Fluconazole Stada, 150 mg capsules
€2.72 €2.47
Antifungal agent, has a highly specific action by inhibiting the activity of cytochrome P450-dependent enzymes of fungi.
Blocks conversion of lanosterol of fungal cells into membrane lipid – ergosterol; increases cell membrane permeability, disrupts its growth and replication.
Fluconazole, being highly selective for cytochrome P450 of fungi, practically does not inhibit these enzymes in humans (in comparison with itraconazole, clotrimazole, econazole and ketoconazole it inhibits cytochrome P450 dependent oxidation processes in human liver microsomes to a lesser extent).
It has no antihydrogenic activity.
It is active in opportunistic mycoses, including those caused by Candida spp. (including generalized candidiasis against immunosuppression), Cryptococcus neoformans and Cossidioides immitis (including intracranial infections), Microsporum spp. and Trichophyton spp.;
in endemic mycoses caused by Blastomyces dermatidis, Histoplasma capsulatum (including immunosuppression).
Pharmacokinetics
Fluconazole is well absorbed after oral administration, the absorption rate of fluconazole is not affected by food intake, its bioavailability is 90%.
The time of maximum concentration after oral administration on an empty stomach of 150 mg of the preparation is 0,5-1,5 h, Cmax is 90% of concentration in plasma in case of per oral administration with a dose of 2,5-3,5 mg/l. T1/2 fluconazole is 30 h.
The binding to plasma proteins is 11-12%. Plasma concentration is in direct dependence on the dose. 90% level of equilibrium concentration is reached by 4-5 days of therapy (when taken once daily).
The administration of a shock dose (on the first day), 2 times the usual daily dose, allows reaching the level of concentration corresponding to 90% of the equilibrium concentration by the second day.
Fluconazole penetrates well into all body fluids. Concentrations of the active substance in breast milk, joint fluid, saliva, sputum and peritoneal fluid are similar to its levels in plasma.
The steady values in vaginal secretion are reached 8 hours after oral administration and are maintained at these levels for at least 24 hours.
Fluconazole penetrates cerebrospinal fluid (CSF) well – in fungal meningitis the concentration in CSF is about 85% of its level in plasma.
In sweat fluid, epidermis and stratum corneum (selective accumulation), concentrations higher than serum concentrations are achieved.
After oral administration of 150 mg on day 7, the concentration in the stratum corneum of the skin is 23.4 mcg/g and, 1 week after the second dose, 7.1 mcg/g; the concentration in the nails after 4 months of use at a dose of 150 mg once a week is 4.05 mcg/g in healthy and 1.8 mcg/g in the affected nails.
The volume of distribution approximates the total water content of the body.
It is an inhibitor of CYP2C9 isoenzyme in the liver. It is excreted mainly by the kidneys (80% – unchanged, 11% – as metabolites).
The clearance of fluconazole is proportional to creatinine clearance. No fluconazole metabolites were detected in peripheral blood.
The pharmacokinetics of fluconazole significantly depends on the functional state of the kidneys, and there is an inverse relationship between the elimination half-life and creatinine clearance.
After hemodialysis within 3 hours plasma concentration of fluconazole decreases by 50%.
Indications
Active ingredient
Composition
1 capsule contains:
The active ingredient:
Fluconazole 150 mg;
Associates:
Lactose,
Potato starch,
Croscarmellose sodium (primellose),
Povidone (polyvinylpyrrolidone low molecular weight medical),
Magnesium stearate,
Talt;
Capsules #1:
Gelatin,
Titanium dioxide,
Quinoline yellow dye [E104],
Sunset Yellow Dye [E110]
How to take, the dosage
Orally, swallowed whole.
Adults and children over 15 years of age (with body weight over 50 kg) in cryptococcal meningitis and cryptococcal infections of other localizations are usually prescribed 400 mg (8 50 mg capsules) on the first day and then continue treatment at a dose of 200 mg (4 50 mg capsules) to 400 mg (8 50 mg capsules) once daily.
The duration of treatment in cryptococcal infections depends on clinical efficacy confirmed by mycological study; in cryptococcal meningitis the course of treatment should be at least 6-8 weeks.
In order to prevent relapse of cryptococcal meningitis in AIDS patients, fluconazole is prescribed at a dose of 200 mg (4 capsules of 50 mg) daily for an extended period of time after completion of the full course of initial therapy.
In candidemia, disseminated candidiasis and other invasive candidiasis infections, the dose is 400 mg (8 50 mg capsules) in the first day and then 200 mg (4 50 mg capsules) daily.
