The information provided below corresponds to the official product information from Patient Information Leaflet provided by the manufacturer.
The text does not contain any of medical advices, mode of administration and prescription plans.
Before beginning any treatment, we kindly advise you to consult your healthcare provider.
Fluconazole is an effective broad-spectrum action antifungal medication indicated for yeast infection and treatment of systemic mycosis. It is recommended to prevent recurrent vaginal candidiasis. Fluconazole can be used to prevent mycotic infection in patients with weak immunity. Fluconazole is a representative of thiazole medicines with a potent antifungal effect. The medication possesses selective inhibiting action on fungal enzymes. It inhibits fungal cytochrome P450, blocks sterol synthesis in the fungal cells, and prevents the conversion of lanosterol into membranous ergosterol. As a result, fluconazole increases the permeability of cell membranes interfering with its growth and replication.
Fluconazole is active against opportunistic mycosis, including caused by Candida spp. (Including generalized candidosis associated with weak immune system), Cryptococcus neoformans (including intracranial infection), Microsporum spp. and Ttichoptyton spp; endemic mycosis caused by Blastomyces dermatitis, Coccidioides immitis, including intracranial infections, and Histoplasma capsulatum.
Fluconazole does not affect the activity of liver enzymes as other antifungals. Being highly selective for fungal cytochrome P450, it does not inhibit these enzymes in human organs. Fluconazole inhibits the cytochrome P450 - dependent oxidative processes in human liver microsomes in a less degree in comparison with other antimycotic agents such as itraconazole, clotrimazole, ketoconazole.
After oral administration Fluconazole is almost completely absorbed from the gastrointestinal tract into the blood circulation. The bioavailability is 90%. Cmax is achieved after 0,5-1,5 h after administration. The equilibrium concentration is achieved after 4-5 day of application. Fluconazole binds to plasma proteins by 11-12%. The concentration of active substances in breast milk, joint fluid, saliva, sputum and peritoneal fluid are similar to those in blood plasma. Fluconazole is excreted by kidney with urine in the form of metabolites (20%) and unchanged form (80%). The pharmacokinetics of fluconazole is significantly dependent on renal function.
- Cryptococcosis (respiratory, skin, mucous membranes), as well as cryptococcal meningitis
Yeast infection (Candidiasis):
- Chronic generalized yeast infection (granulomatous)
- Visceral (endocardium, abdominal, respiratory system, eyes)
- Mucous membranes of the mouth, pharynx, esophagus
- Non-invasive candidiasis of the bronchi and lungs
- Genital: acute and chronic recurrent vaginal candidiasis, candida balanitis
- Skin and nails: athletes foot, dermatophytes, onychomycosis, chromophytosis
Mode of administration
Fluconazole comes in the form of tablets 50mg, 100mg, 150mg and 200mg. Unlike yeast infection products , Fluconazole is not used vaginally. It works through the bloodstream to treat yeast infections. You can take the medication with or without food. Fluconazole tablets should be taken whole swallowing with sufficient amount of water.
Fluconazole is contraindicated for use in the following conditions:
- Reactions of hypersensitivity or allergy to fluconazole or other thiazole medications
- Liver cirrhosis and other liver diseases
- Prolonged QT interval
- Serious kidney diseases including renal failure, pyelonephritis, glomerulonephritis
- Cardiovascular diseases such as heart attacks, strokes, angina, coronary heart disease, arrhythmia
- Pregnancy (Fluconazole is a pregnancy category C meaning that it possesses teratogenic and embryotoxic effect to the fetus. Do not taken the medication during pregnancy)
- Breastfeeding (Fluconazole can pass through breast milk and may cause adverse effects in child).
Although a single oral dose of Fluconazole is usually enough for treating vaginal yeast infections, it should be noted that this medicine is more likely to cause adverse effects compared to the standard vaginal treatments, such as yeast infection ointment or creams.
Treatment with fluconazole should be continued until clinical remission. Premature termination of treatment leads to relapses. It is necessary to control blood picture, liver and renal function during the treatment. In case of renal impairment the therapy must be discontinued. Hepatotoxic effects of fluconazole is usually reversible meaning that symptoms disappear after cessation of therapy. In case of skin rash (Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema polymorphous) developing treatment with fluconazole should be discontinued as well.
The medication must be used with caution in patients with impaired renal function, children, HIV-positive patients.
Fluconazole is usually well tolerated and side effects are not common. The most common Fluconazole side effects include: nausea, headache, stomach discomfort. The frequency of side effects does not exceed 1%.
Other less common Fluconazole side effects include: allergic reactions, anaphylactic reactions, toxic epidermal necrolysis.
Liver and kidney dysfunction, hyperbilirubinemia, increased activity of ALT, AST, alkaline phosphatase.
Convulsions, alopecia, leukopenia, thrombocytopenia, neutropenia, agranulocytosis, hypercholesterolemia, hypertriglyceridemia, hypokalemia.
- Fluconazole increases the effectiveness of coumaric of anticoagulants resulting in prothrombin time. Fluconazole increases the concentration of sulfonylureas derivatives: chlorpropamide, glibenclamide, glipizide and tolbutamide. You should monitor sugar blood levels while the treatment with Fluconazole.
- Thiazide diuretics may increase the level of fluconazole in blood plasma. Hydrochlorothiazide increases the concentration of fluconazole in plasma by 40%.
- Fluconazole increases phenytoin concentrations in blood plasma
- Rifampicin reduces Fluconazole T1/2 by 20% and the AUC - 25%.
- Cyclosporin A. Fluconazole increases the concentration of cyclosporine in the blood.
- Fluconazole may increase the concentration of theophylline in blood, extending T1 / 2 ( the risk of intoxication).
- Medicines that prolong QT interval in combination with Fluconazole potentiate the risk of arrhythmias, including paroxysmal ventricular tachycardia.
- Fluconazole may increase Zidovudine concentration in blood plasma
- Fluconazole increases rifabutin blood levels
- Fluconazole Increases the concentration of short-acting benzodiazepines.
- The medication should not be combined with: Tetrabenazin, Thioridazine, Ranolazine, Quinine, Quinidine, Nilotinib, Dofetilide, Conivaptan
This info corresponds to official PIL provided by legal manufacturer and reviewed by: Dr. Rohit Bansali N.