MOA : Fluconazole inhibits the fungal cytochrome P450 enzyme 14α-demethylase. Mammalian demethylase activity is much less sensitive to fluconazole than fungal demethylase. This inhibition prevents the conversion of lanosterol to ergosterol, an essential component of the fungal cytoplasmic membrane, and subsequent accumulation of 14α-methyl sterols. Fluconazole is primarily fungistatic; however, it may be fungicidal against certain organisms in a dose-dependent manner, specifically Cryptococcus.
Drug Label Information | Brands:
Brands of Fluconazole in Kenya
Ucozole®, Lab and Allied
Zolstan®, Dr. Reddy
- The treatment of non-systemic Candida infections of the vagina (“yeast infections”), throat, and mouth.
- Certain systemic Candida infections in people with healthy immune systems, including infections of the bloodstream, kidney, or joints. Other antifungals are usually preferred when the infection is in the heart or central nervous system, and for the treatment of active infections in people with weak immune systems.
- The prevention of Candida infections in people with weak immune systems, such as those neutropenic due to cancer chemotherapy, those with advanced HIV infections, transplant patients, and premature infants.
- As a second-line agent for the treatment of cryptococcal meningoencephalitis, a fungal infection of the central nervous system.
Fluconazole is contraindicated in patients who:
- have known hypersensitivity to other azole medicines such as ketoconazole;
- are taking terfenadine, if 400 mg per day multidose of fluconazole is administered;
- concomitant administration of fluconazole and quinidine, especially when fluconazole is administered in high dosages;
- take SSRIs such as fluoxetine or sertraline.
Adverse drug reactions associated with fluconazole therapy include:
- Common (≥1% of patients): rash, headache, dizziness, nausea, vomiting, abdominal pain, diarrhea, and/or elevated liver enzymes
- Infrequent (0.1–1% of patients): anorexia, fatigue, constipation
- Rare (<0.1% of patients): oliguria, hypokalaemia, paraesthesia, seizures, alopecia, Stevens–Johnson syndrome, thrombocytopenia, other blood dyscrasias, serious hepatotoxicity including liver failure, anaphylactic/anaphylactoid reactions
- Very rare: prolonged QT interval, torsades de pointes
Fluconazole reduces the metabolism of several drugs by inhibiting CYP3A, including benzodiazepines, calcium channel blockers, ciclosporin, docetaxel and, importantly, warfarin.
The plasma concentrations and toxicity of these drugs will increase during concomitant treatment with fluconazole.
Rifampicin enhances the metabolism of fluconazole.
DOSAGE AND ADMINISTRATION
cryptococcal meningitis: 400mg on the first day then 200mg to 400mg once daily for 6 to 8 weeks
To stop cryptococcal meningitis from coming back : 200mg once daily
Prevention of relapse following acute cryptococcal meningitis in AIDS patients : 100-200mg daily
Coccidioidomycosis : 200mg to 400mg once daily from 11 months for up to 24months
Internal fungal infections Caused by Candida: 800mg on the first day then 400mg once daily.
Mucosal infections affecting the lining of mouth,throat and denture sore mouth: 200mg to 400mg on the first day then 100mg to 200mg daily.
Mucosal thrush-dose depends on where the infection is located: 50mg to 400mg once daily for 7 to 30 days.
To stop mucosal infections affecting the liningof mouth throat:
100mg to 200mg once daily ,0r 200mg 3 times a week.
To reduce reccurence of vaginal thrush:
150mg every third day for a total of 3 doses (day 1,4 and 7) and then once a week for 6 months
Fungal skin and nail infections
50mg once daily,150mg once weekly,300mg to 400mg weeklyfor 1 to 4 weeks (Athlete’s foot 6 weeks,nails infection treatment may be longer)
Prevention of infections caused by Candida in Immunocomprimised patients:
200mg to 400mg once daily while you are at risk of getting an infection
Children to 11 years old
Mucosal thrush and throat infections caused by candida:
3mg per kg of body weight
Cryptococcal meningitis or internal fungal infecion caused by candida:
6mg to 12mg per kg of body weight
To stop children from getting an infection caused by Candida (immunocompromised)
Children 0 to 4 weeks of age
The same dosage as above but given once every 2 days.the maximum dose is 12mg per kg of body weight every 48 hours.
Children less than 2 weeks old:
The same dosage as above but given once every 3 days.the maximum dose is 12mg per kg of body weight every 72 hours.