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Diflucan is an antifungal drug used in treating and preventing systemic and superficial fungal infections. It appears to be as a white crystalline powder and it is soluble in water and also soluble in alcohol.
This drug inhibits the fungal cytochrome P450 and this inhibition prevents the conversion of lanosterol to ergosterol. This drug is fungistatic and may be fungicidal against certain organisms in a dose dependent manner. When this drug was developed by Pfizer, to avoid producing any chiral centers in the drug so that synthesis and purification didn’t encounter hardship with enantiomer separation. The teratogenic compounds found on the drug were discarded.
This drug aims to combat the following microorganisms: Candida spp, Histoplasma capsulatum, Blastomyces dermatitidis, Cryptococcus neoformans, Epidermophyton spp., Trichophyton spp.
This drug is absorbed within 2 hours and bioavailability is not affected by the absence of gastric acid. It was found out that concentrations are measured in the urine, skin and tears 10 times the plasma concentration. Plasma concentration is approximately equal in saliva, vaginal fluid and sputum. The half-life of this drug is 10 % due to metabolism and the remaining are excreted in sweat and urine. Increase risk is found in patients with renal disorders and those patients taking warfarin.
The recommended dose varies between patient groups: ranging from a two week course of 150 mg/day in patient having vulvovaginal candidiasis and 150-300 mg once weekly for resistant skin infection. For pediatric patient, 6-12 mg/kg/d.
Taking this drug is contraindicated with patients having: hypersensitivity to azole medicine and concomitant use of cisapride. There have been reports that using this drug is associated with QT interval prolongation that might lead to serious cardiac arrhythmias. Patients with electrolyte imbalances should consult their physician before taking the said drug.
Taking this drug is also associated with hepatotoxicity and caution in patients with pre-existing liver disease and also not recommended in lactating women.