Class: Anti-infective, Antifungal
- Capsules 250 mg
- Capsules 500 mg
Exact mechanism is unknown; interferes with DNA and RNA synthesis. Active against Candida and Cryptococcus .
Bioavailability is 78% to 89%. C max is 30 to 40 mcg/mL; T max is 1 to 2 h.
The drug is 2.9% to 4% protein bound. It readily penetrates the blood-brain barrier achieving clinically significant concentrations in the CSF.
Primarily renally excreted via glomerular filtration. The t ½ is 2.4 to 4.8 h. More than 90% is excreted in the urine unchanged and about 1% in the urine as metabolite (α-fluoro-β-ureido-propionic acid).
Special PopulationsRenal Function Impairment
Prolonged t ½ (29.9 to 250 h in anuric or nephrectomized patients).
Indications and Usage
Treatment of serious infections caused by susceptible strains of Candida or Cryptococcus .
Dosage and AdministrationAdults
PO 50 to 150 mg/kg/day in divided doses every 6 h.
Drug InteractionsAmphotericin B
Increased therapeutic action and toxicity of flucytosine.Cytosine
Inactivates antifungal activity of flucytosine.
Laboratory Test Interactions
Interferes with creatinine value determinations with dry-slide enzymatic method (Kodak Ektachem analyzer); use Jaffe method.
Cardiac arrest, myocardial toxicity, ventricular dysfunction.
Ataxia, hearing loss, headache, sedation, confusion, fatigue, weakness, dizziness, vertigo, paresthesia, parkinsonism, peripheral neuropathy, pyrexia, hallucinations, psychosis, convulsions.
Rash, pruritus, urticaria, photosensitivity.
Nausea, emesis, abdominal pain, diarrhea, anorexia, duodenal ulcer, GI hemorrhage, dry mouth.
Azotemia, creatinine and BUN elevation, crystalluria, renal failure.
Anemia, agranulocytosis, aplastic anemia, eosinophilia, leukopenia, pancytopenia, thrombocytopenia.
Hepatic function impairment, jaundice, ulcerative colitis, increased bilirubin, elevated hepatic enzymes, acute hepatic injury.
Respiratory arrest, chest pain, dyspnea.
Use with extreme caution in patients with renal function impairment. Close monitoring of hematologic, renal, and hepatic function is essential.
Category C .
Safety and efficacy not established.
Adjust dose according to blood levels and monitor hepatic function.
Bone marrow depression
Use with extreme caution in patients with bone marrow depression or those at risk (eg, hematologic disease, radiation treatment, other bone marrow suppressant drugs).
Nausea, vomiting, diarrhea, CNS changes, leukopenia, thrombocytopenia, hepatitis.
- Advise patient to read patient information leaflet before starting therapy and with each refill.
- Review dosing schedule and prescribed length of therapy with patient. Advise patient that treatment may be prolonged (eg, several weeks or months) and to continue medication until advised to stop using by health care provider.
- Advise patient that medication may cause nausea and/or vomiting. Inform patient that these adverse reactions may be prevented or reduced in severity by taking flucytosine capsules a few at a time over a 15-min period.
- Advise patient that if a dose is missed to take as soon as remembered. However, if it is nearing the time for the next dose, to skip the dose and take the next dose at regularly scheduled time. Caution patient never to double the dose to catch up.
- Remind patient to complete entire course of therapy, even if symptoms of infection have disappeared.
- Advise patient to inform health care provider if infection does not appear to be improving or is getting worse.
- Advise patient to contact health care provider immediately if any of the following occur: fever, sore throat, or other signs of infection; bleeding or unusual bruising; skin rash; persistent nausea or vomiting; dark urine; yellowing of skin or eyes; changes in thinking; abnormal muscle movements or skin sensations.
- Caution patient that drug may cause drowsiness or dizziness and to use caution while driving or performing other tasks requiring mental alertness or coordination until tolerance is determined.
- Advise patient that medication may cause photosensitivity (sensitivity to sunlight) and to avoid unnecessary exposure to sunlight or tanning lamps and to use sunscreens and wear protective clothing until tolerance is determined.
Copyright © 2009 Wolters Kluwer Health.
More about flucytosine
- Other brands: Ancobon