Mycosyst capsules 150mg N2
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Active ingredients
Fluconazole
Release form
Capsules
Composition
Active ingredient: Fluconazole. Concentration of active ingredient (mg): 150 mg
Pharmacological effect
Capsules Mikosist is antifungal agent that prevents the reproduction of some fungi, destroys them. Capsules are intended for the treatment of fungal infections of internal organs, skin, nails and mucous membranes. Severe fungal (candidal) infections with whole-body involvement: the capsules are able to prevent fungal infections in those persons in whom the immune system is impaired or suppressed and unable to overcome fungal infections (eg: patients with AIDS after a bone marrow transplant). Cryptococcal infections of internal organs or the whole organism, as well as treatment of cryptococcal meningitis. Mikosist capsules are able to prevent the resumption of infections and the appearance of further infections in persons with suppressed immunity. Candida infections of the mucous membranes of the mouth, throat, esophagus, respiratory tract and urinary tract. Cutaneous mycoses, foot mycoses, for the treatment of which local preparations were not sufficient.
Pharmacokinetics
After oral administration, fluconazole is well absorbed, its bioavailability is 90%. Tmax after ingestion on an empty stomach 150 mg is 0.5–1.5 hours, and Cmax is 90% of the concentration in plasma when intravenously administered at a dose of 2.5–3.5 mg / kg. Simultaneous food intake does not affect the absorption of the drug taken orally. Plasma concentrations are directly proportional to dose. 90% Css is achieved by the 4–5th day of drug treatment (when taken 1 time per day). The use of the dose on the first day, 2 times the usual daily dose, allows to reach the concentration of fluconazole in plasma equal to 90% of the Css value by the 2nd day. The apparent Vd is close to the total water content in the body. Plasma protein binding - 11–12%. Fluconazole penetrates well into all biological fluids of the body. In the stratum corneum of the epidermis, dermis and sweat fluid, high concentrations are reached that exceed the serum levels. After ingestion of 150 mg on the 7th day, the concentration in the stratum corneum of the skin is 23.4 mcg / g, and 1 week after the second dose is taken - 7.1 mcg / g; concentration in the nails after 4 months of application at a dose of 150 mg 1 time per week - 4.05 mcg / g in healthy and 1.8 mcg / g in the affected nails.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 content of fluconazole in the cerebrospinal fluid reaches 80% of its concentration in plasma. Constant values in the vaginal secretion are reached 8 hours after ingestion and are held at this level for at least 24 hours. It is an inhibitor of the CYP2C9 isoenzyme in the liver. The pharmacokinetics of fluconazole significantly depends on the functional state of the kidneys, and there is an inverse relationship between T1 / 2 and creatinine clearance. T1 / 2 fluconazole is about 30 hours. Fluconazole is excreted mainly by the kidneys; approximately 80% of the administered dose is excreted by the kidneys in unchanged form, 11% in the form of metabolites. Fluconazole clearance is proportional to creatinine clearance. No metabolites of fluconazole were detected in the peripheral blood. After hemodialysis for 3 hours, plasma concentration of fluconazole is reduced by 50%.
Indications
Cryptococcosis, including cryptococcal meningitis and other localizations of this infection (including the lungs, skin), both in patients with a normal immune response and in patients with various forms of immunosuppression (including in AIDS patients, with organ transplantation) . The drug can be used to prevent cryptococcal infection in patients with AIDS, generalized candidiasis, including candidaemia, disseminated candidiasis, and other forms of invasive candidal infection (including infections of the peritoneum, endocardium, eyes, respiratory and urinary tract). Treatment can be carried out in patients with malignant neoplasms, patients in intensive care units, patients receiving cytotoxic or immunosuppressive agents, as well as 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 oral candidiasis associated with wearing dentures), esophagus, non-invasive bronchopulmonary infections, candiduria, candidiasis of the skin. prevention of recurrent oropharyngeal candidiasis in AIDS patients, genital candidiasis: vaginal candidiasis (acute and chronic recurrent), prophylactic use to reduce the frequency of recurrences of vaginal candidiasis (3 or more episodes per year).Candida balanitis, prevention of fungal infections in patients with malignant tumors that are prone to such infections as a result of cytotoxic chemotherapy or radiation therapy, skin mycoses, including mycoses of the feet, body, inguinal region, pityrias, psoriasis, onychomycosis, and candidosis of the skin, deep endemic mycoses, coccidioidomycosis , paracoccidioidomycosis, sporotrichosis and histoplasmosis in patients with normal immunity.
Contraindications
Simultaneous intake of terfenadine or astemizole and other drugs that extend the QT interval, children up to 6 months (for oral administration), increased sensitivity to the drug or azole compounds similar in structure.
