What do Fluconazole tablets help with? Mode of application. Medicinal reference book geotar Interaction with other drugs and other types of interactions

Diseases caused by pathogenic fungi cause a lot of trouble and require immediate treatment. Candidiasis or thrush is a widespread disease in which the mucous membranes of various organs are affected by yeast-like fungi of the genus Candida.

Treatment of thrush in women

According to most experts in the field of treating fungal infections such as Candida, Fluconazole tablets (150 mg capsules) are the price of a comfortable healthy life without fungal diseases.

Fluconazole tablets

The drug inhibits (slows down) the development of pathogenic microorganisms and is one of the effective main drugs in the treatment of thrush and other diseases caused by fungi.

It is important to know! Fungi of the genus Candida are found in the normal composition of the microflora of the mucous membranes of most healthy people. Therefore, the disease is caused not so much by the presence of microorganisms as by their quantity.

Composition of the drug

Fluconazole is available in the form of capsules (tablets) containing granular yellowish or white powder.

It contains flucanozole (150 mg) and excipients: magnesium (calcium) stearate, low molecular weight polyvinylpyrrolidone, potato starch. The capsule body consists of gelatin, titanium dioxide and indigotine.

In pharmacies you can buy analogues of Fluconazole (tablets): Diflucan, Mikosist, Flucostat and others. The price of one package of 150 mg capsules ranges from 200 to 600 rubles, which depends on the manufacturer and the number of capsules in the blister.

Who is prescribed the medicine?

Fluconazole tablets (150 mg capsules), the price of which varies depending on the region of Russia, have a wide spectrum of action and treat candidiasis and mycoses in women, men and children.


A pharmacist, like a doctor, can suggest an effective remedy for thrush. How to advise taking Fluconazole 150 mg tablets.

Important to remember! Candidiasis (thrush) develops with a sharp increase in fungal microorganisms, the spread of which is due to the following factors:

  1. Weakening of the immune system.
  2. Lack of vitamins.
  3. Problems in the intestinal microflora.
  4. Decreased estrogen levels.
  5. Stressful situations.
  6. Violations of intimate hygiene rules.
  7. Fluctuations in hormonal balance as a result of taking contraceptives.

Directions for use and doses

The duration of treatment and the medication regimen are prescribed individually, depending on the type and severity of the disease.

Primary vaginal candidiasis is treated with a one-time dose of the drug

To reduce the frequency of relapses, take 150 mg once a month for 4-6 months. In some cases, the period may be extended.

If the disease has become chronic, then take 150 mg twice a day for 3 days in a row.

Contraindications

The main contraindications to taking the drug are:

  • hypersensitivity to the drug;
  • children under 4 years of age;
  • lactation period.

Consultation with a doctor is necessary if you have liver/kidney problems, a tendency to develop a rash, heart disease, or electrolyte imbalance.

Be careful! If an overdose occurs, then it is recommended to rinse the stomach. In severe cases, doctors prescribe forced diuresis.

Possible side effects

When taking the drug, side effects may occur from different body systems. Headache, nausea, sometimes vomiting, itching, swelling - these are just some of the unpleasant consequences of treatment.


The so-called thrush brings significant discomfort to women. The disease is accompanied by burning and itching in the genitals, a large amount of white discharge with an unpleasant odor.

If the drug is taken incorrectly, the lymphatic system and hematopoietic system, liver, kidneys, and immune system may suffer.

Metabolic disorders, tachycardia, liver failure, jaundice, and skin rash may occur. In some cases, dizziness and convulsions are possible.

Before you start taking the medicine, you should carefully read the instructions for the drug and get the recommendations of your doctor.

Interaction with other drugs

If you are taking other medications while taking Fluconazole, you should consult your doctor. for their combination with Fluconazole. This is especially true: anticoagulants, oral contraceptives, short-acting benzodiazepines, sulfonylureas, concurrent use of Astemizole and Terenadine, as this affects the functioning of the heart.

Consultation is also necessary if the patient is taking:

  • cyclosporine;
  • hydrochlorhyazide;
  • tacrolimus;
  • rifampicin;
  • cisapride;
  • theophylline;
  • zidovudine;
  • phenytoin,
    and some other drugs.

