Analogs of Fluconazole and their differences: what to pay more for? Features of the use of Mikosist. Interaction with other drugs

(antimycotic) drug wide range actions. Mikosist is used for the treatment of systemic fungal diseases (for example, cryptococcosis, sporotrichosis, etc.), as well as candidiasis of the mucous membranes of various organs (oral cavity, vagina, glans penis, etc.) and mycoses skin and nails (for example, dermatophytosis, onychomycosis, pityriasis versicolor).

Dosages, composition and release forms of Mikosist

1. Capsules for oral administration;


2. Solution for intravenous administration(infusion).

Mikosist capsules are available in three different dosages:

• Mikosist 50 – each capsule contains 50 mg of fluconazole;


• Mikosist 100 – each capsule contains 100 mg of fluconazole;


• Mikosist 150 – each capsule contains 150 mg of fluconazole.

Accordingly, to designate capsules with a certain dosage, the name of the drug “Mikosist” is used with a number indicated next to it corresponding to the content of fluconazole. That is, Mikosist 50 are capsules containing 50 mg of fluconazole, Mikosist 100 are 100 mg, respectively, etc.

Mikosist capsules of all dosages contain the following components as excipients:

• Colloidal silicon dioxide;
• Magnesium stearate;
• Talc;
• Povidone;
• Corn starch;
• Lactose.

Mikosyst hard gelatin capsules and caps consist of the following substances:

• Titanium dioxide;
• Gelatin;
• Indigo carmine (capsule cap dye)

Solution for infusion Mikosist is available in glass bottles with a capacity of 100 ml. The fluconazole content in 1 ml of Mikosist solution is 2 mg. Accordingly, 100 ml of solution contains 200 mg of fluconazole. As auxiliary components, the solution for infusion contains only deionized water and sodium chloride (table salt).

The solution for infusion and capsules for oral administration are manufactured by the pharmaceutical concern GEDEON RICHTER, Plc., Hungary.

Photo of the original drug

Absorption, distribution and excretion from the body

After the drug enters the bloodstream, Mikosist penetrates all organs and tissues, creating especially high concentrations in the epidermis, dermis and secretions sweat glands. Moreover, the concentration of Mikosist in tissues is higher than in the blood.

Mykosist penetrates into all biological fluids - sweat, saliva, breast milk, sputum, vaginal secretions, joint, cerebrospinal and peritoneal fluid. In this case, a constant concentration in these liquids is achieved 8 hours after administration and remains unchanged throughout the day.

The half-life (the time during which half of the taken dose of the drug is eliminated from the body) of Mikosist is 30 hours. Mycosist is 80% excreted in the form of soluble metabolites by the kidneys. Therefore, the rate of drug excretion is higher, the better the functional state of the kidneys. The remaining 20% ​​of Mikosist is excreted in feces and sweat.

Mikosist (capsules, solution) – therapeutic effect

Mikosist has a detrimental effect on the following types of pathogenic fungi:

• All types of Candida spp.;


• Cryptococcus neoformans;


• All types of Microsporum spp.;


• All Trichoptyton spp.;


• Blastomyces dermatitides;


• Coccidioides immitis;


• Histoplasma capsulatum.

Mikosist is effective for the treatment of fungal intracranial infections caused by the above types of microorganisms. In addition, Mikosist effectively eliminates fungal infections that develop against the background of severe immunodeficiency.

Unlike other antifungal drugs, Mikosist does not have negative impact to the liver. Therefore, side effects and load on the liver when using Mikosist are significantly lower compared to other antifungal drugs, such as Intraconazole, Clotrimazole, Econazole and Ketoconazole.

What Mikosist treats – indications for use

1. Deep mycoses:
   
   
   • Cryptococcosis of the respiratory system, skin and mucous membranes, as well as cryptococcal meningitis and sepsis;
   • Prevention of cryptococcosis after organ transplantation or in patients with AIDS;
   
   
   • Histoplasmosis;
   
   
   • Coccidioidosis;
   
   
   • Sporotrichosis;
   
   
   • Systemic candidiasis (thrush of various localizations):
     
     
     • Generalized candidiasis (fungal infection of all organs and tissues);
     
     
     • Candidemia (blood infection by fungi of the genus Candida);
     
     
     • Visceral candidiasis (fungal infection of organs abdominal cavity, respiratory system, eyes or heart sac);
     
     
     • Candidiasis of the oral mucosa, pharynx or esophagus;
     
     
     • Candidiasis of the bronchi and lungs;
     
     
     • Genital candidiasis (vagina, penis (balanitis), perineal skin and perianal area);
     
     
     • Candidiasis urinary tract(urethra and ureters);
     
     
     • Candiduria (fungi in the urine in the absence of clinical symptoms of thrush);
     
     
     • Candidiasis of the skin and nails;
     
     
     • Prevention of relapse of candidiasis of the oral cavity and pharynx in patients with AIDS;
   
   
   • Mycoses of the skin of the body, inguinal folds, feet and hands:
     
     
     • Dermatophytosis of the feet and smooth skin;
     
     
     • Onychomycosis (damage to nails);
     
     
     • Pityriasis versicolor (lichen versicolor);
     
     
   
   
   • Prevention of fungal infections in people suffering from malignant tumors, AIDS, secondary immunodeficiencies any etiology;
   
   
   • Prevention of fungal infections during the use of cytostatics (drugs for chemotherapy malignant tumors), antibiotics, radiation therapy, or immunosuppressive agents to suppress graft-versus-host disease after organ transplantation.

   As can be seen from the list above, Mikosist is a very powerful antifungal drug, the range of use of which is not limited to treatment vaginal thrush.

   Instructions for use Mikosist - how to take capsules and inject solution

   The dosage, duration and frequency of use of Mikosist depends on the type of fungal infection. The choice of dosage form - capsules or solution for intravenous administration is determined solely by the person’s well-being. If a person is able to swallow capsules, then Mikosist is used in this form. If a person cannot swallow, then Mikosist is administered as an intravenous infusion. However, as soon as a person regains the ability to swallow, intravenous administration of the drug is replaced with capsules that must be taken orally. When switching from intravenous administration of Mikosist to taking capsules or vice versa, the dosage does not change.

   Capsules should be taken orally with a drink a small amount clean, still water. Capsules can be taken regardless of meals. The solution for infusion must be administered slowly at a rate of no more than 10 ml per minute. Mikosist for intravenous administration can be used in combination with the following solutions:

   • 20% glucose solution;
   
   
   • Ringer's or Ringer-Locke solution;
   
   
   • Hartmann's solution;
   
   
   • Potassium chloride solution on glucose;
   
   
   • Sodium bicarbonate solution;
   
   
   • Saline.

   Mikosist infusion is carried out using a conventional system (“dropper”) using any of the above solutions.

   Mikosist for adults - dosages and duration of use for the treatment of various fungal diseases

   Mycosist for cryptococcosis is used for the first dose in a daily dosage of 400 mg, which is taken completely at one time. In the future, the drug must be taken in a dosage of 200–400 mg once a day for 6–8 weeks. You should stop taking Mikosist only after no fungi are detected in the scraping or culture results. If Mikosist was used to treat cryptococcal meningitis, the duration of therapy should be at least 10 to 12 weeks. Therapy should be terminated only when the analysis cerebrospinal fluid fungi will not be detected.

