Mikosist - instructions for use, analogs, reviews and release forms (capsules or tablets 50 mg, 100 mg and 150 mg, solution for infusions in ampoules) drug for the treatment of candidiasis (thrush) in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Mycosyst. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Mycosyst 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. Mikosist analogs in the presence of existing structural analogues.Use to treat candidiasis (thrush) and other mycoses in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

Mycosyst antifungal drug. Fluconazole (the active substance of the drug Mycosyst), a representative of the class of triazole antifungal agents, is a selective inhibitor of the synthesis of sterols in the fungal cell.

Fluconazole, being highly selective for cytochrome P450 fungi, practically does not inhibit the cytochrome P450 system 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 androgenic activity.

It is active against pathogens caused by Candida spp. (candida), Cryptococcus neoformans (cryptococci), Microsporum spp., Trichophyton spp. Also shown is the activity of fluconazole on models of endemic mycoses, including infections caused by Blastomyces dermatitidis, Coccidioides immitis and Histoplasma capsulatum.

Composition

Fluconazole + auxiliary substances.

Pharmacokinetics

After intravenous administration, Mycosyst penetrates well into the tissues and body fluids. Concentrations of the drug in saliva, sputum, breast milk, articular and peritoneal fluid are similar to its concentration in blood plasma.In patients with fungal meningitis, the fluconazole content in the cerebrospinal fluid reaches 80% of the corresponding plasma concentration. Concentrations in the plasma are in a direct proportion to the dose. 90% equilibrium concentration is reached by 4-5 days with daily administration once a day. The application on the first day of a dose, twice the usual daily dose, allows reaching 90% of the equilibrium concentration by the second day. The apparent volume of distribution approximates the total volume of water in the body. 11-12% of fluconazole binds to plasma proteins. Metabolites in the peripheral blood were not detected. Fluconazole is excreted from the body, mainly by the kidneys; while approximately 80% of the administered dose is excreted unchanged.

Indications

• cryptococcosis: cryptococcal meningitis, cryptococcal infections of the lungs and skin; cryptococcal sepsis; prevention of recurrence of cryptococcosis in AIDS patients, organ transplantation or other cases of immunodeficiency;
• generalized candidiasis; candidemia, disseminated candidiasis and other forms of invasive candidiasis infections (infections of the abdominal cavity, endocardium, eyes, respiratory and urinary tract), incl.in patients receiving a course of cytostatic or immunosuppressive therapy, as well as in the presence of other factors predisposing to the development of candidiasis - treatment and prevention;
• Candidiasis of the mucous membranes: oral cavity, incl. atrophic candidiasis of the oral cavity, associated with the wearing of dentures; pharynx; esophagus and non-invasive bronchopulmonary infections, candiduria; prevention of recurrence of oropharyngeal candidiasis in AIDS patients;
• genital candidiasis: vaginal (acute or chronic recurrent);
• 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, trunk, inguinal region;
• Deep endemic mycoses, including coccidioidomycosis, paracoccidioidomycosis and histoplasmosis in patients with normal immunity.

Forms of release

Capsules 50 mg, 100 mg and 150 mg (sometimes mistakenly called tablets).

Solution for infusions 2 mg / ml (in ampoules).

Other medicinal forms of the drug, whether candles, ointment or cream, do not exist.

Instructions for use and dosing regimen

In cryptococcal infections, the usual dose of Mycosyst is 400 mg once a day on the first day of treatment, and then 200-400 mg once a day. The duration of treatment for cryptococcal infections depends on the clinical efficacy, confirmed by mycological examination, and usually ranges from 6 to 8 weeks.

The recommended duration of treatment for cryptococcal meningitis is 10-12 weeks after a negative result of a microbiological study of a sample of cerebrospinal fluid.

To prevent the recurrence of cryptococcal meningitis in AIDS patients, after completing the full course of primary therapy, Mycosyst is prescribed at a dose of at least 200 mg per day for a long period.

With candidemia, disseminated candidiasis and other invasive candidiasis infections, the dose of fluconazole is 400 mg on the first day and 200 mg on subsequent days. If necessary, the dose of the drug can be increased to 400 mg per day. The duration of treatment depends on clinical effectiveness.

With severe systemic candidiasis, it is possible to increase the dose to 800 mg per day. The duration of therapy depends on clinical effectiveness.Should continue at least 2 weeks after receiving negative blood cultures or after the disappearance of the symptoms of the disease.

