FLURBI프로FEN C화학적 특성, 용도, 생산
개요
Flurbiprofen synthesis was originally reported in 1974. During a study of the pharmacological
properties of a large number of substituted phenylalkanoic acids, including ibuprofen and ibufenac, the most potent
were found to be substituted 2-(4-biphenyl)propionic acids. Further toxicological and pharmacological studies
indicated that flurbiprofen possessed the most favorable therapeutic profile, so it was selected for further clinical
development. It was not marketed until 1987, when it was introduced as the sodium salt as Ocufen, the first topical
NSAID indicated for ophthalmic use in the United States. The indication for Ocufen is the same as that for
Profenal—that is, to inhibit intraoperative miosis induced by prostaglandins in cataract surgery.
화학적 성질
White to Off-White Crystalline Solid
용도
An anti-inflammatory used as an analgesic.
Indications
Flurbiprofen (Ansaid) is indicated for the treatment
of rheumatoid arthritis and osteoarthritis. Its half-life,
longer than that of many of the NSAIDs, allows for
twice daily dosing.The most common adverse effects of
flurbiprofen are similar to those of the other acidic
NSAIDs. Flurbiprofen inhibits both COX isoforms
about equally.
일반 설명
Flurbiprofen (Ansaid, Ocufen, Froben), is another drug inthis class indicated for both acute and long-term managementof RA and OA but with a more complex mechanism ofaction. Unlike the other drugs in this class, it does not undergochiral inversion (i.e., the conversion of the “inactive”[R]-enantiomer to the active, [S]-enantiomer). Similar to aspirinand other salicylates, both flurbiprofen enantiomersblock COX-2 induction as well as inhibiting the nuclearfactor-κB-mediated polymorphonuclear leukocyte apoptosissignaling; therefore, both enantiomers are believed to contributeequally to its overall anti-inflammatory action.
(R)-flurbiprofen is actually a strong clinical candidate forthe treatment of Alzheimer disease, because it has beenshown to reduce Aβ42 production by human cells.
생물학적 활성
Potent inhibitor of cyclooxygenase (IC 50 values are 0.1 and 0.4 μ M for inhibition of human COX-1 and COX-2 respectively). Analgesic, anti-inflammatory and antipyretic in vivo . Inhibits tumor cell growth in vitro and in vivo . Also inhibits fibroblast proliferation in vitro .
Pharmacokinetics
Flurbiprofen is well absorbed after oral administration, with peak plasma levels being attained within 1.5 hours. Food
alters the rate of absorption but not the extent of its bioavailability. It is extensively bound to plasma proteins (99%).and has a plasma half-life of 2 to 4 hours. Metabolism is extensive, with 60 to 70% of flurbiprofen and its metabolites
being excreted as sulfate and glucuronide conjugates. Flurbiprofen shows some interesting metabolic patterns, with
40 to 47% as the 4′-hydroxy metabolite, 5% as the 3′,4′-dihydroxy metabolite, 20 to 30% as the 3′-hydroxy-
4′-methoxy metabolite, and the remaining 20 to 25% of the drug being excreted unchanged. None of these
metabolites demonstrates significant anti-inflammatory activity.
Clinical Use
Flurbiprofen is indicated as an oral formulation for the acute or long-term treatment of rheumatoid arthritis and
osteoarthritis and as an ophthalmic solution for the inhibition of intraoperative miosis.
FLURBI프로FEN 준비 용품 및 원자재
원자재
준비 용품
