Universal reference book for medicines
Product name: FLUKOSTAT ® (FLUCOSTAT)

Active substance: fluconazole

Type: Antifungal medication

Manufacturer: ФАРМСТАНСТАНАР-ЛЕКСРЕДСТВА (Russia)
Composition, form of production and packaging
?
Capsules are opaque, light pink / rosy-brown in color, No. 2; the contents of the capsules are white or almost white powder.
1 caps.

fluconazole 50 mg

Excipients: silicon dioxide colloid (aerosil), corn starch, magnesium stearate, sodium lauryl sulfate, lactose.

The composition of the capsule shell: gelatin, iron dye red oxide (E172), methyl parahydroxybenzoate, propyl parahydroxybenzoate, titanium dioxide (E171), acetic acid.

7 pcs.
- packings of cellular contour (1) - packs cardboard.
?
Capsules are opaque, white, №0; the contents of the capsules are white or almost white powder.
1 caps.

fluconazole 150 mg

Excipients: silicon dioxide colloid (aerosil), corn starch, magnesium stearate, sodium lauryl sulfate, lactose.

The composition of the capsule shell: gelatin, methyl parahydroxybenzoate, propyl parahydroxybenzoate, titanium dioxide (E171), acetic acid.

1 PC.
- packings of cellular contour (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2014.

PHARMACHOLOGIC EFFECT

Antifungal drug.
Fluconazole is a representative of the class of triazole antifungal agents, it is a potent selective inhibitor of the synthesis of sterols in the fungal cell.
It is active against pathogens of opportunistic mycoses, incl.
caused by Candida spp., Cryptococcus neoformans, Microsporum spp., Trichophyton spp. Also shown is the activity of fluconazole on models of endemic mycoses, including infections caused by Blastomyces dermatitidis, Coccidioides immitis and Histoplasma capsulatum.
PHARMACOKINETICS

Suction

After oral administration fluconazole is well absorbed.
Bioavailability is 90%. C max fluconazole in blood plasma after taking an empty stomach at a dose of 150 mg is 90% of its plasma content with iv administration in a dose of 2.5-3.5 mg / l.
T max is achieved in 0.5-1.5 hours after administration.
Simultaneous food intake does not affect absorption during ingestion.
Concentration in plasma is directly proportional to the dose taken.

Distribution

90% C ss is reached by the 4th-5th day of treatment with the drug (when taken 1 time / day).

The introduction of a shock dose (on day 1), which is 2 times higher than the average daily dose, allows reaching 90% C ss level by the 2nd day.
Apparent V dapproximates the total water content in the body. Binding to proteins - 11-12%.
Fluconazole well penetrates into all body fluids.
The concentrations of fluconazole in saliva and sputum are similar to those in plasma. In patients with fungal meningitis, fluconazole concentrations in the cerebrospinal fluid are about 80% of its levels in the plasma.
In the stratum corneum, epidermis, dermis and sweat fluid, high concentrations are achieved, which exceed the serum levels.

Excretion

T 1/2 is about 30 hours.

Fluconazole is excreted mainly by the kidneys;
approximately 80% of the administered dose is found in the urine unchanged. The clearance of fluconazole is proportional to QC. Metabolites of fluconazole in the blood were not detected.
INDICATIONS

- cryptococcosis, including cryptococcal meningitis and other localizations of this infection (including lungs, skin), both in patients with normal immune response, and in patients with various forms of immunosuppression (including AIDS patients, during transplantation bodies);
the drug can be used to prevent cryptococcal infection in AIDS patients;
- generalized candidiasis, including candidemia, disseminated candidiasis and other forms of invasive candidiasis infection (including peritoneal, endocardial, eye, respiratory and urinary tract infections).
Treatment can be performed in patients with malignant neoplasms, in intensive care units, in patients receiving cytotoxic or immunosuppressive agents, and in the presence of other factors predisposing to the development of candidiasis;
Candidiasis of mucous membranes, incl.
oral cavity and pharynx (including atrophic candidiasis of the oral cavity, associated with the wearing of dentures), esophagus, non-invasive bronchopulmonary infections, candiduria; prevention of recurrence of oropharyngeal candidiasis in AIDS patients;
- genital candidiasis: treatment of vaginal candidiasis (acute and chronic recurrent), preventive use to reduce the frequency of recurrences of vaginal candidiasis (3 or more episodes a year);
Candidiasis 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;

- Mycosis of the skin, including mycosis of the feet, body, inguinal region, pityriasis, onychomycosis and skin candidiasis;

- Deep endemic mycoses, including coccidioidomycosis, paracoccidioidomycosis, sporotrichosis and histoplasmosis in patients with normal immunity.

DOSING MODE

The drug is taken orally.

Adults with cryptococcal meningitis and cryptococcal infections of other localization on the first day are prescribed 400 mg, and then continue treatment at a dose of 200-400 mg 1 time / day.
Duration of treatment for cryptococcal infections depends on clinical efficacy, confirmed by mycological examination; In cryptococcal meningitis, therapy is usually continued for at least 6-8 weeks.
To prevent the recurrence of cryptococcal meningitis in AIDS patients , after the completion of a full course of primary treatment, fluconazole therapy at a dose of 200 mg / day can be continued for a long time.