Shelf life and storage

The medicine is kept in a dry place, out of reach of the sun, at a temperature of 15 to 25° C. Shelf life – 3 years.

What is important to know about Fluconazole

Composition of the drug Fluconazole is rapidly absorbed. You can take the medicine with food, this does not reduce its absorption; after an hour and a half, the concentration of the drug in the blood reaches its peak.

Note! Diagnosis and treatment should be supervised by a doctor. The onset of improvement does not necessarily indicate complete recovery. To avoid a recurrence of the disease or to prevent it from becoming chronic, you must follow the recommendations of a specialist.

The opinion of doctors does not exclude an individual reaction to the drug

Where to buy Fluconazole tablets and their price

Fluconazole (tablets) can be bought in Russian pharmacies without a prescription. The price of a package of 150 mg capsules depends on the region and ranges from 12 to 50 rubles. Now you can buy the drug via the Internet by choosing from a network of pharmacies. The courier will deliver it to your home.

The active ingredient Fluconazole has been on the market for many years, so the pharmacy will recommend a reliable manufacturer at a reasonable price. It is not a problem to buy not only Fluconazole (tablets), but also its analogues produced by different companies.

The price of a blister with a 150 mg capsule, in this case, is significantly higher from foreign manufacturers. Prices start here from 200 rubles.

Fluconazole is one of the most effective and inexpensive drugs in the treatment of diseases caused by various fungal infections. Before using the drug, it is recommended to read the instructions to avoid undesirable consequences. Be healthy and take care of yourself!

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Fluconazole is an antimycotic drug that has proven itself to be an effective remedy against various types of fungus. It is used for mild, acute and chronic forms of diseases such as candidiasis, thrush, lichen, onychomycosis and many other mycoses.

Fluconazole does not just destroy the most noticeable symptoms, leaving the “infection” deep inside, as many other drugs do - it specifically affects the causative agent of the infection.

The main pharmacological action of Fluconazole is antifungal. The components of the product reduce the protective properties of the cell membrane of microorganisms, thereby stopping their reproduction, growth and development. It is quickly absorbed by the body and then excreted through the kidneys. It is used not only for treatment, but also for the prevention of possible relapse of mycosis.

Fluconazole is available in capsule form (50 and 150 mg). Inside is a white powder. The presence of foreign contamination is not allowed. The active substance is fluconazole, well-known to many. Additional components include anhydrous silicon dioxide, which is included in the composition of many products, lactose monohydrate, sodium lauryl sulfate, and starch.

The shell of Fluconazole capsules contains titanium dioxide, which helps get rid of the unpleasant symptoms of the fungus. The drug is also available as film-coated tablets (containing magnesium stearate), special solution and powder.

Fluconazole capsules 150 and 50 mg photo

It is worth noting that Fluconazole capsules (150 mg) are very popular, instructions for use are available below. However, this description is suitable for other dosage forms - for example, tablets or solution.

  • cryptococcosis;
  • generalized candidiasis of any form;
  • , including those caused by the installation of dentures;
  • in any form and in case of relapse;
  • prevention of mycoses in patients with tumors;
  • mycoses of the body and feet;
  • lichen (mostly -);
  • endemic mycoses.

In some cases, Fluconazole is used for children over 5 years of age if benefit is more likely than harm. In this case, the dosage and duration of use are discussed only with a doctor on an individual basis.

Instructions for use of Fluconazole by type of disease

symptoms of foot fungus

Fluconazole is administered orally. Check with your specialist for the duration of treatment and exact dosage. The following are average standard values ​​that are appropriate for most patients.

Cryptococcosis: the first day of therapy – 400 mg, then treatment continues at 200 mg/day. It is possible to get rid of cryptococcal meningitis within 6-8 weeks. Prevention lasts a long period of time after completion of the main drug course. The amount of the drug these days is 200 mg/day.

Generalized candidiasis: about 100 mg/day. The exact dosage should be discussed with a specialist. The duration of therapy is from 2-3 weeks. If there is a risk of worsening the disease, the dose of medication is often increased to 400 mg/day.