   Mikosist for candidemia and candidiasis of internal organs on the first day of treatment is taken in a dose of 400 mg once. In the future, Mikosist should be taken 200 mg once a day for several weeks. If the drug is ineffective, you can increase the daily dosage to 400–800 mg. Treatment should be continued until clinical symptoms disappear completely.

   Mycosist for oropharyngeal candidiasis (oral cavity, pharynx or esophagus) should be taken 50–100 mg once a day for 1–2 weeks. To prevent relapses of this type of candidiasis in patients with AIDS, it is necessary to take 1 capsule of Mikosist 150 mg per week.

   Mycosist for atrophic candidiasis of the oral cavity, provoked by wearing dentures, should be taken 50 mg once a day for two weeks. On the background antifungal therapy It is necessary to treat dentures daily with antiseptic solutions.

   Mikosist at candida infections esophagus, bronchi, lungs, skin, mucous membranes and candiduria should be taken 50–100 mg once a day for 2–4 weeks. In case of severe fungal infection of the mucous membranes, the dosage of Mikosist can be increased to 100 – 200 mg per day.

   Mycosist for dermatophytosis of the skin should be taken 150 mg once a week or 50 mg every day for 2 to 4 weeks. When treating fungal infections of the feet, the course of treatment should be extended to 6 weeks.

   Mycosist for onychomycosis (fungal infections of the nails) must be taken 150 mg once a week until the new nail plate has completely grown. Typically, fingernails change within 3–6 months, and toenails within 6–12 months. Accordingly, the duration of treatment for onychomycosis of the fingers will be 3–6 months, and for the feet – 6–12 months.

   Mikosist for the prevention of fungal infections in people suffering from malignant neoplasms various organs, it is necessary to take 50 mg once a day as long as radiation therapy or chemotherapy is carried out.

   Mikosist for the treatment of vaginal candidiasis must be taken once at a dose of 150 mg. For chronic vaginal candidiasis, it is recommended to take 150 mg once a month for 4 to 12 months to prevent relapses.

   Mikosist for deep mycoses must be taken 200–400 mg once a day for two years. In principle, the duration of treatment is determined individually based on signs of clinical recovery. Coccidioidomycosis may require treatment for 11 to 24 months, paracoccidioidomycosis for 2 to 17 months, and histoplasmosis for 2 to 17 months. However, you can stop taking Mikosist only when, according to test results, fungi are no longer detected in the tissues of the body.

   Mikosist at pityriasis versicolor you need to take 50 mg once a day for 2 to 4 weeks. You can also take the drug 300 mg once every seven days for two weeks.

   Mikosist for children

   Maximum daily dosage for children should not exceed that for adults. The duration of therapy with Mikosist depends on the onset of clinical recovery. Typically, treatment is continued until fungi are no longer detected in tests.

   The dosage of Mikosist for children is calculated individually based on body weight. The calculation is made based on the ratio of 3 – 12 mg of fluconazole per kilogram of weight per day. For example, a child weighs 10 kg. This means that the daily dose of Mikosist for him can be: 3*10 = 30 and 12*10 = 120, that is, from 30 to 120 mg of the drug. The heavier fungal infection in a child, the higher the dosage of Mikosyst (within the permissible calculated spread) is used for its treatment.

   Mikosist should only be administered intravenously to newborn children, as they are unable to swallow the capsule. The solution is administered slowly, dosages are calculated according to the same rules as for older children (at the rate of 3 - 12 mg per kilogram of weight per day). However, for newborn children under 1 month of age, Mikosist is administered at intervals of 3 days. For infants aged 1 – 12 months, Mikosist is administered with a minimum interval of 2 days.

   To old people;

   Elderly people take Mikosist in standard dosages for adults if they do not suffer from kidney disease. If a person suffers from kidney disease, then the dosage of Mikosist is calculated individually and adjusted before each dose based on creatinine clearance.

   Mikosist 150 for thrush

   Vaginal thrush in women for effective treatment requires a single dose of Mikosist 150 mg capsule. If it is impossible to buy Mikosist in a dosage of 150 mg for some reason, then you should purchase three capsules of 50 mg or one 100 mg and 50 mg each. To treat thrush, you need to take 150 mg of Mikosist at a time, that is, either one 150 mg capsule, or all three 50 mg each, or two - one 100 mg and the second 50 mg. This single use of 150 mg of Mikosist is quite sufficient for treatment vaginal thrush among women. However, if a woman has chronic candidiasis (thrush), recurrent more than three times a year, then for its treatment it is necessary to adhere to the following regimen:
   • At the time of exacerbation, take 150 mg of Mikosist once;
   
   
   • Then, for 6 to 12 months, take another capsule of Mikosyst 150 mg once a month. The interval between taking Mikosist should be one month.

   Mikosist for men with thrush of the penis

   For the treatment of uncommon candidiasis balanitis or balanoposthitis (thrush of the penis), a single dose of Mikosist at a dose of 150 mg is sufficient for both men and women. However, if fungal infection penis is pronounced, then for its treatment it is recommended to use Mikosist according to the following scheme:
   • On the first day of treatment, take 150 mg of Mikosist at a time;
   
   
   • Over the next 7–10 days, take 50–100 mg of Mikosist once a day.
   If a man does not note the presence of candidiasis of the penis, but his partner is being treated for thrush, then he is recommended to take a single dose of 150 mg of Mikosist for prevention.

   Mikosist during pregnancy and breastfeeding

   Since the active substance of Mikosyst, fluconazole, penetrates the placenta to the fetus and into breast milk, ending up in them in the same concentration as in the woman’s blood, it can be used during pregnancy and breastfeeding only if the expected benefit exceeds possible risk for a child.

   Currently, given the one-time use and fairly big number Observations that have shown in practice that the drug is harmless to the fetus, doctors consider the use of Mikosist for the treatment of vaginal thrush during pregnancy and breastfeeding to be completely safe. In other cases, when more is expected long-term use Mikosista, it is contraindicated in pregnant and lactating women.

   Features of using Mikosist

   The drug can have a toxic effect on the liver, so during the entire period of treatment with Mikosist it is necessary to monitor the functioning of the organ. If signs of toxic liver damage appear (jaundice, increased activity of AST, ALT, etc.), it is necessary to urgently stop taking Mikosist.

   If any rash appears on the skin that can be associated with the use of Mikosist, the drug should also be stopped immediately. However, if severe systemic fungal diseases are being treated, then when a rash appears, it is necessary to continue therapy while carefully monitoring the dynamics of the rash. In such a situation, you should stop taking Mikosist only if bullous lesions of the skin or erythema multiforme develop.

   If a person receives anticoagulants at the same time as Mikosist indirect action(for example, Warfarin, Thrombostop, etc.), then prothrombin time (PTI) should be monitored every week.

   Mycosist can provoke dizziness, so during treatment it is recommended to abandon any activity associated with the need for increased attention and rapid response, including from driving a car. However, if this is not possible, then when carrying out activities that require high speed psychomotor reactions, you must be careful and carefully follow safety rules.

