5-Fluorocytosine
Brand names,
5-Fluorocytosine
Analogs
5-Fluorocytosine
Brand Names Mixture
5-Fluorocytosine
Chemical_Formula
C4H4FN3O
5-Fluorocytosine
RX_link
http://www.rxlist.com/cgi/generic3/flucytosine.htm
5-Fluorocytosine
fda sheet
5-Fluorocytosine
msds (material safety sheet)
5-Fluorocytosine
Synthesis Reference
No information avaliable
5-Fluorocytosine
Molecular Weight
129.093 g/mol
5-Fluorocytosine
Melting Point
296 oC
5-Fluorocytosine
H2O Solubility
10.5 g/L
5-Fluorocytosine
State
Solid
5-Fluorocytosine
LogP
-0.062
5-Fluorocytosine
Dosage Forms
Capsule (250mg and 500mg)
5-Fluorocytosine
Indication
For the treatment (in combination with amphotericin B) of serious infections caused by susceptible strains of Candida (septicemia, endocarditis and urinary system infections) and/or Cryptococcus (meningitis and pulmonary infections).
5-Fluorocytosine
Pharmacology
Flucytosine is an antimetabolite that acts as an antifungal agent with in vitro and in vivo activity against Candida and Cryptococcus. Flucytosine enters the fungal cell via cytosine permease; thus, flucytosine is metabolized to 5-fluorouracil within fungal organisms. The 5-fluorouracil is extensively incorporated into fungal RNA and inhibits synthesis of both DNA and RNA. The result is unbalanced growth and death of the fungal organism. Antifungal synergism between Ancobon and polyene antibiotics, particularly amphotericin B, has been reported.
5-Fluorocytosine
Absorption
Rapidly and virtually completely absorbed following oral administration. Bioavailability 78% to 89%.
5-Fluorocytosine
side effects and Toxicity
Oral, rat: LD50 = >15 gm/kg.
5-Fluorocytosine
Patient Information
Bone marrow toxicity can cause anemia, leukopenia, pancytopenia, thrombocytopenia and, rarely, agranulocytosis and eosinophilia. Other side effects can be nausea, vomiting, anorexia, bloating, diarrhea, and, rarely, bowel perforation. Reversible elevations in liver enzymes have been reported. Occasionally, rashes may be a side effect. Some side effects that have only been seen very rarely are confusion, hallucinations, headaches, sedation, vertigo and liver enlargement.There has also been a case of severe allergic-type reaction to the drug in at least one person with AIDS. This type of reaction is called anaphylaxis.
5-Fluorocytosine
Organisms Affected
Yeast and other fungi