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Overview
| Generic Names: | Nabumetona; Nabumetonum [INN-Latin] |
|---|---|
| Trade Names: | Arthaxan; Balmox; Consolan; Dolsinal; Flambate; Listran; Mebutan; Nabuser; Prodac; Relafen; Relif; Relifen; Relifex; Unimetone |
| PharmGKB Accession Id: | PA450572 |
Description
Nabumetone is a non-steroidal anti-inflammatory drug of the arylalkanoic acid family (which includes diclofenac). Marketed under the brand name Relafen, it has been shown to have a slightly lower risk of gastrointestinal side effects than most other non-selective NSAID's. (source: Drug Bank)
Indication
For acute and chronic treatment of signs and symptoms of osteoarthritis and rheumatoid arthritis. (source: Drug Bank)
ATC Therapeutic Category
- M01AX:Other antiinflammatory and antirheumatic agents, non-steroids
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
The parent compound is a prodrug, which undergoes hepatic biotransformation to the active component, 6-methoxy-2-naphthylacetic acid (6MNA), that is a potent inhibitor of prostaglandin synthesis, most likely through binding to the COX-1 and COX-2 receptors. (source: Drug Bank)
Pharmacology
Nabumetone is a naphthylalkanone. It is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic and antipyretic properties in pharmacologic studies. As with other nonsteroidal anti-inflammatory agents, its mode of action is not known. However, the ability to inhibit prostaglandin synthesis may be involved in the anti-inflammatory effect. (source: Drug Bank)
Food Interactions
Avoid alcohol.
Take with food for faster absorption.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Undergoes rapid biotransformation to the principal active metabolite, 6-methoxy-2-naphthylacetic acid (6MNA). Approximately 35% of a 1000 mg oral dose of nabumetone is converted to 6MNA and 50% is converted into unidentified metabolites which are subsequently excreted in the urine. (source: Drug Bank)
Protein Binding
The active metabolite, 6MNA, is more than 99% bound to plasma proteins. (source: Drug Bank)
Absorption
Well absorbed from the gastrointestinal tract. Coadministration of food increases the rate of absorption and subsequent appearance of 6MNA (the active metabolite) in the plasma but does not affect the extent of conversion of nabumetone into 6MNA. (source: Drug Bank)
Toxicity
The one overdose occurred in a 17-year-old female patient who had a history of abdominal pain and was hospitalized for increased abdominal pain following ingestion of 30 nabumetone tablets (15 grams total). Stools were negative for occult blood and there was no fall in serum hemoglobin concentration. The patient had no other symptoms. (source: Drug Bank)
Isomeric SMILES Code:
CC(=O)CCc1ccc2cc(ccc2c1)OC (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
|
NR1I2 |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| PTGS1 |
|
(source: Drug Bank) |
| PTGS2 |
|
(source: Drug Bank) |
PharmGKB Curated Pathways
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| acenocoumarol |
|
The NSAID increases the anticoagulant effect (source: Drug Bank) |
| alendronate |
|
Increased risk of gastric toxicity (source: Drug Bank) |
| cyclosporine |
|
Monitor for nephrotoxicity (source: Drug Bank) |
| dicumarol |
|
The NSAID increases the anticoagulant effect (source: Drug Bank) |
| methotrexate |
|
The NSAID increases the effect and toxicity of methotrexate (source: Drug Bank) |
| warfarin |
|
The NSAID increases the anticoagulant effect (source: Drug Bank) |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.
