Fluconazole Review Article |
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Fluconazole is used for the treatment of vaginal yeast infection due to candida. Basically it is an anti fungal antibiotic. It can be used for the treatment of any kind of fungus in any part of the body including mouth, throat, oesophagus, lungs, bladder, genital area and blood. It also helps to prevent fungal infection in people with weak immune systems caused by cancer treatment, bone marrow transplant or AIDS. It is recommended not to take this medication if allergic to fluconazole. It is mandatory to follow doctor’s instruction and the restriction on food and beverages. The usual dose for vaginal candidiasis is of 150 mg orally per day.
| Dosage |
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| 50 mg |
60 tab ($0.78 per tab) Manufactured in EU |
USD 47.00 |
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| 150 mg |
60 tab ($1.40 per tab) |
USD 84.00 |
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| 150 mg |
100 tab ($1.32 per tab) |
USD 132.00 |
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| 150 mg |
200 tab ($1.24 per tab) |
USD 247.00 |
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Indications:
Fluconazole is indicated for the treatment and prophylaxis of fungal infections where other antifungals have failed or are not tolerated (e.g. due to adverse effects), including:
Candidiasis caused by susceptible strains of Candida
Tinea corporis, tinea cruris or tinea pedis
Onychomycosis
Cryptococcal meningitis
Fluconazole can be used first-line for the following indications:[4]
Coccidioidomycosis
Cryptococcosis
Histoplasmosis
Prophylaxis of candidiasis in immunocompromised people
Dosage:
Dosage, varies with indication and between patient groups, ranging from: a two week course of 150 mg/day for vulvovaginal candidiasis, to 150¨C300 mg once weekly for resistant skin infections or some prophylactic indications. 500¨C600 mg/day may be used for systemic or severe infections, and in urgent infections such as meningitis caused by yeast 800 mg/day have been used. Pediatric doses are measured at 6-12 mg/kg/d . A loading dose will be indicated when entering a daily dosage schedule, for example a loading dose of 200 mg on the first day is commonly used with 150 mg/day following that.
Contraindications:
Fluconazole is contraindicated in patients with:
Known hypersensitivity to fluconazole or other azole antifungals
Concomitant use of cisapride, due to risk of serious cardiac arrhythmias (relative contraindication).
Pregnancy
Precautions:
Fluconazole therapy has been associated with QT interval prolongation, which may lead to serious cardiac arrhythmias. Thus it is used with caution in patients with risk factors for prolonged QT interval such as electrolyte imbalance or use of other drugs which may prolong the QT interval (particularly cisapride).
Fluconazole has also rarely been associated with severe or lethal hepatotoxicity and liver function tests are usually performed regularly during prolonged fluconazole therapy. Additionally, it is used with caution in patients with pre-existing liver disease.
High concentrations of fluconazole have been detected in human breast milk from patients receiving fluconazole therapy, thus its use is not recommended in breastfeeding mothers.[2]
Adverse effects:
Adverse drug reactions associated with fluconazole therapy include:
Common: rash, headache, dizziness, nausea, vomiting, abdominal pain, diarrhea, and/or elevated liver enzymes
Infrequent: anorexia, fatigue, constipation
Rare: oliguria, hypokalaemia, paraesthesia, seizures, alopecia, Stevens-Johnson syndrome, thrombocytopenia, other blood dyscrasias, serious hepatotoxicity including hepatic failure, anaphylactic/anaphylactoid reactions
Very rare: prolonged QT interval, torsades de pointes.
Mechanism of action:
Like other imidazole- and triazole-class antifungals, fluconazole inhibits the fungal cytochrome P450 enzyme 14¦Á-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 14¦Á-methyl sterols. Fluconazole is primarily fungistatic, however may be fungicidal against certain organisms in a dose-dependent manner. Interestingly, when fluconazole was in development at Pfizer it was decided early in the process to avoid producing any chiral centers in the drug so that subsequent synthesis and purification did not encounter difficulties with enantiomer separation and associated variations in biological effect. A number of related compounds were found to be extremely potent teratogens and subsequently discarded.
Fluconazole notes:
Commonly known by the trade names Diflucan or Trican (Pfizer), the generic fluconazole drug possess antifungal properties that makes it best to be used for the treatment and prevention of superficial and systemic fungal infections. Appearing as a white crystalline powder, this drug is somewhat soluble in water and alcohol. fluconazole fungal activity is indicated for the treatment and prophylaxis of fungal infections. They are prescribed for treating various conditions like Candidiasis due to susceptible strains of Candida, Onychomycosis, Tinea corporis, tinea cruris or tinea pedis, Cryptococcal meningitis etc. Fluconazole are also prescribed as the best medication for a number of other infections caused by Cryptococcosis, Coccidioidomycosis, Histoplasmosis along with prophylaxis of candidiasis in immuno deficient people.
The diflucan dosage varies with between patient groups and indications. The drug dosage ranges from a two week course of fluconazole 150 mg per day for vulvovaginal candidiasis to 150¨C300 mg once weekly for chronic skin infections or a few prophylactic symptoms. The trican dosage of 500¨C600 mg/day may be prescribed for systemic or severe infections along with infections that require urgent treatment including meningitis caused due to yeast for which 800 mg/day of dosage is directed. Pediatric doses are given at 6-12 mg/kg/d.
The functioning of this drug is similar to other antifungal drugs as fluconazole prevents the action of fungal cytochrome P450 enzyme 14¦Á-demethylase from causing infection. As a result of this inhibition, the conversion of lanosterol to ergosterol is prevented. lanosterol is an essential component of the fungal cytoplasmic membrane and consequent accumulation of 14¦Á-methyl sterols is prevented. However, Diflucan should be avoided by breastfeeding mothers as it can be excreted through the milk.
Diflucan side effects include: diarrhea, abdominal pain, rash, headache, fatigue, nausea, dizziness, vomiting, enzymesanorexia, constipation etc. Other rare symptoms include oliguria, alopecia, hypokalaemia, paraesthesia, seizures, Stevens-Johnson syndrome, thrombocytopenia, hepatotoxicity and so on.
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 Fluconazole Review Article
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