Mycomax capsules 150 mg 3 pieces
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Active ingredients
Fluconazole
Release form
Capsules
Composition
1 capsule contains the active substance: fluconazole 150 mg, excipients: lactose monohydrate; pregelatinized starch; colloidal silicon dioxide; magnesium stearate; sodium lauryl sulfate Ingredients; 150 mg capsules: Patent blue dye (E131), titanium dioxide (E171), gelatin, black ink (Attramentum nigrum) - shellac, ferric oxide black, n-butanol, industrial methylated alcohol, soy lecithin, antifoam DC 1510;
Pharmacological effect
Fluconazole, a representative of the class of triazole antifungal agents, is a potent selective inhibitor of sterol synthesis in the cell of fungi.; The drug is effective in opportunistic mycoses, including caused by Candida spp., Cryptococcus neoformans, Microsporum spp., Trichophyton spp. Fluconazole activity has also been shown on models of endemic mycoses, including infections caused by Blastomyces dermatitidis, Coccidiodes immitis and Histoplasma capsulatum .;
Pharmacokinetics
After oral administration, fluconazole is well absorbed, its bioavailability is 90%. Cmax after ingestion on an empty stomach at a dose of 150 mg is 90% of the content in plasma with a / in a dose of 2.5-3.5 mg / l. Simultaneous food intake does not affect the absorption of the drug taken orally. Cmax in plasma is reached in 0.5–1.5 h after administration. Fluconazole T1 / 2 is about 30 h. Plasma concentrations are directly proportional to dose. 90% level of equilibrium concentration is achieved by 4–5 days of drug treatment (when taken 1 time / day) .; The administration of a loading dose (on the first day), 2 times higher than the usual daily dose, allows you to reach a level corresponding to 90% equilibrium concentration, to the second day. The apparent volume of distribution 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. Concentrations of the drug in saliva and sputum are similar to its plasma levels. In patients with fungal meningitis, the content of fluconazole in the cerebrospinal fluid reaches 80% of its plasma level. In the stratum corneum, epidermis, dermis and sweat fluid, high concentrations are reached that exceed the serum levels. Fluconazole is excreted mainly by the kidneys approximately 80% of the administered dose is excreted in the urine unchanged. Fluconazole clearance is proportional to creatinine clearance. No metabolites of fluconazole were detected in the peripheral blood;
Indications
Cryptococcosis, including cryptococcal meningitis and other localizations of this infection (including in the lungs, on the skin), both in patients with a normal immune response, and with various forms of immunosuppression (including in AIDS patients, during 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 candidal infections (peritoneal, endocardial, eye, respiratory and urinary tract infections); Candiduria,. Treatment can be carried out in patients with malignant neoplasms, patients of intensive care units, patients undergoing a course of cytostatic or immunosuppressive therapy, as well as in the presence of other factors predisposing to the development of candidiasis; mucosal candidiasis, incl. oral cavity and pharynx (including atrophic candidiasis of the oral cavity associated with the wearing of dentures), esophagus, non-invasive bronchopulmonary candidiasis; prevention of recurrence of oropharyngeal candidiasis in AIDS patients; genital candidiasis: vaginal candidiasis (acute and chronic recurrent), prophylactic use in order to reduce the frequency of recurrences of vaginal candidiasis (3 or more episodes per year); candidal balanitis; prevention of fungal infections in patients with malignant neoplasms, which are predisposed to such infections as a result of chemotherapy with cytostatics or radiation therapy; mycoses of the skin, including mycoses of the feet, body, inguinal region, pityriasis versicolor, onychomycosis; skin candidiasis; deep endemic mycoses, including coccidioidomycosis, paracoccidioidomycosis, sporotrichosis and histoplasmosis in patients with normal immunity;
Contraindications
Hypersensitivity to the drug or similar azole compounds in structure; co-administration of terfenadine or astemizole and other drugs that prolong the QT interval; children's age (up to 3 years) .; With caution: hepatic and / or renal failure, concomitant use of potentially hepatotoxic drugs, alcoholism;
Use during pregnancy and lactation
Use of the drug in pregnant women is inappropriate, with the exception of severe or life-threatening forms of fungal infections, if the intended effect exceeds the possible risk to the fetus. Fluconazole is in breast milk at the same concentration as in plasma, therefore its administration during lactation is not recommended;
