Fluconazole capsules 150 mg 1 pc
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Active ingredients
Fluconazole
Release form
Capsules
Composition
1 capsule contains: Active ingredient: fluconazole 150 mg.
Pharmacological effect
Antifungal agent, a triazole derivative. It is a selective inhibitor of the synthesis of sterols in the cell of fungi. Fluconazole has a high specificity for fungal enzymes that are dependent on cytochrome P450. When taken orally and when i / v administration, fluconazole was active on various models of fungal infections in animals. Fluconazole is active in opportunistic mycoses, including caused by Candida spp., including generalized candidiasis in immunocompromised animals; Cryptococcus neoformans, including intracranial infections; Microsporum spp. and Trychoptyton spp. Active in models of endemic mycoses in animals, including infections caused by Blastomyces dermatitidis, Coccidioides immitis, including intracranial infections, and Histoplasma capsulatum in animals with normal and reduced immunity.
Pharmacokinetics
Fluconazole is well absorbed, its plasma levels (and total bioavailability) exceed 90% of plasma levels of fluconazole when administered intravenously and intravenously. Simultaneous ingestion does not affect absorption by ingestion. Cmax is achieved within 0.5-1.5 hours after ingestion of fluconazole on an empty stomach. Plasma concentration is proportional to the dose. 90% Css is reached by the 4-5th day after the start of therapy (with repeated administration of 1 time / day). The administration of the loading dose (on the 1st day), 2 times the average daily dose, allows you to reach a Css of 90% by the 2nd day. The apparent Vd is close to the total water content in the body. Plasma protein binding is low (11-12%). Fluconazole penetrates well into all body fluids. The levels of fluconazole in saliva and sputum are similar to its plasma concentrations. In patients with fungal meningitis, the levels of fluconazole in the cerebrospinal fluid make up about 80% of its levels in the blood plasma. In the stratum corneum, epidermis-dermis, and sweat fluid, high concentrations are reached that exceed the serum levels. Fluconazole builds up in the stratum corneum. When taken in a dose of 50 mg 1 time / day, the concentration of fluconazole after 12 days was 73 mcg / g, and 7 days after stopping treatment - only 5.8 mcg / g. When used in a dose of 150 mg 1 time / week.The concentration of fluconazole in the stratum corneum on the 7th day was 23.4 mcg / g, and 7 days after the second dose was taken - 7.1 mcg / g. The concentration of fluconazole in the nails after 4 months of use at a dose of 150 mg 1 time / week. amounted to 4.05 mcg / g in healthy and 1.8 mcg / g in affected nails; 6 months after completion of therapy, fluconazole was still detected in the nails. Fluconazole is excreted mainly by the kidneys; approximately 80% of the administered dose is detected in the urine unchanged. Clearance of fluconazole is proportional to QC. Circulating metabolites were not found. Long-lasting T1 / 2 from blood plasma allows you to take fluconazole once for vaginal candidiasis and 1 time / day or 1 time / week. with other indications.
Indications
Cryptococcosis, including cryptococcal meningitis and infections of other localization (for example, lungs, skin), including in patients with a normal immune response and in patients with AIDS, recipients of transplanted organs and patients with other forms of immunodeficiency; supportive therapy to prevent the recurrence of cryptococcosis in AIDS patients. Generalized candidiasis, including candidaemia, disseminated candidiasis and other forms of invasive candidal infection, such as infections of the peritoneum, endocardium, eyes, respiratory and urinary tract, including in patients with malignant tumors who are in ICUs and are receiving cytotoxic or immunosuppressive agents, as well as in patients with other factors predisposing to the development of candidiasis. Candidiasis of the mucous membranes, including mucous membranes of the oral cavity and pharynx, esophagus, non-invasive broncho-pulmonary infections, candiduria, skin - mucous and chronic atrophic candidiasis of the oral cavity (associated with the wearing of dental prostheses), including in patients with normal and suppressed immune function; prevention of recurrent oropharyngeal candidiasis in AIDS patients. Genital candidiasis; acute or recurrent vaginal candidiasis; prevention to reduce the frequency of recurrences of vaginal candidiasis (3 or more episodes per year); Candida balanitis. Mycoses of the skin, including mycoses of the feet, body, inguinal region, pityriasis versicolor, onychomycosis, and skin candidal infections. Deep endemic mycoses in patients with normal immunity, coccidioidomycosis, paracoccidioidomycosis, sporotrichosis, and histoplasmosis. predisposed to the development of such infections as a result of cytotoxic chemotherapy or radiation therapy.