   Overdose;

   An overdose of Mikosist is possible when taking more than 800 mg of the drug per day. Symptoms of overdose include nausea, vomiting, diarrhea, seizures, hallucinations, and paranoia. For treatment, you must first rinse the stomach, give the poisoned person a diuretic drinking plenty of fluids and perform hemodialysis. Suppress painful symptoms with appropriate medications as needed.

   Interaction of Mikosist with other drugs

   Mikosist can reduce or increase the effects of indirect anticoagulants, such as Warfarin, Thrombostop and others, as a result of which, when using these drugs in combination, it is necessary to monitor the prothrombin time (PTI, INR).

   Mikosist can enhance the effect of Phenytoin, sulfonylurea derivatives (Glibenclamide, Gliquidone, etc.), Rifabutin, Cyclosporine, Zidovudine, Theophylline, Midazolam and Tacrolimus. Therefore, when using Mikosist simultaneously with these drugs, it is necessary to reduce the dosage of the latter and carefully monitor the development side effects.

   Hydrochlorothiazide and Rifampicin reduce the concentration and, accordingly, the severity of the action of Mikosist when used simultaneously. Therefore, when using them simultaneously, it is recommended to increase the dosage of Mikosist by 25 - 30%.

   Mikosist in combination with Cisapride and H1-antihistamines - terfenadine derivatives (for example, Bronal, Trexin, etc.) is prohibited, since this combination can provoke cardiac arrhythmia.

   Mikosist - contraindications for use

   The entire set of contraindications to the use of Mikosist is divided into two categories - relative and absolute. If there are absolute contraindications, the drug cannot be used under any circumstances. If there are relative contraindications, the drug can be used, but with caution, carefully monitoring the occurrence of side or undesirable effects, the development of which requires urgent withdrawal of Mikosist. In principle, in the presence of relative contraindications, Mikosist can be used if the expected benefit outweighs the possible harm.

   Absolute contraindications to the use of Mikosist include the following:

   • Simultaneous use with Cisapride, Astemizole, and drugs containing terfenadine (for example, Bronal, Trexin, etc.);
   
   
   • Breastfeeding period;
   
   
   • Hypersensitivity or allergic reactions to any substances included in the drug;
   
   
   • Hypersensitivity or allergy to drugs containing azole compounds (for example, Imidazole, Clotrimazole, Zalain, Livarol, Lomexin, etc.);
   
   
   • Child under 6 months of age (only for capsules as the child is not able to swallow them).

   TO relative contraindications The uses of Mikosist include the following:

   • Kidney failure;
   
   
   • Liver failure;
   
   
   • The appearance of a rash during the use of Mikosist for the treatment of superficial and systemic fungal infections;
   
   
   • Simultaneous use of Rifabutin;
   
   
   • A high risk of developing arrhythmia in a person (for example, due to heart disease, an imbalance of electrolytes and taking drugs that provoke arrhythmias);
   
   
   • Intolerance acetylsalicylic acid(Aspirin);
   
   
   • Pregnancy

   Mikosist - side effects

   Mycosist penetrates almost all tissues, so it can provoke side effects from any organs and systems.
   Currently, the following side effects of Mikosist have been identified and proven:
   
   
   1. From the digestive tract:
      • Nausea;
      
      
      • Vomit;
      
      
      • Diarrhea;
      
      
      
      
      
      • Taste disturbances;
      
      
      • Malfunction of baking ( increased concentration bilirubin, transaminase activity - AST, ALT, alkaline phosphatase in the blood, hepatitis, jaundice, necrosis of liver cells);
   
   
   2. From the outside nervous system :
   
   
   3. From the hematopoietic organs:
      • Decrease in the total number of leukocytes in the blood;
      
      
      • Decrease in the total number of platelets in the blood;
      
      
      • Decrease in the number of neutrophils in the leukoformula;
      
      
      • Simultaneous decrease in the number of neutrophils, basophils and eosinophils in the leukoformula;
   
   
   4. Allergic reactions:
      • Skin rashes;
      
      
      • Exudative erythema multiforme;
      
      
      • Stevens-Johnson syndrome;
      
      
      • Lyell's syndrome;
      
      
      • Anaphylactic reactions (Quincke's edema, urticaria, massive itching of the entire skin);
      
      
      • Bronchial asthma (most often develops in people who cannot tolerate Aspirin);
   
   
   5. From the outside of cardio-vascular system:
      • Arrhythmia (ventricular fibrillation or flutter);
      
      
      • Changes in the ECG (increased duration of the QT interval);
   
   
   6. From the endocrine organs (metabolism):
      • Increased concentration of total cholesterol in the blood;
      
      
      • Increased concentration of triglycerides (TAG, TG) in the blood;
      
      
      • Decreased potassium concentration in the blood (hypokalemia);
   
   
   7. From other organs and systems:
      • Impaired kidney function;
      
      

   Mikosist - analogues

   Currently on the domestic pharmaceutical market There are analogues and synonyms of Mikosist. Synonyms are antifungal drugs, which, like Mikosist, contain fluconazole as an active ingredient. Analogs of Mikosist are drugs that contain another active substance (not fluconazole), but have an antifungal effect of similar strength and spectrum.

   Synonymous drugs for Mikosist are the following:

   1. Vero-Fluconazole capsules;
   2. Diflazon capsules and solution for infusion;
   
   
   3. Difluzol capsules
   4. Diflucan capsules, powder for suspension and solution for infusion;
   5. Miconil solution for infusion;
   6. Medoflucon capsules and solution for infusion;
   7. Mycomax capsules, syrup and solution for infusion;
   8. Mikoflucan tablets and solution for infusion;
   9. Nofung capsules;
   10. Procanazole capsules;
   11. Fangiflu capsules;
   12. Fluzol capsules;
   13. Flucosan solution for infusion;
   14. Flucoside capsules;
   15. Flucomabol solution for infusion;
   16. Fluconazole capsules, tablets and solution for infusion;
   17. Fluconorm capsules;
   18. Flucorus solution for infusion;
   19. Flunol capsules;
   20. Flucostat capsules and solution for infusion;
   21. Forkan capsules and solution for infusion;
   22. Funzol capsules;
   23. Ciskan capsules.
   The analogue drugs of Mikosist are the following:
   • Vfend tablets and lyophilisate for the preparation of solution for infusion;
   • Voriconazole Canon tablets;
   • Irunin capsules;
   • Itrazole capsules;
   • Itraconazole capsules;
   • Canditral capsules;
   • Myconihol capsules;
   • Noxafil suspension for oral administration;
   • Orungal capsules and oral solution;
   • Orungamine capsules;
   • Orunit capsules;
   • Rumicosis capsules;
   • Teknazole capsules.

   Mikosist - reviews

   Currently, approximately 80% of reviews about Mikosist are positive, and 20% are negative. Moreover, reviews, as a rule, are left by people who have used the drug to treat vaginal thrush, fungal tonsillitis and stomatitis in children and adults.

   Most positive reviews about the drug is due to the fact that Mikosist has a good therapeutic effect, allowing it to quickly cure thrush of the genital organs and oral cavity. In positive reviews, people who have used the drug to treat fungal infections note the following inherent advantages of Mikosist - rapid onset of clinical recovery, high efficiency, reliable cure without recurrence of thrush in the future, the possibility of use in children and pregnant women, convenient dosages, help against any type of candidiasis . Separately, women note high efficiency Mikosysta in the treatment of genital thrush caused by resistant or atypical varieties of fungi of the genus Candida. Disadvantages of Mikosist according to people who wrote about the drug positive reviews, are its relative high cost and too long and detailed instructions.

