Fluconazole

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

Candican®, Marck
Candinil®, Healthcare
Candizole®, Regal
Criptocan®, Sphinx
Cytcan®, Coral
Diconazol®, Cosmos
Diflucan®, Pfizer
Eflicon®, Elys
FCN®, Intas
Fcozole®, Medicraft
Flucan®, Bombay
Flucaz®, Agio
Flucimet®, Metro
Flucon®, Nic
Fluconal®, Acme
Fluconazole®, Arrow
Fluconazole®, Shelys
Flugal®, Square
Flutrox®, Universal
Fluzon®, Cadila
Flunginazol®, Unicorn
GVfluc®, GVS
Fungistop®, Fourrts
Logican®, Medreich
Nocanz®, Flamingo
Odaft®, Plethico
Omastin®, Beximco
Pharmazole®, Pharmaniaga
Stabilanol®, Pharmathen
Syscan®, Torrent
Treflucan®, EIPICO
Triconal®, T3A
Ucozole®, Lab and Allied
Zilcan®, GSK
Zolocan®, Meyer
Zolstan®, Dr. Reddy
Zorcan®, Cipla

Indications

  • 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.

Contraindications

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 effects

Adverse drug reactions associated with fluconazole therapy include:

Drug Interactions

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.

Genital thrush:
150mg stat

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.