FLUCAN 150 (Fluconazole USP)

FLUCAN 150 (Fluconazole USP)

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FLUCAN 150 (Fluconazole USP)

Fluconazole, bis-triazole anti-fungal, has increase in anti-fungal activity & expanded anti-fungal spectrum. Nitrogen of azole ring binds to haem of fungal CYP450 enzyme lanosterol leads abnormalities in membrane permeability & effective against strains of Candida, Cryptococcus neoformans, Blastomyces dermatitidis, Histoplasma capsulatum and Coccidioides immitis.

Pharmacokinetics

Oral bioavailability of Fluconazole is over 90%. Cmax is 1 to 2 hours with T1/2 of 30 hours. Steady state concentration within 5-10 days following oral 50-400mg once daily. Low plasma protein binding (11-12%). Approximately 80% renal excretion as unchanged drug. Pharmacokinetics is affected by reduction in renal function.

Indications

Vaginal & systemic candidiasis including candidaemia, disseminated candidiasis & other invasive candida infection including peritoneum, endocardium, pulmonary & urinary tracts. Tinea corporis, Tinea cruris, Tinea versicolor and dermal candida infections.

Mucosal Candidiasis including oropharyngeal, oesophageal, non-invasive bronchopulmonary infections, candiduria, mucocutaneous and chronic oral atrophic candidiasis.

Cryptococcosis including cryptococcal meningitis and infections of other sites. For prevention of fungal infections in patients at risk following cytotoxic chemotherapy or radiotherapy.

Contraindications

In patients with known hypersensitivity to Fluconazole and advanced liver disease.

Special precautions and warning

Monitor patient with abnormal liver function & Immuno-compromised. Not recommended in children below 16 years. Abnormalities of hepatic, renal, haematological and other biochemical function test have been observed during treatment with Fluconazole. AIDS patients may develop severe cutaneous reactions. In patients with invasive/systemic fungal infections who develop rashes, discontinue Fluconazole if bullous lesions or erythema multiforme develop.

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Pregnancy & lactation

Fluconazole should be used in pregnancy only if the benefits outweigh the risks. Since it is secreted in human milk, it should not be used in lactating women.

Dosage and administration

Vaginal candidiasis & Mucosal candidiasis: 1 tablet daily for 7-14 days

Orapharyngeal candidiasis: 1 tablet 7-14 days

Esophageal candidiasis: 1 tablet daily for 14-30 days

Systemic candidiasis: 3 tablets on first day, followed by 1 tablet daily

Dermatomycosis, Onychomycosis: 1 tablet weekly for 2-4 weeks

Adverse effects

Nausea, vomiting, abdominal pain, diarrhoea, headache and skin rash. Mild transient, reversible increase in liver enzymes. Rarely serious hepatotoxicity & anaphylaxis.

Drug interactions

Fluconazole prolongs prothrombin times of coumarin and phenytoin levels and AUC resulting in phenytoin toxicity. Concomitant administration of Fluconazole and cyclosporine may result in increase in cyclosporine levels. Concomitant administration of Fluconazole results in increased plasma concentration and reduced metabolism of anti-diabetic agents. Concomitant administration with rifampicin decreases AUC for Fluconazole by 20%.

Overdosage

Supportive measures and symptomatic treatment with gastric lavage may be adequate.

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