   Negative reviews about Mikosist associated with the lack of what was expected clinical effect. There are practically no reviews that indicate that the drug did not help cure thrush at all. And a negative opinion about Mikosist is formed according to the following mechanism - a person expects an instant effect from the drug, which will literally completely normalize his condition and make him completely healthy. However, Mikosist is not a “magic capsule” that will get rid of all diseases; it effectively destroys only fungi. If you are in the mood for a “full recovery,” a person takes Mikosist, which actually eliminates thrush, but general state does not become excellent, since the problems that led to the manifestation of candidiasis remain and need to be treated separately. As a result, the result is completely different from the one the person was expecting (“full recovery”) and disappointment quite naturally appears. It is against this background that negative reviews are left.

   Mikosist, Fluconazole, Flucostat and Diflucan - what is the difference?

   Both Mikosist, and Diflucan, and Fluconazole, and Flucostat are antifungal drugs containing fluconazole as the active ingredient.

   However, this does not mean that they are exactly the same. Two drugs - Mikosist and Diflucan - are branded, and Fluconazole and Flucostat are so-called generics. And this is precisely the fundamental and huge difference between the drugs.

   A brand-name drug is a medicine developed by a pharmaceutical concern, tested for side effects and subject to quality control at all stages of production. In addition, the branded drug contains pure active substance without impurities, so it is well tolerated, works well and quickly and rarely causes side effects.

   These drugs are Mikosist and Diflucan. Mikosist is produced by the Hungarian concern GEDEON RICHTER, and Diflucan is produced by the French PFIZER.

   However, each branded drug has a patent validity period, after which any pharmaceutical companies can take the proportions of its composition and begin manufacturing their own medicine from existing ones. chemical substances, giving it a different name.

   Regarding Mikosist it looks like this: development company original drug indicates the contents in the instructions active substance 50, 100 and 150 mg fluconazole. After the patent expires, any pharmaceutical plant can purchase fluconazole or synthesize it in its laboratories and begin making its own antifungal drug, adding the same amount of active substance to it, but giving it a different name. These drugs are called generics.

   However, pharmaceutical factories producing generics do not control the quality of the fluconazole used, use other excipients, do not test the drug, do not monitor side effects, etc. All this leads to the fact that the quality of generics is significantly lower compared to branded drugs.

   Therefore, Mikosist and Diflucan have a clear advantage in the effectiveness and quality of components, as well as the rare development of side effects compared to Fluconazole and Flucostat. However, there are no fundamental differences between Mikosist and Diflucan, so you can choose any drug that a person likes more for some subjective reasons, since a positive psychological attitude always increases effectiveness drug therapy. However, branded drugs are always more expensive, which is a significant barrier to their use.

   Fluconazole and Flucostat are generics, so their effectiveness is lower than that of Diflucan and Mikosist, and the severity and frequency of side effects, on the contrary, is higher. There is no fundamental difference between Fluconazole and Flucostat, so you can choose any drug.

   Mikosist (50, 100 and 150) – price

   The cost of Mikosist in different pharmacies varies from 10 to 25%, which is explained by different pricing policies of retail chains, as well as the costs of storing and transporting the drug. Cost of various dosage forms and dosages of Mikosist are reflected in the table.
   

   Mikosist – where to buy?

   You can buy Mikosist in any regular pharmacy or online store. When purchasing, you should pay attention to the expiration date, which is 2 years from the date of production for the solution and 5 years for capsules. Mikosist should be stored in a cool, dark and dry place at a temperature not exceeding 30°C. Improper storage conditions reduce the effectiveness of the drug.
   Before use, you should consult a specialist.

In this article you can find instructions for use medicinal product Mikosist. Feedback from site visitors - consumers - is presented of this medicine, as well as the opinions of specialist doctors on the use of Mikosist in their practice. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Analogues of Mikosist if available structural analogues. Use for the treatment of candidiasis (thrush) and other mycoses in adults, children, as well as during pregnancy and breastfeeding. Composition of the drug.

Mikosist- antifungal drug. Fluconazole (the active ingredient of the drug Mikosist), a representative of the class of triazole antifungal agents, is selective inhibitor synthesis of sterols in fungal cells.

Fluconazole, being highly selective for cytochrome P450 of fungi, practically does not inhibit the cytochrome P450 system in the human body (in comparison with itraconazole, clotrimazole, econazole and ketoconazole, it suppresses cytochrome P450-dependent oxidative processes in human liver microsomes to a lesser extent).

Does not have androgenic activity.

Active against pathogens of mycoses caused by Candida spp. (candida), Cryptococcus neoformans (cryptococci), Microsporum spp., Trichophyton spp. Fluconazole has also been shown to be active in models of endemic mycoses, including infections caused by Blastomyces dermatitidis, Coccidioides immitis and Histoplasma capsulatum.

Compound

Fluconazole + excipients.

Pharmacokinetics

After intravenous administration, Mikosist penetrates well into body tissues and fluids. Concentrations of the drug in saliva, sputum, breast milk, joint and peritoneal fluid are similar to its concentration in blood plasma. In patients with fungal meningitis, the content of fluconazole in the cerebrospinal fluid reaches 80% of the corresponding concentration in plasma. Plasma concentrations are directly proportional to dose. 90% equilibrium concentration is achieved by 4-5 days with daily administration once a day. Use on the first day of a dose twice as high as usual daily dose, allows you to achieve 90% equilibrium concentration by the second day. The apparent volume of distribution approaches the total volume of water in the body. 11-12% of fluconazole is bound to plasma proteins. No metabolites were detected in peripheral blood. Fluconazole is excreted from the body mainly by the kidneys; in this case, approximately 80% of the administered dose is excreted unchanged.

Indications

• cryptococcosis: cryptococcal meningitis, cryptococcal infections of the lungs and skin; cryptococcal sepsis; prevention of relapse of cryptococcosis in patients with AIDS, organ transplantation or other cases of immunodeficiency;
• generalized candidiasis; candidemia, disseminated candidiasis and other forms of invasive candidal infections (infections of the abdominal cavity, endocardium, eyes, respiratory and urinary tract), incl. in patients receiving a course of cytostatic or immunosuppressive therapy, as well as in the presence of other factors predisposing to the development of candidiasis - treatment and prevention;
• candidiasis of the mucous membranes: oral cavity, incl. atrophic candidiasis of the oral cavity associated with wearing dentures; pharynx; esophagus and non-invasive bronchopulmonary infections, candiduria; prevention of relapse of oropharyngeal candidiasis in patients with AIDS;
• genital candidiasis: vaginal (acute or chronic recurrent);
• prevention of fungal infections in patients with malignant neoplasms who are predisposed to such infections as a result of chemotherapy with cytostatics or radiation therapy;
• mycoses of the skin, body, groin area;
• deep endemic mycoses, including coccidioidomycosis, paracoccidioidomycosis and histoplasmosis in patients with normal immunity.

Release forms

Capsules 50 mg, 100 mg and 150 mg (sometimes mistakenly called tablets).

