Fluconazole-Stad capsule 150g N1
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Active ingredients
Fluconazole
Release form
Capsules
Composition
Fluconazole 150 mg; Excipients: lactose, pregelatinized starch, low molecular weight polyvinylpyrrolidone, magnesium stearate, croscarmellose sodium.
Pharmacological effect
Antifungal
Pharmacokinetics
After oral administration, fluconazole is well absorbed, food intake does not affect the rate of absorption of fluconazole, its bioavailability is 90%. The time to reach the maximum concentration after oral administration on an empty stomach 150 mg of the drug is 0.5-1.5 hours, Cmax is 90% of the concentration in plasma with a / in a dose of 2.5-3.5 mg / l. T1 / 2 of fluconazole is 30 hours. Communication with plasma proteins - 11–12%. Plasma concentration is directly dose dependent. 90% level of equilibrium concentration is achieved by the 4–5th day of drug treatment (when taken 1 time per day). Injection of a loading dose (on the first day), 2 times the usual daily dose, allows you to reach a concentration level corresponding to 90% equilibrium concentration , by the second day. Fluconazole penetrates well into all biological fluids of the body. The concentration of the active substance in breast milk, articular fluid, saliva, sputum and peritoneal fluid is similar to its plasma levels. Constant values in vaginal secretion are reached 8 hours after ingestion and are held at this level for at least 24 hours. Fluconazole penetrates well into the cerebrospinal fluid (CSF) - with fungal meningitis the concentration in CSF is about 85% of its plasma level. In the sweat fluid, epidermis and the stratum corneum (selective accumulation) concentrations exceeding the serum levels are achieved. 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. The volume of distribution is close to the total water content in the body. It is an inhibitor of the CYP2C9 isoenzyme in the liver. Excreted mainly by the kidneys (80% - unchanged, 11% - in the form of metabolites). Fluconazole clearance is proportional to creatinine clearance. There are no metabolites of fluconazole in the peripheral blood. Fluconazole pharmacokinetics significantly depends on the functional state of the kidneys, and there is an inverse relationship between the half-life and creatinine clearance. 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, in organ transplants ); The drug can be used for the prevention of cryptococcal infection in patients with AIDS, generalized candidiasis, including candidemia, disseminated candidiasis and other forms of invasive candidal infections (infections of the peritoneum, endocardium, eyes, respiratory and urinary tracts). Treatment can be carried out in patients with malignant neoplasms, patients in the intensive care unit, 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, including oral cavity and pharynx (including atrophic candidiasis of the oral cavity, associated with the wearing of dentures), esophagus, non-invasive bronchopulmonary candidiasis, candiduria, candidiasis of the skin; prevention of recurrent oropharyngeal candidiasis in patients with AIDS, 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); candidal balanitis; prevention of fungal infections in patients with malignant neoplasms 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; scaly varicolor, onychomycosis; skin candidiasis; deep endemic mycoses, including coccidioidomycosis, paracoccidioidomycosis, sporotrichosis, and histoplasmosis in patients with normal immunity.
Contraindications
Hypersensitivity to the drug (including to other azole antifungal drugs in history), simultaneous administration of terfenadine (against the background of continuous intake of fluconazole at a dose of 400 mg / day or more) or astemizole, as well as other drugs that extend the QT interval; children up to 4 years. With caution: hepatic and / or renal failure, the appearance of a rash against the background of the use of fluconazole in patients with surface fungal infection and invasive / systemic fungal infections,simultaneous administration of terfenadine and fluconazole at a dose of less than 400 mg / day, simultaneous administration of potentially hepatotoxic drugs, alcoholism, potentially arrhythmic conditions in patients with multiple risk factors (organic heart disease, electrolyte imbalance, simultaneous administration of drugs causing arrhythmias), pregnancy.
Use during pregnancy and lactation
The use of the drug in pregnant women is impractical, with the exception of severe or life-threatening forms of fungal infections, when the potential benefit of using fluconazole for the mother significantly exceeds the risk for the fetus.