Fluconazole for candidiasis of the mucous membranes and skin: 50 to 150 mg/day. Treatment – ​​up to 1-2 months; if the disease is caused by wearing dentures, then they need to be treated with an antiseptic until recovery occurs. Usually this is 2-3 weeks.

Fluconazole for thrush in women used in the amount of 150 mg/day. Often a one-time dose of the drug is enough. It is often prescribed as a prophylaxis during menstruation, since at this time the likelihood of relapse or exacerbation of the disease is especially high.

Nail fungus. According to the instructions, you need to take 150 mg of Fluconazole for nail fungus - use should be weekly until complete recovery. The main criterion is the regrowth of the affected nail plate. It should have a pink color, not be partially deformed, not crumble or break.

  • On average, patients cope with the disease in 6 months for infected fingernails and in 9-12 months for infections on the feet.

For warning for the occurrence of mycoses in patients with tumors, 200 mg of the drug per day is used after completion of the main course of treatment.

For mycoses of the body and feet There are two treatment regimens. One of them is to use Fluconazole 150 mg (1 capsule), the instructions state that this amount should be used weekly. The second option is 50 mg/day. The treatment period is up to a month, but when the legs are infected, it often takes up to 6 weeks for complete recovery. At the end of therapy, peeling, itching, irritation and redness will disappear. There should be no pain when walking.

Pityriasis versicolor requires a double dosage of Fluconazole 150 mg - a total of 300 mg/week. The duration of therapy is about 14 days, it is advisable to use the product on the same day. Sometimes a single dose of 400 mg of the drug helps. Another treatment regimen is 50 mg/day for 3-4 weeks.

Deep endemic mycoses require the use of the drug in amounts of 200 to 400 mg daily. The duration of therapy is usually long - 2-3 years, if the patient unquestioningly follows all the doctor’s instructions.

Contraindications, side effects and overdose

The main limitation of Fluconazole is the presence of hypersensitivity to a particular component of the drug or the entire composition, as well as a history of other antimycotic drugs.

Other contraindications:

  • simultaneous use of terfenadine and drugs based on it, if the amount of Fluconazole used is 400 mg/day;
  • age up to 4 years.

With caution: alcoholism, kidney and/or liver failure, pregnancy, patients with possible arrhythmia, old age.

Fluconazole is not an antibiotic, so it does not cause severe damage to the immune system. The list of side effects includes:

  • nausea followed by vomiting, changes in taste, refusal to eat (loss of appetite, which goes away when you stop using the medicine), diarrhea, flatulence, hepatitis and jaundice (rarely);
  • severe headache, dizziness, fatigue;
  • leukopenia (rare);
  • typical allergic reactions - swelling, rash, itching, burning, as well as symptoms of urticaria, very rarely - anaphylactic shock;
  • interruptions in the functioning of the kidneys and/or liver.

Signs of an overdose of Fluconazole are hallucinations, a state of shock with paranoid behavior. Treatment consists of gastric lavage and a subsequent visit to the doctor.

Special instructions, pregnancy and breastfeeding

Remember that Fluconazole therapy cannot be interrupted, otherwise a relapse or exacerbation of the disease will occur. It is necessary to monitor the normal functioning of the liver and kidneys. If there are any signs of disruption to their functioning, consult a doctor, in which case you will have to stop using the product. This is especially true for older people.

If side effects occur, Fluconazole should be discontinued. The only exception is mild manifestations of allergies, but this can also be resolved together with a specialist.

In AIDS patients, itching, burning and due to fungal infections of the skin occur more often. If the cause of these symptoms is the use of Fluconazole, then the medicine must be stopped.

Slowing down the reaction and making it difficult to focus attention are unlikely, so the medication is approved for use by people driving various mechanisms and/or cars.

It is not recommended to use Fluconazole during pregnancy. The exception is a threat to the life of the mother. But at the same time, the probable benefit must exceed the possible risk to the life of the woman and the unborn child.

  • During lactation, the use of the drug is strictly prohibited. The concentration of the drug components in milk and plasma is the same.