Solution for infusion 2 mg/ml (in ampoules).

There are no other dosage forms of the drug, be it suppositories, ointment or cream.

Instructions for use and dosage regimen

For cryptococcal infections, the usual dose of Mikosist is 400 mg 1 time per day on the first day of treatment, then 200-400 mg 1 time per day. The duration of treatment for cryptococcal infections depends on clinical effectiveness, confirmed by mycological research, and usually ranges from 6 to 8 weeks.

To prevent relapse of cryptococcal meningitis in AIDS patients after completing the full course of primary therapy, Mikosist is prescribed at a dose of at least 200 mg per day for a long period.

For candidemia, disseminated candidiasis and other invasive candidal infections, the dose of fluconazole is 400 mg on the first day and 200 mg on subsequent days. If necessary, the dose of the drug can be increased to 400 mg per day. The duration of treatment depends on clinical effectiveness.

For severe systemic candidiasis, the dose may be increased to 800 mg per day. The duration of therapy depends on clinical effectiveness. Should be continued for at least 2 weeks after a negative blood culture has been obtained or after symptoms have resolved.

For oropharyngeal candidiasis, including patients with immunocompromised patients, the usual dose of fluconazole is 50-100 mg once a day for 7-14 days. To prevent relapses of oropharyngeal candidiasis in patients with AIDS after completing the full course of primary therapy - 150 mg once a week. If necessary, treatment can be extended, especially in severe immune disorders.

For atrophic oral candidiasis associated with wearing dentures, fluconazole is usually prescribed 50 mg once a day for 14 days in combination with antiseptics for processing the prosthesis.

For other candidiasis infections, for example, esophagitis, non-invasive bronchopulmonary infections, candiduria, candidiasis of the skin and mucous membranes, the daily dose is 50-100 mg for 14-30 days.

For severe candidiasis of the mucous membranes - 100-200 mg per day.

For the prevention of fungal infections in patients with malignant neoplasms, the dose of Mikosist is 50 mg 1 time per day as long as the patient is in the group increased risk due to cytostatic or radiation therapy.

At vaginal candidiasis- 150 mg once. To reduce the frequency of relapses, use 150 mg once a month for 4-12 months, sometimes more frequent use may be required.

For the prevention of candidiasis, the recommended dose of fluconazole is 50-400 mg once a 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 long-lasting neutropenia, the recommended dose is 400 mg 1 time per day. Fluconazole is prescribed several days before the expected onset of neutropenia; after the number of neutrophils increases to more than 1000/μl, treatment is continued for another 7 days.

For deep endemic mycoses, it may be necessary to use the drug at a dose of 200-400 mg per day for 2 years. The duration of therapy is determined individually; it can be 11-24 months for coccidioidomycosis; 2-17 months for paracoccidioidomycosis and 3-17 months for histoplasmosis.

In children, the drug should not be used in a daily dose higher than that in adults. The duration of treatment depends on the clinical and mycological effect.

For the treatment of generalized candidiasis and cryptococcal infection, the recommended dose is 6-12 mg/kg per day, depending on the severity of the disease.

For the prevention of fungal infections in children with reduced immunity, in whom the risk of developing infection is associated with neutropenia developing as a result of cytotoxic chemotherapy or radiation therapy, the drug is prescribed at 3-12 mg/kg per day, depending on the severity and duration of the induced neutropenia.

In newborns, Mikosist is eliminated more slowly, therefore, in the first 2 weeks of life, the drug is prescribed in the same dose (in mg/kg) as in older children, but with an interval of 72 hours. For children aged 3-4 weeks, the same dose is administered with at intervals of 48 hours.

In elderly patients in the absence of renal impairment, the usual dosage recommendations should be followed.

Rules for using the drug

Administer intravenously at a rate of no more than 20 mg (10 ml) per minute. When converting from intravenous administration to taking capsules and vice versa, there is no need to change the daily dose of the drug.

Mikosist solution for infusion is compatible with the following solutions: 20% glucose solution, Ringer's solution, Hartmann's solution, potassium chloride solution in glucose, sodium bicarbonate solution, 0.9% sodium chloride solution. Fluconazole infusions can be administered using conventional transfusion sets using one of the solutions listed above.

Side effect

• nausea, vomiting;
• diarrhea;
• flatulence;
• abdominal pain;
• change in taste;
• liver dysfunction (hyperbilirubinemia, increased activity of liver transaminases, alkaline phosphatase, jaundice, hepatitis, hepatocellular necrosis, including fatal);
• headache;
• dizziness;
• convulsions;
• leukopenia, thrombocytopenia, neutropenia, agranulocytosis;
• skin rash;
• exudative erythema multiforme (including Stevens-Johnson syndrome);
• toxic epidermal necrolysis (Lyell's syndrome);
• anaphylactoid reactions (including angioedema, facial swelling, urticaria, skin itching);
• bronchial asthma (more often with intolerance to acetylsalicylic acid);
• increase in the duration of the QT interval on the ECG;
• ventricular fibrillation/flutter;
• hypercholesterolemia;
• hypokalemia;
• renal dysfunction;
• alopecia.

Contraindications

• simultaneous use of terfenadine (against the background constant reception fluconazole at a dose of 400 mg per day and above) and cisapride, because both drugs prolong the QT interval and increase the risk of developing severe cardiac arrhythmias;
• simultaneous use astemizole;
• lactation period (breastfeeding);
• children up to 6 months (for oral administration);
• increased sensitivity to the components of the drug or azole compounds similar in structure.

Use during pregnancy and breastfeeding

The use of Mikosist during pregnancy is only possible if the potential benefit to the mother outweighs the risk to the fetus.

Fluconazole is determined in breast milk in the same concentration as in plasma, therefore its administration during lactation is contraindicated.

Use in elderly patients

In elderly patients in the absence of signs of renal failure, the usual dosage regimen should be followed.

Use in children

special instructions

Treatment with fluconazole must be continued until clinical and hematological remission occurs. Premature cessation of treatment leads to relapses.

Since fluconazole is eliminated primarily by the kidneys, caution should be exercised in patients with renal failure. At long-term treatment fluconazole dosing should be carried out taking into account QC.

In rare cases, the use of Mikosist was accompanied toxic effect on the liver, incl. and fatal, mainly in patients with serious concomitant diseases. It is necessary to monitor liver function. If signs of liver damage appear that may be associated with taking fluconazole, the drug should be discontinued.

While taking the drug, patients experienced rare cases development of exfoliative skin reactions such as Stevens-Johnson syndrome and toxic epidermal necrolysis. Patients with AIDS and cancer are more likely to develop severe skin reactions when using many drugs. If a patient develops a rash during treatment for a superficial fungal infection that can be associated with the use of fluconazole, the drug should be discontinued. If rash occurs in patients with invasive/systemic fungal infections, they should be monitored closely and fluconazole should be discontinued if bullous lesions or erythema multiforme develop.

It is necessary to monitor prothrombin time in patients receiving fluconazole and indirect anticoagulants coumarin series.

Impact on the ability to drive vehicles and operate machinery

Patients should use caution when administering vehicles or when operating machinery, as dizziness may occur during treatment with fluconazole.

Drug interactions

In patients receiving Mikosist and indirect coumarin anticoagulants, careful monitoring of prothrombin time is necessary, as it may increase.

