Fluconazole - instructions for use, reviews, analogs and formulations (capsules and tablets 50 mg, 100 mg and 150 mg) of the drug for treatment of thrush, candidiasis and other mycoses in adults, children and pregnancy

In this article, you can read the instructions for using the drug Fluconazole. Presented are reviews of visitors to the site - consumers of this medication, as well as the opinions of doctors of specialists on the use of Fluconazole in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Fluconazole in the presence of existing structural analogues. Use to treat thrush, candidiasis and other forms of mycosis in adults, children, as well as during pregnancy and lactation.

Fluconazole - antifungal agent, has a highly specific effect, inhibiting the activity of fungal enzymes. Blocking the conversion of lanosterol of fungal cells to ergosterol; increases the permeability of the cell membrane, disrupts its growth and replication.

Fluconazole, being highly selective for cytochrome P450 fungi, practically does not inhibit these enzymes in the human body (in comparison with itraconazole, clotrimazole, econazole and Ketoconazole less inhibits oxidative processes dependent on cytochrome P450 in human liver microsomes). Does not have anti-androgenic activity.

Active with opportunistic fungal infections, incl. caused by Candida spp. (including generalized forms of candidiasis on the background of immunodepression), Cryptococcus neoformans and Coccidioides immitis (including meningitis and encephalitis), Microsporum spp. and Trichophyton spp; with endemic mycoses caused by Blastomyces dermatidis, Histoplasma capsulatum (including with immunodepression).

Pharmacokinetics

After oral administration fluconazole is well absorbed, food intake does not affect the rate of absorption of fluconazole, its bioavailability is 90%. Fluconazole well penetrates into all body fluids. The concentration of the active substance in breast milk, articular fluid, saliva, sputum and peritoneal fluid is similar to that in blood plasma.Constant values ​​in vaginal secretions are reached 8 hours after ingestion and remain at this level for at least 24 hours. Fluconazole well penetrates into the cerebrospinal fluid (CSF); in fungal meningitis, the concentration in the CSF is about 85% of its plasma level. In the fluid, epidermis and stratum corneum (selective accumulation), concentrations exceeding serum levels are achieved. It is excreted mainly by the kidneys (80% - unchanged, 11% - in the form of metabolites).

Indications

• cryptococcosis, including cryptococcal meningitis and other localizations of this infection (including lungs, skin), both in patients with normal immune response, and in patients with different forms of immunodepression (including AIDS patients, organ transplantation ); the drug can be used to prevent cryptococcal infection in AIDS patients;
• generalized candidiasis, including candidemia, disseminated candidiasis and other forms of invasive candidiasis infections (peritoneal, endocardial, eye, respiratory and urinary tract infections). Treatment can be conducted in patients with malignant neoplasms, in intensive care units, in patients undergoing cytostatic or immunosuppressive therapy,and also in the presence of other factors predisposing to the development of candidiasis;
• candidiasis of the mucous membranes, including the oral cavity and pharynx (including atrophic candidiasis of the oral cavity associated with the wearing of dentures), esophagus, non-invasive bronchopulmonary candidiasis, candiduria, candidiasis of the skin; prevention of recurrence of oropharyngeal candidiasis in AIDS patients;
• genital candidiasis: vaginal candidiasis (acute and chronic recurrent), preventive use to reduce the frequency of recurrences of vaginal candidiasis (3 or more episodes a year);
• Candidiasis balanitis;
• prevention of fungal infections in patients with malignant neoplasms that are predisposed to such infections as a result of chemotherapy with cytostatics or radiation therapy;
• mycosis of the skin, including mycosis of the feet, the body, the groin area;
• pityriasis (lichen variegated) deprive;
• onychomycosis;
• candidiasis of the skin;
• Deep endemic mycoses, including coccidiomycosis and histoplasmosis, in patients with normal immunity.

Forms of release

Capsules 50 mg, 100 mg and 150 mg.

Tablets, film-coated 50 mg, 100 mg, 150 mg.

Solution for infusion 2 mg / ml (injection form, in injections).

Instructions for use and dosage

Inside.

Adults and children over 15 years of age (body weight over 50 kg) with cryptococcal meningitis and cryptococcal infections of other locations on the first day are usually prescribed 400 mg (8 capsules of 50 mg), and then continue treatment at a dose of 200 mg (4 capsules of 50 mg ) - 400 mg (8 capsules of 50 mg) once a day. The duration of treatment for cryptococcal infections depends on the clinical efficacy, confirmed by mycological examination; when cryptococcal meningitis treatment course should be at least 6-8 weeks.

To prevent the recurrence of cryptococcal meningitis in AIDS patients, after completion of the full course of primary therapy, fluconazole is administered at a dose of 200 mg (4 capsules 50 mg) per day for a long period of time.

When candidemia, disseminated candidiasis and other invasive candidiasis infections on the first day of the dose is 400 mg (8 capsules of 50 mg), and then - 200 mg (4 capsules of 50 mg) per day. With insufficient clinical effectiveness, the dose of the drug can be increased to 400 mg (8 capsules 50 mg) per day. The duration of therapy depends on the clinical effectiveness of the drug (100% of the recommended dose).

With SC from 11 to 50 ml / min 50% of the recommended dose or usual dose is applied once in 2 days.

Patients on hemodialysis, one dose of the drug is used after each session of hemodialysis.