Analogues of Fluconazole, list of drugs

If a decision has been made to replace Fluconazole with an analogue due to its lack of effectiveness or severe side effects, pay attention to the following drugs:

  1. Diflazon;
  2. Mycomax;
  3. Mikosist;
  4. Diflucan;
  5. Flucostat.

Despite the fact that the above drugs have similar compositions, actions, indications and contraindications (sometimes), it is recommended to consult a doctor before changing medications. Instructions for use of Fluconazole, reviews and prices for analogues do not apply and should not be used as a guide to the use, prescription or independent replacement of Fluconazole with an analogue.

Remember that the use of any medicine must be previously agreed with your doctor, and Fluconazole is no exception.

Latin name

Release form

1 capsule contains:

Active substance: fluconazole 150 mg;

Excipients: lactose monohydrate; pregelatinized starch; colloidal anhydrous silicon dioxide; magnesium stearate; sodium lauryl sulfate.

Package

pharmachologic effect

Fluconazole is an antifungal.

Pharmacodynamics

An antifungal agent that has a highly specific effect, inhibiting the activity of fungal enzymes dependent on cytochrome P450. Blocks the conversion of lanosterol from fungal cells into the membrane lipid - ergosterol; increases the permeability of the cell membrane, disrupts its growth and replication.

Fluconazole, being highly selective for fungal cytochrome P450, practically does not inhibit these enzymes 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 antiadrogenic activity.

Active against opportunistic mycoses, incl. caused by Candida spp. (including generalized forms of candidiasis due to immunosuppression), Cryptococcus neoformans and Coccidioides immitis (including intracranial infections), Microsporum spp. and Trichophyton spp.; for endemic mycoses caused by Blastomyces dermatidis, Histoplasma capsulatum (including immunosuppression).

Pharmacokinetics

After oral administration, fluconazole is well absorbed; food intake does not affect the rate of absorption of fluconazole, its bioavailability is 90%.

The time to reach the maximum concentration after oral administration of 150 mg of the drug on an empty stomach is 0.5-1.5 hours, Cmax is 90% of the plasma concentration when administered intravenously at a dose of 2.5-3.5 mg/l. T1/2 fluconazole is 30 hours. Communication with plasma proteins is 11-12%. Plasma concentration is directly dependent on dose. 90% level of equilibrium concentration is achieved by the 4-5th day of treatment with the drug (when taken once a day).

Administration of a loading dose (on the first day), 2 times higher than the usual daily dose, allows one to achieve a concentration level corresponding to 90% of the equilibrium concentration by the second day.

Fluconazole penetrates well into all biological fluids of the body. Concentrations of the active substance in breast milk, joint fluid, saliva, sputum and peritoneal fluid are similar to its levels in plasma. Constant values ​​in vaginal secretions are achieved 8 hours after oral administration and are maintained at this level for at least 24 hours. Fluconazole penetrates well into the cerebrospinal fluid (CSF) - with fungal meningitis, the concentration in the CSF is about 85% of its level in plasma. In sweat fluid, epidermis and stratum corneum (selective accumulation) concentrations exceeding serum levels are achieved. 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/g; concentration in nails after 4 months of use at a dose of 150 mg once a week is 4.05 mcg/g in healthy and 1.8 mcg/g in affected nails. The volume of distribution approaches the total water content of the body.

It is an inhibitor of the CYP2C9 isoenzyme in the liver. It is excreted primarily by the kidneys (80% unchanged, 11% in the form of metabolites). Fluconazole clearance is proportional to creatinine clearance. No fluconazole metabolites were detected in peripheral blood.

The pharmacokinetics of fluconazole depends significantly on the functional state of the kidneys, and there is an inverse relationship between the half-life and creatinine clearance. After hemodialysis for 3 hours, the concentration of fluconazole in plasma decreases by 50%.

