Flucytosin Produkt Beschreibung

Fluorocytosine Struktur
2022-85-7
  • CAS-Nr.2022-85-7
  • Bezeichnung:Flucytosin
  • Englisch Name:Fluorocytosine
  • Synonyma:Flucytosin
    5-FC;ancobon;ancotil;ALCOBON;ro2-9915;FLUCYSTINE;FLUCYTOSIN;FLUCYTOSINE;fluocytosine;Flurocytosine
  • CBNumber:CB6744939
  • Summenformel:C4H4FN3O
  • Molgewicht:129.09
  • MOL-Datei:2022-85-7.mol
Flucytosin physikalisch-chemischer Eigenschaften
  • Schmelzpunkt: :298-300 °C (dec.)(lit.)
  • Dichte :1.3990 (estimate)
  • storage temp.  :2-8°C
  • Löslichkeit :Sparingly soluble in water, slightly soluble in ethanol (96 per cent)
  • Aggregatzustand :Crystalline Powder
  • pka :3.26(at 25℃)
  • Farbe :White to almost white
  • Wasserlöslichkeit :1.5g/100mL (25 ºC)
  • Sensitive  :Light Sensitive
  • Merck  :14,4125
  • BRN  :127285
  • Stabilität: :Light Sensitive
  • InChIKey :XRECTZIEBJDKEO-UHFFFAOYSA-N
  • CAS Datenbank :2022-85-7(CAS DataBase Reference)
Sicherheit

Fluorocytosine Chemische Eigenschaften,Einsatz,Produktion Methoden

  • R-Sätze Betriebsanweisung: R40:Verdacht auf krebserzeugende Wirkung.
    R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
  • S-Sätze Betriebsanweisung: S22:Staub nicht einatmen.
    S24/25:Berührung mit den Augen und der Haut vermeiden.
    S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
    S36/37:Bei der Arbeit geeignete Schutzhandschuhe und Schutzkleidung tragen.
    S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
    S27:Beschmutzte, getränkte Kleidung sofort ausziehen.
    S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
  • Chemische Eigenschaften White Crystalline Solid
  • Verwenden antidiabetic
  • Verwenden antifungal and antimicrobial agent
  • Verwenden 5-FC is a toxic antifungal/antimicrobial agent
  • Definition ChEBI: An organofluorine compound that is cytosine that is substituted at position 5 by a fluorine. A prodrug for the antifungal 5-fluorouracil, it is used for the treatment of systemic fungal infections.
  • Trademarks Ancobon (Valeant).
  • Antimicrobial activity The spectrum of activity is restricted to Candida spp., Cryptococcus spp. and some fungi causing chromoblastomycosis.
  • Acquired resistance About 2–3 of Candida spp. isolates (more in some centers) are resistant before treatment starts, and resistance may develop during treatment. The most common cause of resistance appears to be loss of the enzyme uridine monophosphate pyrophosphorylase.
  • Pharmazeutische Anwendungen A synthetic fluorinated pyrimidine available for intravenous infusion or oral administration.
  • Mechanism of action Flucytosine (5-flucytosine, 5-FC; Ancoban) is a fluorinated pyrimidine analogue of cytosine that was originally synthesized for possible use as an antineoplastic agent. 5-FC is converted to 5-fluorouracil inside the cell by the fungal enzyme cytosine deaminase. Subsequently, 5-FC metabolites interfere with fungal DNA synthesis by inhibiting thymidylate synthetase. Incorporation of these metabolites into fungal RNA may inhibit protein synthesis.
  • Pharmakokinetik Oral absorption: Complete
    Cmax 25 mg/kg 6-hourly oral: 70–80 mg/L after 1–2 h
    Plasma half-life: 3–6 h
    Volume of distribution: 0.7–1 L/kg
    Plasma protein binding c. 12%
    Absorption is slower in persons with impaired renal function, but peak concentrations are higher. Levels in the CSF are around 75% of the simultaneous serum concentration. More than 90% of a dose of flucytosine is excreted in the urine in unchanged form. The serum half-life is much longer in renal failure, necessitating modification of the dosage regimen: for patients with a creatinine clearance below 40 mL/ min the dosage interval should be doubled to 12 h; in severe renal failure the dosage interval should be further increased to once daily or less, based on frequent serum drug concentration measurements.
