Full Prescribing Info
Each capsule contains: Fluconazole 150 mg.
Pharmacology: Pharmacokinetics: Fluconazole is well absorbed following oral administration, bioavailability from the oral route being 90% or more of that from the intravenous route. Mean peak plasma concentrations of 6.72 ug per mL have been reported in healthy subjects following a 400 mg oral dose. Peak concentrations are reached within 1 to 2 hours of oral administration. Plasma concentrations are proportional to the dose over a range of 50 to 400 mg. Multiple dosing leads to increases in peak plasma concentrations; steady-state concentrations are reached in 6 to 10 days but may be attained on day 2 if a loading dose is given.
Fluconazole is widely distributed and the apparent volume of distribution is close to that of total body water. Concentrations in breast milk, joint fluid, sputum, vaginal fluids, and peritoneal fluid are similar to those achieved in plasma. Concentrations in cerebrospinal fluid range from 50 to 90% of plasma concentrations, even in the absence of meningeal inflammation. Protein binding is only about 12%.
Eighty percent or more of fluconazole is excreted unchanged in the urine; about 11% excreted as metabolites. The elimination half-life of fluconazole is about 30 hours and is increased in patients with impaired renal function. Fluconazole is removed by dialysis.
Microbiology: Antimicrobial Action: Fluconazole is a triazole antifungal drug which in sensitive fungi inhibits cytochrome dependent enzymes resulting in impairment of ergosterol synthesis in fungal cell membranes. It is active against Blastomyces dermatitidis, Candida, Coccidioides immitis, Cryptococcus neoformans, Epidermophyton, Histoplasma capsulatum, Microsporum, and Trichophyton.
Resistance has developed in some Candida following long-term prophylaxis with fluconazole, and cross-resistance with other azoles has been reported.
It is used for superficial mucosal (oropharyngeal, oesophageal, or vaginal) candidiasis and for fungal skin infections. It is also given for systemic infections including systemic candidiasis, coccidioidomycosis, and cryptococcosis, and has been tried in blastomycosis, chromoblastomycosis, histoplasmosis, and sporotrichosis.
Dosage/Direction for Use
For superficial mucosal candidiasis (other than genital candidiasis) the usual dose of fluconazole in the UK is 50 mg daily, although 100 mg daily may be given if necessary. Treatment usually continues for 7 to 14 days in oropharyngeal candidiasis (except in severely immunocompromised patients), for 14 days in atrophic oral candidiasis associated with dentures, and for 4 to 30 days in other mucosal candidal infections including oesophagitis. Higher dose are recommended in the USA where an initial dose of fluconazole 200 mg and at least 14 days after resolution of symptoms for oesophageal infections; doses of up to 400 mg daily may be used for oesophageal candidiasis if necessary.
Fluconazole 150 mg by mouth as a single dose may be used for vaginal candidiasis or candidal balanitis. Dermatophytosis, pityriasis versicolor, and candida infections of the skin may be treated with fluconazole 50 mg daily for up to 6 weeks.
Systemic candidiasis, cryptococcal meningitis, and other cryptococcal infections may be treated with an initial dose of fluconazole 400 mg followed by 200 to 400 mg daily. Duration of therapy is based on clinical and mycological response, but is usually at least 6 to 8 weeks in cryptococcal meningitis. Fluconazole may also be used in daily doses of 100 to 200 mg to prevent relapse following a primary course of antifungal treatment for acute cryptococcal meningitis in patients with AIDS.
In immunocompromised patients at risk of fungal infections, fluconazole may be given prophylactically in a dose of 50 to 400 mg daily.
Suggested doses for children over 4 weeks of age are 3 mg per kg daily for superficial infections (a loading dose of 6 mg per kg may be used on the first day if necessary), and 6 to 12 mg per kg daily for systemic infection. For prophylaxis in immunocompromised children, a dose of 3 to 12 mg per kg daily has been recommended. For infants under 2 weeks of age, these doses should be given once every 72 hours; for children aged between 2 and 4 weeks, the doses should be given every 48 hours. A maximum dose of 400 mg daily should not be exceeded in children, or 12 mg per kg at appropriate intervals in infants.
Patients with renal impairment may require dosage reduction. Normal loading or initial doses should be given on the first day of treatment and subsequent doses of fluconazole should be adjusted according to creatinine clearance. If the creatinine clearance is more than 50 mL per minute, the standard dose can be given. If the creatinine clearance is 11 to 50 mL per minute, half the standard dose can be given. Patients on regular haemodialysis should receive a standard dose of fluconazole after every dialysis session. No dosage adjustment is needed in patients with renal impairment given single-dose therapy or as prescribed by the physician.
Special Precautions
Fluconazole should be used with caution in patients with impaired renal or hepatic function.
Teratogenicity has occurred in animal given high doses of fluconazole and its use is not recommended in pregnancy. It should not be given to breast-feeding women.
Use In Pregnancy & Lactation
Teratogenicity has occurred in animal given high doses of fluconazole and its use is not recommended in pregnancy. It should not be given to breast-feeding women.
Adverse Reactions
Adverse effects reported with fluconazole most commonly affects the gastro-intestinal tract and include abdominal pain, diarrhea, flatulence, nausea, and vomiting. Other adverse effects include headache, dizziness, leucopenia, thrombocytopenia, and raised liver enzyme values. Serious hepatic toxicity has been reported in patients with severe underlying disease. Anaphylaxis and angioedema have been reported rarely.
Skin reactions are rare but exfoliative cutaneous reaction such as toxic epidermal necrolysis and Stevens-Johnson syndrome have occurred, more commonly in patients with AIDS.
Drug Interactions
Concomitant administration of rifampicin with fluconazole results in reduced plasma concentrations of fluconazole. Administration of hydrochlorothiazide and fluconazole has resulted in clinically insignificant increases in plasma-fluconazole concentrations.
Fluconazole may interfere with the metabolism of some drug if given concomitantly, presumably through inhibition of cytochrome (CYP3A4). This may account for the reported increases in plasma concentrations of phenytoin and sulphonylurea hypoglycaemics and reductions in the production of a toxic metabolite of sulphamethoxazole. Increases in plasma concentrations of cyclosporine, nortriptyline, rifabutin, tacrolimus, and zidovudine have also been reported.
Increases in terfenadine concentrations following high doses of fluconazole have been associated with ECG abnormalities. A similar effect may be anticipated with astemizole. Concurrent administration of fluconazole and cisapride could result in increased cisapride concentrations and associated toxicity. The concomitant use of fluconazole with astemizole, cisapride, terfenadine should be avoided because of the risk of cardiac arrhythmias.
Fluconazole may also increase the effect of some oral anticoagulants and reduce the clearance of theophylline. The efficacy of oral contraceptives may be reduced.
Store at temperatures not exceeding 30°C.
MIMS Class
ATC Classification
J02AC01 - fluconazole ; Belongs to the class of triazole derivatives. Used in the systemic treatment of mycotic infections.
Cap 150 mg x 4's.
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