Dosage and administration
Inside.; For adults with cryptococcal meningitis and cryptococcal infections of other sites, 400 mg is usually prescribed on the first day, and then continue treatment at a dose of 200–400 mg 1 time / day. The duration of treatment for cryptococcal infections depends on the clinical efficacy confirmed by mycological examination; with cryptococcal meningitis, it 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, fluconazole is prescribed at a dose of 200 mg / day. over a long period of time. With candidemia, disseminated candidiasis and other invasive candidal infections, the dose is usually 400 mg on the first day, and then 200 mg each. With insufficient clinical efficacy, the dose of the drug may be increased to 400 mg / day. The duration of therapy depends on the clinical efficacy. In case of oropharyngeal candidiasis, the drug is usually prescribed 50–100 mg 1 time per day; the duration of treatment is 7–14 days. If necessary, in patients with a pronounced decrease in immunity, treatment may be more prolonged. In case of atrophic oral candidiasis associated with the wearing of dentures, fluconazole is usually prescribed 50 mg 1 time per day. for 14 days in combination with local antiseptics for the treatment of the prosthesis.; At other sites of candidiasis (except genital candidiasis), for example, esophagitis, non-invasive bronchopulmonary lesions, candiduria, candidiasis of the skin and mucous membranes, etc., the effective dose is usually makes 50–100 mg / days with a duration of treatment of 14–30 days. To prevent recurrence of oropharyngeal candidiasis in patients with AIDS, after completing a full course of primary therapy, the drug can be administered 150 mg once a week. In vaginal candidiasis, fluconazole is taken once orally in a dose of 150 mg. To reduce the frequency of recurrences of vaginal candidiasis, the drug can be used at a dose of 150 mg 1 time per month. The duration of therapy is determined individually; it varies from 4 to 12 months. Some patients may need more frequent use.; For Candida-induced balanitis, fluconazole is administered once daily at a dose of 150 mg orally. For the prevention of candidiasis, the recommended dose of fluconazole is 50-400 mg 1 time / day, depending on the 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 time / day. Fluconazole is prescribed a few days before the expected appearance of neutropenia; after an increase in the number of neutrophils of more than 1000 / mm3, the treatment is continued for another 7 days. With mycoses of the skin, including mycoses of the feet, skin of the inguinal region, and skin candidiasis, the recommended dose is 150 mg once a week or 50 mg 1 time / day. 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) .; For pityaisea - 300 mg once a week for 2 weeks, some patients need a third dose of 300 mg per week, while in some cases a single dose of 300–400 mg is sufficient; An alternative treatment regimen is the use of 50 mg 1 time per day for 2-4 weeks. For onychomycosis, the recommended dose is 150 mg 1 time per week. Treatment should be continued until the infected nail is replaced (the uninfected nail grows). Normally, it takes 3–6 and 6–12 months to re-grow nails on the fingers and feet, respectively. For deep endemic mycoses, you may need to use the drug at a dose of 200–400 mg / day. for a period of up to 2 years. The duration of therapy is determined individually; it may be 11-24 months with coccidioidomycosis; 2-17 months - with paracoccidioidomycosis; 1–16 months - with sporotrichosis and 3–17 months - with 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 that would exceed that in adults. The drug is used daily 1 time / day. When mucosal candidiasis, the recommended dose of fluconazole is 3 mg / kg / day. On the first day, a loading dose of 6 mg / kg can be given in order to achieve constant equilibrium concentrations more quickly.; For the treatment of generalized candidiasis or cryptococcal infection, the recommended dose is 6–12 mg / kg / day, depending on the severity of the disease. 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 for 3-12 mg / kg / day.depending on the severity and duration of preservation of induced neutropenia. In children with impaired renal function, the daily dose of the drug should be reduced (in the same proportion as in adults) in accordance with the severity of renal failure.; In elderly patients in the absence of disorders renal function should follow the usual dosage regimen of the drug. Patients with renal insufficiency (Cl creatinine - <50 ml / min) should be adjusted as indicated below.; Use of the drug in patients with impaired renal function; Fluconazole is excreted mainly in the urine unchanged. When taken once a dose change is not required. When you reappoint the drug in patients with impaired renal function, you must first enter the loading dose from 50 to 400 mg. If Cl creatinine is> 50 ml / min, the usual dose of the drug is applied (100% of the recommended dose). With Cl creatinine from 11 to 50 ml / min, a dose of 50% is recommended. Patients who are regularly on dialysis, a single dose of the drug is used after each session of hemodialysis;