Precautionary measures
In the presence of sensitivity to lactose (milk sugar), it is necessary to take into account that the capsules contain anhydrous lactose: Mikosist 50 mg capsules: 49.5 mg of anhydrous lactose in one capsule Mikosist capsules 100 mg: 99.0 mg of anhydrous lactose in one capsule Mikosist capsules 150 mg : 148.5 mg anhydrous lactose in one capsule. If your doctor warns you about the presence of intolerance to some sugars, consult your doctor before starting a course of therapy with Mikosist capsules.
Use during pregnancy and lactation
Before taking any medication, consult your doctor or pharmacist. Mikosist capsules can be given to pregnant women only if they have severe fungal infections that require immediate treatment. During pregnancy, mono capsules should be used only as prescribed by a doctor, in the dose determined by the doctor and the duration of therapy. Fluconazole passes into the mother's milk, so if necessary, Mycosist therapy during breastfeeding, feeding should be suspended.
Dosage and administration
Adults with cryptococcal meningitis and cryptococcal infections of another location are prescribed 400 mg on the first day, and then continue treatment at a dose of 200-400 mg 1 will dissolve. The duration of treatment of cryptococcal infections depends on the clinical efficacy confirmed by mycological research. with cryptococcal meningitis, the therapy is usually continued for at least 6-8 weeks. To prevent the recurrence of cryptococcal meningitis in AIDS patients, after completing the full course of primary treatment, therapy with fluconazole at a dose of 200 mg / day can be continued for a very long time.With candidemia, disseminated candidiasis and other invasive candidal infections, the dose averages 400 mg on the first day, and then 200 mg / day. With insufficient clinical efficacy, the dose may be increased to 400 mg / day. The duration of therapy depends on the clinical effectiveness. When oropharyngeal candidiasis drug is prescribed, on average, 50-100 mg 1 will be distributed. the duration of therapy is 7-14 days. If necessary, in patients with a pronounced decrease in immunity, treatment may be longer. In case of atrophic oral candidiasis associated with the wearing of dentures, the drug is prescribed in an average dose of 50 mg 1 will be distributed within 14 days in combination with local antiseptic agents for the treatment of the prosthesis. For other candidal infections of the mucous membranes (except for genital candidiasis), for example, esophagitis, non-invasive bronchopulmonary lesions, candiduria, candidiasis of the skin and mucous membranes, the effective dose averages 50-100 mg / day with a duration of treatment of 14-30 days. For the prevention of recurrence of oropharyngeal candidiasis in AIDS patients after the completion of the full course of primary therapy, fluconazole may be prescribed 150 mg 1 razned. In vaginal candidiasis, fluconazole is taken once orally at a dose of 150 mg. To reduce the frequency of recurrences of vaginal candidiasis, the drug can be used in a dose of 150 mg 1 size. The duration of therapy is determined individually. it varies from 4 to 12 months. Some patients may need more frequent use. When balanitis caused by Candida, fluconazole is administered once at a dose of 150 mg orally. For the prevention of candidiasis, the recommended dose of fluconazole is 50-400 mg 1, depending on the degree of risk of developing a fungal infection. If there is a high risk of generalized infection, for example, in patients with expected severe or prolonged neutropenia, the recommended dose is 400 mg 1 per day. Fluconazole is prescribed a few days before the expected appearance of neutropenia. after increasing the number of neutrophils over 1000 mcl, the treatment is continued for another 7 days. In case of mycoses of the skin, including mycoses of the feet, smooth skin, inguinal area and skin candidiasis, the recommended dose is 150 mg for 1 week or 50 mg for 1 time.The duration of therapy in normal cases is 2-4 weeks, however, with mycoses of the feet, longer therapy may be required (up to 6 weeks). With pityriasis herpes, the recommended dose is 300 mg 1 time. within 2 weeks. some patients require a third dose of 300 mg. while in some cases it is enough to take a single dose of the drug in a dose of 300-400 mg. An alternative treatment regimen is the use of the drug in 50 mg 1 dose within 2-4 weeks. In onychomycosis, the recommended dose is 150 mg 1 time. Treatment should be continued until the infected nail is replaced (the uninfected nail grows). Normally, it takes 3-6 months and 6-12 months, respectively, to re-grow nails on the fingers and feet. With deep endemic mycoses, it may be necessary to use the drug in a dose of 200-400 mg / day for up to 2 years. The duration of therapy is determined individually. it is 11-24 months for coccidioidomycosis, 2-17 months for paracoccidioidomycosis, 1-16 months for sporotrichosis and 3-17 months for histoplasmosis. In children, as with similar infections in adults, the duration of treatment depends on the clinical and mycological effect. In children, the