Mycoflucan is an antifungal drug.
Release form and composition
Mycoflucan is available in the following dosage forms:
- Tablets: flat, round, almost white or white, with a facet; 50 mg tablets: with an “F” impression on the one hand and “50” on the other; 150 mg tablets: with a “F150” impression on one side and a dividing risk on the other (1, 4, 7 pieces in blisters, 1 each, or 2 blisters in a carton box);
- Solution for infusion: clear, colorless (100 ml in polyethylene bottles, 1 bottle in a carton box).
The composition of 1 tablet includes:
- Active ingredient: fluconazole - 50 or 150 mg;
- Auxiliary components (tablets 50/150 mg, respectively): microcrystalline cellulose - 22.75 / 68.25 mg; lactose - 30/90 mg; croscarmellose sodium - 5.75 / 17.25 mg; Povidone K30 - 4/12 mg; colloidal silicon dioxide, 0.75 / 2.25 mg; magnesium stearate - 0.75 / 2.25 mg; purified talc - 1/3 mg.
The composition of 100 ml solution for infusion includes:
- Active ingredient: fluconazole - 200 mg;
- Auxiliary components: sodium chloride - 900 mg; edetate disodium - 5 mg; water for injection - up to 100 ml.
Indications for use
- Systemic lesions caused by cryptococcus (Cryptococcus), including sepsis, meningitis, infections of the skin and lungs in patients with a normal immune response and various forms of immunosuppression (including AIDS patients, organ transplants). Mycoflucan is also prescribed to AIDS patients as a supportive therapy to prevent the development of infection;
- Generalized candidiasis: candidemia, disseminated candidiasis, occurring with lesions of the endocardium, eyes, respiratory organs, abdominal cavity and urinary organs. Mycoflucan can be used in patients with malignant neoplasms and undergoing immunosuppressive or cytostatic therapy, as well as in the presence of other factors predisposing to their development (treatment and prevention);
- Candidiasis of the mucous membranes: esophagus, pharynx, oral cavity, candiduria, non-invasive bronchopulmonary candidiasis, mucocutaneous and chronic oral atrophic candidiasis (associated with dental prostheses). Mycoflucan is also prescribed to AIDS patients as a supportive therapy to prevent the development of infection;
- Genital candidiasis: vaginal (recurrent and acute). Perhaps prophylactic use of Mikoflyukan to reduce the frequency of recurrence of the disease (from three episodes per year). Candida balanitis (for the drug in the form of tablets);
- Skin mycoses: inguinal area, body and feet, pityriasis versicolor, onychomycosis, skin candidal infections (for the drug in the form of tablets);
- Deep endemic mycoses (sporotrichosis, paracoccidioidomycosis, coccidiomycosis, histoplasmosis) in patients with a normal immune response.
As a prophylactic agent, Mycoflucan is prescribed in the following cases:
- Fungal infections in patients with malignant tumors on the background of chemotherapy or radiation therapy;
- Oropharyngeal candidiasis in patients with AIDS;
- Candidiasis in the presence of a high risk of generalized infection (for example, with long-lasting or severe neutropenia).
- Simultaneous administration with terfenadine (with regular use of Mikoflyukan in a daily dose of 400 mg) or astemizole;
- Breastfeeding period;
- Hypersensitivity to the components of the drug (including hypersensitivity to other azole drugs).
Mycoflucan should be used with caution in the following diseases / conditions:
- Potentially proarrhythmic states in patients with multiple risk factors (for example, against the background of organic heart disease, electrolyte imbalance, simultaneous use of drugs causing arrhythmias);
- Rash during therapy in patients with systemic / invasive fungal infections and superficial fungal infection;
- Liver failure;
- Simultaneous administration with terfenadine with the use of Mikoflyukan in a daily dose of up to 400 mg;
- Pregnancy (use of the drug is possible only if there are potentially life-threatening and severe fungal infections in cases where the expected benefit of the use of Micoflucan for the mother is significantly higher than the possible risk to the fetus).