Side effects
On the part of the digestive system: changes in taste, vomiting, nausea, diarrhea, flatulence, abdominal pain, rarely - abnormal liver function (jaundice, hepatitis, hepatonecrosis, hyperbilirubinemia, increased activity of ALT, AST, ALP); From the nervous system: headache , dizziness, rarely - convulsions. From the side of hematopoietic organs: 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: hallucinations, paranoid behavior.; Treatment: symptomatic, gastric lavage, forced diuresis. Hemodialysis for 3 hours reduces plasma concentration by approximately 50% .;
Interaction with other drugs
With the use of fluconazole with warfarin, PV increases (on average by 12%). In this regard, it is recommended to closely monitor the performance of PV in patients receiving the drug in combination with coumarin anticoagulants. Fluconazole increases the half-life from plasma of oral hypoglycemic agents derived from sulfonylurea (chlorpropamide, glibenclamide, glipizide, tolbutamide) in healthy people.The combined use of fluconazole and oral hypoglycemic agents in patients with diabetes is allowed, but the physician must bear in mind the possibility of developing hypoglycemia. Simultaneous use of fluconazole and phenytoin can lead to an increase in plasma phenytoin concentration to a clinically significant degree. Therefore, if necessary, the joint use of these drugs need to monitor the concentration of phenytoin with the correction of its dose in order to maintain the level of the drug within the therapeutic interval. Combination with rifampicin leads to a decrease in AUC by 25% and shortening T1 / 2 of plasma fluconazole by 20%. Therefore, it is advisable to increase the dose of fluconazole in patients receiving rifampicin at the same time. It is recommended to monitor the concentration of cyclosporine in the blood of patients receiving fluconazole, since the use of fluconazole and cyclosporine in patients with a transplanted kidney (when taking fluconazole at a dose of 200 mg / day) leads to a slow increase in plasma cyclosporine concentration. Patients who receive high doses of theophylline or who are likely to develop theophylline intoxication should be monitored for the purpose of early detection of symptoms of theophylline overdose, since receiving fluconazole leads to a decrease in the average rate of plasma clearance of theophylline from plasma. With simultaneous use of fluconazole and terfenadine, cisapride, cases of unwanted heart reactions are described, including paroxysmal ventricular tachycardia (torsades de pointes); Simultaneous use of fluconazole and hydrochlorothiazide may lead to an increase in concentration fluconazole in plasma by 40%; there are reports of the interaction of fluconazole and rifabutin, accompanied by an increase in serum levels of the latter. With the simultaneous use of fluconazole and rifabutin, cases of uveitis are described. Patients receiving rifabutin and fluconazole at the same time should be carefully observed. In patients receiving the combination of fluconazole and zidovudine, there is an increase in the concentration of zidovudine, which is caused by a decrease in the conversion of the latter to its main metabolite, therefore, an increase in side effects of zidovudine is to be expected;
special instructions
In rare cases, the use of fluconazole was accompanied by toxic changes in the liver, including fatal, mainly in patients with serious concomitant diseases. In the case of hepatotoxic effects associated with fluconazole, they are not markedly dependent on the total daily dose, duration of therapy, sex and age of the patient. The hepatotoxic effect of fluconazole has usually been reversible; his symptoms disappeared after cessation of therapy. When clinical signs of liver damage appear that may be associated with fluconazole, the drug should be discontinued. AIDS patients are more likely to develop severe skin reactions with the use of many drugs. In cases where a rash develops in patients with a surface fungal infection and is regarded as definitely associated with fluconazole, the drug should be discontinued. When a rash appears in patients with invasive / systemic fungal infections, they should be carefully monitored and fluconazole should be canceled when there is a bullous change or erythema multiforme.