Acute Porphyria Drug Database

Monograph

M01AX01 - Nabumetone
Propably not porphyrinogenic
PNP

Rationale
Nabumetone and its metabolite is metabolised by CYP1A2 and CYP2C9, respectively in vitro. No clinical observations of CYP-induction or –inhibition. Risk for gastrointestinal adverse events in the form of nausea and diarrhoea motivates vigilance against insufficient intake of food, especially of carbohydrate.
Chemical description
Nabumetone is a prodrug and is metabolised to the active metabolite, 6-methoxy-2-naphtylacetic acid (6-MNA).
Therapeutic characteristics
Nabumetone is indicated for the treatment of rheumatoid arthritis and osteoarthritis. Common side effects that can be potentially porphyrinogenic through reduction in carbohydrate intake and that also can be confused with an acute porphyria attack are abdominal pain, nausea, diarrhoea, dyspepsia and obstipation. A less common side effect is pseudo porphyria.
Metabolism and pharmacokinetics
Nabumetone is a prodrug and goes through extensive first-pass metabolism. It is metabolised to 6-MNA (SPC), then hydroxylated to 6-HNA (Matsumoto 2011) and conjugated before excretion in urine (Matsumoto 2011 and SPC). In vitro data indicate that CYP1A2 have a central role in the nabumetone bioactivation and that CYP2B6, CYP2C19, CYP2D6 and CYP2E1 might act as minor metabolic pathways (Turpeinen 2009). In vitro data also suggests that CYP2C9 metabolise 6-MNA to 6-HNA (Matusmoto 2011). 6-MNA has been shown to be a very weak inhibitor of CYP2C9 in human liver microsomes and to have no significant effect on CYP1A2, CYP2A6, CYP2C, CYP2D6 and CYP3A4 (Matsumoto 2011). No drug-drug interactions has been reported with nabumetone as a perpetrator concerning CYP enzymes (DRUID and Interaktionsdatabasen), which may indicate that it is not an inducer or an inhibitor of them.
IPNet drug reports
Uneventful use reported in 1 patient with acute porphyria.

References

# Citation details PMID
*Scientific articles
1. In vitro characterization of the cytochrome P450 isoforms involved in the metabolism of 6-methoxy-2-napthylacetic acid, an active metabolite of the prodrug nabumetone.
Matsumoto K, Nemoto E, et al. Biol Pharm Bull. 2011;34(5):734-9.
2. A predominate role of CYP1A2 for the metabolism of nabumetone to the active metabolite, 6-methoxy-2-naphthylacetic acid, in human liver microsomes.
Turpeinen M, Hofmann U, et al. Drug Metab Dispos. 2009 May;37(5):1017-24.
*Drug interaction databases
3. DRUID. nabumeton
4. Interaktionsdatabasen. nabumeton
*Summary of Product Characteristics
5. Norwegian medicines agency. Summary of Product Characteristics (SPC). Nabumetone.

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Tradenames and packages
From some sources, we get a list of packages (United Kingdom, Ireland, Estonia). Other sources contain more or less "clean" versions of the trade name (Denmark, Finland, Iceland, Lithuania, Norway). What you see here is the raw data we get from each country, so there will appear to be duplicates. The bold names are the searchable terms. The gray names that follow are all mapped to the bolded term.
Note: The cleaning is done automatically by a proprietary algorithm, and it may produce errors. We strive to improve it continuously.
Netherlands
Mebutan · Mebutan 1 g, tabletten · Mebutan 500 mg, tabletten · Mebutan Dispers 1 g, tabletten
Belgium
Gambaran · Gambaran 500 mg compr. pellic. · Nabumeton · Nabumeton Tillomed 500 mg compr. pellic.
United Kingdom
Nabumetone · Nabumetone 500mg tablets · Nabumetone 500mg/5ml oral suspension · Relifex · Relifex 500mg dispersible tablets · Relifex 500mg tablets · Relifex 500mg/5ml oral suspension
Denmark
Relifex
Norway
Relifex
Poland
Nabuton VP
Luxembourg
GAMBARAN
Iceland
Relifex
Latvia
Relifex
 
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