Indications

  • cryptococcosis, including cryptococcal meningitis and other localizations of this infection (including lungs, skin), both in patients with a normal immune response and in patients with various forms of immunosuppression (including in patients with AIDS, with organ transplantation ); the drug can be used to prevent cryptococcal infection in patients with AIDS;
  • generalized candidiasis, including candidemia, disseminated candidiasis and other forms of invasive candidal infections (infections of the peritoneum, endocardium, eyes, respiratory and urinary tract). Treatment can be carried out in patients with malignant neoplasms, patients in the intensive care unit, patients undergoing cytostatic or immunosuppressive therapy, as well as in the presence of other factors predisposing to the development of candidiasis;
  • candidiasis of the mucous membranes, incl. oral cavity and pharynx (including atrophic candidiasis of the oral cavity associated with wearing dentures), esophagus, non-invasive bronchopulmonary candidiasis, candiduria, cutaneous candidiasis; prevention of relapse of oropharyngeal candidiasis in patients with AIDS;
  • genital candidiasis: vaginal candidiasis (acute and chronic recurrent), prophylactic use to reduce the frequency of relapses of vaginal candidiasis (3 or more episodes per year); candidal balanitis;
  • 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, including mycoses of the feet, body, and groin area; pityriasis versicolor (varicolored) lichen, onychomycosis; skin candidiasis;
  • deep endemic mycoses, including coccidioidomycosis, paracoccidioidomycosis, sporotrichosis and histoplasmosis in patients with normal immunity.

Contraindications

  • hypersensitivity to the drug (including a history of other azole antifungal drugs);
  • simultaneous use of terfenadine (while constantly taking fluconazole at a dose of 400 mg/day or more) or astemizole, as well as other drugs that prolong the QT interval;
  • children under 4 years of age.

With caution: liver and/or renal 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 terfenadine and fluconazole at a dose of less than 400 mg/day, simultaneous use of potentially hepatotoxic drugs, alcoholism, potentially proarrhythmogenic conditions in patients with multiple risk factors (organic heart disease, electrolyte imbalance, concomitant use of drugs that cause arrhythmias), pregnancy.

Use during pregnancy and breastfeeding

The use of the drug in pregnant women is not advisable, with the exception of severe or life-threatening forms of fungal infections, when the potential benefit of fluconazole for the mother significantly outweighs the risk to the fetus.

Since the concentration of fluconazole in breast milk and plasma is the same, the use of the drug during lactation is contraindicated.

Directions for use and doses

For adults and children over 15 years of age (body weight more than 50 kg) for cryptococcal meningitis and cryptococcal infections of other localizations, 400 mg (8 capsules of 50 mg each) is usually prescribed on the first day, and then treatment is continued at a dose of 200 mg (4 capsules of 50 mg each). ) - 400 mg (8 capsules of 50 mg each) 1 time per day. The duration of treatment for cryptococcal infections depends on clinical effectiveness confirmed by mycological examination; for cryptococcal meningitis, the course of treatment should be at least 6-8 weeks.

To prevent relapse of cryptococcal meningitis in patients with AIDS, after completing the full course of primary therapy, fluconazole is prescribed at a dose of 200 mg (4 capsules of 50 mg) per day for a long period of time.

For candidemia, disseminated candidiasis and other invasive candidal infections, on the first day the dose is 400 mg (8 capsules of 50 mg), and then 200 mg (4 capsules of 50 mg) per day. If clinical effectiveness is insufficient, the dose of the drug can be increased to 400 mg (8 capsules of 50 mg each) per day. The duration of therapy depends on clinical effectiveness.

For oropharyngeal candidiasis, the drug is usually prescribed 150 mg once a day, the duration of treatment is 7-14 days. If necessary, in patients with a pronounced decrease in immunity, treatment may be longer.

To prevent relapses of oropharyngeal candidiasis in patients with AIDS after completing the full course of primary therapy - 150 mg once a week.

For atrophic oral candidiasis associated with wearing dentures - 50 mg once a day for 14 days in combination with local antiseptic drugs to treat the denture.

For other localizations of candidiasis (except genital), for example, esophagitis, non-invasive bronchopulmonary lesions, candiduria, candidiasis of the skin and mucous membranes, etc., the effective dose is usually 150 mg/day with a treatment duration of 14-30 days.

For vaginal candidiasis, fluconazole is taken orally once at a dose of 150 mg. To reduce the frequency of relapses of vaginal candidiasis, the drug can be used at a dose of 150 mg once a month. The duration of therapy is determined individually; it varies from 4 to 12 months. Some patients may require more frequent use.

For balanitis caused by Candida, fluconazole is prescribed orally as a single dose of 150 mg/day.