In case of insufficient clinical efficacy, the dose of the drug may be increased to 400 mg (8 50 mg capsules) per day. The duration of therapy depends on clinical effectiveness.
In oropharyngeal candidiasis the drug is usually prescribed 150 mg once daily; duration of treatment is 7-14 days. If necessary, in patients with severe immune impairment the treatment may be longer.
For prevention of relapses of oropharyngeal candidiasis in AIDS patients after completion of the complete course of initial therapy, 150 mg once weekly.
In atrophic oral candidiasis associated with wearing dentures, 50 mg once a day for 14 days in combination with local antiseptic medications for denture treatment.
In other localizations of candidiasis (except genital candidiasis), such as esophagitis, non-invasive bronchopulmonary lesions, candiduria, candidiasis of the skin and mucous membranes, etc., the effective dose is usually 150 mg daily for a treatment duration of 14-30 days.
In case of vaginal candidiasis, fluconazole is taken once orally in a dose of 150 mg. To reduce the frequency of recurrence of vaginal candidiasis, the drug may be used in 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.
In cases of balanitis caused by Candida, fluconazole is given orally in a single dose of 150 mg daily.
For prevention of candidiasis, the recommended dose is 50-400 mg once daily, depending on the degree of risk of fungal infection.
For prevention of candidiasis in patients with malignancies, the recommended dose of fluconazole is 150-400 mg once daily, depending on the degree of risk of fungal infection.
If there is a high risk of generalized infection, such as in patients with expected severe or prolonged neutropenia, the recommended dose is 400 mg/day.
Fluconazole is prescribed several days before the expected onset of neutropenia; after an increase in neutrophil count above 1,000/μL, treatment is continued for an additional 7 days.
In mycoses of the skin, including mycoses of the feet, smooth skin, and groin, and candidiasis of the skin, the recommended dose is 150 mg once weekly or 50 mg once daily; the dosing regimen depends on the clinical and mycological effect.
The duration of therapy in usual cases is 2-4 weeks, but in case of mycoses of feet it may be necessary to use longer therapy (up to 6 weeks).
In rubella, 300 mg (2 capsules of 150 mg) once weekly for 2 weeks; some patients need a third dose of 300 mg weekly, while in some cases a single dose of 300-400 mg is sufficient; an alternative regimen is 50 mg once daily 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 back). It normally takes 3-6 months and 6-12 months, respectively, for the nails on the fingers and feet to grow back.
In deep endemic mycoses, it may be necessary to use the drug at a dose of 200 mg (4 50 mg capsules) to 400 mg (8 50 mg capsules) per day for up to 2 years.
The duration of therapy is determined individually; it may 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 in 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 of adults, i.e., no more than 400 mg per day. The drug is used daily once a day.
In patients who are regularly on dialysis, one dose of the drug is used after each session of hemodialysis.
Interaction
Protrombin time increases (on average by 12%) when using fluconazole with warfarin.
In this regard, it is recommended to carefully monitor prothrombin time in patients receiving the drug in combination with coumarin anticoagulants.
The half-life of oral hypoglycemic agents – sulfonylurea derivatives (chlorpropamide, glibenclamide, glipizide, tolbutamide) may be increased when concomitantly taking fluconazole.
The concomitant use of fluconazole and phenytoin may increase plasma concentrations of phenytoin to a clinically significant degree.
Therefore, if co-administration of these drugs is necessary, phenytoin concentrations should be monitored with dose adjustments to maintain drug levels within the therapeutic interval.
Combination with rifampin decreases AUC by 25% and shortens plasma elimination half-life of fluconazole by 20%. Therefore, in patients receiving rifampicin concomitantly, it is reasonable to increase fluconazole dose.
The concentration of cyclosporine may increase when concomitant use with fluconazole at a dose of 200 mg/day.
In case of concomitant use with theophylline, the average plasma clearance rate of theophylline may decrease.
In concomitant use of fluconazole and cisapride, plasma concentrations of cisapride may increase significantly; there have been reports of adverse reactions in the heart, including ventricular fibrillation/torsades de points and prolongation of QT interval in ECG.
The concomitant use of azole antifungals and terfenadine may cause significant increases in plasma terfenadine levels: serious arrhythmias may occur as a result of the QT interval prolongation.
The concomitant use of fluconazole and hydrochlorothiazide may increase fluconazole plasma concentrations by 40%.
There have been reports of interaction between fluconazole and rifabutin with increased serum levels of the latter.
