Drug Interaction:
NSAIDs include-
Propionic acid- Fenoprofen, Flurbiprofen, Ibiprofen, Ketoprofen, Naproxen, Naproxen Sodium, Oxaprozin Acetic acids- Diclofenac sodium, Etodolac, Indomethicin, Ketorolac, Nabumetone, Sulindac, Tolmetin Fenamates (anthralic acids) - Meclofenamate, Mefenamic acxid Oxicams- Piroxicam
Refer- Ibuprofen
Drug interactions - summary
Warfarin- they are likely to displace other protein-bound drugs from their sites eg. anticoagulants, warfarin
Antacids Antacids does not affect the bioavailability of nabumetone
Food Bioavailability of 6-MNA is unaffected when taken with food,but increased when taken along with milk.
Indication:
Osteoarthiritis
Rheumatoid arthiritis
Apporved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
Nabumetone NSAID 18-05-1999
NSAIDs include- Propionic acid- Fenoprofen, Flurbiprofen, Ibuprofen, Ketoprofen, Naproxen, Naproxen Sodium, Oxaprozin Acetic acids- Diclofenac sodium, Etodolac, Indomethicin, Ketorolac, Nabumetone, Sulindac, Tolmetin Fenamates (anthralic acids) - Meclofenamate, Mefenamic acxid Oxicams- Piroxicam
Refer- Ibuprofen
Adverse Reaction:
Gastrointestinal ulceration and bleeding, Abdominal pain, dyspepsia, Diarrhoea, nausea, flatulance, Stomatitis, headache, Tinitis, dizziness, Rash, pruritis, Constipation, edema, Insomnia, nervousness, Somnolence
Contra-Indications:
Active peptic ulceration severe hepatic impairment Hypersensitivity to the drug Patients in whom other NSAIDs or aspirin are likely to induce asthma, urticaria, or other type of allergic reactions.
Special precautions:
Use in children not recommended Pregancy and lactation- safety not established Patients suffering from renal failure are likely to accumulate the inactive metabolites
Patients with impaired renal function, heart failure, liver dysfunction and those on diuretics and elderly are at greater risk of precipitating renal decomposition.
Severe GIT ulcerations and bleeding can occur without warning symptoms Monitor patients for early sign or symptoms
Dosages/ Overdosage Etc:
Osteoarthiritis Rheumatoid arthiritis
Dosage-
2 tabs as a single dose bedtime dose In more severe cases an additional 1 to 2 tabs may be given in the morning
Elderly- 1 to 2 tabs daily Not recommended for children
Other Information:
EVIDENCE BASED MEDICINE (April 2003)
Pain of Osteoarthiritis
Comparative effectiveness of various interventions
Beneficial
1. Systemic simple analgesics (eg paracetamol for short term pain relief, and improvement in function)
2. Systemic NSAIDs (short term pain relief and improvement in function)
3. Topical agents (short term pain relief)
Likely to be beneficial
1. Education, dietary advice,empowerment and support ( improved knowledge of disease and pain relief)
2. Physical support (pain relief and improvement in function)
KEY POINTS
1. There is no good evidence that NSAIDs were superior to simple analgesics such as paracetamol or to suggest that any one of the many available NSAIDs had greater efficacy in relieving pain of osteoarthritis.
2. One systematic review of randomised controlled trials has found that topical agents provide pain relief in patients with osteoarthritis and offer a non-toxic alternative to systemic drug treatment. However there is no evidence to indicate whether the prescribed agents were superior to less expensive, non-prescribtion drugs over the counter (OTC) alternatives, or to other local treatments such as hot or cold packs.
Patient Information:
NSAIDs include-
Propionic acid- Fenoprofen, Flurbiprofen, Ibuprofen, Ketoprofen, Naproxen, Naproxen Sodium, Oxaprozin Acetic acids- Diclofenac sodium, Etodolac, Indomethicin, Ketorolac, Nabumetone, Sulindac, Tolmetin Fenamates (anthralic acids) - Meclofenamate, Mefenamic acxid Oxicams- Piroxicam
Refer- Ibuprofen
1. Patients with impaired renal function, heart failure are at a greater risk of precipitating renal decomposition
2.Safety for use during pregnancy and laction not established
3.Safety for use on children not established.
Pharmacology/ Pharmacokinetics:
Pharmacolgy:
Nabumetone is a weak cyclo-oxygenase inhibitor and is converted by the liver to( 6-MNA) 6-methoxy-2-Napththylacetic acid a potent inhibitor of prostanoid synthesis.
Pharmcokinetics:
Following oral administration, Nabumetone is well absorbed from the GIT. The peak synovial concentration of the active metabolite, 6-MNA in patients with rheumatoid arthritis was 10-16 mg/L attained within 4-12 hours of administration. Nabumetone's active metabolite is extensively bound to plasma. The mean plasma half-life is 22 hours, and the mean plasma clearance of 6-MNA is 20-30 ml/min and elimination half-life is 24 hours approximately
Interaction with Food:
Bioavailability of 6-MNA is unaffected when taken with food, but increased when taken along with milk.
Pregnancy and lactation:
Safety during pregnancy and lactation not established Safety on use for children not established