Children under three years old are recommended to use the drug in the form of an infusion solution.
Dosing and Administration
Mycoflucan in the form of tablets is taken orally, the solution for infusion is administered intravenously at a rate of not more than 200 mg per hour.
The daily dose of the drug is determined by the nature and severity of the fungal infection.
When transferring from intravenous administration of Mikoflyukan to oral administration and vice versa, the daily dose should not be changed.
Mycoflucan in the form of an infusion solution is compatible with a solution of potassium chloride in glucose, 20% glucose solution, Hartman solution, 0.9% sodium chloride solution, Ringer's solution, 4.2% sodium bicarbonate solution. Infusion can be performed using conventional transfusion kits using one of the above listed solvents.
The multiplicity of the drug - 1 time per day.
Adults and children from 15 years old (with a body weight of 50 kg) are usually prescribed the following dosing regimen (daily dose):
- Cryptococcal meningitis and cryptococcal infections of other sites: 400 mg on the first day, then 200-400 mg daily. The duration of the treatment course is determined by the clinical efficacy confirmed by the results of mycological studies. When treating cryptococcal meningitis, it is usually 6-8 weeks. After the end of the full primary course of treatment, 200 mg are usually prescribed for a long time every day for the prevention of relapse;
- Candidemia, disseminated candidiasis and other invasive infections caused by Candida spp.: 400 mg on the first day, then 200 mg daily (according to indications, a 2-fold dose increase is possible). The duration of the treatment course is determined by the clinical efficacy of Mikoflyukan;
- Oropharyngeal candidiasis: 150 mg daily. The duration of treatment is 1-2 weeks, with a pronounced decrease in immunity, longer therapy is possible. After the end of the full primary course of treatment for the prevention of relapse, patients with AIDS are usually long-term prescribed 150 mg once a week;
- Atrophic candidiasis of the oral cavity caused by dentures: 50 mg daily. The duration of the treatment course is 2 weeks. For the treatment of the prosthesis at the same time should use local antiseptic preparations;
- Other localizations of candidiasis, including esophagitis, non-invasive bronchopulmonary lesions, candiduria, candidiasis of the skin and mucous membranes (except for the treatment of genital candidiasis): 150 mg daily. The duration of the treatment course is from 2 weeks to 1 month;
- Vaginal candidiasis: 150 mg once. If necessary, reduce the frequency of relapses. Micoflucan is prescribed 150 mg once a month (possibly more frequent use of the drug). The duration of the course of treatment the doctor determines individually, it can be from 4 to 12 months;
- Balanitis caused by fungi Candida: 150 mg once;
- Candidiasis (prevention): 50-400 mg. The dose is determined by the degree of risk of developing a fungal infection, the maximum (400 mg) is usually prescribed to patients with a high risk of developing a generalized infection, for example, with long-lasting or expected severe neutropenia. Mycoflucan is recommended to be taken several days before the expected development of neutropenia; after an increase in the number of neutrophils greater than 1000 / mm³, the administration of the drug is continued for another week;
- Mycoses of the skin, including the treatment of mycoses of smooth skin, feet and skin in the groin area: 50 mg daily or 150 mg 1 time per week. The average duration of the treatment course is 2-4 weeks, in the treatment of mycoses of the feet - up to 6 weeks;
- Pityriasis versicolor: 300 mg 1 time per week. The average duration of the treatment course is 2 weeks. In some cases, it is necessary to take a third dose, sometimes a single dose of 300-400 mg is sufficient to achieve a clinical effect. Mycoflucan can also be taken daily in 50 mg for 14-28 days;
- Onychomycosis: 150 mg once a week. Therapy is carried out before replacing the infected nail (on average, 3-6 months for fingernails and 6-12 months - toes);
- Deep endemic mycoses: 200-400 mg daily. The average duration of the treatment course is 2 years (coccidiomycosis - 11-24 months; sporotrichosis - 1-16 months; paracoccidiomycosis - 2-17 months; histoplasmosis - 3-17 months).