For the prevention of candidiasis, the recommended dose is 50-400 mg 1 time per day, depending on the degree of risk of developing a fungal infection. For the prevention of candidiasis in patients with malignant neoplasms, the recommended dose of fluconazole is 150-400 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/day. Fluconazole is prescribed several days before the expected onset of neutropenia; after the number of neutrophils increases to more than 1 thousand/μl, treatment is continued for another 7 days.

For skin mycoses, including mycoses of the feet, skin of the groin area, and skin candidiasis, the recommended dose is 150 mg once a week or 50 mg once a day, the dosage regimen depends on the clinical and mycological effect. The duration of therapy in normal cases is 2-4 weeks, however, with mycoses of the feet, longer therapy (up to 6 weeks) may be required.

For pityriasis versicolor - 300 mg (2 capsules of 150 mg) once a week for 2 weeks, some patients require a third dose of 300 mg per week, while in some cases a single dose of 300-400 mg is sufficient; An alternative treatment regimen is to use 50 mg once a day for 2-4 weeks.

For onychomycosis, the recommended dose is 150 mg once a week. Treatment should be continued until the infected nail is replaced (the uninfected nail regrows). It normally takes 3-6 months and 6-12 months for fingernails and toenails to re-grow, respectively.

For deep endemic mycoses, it may be necessary to use the drug at a dose of 200 mg (4 capsules of 50 mg) - 400 mg (8 capsules of 50 mg) per day for up to 2 years. The duration of therapy is determined individually; it can be 11-24 months for coccidioidomycosis, 2-17 months for paracoccidioidomycosis, 1-16 months for sporotrichosis and 3-17 months for histoplasmosis.

In children, as 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 that would exceed that in adults, i.e. no more than 400 mg/day. The drug is used daily, once a day.

Side effects

From the digestive system: decreased appetite, taste changes, abdominal pain, vomiting, nausea, diarrhea, flatulence, rarely - impaired liver function (jaundice, hepatitis, hepatonecrosis, hyperbilirubinemia, increased activity of alanine aminotransferase, aspartate aminotransferase, increased activity of alkaline phosphatase, hepatocellular necrosis ), incl. heavy.

From the nervous system: headache, dizziness, excessive fatigue, rarely - convulsions.

From the hematopoietic organs: rarely - leukopenia, thrombocytopenia (bleeding, petechiae), neutropenia, agranulocytosis.

Allergic reactions: skin rash, rarely - exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), anaphylactoid reactions (including angioedema, facial edema, urticaria, skin itching) .

From the cardiovascular system: increased duration of the QT interval, ventricular fibrillation/flutter.

Other: rarely - renal dysfunction, alopecia, hypercholesterolemia, hypertriglyceridemia, hypokalemia.

special instructions

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

During treatment, it is necessary to monitor blood counts, kidney and liver function. If renal and liver dysfunction occurs, you should stop taking the drug.

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. In the case of hepatotoxic effects associated with fluconazole, there was no obvious dependence on the total daily dose, duration of therapy, gender and age of the patient. The hepatotoxic effects of fluconazole were usually reversible; its signs disappeared after cessation of therapy. If clinical signs of liver damage that may be associated with fluconazole appear, the drug should be discontinued.

People with AIDS are more likely to develop severe skin reactions when taking many drugs. In cases where a rash develops in patients with a superficial fungal infection and is assessed as definitely related to fluconazole, the drug should be discontinued. If a rash appears in patients with invasive/systemic fungal infections, they should be carefully monitored and fluconazole should be discontinued if bullous changes or erythema multiforme occur.

Caution should be exercised when taking fluconazole concomitantly with cisapride, rifabutin or other drugs metabolized by the cytochrome P 450 system.

Drug interactions

When fluconazole is used with warfarin, the PT increases (by an average of 12%). In this regard, it is recommended to carefully monitor PT parameters in patients receiving the drug in combination with coumarin anticoagulants.

Fluconazole increases the plasma half-life of oral hypoglycemic agents - sulfonylurea derivatives (chlorpropamide, glibenclamide, glipizide, tolbutamide) in healthy people. The combined use of Fluconazole and oral hypoglycemic agents in patients with diabetes is allowed, but the doctor must keep in mind the possibility of developing hypoglycemia.