With oropharyngeal candidiasis, including patients with impaired immunity, the usual dose of fluconazole is 50-100 mg once a day for 7-14 days. To prevent the recurrence of oropharyngeal candidiasis in AIDS patients after completing the full course of primary therapy - 150 mg once a week. If necessary, the treatment can be prolonged, especially with severe immunity disorders.

With atrophic candidiasis of the oral cavity associated with the wearing of dentures, fluconazole is usually prescribed at 50 mg once a day for 14 days in combination with antiseptic agents to treat the prosthesis.

In other candidiasis infections, for example, with esophagitis, noninvasive bronchopulmonary infections, candiduria, candidiasis of the skin and mucous membranes, the daily dose is 50-100 mg for 14-30 days.

In severe candidiasis of the mucous membranes - 100-200 mg per day.

For the prevention of fungal infections in patients with malignant neoplasms, the dose of Mycosyst is 50 mg once a day until the patient is at a high risk because of cytotoxic or radiation therapy.

With vaginal candidiasis - 150 mg once.To reduce the frequency of relapses, once a month, 150 mg are used for 4-12 months, sometimes more frequent use may be required.

For the prevention of candidiasis, the recommended dose of fluconazole is 50-400 mg once a day, depending on the degree of risk of fungal infection. If there is a high risk of generalized infection, for example, in patients with expected severe or persistent neutropenia, the recommended dose is 400 mg once daily. Fluconazole is prescribed several days before the expected appearance of neutropenia; after an increase in the number of neutrophils more than 1000 / μl, treatment is continued for another 7 days.

With deep endemic mycoses, it may be necessary to use the drug at a dose of 200-400 mg per day for 2 years. The duration of therapy is determined individually; it can be 11-24 months with coccidioidomycosis; 2-17 months with paracoccidioidomycosis and 3-17 months with histoplasmosis.

In children, the drug should not be used in a daily dose exceeding that of adults. The duration of treatment depends on the clinical and mycological effect.

In candidiasis of mucous membranes, the recommended dose of fluconazole is 3 mg / kg per day.On the first day, a shock dose of 6 mg / kg can be given to achieve a more rapid equilibrium concentration.

For the treatment of generalized candidiasis and cryptococcal infection, the recommended dose is 6-12 mg / kg per day, depending on the severity of the disease.

For the prevention of fungal infections in children with reduced immunity, where the risk of infection is associated with neutropenia, resulting from cytotoxic chemotherapy or radiation therapy, the drug is prescribed at 3-12 mg / kg per day, depending on the severity and duration of preservation of induced neutropenia.

In newborns, Mycosyst is slower, therefore in the first 2 weeks of life the drug is administered at the same dose (in mg / kg) as in older children, but at an interval of 72 hours. Children aged 3-4 weeks are administered the same dose with an interval of 48 hours.

In elderly patients in the absence of violations of the kidneys should follow the usual recommendations for dosing the drug.

Application rules

Enter intravenously drip at a rate of not more than 20 mg (10 ml) per minute. When transferring from / in the introduction to taking capsules and vice versa, there is no need to change the daily dose of the drug.

Mycosyst infusion solution is compatible with the following solutions: 20% glucose solution, Ringer's solution, Hartman's solution, potassium chloride solution in glucose, sodium bicarbonate solution, 0.9% sodium chloride solution. Infusions of fluconazole can be performed with conventional transfusion kits using one of the solutions listed above.

Side effect

• nausea, vomiting;
• diarrhea;
• flatulence;
• abdominal pain;
• change in taste;
• impaired liver function (hyperbilirubinemia, increased activity of hepatic transaminases, alkaline phosphatase, jaundice, hepatitis, hepatocellular necrosis, including fatal);
• headache;
• dizziness;
• convulsions;
• leukopenia, thrombocytopenia, neutropenia, agranulocytosis;
• skin rash;
• multi-form exudative erythema (including Stevens-Johnson syndrome);
• toxic epidermal necrolysis (Lyell's syndrome);
• anaphylactoid reactions (including angioedema, facial edema, hives, itching of the skin);
• bronchial asthma (more often with intolerance of acetylsalicylic acid);
• an increase in the duration of the QT interval on the ECG;
• fibrillation / flutter of the ventricles;
• hypercholesterolemia;
• hypokalemia;
• impaired renal function;
• alopecia.

