ナブメトン 化学特性,用途語,生産方法
効能
鎮痛薬, 抗炎症薬, シクロオキシゲナーゼ阻害薬
商品名
レリフェン (三和化学研究所)
説明
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.
化学的特性
White Powder
使用
Nabumetone is an anti-inflammatory and antibacterial agent (1). A non-steroidal anti-inflammatory prodrug used for treatment of inflammatory and degenerative rheumatic diseases.
適応症
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.
定義
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.
一般的な説明
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.
薬物動態学
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.
臨床応用
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
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原材料
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