FLUCYTOSINE

Synthetic fluorinated pyrimidine antimycotic with a narrow spectrum of antifungal activity. Mainly effective against Cryptococcus and Candida spp

Dosage Forms

Injection

10 mg/ml

Uses

  • Cryptococcal meningitis
  • Systemic candidiasis
  • Systemic yeast and fungal infections

Dose and Duration

Cryptococcal meningitis and systemic candidosis (in combination with Amphotericin B in severe cases)
Adult and child: by IV infusion over 20–40 minutes, 50 mg/kg every 6 hours for up to 7 days (at least 4 months in cryptococcal meningitis). In extremely sensitive organisms, use half dose

By mouth, 50–150 mg/kg daily in divided doses

Note: In renal impairment, increase dosing intervals
Moderate renal impairment: 50 mg/kg every 24 hours
Mild renal impairment: 50 mg/kg every 12 hours
Severe renal impairment: initially 50 mg/kg, then adjust subsequent doses based on serum concentration of flucytosine to maintain plasma levels of 20–50 micrograms/ml

Contraindications

  • Hypersensitivity to flucytosine
  • Co-administration with antiviral nucleoside drugs like brivudine, sorivudine

Side Effects

  • Nausea, vomiting, diarrhoea
  • Skin rashes
  • Alteration in liver function tests

Pregnancy

  • Do not use

Breast-feeding

  • Do not use

Storage

  • Store between 18ᵒC and 25ᵒC (see caution)

⚠️ Caution

  • Monitor trough plasma concentrations. Concentrations above 75 micrograms/ml are myelotoxic
  • Precipitation may occur when flucytosine is stored below 18ᵒC and decomposition to fluorouracil if stored at 25ᵒC for long periods
  • Use with caution in blood disorders and if amphotericin B is used concomitantly since both are nephrotoxic
  • Monitor liver, kidney function, and blood counts before treatment and thereafter weekly in prolonged therapy
  • Carry out sensitivity testing since resistance to flucytosine may develop during treatment