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Fluconazole

is a triazole antifungal drug used in the treatment and prevention of superficial and systemic fungal infections. In a bulk powder form, it appears as a white crystalline powder, and it is very slightly soluble in water and soluble in alcohol. It is commonly marketed under the trade name Diflucan  or Trican. In Mexico it is sold over the counter as Alfumet, Afungil or Dofil. It is marketed under the brand name Candivast in the Persian Gulf area.  It is ingested.

To quote “Like other imidazole- and triazole-class antifungals, 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.  A number of related compounds were found to be extremely potent teratogens, and were subsequently discarded”.

Fluconazole is used  against the following microorganisms:

• Blastomyces dermatitidis
• Candida spp. (except C. krusei and C. glabrata)
• Coccidioides immitis
• Cryptococcus neoformans
• Epidermophyton spp.
• Histoplasma capsulatum
• Microsporum spp.
• Trichophyton spp.

The instructions for it say “Please take note that this is NOT for anyone under the age of eighteen. This variety can cause many problems to the abdomen on a younger child”  There are also warnings not to take it if you are pregnant or breast feeding as “Fluconazole is secreted in human milk at concentrations similar to plasma”.

Side effects

• Heart failure - Fluconazole therapy has been associated with QT interval prolongation, which may lead to serious cardiac arrhythmias.

•  Liver damage - Fluconazole has been associated with severe or lethal hepatotoxicity and liver function tests are usually performed regularly during prolonged fluconazole therapy. “Notify your doctor immediately if you develop nausea, vomiting, abdominal pain, unusual fatigue, loss of appetite, yellow skin or eyes, itching, dark urine, or clay-colored stools”.

•  ‘Allergic reaction’ - Some people are 'allergic' to azole(s), so those allergic to other azole drugs might be allergic to fluconazole.  Severe allergic reaction like anaphylaxis has been reported, sometimes resulting in death.

• Foetus abnormalities -  Some azole drugs may disrupt estrogen production in pregnancy, affecting pregnancy outcome.  ‘Fluconazole/Diflucan has been associated with a rare and distinct set of birth defects in infants.

• Drug interactions - Fluconazole is an inhibitor of the human cytochrome P450 system, particularly the isozyme CYP2C9 (CYP3A4 to lesser extent). In theory, therefore, fluconazole decreases the metabolism and increases the concentration of any drug metabolised by these enzymes.

• Other -  anorexia, fatigue, constipation,  oliguria, hypokalaemia, paraesthesia, seizures, alopecia, Stevens-Johnson syndrome, thrombocytopenia, other blood dyscrasias,

Time on Fluconazole when people have Hallucination  :