Instructions for Mycosyst
Pharmacological properties Mycosyst Tablet:
Fluconazole (2- (2,4-difluorophenyl) -1,3-bis (1P-1,2,4-triazol-1-yl) -2-propanol) is an antifungal drug belonging to the group of bis- triazoles. The mechanism of antifungal action is due to the ability to disrupt the biosynthesis of ergosterol, which is necessary for building the cell membrane of fungi. It is effective for systemic infections caused by fungi of the genus Candida and Cryptococcus neoformans, Histoplasma capsulatum, Blastomyces dermatitidis, Coccidioides immitis , fungi of the genus Microsporum and Trichophyton.
The pharmacokinetics of Mycosyst when administered orally and intravenously are the same. Well absorbed after oral administration. The intake of food, antacids does not affect the absorption of fluconazole . Bioavailability is 90%. The maximum concentration in blood plasma Mycosyst after oral administration is reached after 1-2 hours, the half-life is about 30 hours. Simultaneous food intake does not affect the absorption of the drug, 90% of the equilibrium concentration level is reached by the 4-5th day of treatment (when taken 1 time per day). On the 1st day of treatment, the administration of a loading(2 times the usual daily dose) by the 2nd day allows reaching a level corresponding to 90% of the equilibrium concentration. 11-12% of the drug binds to blood plasma proteins .It easily penetrates into the biological fluids of the body and through the BBB, so it can be effectively used for intracranial infections. With meningitis caused by fungi, the concentration of the drug in the cerebrospinal fluid reaches approximately 80% of the level in the blood plasma. Concentrations of fluconazole in saliva and sputum are similar to those in blood plasma. Higher concentrations are achieved in all layers of the skin than in blood serum. Fluconazole accumulates in the stratum corneum. When taken in a dose of 50 mg once a day, the concentration of Mycosyst after 12 days of treatment is 73 μg / g, and after 7 days after stopping treatment - 5.8 μg / g; when taken in a quantity of 150 mg once a week, the concentration of fluconazolein the stratum corneum on the 7th day is 23.4 μg / g, and 7 days after taking the second quantity - 7.1 μg / g. After 4 months of application at a dose of 150 mg once a week, the concentration of fluconazole is 4.05 μg / g in healthy and 1.8 μg / g in affected nails. 6 months after the end of therapy, fluconazole is still detected in the nails. It is excreted mainly in the urine (about 80% of the administered dose unchanged, 11% in the form of metabolites). The long half-life of fluconazole makes it possible to prescribe it once for vaginal candidiasis and take it once a day or once a week for course use for other indications.
Indications Mycosyst:
- Systemic candidiasis - candidemia
- disseminated candidiasis (endocardium, abdominal organs, respiratory tract, genitourinary system, eyes)
- mucosal candidiasis - oropharyngeal
- non-invasive bronchopulmonary and esophageal
- candiduria
- chronic atrophic oral candidiasis (thrush caused by dentures
- acute or recurrent vaginal candidiasis
- prophylactic use to reduce the frequency of recurrence of vaginal candidiasis (≥3 episodes per year); candidal balanitis
- candidiasis of the skin
- Diseases caused by dermatophytes, with the ineffectiveness of topical application of antifungal agents: mycoses of the feet, trunk, lower leg, pityriasis versicolor, onychomycosis.
- Endemic mycoses: coccidioidomycosis, paracoccidioidomycosis, sporotrichosis and histoplasmosis in patients with normal immune status.
- Systemic lesions caused by fungi of the genus Cryptococcus , in particular mycoses of the respiratory tract, skin and mucous membranes, cryptococcal meningitis; prevention of relapses of cryptococcal infection in AIDS patients.
- Prevention of mycoses in patients receiving cytostatic or radiation therapy.
- For the treatment of patients who have undergone organ transplantation and receive antibiotics, cytostatic and immunosuppressive therapy, or in the case when there is a risk of infection with fungi for other reasons.
