페닐부타존 C화학적 특성, 용도, 생산
개요
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.
화학적 성질
Off-Whtie Solid
용도
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.
World Health Organization (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withdrawn at the national level or retained with rigorously restricted indications for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.
일반 설명
Odorless white or off-white crystalline powder. Tasteless at first, but slightly bitter aftertaste. pH (aqueous solution) 8.2.
공기와 물의 반응
Phenylbutazone is relatively stable at ambient temperatures. Aqueous decomposition of Phenylbutazone occurs by hydrolysis and oxidation. Insoluble in water.
반응 프로필
Phenylbutazone is incompatible with strong oxidizers, strong acids and strong bases. .
화재위험
Flash point data for Phenylbutazone are not available; however, Phenylbutazone is probably combustible.
Safety Profile
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
Purification Methods
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.]
페닐부타존 준비 용품 및 원자재
원자재
준비 용품
