs). It is used primarily to reduce pain, swelling, and joint stiffness from rheumatoid arthritis or osteoarthritis.

Introduction

Nabumetone belongs to a class of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs). It is used primarily to reduce pain, swelling, and joint stiffness from rheumatoid arthritis or osteoarthritis.

Pharmacological class: NSAID

Indications

  • Osteoarthritis
  • Rheumatoid arthritis
  • Mild to moderate pain

Pharamcological Action

Nabumetone is a nonsteroidal anti-inflammatory drug (NSAID) of the arylalkanoic acid family. Nabumetone is a prodrug that upon hepatic catalysis converts into the active moiety 6-methoxy-2-naphthylacetic acid (6MNA). 6MNA inhibits the activity of the enzymes cyclo-oxygenase I and II, resulting in decreased formation of precursors of prostaglandins and thromboxanes. The resulting decrease in prostaglandin synthesis is responsible for the therapeutic effects of nabumetone.

Dosage

  • Osteoarthritis

Initial dose: 1000 mg orally, once a day

Maintenance dose: 1500 to 2000 mg orally per day in 1 or 2 divided doses

Maximum dose: 2000 mg/day

  • Rheumatoid Arthritis

Initial dose: 1000 mg orally, once a day

Maintenance dose: 1500 to 2000 mg orally per day in 1 or 2 divided doses

Maximum dose: 2000 mg/day

Pharmacokinetics

Nabumetone is well absorbed from the GI tract and diffuses readily into the synovia fluid. Nabumetone is metabolized to an active metabolite 6-methoxy-2-napthylacetic acid (6-MNA) and inactive metabolites; extensive first-pass effect; ~35% converted to 6MNA and 50% converted to unidentified metabolites. The active metabolite is excreted in urine (80%) and feces (9%). 

Contraindications

  • Contraindicated in patients with a history of hypersensitivity to nabumetone or excipients
  • Contraindicated in patients who have experienced asthma, urticaria, or allergic type reactions after taking acetylsalicylic acid or other NSAIDs. Severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients
  • Contraindicated in patients with severe hepatic failure
  • Contraindicated in patients with a history of GI bleeding or perforation, related to previous NSAIDs therapy
  • Contraindicated in patients with active, or history of recurrent, peptic ulcer/haemorrhage
  • Contraindicated in the third trimester of pregnancy and in nursing mothers
  • Contraindicated in patients with severe heart failure, and in patients with current cerebrovascular or other hemorrhage

Drug Interactions

  • Concomitant administration with corticosteroids increases risk of gastrointestinal ulceration or bleeding.
  • NSAIDs may enhance the effects of anticoagulants, such as warfarin and other anticoagulants.
  • Concomitant administration with anti-platelet agents and selective serotonin reuptake inhibitors (SSRIs) increases risk of gastrointestinal bleeding.
  • Hyperkalaemia might develop, particularly with concomitant potassium-sparing diuretics administration.

Side effects

Common (affecting between 1 in10 to 1 in 100)

  • Headache
  • Itching skin
  • Nausea
  • Rash
  • Stomach pain
  • Swelling

Uncommon (affecting 1 in 100 to 1 in 1000)

  • Burning feeling in chest or stomach
  • Indigestion
  • Stomach upset
  • Swelling or inflammation of the mouth
  • Tenderness in stomach area
  • Vomiting

Very rare (affecting less than 1 in 10,000)

  • Bleeding gums
  • Blistering, peeling, loosening of skin
  • Chest pain
  • Difficult or labored breathing
  • Fluid-filled skin blisters
  • General feeling of tiredness or weakness
  • Light-colored stools
  • Severe sunburn
  • Stomach bloating, burning, or cramping
  • Vaginal bleeding
  • Vomiting of blood or material that looks like coffee grounds

Precautions

  • Avoid in patients with known allergies to aspirin or other NSAIDs
  • Avoid in patients with asthma or with a history of worsening breathing after taking NSAIDs)
  •  Avoid in patients with heart failure or kidney disease
  • Avoid in patients with high blood pressure, liver disease and stroke

Clinic Evidence

In a double blind, randomized, parallel group study, 298 patients with rheumatoid arthritis received nabumetone (2000 mg/day) or naproxen (1000 mg/day) for 3 months. At the end point, nabumetone treated patients exhibited significant improvement in pain, Ritchie articular index, and duration of morning stiffness when compared to baseline. In contrast, naproxen treated patients showed significant improvement only in Ritchie articular index. Nabumetone was significantly more effective than naproxen for pain relief. Nabumetone was better tolerated than naproxen.1

References

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