Concomitant use of Fluconazole and phenytoin may lead to an increase in plasma phenytoin concentrations to a clinically significant extent. Therefore, if it is necessary to use these drugs together, it is necessary to monitor the concentration of phenytoin with dose adjustment in order to maintain drug levels within the therapeutic interval.

Combination with rifampicin leads to a decrease in AUC by 25% and a shortening of the plasma half-life of fluconazole by 20%. Therefore, for patients receiving rifampicin at the same time, it is advisable to increase the dose of Fluconazole.

It is recommended to monitor the concentration of cyclosporine in the blood in patients receiving Fluconazole, because the use of fluconazole and cyclosporine in patients with a kidney transplant (taking Fluconazole at a dose of 200 mg/day) leads to a slow increase in the concentration of cyclosporine in plasma.

Patients who receive high doses of theophylline or who are at risk of developing theophylline toxicity should be monitored for early detection of symptoms of theophylline overdose, because taking fluconazole leads to a decrease in the average rate of clearance of theophylline from plasma.

With the simultaneous use of fluconazole with terfenadine and cisapride, cases of adverse reactions from the heart, including paroxysms of ventricular tachycardia (torsades de points), have been described.

Concomitant use of fluconazole and hydrochlorothiazide can lead to an increase in plasma concentrations of fluconazole by 40%.

There are reports of interaction between fluconazole and rifabutin, accompanied by an increase in serum levels of the latter. Cases of uveitis have been described with the simultaneous use of Fluconazole and rifabutin. Patients receiving rifabutin and fluconazole simultaneously should be carefully monitored.

In patients receiving a combination of fluconazole and zidovudine, an increase in the concentration of zidovudine is observed, which is caused by a decrease in the conversion of the latter to its main metabolite, so an increase in the side effects of zidovudine should be expected.

Increases the concentration of midazolam, and therefore increases the risk of developing psychomotor effects (most pronounced when fluconazole is used orally than intravenously).

Increases the concentration of tacrolimus, which increases the risk of nephrotoxicity.

Overdose

Symptoms: hallucinations, paranoid behavior.

Treatment: symptomatic - gastric lavage, forced diuresis. Hemodialysis within 3 hours reduces plasma concentrations by approximately 50%.

Storage conditions

In a dry place, protected from light, at a temperature of 15-25 °C.

A fungus is a microorganism that can cause serious illness. It can affect the skin (it especially loves the feet and palms), nail plates, mucous membranes and even internal organs.

A fungal infection causes a lot of inconvenience, so it is necessary to get rid of it and, preferably, do this at an early stage of the infection. One of the effective drugs that helps cope with this annoying disease is Fluconazole.

Pharmacological properties

Fluconazole is an antifungal agent. Its specific effect on infection is manifested by inhibiting the activity of enzymes that are important for fungi and depend on cytochrome P450.

Fluconazole photo

The drug also prevents the conversion of lanosterol to ergosterol. Due to depressurization of the cell membrane, the growth and development of the cells that make up the fungus are disrupted. Consequently, the microorganism dies.

The drug selectively inhibits enzymes, negatively affecting cytochrome P450, and at the same time does not suppress the biologically active substances of the human body at all. It also does not reduce the concentration of male sex hormones in the blood.

What does Fluconazole help with?

The drug is indicated for the following diseases:

Fluconazole is also used as a prophylaxis:

  • genital candidiasis, which worsens more than 3-4 times a year;
  • fungal infections in patients suffering from cancer and AIDS;
  • thrush if you have had sexual contact with a sick partner.

The drug is taken orally.

Instructions for use of Fluconazole: For the treatment of cryptococcal meningitis, as well as other cryptococcal infections, it is recommended that adolescents and adults (weighing more than 45 kg) take Fluconazole according to a specific regimen: a single daily dose should be 400 mg (eight capsules of 50 mg each), in subsequent days - 200 mg (four 50 mg capsules). The course of treatment depends on the severity of the disease and is determined by the attending physician. On average, the duration of therapy is 6-8 weeks.