Dosage and administration
Inside. Adults and children over 15 years old (weighing more than 50 kg) with cryptococcal meningitis and cryptococcal infections of other sites on the first day are usually prescribed 400 mg (8 capsules 50 mg each), and then continue treatment at a dose of 200 mg (4 capsules by 50 mg) - 400 mg (8 capsules 50 mg) 1 time per day. The duration of treatment for cryptococcal infections depends on the clinical efficacy confirmed by mycological examination; for cryptococcal meningitis, the treatment should be at least 6–8 weeks. To prevent the recurrence of cryptococcal meningitis in AIDS patients, after completing the full course of primary therapy, fluconazole is prescribed at a dose of 200 mg (4 capsules of 50 mg) per day for a long period of time In candidaemia, disseminated candidiasis and other invasive candidal infections in the first day, the dose is 400 mg (8 capsules 50 mg), and then 200 mg (4 capsules 50 mg) per day. With insufficient clinical efficacy, the dose of the drug can be increased to 400 mg (8 capsules of 50 mg) per day. The duration of therapy depends on the clinical efficacy. In oropharyngeal candidiasis, the drug is usually prescribed 150 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 longer. To prevent recurrence of oropharyngeal candidiasis in AIDS patients, after completing the full course of primary therapy, 150 mg once a week. In atrophic oral candidiasis,associated with the wearing of dental prostheses - 50 mg 1 time per day for 14 days in combination with local antiseptic drugs for the treatment of the prosthesis. At other localizations of candidiasis (except for genital), for example, esophagitis, non-invasive bronchopulmonary lesion, candidiasis, skin candidiasis and mucous membranes, etc., the effective dose is usually 150 mg / day with a duration of treatment of 14-30 days. 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 at a dose of 150 mg once a month. 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 orally once at a dose of 150 mg / day. For prevention of candidiasis, the recommended dose is 50–400 mg once a day, depending on the degree of risk of developing a fungal infection. For the prevention of candidiasis in patients with malignant tumors, the recommended dose of fluconazole is 150-400 mg 1 time per day, 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 / day. Fluconazole is prescribed a few days before the expected appearance of neutropenia; after increasing the number of neutrophils more than 1 thousand / μl, the treatment is continued for another 7 days. In mycoses of the skin, including mycoses of the feet, skin of the inguinal region, and candidiasis of the skin, the recommended dose is 150 mg once a week or 50 mg once a day, dosing regimen depends on the clinical and mycological effect. The duration of therapy in normal cases is 2–4 weeks, however, for mycoses of the feet, longer therapy (up to 6 weeks) may be required. For chitheriasis - 300 mg (2 capsules 150 mg) once a week for 2 weeks, some patients a third dose of 300 mg per week is required, while in some cases, a single dose of 300–400 mg is sufficient; An alternative treatment regimen is the use of 50 mg once a day for 2-4 weeks. In onychomycosis, the recommended dose is 150 mg once a week.Treatment should be continued until the infected nail is replaced (the uninfected nail grows). Normally, it takes 3–6 months 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 mg (4 capsules 50 mg each) - 400 mg (8 capsules 50 mg each). mg) per day for up to 2 years. The duration of therapy is determined individually; it can be 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 that would exceed that in adults, i.e. no more than 400 mg / day. The drug is used daily 1 time per day.
Side effects
From the digestive system: loss of appetite, changes in taste, abdominal pain, vomiting, nausea, diarrhea, flatulence, rarely - liver dysfunction (jaundice, hepatitis, gepatonekroz, hyperbilirubinemia, increased alanine aminotransferase activity, aspartate aminotransferase, increased alkaline phosphatase activity, hepatocellular necrosis ), including Severe. From the nervous system: headache, dizziness, excessive fatigue, rarely - convulsions. From the blood-forming organs: rarely - leukopenia, thrombocytopenia (bleeding, petechia), neutropenia, agranulocytosis. Allergic reactions: skin rash, rarely - multiforme, agranulocytosis. Allergic reactions: skin rash, rarely - multiforme, agranulocytosis. (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), anaphylactoid reactions (including angioedema, swelling of the face, urticaria, itchy skin). From the side of the cardiovascular system: an increase in lzhitelnosti interval QT, flicker / flutter zheludochkov.Prochie: rarely - renal dysfunction, 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 the plasma of oral hypoglycemic agents - sulfonylurea derivatives (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 keep 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, joint use of these drugs should monitor the concentration of phenytoin with the correction of its dose in order to maintain the level of the drug within the therapeutic interval. The combination with rifampicin leads to a decrease in AUC by 25% and shortening the plasma half-life of 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 (fluconazole intake in 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 to early detection of symptoms of overdose of theophylline, because Reception of fluconazole leads to a decrease in the average rate of clearance of theophylline from plasma. With simultaneous use of fluconazole with terfenadine and cisapride, cases of unwanted heart reactions are described, including paroxysmal ventricular tachycardia (torsades de points). Simultaneous use of fluconazole and hydrochlorothiazide can lead to an increase in fluconazole concentration. plasma by 40%. There are reports of the interaction of fluconazole and rifabutin, accompanied by an increase in serum levels of the latter. With simultaneous use of fluconazole and rifabutin, cases of uveitis are described.Patients receiving a combination of fluconazole and zidovudine should be carefully observed in patients receiving rifabutin and fluconazole at the same time. An increase in zidovudine concentration is observed, 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. which increases the risk of psychomotor effects (most pronounced when using fluconazole inward than in / in). It increases the concentration of tacrolimus, due to it increases the risk of nephrotoxicity.
special instructions
Treatment should continue until clinical and hematologic remission. Premature discontinuation of treatment leads to relapses. During treatment, it is necessary to monitor blood parameters, kidney and liver function. If a violation of the functions of the kidneys and liver occurs, the use of the drug should be discontinued. 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. 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. 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. Care should be taken while taking fluconazole with cisapride, rifabutin or other drugs metabolized by cytochrome P 450 system.