Side effect

• decreased appetite;
• change in taste;
• nausea, vomiting;
• diarrhea;
• flatulence;
• abdominal pain;
• vomiting;
• headache;
• dizziness;
• excessive fatigue;
• convulsions;
• leukopenia;
• thrombocytopenia (bleeding, petechiae);
• neutropenia;
• agranulocytosis;
• skin rash;
• anaphylactoid reactions (including angioedema, facial edema, hives, itching of the skin);
• impaired renal function;
• alopecia;
• hypercholesterolemia, hypertriglyceridemia, hypokalemia.

Contraindications

• increased sensitivity to the drug (including other azole antifungal drugs in history);
• simultaneous reception of terfenadine (against the background of the continuous use of fluconazole at a dose of 400 mg per day or more) or astemizole, as well as other drugs that extend the QT interval;
• children under 1 year.

Application in pregnancy and lactation

The use of the drug in pregnant women is not advisable, except for severe or life-threatening forms of fungal infections, when the potential benefit from using fluconazole for the mother significantly exceeds the risk for the fetus.

Since the concentration of fluconazole in breast milk and in plasma is the same, it is contraindicated to apply the drug during lactation.

Use in children

Contraindicated in children under 1 year.

special instructions

Treatment should continue until the appearance of clinical-hematologic remission. Premature termination of treatment leads to relapse.

In rare cases, the use of fluconazole was accompanied by toxic changes in the liver, incl. with a fatal outcome, mainly in patients with serious concomitant diseases. In the case of hepatotoxic effects associated with fluconazole, there was no apparent dependence on total daily dose, duration of therapy, sex and age of the patient. The hepatotoxic effect of fluconazole was usually reversible; signs of it disappeared after discontinuation of therapy. If there are clinical signs of liver damage that may be associated with fluconazole, the drug should be discontinued.

Patients with AIDS are more likely to develop severe skin reactions with many drugs. In those cases where the rash develops in patients with superficial fungal infection and it is regarded as definitely associated with fluconazole, the drug should be discontinued. When rashes appear in patients with invasive systemic fungal infections,they should be carefully observed and discarded fluconazole with the appearance of bullous changes or erythema multiforme.

Care should be taken when taking fluconazole simultaneously with cisapride, rifabutin, or other drugs metabolized by the cytochrome P450 system.

Simultaneous reception of a preparation with alcohol is undesirable.

Drug Interactions

When using fluconazole with warfarin, prothrombin time increases (on average by 12%). It is recommended to monitor prothrombin time when fluconazole is combined with coumarin anticoagulants

Fluconazole increases T1 / 2 from the plasma of oral hypoglycemic agents - derivatives of sulfonylureas (chlorpropamide, glibenclamide, glipizide, tolbutamide) in healthy people. Joint use of fluconazole and oral hypoglycemic agents in diabetic patients is allowed, but the doctor should keep in mind the possibility of developing hypoglycemia.

The simultaneous use of fluconazole and phenytoin can lead to an increase in the concentration of phenytoin in the plasma to a clinically significant degree.Therefore, when it is necessary to jointly use these drugs, it is necessary to monitor the concentrations of phenytoin with correction of its dose in order to maintain the drug concentration within the therapeutic interval.

It is recommended that the concentration of cyclosporin in the blood be monitored in patients receiving fluconazole. when using fluconazole and cyclosporine in patients with kidney transplantation, fluconazole administration at a dose of 200 mg per day leads to a slow increase in the plasma cyclosporin concentration.

Patients who receive high doses of theophylline or who are likely to develop theophylline intoxication should be monitored to detect symptoms of a theophylline overdose, simultaneous administration of fluconazole leads to a decrease in the clearance of theophylline from the blood plasma.

There have been reports of an interaction between fluconazole and rifabutin, accompanied by an increase in serum concentration of the latter. With the simultaneous use of fluconazole and rifabutin, cases of uveitis are described. It is necessary to carefully observe patients who are simultaneously receiving rifabutin and fluconazole.

In patients receiving a combination of fluconazole and zidovudine, an increase in the concentration of zidovudine is observed, which is caused by a decrease in the conversion of the latter into its main metabolite, so the side effects of zidovudine should be expected to increase.

With simultaneous application of fluconazole, terfenadine and cisapride, cases of unwanted reactions from the heart, including pirouette-type arrhythmia, have been described.

Simultaneous use of fluconazole and hydrochlorothiazide may increase the concentration of fluconazole by 40%.

Increases the concentration of midazolam, which increases the risk of developing psychomotor effects (more pronounced when fluconazole is administered orally than intravenously).

Analogs of the drug Fluconazole

Structural analogs for the active substance:

• Vero-Fluconazole;
• Disorel-Sanovel;
• Diflason;
• Diflucan;
• Mikonil;
• Medoflucon;
• Mycomomax;
• Mycosyst;
• Mycoflucan;
• Nofung;
• Procanazole;
• Fangifflu;
• Flucosan;
• Flukoside;
• Flukomabol;
• Flucomycid SEDIKO;
• Fluconazole Hexal;
• Fluconazole-Teva;
• Flukonorm;
• Flukoral;
• Flukoreem;
• Flucostat;
• Forkan;
• Fungolon;
• Ciscan.

Similar medicines:

Other medicines: