Nabumetone
- CAS No.
- 42924-53-8
- Chemical Name:
- Nabumetone
- Synonyms
- RELAFEN;relifex;Nabumeton;brl147777;BRL-14777;NABUMETONE;Nabumetone RS;Nabumetone CRS;Nabumetone (DMF);Nabumetone (200 mg)
- CBNumber:
- CB2386779
- Molecular Formula:
- C15H16O2
- Molecular Weight:
- 228.29
- MOL File:
- 42924-53-8.mol
- Modify Date:
- 2024/8/7 19:09:42
| Melting point | 80-810C |
|---|---|
| Boiling point | 330.1°C (rough estimate) |
| Density | 1.0657 (rough estimate) |
| refractive index | 1.5542 (estimate) |
| storage temp. | Sealed in dry,2-8°C |
| solubility | Soluble in alcohol or chloroform |
| form | Solid |
| color | White |
| Water Solubility | 6mg/L(22.5 ºC) |
| BCS Class | 2/4 |
| CAS DataBase Reference | 42924-53-8(CAS DataBase Reference) |
| NIST Chemistry Reference | Nabumetone(42924-53-8) |
Nabumetone price More Price(3)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich(India) | N6142 | Nabumetone analytical standard | 42924-53-8 | 5G | ₹16313.28 | 2022-06-14 | Buy |
| Sigma-Aldrich(India) | PHR3056 | Nabumetone pharmaceutical secondary standard, certified reference material | 42924-53-8 | 500MG | ₹18066.93 | 2022-06-14 | Buy |
| Sigma-Aldrich(India) | N6142 | Nabumetone analytical standard | 42924-53-8 | 10G | ₹22635.08 | 2022-06-14 | Buy |
Nabumetone Chemical Properties,Uses,Production
Description
Nabumetone is a non-acidic, nonsteroidal antiinflammatory agent formally related to naproxen. Its main circulating metabolite is 6-methoxy-2-naphthylacetic acid (α-nornaproxen). Administered once daily (Tsub>1/2 * 30 hrs), nabumetone is reported to be effective in the treatment of rheumatoid and osteoarthritis.
Chemical Properties
White Powder
Uses
Nabumetone is an anti-inflammatory and antibacterial agent (1). A non-steroidal anti-inflammatory prodrug used for treatment of inflammatory and degenerative rheumatic diseases.
Indications
Nabumetone (Relafen) is approved for rheumatoid arthritis, osteoarthritis, and pain management. Its long half-life allows for once-daily dosing. Although this drug is a weak inhibitor of COX, it is metabolized in the liver to 6-methoxy-2-naphthylacetic acid (6-MNA), a strong COX inhibitor that is chemically similar to naproxen. As with most NSAIDs, GI side effects are most commonly reported. The incidence of gastric ulceration is lower with nabumetone than with many other NSAIDs.This is due to its nature as a prodrug, not to COX-2 selectivity. Lower-bowel complaints, rashes, and CNS disturbances are common adverse effects.
Definition
ChEBI: A methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthylacetic acid, following oral administration. It is s own to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs.
General Description
Nabumetone (Relafen), a nonacidic NSAID prodrug, isclassified as an arylacetic acid, because it undergoes rapidhepatic metabolism to its active metabolite, 6-methoxy-2-naphthylacetic acid. Similar to the other arylacetic aciddrugs, it is used in short- or long-term management of RAand OA. Being nonacidic, it does not produce significantprimary insult to the GI mucosa lining and also has no effecton prostaglandin synthesis in gastric mucosa, thus producingminimum secondary GI damage when comparedwith other conventional NSAIDs.
Pharmacokinetics
Nabumetone is absorbed primarily from the duodenum. Milk and food increase the rate of absorption and the bioavailability of the active metabolite. Plasma concentrations of unchanged drug are too low to be detected in most subjects after oral administration, so most pharmacokinetic studies have involved the disposition of the active metabolite. Pharmacokinetic properties are altered in elderly patients, with higher plasma levels of the active metabolite being noted. Nabumetone undergoes rapid and extensive metabolism in the liver, with a mean absolute bioavailability of the active metabolite of 38%. The metabolism of nabumetone is illustrated in Figure 36.15. The major, most active metabolite is 6MNA, but the initial alcohol metabolite, a minor product, and its esters also possess significant anti-inflammatory properties.
Clinical Use
Nabumetone is indicated for the acute and chronic treatment of the signs and symptoms of osteoarthritis and rheumatoid arthritis. The recommended starting dosage is 1,000 mg as a single dose with or without food. More symptomatic relief of severe or persistent symp-toms may be obtained at doses of 1,500 or 2,000 mg/day
Nabumetone Preparation Products And Raw materials
Raw materials
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| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| AVD pharmaceuticals Pvt Ltd | +919860835260 | Pune, India | 102 | 58 | Inquiry |
| SHOBHA LIFE SCIENCES PRIVATE LIMITED | +919121212469 | Hyderabad, India | 31 | 58 | Inquiry |
| KARPSCHEM LABORATORIES | +91-7249203006 +91-7249203006 | Maharashtra, India | 786 | 58 | Inquiry |
| Divis Laboratories Ltd | +91-4066966413 +91-4066966413 | Hyderabad, India | 34 | 58 | Inquiry |
| Arch Pharmalabs Ltd | +91-2242871210 +91-2242871210 | Maharashtra, India | 51 | 58 | Inquiry |
| Acute Research | +91-9825068697 +91-9825068697 | Gujarat, India | 43 | 58 | Inquiry |
| Alfa Omega Pharma | +91-8050045945 +91-9972665399 | Maharashtra, India | 126 | 58 | Inquiry |
| Mylan Laboratories Ltd | +91-4023550543 +91-4030866666 | Telangana, India | 150 | 58 | Inquiry |
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
| Supplier | Advantage |
|---|---|
| AVD pharmaceuticals Pvt Ltd | 58 |
| SHOBHA LIFE SCIENCES PRIVATE LIMITED | 58 |
| KARPSCHEM LABORATORIES | 58 |
| Divis Laboratories Ltd | 58 |
| Arch Pharmalabs Ltd | 58 |
| Acute Research | 58 |
| Alfa Omega Pharma | 58 |
| Mylan Laboratories Ltd | 58 |
| CLEARSYNTH LABS LTD. | 58 |
| A.J Chemicals | 58 |
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