플루코나졸
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플루코나졸 속성
- 녹는점
- 138-140°C
- 끓는 점
- 579.8±60.0 °C(Predicted)
- 밀도
- 1.05
- 인화점
- 9℃
- 저장 조건
- 2-8°C
- 용해도
- DMSO: 5mg/mL 에 용해됨
- 물리적 상태
- 고체
- 물리적 상태
- 단단한 모양
- 산도 계수 (pKa)
- pKa 1.76±0.1(H2O t=24 I=0.1(NaCl)) (Uncertain)
- 색상
- 흰색에서 황백색까지
- 수용성
- 1g/L(온도 미표시)
- Merck
- 14,4122
- BCS Class
- 1,3
- InChI
- InChI=1S/C13H12F2N6O/c14-10-1-2-11(12(15)3-10)13(22,4-20-8-16-6-18-20)5-21-9-17-7-19-21/h1-3,6-9,22H,4-5H2
- InChIKey
- RFHAOTPXVQNOHP-UHFFFAOYSA-N
- SMILES
- C1(C=CC(F)=CC=1F)C(O)(CN1N=CN=C1)CN1N=CN=C1
- CAS 데이터베이스
- 86386-73-4(CAS DataBase Reference)
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
위험품 표기 | Xn,Xi,T,F | ||
---|---|---|---|
위험 카페고리 넘버 | 22-36/37/38-20/21/22-39/23/24/25-23/24/25-11 | ||
안전지침서 | 26-36-36/37/39-24/25-45-36/37-16-7 | ||
유엔번호(UN No.) | UN1230 - class 3 - PG 2 - Methanol, solution | ||
WGK 독일 | 3 | ||
RTECS 번호 | XZ4810000 | ||
HS 번호 | 29336990 | ||
유해 물질 데이터 | 86386-73-4(Hazardous Substances Data) |
플루코나졸 C화학적 특성, 용도, 생산
개요
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.화학적 성질
Fluconazole-D4 is White to Off-White Solid용도
Labelled Fluconazole (F421000). Used as an antifungal.Indications
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.Antimicrobial activity
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.원료
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.일반 설명
Fluconazole is used to treat adult neutropenic patients with invasive candidiasis (IC).Pharmaceutical Applications
A synthetic bis(triazole) available for oral or parenteral administration. A prodrug formulation, fosfluconazole, is available for intravenous use in Japan.생물학적 활성
Triazole antifungal agent. Effective against Candida strains in vitro and in vivo .Pharmacokinetics
Oral absorption: >93%Cmax 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).
Pharmacology
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.Clinical Use
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.
부작용
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.플루코나졸 준비 용품 및 원자재
원자재
METHYL 2,4-DIFLUOROBENZOATE
Grignard reagent
1,2,4-트리아졸
에틸알코올
1-브로모-2,4-디플로로벤젠
메탄술폰산
비스 (클로로메틸) 케톤
사이클로헥세인
톨루엔
탄산 칼륨
tert-부틸알코올
디에틸에테르
M-페닐렌다이아민
이소프로필알코올
2,4 DIFLUOROBENZENE
디플르오르벤젠(1,3-)
염화알루미늄
클로로아세틸 클로라이드
트리메틸술폭소늄 아이오다이드
수산화칼륨
준비 용품
플루코나졸 공급 업체
글로벌( 1088)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Hebei Yanxi Chemical Co., Ltd. | +86-17531190177; +8617531190177 |
peter@yan-xi.com | China | 5873 | 58 |
Hebei Guanlang Biotechnology Co,.LTD | +8619930503252 |
daisy@crovellbio.com | China | 5828 | 58 |
Hebei Dangtong Import and export Co LTD | +8619831957301 |
admin@hbdangtong.com | China | 983 | 58 |
Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 |
info@fdachem.com | China | 20294 | 58 |
Sigma Audley | +86-18336680971 +86-18126314766 |
nova@sh-teruiop.com | China | 491 | 58 |
Shaanxi TNJONE Pharmaceutical Co., Ltd | +8618740459177 |
sarah@tnjone.com | China | 1143 | 58 |
HEBEI SHENGSUAN CHEMICAL INDUSTRY CO.,LTD | +8615383190639 |
admin@86-ss.com | China | 1000 | 58 |
Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 |
sales@capotchem.com | China | 29798 | 60 |
Shanghai Bojing Chemical Co.,Ltd. | +86-86-02137122233 +8613795318958 |
bj1@bj-chem.com | China | 299 | 55 |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21668 | 55 |
플루코나졸 관련 검색:
1-((비스(4-플루오로페닐)메틸실릴)메틸)-1H-1,2,4-트리아졸 벤질 알코올 과산화 벤조일 염화벤질 초산 벤질 1,1,1,3,3,3-헥사플루오로-2-프로판올 플루퀸코나졸 벤질벤조에이트 벤질 뷰틸산 플루오린(불소) 플루코나졸
1-PHENYL-2-PROPANOL
1-[[(2S,3S)-3-(2-Chlorophenyl)-2-(4-fluorophenyl)oxiran-2-yl]methyl]-1,2,4-triazole
beta-Methylphenethyl alcohol
1-METHYL-1,2,4-TRIAZOLE
Trimethylsulfoxonium iodide
2-(2-fluorophenyl)-1,3-di(1H-1,2,4-triazol-1-yl)propan-2-ol
Faropenem sodium