フェニルブタゾン 化学特性,用途語,生産方法
外観
白色〜わずかにうすい黄色, 結晶性粉末〜粉末
溶解性
エタノール及びアセトンに溶け、水にほとんど溶けない。
用途
フェニルブタゾン (Phenylbutazone) は非ステロイド性抗炎症薬の一つで、短期的な鎮痛および動物の解熱に用いられる。 しばしば "bute" と略され。
鎮痛剤: 感染症や捻挫、オーバーユース傷害、屈腱炎、関節痛、関節炎、蹄葉炎などの筋骨格系障害(英語版)に際して鎮痛のために用いられる。他の非ステロイド性抗炎症薬と同様、運動器の組織に直接作用して炎症を抑え、炎症による二次傷害を防ぎ、痛みを緩和し、関節可動域を維持する。筋骨格系障害そのものを治癒するわけではなく、疝痛にも効果がある。
解熱薬: 発熱をやわらげるために用いられる。
効能
鎮痛薬, 抗炎症薬, 解熱薬, 抗リウマチ薬, シクロオキシゲナーゼ阻害薬
説明
Phenylbutazone, one of the earliest NSAIDs
introduced, is now indicated for the symptomatic
relief of rheumatoid arthritis, osteoarthritis, psoriatic arthritis, ankylosing spondylitis, gout, and
acute superficial thrombophlebitis. The gastrointestinal and bone marrow toxicity observed in its early use have been greatly
reduced by lower dosage (300 mg/d). Nevertheless, it is used primarily where other drugs have
failed and then only for short-term therapy. The
drug has a long serum half-life of about 100 h. It
is a moderately active cyclooxygenase inhibitor
and it suppresses both spontaneous and chemotactic motility of neutrophils. In addition to the
serious gastrointestinal and hematological adverse effects, sodium and water retention, rash,
vertigo, and dermatitis are observed.
化学的特性
Off-Whtie Solid
使用
Phenylbutazone, a nonsteroidal anti-inflammatory drug, is an efficient reducing cofactor for the peroxidase activity of COX. Phenylbutazone-dependent inactivation of COX and prostacyclin synthase is markedly increased in the presence of 100 μM hydrogen peroxide with half-maximal effects at Phenylbutazone concentrations of 100 and 25 μM for COX and prostacyclin synthase, respectively.
世界保健機関(WHO)
Phenylbutazone, a pyrazolone derivative with anti-inflammatory,
analgesic and antipyretic activity, was introduced in 1949 for the treatment of
rheumatic disorders. Its use was subsequently associated with serious and
sometimes fatal adverse reactions, notably cases of aplastic anaemia and
agranulocytosis. Many national drug regulatory authorities consider that more
recently introduced drugs offer a safer alternative for most, if not all, patients
requiring anti-inflammatory agents. Phenylbutazone has thus been either
withdrawn at the national level or retained with rigorously restricted indications for
patients unresponsive to other therapy. These restrictions also apply, in general, to
combination products containing phenylbutazone.
一般的な説明
Odorless white or off-white crystalline powder. Tasteless at first, but slightly bitter aftertaste. pH (aqueous solution) 8.2.
空気と水の反応
Phenylbutazone is relatively stable at ambient temperatures. Aqueous decomposition of Phenylbutazone occurs by hydrolysis and oxidation. Insoluble in water.
反応プロフィール
Phenylbutazone is incompatible with strong oxidizers, strong acids and strong bases. .
火災危険
Flash point data for Phenylbutazone are not available; however, Phenylbutazone is probably combustible.
安全性プロファイル
Suspected human
carcinogen producing leukemia. A human
poison by parenteral route. An experimental poison by ingestion, intraperitoneal,
subcutaneous, intravenous, and
intramuscular routes. Human systemic
effects by ingestion and possibly other
routes: fever, blood pressure increase, other
unspecified vascular effects, damage to
kidney tubules and glomeruli, decreased
urine volume, blood in the urine, reduction
in the number of whte blood cells, and
agranulocytosis. Experimental teratogenic
and reproductive effects. Human mutation
data reported. An eye irritant. An antiinflammatory agent. When heated to
decomposition it emits toxic fumes of NOx
純化方法
Crystallise the dione from EtOH. Its pK2 3 is 4.52 (in H2O), 4.89 (in 50% aqueous EtOH) and 5.25 (80% 2-methoxyethanol). It complexes with Hg2+, Cd2+ and Zn2+. It has UV with max at 239.5nm in MeOH+50% aqueous HClO4 and 264nm in aqueous 0.1N NaOH. [Beilstein 24 III/IV 1123.]
フェニルブタゾン 上流と下流の製品情報
原材料
準備製品