Flucorus

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Flucorus: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Use in the elderly
14. Drug interactions
15. Analogs
16. Terms and conditions of storage
17. Terms of dispensing from pharmacies
18. Reviews
19. Price in pharmacies

Latin name: Flucorus

ATX code: J02AC01

Active ingredient: fluconazole (Fluconazole)

Producer: Sintez, JSC (Russia)

Description and photo update: 2019-05-07

Prices in pharmacies: from 109 rubles.

Buy

Flucorus is an antifungal agent.

Release form and composition

Dosage form - solution for infusion: transparent, colorless or slightly yellowish [50 and 100 ml in glass dark or colorless 100 ml bottles, sealed with rubber stoppers and crimped caps, in a cardboard box 1 bottle and instructions for the use of Flucorus; 100 ml in glass dark or colorless bottles of 100 ml, sealed with rubber stoppers and crimped caps, in a cardboard box 1 bottle and polymer suspension (or without suspension); packing for hospitals - in a box made of corrugated cardboard 35 vials or bottles with polymer suspensions (or without suspensions)].

Composition of 1 ml solution:

active substance: fluconazole - 2 mg;
auxiliary components: sodium chloride, water for injection.

Pharmacological properties

Pharmacodynamics

The active ingredient of Flucorus - fluconazole - is a representative of the class of triazole antifungal agents. It has a highly specific effect, inhibiting the activity of fungal enzymes dependent on cytochrome P ₄₅₀. Blocks the conversion of fungal lanosterol into ergosterol. Increases the permeability of the cell membrane, disrupts cell growth.

Being highly selective for cytochrome P _{450 of} fungi, fluconazole has almost no inhibitory effect on these enzymes in the human body (unlike econazole, clotrimazole, itraconazole and ketoconazole, it inhibits less oxidative processes in liver microsomes dependent on cytochrome P ₄₅₀). Does not possess antiandrogenic activity.

Fluconazole is active against opportunistic mycoses, including those caused by Coccidioides immitis (including intracranial infections), Cryptococcus neoformans, Candida spp. (including generalized forms of candidiasis against the background of immunosuppression), Trichophyton spp., Microsporum spp. Effective for endemic mycoses caused by Blastomyces dermatitidis and Histoplasma capsulatum (including with immunosuppression).

Pharmacokinetics

After intravenous (IV) administration, fluconazole penetrates well into tissues and body fluids. Plasma concentration is directly proportional to the dose applied. Penetrates into joint fluid, saliva, sputum, peritoneal fluid and breast milk in concentrations similar to plasma. In the stratum corneum, epidermis and sweat fluid, the drug creates concentrations higher than in the blood serum.

Flucorus penetrates well into the cerebrospinal fluid, where, with fungal meningitis, its concentration is about 85% of the plasma concentration.

About 90% of the equilibrium plasma concentration (C _ss) is achieved on the 4-5th day of treatment. To reach this level by the 2nd day, the introduction on the first day of a loading dose (2 times higher than the usual daily) allows.

The apparent volume of distribution (V _d) approximately corresponds to the total fluid content in the body. Plasma proteins bind about 11-12%.

Fluconazole is an inhibitor of the CYP2C9 isoenzyme in the liver. It is excreted mainly by the kidneys: unchanged - 80%, in the form of metabolites - 11%. The half-life (T _½) is 30 hours.

The clearance of fluconazole is proportional to the clearance of creatinine (CC), its pharmacokinetic parameters largely depend on the state of renal function. In this case, T _{½ is} inversely proportional to KK. After a hemodialysis session for 3 hours, the plasma concentration of fluconazole is reduced by 2 times.

With intravenous and oral administration of fluconazole, the pharmacokinetics of the drug are similar, which makes it possible to transfer patients from one dosage form to another without difficulty.

Indications for use

deep endemic mycoses (histoplasmosis, coccidioidomycosis) in patients with normal immunity;
cryptococcosis, including cryptococcal meningitis and infections of other localization (for example, skin, lungs), in patients with normal immunity and in patients with various forms of immunosuppression [for example, with organ transplantation or acquired immunodeficiency syndrome (AIDS)], maintenance therapy with the purpose of preventing recurrence of cryptococcosis in AIDS patients;
generalized candidiasis, including candidemia, disseminated candidiasis, as well as other forms of invasive candidiasis infection, including infections of the urinary tract, bronchopulmonary system, endocardium, peritoneum and eyes, including in patients taking cytotoxic or immunosuppressive drugs, and patients with malignant tumors in intensive care units, or other risk factors that predispose to the development of candidiasis;
prevention of candidiasis in patients at high risk of generalized infection (for example, with severe or long-term neutropenia);
oropharyngeal candidiasis, candidiasis of the esophagus and mucous membranes in children.