Fluconazole for simultaneous administration can prolong T1/2 of sulfonylurea derivatives, therefore, when joint use the possibility of hypoglycemia should be taken into account.

The simultaneous use of Mikosist and phenytoin may be accompanied by an increase in the concentration of phenytoin to a clinically significant extent, which requires a reduction in its dose.

The combined use of fluconazole and rifabutin is accompanied by an increase in the serum concentration of the latter, and the development of uveitis is possible.

When using fluconazole and cyclosporine together, it is recommended to monitor the concentration of the latter in the blood, as it may increase.

Given the occurrence of serious, life-threatening arrhythmias in patients taking antifungal agents- azole derivatives in combination with terfenadine, their joint reception contraindicated.

Cases have been described with the simultaneous use of Mikosist and cisapride adverse reactions from the heart, including paroxysms of ventricular tachycardia. Simultaneous use is contraindicated.

When combined with fluconazole, it is possible to increase the concentration of zidovudine in the blood plasma. Patients receiving this combination should be monitored for side effects of zidovudine.

Taking fluconazole leads to a decrease in average speed clearance of theophylline from blood plasma, therefore, the risk of developing the toxic effect of theophylline and its overdose increases.

The simultaneous use of fluconazole and midazolam leads to a significant increase in the concentration of the latter in the blood plasma and the risk of developing psychomotor reactions.

When taking fluconazole and hydrochlorothiazide simultaneously, the concentration of fluconazole in the blood plasma increases by 40%.

When fluconazole and tacrolimus are taken simultaneously, the concentration of the latter in the blood serum increases, which leads to an increased risk of nephrotoxicity.

Analogues of the drug Mikosist

Structural analogues of the active substance:

• Vero Fluconazole;
• Disorel Sanovel;
• Diflazon;
• Diflucan;
• Maiconil;
• Medoflucon;
• Mycomax;
• Mycoflucan;
• Nofung;
• Procanazole;
• Fangiflu;
• Flucosan;
• Flucoside;
• Flucomabol;
• Flucomicide;
• Fluconazole;
• Fluconorm;
• Flucoral;
• Flucorus;
• Flucorem;
• Flucostat;
• Forkan;
• Fungolon;
• Ciskan.

If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.

Description of the drug

Fluconazole, being highly selective for cytochrome P450 of fungi, practically does not inhibit the cytochrome P450 system in the human body (in comparison with itraconazole, clotrimazole, econazole and ketoconazole, it suppresses cytochrome P450-dependent oxidative processes in human liver microsomes to a lesser extent).

Does not have androgenic activity.

Active regarding pathogens of mycoses caused by Candida spp., Cryptococcus neoformans, Microsporum spp., Trichophyton spp. Fluconazole has also been shown to be active in models of endemic mycoses, including infections caused by Blastomyces dermatitidis, Coccidioides immitis and Histoplasma capsulatum.

List of analogues

Note! The list contains synonyms Mikosist having similar composition, so you can choose a replacement yourself, taking into account the form and dose of the medicine prescribed by your doctor. Give preference to manufacturers from the USA, Japan, Western Europe, as well as well-known companies from of Eastern Europe: KRKA, Gedeon Richter, Actavis, Aegis, Lek, Hexal, Teva, Zentiva.

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Official instructions for use

Mikosist ® (MYCOSYST ®)

Pharmacological properties

Indications for use

Contraindications

Pregnancy and lactation

Directions for use and doses

Side effects

Overdose

Interaction with other drugs

special instructions

Release form

Best before date

Storage conditions

Vacation conditions

Manufacturer

The information on the page was verified by physician-therapist E.I. Vasilyeva.

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Good day, I would like to warn you about the use of the drug Mikosist. Found fungi in the intestines, took 150 mg. Previously, there was no allergy to fluconazole. After an hour or a few hours at most, itching began in the vagina, and in the morning I woke up to find very swollen lips, red eyes, red spots all over the outer part of the vagina, and hives all over the body. I took loratadine... Good day, I would like to warn you about the use of the drug Mikosist.
Found fungi in the intestines, took 150 mg. Previously, there was no allergy to fluconazole.
After an hour or a few hours at most, itching began in the vagina, and in the morning I woke up to find very swollen lips, red eyes, red spots all over the outer part of the vagina, and hives all over the body. I took loratadine and my lips cleared up a little.
Not understanding what was going on at first, I used zalain for thrush (cream and suppository), nothing helped. In the end, herpes began at the spots, which never happened. I went to a gynecologist, got tested, and my fears were confirmed.
As prescribed by another doctor, I drank mycosist again, the reaction was exactly the same as described above.
Having felt the first itching in the vagina, I immediately took loratadine, woke up in the morning with less severe syndromes, slightly less swollen lips and less itching. Now I apply acyclovir, I’m afraid herpes will start on the hives.
Thanks to the producers of mykosist.
I don't recommend it at all. Terrible drug.
P.S. I had never had an allergy before.

Thrush is an infection that can appear at any time and from anything. I have a special relationship with this disease. My body reacts very negatively to climate change, change of environment, even change of tap water. As a result, candidiasis occurs quite often. Why haven't I tried pills... Thrush is an infection that can appear at any time and from anything. I have a special relationship with this disease. My body reacts very negatively to climate change, change of environment, even change of tap water. As a result, candidiasis occurs quite often. No matter what I have tried, tablets, suppositories, creams, and douching, everything helps only for a certain period until a new definite factor in my life. Until I met a former classmate who has been working as a gynecologist in a prestigious clinic for many years. Somehow they opened up and I told her my problem. To which she invited me to her place for examination. Based on the results of all the tests, she prescribed me a course of treatment, which included Mikosist. I was surprised that there were only 2 tablets, but I read the instructions about the drug and believed it. I completed the course of treatment, repeated tests showed that there was no thrush. So far I feel great, let's hope it stays that way. I also recommended Mikosist to my sister. She took it and also got rid of the discharge.

pharmachologic effect

Antifungal drug. Fluconazole, a member of the triazole antifungal class, is a selective inhibitor of sterol synthesis in fungal cells.

Fluconazole, being highly selective for cytochrome P450 of fungi, practically does not inhibit the cytochrome P450 system in the human body (in comparison with itraconazole, clotrimazole, econazole and ketoconazole, it suppresses cytochrome P450-dependent oxidative processes in human liver microsomes to a lesser extent).

Does not have androgenic activity.

Active regarding pathogens of mycoses caused by Candida spp., Cryptococcus neoformans, Microsporum spp., Trichophyton spp. Fluconazole has also been shown to be active in models of endemic mycoses, including infections caused by Blastomyces dermatitidis, Coccidioides immitis and Histoplasma capsulatum.

Pharmacokinetics

Suction

After oral administration, fluconazole is well absorbed, its bioavailability is 90%. Cmax after oral administration on an empty stomach of 150 mg is achieved after 0.5-1.5 hours and is 90% of the plasma concentration when administered intravenously at a dose of 2.5-3.5 mg/kg. Concomitant food intake does not affect the absorption of the drug taken orally.