For children, the daily dose of Mycoflucan is calculated on the basis of body weight, but it should not exceed the adult dose. As a rule, in children apply the following dosing regimen (daily dose):
- Candidosis of the esophagus: once 3 mg / kg (children 3-6 years old with a body weight from 15 to 20 kg - 50 mg; 7-9 years with a body weight from 21 to 29 kg - 50-100 mg; 10-12 years with a mass bodies from 30 to 40 kg - 100-150 mg; 12-15 years old with a body weight of 40 to 50 kg - 100-150 mg). The average duration of the treatment course is at least 21 days, after the regression of symptoms, another 14 days;
- Candidiasis of the mucous membranes (on the first day of therapy / in the future): once 3 mg / kg (children 3-6 years old with a body weight from 15 to 20 kg - 100-150 / 50 mg; 7-9 years with a body weight from 21 to 29 kg - 100-200 / 100 mg; 10-12 years old with a body weight of 30 to 40 kg - 100-150 / 50-100 mg; 12-15 years old with a body weight of 40 to 50 kg - 250-300 / 100 -150 mg). The average duration of the treatment course is at least 21 days;
- Generalized candidiasis and cryptococcal infections (including meningitis): once 6-12 mg / kg (children 3-6 years old with a body weight from 15 to 20 kg - 100-250 mg; 7-9 years old with a body weight from 21 to 29 kg - 100-300 mg; 10-12 years old with a body weight of 30 to 40 kg - 200-350 mg; 12-15 years old with a body weight of 40 to 50 kg - 250-400 mg). The average duration of the treatment course is 10-12 weeks.
In children with reduced immunity for the prevention of fungal infections in the presence of a risk of developing an infection associated with neutropenia due to radiation therapy or cytotoxic therapy, Mikoflyukan is administered once at a dose of 3–12 mg / kg per day (children 3–6 years old with a body weight from 15 to 20 kg - 50-250 mg; 7-9 years old with a body weight of 21 to 29 kg - 50-300 mg; 10-12 years old with a body weight of 30 to 40 kg - 100-350 mg; 12-15 years with a body weight of 40 to 50 kg - 100-400 mg). The drug is continued until the elimination of induced neutropenia.
With functional disorders of the kidneys, the daily dose of Mikoflyukan in children is reduced in the same proportional dependence as in adults.
Elderly patients in the absence of functional disorders of the kidney dosing regimen should not be adjusted.
Patients with renal insufficiency (with creatinine clearance less than 50 ml per minute) with a single dose of mycoflucan orally, do not need to change the dose. With re-appointment, first take a loading dose (50-400 mg).
Depending on the clearance of creatinine orally prescribe:
- More than 40 ml per minute: the usual dose 1 time per day;
- 21-40 ml per minute: the usual dose 1 time in 2 days or 1/2 dose daily;
- 10-20 ml per minute: the usual dose 1 time in 3 days or 1/3 doses daily.
When using mycoflucan in the form of an infusion solution, it is usually prescribed:
- More than 50 ml per minute: the usual dose;
- Less than 50 ml per minute (without dialysis): 1/2 the usual dose.
Regularly being on dialysis patients after each session, prescribe a single dose of the drug.
The solution of Mycoflucan contains 0.9% sodium chloride solution; each vial contains 100 ml of 15 mmol of chlorine and sodium ions, which must be taken into account by patients who need to limit their fluid or sodium intake.
As a rule, mycoflucan in any dosage form is well tolerated.