Contraindications

• simultaneous reception of terfenadine (against the background of a constant intake of fluconazole at a dose of 400 mg per day and above) and cisapride, both drugs extend the QT interval and increase the risk of severe cardiac rhythm disturbances;
• simultaneous use of astemizole;
• lactation period (breastfeeding);
• children's age up to 6 months (for oral administration);
• hypersensitivity to the components of the drug or a similar structure of azole compounds.

Application in pregnancy and lactation

The use of Mikosist during pregnancy is possible only if the potential benefit to the mother exceeds the risk to the fetus.

Fluconazole is defined in breast milk in the same concentration as in plasma, so its use during lactation is contraindicated.

Application in elderly patients

In elderly patients in the absence of signs of renal failure should follow the usual dosage regimen.

Use in children

The drug is used according to the indications, in the recommended form of release and in doses taking into account the age of the patient. Contraindicated in children under 6 months (for oral administration).

special instructions

Treatment with fluconazole should be continued until the appearance of clinical-hematologic remission. Premature termination of treatment leads to relapse.

Since fluconazole is excreted mainly by the kidneys, caution should be exercised in patients with renal insufficiency. With long-term treatment with fluconazole, dosing should be performed taking into account KK.

In rare cases, the use of Mycosyst was accompanied by a toxic effect on the liver, incl. and fatal, mainly in patients with serious concomitant diseases. It is necessary to monitor liver function. If there are signs of liver damage that may be associated with the use of fluconazole, the drug should be discontinued.

Against the background of taking the drug, patients had rare cases of development of exfoliative skin reactions, such as Stevens-Johnson syndrome and toxic epidermal necrolysis. Patients with AIDS and malignant neoplasms are more likely to develop severe skin reactions with many drugs. If the patient develops a superficial fungal infection of the rash during treatment, which can be associated with the use of fluconazole, the drug should be discontinued.If rashes appear in patients with invasive / systemic fungal infections, fluconazole should be carefully monitored and discarded when bullous lesions or erythema multiforme occur.

It is necessary to monitor prothrombin time in patients simultaneously receiving fluconazole and indirect anticoagulants of the coumarin series.

Impact on the ability to drive vehicles and manage mechanisms

Patients should be careful when driving vehicles or when working with machinery, since dizziness may occur during fluconazole treatment.

Drug Interactions

Patients receiving Mikosist and indirect anticoagulants of the coumarin series need careful monitoring of prothrombin time, as it may increase.

Fluconazole, when taken concomitantly, can prolong the T1 / 2 derivatives of sulfonylureas, so when combined, the possibility of developing hypoglycemia should be considered.

Simultaneous use of Mycosyst and phenytoin may be accompanied by an increase in the concentration of phenytoin in a clinically significant degree, which requires a reduction in its dose.

The combined use of fluconazole and rifabutin is accompanied by an increase in the serum concentration of the latter, possibly the development of uveitis.

With the combined use of fluconazole and cyclosporine, it is recommended to monitor the concentration of the latter in the blood, as it may increase.

Given the occurrence of serious, life-threatening arrhythmias in patients taking antifungal agents - azole derivatives in combination with terfenadine, their joint administration is contraindicated.

With simultaneous administration of Mycosyst and cisapride, cases of unwanted reactions from the heart, including paroxysms of ventricular tachycardia, are described. Simultaneous reception is contraindicated.

When combined with fluconazole, an increase in the concentration of zidovudine in the blood plasma is possible. Patients receiving this combination should be observed to identify side effects of zidovudine.

The administration of fluconazole leads to a decrease in the average clearance rate of theophylline from the blood plasma, hence the risk of toxic theophylline and its overdose increases.

Simultaneous application of fluconazole and midazolam leads to a significant increase in the concentration of the latter in blood plasma and the risk of developing psychomotor reactions.

With the simultaneous administration of fluconazole and hydrochlorothiazide, the concentration of fluconazole in the blood plasma increases by 40%.

With the simultaneous administration of fluconazole and tacrolimus, the concentration of the latter in the serum increases, which leads to an increased risk of nephrotoxicity.

Analogues of the drug Mikosist

Structural analogs for the active substance:

• Vero Fluconazole;
• Disorel of Sanovel;
• Diflason;
• Diflucan;
• Mikonil;
• Medoflucon;
• Mycomomax;
• Mycoflucan;
• Nofung;
• Procanazole;
• Fangifflu;
• Flucosan;
• Flukoside;
• Flukomabol;
• Flucomycid;
• Fluconazole;
• Flukonorm;
• Flukoral;
• Flukorus;
• Flukoreem;
• Flucostat;
• Forkan;
• Fungolon;
• Ciscan.

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