Flucostat capsules 150 mg 2 pcs
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Active ingredients
Fluconazole
Release form
Capsules
Composition
Active ingredient: Fluconazole (fluconazole) Active ingredient concentration (mg): 150 mg
Pharmacological effect
Antifungal medication. Fluconazole - a member of the class of triazole antifungal agents, is a powerful selective inhibitor of sterol synthesis in the cell of fungi. It is active against pathogens of opportunistic mycoses, including caused by Candida spp., Cryptococcus neoformans, Microsporum spp., Trichophyton spp. Fluconazole activity has also been shown in models of endemic mycoses, including infections caused by Blastomyces dermatitidis, Coccidioides immitis and Histoplasma capsulatum.
Pharmacokinetics
AbsorptionAfter ingestion, fluconazole is well absorbed. Bioavailability is 90%. Cmax of fluconazole in the blood plasma after ingestion on an empty stomach at a dose of 150 mg is 90% of its content in plasma when administered intravenously at a dose of 2.5-3.5 mg / l. Tmax is achieved 0.5-1.5 hours after administration. Simultaneous food intake does not affect absorption by ingestion. The concentration in plasma is directly proportional to the dose taken. The distribution of 90% Css is reached by 4-5 days of drug treatment (when taken 1 time / day). The administration of a loading dose (on day 1), 2 times the average daily dose, it allows to reach 90% Css level by the 2nd day. The apparent Vd is close to the total water content in the body. Binding to proteins - 11-12%. Fluconazole penetrates well into all biological fluids of the body. Fluconazole concentrations in saliva and sputum are similar to plasma concentrations. In patients with fungal meningitis, the concentration of spinal fluid in the cerebrospinal fluid is about 80% of its plasma levels. In the stratum corneum, epidermis, dermis and sweat fluid, high concentrations are reached that exceed the serum levels. Excretion of T1 / 2 is about 30 hours. the kidneys; approximately 80% of the administered dose is found unchanged in the urine. Clearance of fluconazole is proportional to QC. No metabolites of fluconazole were detected.
Indications
- cryptococcosis, including cryptococcal meningitis and other localizations of this infection (including lungs, skin), both in patients with a normal immune response, and in patients with various forms of immunosuppression (including in AIDS patients, during transplantation organs); the drug can be used for the prevention of cryptococcal infection in patients with AIDS - generalized candidiasis, including candidaemia, disseminated candidiasis, and other forms of invasive candidal infection (includinginfections of the peritoneum, endocardium, eyes, respiratory and urinary tract). The 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, incl. oral cavity and pharynx (including atrophic candidiasis of the oral cavity associated with the wearing of dental prostheses), esophagus, non-invasive bronchopulmonary infections, candiduria; prevention of recurrent oropharyngeal candidiasis in AIDS patients; genital candidiasis: treatment of 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 neoplasms that are predisposed to such infections as a result of cytotoxic chemotherapy or radiation therapy; Mycoses of the skin, including mycoses of the feet, body, inguinal region, pityrias, versicolor psoriasis, onychomycosis and skin candidiasis; Deep endemic mycoses, including coccidioidomycosis, paracoccidioidomycosis, sporotrichosis and histoplasmosis in patients with normal immunity.
Contraindications
- simultaneous administration of drugs that prolong the QT interval (including terfenadine or astemizole); - children up to 3 years; - hypersensitivity to the drug or azole compounds similar in structure. With caution, use the drug for hepatic and / or renal failure , while taking potentially dangerous hepatotoxic drugs, in alcoholism, in the case of proarrhythmic conditions in patients with multiple risk factors (organic heart disease, electrolyte disorders Balance is, concurrent medication, causing arrhythmias).
Precautionary measures
Care must be taken with the simultaneous use of fluconazole with cisapride, astemizole, rifabutin, tacrolimus, or other drugs metabolized by isoenzymes of the cytochrome P450 system.
Use during pregnancy and lactation
Use of Flucostat during pregnancy is possible only in the case of severe and potentially life-threatening fungal infections, when the expected benefit of treatment outweighs the possible risk to the fetus. Because fluconazole is excreted in breast milk at concentrations close to the plasma concentrations during breastfeeding, it is not recommended to prescribe the drug.
