Кетопрофен химические свойства, назначение, производство
Химические свойства
White Crystalline Solid
Использование
Ketoprofen, a propionic acid derivative, is a nonsteroidal anti-inflammatory agent (NSAIA) with analgesic and antipyretic properties.
Определение
ChEBI: An oxo monocarboxylic acid that consists of propionic acid substituted by a 3-benzoylphenyl group at position 2.
Показания
Ketoprofen (Orudis) is indicated for use in rheumatoid
and osteoarthritis, for mild to moderate pain, and in
dysmenorrhea. The most frequently reported side effects
are GI (dyspepsia, nausea, abdominal pain, diarrhea,
constipation, and flatulence) and CNS related
(headache, excitation). Edema and increased blood urea nitrogen have also been noted in more than 3% of
patients. Ketoprofen can cause fluid retention and increases
in plasma creatinine, particularly in the elderly
and in patients taking diuretics.
Общее описание
Ketoprofen (Orudis, Rhodis) and suprofen (Profenal) areclosely related to fenoprofen in their structures, properties,and indications. Even though ketoprofen has been approvedfor OTC use (Orudis KT, Actron), its GI side effects aresimilar to indomethacin, and therefore its useshould be closely monitored, especially in patients with GIor renal problems.
Контактные аллергены
Ketoprofen is an anti-inflammatory drug, used both
topically and systemically. It is above all a photoaller-
gen, responsible for photoallergic or photo-worsened
contact dermatitis, with sun-induced, progressive,
severe, and durable reactions. Recurrent photosensitiv-
ity is possible for many years. Photosensitivities are
expected to thiophene-phenylketone derivatives such
as tiaprofenic acid and suprofen, to ketoprofen esters
such as piketoprofen, and to benzophenone derivatives
(see above) such as fenofibrate and benzophenone-3.
Concomitant photosensitivities without clinical rel-
evance have been observed to fenticlor, tetrachloro-
salicylanilide, triclosan, tribromsalan, and bithionol.
Фармакокине?тика
Ketoprofen is rapidly and nearly completely absorbed on oral administration, reaching peak plasma levels within 0.5
to 2 hours. It is highly plasma protein bound (99%) despite a lower acidity (pKa = 5.9) than some other NSAIDs. Wide
variation in plasma half-lives has been reported. It is metabolized by glucuronidation of the carboxylic acid, CYP3A4
and CYP2C9 hydroxylation of the benzoyl ring, and reduction of the keto function.
Клиническое использование
Ketoprofen, unlike many NSAIDs, inhibits the synthesis of leukotrienes and leukocyte
migration into inflamed joints in addition to inhibiting the biosynthesis of prostaglandins. It stabilizes the lysosomal
membrane during inflammation, resulting in decreased tissue destruction. Antibradykinin activity also has been
observed. Bradykinin is released during inflammation and can activate peripheral pain receptors. In addition to
anti-inflammatory activity, ketoprofen also possesses antipyretic and analgetic properties. Although it is less potent
than indomethacin as an anti-inflammatory agent and an analgetic, its ability to produce gastric lesions is about the
same.
Профиль безопасности
Poison by ingestion,subcutaneous, intravenous, rectal, and intraperitoneal routes. Human systemic effects by an unspecified route:headache, nausea or vomiting, and degenerative changesin the brain, changes in kidney tubules. An experimentalteratogen.
Кетопрофен препаратная продукция и сырье
сырьё
препарат