Consumer medicine information

1 Name of Medicine

Fluconazole.

2 Qualitative and Quantitative Composition

Fluconazole-Baxter, Injection for Intravenous Infusion is a clear colourless infusion containing 2 mg/mL of fluconazole in 0.9% saline (sodium chloride dissolved in water for injection) solution. Each 100 mL of the solution contains 15.4 mmol of sodium. The pH of the solution is 4.0 - 8.0.
Each 50 mL vial of solution contains 100 mg of fluconazole, each 100 mL vial of solution contains 200 mg of fluconazole and each 200 mL vial of solution contains 400 mg of fluconazole. Vials are for single use only.

3 Pharmaceutical Form

Injection for intravenous infusion.

4 Clinical Particulars

4.9 Overdose

The minimal lethal human dose has been not established. There have been reports of overdosage with fluconazole, and in one case, a 42-year-old patient infected with human immunodeficiency virus developed hallucinations and exhibited paranoid behaviour after reportedly ingesting 8,200 mg of fluconazole. The patient was admitted to hospital, and his condition resolved within 48 hours.
Signs and symptoms are likely to be an extension of those under Section 4.8 Adverse Effects (Undesirable Effects).
There is no specific antidote. Treatment is symptomatic and supportive, including respiratory and cardiovascular function. Monitor for hypokalaemia and elevated liver enzymes; and obtain a full blood count to monitor for possible thrombocytopenia and agranulocytosis.
Fluconazole is largely excreted in the urine; forced volume diuresis would probably increase the elimination rate. A three-hour haemodialysis session decreases plasma levels by approximately 50%.
For information on the management of overdose, contact the Poisons Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.3 Preclinical Safety Data

Genotoxicity. Fluconazole, with or without metabolic activation, was negative in tests for mutagenicity in 4 strains of Salmonella typhimurium and in the mouse lymphoma system. Cytogenetic studies in vivo and in vitro showed no evidence of chromosomal mutations.
Carcinogenicity. Fluconazole showed no evidence of carcinogenic potential in mice and rats treated orally for 24 months at doses of 2.5 mg/kg/day, 5 mg/kg/day or 10 mg/kg/day (approximately 2-7-time recommended human dose). Male rats treated with 5 mg/kg/day and 10 mg/kg/day had an increased incidence of hepatocellular adenomas.

6 Pharmaceutical Particulars

6.7 Physicochemical Properties

Fluconazole is a white to off-white crystalline powder which is sparingly soluble in water and saline.
Chemical structure. The chemical formula is C₁₃H₁₂F₂N₆O and the molecular weight is 306.3.
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSFLUCON.gif Fluconazole is a bis-triazole, 2-(2,4-difluorophenyl)-1,3-bis(1H-1,2,4-triazol-1-yl)propan-2-ol.
CAS number. The CAS number is 86386-73-4.

7 Medicine Schedule (Poisons Standard)

S4 - Prescription only medicine.

Summary Table of Changes

https://stagingapi.mims.com/au/public/v2/images/fulltablegif/FLUBAXST.gif