drug should not be used in a daily dose in excess of that in adults. The drug is used daily 1 rassut. For the treatment of generalized candidiasis and cryptococcal infection, the recommended dose is 6-12 mgggsut depending on the severity of the disease. For the prevention of fungal infections in children with reduced immunity, in whom the risk of developing an infection is associated with neutropenia, developing as a result of cytotoxic chemotherapy or radiation therapy, the drug is prescribed at 3–12 mg mg / day depending on the severity and duration of induced neutropenia. For candidiasis of the mucous membranes, the recommended dose of fluconazole is 3 mgggsut. On the first day, a loading dose of 6 mgkg can be administered in order to more quickly achieve constant equilibrium concentrations. When prescribing a solution of dinfusion to newborns, it should be taken into account that fluconazole is eliminated more slowly, therefore, in the first 2 weeks of life, the drug is prescribed in the same dose (based on mg / g body weight) as older children, but with an interval of 72 hours. 3 and 4 weeks of life the same dose is administered at intervals of 48 hours.In children with impaired renal function, the daily dose of the drug should be reduced (in the same proportional relationship as in adults) in accordance with the severity of renal failure. In elderly patients, in the absence of signs of renal failure, the usual dosing regimen of the drug should be followed. Correction of the dosage regimen is required for patients with renal insufficiency (CK less than 50 ml min). Fluconazole is excreted mainly in the urine unchanged. When taken once a dose change is not required. When reappointment to patients with impaired renal function, you should enter the loading dose from 50 mg to 400 mg. With KK more than 50 mlmin average recommended dose of the drug. with QA from 11 to 50 mlmin, a dose of 50% of the recommended dose is applied. Patients who are regularly on hemodialysis, a single dose of the drug is administered after each hemodialysis session. Rules for the introduction of the solution for infusion. Fluconazole in the form of a solution for infusion is administered intravenously at a rate of not more than 20 mg (10 ml) per minute. When translating from the introduction of the capsule to receive capsules and vice versa, there is no need to change the daily dose of the drug. The solution for infusion is compatible with the following solutions: 20% dextrose solution (glucose), Ringer's solution, Hartmann solution, potassium chloride solution in dextrose, sodium bicarbonate solution 4. 2%, 0. 9% sodium chloride solution. Fluconazole infusions can be performed using conventional transfusion kits using one of the above fluids.
Side effects
On the part of the digestive system: nausea, vomiting, flatulence, abdominal pain, diarrhea. rarely, liver dysfunction (hyperbilirubinemia, increased activity of liver enzymes ALT, AST, ALP). CNS: headache. rarely convulsions. From the hematopoietic system: rarely - leukopenia, thrombocytopenia, neutropenia, agranulocytosis. Allergic reactions: skin rash. rarely, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), anaphylactoid reactions. Other: rarely - impaired renal function, alopecia, hypercholesterolemia, hypertriglyceridemia, hypokalemia.
Overdose
Symptoms: nausea, vomiting, diarrhea; in severe cases, convulsions, hallucinations, paranoid behavior may occur. Treatment: symptomatic (gastric lavage, forced diuresis, hemodialysis). After a 3-hour hemodialysis session, the concentration of fluconazole in the blood plasma decreases by approximately 50%.
Interaction with other drugs
Be sure to inform the doctor and pharmacist about the used and recently applied other drugs, including drugs that are sold without a doctor's prescription. Be sure to inform your doctor if you are taking any of these groups of drugs: anticoagulants (coumarin derivatives), antidiabetic agents (for the treatment of diabetes mellitus) (eg: chlorpropamid, glibenclamide, glipizide, and tolbutamide), diuretics used to force urine output and to reduce blood pressure (eg: hydrochlorothiazide), phenytoin for the treatment of epilepsy, rifampicin or rifabutin (antibiotics), midazolam, triazolam (hypnotics, sedatives), atorvastatin, simvastatin (drugs that reduce the level of blood cholesterol), nifedipine, nicardipine (for treating hypertension), cyclosporin or tacrolimus (drugs acting on the immune system), theophylline (for treating bronchial asthma), zidovudine or azidothymidine (AZT) (for treating AIDS), amitriptyline ( for the treatment of depression), losartan (for the treatment of hypertension). The simultaneous use of Mikosist capsules with food or beverages: Food does not affect the absorption of the active substance from Mikosist capsules. Mikosist capsules can be taken regardless of the meal.
special instructions
The effect of the drug on the ability to control the car and working mechanisms. According to experience, the reception of Mikosist capsules in all likelihood does not affect the ability to drive vehicles and control the working mechanisms.