In concomitant use of fluconazole and rifabutin there have been cases of uveitis. Patients receiving rifabutan and fluconazole concomitantly should be closely monitored.
In patients receiving a combination of fluconazole and zidovudine an increase in concentration of zidovudine is observed, which is caused by decrease of conversion of the latter to its main metabolite, therefore an increase in side effects of zidovudine should be expected.
Enhances concentrations of midazolam, due to which the risk of psychomotor effects increases (more pronounced when using fluconazole orally than intravenously).
Enhances tacrolimus concentrations, due to which the risk of nephrotoxic effects increases.
Special Instructions
Treatment must be continued until clinical and hematological remission occurs. Premature discontinuation of treatment leads to relapses.
In rare cases the use of fluconazole has been accompanied by toxic liver changes, including fatal, mainly in patients with serious comorbidities.
In the case of hepatotoxic effects associated with fluconazole, no clear dependence on the total daily dose, duration of therapy, sex, and age of the patient was noted.
Hepatotoxic effects of fluconazole were usually reversible; symptoms disappeared after discontinuation of therapy.
In case of clinical signs of liver damage that may be associated with fluconazole, the drug should be discontinued.
AIDS patients are more prone to develop severe skin reactions with many drugs.
In cases where patients with superficial fungal infections develop a rash and it is considered definitely related to fluconazole, the drug should be discontinued.
If rash occurs in patients with invasive/systemic fungal infections, they should be closely monitored and fluconazole should be discontinued if bullous changes or erythema multiforme appear.
Caution should be exercised when fluconazole is coadministered with rifabutin or other drugs metabolized by the cytochrome P450 system.
When fluconazole is used together with oral hypoglycemic agents (chlorpropamide, glibenclamide, glipizide, tolbutamide) in diabetic patients, the blood glucose level should be controlled (possibility of hypoglycemia).
The monitoring of cyclosporine blood concentrations during concomitant use with fluconazole is recommended.
Patients who receive high doses of theophylline concomitantly with fluconazole, or who are likely to develop theophylline intoxication, should be monitored for early detection of symptoms of theophylline overdose.
Influence on driving and operating ability
A impairment in driving and operating ability associated with the use of the drug is unlikely.
Contraindications
With caution: Hepatic and/or renal insufficiency, appearance of rash on fluconazole in patients with superficial fungal infection and invasive/systemic fungal infections,
concomitant administration of terfenadine and fluconazole at a dose less than 400 mg/day, concomitant administration of potentially hepatotoxic medications, alcoholism, potentially proarrhythmogenic conditions in patients with
Multiple risk factors (organic heart disease, electrolyte imbalances, concomitant administration of arrhythmic medications), pregnancy.
Side effects
Gastrointestinal system disorders:
decreased appetite, changes in taste, nausea, vomiting, abdominal pain, flatulence, diarrhea, rarely – disorders of liver function (hyperbilirubinemia, increased alanine aminotransferase activity, aspartate aminotransferase activity, increased alkaline phosphatase activity, jaundice, hepatitis, hepatocellular necrosis).
Nervous system disorders:
Headache, dizziness, excessive fatigue, rarely seizures.
Hematopoietic organs:
rarely – leukopenia, thrombocytopenia (bleeding, petechiae), neutropenia, agranulocytosis.
Cardiovascular system disorders:
increased Q-T interval duration, ventricular fibrillation/tripping.
Allergic reactions:
cutaneous rash, rarely – multiform exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell syndrome), anaphylactoid reactions (including angioedema, facial edema, urticaria, skin itching).
Other:
Rarely – renal dysfunction, alopecia, hypercholesterolemia, hypertriglyceridemia, hypokalemia.
Overdose
Symptoms: hallucinations, paranoid behavior.
The treatment is symptomatic: gastric lavage, forced diuresis.
Hemodialysis for 3 h reduces the concentration in Plasma by approximately 50%.
Pregnancy use
The use of the drug in pregnant women is inadvisable, except for severe or life-threatening forms of fungal infections when the potential benefit to the mother from fluconazole significantly exceeds the risk to the fetus.
Because the concentration of fluconazole in breast milk and plasma is the same, it is contraindicated during lactation.
Similarities
Weight | 0.015 kg |
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Shelf life | 3 years. |
Conditions of storage | In a dry, light-protected place at a temperature not exceeding 25 ° C. |
Manufacturer | Chemopharm LLC, Russia |
Medication form | capsules |
Brand | Chemopharm LLC |
Other forms…
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