With candidemia, disseminated candidiasis and other invasive candidiasis 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 clinical effectiveness.
With oropharyngeal candidiasis, the drug is prescribed on average 50-100 mg once a day;
the duration of therapy is 7-14 days. If necessary, in patients with a marked decrease in immunity, treatment may be longer.
With atrophic candidiasis of the oral cavity associated with wearing dentures , the drug is prescribed at an average dose of 50 mg 1 time / day for 14 days in combination with local antiseptic agents for prosthesis treatment.

With other localizations of candidiasis (with the exception of genital candidiasis), for example, esophagitis, noninvasive bronchopulmonary disease, candiduria, candidiasis of the skin and mucous membranes, the effective dose is on the average 50-100 mg / day with a treatment duration of 14-30 days.

To prevent the recurrence of oropharyngeal candidiasis in AIDS patients after completion of the full course of primary therapy, fluconazole can be administered at 150 mg once a week.

With vaginal candidiasis, fluconazole is taken once inside 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 1 time / month. The duration of therapy is determined individually; it varies from 4 to 12 months. Some patients may need more frequent use.
With balanitis caused by Candida spp.
, fluconazole is administered once in 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 degree of risk of fungal infection.
If there is a high risk of generalized infection, for example, in patients with expected severe or persistent neutropenia, the recommended dose is 400 mg 1 time / day. Fluconazole is prescribed several days before the expected appearance of neutropenia; after an increase in the number of neutrophils more than 1000 / μl, treatment is continued for another 7 days.
With mycosis of the skin , including mycosis of the feet, smooth skin, inguinal area and skin candidiasis, the recommended dose is 150 mg 1 time / week.
or 50 mg once a day. The duration of therapy in usual cases is 2-4 weeks. However, with foot mycoses, longer therapy (up to 6 weeks) may be required.
With pityriasis, 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 it is sufficient to take a single dose of the drug at a dose of 300-400 mg. An alternative treatment regimen is the use of the drug at 50 mg once a day for 2-4 weeks.
With onychomycosis the recommended dose is 150 mg 1 time / week.
Treatment should continue until the replacement of the infected nail (growth of uninfected nail).To re-grow the nails on the fingers and toes, it normally takes 3-6 months and 6-12 months, respectively.
With deep endemic mycoses, it may be necessary to use the drug at a dose of 200-400 mg / day for up to 2 years.
The duration of therapy is determined individually and is 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 exceeding that of adults. Flucostat is used daily 1 time / day.
In mucosal candidiasis, the recommended dose of fluconazole is 3 mg / kg / day.
On the first day, a shock dose of 6 mg / kg may be prescribed to achieve a more rapid equilibrium equilibrium concentration.
For the treatment of generalized candidiasis and cryptococcal infection, the recommended dose is 6-12 mg / kg / day, depending on the severity of the disease.

For the prevention of fungal infections in children with reduced immunity , where the risk of infection is associated with neutropenia, resulting from cytotoxic chemotherapy or radiation therapy, the drug is prescribed at 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 proportional relationship as in adults) according to the degree of renal insufficiency.

In elderly patients in the absence of violations of kidney function, the drug is used in accordance with the usual dosing regimen.

In patients with impaired renal function with a single admission, a dose change is not required.
With repeated use of the drug with QC more than 50 ml / min, thedrug is given in an average dose. With SC from 11 to 50 ml / min , a shock dose of 50 mg to 400 mg should first be prescribed, then a dose of 50% of the recommended dose. Patients who regularly undergo dialysis are given one dose after each hemodialysis session.
SIDE EFFECT

On the part of the digestive system: a change in taste, nausea, flatulence, vomiting, abdominal pain, diarrhea;
rarely - violations of the liver (jaundice, hepatitis, hepatonecrosis, hyperbilirubinemia, increased activity of ALT, AST, APF).
From the side of the central nervous system: headache, dizziness;
rarely convulsions.
From the hemopoietic system: rarely - leukopenia, thrombocytopenia, agranulocytosis.

From the cardiovascular system: an increase in the duration of the QT interval, flicker, flutter of the ventricles.

Allergic reactions: skin rash;
rarely - malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), anaphylactoid reactions.
From the side of metabolism: rarely - hypercholesterolemia, hypertriglyceridemia, hypokalemia.

Other: rarely - violations of kidney function, alopecia.

CONTRAINDICATIONS

- simultaneous reception of drugs that extend the interval of QT (including terfenadine or astemizole);

- children's age till 3 years;

- hypersensitivity to the drug or similar in structure to azole compounds.

With caution , the drug should be used for liver and / or kidney failure, concomitantly with the administration of potentially dangerous hepatotoxic drugs, with alcoholism, in the case of proarrhythmogenic conditions in patients with multiple risk factors (organic heart disease, electrolyte balance disorders, simultaneous use of medications that cause arrhythmias).

