Description
Generic
Fluconazole
Indication
Fluconazole is indicated in the treatment of acute or recurrent vaginalcandidiasis,mucosal candidiasis (as oropharyngeal candidiasis,oesophagitis,candiduria), systemic candidiasis and cryptococcal infections (including meningitis).
Pharmacology
Fluconazole is a triazole antifungal drug which acts by inhibition of the ergosterol component of the fungal cell membrane. It is active against abroad spectrum of fungal pathogens and is available for oral use.Following oral administration, absorption is rapid and extensive (>90%).Bioavailability is the same in the fasting and fed states.The bioavailability of Fluconazole is unaffected by gastric pH. The plasma half-life is approximately 30h. The plasma protein binding of Fluconazole is low, at 11% and the drug is widely distributed throughout the body.Most of the dose of Fluconazole is excreted unchanged in the urine, the reminder of the dose being eliminated in the urine as metabolites.
Dosage & Administration
Adults
Since oral absorption is rapid and almost complete, the daily dose of Fluconazole is the same for oral and intravenous administration.
Oropharyngeal Candidiasis: The recommended dosage of Fluconazole for oropharyngeal candidiasis is 200 mg on the first day, followed by 100 mg once daily for 7-14 days.
Esophageal Candidiasis:The recommended dosage of Fluconazole for esophageal candidiasisis 200 mg on the first day,followed by 100 mg once daily for 2-3 weeks.
Systemic Candidiasis and Cryptococcal Meningitis: 400 mg daily followed by 200 mg once daily.The recommended duration of treatment for initial therapy of cryptococcal meningitisis 10 to 12 weeks.
Acute or recurrent vaginal candidiasis: Single dose of 150 mg.
Urinary Tract Infections and Peritonitis: 50 to 200 mg once daily.
Prophylaxis in Patients Undergoing Bone Marrow Transplantation: 400 mg once daily.
Children
Oropharyngeal Candidiasis: The recommended dosage of Fluconazole for oropharyngeal candidiasis in children is 6 mg/kg on the first day, followed by 3 mg/kg once daily. Treatment should be administered for at least 2 weeks to decrease the likelihood of relapse. Esophageal
Candidiasis: Recommended dosage of Fluconazole in children is 6 mg/kg on the first day,followed by 3 mg/kg once daily.
Cryptococcal meningitis:Initial therapy should be started with 6 to 12 mg/kg daily.Doses up to 12 mg/kg/day may be used for three weeks and treatment for initial therapy of cryptococcal meningitisis 10 to 12 weeks.
Interaction
Concomitant utilize of cyclosporin or phenytoin with Fluconazole increments the plasma level of cyclosporin or phenytoin. Concomitant utilize of Fluconazole & warfarin draws out the prothrombin time. Rifampicin level is diminished when utilized with Fluconazole.
Contraindications
Fluconazole is contraindicated to patients hypersensitive to this drug and in advanced liver disease.
Side Effects
Nausea, abdominal discomfort, diarrhoea and flatulence, occasionallyabnormalities of liver enzymes; rarely rash; angioedema and anaphylaxis reported.
Pregnancy and Lactation
US FDA Pregnancy category of Fluconazole is C. So, Fluconazole ought to be maintained a strategic distance from in pregnancy and lactation unless the potential benefits to the other exceed the conceivable dangers to the baby.
Precautions & Warnings
Caution should be taken in renal impairment, pregnancy and breast feeding and in raised liver enzymes. The use of Fluconazole in lactating mothers is not recommended.
Therapeutic Class
Drugs for subcutaneous and mycoses
Storage Conditions
Store below 30°C. Protect from light & moisture. Remaining reconstituted suspension should not be used after 7 days. If it is kept under freezing temperature (2 °C – 8 °C), it can be used for 14 days. Keep out of the reach of children.
Pharmaceutical Name
Square Pharmaceuticals Ltd.
