フルコナゾール 化學(xué)特性,用途語(yǔ),生産方法
外観
白色?ほとんど白色, 結(jié)晶?粉末
溶解性
エタノールにやや溶けやすく、水に溶けにくい。
用途
トリアゾール系抗真菌剤です。
真菌細(xì)胞において、膜成分のエルゴステロー
ル生合成の抑制作用を示します。
用途
薬理?生理作用研究用。
用途
in vitro 及びin vivo においてカンジダ菌に対し強(qiáng)力な作用を示します。トリアゾール系抗真菌
薬作用を示します。
用途
in vitro 及びin vivo においてカンジダ屬に対し強(qiáng)力な作用を示します。トリアゾール系抗真菌
薬作用を示します。
用途
フルコナゾールは、深在性真菌癥に用いられるアゾール系の抗真菌薬。日本では、ファイザーがジフルカンとして販売しているほか、いくつかの後発醫(yī)薬品が販売されている。剤形には、カプセル剤、ドライシロップ、注射液がある。
カンジダ屬およびクリプトコッカス屬による 真菌血癥、呼吸器真菌癥、消化管真菌癥、尿路真菌癥、真菌髄膜炎。造血幹細(xì)胞移植患者における深在性真菌癥の予防。カンジダ屬に起因する腟炎および外陰腟炎（カプセル剤のみ）。
用途
トリアゾール系抗真菌剤です。
真菌細(xì)胞において、膜成分のエルゴステロー
ル生合成抑制作用を示します。
効能
抗真菌薬, エルゴステロール合成阻害薬
商品名
ジフルカン (ファイザー); ジフルカン (ファイザー); ジフルカン (ファイザー)
説明
Fluconazole-D4 is the f i t member of a new generation of stable and orally active antifungals, the triazoles. It is highly effective in the treatment of dermal and vaginal fungal infections; new indications currently under investigation include severe systemic mycoses such as disseminated candidiasis and cryptococcal meningitis in immunocompromised patients.
化學(xué)的特性
Fluconazole-D4 is White to Off-White Solid
使用
Labelled Fluconazole (F421000). Used as an antifungal.
適応癥
Fluconazole (Diflucan) may be better absorbed and is
possibly less hepatotoxic than ketoconazole, but it is
considerably more expensive, an important consideration
given the required length of therapy for most cutaneous
fungal diseases.
抗菌性
The spectrum is limited, but includes most Candida spp.,
Cryptococcus spp., dermatophytes and dimorphic fungi (Blast.
dermatitidis, Coccidioides spp., Hist. capsulatum and Paracoccidioides
brasiliensis). Strains of C. krusei appear to be insensitive.
獲得抵抗性
Resistant strains of C. albicans have been isolated from AIDS
patients given long-term treatment for oral or esophageal
candidosis. Strains of C. glabrata frequently become resistant
during short courses of treatment. There are a few reports
of fluconazole-resistant strains of Cryp. neoformans recovered
from AIDS patients with relapsed meningitis. Most, but not
all, C. albicans and C. glabrata strains resistant to fluconazole
are cross-resistant to other azoles.
一般的な説明
Fluconazole is used to treat adult neutropenic patients with invasive candidiasis (IC).
応用例（製薬）
A synthetic bis(triazole) available for oral or parenteral administration.
A prodrug formulation, fosfluconazole, is available
for intravenous use in Japan.
生物活性
Triazole antifungal agent. Effective against Candida strains in vitro and in vivo .
薬物動(dòng)態(tài)學(xué)
Oral absorption: >93%
C
max 50 mg oral: c. 1 mg/L after 2 h
Plasma half-life: 25–30 h
Volume of distribution: 0.6–0.8 L/kg
Plasma protein binding; <10%
Absorption
Oral absorption is rapid (1–3 h) and is not affected by food or intragastric pH. Blood concentrations increase in proportion to dosage. Maximum serum concentrations increase to about 2–3 mg/L after repeated dosing with 50 mg.
Distribution
It is widely distributed, achieving therapeutic concentrations in most tissues and body fluids. Concentrations in cerebrospinal fluid (CSF) are 50–60% of the simultaneous serum concentration in normal individuals and even higher in patients with meningitis.
Metabolism and excretion
More than 90% of an oral dose is eliminated in the urine: about 80% as unchanged drug and 10% as inactive metabolites. The drug is cleared by glomerular filtration, but there is significant tubular reabsorption. The plasma half-life is prolonged in renal failure, necessitating adjustment of the dosage.Fluconazole-D4 is removed during hemodialysis and, to a lesser extent, during peritoneal dialysis. In children the volume of distribution and plasma clearance are increased, and the half-life is considerably shorter (15–25 h).
薬理學(xué)
It has good oral absorption,
is well tolerated, and is preferentially taken up in keratinized tissues, reaching
concentrations up to 50 times that in plasma. This allows for once-weekly
dosing in most cases.
臨床応用
Fluconazole is very effective in the treatment of infections
with most Candida spp. Thrush in the end-stage
AIDS patient, often refractory to nystatin, clotrimazole,
and ketoconazole, can usually be suppressed with oral
fluconazole.AIDS patients with esophageal candidiasis
also usually respond to fluconazole.
Fluconazole may be an acceptable alternative to
amphotericin B in the initial treatment of mild cryptococcal
meningitis, and it has been shown to be superior
to amphotericin B in the long-term prevention of relapsing
meningitis (such patients require lifelong treatment.).
Coccidioidal meningitis, previously treated with
both intravenous and intrathecal amphotericin B, appears
to respond at least as well to prolonged oral fluconazole
therapy. Aspergillosis, mucormycosis, and
pseudallescheriasis do not respond to fluconazole treatment.
Sporotrichosis, histoplasmosis, and blastomycosis
appear to be better treated with itraconazole, although
fluconazole does appear to have significant activity
against these dimorphic fungi.
副作用
Fluconazole is well tolerated. Nausea, vomiting, abdominal
pain, diarrhea, and skin rash have been reported in
fewer than 3% of patients. Asymptomatic liver enzyme
elevation has been described, and several cases of drugassociated
hepatic necrosis have been reported. Alopecia
has been reported as a common adverse event in
patients receiving prolonged high-dose therapy. Coadministration
of fluconazole with phenytoin results in increased
serum phenytoin levels.
フルコナゾール 上流と下流の製品情報(bào)
原材料
準(zhǔn)備製品