Contraindications
The simultaneous use of terfenadine during repeated use of fluconazole at a dose of 400 mg / day or more; simultaneous use of cisapride; hypersensitivity to fluconazole; hypersensitivity to azole derivatives with a structure similar to fluconazole.
Precautionary measures
Application for violations of the liver, Fluconazole should be used with caution in patients with severely impaired liver function. Application of disorders of renal function Fluconazole should be used with caution in patients with severe impaired renal function. In case of impaired renal function, the dose of fluconazole should be reduced. Use in children It is contraindicated in children under 1 year.
Use during pregnancy and lactation
Adequate and controlled studies of the safety of fluconazole in pregnant women have not been conducted. Fluconazole should be avoided during pregnancy, except in cases of severe and potentially life-threatening fungal infections, when the expected benefit of treatment outweighs the possible risk to the fetus. Women of childbearing age should use reliable contraceptives during treatment. Fluconazole is determined in breast milk at concentrations close to plasma, so use during lactation (breastfeeding) is not recommended.
Dosage and administration
Individual. It is intended for oral and iv administration. For adults, depending on the indications, treatment regimen and clinical situation, the daily dose is 50-400 mg, the frequency of application is 1 time / day. For children, the dose is 3-12 mg / kg / day, the multiplicity of application - 1 time / day. In patients with impaired renal function, the dose of fluconazole is reduced depending on the CC. The duration of treatment depends on the clinical and mycological effect.
Side effects
On the part of the nervous system: headache, dizziness, convulsions, taste change. On the part of the digestive system: abdominal pain, diarrhea, flatulence, nausea, dyspepsia, vomiting, hepatotoxicity (including rare cases with fatal outcome), increased levels of alkaline phosphatase, bilirubin, serum aminotransferase levels (ALT and AST), abnormal liver function, hepatitis, hepatocellular necrosis, jaundice. From the side of the cardiovascular system: an increase in the QT interval on the ECG,flicker / fluttering of the ventricles. Dermatological reactions: rash, alopecia, exfoliative skin diseases, including Stevens-Johnson syndrome and toxic epidermal necrolysis. in plasma, hypokalemia. Allergic reactions: anaphylactic reactions (including angioedema, swelling of the face, urticaria, pruritus).
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 simultaneous use with warfarin, fluconazole increases the prothrombin time (by 12%), and therefore the development of bleeding (hematomas, bleeding from the nose and gastrointestinal tract, hematuria, melena) is possible. In patients receiving coumarin anticoagulants, it is necessary to constantly monitor the prothrombin time. After ingesting midazolam, fluconazole significantly increases midazolam concentration and psychomotor effects, and this effect is more pronounced after ingestion of fluconazole inside. If necessary, concomitant therapy with benzodiazepines of patients taking fluconazole should be monitored with the aim of appropriately reducing the dose of benzodiazepine. With the simultaneous use of fluconazole and cisapride, undesirable cardiovascular reactions are possible, including ventricular fibrillation / flutter (pirouette type arrhythmia). The use of fluconazole at a dose of 200 mg 1 time / day and cisapride at a dose of 20 mg 4 times / day leads to a pronounced increase in plasma concentrations of cisapride and an increase in the QT interval on the ECG. Simultaneous use of cisapride and fluconazole is contraindicated. In patients after kidney transplantation, the use of fluconazole at a dose of 200 mg / day leads to a slow increase in the concentration of cyclosporine. However, with repeated administration of fluconazole at a dose of 100 mg / day, no change in the concentration of cyclosporin in bone marrow recipients was observed. With simultaneous use of fluconazole and cyclosporine, it is recommended to monitor the concentration of cyclosporine in the blood. Repeated use of hydrochlorothiazide simultaneously with fluconazole leads to an increase in the concentration of fluconazole in plasma by 40%.The effect of this severity does not require a change in the dosage regimen of fluconazole in patients receiving diuretics at the same time, but this should be taken into account. With simultaneous use of a combined oral contraceptive with fluconazole at a dose of 50 mg, no significant effect on the level of hormones is found, whereas with daily administration of 200 mg fluconazole AUC of ethinyl estradiol and levonorgestrel increases by 40% and 24%, respectively, and when taking 300 mg of fluconazole 1 time per week - AUC of ethinyl estradiol and norethindrone age t 24% and 13% respectively. Thus, repeated use of fluconazole in the indicated doses is unlikely to affect the effectiveness of the combined oral contraceptive. Simultaneous use of fluconazole and phenytoin may be accompanied by a clinically significant