broad spectrum antifungal
Each capsule contains fluconazole 150 mg.
Pharmacological Properties :
Fluconazole is a triazole antifungal drug which in sensitive fungi inhibits cytochrome P-450 dependent enzymes resulting in impairment of ergosterol synthesis in fungal cell membranes.
It is active against a broad spectrum of yeasts and other fungal pathogens including: Blastomyces dermatitidls, Candida spp., Coccimoides Immitis, Cryptococcus neoformans, Epidermophyton spp., histoplasma capsulatum, microsporum spp., and trichophyton spp.
Fungican (fluconazole) is well absorbed following oral administration Bioavailability of oral fluconazole is over 90% of the level achieved
after intravenous administration. Oral absorption is not affected by food or gastric pH. Peak plasma concentrations are reached within
1-2 hours of oral administration with a terminal elimination plasma half-life of 30 hours. Plasma concentrations are proportional to the
dose. Multiple dosing leads to increase in peak plasma concentrations. Steady-state concentrations are reached within 5 to 10 days but may be attained on the second day, if a loading dose is given.
The plasma protein1J1nding offluconazole is 11% The drug is widely distributed throughout the body with an apparent volume of distribution approximately equal to total body water. Concentrations in breast milk, joint fluid, saliva, sputum, vaginal fluid, and peritoneal fluid are similar to those achieved in plasma Concentrations in the cerebrospinal fluid range from 50 to 90% of plasma concentrations even in. the absence of meningeal inflammation. Urinary- concentrations and those in skin are 10-fold greater than in plasma.
80% or more of fluconazole is excreted unchanged in the urine; about 11 % is excreted in the urine as metabolites. The pharmacokinetics of fluconazole are markedly affected by reduction in renal function. There is an inverse relationship between the elimination half life and creatinine clearance. Fluconazole is removed by dialysis.
– Superficial mucosal (oropharyngeal, esophageal, or vaginal) candidiasis.
– Dermatomycosis, including tinea pedis, tinea corporis, tinea cruris, tinea versicolor, tinea unguium (onychomycosis) and dermal candidal infections.
– Systemic candidal infection e.g., Urina tract infections, peritonitis, candidemia, di minated candidiasis, and pneumonia.
– Deep mycoses, including blastomycosis, coccidioidomycosis, histoplasmosis, and sporotrichosis.
– Cryptococcosis including cryptococcal menin
– Prophylaxis for fungal infections in patients malignancy who are receiving chemotherap ractiation therapy.
– Prophylaxis of serious fungal infections in patients with human immunodeficiency virus (HIV) infection.
– Known hypersensitivity to fluconazole
– Advanced liver disease
– Co-administration with terfenadine
• Fluconazole has been associated with rare cases of serious hepatic toxicity, including fatalities. Instances of fatal hepatic reactions occurred primarily in patients with serious underlying medical conditions (AIDS & malignancy).Patients who develop abnormal liver function tests during fluconazole therapy should be monitored
for the development of more severe hepatic injury. Fluconazole therapy should be discontinued if signs & symptoms consistent with liver disease develop.
• Patients have rarely developed exfoliative skin disorders during treatment with fluconazole. In patients with serious underlying diseases (predominantly AIDS & malignancy), these have rarely resulted in a fatal outcome. Patients who develop rashes during treatment with fluconazole should be monitored closely and the drug is discontinued if lesions progress.
• Pregnancy There are limited data on the use of fluconazole in
pregnant women. Fluconazole should be used during pregnancy only when the benefit clearly outweighs the risk.
• Lactation Fluconazole is excreted in breast milk at concentrations similar to plasma. Therefore, the use of fluconazole in nursing mothers is not recommended.
Adverse Effects :
Fluconazole is generally well tolerated. Adverse effects reported with fluconazole most commonly affect the gastrointestinal tract and
include abdominal pain, diarrhoea, 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
Skin reactions are rare but exfoliative cutaneous reactions 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 reduce plasma concentrations of fluconazole. Administration of hydrochlorothiazide with fluconazole has resulted in clinically insignificant increases in plasma fluconazole concentrations.
Fluconazole may interfere with metabolism of some drugs if given concomitantly, through the inhibition of cytochrome P-450. 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 cyclosporin, rifabutin, tacrolimus and zidovudine have also been reported.
Increases in terfenadine concentrations following high doses of fluconazole have been associated with ECG abnormalities. The concomitant use of fluconazole with terfenadine should be avoided
because of the risk of cardiac arrhythmias. Fluconazole may increase the effect of some oral anticoagulants and reduce the clearance of
theophylline. The efficacy of oral contraceptives may be reduced.
Dosage and Administration :
1- Vaginal candidiasis :
One capsule (150 mg) as a single dose. To reduce the incidence of recurrent vaginal candidiasis, one capsule (150 mg) once monthly
dose may be used. The duration of therapy should be individualized, but ranges from 4-12 months.
2-For dermal infections including tinea pedis, corporis, cruris and candida infections : the recommended dose is one capsule (150 mg) once weekly. Duration of treatment 2-4 weeks, tinea pedis may require up to 6 weeks.
Tinea versicolor: 2 capsules (300 mg) once weekly for 2-3 weeks.
Onychomycosis: One capsule (150 mg) once weekly for 3-6 months (fingernails) and 6-12 months (toenails).
3-0ropharyngeal and esophageal candidiasis :
One capsule (150 mg) daily for 7-14 days (except in severely immunocompromised patients); for 14 days in atrophic oral candidiasis associated with dentures; for 14-30 days in other mucosal infections: esophagitis, non-invasive bronchopulmonary infections.
4-Systemic candidiasis, cryptococcal meningitis and other cryptococcal infections :
Treated with an initial dose of 2-3 capsules (300- 450 mg) on the first day, followed by 1-2 capsules (150-300 mg) daily. Duration of therapy is based on clinical & mycological response, but is usually
at least 6-8 weeks in cryptococcal meningitis. Fluconazole may also be used in daily doses of 100-200 mg to prevent relapse following a
primary course of treatment for acute cryptococcal meningitis in patients with AIDS.
5-ln immunocompromised patients at risk of fungal infections: fluconazole may be given prophylactically in a dose of 50-400 mg daily. In patients with renal impairment
Sinc fluconazole is primarily excreted by the kidneys, fluconazole dosage must be adjusted for renal impairment according to creatinine clearance.
Initial loading dose of 50-400 mg should be given on the first day of treatment, after the loading dose, the daily dose (according to indications) should be based on the following table:
Creatinine clearance (ml/min) Percent of recommended
regular dialysis 100% after each diaylsis
No dosage adjustment is needed in patients with renal impairment given single-dose therapy.
How Supplied :
Fungican® capsules: Pack of one capsule containing 150 mg fluconazole.
Keep all medicaments out of reach of children
Product of :
AMOUN PHARMACEUTICAL Co. SA£.
H-Obour City, Cairo, Egypt. .