Distribution

After oral and intravenous administration, fluconazole penetrates well into all tissues and fluids of the body. In the stratum corneum of the epidermis, dermis and sweat fluid, high concentrations are reached that exceed serum concentrations. After oral administration 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 taking the second dose - 7.1 mcg/kg, the concentration in the nails after 4 months of use at a dose of 150 mg 1 time/week - 4.05 mcg/g in healthy and 1.8 mcg/g in affected nails. Concentrations of the drug in saliva, sputum, breast milk, joint and peritoneal fluid are similar to its concentration in blood plasma. In patients with fungal meningitis, the content of fluconazole in the cerebrospinal fluid reaches 80% of the corresponding concentration in plasma. Constant values ​​in vaginal secretions are achieved 8 hours after oral administration and are maintained at this value for at least 24 hours.

Plasma concentrations are directly proportional to dose. 90% equilibrium concentration is achieved by 4-5 days with daily oral or intravenous administration 1 time / day.

Use on the first day of a dose 2 times higher than the usual daily dose allows you to achieve 90% of the equilibrium concentration by the second day. The apparent V d approaches the total volume of water in the body. 11-12% of fluconazole is bound to plasma proteins.

Metabolism and excretion

It is an inhibitor of the CYP2C9 isoenzyme in the liver. No fluconazole metabolites were detected in peripheral blood.

T1/2 - 30 hours. The pharmacokinetics of fluconazole significantly depends on the functional state of the kidneys, and there is an inverse relationship between T1/2 and creatinine clearance. Fluconazole is excreted from the body mainly by the kidneys; in this case, approximately 80% of the administered dose is excreted unchanged. Fluconazole clearance is directly proportional to creatinine clearance.

After hemodialysis for 3 hours, the concentration of fluconazole in plasma decreases by 50%.

Indications

— cryptococcosis: cryptococcal meningitis, cryptococcal infections of the lungs and skin; cryptococcal sepsis; prevention of relapse of cryptococcosis in patients with AIDS, organ transplantation or other cases of immunodeficiency;

- generalized candidiasis; candidemia, disseminated candidiasis and other forms of invasive candidal infections (infections of the abdominal cavity, endocardium, eyes, respiratory and urinary tract), incl. in patients receiving a course of cytostatic or immunosuppressive therapy, as well as in the presence of other factors predisposing to the development of candidiasis - treatment and prevention;

— candidiasis of the mucous membranes: oral cavity, incl. atrophic candidiasis of the oral cavity associated with wearing dentures; pharynx; esophagus and non-invasive bronchopulmonary infections, candiduria; prevention of relapse of oropharyngeal candidiasis in patients with AIDS;

- genital candidiasis: vaginal (acute or chronic recurrent);

- prevention of fungal infections in patients with malignant neoplasms who are predisposed to such infections as a result of chemotherapy with cytostatics or radiation therapy;

- mycoses of the skin, trunk, groin area;

— deep endemic mycoses, including coccidioidomycosis, paracoccidioidomycosis and histoplasmosis in patients with normal immunity.

Dosage regimen

At cryptococcal infections The usual dose of fluconazole is 400 mg 1 time / day on the first day of treatment, subsequently - 200-400 mg 1 time / day. The duration of treatment for cryptococcal infections depends on the clinical effectiveness confirmed by mycological examination, and usually ranges from 6 to 8 weeks.

For prevention of relapse of cryptococcal meningitis in patients with AIDS after completing the full course of primary therapy, fluconazole is prescribed at a dose of at least 200 mg/day for a long period.

At candidemia, disseminated candidiasis and other invasive candidal infections The dose of fluconazole is 400 mg on the first day and 200 mg on subsequent days. If necessary, the dose of the drug can be increased to 400 mg/day. The duration of treatment depends on clinical effectiveness.

At severe systemic candidiasis it is possible to increase the dose to 800 mg/day. The duration of therapy depends on clinical effectiveness. Should be continued for at least 2 weeks after a negative blood culture has been obtained or after symptoms have resolved.

At oropharyngeal candidiasis, including patients with impaired immunity, the usual dose of fluconazole is 50-100 mg 1 time / day for 7-14 days. For prevention of relapses of oropharyngeal candidiasis in patients with AIDS after completing the full course of primary therapy - 150 mg once a week. If necessary, treatment can be extended, especially in severe immune disorders.

At atrophic candidiasis of the oral cavity associated with wearing dentures, fluconazole is usually prescribed 50 mg 1 time / day for 14 days in combination with antiseptic agents for treating the prosthesis.

At other candidiasis infections, for example, esophagitis, non-invasive bronchopulmonary infections, candiduria, candidiasis of the skin and mucous membranes the daily dose is 50-100 mg for 14-30 days.

At severe candidiasis of the mucous membranes- 100-200 mg/day.

For prevention of fungal infections in patients with malignant neoplasms the dose of fluconazole is 50 mg 1 time/day as long as the patient is at increased risk due to cytostatic or radiation therapy.

At vaginal candidiasis- 150 mg once. To reduce the frequency of relapses, use 150 mg once a month for 4-12 months, sometimes more frequent use may be required.

For prevention of candidiasis The recommended dose of fluconazole is 50-400 mg 1 time/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 long-lasting neutropenia, the recommended dose is 400 mg 1 time / day. Fluconazole is prescribed several days before the expected onset of neutropenia; after the number of neutrophils increases to more than 1000/μl, treatment is continued for another 7 days.

At deep endemic mycoses It may be necessary to use the drug at a dose of 200-400 mg/day for 2 years. The duration of therapy is determined individually; it can be 11-24 months with coccidioidomycosis; 2-17 months at paracoccidioidomycosis and 3-17 months with histoplasmosis.

U children the drug should not be used in a daily dose exceeding that in adults. The duration of treatment depends on the clinical and mycological effect.

At candidiasis of the mucous membranes The recommended dose of fluconazole is 3 mg/kg/day. On the first day, a loading dose of 6 mg/kg may be prescribed in order to more quickly achieve equilibrium concentration.

For treatment of generalized candidiasis and cryptococcal infection The recommended dose is 6-12 mg/kg/day depending on the severity of the disease.

For prevention of fungal infections inchildrenwith reduced immunity, in whom the risk of developing infection is associated with neutropenia developing as a result of cytotoxic chemotherapy or radiation therapy, the drug is prescribed at 3-12 mg/kg per day, depending on the severity and duration of persistence of induced neutropenia.

U newborns fluconazole is eliminated more slowly, so in the first 2 weeks of life the drug is prescribed in the same dose (in mg/kg) as in older children, but with an interval of 72 hours. Children aged 3-4 weeks the same dose is administered at intervals of 48 hours.

U elderly patients in the absence of renal dysfunction, the usual recommendations for dosing of the drug should be followed.

For patients with impaired renal function (KR< 50 мл/мин) the dosage regimen should be adjusted. Fluconazole is excreted primarily by the kidneys unchanged. With a single dose of fluconazole, no dose changes are required. If a course of treatment is necessary in patients (including children) with impaired renal function, a loading dose of 50 mg to 400 mg should be initially administered. Subsequently, the daily dose, depending on the indications, is determined according to the following table.

Rules for using the drug

Administer intravenously at a rate of no more than 20 mg (10 ml) per minute. When converting from intravenous administration to taking capsules and vice versa, there is no need to change the daily dose of the drug.