Contraindications

Absolute:

lengthening of the QT interval on the electrocardiogram (congenital or detected);
lactation period;
the simultaneous use of drugs that can lengthen the QT interval (for example, antiarrhythmics of IA and III classes);
simultaneous use of terfenadine (against the background of constant intake of fluconazole in a daily dose of 400 mg), pimozide, quinidine, astemizole, cisapride;
hypersensitivity to any component of the drug or other azole antifungal agents.

Relative (Flucorus solution is used with caution, provided that the benefits exceed the possible risks):

liver failure;
potentially arrhythmogenic conditions in patients with multiple risk factors (electrolyte imbalance, organic heart disease, taking drugs that cause arrhythmias);
the appearance of a rash against the background of the use of fluconazole in patients with superficial fungal infection and invasive / systemic fungal infections;
the simultaneous use of terfenadine (while taking fluconazole in a daily dose of less than 400 mg);
pregnancy.

Flucorus, instructions for use: method and dosage

Flucorus solution is injected intravenously at a rate of up to 200 mg / h.

The doctor determines the daily dose of the drug individually, depending on the type and severity of the fungal infection.

Recommended dosages for adults:

cryptococcal meningitis, cryptococcal infections of other localizations: on the first day - an average of 400 mg, then - 200-400 mg once a day. Treatment for cryptococcal meningitis is at least 6-8 weeks. The duration of therapy for cryptococcal infections is determined by the clinical efficacy of Flucorus, confirmed by a mycological study;
prevention of recurrence of cryptococcal meningitis in AIDS patients (after the end of the full course of primary therapy): 200 mg 1 time per day for a long time, if necessary, the patient can be transferred to the oral dosage form of fluconazole;
candidemia, disseminated candidiasis and other invasive candidal infections: on the first day - on average 400 mg, then - 200 mg per day, it is possible to increase the daily dose to 400 mg, depending on the clinical situation. The duration of therapy depends on the clinical picture;
prevention of candidiasis in the presence of a high risk of generalized infection (for example, in patients with long-term or severe neutropenia): 400 mg 1 time per day. Flucorus begins to be administered a few days before the expected appearance of neutropenia, treatment is continued for another 7 days after the increase in the number of neutrophils by more than 1000 / μL;
deep endemic mycoses: 200-400 mg per day. The duration of treatment is determined individually, with coccidioidomycosis, the course is 11-24 months, with histoplasmosis - 3-17 months (if necessary, the patient is transferred to the oral dosage form of fluconazole).

Recommended daily doses of Flucorus for children:

cryptococcal meningitis, cryptococcal infections of other localizations, generalized candidiasis: 6-12 mg / kg, duration of therapy - 10-12 weeks (until the elimination of the pathogen in the cerebrospinal fluid, confirmed by laboratory tests);
prevention of relapse of cryptococcal meningitis in children with AIDS (after the end of the full course of primary therapy): 6 mg / kg. The duration of admission is determined individually, Flucorus can be used for a long time;
oropharyngeal candidiasis: on the first day - 6 mg / kg, then - 3 mg / kg. The minimum duration of treatment is 2 weeks;
candidiasis of the mucous membranes: 3 mg / kg, if necessary, a more rapid achievement of a constant equilibrium concentration of Flucorus on the first day, a loading dose of 6 mg / kg is prescribed. The minimum duration of treatment is 3 weeks;
esophageal candidiasis: 3 mg / kg, if necessary to achieve a constant equilibrium concentration of the drug more quickly on the first day, a loading dose of 6 mg / kg is prescribed. In severe cases, the daily dose may be increased to 6–12 mg / kg. Treatment is carried out for at least 3 weeks and for another 2 weeks after regression of the symptoms of the disease;
prevention of fungal infections with reduced immunity, if the risk of infection is associated with the development of neutropenia due to radiation therapy or cytotoxic chemotherapy: 3-12 mg / kg. Treatment is continued until the induced neutropenia is eliminated.