PREGNANCY AND LACTATION

The use of Flucostat in pregnancy is possible only in the case of severe and potentially life-threatening fungal infections, when the expected benefit of treatment exceeds the possible risk to the fetus.

Since fluconazole is excreted in breast milk in concentrations close to plasma concentrations, it is not recommended to prescribe the drug during breastfeeding.

APPLICATION FOR FUNCTIONS OF THE LIVER

Patients with renal insufficiency (CC <50 ml / min) require a correction of the dosing regimen.

Fluconazole is excreted mainly with urine in unchanged form.
With a single admission, a dose change is not required. In patients (including children and the elderly) with impaired renal function, when taking the drug again, a shock dose of 50 mg to 400 mg should be initially administered.
For CK> 50 ml / min , the recommended average dose of the drug is used;
at KK from 11 to 50 ml / min , a dose of 50% of the recommended dose is applied.Patients regularly on hemodialysis receive a single dose of the drug after each hemodialysis session.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution should be used in patients with hepatic insufficiency, while taking potentially dangerous hepatotoxic drugs, with alcoholism.

If there are clinical signs of liver damage that may be associated with fluconazole, the drug should be discontinued.

APPLICATION FOR CHILDREN

Contraindication: children under 3 years.

APPLICATION IN ELDERLY PATIENTS

In elderly patients in the absence of violations of kidney function, the drug is used in accordance with the usual dosing regimen.

SPECIAL INSTRUCTIONS

In rare cases, the use of fluconazole was accompanied by toxic changes in the liver, incl.
with a fatal outcome, mainly in patients with serious concomitant diseases.There was no clear dependence of the frequency of 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; signs of it disappeared after discontinuation of therapy. If there are clinical signs of liver damage that may be associated with fluconazole, the drug should be discontinued.
Patients with AIDS are more likely to develop severe skin reactions with many drugs.
When a patient who is receiving treatment for a superficial fungal infection, a rash that can be associated with fluconazole, the drug should be discarded. When rashes appear in patients with invasive / systemic fungal infections, fluconazole should be carefully monitored and discarded when bullous lesions or erythema multiforme occur.
Caution should be exercised when using fluconazole simultaneously with cisapride, astemizole, rifabutin, tacrolimus, or other drugs metabolized by isoenzymes of the cytochrome P450 system.

OVERDOSE

Symptoms: hallucinations, paranoid behavior.

Treatment: recommended gastric lavage and symptomatic therapy.
Since fluconazole is excreted in the urine, forced diuresis increases its excretion. Conduction of hemodialysis within 3 hours reduces the concentration of fluconazole in the plasma by approximately 50%.
DRUG INTERACTION

When using fluconazole with warfarin, prothrombin time increased by 12%.
In this regard, it is recommended to monitor prothrombin time in patients receiving Flucostat ® in combination with coumarin anticoagulants.
With simultaneous use of fluconazole increases T 1/2 oral hypoglycemic drugs - derivatives of sulfonylureas (chlorpropamide, glibenclamide, glipizide and tolbutamide).
The joint administration of fluconazole and oral hypoglycemic drugs is allowed, but the possibility of developing hypoglycemia should be taken into account.
The simultaneous use of fluconazole and phenytoin may be accompanied by an increase in the concentration of phenytoin in a clinically significant degree.
Therefore, when a combined use of these drugs is necessary, monitoring of the concentration of phenytoin with correction of its dose is necessary in order to provide a therapeutic concentration in the blood plasma.
Simultaneous application of fluconazole and rifampicin leads to a 25% reduction in AUC and a 20% decrease in T 1/2 of fluconazole from the plasma.
Therefore, in patients receiving rifampicin simultaneously, a dose of fluconazole is recommended to be increased.
It is recommended that the concentration of cyclosporin in the blood be monitored in patients receiving fluconazole.
when using fluconazole and cyclosporine in patients with kidney transplantation, fluconazole administration at a dose of 200 mg / day leads to a slow increase in the concentration of cyclosporine in the blood plasma.
Patients receiving theophylline in high doses, or who are likely to develop theophylline intoxication, should be monitored for the early detection of the symptoms of a theophylline overdose, tk.
simultaneous administration of fluconazole leads to a decrease in the average clearance rate of theophylline from plasma.
With the simultaneous use of fluconazole and terfenadine or cisapride, cases of unwanted reactions from the heart, including paroxysms of ventricular tachycardia (pirouette-type arrhythmias) have been described.

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. It is necessary to carefully observe patients who are simultaneously receiving rifabutin and fluconazole.
With the simultaneous use of fluconazole and zidovudine, there is an increase in zidovudine in the plasma, which is caused by a decrease in the conversion of the latter into its metabolite.

With the simultaneous use of fluconazole with midazolam increases the risk of psychomotor effects, with tacrolimus - increases the risk of nephrotoxicity.

TERMS OF RELEASE FROM PHARMACY

The drug is approved for use as a means of OTC.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children at a temperature of 15 ° to 25 ° C.
Shelf life - 2 years.
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