Mycosyst Uses:
Inside or in the form of intravenous infusion Mycosyst (maximum injection rate - 10 ml / min), depending on the patient's condition. The daily dose does not change depending on the route of administration. 100 ml of infusion solution contains 200 mg of fluconazole , 0.9% sodium chloride solution .
Intravenous infusion is compatible with the following infusion solutions: 20% glucose solution, Ringer's solution, potassium chloride solution in glucose (composition: in 1000 ml of water for injection - 3.8 g of potassium chloride , 33.75 g anhydrous glucose, 5 g of 0.1-N hydrochloric acid), sodium bicarbonate solution (composition: 1000 ml of water for injection - 13 g of sodium bicarbonate), isotonic sodium chloride solution .
For adults, Fluconazole the daily dose is determined individually, taking into account the nature and severity of the infection. Treatment continues until clinical and hematological remission (with the exception of acute vaginal candidiasis, which is usually cured with a single amount of 150 mg). Premature discontinuation of treatment Mycosyst leads to relapse. Cryptococcal meningitis in AIDS patients, as well as recurrent oropharyngeal candidiasis, usually require long-term treatment Mycosyst.
For candidemia, disseminated candidiasis and other invasive forms of candidiasis, Mycosyst is usually prescribed at a dose of 400 mg on the 1st day of therapy, and then 200 mg / day. Depending on the clinical picture, the daily dose can be increased to 400 mg. The duration of treatment depends on the patient's condition.
For cryptococcal meningitis and other cryptococcal infections, 400 mg Mycosyst is prescribed on the 1st day, then 200–400 mg once a day. The duration of the course of treatment depends on the clinical and mycological picture, and in case of cryptococcal meningitis, it should be at least 6–8 weeks. For the prevention of cryptococcal meningitis in AIDS patients, after treatment, 200 mg / day can be prescribed continuously.
With oropharyngeal candidiasis, the daily amount Mycosyst is 50–100 mg for 7–14 days. For patients with severe immunodeficiency conditions, the drug can be prescribed for a longer period. With atrophic candidiasis of the oral cavity, the usual daily dose is 50 mg for 14 days with simultaneous local treatment. For other candidiasis of the mucous membranes, for example, with esophagitis, non-invasive bronchopulmonary candidiasis, candiduria, mucocutaneous candidiasis, it is usually prescribed in a dose of 50-100 mg / day for 14-30 days. For severe lesions of the mucous membranes caused by fungi of the genus Candida, the daily dose can be increased to 100 mg.
To prevent relapse of candidiasis in patients with reduced immunity, the drug Mycosyst is prescribed in a daily dose of 50-400 mg.
With mycoses of the feet, trunk, lower leg caused by dermatophytes, and candidiasis of the skin, the recommended is 150 mg once a week or 50 mg / day. Treatment is carried out within 2-4 weeks, but with mycoses of the feet, a 6-week course may be required. For the treatment of pityriasis versicolor, the recommended is 50 mg / day for 2–4 weeks. With onychomycosis, the recommended is 150 mg once a week until the infected nail is completely replaced with a healthy one. The growth of a nail usually takes 3–6 months, while the growth of nails on the big toes takes a longer time - up to 6–12 months. The growth rate of nails is not the same; in old age it slows down.
For paracoccidioidomycosis, histoplasmosis, sporotrichosis, Mycosyst is used at a amount of 200–400 mg / day for 1–2 years. In coccidioidomycosis, the dose is determined individually and the treatment lasts 1–2 years.
In acute vaginal candidiasis, 150 mg of Mycosyst is used once. For chronic, often recurrent vaginal candidiasis, the course of treatment can be repeated: 150 mg / month for several months.
In renal failure, the amount should be reduced depending on the degree of dysfunction. With a single administration of the drug (vaginal candidiasis), the dose should not be changed. With continuous therapy, patients with reduced renal function should begin treatment with a loading dose of 50-400 mg. Then the frequency of use or dose is changed taking into account creatinine clearance:
For children , as well as for adults, Fluconazole the dose and duration of treatment are set individually, depending on the clinical and mycological effect. Fluconazole is used every day, once a day. The daily dose should not exceed the maximum adult dose.