Mikosist ® solution for infusion is compatible with the following solutions: 20% glucose solution, Ringer's solution, Hartmann's solution, potassium chloride solution in glucose, sodium bicarbonate solution, 0.9% sodium chloride solution. Fluconazole infusions can be administered using conventional transfusion sets using one of the solutions listed above.

Side effect

From the digestive system: nausea, vomiting, diarrhea, flatulence, abdominal pain, change in taste, liver dysfunction (hyperbilirubinemia, increased activity of liver transaminases, alkaline phosphatase, jaundice, hepatitis, hepatocellular necrosis, including death).

From the nervous system: headache, dizziness, convulsions.

From the hematopoietic organs: leukopenia, thrombocytopenia, neutropenia, agranulocytosis.

Allergic reactions: skin rash, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), anaphylactoid reactions (including angioedema, facial edema, urticaria, skin itching), bronchial asthma (more often with intolerance to acetylsalicylic acid).

From the cardiovascular system: increase in the duration of the QT interval on the ECG, ventricular fibrillation/flutter.

From the side of metabolism: hypercholesterolemia, hypertriglyceridemia, hypokalemia.

Others: renal dysfunction, alopecia.

Contraindications for use

- simultaneous use of terfenadine (against the background of constant use of fluconazole at a dose of 400 mg/day or higher) and cisapride, because both drugs prolong the QT interval and increase the risk of developing severe cardiac arrhythmias;

- simultaneous use of astemizole;

- lactation period (breastfeeding);

- lactose intolerance, lactase deficiency, glucose-galactose malabsorption;

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

WITH caution: liver and/or kidney failure; the appearance of a rash during the use of fluconazole in patients with superficial fungal infection and invasive/systemic fungal infections; simultaneous use of fluconazole with rifabutin or other drugs metabolized by isoenzymes of the cytochrome P450 system; simultaneous use of terfenadine and fluconazole at a dose of less than 400 mg/day; potentially proarrhythmogenic conditions in patients with multiple risk factors (organic heart disease, electrolyte imbalance, concomitant use of drugs that cause arrhythmias); intolerance to acetylsalicylic acid; pregnancy.

Use during pregnancy and breastfeeding

The use of Mikosist ® during pregnancy is possible only if the potential benefit to the mother outweighs the risk to the fetus.

Fluconazole is determined in breast milk in the same concentration as in plasma, therefore its administration during lactation is contraindicated.

Use in children

Overdose

Symptoms: nausea, vomiting, diarrhea; in severe cases, convulsions, hallucinations, and paranoid behavior may occur.

Treatment: gastric lavage, forced diuresis, hemodialysis, symptomatic therapy. After a 3-hour hemodialysis session, the concentration of fluconazole in the blood plasma decreases by approximately 50%.

Drug interactions

In patients receiving fluconazole and indirect coumarin anticoagulants, careful monitoring of prothrombin time is necessary, as it may increase.

Fluconazole, when taken simultaneously, can prolong T1/2 of sulfonylurea derivatives, therefore, when using them together, 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 to a clinically significant extent, which requires a reduction in its dose.

When taking rifampicin and fluconazole simultaneously, the Cmax and T1/2 of the latter decreases, therefore, if combined use is necessary, the dose of fluconazole should be increased.

The combined use of fluconazole and rifabutin is accompanied by an increase in the serum concentration of the latter, and the development of uveitis is possible.

When using fluconazole and cyclosporine together, it is recommended to monitor the concentration of the latter in the blood, as it may increase.

Given the occurrence of serious, life-threatening arrhythmias in patients taking antifungal agents - azole derivatives in combination with terfenadine, their combined use is contraindicated.

When taking fluconazole and cisapride simultaneously, cases of adverse reactions from the heart, including paroxysms of ventricular tachycardia, have been described. Simultaneous use is contraindicated.

When combined with fluconazole, it is possible to increase the concentration of zidovudine in the blood plasma. Patients receiving this combination should be monitored for side effects of zidovudine.

Taking fluconazole leads to a decrease in the average rate of clearance of theophylline from blood plasma, therefore, the risk of developing the toxic effect of theophylline and its overdose increases.

The simultaneous use of fluconazole and midazolam leads to a significant increase in the concentration of the latter in the blood plasma and the risk of developing psychomotor reactions.

When taking fluconazole and hydrochlorothiazide simultaneously, the concentration of fluconazole in the blood plasma increases by 40%.

When fluconazole and tacrolimus are taken simultaneously, the concentration of the latter in the blood serum increases, which leads to an increased risk of nephrotoxicity.

Caution must be exercised when using fluconazole in patients simultaneously receiving other drugs metabolized by isoenzymes of the cytochrome P450 system.

Conditions for dispensing from pharmacies

The drug in capsule form is approved for use as an over-the-counter product.

The drug in the form of a solution for infusion is available with a prescription.

Storage conditions and periods

The drug should be stored out of the reach of children at a temperature not exceeding 30°C. The shelf life of capsules is 5 years, solution for infusion is 2 years.

Use for liver dysfunction

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. The hepatotoxic effect of fluconazole is usually reversible; its signs disappeared after cessation of therapy. When clinical signs liver damage that may be associated with fluconazole, the drug should be discontinued.

Use for renal impairment

Patients with renal failure (KR<50 мл/мин) correction of the dosage regimen is required.

Fluconazole is excreted mainly in the urine unchanged. When taken once, no dose change is required. When re-prescribed to patients with impaired renal function, a loading dose of 50 mg to 400 mg should be administered.

At CC>50 ml/min the average recommended dose of the drug is used; at CC from 11 to 50 ml/min a dose of 50% of the recommended dose is used. For patients regularly undergoing hemodialysis, one dose of the drug is administered after each hemodialysis session.

Use in elderly patients

U elderly patients in the absence of signs of renal failure, the usual dosage regimen of the drug should be followed.

special instructions

Treatment with fluconazole must be continued until clinical and hematological remission occurs. Premature cessation of treatment leads to relapses.

Since fluconazole is eliminated primarily by the kidneys, caution should be exercised in patients with renal impairment. During long-term treatment with fluconazole, dosing should be carried out taking into account QC.

In rare cases, the use of fluconazole was accompanied by toxic effects on the liver, incl. and death, mainly in patients with serious underlying medical conditions. It is necessary to monitor liver function. If signs of liver damage appear that may be associated with taking fluconazole, the drug should be discontinued.

While taking the drug, patients experienced rare cases of exfoliative skin reactions, such as Stevens-Johnson syndrome and toxic epidermal necrolysis. Patients with AIDS and cancer are more likely to develop severe skin reactions when using many drugs. If a patient develops a rash during treatment for a superficial fungal infection that can be associated with the use of fluconazole, the drug should be discontinued. If rash occurs in patients with invasive/systemic fungal infections, they should be monitored closely and fluconazole should be discontinued if bullous lesions or erythema multiforme develop.

Caution is required when taking fluconazole simultaneously with rifabutin or other drugs metabolized by isoenzymes of the cytochrome P450 system.

It is necessary to monitor prothrombin time in patients simultaneously receiving fluconazole and indirect coumarin anticoagulants.

Impact on the ability to drive vehicles and operate machinery

Patients should be careful when driving or operating machinery, as dizziness may occur during treatment with fluconazole.