(1997; 132 pages) [French] [Spanish]
Capsule or tablet, 50 mg, 100 mg, 150 mg, 200 mg
Powder for oral suspension, 10 mg or 40 mg in 25-ml bottle
Fluconazole is a triazole derivative with a broad spectrum of antifungal activity. It is well absorbed and passes readily across the blood-brain barrier into the cerebrospinal fluid. The plasma half-life is about 30 hours. It is slowly eliminated unchanged in the urine.
Fluconazole is currently expensive, which may limit its availability.
• resistant oropharyngeal candidosis in patients with HIV infection
• vaginal candidosis
• cryptococcal meningitis1
• serious systemic candidal infections, in particular of the urinary tract, peritoneum and lungs, with skin involvement.
1 For further information, see WHO model prescribing information: drugs used in sexually transmitted diseases and HIV infection. Geneva, World Health Organization, 1995.
Dosage and administration
Resistant oropharyngeal candidosis:
200 mg as an initial loading dose, followed by 100 mg daily for 21 days.
400 mg as an initial loading dose, followed by 200 mg daily for at least 4 weeks.
150 mg as a single oral dose.
3-6 mg/kg as an initial loading dose, followed by 3 mg/kg daily for up to 4 weeks.
Hypersensitivity to azole derivatives.
Dosage should be reduced in accordance with the creatinine clearance rate in patients with renal impairment.
Hepatic function should be monitored when treatment is prolonged.
Women of child-bearing age should take effective contraceptive precautions during treatment and for several weeks thereafter. Anaphylaxis occurs rarely.
Use in pregnancy and lactation
Fluconazole has been shown to have teratogenic potential when given in high doses to experimental animals. The need for treatment must be determined by the condition of the mother. Breast-feeding should be interrupted during treatment.
Fluconazole is generally well tolerated. Nausea is the most frequently reported adverse effect. Vomiting and abdominal distension and discomfort have also been reported.
Elevation of hepatic enzyme levels, which occurs in a small percentage of individuals, is readily reversible in the early stages. Treatment should be discontinued if signs develop that are suggestive of hepatic disease.
Fluconazole should be withdrawn if skin rashes progress during treatment. Exfoliative skin disorders have been reported, but a causal association has not been established.
Anaphylaxis occurs rarely.
The hepatic metabolism of other lipid-soluble drugs, such as ciclosporin, phenytoin, sulfonylureas, theophylline and warfarin, is inhibited.
Rifampicin accelerates the clearance of fluconazole.
Concomitant administration of terfenadine should be avoided since it has been associated with serious, sometimes fatal, cardiac dysrhythmias.
No experience has been gained with overdosage of fluconazole. Induction of emesis and gastric lavage may be tried in the case of accidental overdosage.
Fluconazole capsules, tablets and powder for oral suspension should be kept in well-closed containers, protected from light. After reconstitution the oral suspension is stable for up to 14 days below 30 °C.