Dosage and administration
The drug is taken orally. Adults with cryptococcal meningitis and cryptococcal infections of another location on the first day, 400 mg is prescribed, and then continue the 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, 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 long time. In candidaemia, 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 efficacy. In oropharyngeal candidiasis, the drug is prescribed on average 50-100 mg 1 time / day; 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 dental prostheses, the drug is prescribed in an average dose of 50 mg 1 time / day for 14 days in combination with local antiseptic agents for the treatment of the prosthesis. In other localizations of candidiasis (with the exception of genital candidiasis), for example, esophagitis, non-invasive bronchopulmonary lesions, candiduria, candidiasis of the skin and mucous membranes, the effective dose is on average 50-100 mg / day with a duration of treatment of 14-30 days. To prevent recurrence of oropharyngeal candidiasis in AIDS patients, after completing the full course of primary therapy, fluconazole can be given 150 mg 1 time per week. For 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 time / month. The duration of therapy is determined individually; it varies from 4 to 12 months. Some patients may need more frequent use. For balanitis caused by Candida spp., Fluconazole is administered once at a dose of 150 mg orally. For 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 / μl, the treatment is continued for another 7 days. In mycoses of the skin, including mycoses of the feet, smooth skin, inguinal region and skin candidiasis, the recommended dose is 150 mg 1 time / 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 pitya versicolor the recommended dose is 300 mg 1 time / week. within 2 weeks; some patients require a third dose of 300 mg / week, while in some cases a single dose of 300-400 mg is sufficient. An alternative treatment regimen is the use of the drug at 50 mg 1 time / day for 2-4 weeks. In onychomycosis, the recommended dose is 150 mg 1 time / week. Treatment should be continued until the infected nail is replaced (the uninfected nail grows). For the re-growth of nails on the fingers and feet normally takes 3-6 months and 6-12 months, respectively. For deep endemic mycoses, you may need to use the drug in a dose of 200-400 mg / day for up to 2 years. The duration of treatment is determined individually and amounts to 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. Flucostat is used daily 1 time / day. In case of 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 treatment of generalized candidiasis and cryptococcal infection, the recommended dose is 6-12 mg / kg / day, depending on the severity of the disease. To prevent 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 / kg / day, depending on the severity and the 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 adults) in accordance with the severity of renal failure. In elderly patients, in the absence of renal impairment, the drug is used in accordance with with the usual dosing regimen. Patients with impaired renal function with a single dose do not need to change the dose of the drug. With repeated use of the drug in CC more than 50 ml / min, the drug is prescribed in the average dose. When QA is from 11 to 50 ml / min, you must first assign a loading dose of 50 mg to 400 mg, then a dose of 50% of the recommended dose. Patients who regularly undergo dialysis are prescribed a single dose of the drug after each hemodialysis session.
Side effects
On the part of the digestive system: change in taste, nausea, flatulence, vomiting, abdominal pain, diarrhea; rarely, liver dysfunction (jaundice, hepatitis, hepatonecrosis, hyperbilirubinemia, increased activity of ALT, AST, ALP). For the central nervous system: headache, dizziness; rarely - convulsions. From the hematopoietic system: rarely - leukopenia, thrombocytopenia, agranulocytosis. From the side of the cardiovascular system: an increase in the duration of the QT interval, flicker, ventricular flutter. Allergic reactions: skin rash; rarely, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), anaphylactoid reactions. On the metabolic side: rarely, hypercholesterolemia, hypertriglyceridemia, hypokalemia.
Overdose
Symptoms: hallucinations, paranoid behavior. Treatment: gastric lavage and symptomatic therapy is recommended. Since fluconazole is excreted in the urine, forced diuresis increases its excretion. Conducting hemodialysis for 3 h reduces the concentration of fluconazole in plasma by about 50%.
Interaction with other drugs
When using fluconazole with warfarin, an increase in prothrombin time was noted by 12%. In this regard, it is recommended to control the prothrombin time in patients receiving Flucostat in combination with coumarin anticoagulants. With simultaneous use of fluconazole, T1 / 2 increases oral hypoglycemic drugs - sulfonylurea derivatives (chlorpropamide, glybenclamide, glipizide and tolbutamide). The joint appointment of fluconazole and oral hypoglycemic drugs is allowed, but the possibility of hypoglycemia should be considered. Simultaneous use of fluconazole and phenytoin may be accompanied by an increase in the concentration of phenytoin in a clinically significant degree. Therefore, if necessary, the combined use of these drugs requires monitoring the concentration of phenytoin with the correction of its dose to ensure therapeutic plasma concentrations. Simultaneous use of fluconazole and rifampicin leads to a decrease in AUC by 25% and shortening T1 / 2 of fluconazole from plasma by 20%. Therefore, in patients receiving rifampicin at the same time, the dose of fluconazole is recommended to be increased. It is recommended to control the concentration of cyclosporine in the blood of patients receiving fluconazole, since when fluconazole and cyclosporine are used in patients with a transplanted kidney, fluconazole intake in a dose of 200 mg / day leads to a slow increase in plasma cyclosporine concentration. Patients who receive theophylline in high doses, or who are likely to develop theophylline intoxication, should be monitored with the purpose of early detection of symptoms of an overdose of theophylline, since co-administration of fluconazole leads to a decrease in the average rate of clearance of theophylline from plasma. With simultaneous use of fluconazole and terfenadine or cisapride, cases of unwanted heart reactions, including paroxysmal ventricular tachycardia (arrhythmias of pirouette type), are reported. levels of the latter.With the simultaneous use of fluconazole and rifabutin, cases of development of uveitis are described. Patients receiving concomitant rifabutin and fluconazole should be carefully monitored. With simultaneous use of fluconazole and zidovudine, there is an increase in plasma zidovudine concentration, which is caused by a decrease in the metabolism of the latter into its metabolite. .
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. There is no marked dependence of the frequency of development of the hepatotoxic effects of fluconazole on the total daily dose, duration of therapy, sex and age of the patient. The hepatotoxic effect of fluconazole is usually reversible; his symptoms disappeared after cessation of therapy. With the appearance of clinical signs of liver damage 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. When a rash appears in a patient receiving treatment for a superficial fungal infection, which can be 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 lesion or erythema multiforme.