  • Pharmakologie 5-FC is well absorbed orally, with greater than 90% bioavailability. The serum half-life is 3 to 5 hours, with serum levels peaking 4 to 6 hours after a single dose.The drug is widely distributed in body fluids, with cerebrospinal fluid levels 60 to 80% of serum levels.The drug also penetrates well into urine, aqueous humor, and bronchial secretions.Minimal serum protein binding allows more than 90% of each dose to be excreted in the urine; significant dosage reductions are required in the presence of renal impairment. 5-FC can be removed by both hemodialysis and peritoneal dialysis. 5-FC conversion to toxic metabolites may occur in mammalian cells to a limited extent, which accounts for 5-FC toxicity.
  • Clinical Use Candidosis (in combination with amphotericin B or fluconazole)
    Cryptococcosis (in combination with amphotericin B or fluconazole)
    Monitoring of flucytosine concentrations is desirable in all patients, and mandatory in those with renal impairment.
  • Clinical Use 5-Fluorocytosine, 5-FC, 4-amino-5-fluoro-2(1H)-pyrimidinone, 2-hydroxy-4-amino-5-fluoropyrimidine (Ancobon). 5-Fluorocytosine is an orally active antifungal agent with a very narrow spectrum of activity. It is indicated only for the treatment of serious systemic infections caused by susceptible strains of Candida and Cryptococcus spp.The mechanism of action of 5-fluorocytosine (5-FC)has been studied in detail.The drug enters the fungal cell by active transport onATPases that normally transport pyrimidines. Once insidethe cell, 5-fluorocytosine is deaminated in a reaction catalyzedby cytosine deaminase to yield 5-fluorouracil(5-FU). 5-Fluorouracil is the active metabolite of the drug.5-Fluorouracil enters into pathways of both ribonucleotideand deoxyribonucleotide synthesis. The fluororibonucleotidetriphosphates are incorporated into RNA, causingfaulty RNA synthesis. This pathway causes cell death. Inthe deoxyribonucleotide series, 5-fluorodeoxyuridinemonophosphate (F-dUMP) binds to 5,10-methylenetetrahydrofolicacid, interrupting the one-carbon pool substratethat feeds thymidylate synthesis. Hence, DNA synthesisis blocked.
  • Clinical Use Flucytosine has significant antifungal activity against C. albicans, other Candida spp., C. neoformans, and the fungal organisms responsible for chromomycosis. Not considered the drug of choice for these fungal infections, 5-FC does remain useful as part of combination therapy for systemic candidiasis and cryptococcal meningitis and as an alternative drug for chromomycosis. When it is used as monotherapy, resistance and clinical failure are common. Potential mechanisms for drug resistance include decreased fungal cell membrane permeability and reduced levels of fungal cytosine deaminase. Combination therapy with amphotericin B and flucytosine in the treatment of cryptococcal meningitis and deep-seated Candida infections, such as septic arthritis and meningitis, permits reduced dosing of amphotericin B and prevents the emergence of 5-FC resistance. When higher doses of amphotericin B are used, combination therapy with 5-FC confers no additional clinical benefit except in the treatment of Candida endophthalmitis, where tissue penetration remains problematic.
  • Nebenwirkungen When 5-FC is prescribed alone to patients with normal renal function, skin rash, epigastric distress, diarrhea, and liver enzyme elevations can occur.When it is prescribed to patients with renal insufficiency or to patients receiving concurrent amphotericin B therapy, blood levels of 5-FC may rise, and bone marrow toxicity leading to leukopenia and thrombocytopenia is common. 5-FC serum levels should be closely monitored in patients with renal insufficiency. Because of baseline leukopenia, 5-FC is often not tolerated by end-stage HIVinfected patients with disseminated fungal infection.