increase in the concentration of phenytoin. With this combination, the concentration of phenytoin should be monitored and its dose adjusted accordingly to ensure therapeutic serum concentrations. Simultaneous use of fluconazole and rifabutin can lead to an increase in serum concentrations 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 monitored. Simultaneous use of fluconazole and rifampicin results in a 25% decrease in AUC and a T1 / 2 duration of fluconazole by 20%. In patients simultaneously taking rifampicin, it is necessary to take into account the feasibility of increasing the dose of fluconazole. Fluconazole, while taking it simultaneously, leads to an increase in T1 / 2 oral sulfonylurea preparations (chlorpropamide, glibenclamide, glipizide and tolbutamide). Patients with diabetes mellitus can be prescribed together fluconazole and oral sulfonylurea drugs, but the possibility of hypoglycemia should be considered. Simultaneous use of fluconazole and tacrolimus leads to an increase in plasma concentrations of the latter. Cases of nephrotoxicity are described. With this combination, patients should be carefully monitored. With the simultaneous use of azole antifungal agents and terfenadine, serious arrhythmias may occur as a result of an increase in the QT interval.When taking fluconazole at a dose of 200 mg / day, an increase in the QT interval is not established, however, the use of fluconazole at doses of 400 mg / day and above causes a significant increase in plasma terfenadine concentration. Simultaneous administration of fluconazole in doses of 400 mg / day or more with terfenadine is contraindicated. Fluconazole treatment in doses of less than 400 mg / day in combination with terfenadine should be carefully monitored. When used simultaneously with fluconazole at a dose of 200 mg for 14 days, the average plasma clearance of theophylline is reduced by 18%. When fluconazole is prescribed to patients taking theophylline in high doses, or patients with an increased risk of the toxic action of theophylline, the symptoms of theophylline overdose should be observed and, if necessary, the therapy should be adjusted accordingly. Zidovudine concentrations increase, probably due to a decrease in the metabolism of the latter to its main metabolite. Before and after treatment with fluconazole at a dose of 200 mg / day for 15 days, patients with AIDS and ARC (AIDS-related complex) showed a significant increase in zidovudine AUC (20%). When used in HIV-infected patients, zidovudine at a dose of 200 mg every 8 hours for 7 days in combination with fluconazole at a dose of 400 mg / day or without it with an interval of 21 days between the two regimens, a significant increase in zidovudine AUC (74%) was established, while using it with fluconazole. Patients receiving this combination should be monitored to detect side effects of zidovudine. Simultaneous use of fluconazole with astemizole or other drugs whose metabolism is performed by isoenzymes of the cytochrome P450 system may be accompanied by an increase in serum concentrations of these agents. With such combinations, patients should be carefully monitored.
special instructions
It is used with caution in disorders of liver function during the use of fluconazole, with the appearance of a rash against the background of fluconazole in patients with surface fungal infection and invasive / systemic fungal infections, while using terfenadine and fluconazole at a dose of less than 400 mg / dayin potentially proarrhythmic conditions in patients with multiple risk factors (organic heart disease, electrolyte imbalance, and concomitant development of these disorders). The hepatotoxic effect of fluconazole has usually been reversible; his symptoms disappeared after cessation of therapy. It is necessary to monitor the condition of patients whose liver function indicators are disturbed during treatment with fluconazole in order to detect signs of more serious liver damage. If clinical signs or symptoms of liver damage appear that may be associated with fluconazole, it should be canceled. Patients with AIDS are more likely to develop severe skin reactions with many drugs. When a patient receiving treatment for a superficial fungal infection appears to have a rash that can be associated with the use of fluconazole, it should be canceled. When rashes appear in patients with invasive / systemic fungal infections, they should be carefully observed and fluconazole should be canceled when bullous lesions or erythema multiforme occur. and ventricular fibrillation / flutter was rarely observed in patients with multiple risk factors such as organic heart disease, electrolyte imbalance and posobstvuyuschaya development of such disorders accompanying terapiya.Terapiyu can begin until the culture results and other laboratory tests. However, anti-infective therapy needs to be adjusted accordingly when the results of these studies are known. There have been reports of cases of superinfection caused by Candida strains other than Candida albicans, which often do not show sensitivity to fluconazole (for example, Candida krusei). In such cases, alternative antifungal therapy may be required.