However, the following side effects may develop during therapy:
- Cardiovascular system: rarely - fluttering / ventricular fibrillation, an increase in the duration of the QT interval;
- The digestive system: infrequently - abdominal pain, nausea, flatulence, diarrhea, vomiting, change in taste; rarely, functional disorders of the liver (jaundice, hyperbilirubinemia, increased activity of aspartate aminotransferase, alanine aminotransferase and alkaline phosphatase, hepatocellular necrosis, hepatitis), incl. fatal;
- Central nervous system: infrequently - dizziness, headache; rarely seizures;
- Organs of hematopoiesis: rarely - agranulocytosis, thrombocytopenia, leukopenia, neutropenia;
- Allergic reactions: rarely - skin rash; rarely, toxic epidermal necrolysis (Lyell's syndrome), erythema multiforme exudative (including Stevens-Johnson syndrome), anaphylactoid reactions (including urticaria, angioedema, pruritus, swelling of the face);
- Other: rarely - alopecia, renal dysfunction, hypokalemia, hypercholesterolemia, hypertriglyceridemia.
Mikoflyukan should be used before the appearance of clinical and hematological remission, since the premature withdrawal of the drug can cause the development of relapses.
Therapy can be started in the absence of the result of seeding or other laboratory tests necessary for making a diagnosis. After receiving them, you may need to adjust the dosage regimen.
During the use of Mikoflyukan need to monitor blood parameters, liver function and kidney. With simultaneous use of the drug with anticoagulants coumarin range should be monitored prothrombin index. With the development of functional disorders of the liver and kidney therapy should be discontinued.
In some cases, the use of Mycoflucan was accompanied by toxic changes in the liver. With the appearance of clinical signs of such changes, which may be associated with ongoing treatment, the drug is canceled.
In cases where patients with a superficial fungal infection develop a rash, and its occurrence can be regarded as definitely associated with the use of the drug, therapy should be interrupted. When a rash develops in patients with systemic / invasive fungal lesions, they should be carefully monitored and, if a multiforme erythema or bullous changes occur, discard Mikoflucan.
During therapy, it is recommended to monitor the concentration of cyclosporine in the blood, since in patients with a transplanted kidney, taking Mikoflyukan at a daily dose of 200 mg may lead to a gradual increase in the concentration of cyclosporine in the plasma.
Care should be taken when using mycoflucan with rifabutin, cisapride or other drugs that are metabolized by the cytochrome P450 system.
With the simultaneous use of Mikoflyukan with some drugs, undesirable effects may occur (T1 / 2 - half-life of the substance, AUC - the total concentration of the drug in blood plasma):
- Theophylline: its T1 / 2 lengthening and, respectively, increase in risk of development of intoxication (correction of its dose is required).
- Coumarin anticoagulants (for example, warfarin): an increase in prothrombin time (with a joint appointment requires careful monitoring of the prothrombin time);
- Hydrochlorothiazide: an increase in the concentration of fluconazole in plasma (with a joint appointment, a change in the dosage regimen is not required in the case of use with diuretics);
- Cisapride: possible development of adverse reactions of the heart, including the occurrence of ventricular tachycardia paroxysms (arrhythmia type "pirouette");
- Sulfonylurea drugs (glibenclamide, tolbutamide, chlorpropamide, glipizide): prolong their T1 / 2, which can cause the development of hypoglycemia (with a joint appointment requires a dose adjustment of hypoglycemic drugs);
- Zidovudine: an increase in its concentration, and, accordingly, its side effects;
- Phenytoin: a clinically significant increase in its concentration (with a joint appointment, it is necessary to select its dose, providing a therapeutic concentration in serum);
- Midozalam: an increase in the risk of development of psychomotor effects (more pronounced when using mycoflucan inside);
- Rifampicin: a decrease in AUC and the duration of T1 / 2 fluconazole (dose adjustment may be required);
- Tacrolimus: an increase in its concentration and, accordingly, an increased risk of nephrotoxic action;
- Rifabutin: an increase in its serum concentrations, the risk of uveitis (requires careful monitoring of the patient's condition).
During simultaneous use of Mikoflyukan with cyclosporine, the concentration of the latter in the blood should be monitored.
Terms and conditions of storage
Store in a dark, dry place inaccessible to children at temperature up to 25 ° C (do not freeze solution for infusion).
Shelf life is:
- Pills - 3 years;
- Solution for infusions - 2 years.