  • Nebenwirkungen Nausea, vomiting, abdominal pain and diarrhea are common. Serious side effects include myelosuppression and hepatic toxicity; they occur more frequently when serum concentrations exceed 100 mg/L.
    The nephrotoxic effects of amphotericin B can result in elevated blood concentrations of flucytosine, and levels of the latter drug should be monitored when these compounds are administered together.
Fluorocytosine Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Flucytosin Anbieter Lieferant Produzent Hersteller Vertrieb Händler.
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2022-85-7, Fluorocytosine Verwandte Suche:
  • 4-amino-5-fluoro-2(1h)-pyrimidinon
  • 4-Amino-5-fluoro-2(1H)-pyrmidinone
  • 5-fluorocystosine
  • 5-fluorocytosin
  • 5-fluoro-cytosin
  • fluocytosine
  • 4-Amino-5-Fluoro-2(1H)-pyrimidine, Flucytosine, 5-FC
  • 5-Fluorocytosine98%
  • 5-FLUOROCYTOSINE(FLUCYTOSINE)
  • FLUCYTOSINE (5-FLUOROCYTOSINE)
  • 5-FLUOROCYTOSINE USP/BP
  • 6-Amino-5-fluoro-1H-pyrimidin-2-one
  • 5-FLUOROCYTOSINE extrapure
  • Flurocytosine
  • 4-amino-5-fluoro-2(1H)-pyrimidinone, Flucytosine
  • 2(1H)-Pyrimidinone, 6-amino-5-fluoro-
  • 5-Fluorocytosine,4-amino-5-fluoro-2(1H)-pyrimidinone, Flucytosine
  • Flucytosine (200 mg)G0E1511.000mg/mg(dr)
  • 5-FC,RO 2-9915
  • 4-Amino-5-fluoropyrimidin-2(1H)-one, 4-Amino-1,2-dihydro-5-fluoro-2-oxopyrimidine
  • ro2-9915
  • TIMTEC-BB SBB000061
  • FLUCYSTINE
  • FLUCYTOSIN
  • FLUCYTOSINE
  • fluorocytosine
  • 2-hydroxy-4-amino-5-fluoropyrimidine
  • 5-FLUOROCYTOSINE
  • 5-FLUCYTOSINE
  • 5-FC
  • ancobon
  • ancotil
  • ALCOBON
  • 4-AMINO-5-FLUORO-2(1H)-PYRIMIDINE
  • 4-amino-5-fluoro-2(1h)-pyrimidinone
  • 4-AMINO-5-FLUORO-2-HYDROXYPYRIMIDINE
  • 4-AMINO-5-FLUORO-3H-PYRIMIDIN-2-ONE
  • 5-Flurocytosine
  • 4-amino-5-fluoropyrimidin-2(1H)-one
  • 5-FLUOR-CYTOSIN
  • 5-FLUROCYTOSINE/FLUCYTOSINE
  • FlucytosineTablets
  • 2(1H)-Pyrimidinone, 4-amino-5-fluoro- (9CI)
  • 4-Amino-5-fluoro-2[1H]-pyrimidone
  • 5-Fluorocytosine, 99+%
  • Flucytosine (200 mg)
  • 4-aMino-1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxyMethyl)oxolan-2-yl]-5-fluoro-1,2-dihydropyriMidin-2-one
  • NSC 103805 6-AMino-5-fluoro-
  • 4-Amino-5-fluoro-2-hydroxypyrimidine Flucytosine
  • 6-AMino-2-oxo-5-fluoropyriMidine
  • 5-Fluorocytosine USP/EP
  • 5 - fluorine cytosine
  • 6-amino-5-fluoro-2(1H)-pyrimidinone
  • Flucytosine for system suitability
  • 5-Fluorocytosine Vetec(TM) reagent grade, 99%
  • 4-amino-5-fluoropyrimidin-2-ol
  • 4-Amino-5-fluoro-2-hydroxypyrimidine 4-amino-5-fluoro-2(1H)-pyrimidinone Flucytosine
  • 2022-85-7