Do not use Flucorus in children in daily doses exceeding those in adults, i.e. more than 400 mg. The solution is injected once a day. With long-term treatment, it is possible to switch to an oral preparation containing fluconazole.

In newborns, fluconazole is excreted more slowly, therefore, in the first 2 weeks after birth, the interval between injections of the drug is increased to 72 hours, from the 2nd to the 4th week - up to 48 hours. Then Flucorus is used in accordance with the usual dosage regimen.

Elderly people in the absence of impaired renal function do not need to adjust the dose.

Patients with functional impairments of the kidneys (creatinine clearance <50 ml / min) are initially administered a loading dose of Flucorus - from 50 to 400 mg, then the dose is reduced by 2 times. Patients on dialysis receive the drug in full dose after each session.

Side effects

Flucorus is generally well tolerated. In rare cases, the following side effects are noted (according to the frequency of development, they are classified as follows: often - <1%, infrequently - 0.1-1%, rarely - 0.01-0.1%, very rarely - <0.01%):

allergic reactions: infrequently - skin rash; rarely - anaphylactoid reactions (including itchy skin, urticaria, facial edema, angioedema), toxic epidermal necrolysis (Lyell's syndrome), exudative erythema multiforme (including Stevens-Johnson syndrome);
on the part of the cardiovascular system: rarely - an increase in the duration of the QT interval; very rarely - ventricular fibrillation / flutter;
from the central nervous system: infrequently - dizziness, headache; rarely - convulsions;
on the part of the hematopoietic organs: rarely - agranulocytosis, thrombocytopenia, neutropenia, leukopenia;
from the digestive system: infrequently - a change in taste, abdominal pain, flatulence, diarrhea, vomiting, nausea; rarely - liver dysfunction (increased alkaline phosphatase, aspartate aminotransferase and alanine aminotransferase, hyperbilirubinemia, jaundice, hepatitis, hepatocellular necrosis), including fatal;
others: rarely - hypertriglyceridemia, hypercholesterolemia, hypokalemia, impaired renal function, alopecia.

Overdose

Excessive doses of Flucorus can cause hallucinations and paranoid behavior.

Treatment is symptomatic. The forced diuresis is shown. Hemodialysis for 3 hours reduces the plasma concentration of fluconazole by about 2 times.

special instructions

It is allowed to start treatment with Flucorus until culture results or other laboratory data are obtained, but when the results become known, it is necessary to adjust the therapy regimen.

Treatment is continued until clinical and microbiological remission appears. In case of premature discontinuation of therapy, the risk of disease recurrence is high.

Flucorus contains 0.9% sodium chloride solution: in 100 ml of solution - 15 mmol of sodium and chlorine ions. In patients requiring sodium or fluid restriction, the rate of fluid administration should be considered.

During therapy, control of the concentration of fluconazole in the blood, blood parameters, liver and kidney function is indicated. If functional disorders of the liver / kidneys are detected, Flucorus is canceled.

In rare cases, fluconazole causes hepatotoxic effects, they do not depend on the dose, duration of therapy, gender and age of the patient. Toxic changes in the liver are usually reversible, their signs disappear after the end of treatment. If clinical symptoms of liver damage appear, presumably associated with fluconazole, the administration of Flucorus should be discontinued.

With the simultaneous use of coumarin anticoagulants, monitoring of prothrombin time is required.

Fluconazole, like some other azoles, can prolong the QT interval. In this regard, careful monitoring of the condition and monitoring of the electrocardiogram is required in patients at risk of developing arrhythmias, especially in the presence of electrolyte imbalance, organic damage to the myocardium or cardiac pathways, as well as in the case of simultaneous maintenance cardiotropic therapy. With the joint appointment of drugs with a narrow therapeutic range, metabolized with the participation of isoenzymes CYP3A4 and CYP2C9, it is necessary to monitor the patient's condition.

AIDS patients are more susceptible to the development of severe skin reactions against the background of the use of various medications. In cases where the appearance of a rash in patients with superficial fungal infection is definitely associated with the use of fluconazole, Flucorus is canceled.

If a rash occurs in patients with systemic fungal infections, close monitoring is required. If bullous changes or erythema multiforme occur, Flucorus should be canceled.