With candidiasis of the mucous membranes on the 1st day, 6 mg / kg is prescribed, then 3 mg / kg / day. For systemic candidiasis or cryptococcal infection, the recommended amount is 6–12 mg / kg, depending on the severity of the disease.
For prophylactic purposes, children with neutropenia are prescribed the drug in a daily of 3–12 mg / kg.
In case of impaired renal function Mycosyst Uses, the daily amount for children should be reduced in accordance with the instructions for adults.
For children in the first weeks of life, the drug is prescribed in the same (in mg / kg) as for older children, but every 3 days, that is, with an interval of 72 hours, since Mycosyst is excreted slowly in newborns . For children aged 3-4 weeks, the same dose is used every 2 days, that is, with an interval of 48 hours.
Contraindications Mycosyst:
Absolute - hypersensitivity to fluconazole or other azole derivatives. During pregnancy, due to the lack of sufficient clinical experience in using the drug, the benefits and risks of treatment should be carefully compared, prescribing Mycosyst only for health reasons. Breastfeeding during the course of treatment with the drug is contraindicated. Children are treated only for health reasons in cases where there is no alternative treatment.
Side effects Mycosyst:
Nausea, vomiting, lower abdominal pain, flatulence, diarrhea, skin rash, headache. In some patients, especially those with a severe underlying disease (cancer, AIDS), kidney and liver damage, hematopoiesis disorders are possible, but their causal relationship with fluconazole intake has not been established.
Skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis, bullous rash, polymorphic erythema) are most likely in patients with acquired immunodeficiency states; if a skin rash develops, treatment with fluconazole should be discontinued. In AIDS patients taking fluconazole, noted seizures, leukopenia, thrombocytopenia and alopecia, however, a causal relationship with the drug intake has not been established. Like other azole derivatives, anaphylactic reactions may develop with fluconazole . If symptoms suggesting liver damage occur, fluconazole should be discontinued. The hepatotoxic effect of fluconazole is usually reversible; symptoms disappear after stopping therapy.
special instructions Mycosyst:
Treatment Mycosyst Uses can be started in the absence of mycological test results, but when they are obtained, an appropriate correction of fungicidal therapy is necessary.
100 ml of an infusion solution contains 15 mmol of Na + ions , which must be taken into account when treating patients who should limit sodium intake.
Interactions Mycosyst:
Despite the lack of data on chemical incompatibility, Mycosyst it is not recommended to mix the drug with other infusion solutions.
When used simultaneously with indirect anticoagulants, it can cause prolongation of prothrombin time (on average by 12%).
Fluconazole can inhibit the metabolism of oral antidiabetic drugs (sulfonylurea derivatives) with the development of hypoglycemia.
Thiazide diuretics can increase plasma levels of fluconazole by approximately 40%. Fluconazole can significantly increase the level of phenytoin in the blood plasma, therefore, when they are used simultaneously, the level of phenytoin in the blood should be monitored .
When fluconazole was administered to patients receiving rifampicin for a long time , the AUC for fluconazole decreased by 25%, and the half-life decreased by 20%, which may require an increase of the Mycosyst.
With the simultaneous use of Mycosyst with cyclosporine, it is recommended to control the level of cyclosporine in the blood plasma.
Fluconazole can reduce theophylline clearance by an average of 18%, which may require reduction of the latter.
Azole derivatives, when combined with terfenadine, can cause the development of arrhythmias.
With the simultaneous use of Mycosyst with cidovudine, it is possible to increase the AUC for the latter by 20–74%, which requires monitoring of its concentration in the blood.
Overdose Mycosyst:
The stomach is washed, symptomatic treatment is prescribed. Forced diuresis accelerates the renal excretion of the drug Mycosyst. Three-hour hemodialysis reduces the concentration of the drug in the blood plasma by approximately 50%.