It is necessary to control the concentration of cyclosporine in the blood in patients after kidney transplantation receiving fluconazole in a daily dose of 200 mg, since such patients have a slow increase in the plasma concentration of cyclosporine. Special care should be taken when using rifabutin or other drugs that are metabolized by the cytochrome P ₄₅₀ system together.

Simultaneous administration of cisapride is contraindicated.

Influence on the ability to drive vehicles and complex mechanisms

Given the safety profile of fluconazole, it is unlikely to have a negative effect on reaction rate and ability to concentrate.

Application during pregnancy and lactation

During pregnancy, Flucorus can be used only in cases where the expected benefit is definitely higher than the potential risks, i.e. when a woman's fungal infection is severe and potentially life-threatening.

Fluconazole passes into breast milk and creates concentrations similar to those in plasma. In this regard, during lactation, Flucorus is contraindicated.

Pediatric use

The drug is used in pediatrics according to indications. Flucorus is used with caution to treat newborn children; correction of the dosage regimen is required.

With impaired renal function

In case of functional impairment of the kidneys (creatinine clearance <50 ml / min), it is recommended to administer the first loading dose from 50 to 400 mg and further decrease the daily dose by 2 times.

For patients on dialysis, Flucorus is administered in full dose after each session.

For violations of liver function

Flucorus should be used with caution in liver failure.

Use in the elderly

Elderly people in the absence of impaired renal function do not need to adjust the dose.

Drug interactions

coumarin anticoagulants (for example, warfarin): increases prothrombin time by about 12%. It is necessary to control this indicator;
oral hypoglycemic drugs, sulfonylurea derivatives (glipizide, tolbutamide, glibenclamide, chlorpropamide): their half-life increases, which is fraught with the development of hypoglycemia. It is required to control the concentration of glucose in the blood and, if necessary, adjust the dose of the hypoglycemic agent;
diuretics (including hydrochlorothiazide): the plasma concentration of fluconazole increases by 40%, but a decrease in the dose of Flucorus is not required;
oral contraceptives: their effectiveness is not reduced;
cyclosporine: a change in its concentration in the blood is possible. This indicator should be monitored;
tacrolimus: its concentration in the blood increases, which entails the risk of developing nephrotoxic effects;
rifampicin: decreases by 25% AUC (area under the concentration-time curve) and by 20% the T _½ period of fluconazole, which requires an increase in the dose of Flucorus;
rifabutin: an increase in its serum concentration is possible, the development of uveitis. Monitoring of the patient's condition is required;
midazolam: its content in the blood increases, which entails an increased risk of psychomotor effects;
phenytoin: its level in the blood increases, which is accompanied by clinically significant manifestations. It is necessary to control the concentration of the drug and, if necessary, adjust the dose;
cisapride: possible development of adverse reactions from the heart, including paroxysms of ventricular tachycardia (torsade de pointes);
terfenadine: when used simultaneously with fluconazole in daily doses up to 400 mg, careful medical supervision is required; the use of terfenadine in combination with fluconazole in daily doses of more than 400 mg is contraindicated;
zidovudine: its concentration in the blood increases, as a result of which its side effects may increase;
azithromycin, voriconazole: a change in their plasma concentrations is possible. Control and, if necessary, dose adjustment is required;
theophylline: its half-life increases, the risk of intoxication increases, which requires correction of the dosage regimen.

Analogs

Flucorus analogs are: Diflazon, Diflucan, Mykonil, Medoflucon, Mikomax, Mikosist, Mikoflucan, Nofung, Procanazole, Flucosan, Fluconazole, Fluconorm, Flukorem, Forcan, Flucostat, Flucomabol, Flucosid, Vero-Fluconazol.

Terms and conditions of storage

Store at a temperature not exceeding 30 ° C, out of the reach of children.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Flucorus

There are no reviews about Flucorus on specialized forums and sites. Patients speak positively about fluconazole (an active substance that is also a part of many antifungal drugs): the drug is effective in many fungal diseases, is well tolerated, and is inexpensive.

The negative aspects include possible side effects and negative effects on the liver.

The price of Flucorus in pharmacies

The approximate price for Flucorus for 1 bottle of 100 ml is 85–111 rubles.

Flucorus: prices in online pharmacies

Drug name

Price

Pharmacy

Flucorus 2 mg / ml solution for infusion 100 ml 1 pc.

109 RUB

Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!