Treatment of generalized candidiasis follows a similar scheme. On the first day the patient takes 400 mg, and on subsequent days – 200 mg. If the course is severe and advanced, then treatment with a single “impact” dose of 400 mg lasts from 2 to 5 days (at the discretion of the doctor). Treatment of pityriasis versicolor should be carried out according to a similar scheme.

If the skin and nail plate are affected by mycosis, pulse therapy is recommended. According to the instructions for use, Fluconazole 150 mg should be taken once every 7 days. Treatment for nail fungus lasts until a healthy translucent horny plate grows. On average, it lasts from 3 to 6 months, in severe cases – up to a year. The duration of treatment for skin fungus is much shorter and is approximately 4 to 6 weeks.

Fluconazole is also effective for deep endemic mycoses. Treatment is very long and sometimes lasts for several years. The daily intake, depending on the complexity of the course, ranges from 200 to 400 mg. The duration of treatment for histoplasmosis and sporotrichosis is recommended from several months to one and a half years, and for coccidioidomycosis - from one to two years.

If the patient is undergoing hemodialysis, he is recommended to take 50 mg after each session.

How to take Fluconazole for thrush?

In order to effectively get rid of thrush (candidiasis), women and men are recommended to undergo treatment at the same time. During therapy, it is best to abstain from sexual intercourse. The treatment regimen for candidiasis of both partners is the same.

The chronic form of the disease is much more difficult to treat. The treatment regimen is as follows: take 150 mg of the drug twice a day for three days. Then treatment with a similar dosage is recommended on the first day of the menstrual cycle. The duration of therapy is from 1/2 to 1 year.

To treat thrush of the oral cavity, pharynx and esophagus, more gentle therapy is used. Thus, the patient is recommended to take a single daily dose of 50-100 mg for a week. For intestinal candidiasis, the regimen is slightly different: 50 mg 2 times a day. The course of treatment is also 5-7 days.

Before taking Fluconazole, you should consult your doctor!

Contraindications for Fluconazole

  • hypersensitivity to the drug and severe allergic reactions to it in the past;
  • parallel use of Terfenadine and Astemizole and other drugs that affect the electrical systole of the ventricles.

For children under 4 years of age, the drug is strictly contraindicated!

Treatment should be carried out with extreme caution for those who suffer from liver and kidney dysfunction. When taking hepatotoxic drugs and drugs that affect heart rhythm simultaneously, you should consult your doctor about the possible risks. If during treatment a rash of unknown origin appears on the skin, then it is necessary to temporarily stop therapy to exclude an allergic reaction.

Fluconazole during pregnancy and breastfeeding

The use of an antifungal agent during pregnancy is contraindicated, except in cases where the infection threatens the life of the mother.

According to the instructions for use of Fluconazole, during the period of active therapy, the concentration of the main substance in milk and plasma is the same, therefore, during lactation, treatment with an antifungal agent is prohibited.

Overdose

Fluconazole in capsules or tablets should be used according to the instructions. Otherwise, the patient may experience signs of intoxication: nausea, vomiting, loose stools, and sometimes hallucinations and other mental abnormalities.

At the first signs of poisoning, you should seek medical help. In a hospital setting, gastric and intestinal lavage is performed, and in severe cases, hemodialysis is performed.

special instructions

Therapy must be continued according to the regimen prescribed by the doctor. The disappearance of visible signs of the disease can in no way be regarded as a cure. If you stop treatment without permission at this stage, the fungal infection may return again.

If you suspect a fungal infection, you should seek help from a dermatologist (if the skin is involved), a gynecologist (curd-like vaginal discharge) or a pediatrician (the child has white specks or plaque in the mouth).

It is not recommended to start treatment with Fluconazole on your own!

Timely diagnosis is the key to a speedy recovery! Fungus is not only unpleasant and unsightly, it is also dangerous. Do not forget to adhere to the rules of personal hygiene during treatment so as not to “reward” your household with an insidious infection.



General characteristics. Compound:

Active ingredient: fluconazole - 0.050 g or 0.150 g;

excipients: lactose monohydrate (milk sugar) - 0.1804 g or
0.19265 g, pregelatinized starch - 0.0012 g or 0.00175 g, povidone (low molecular weight polyvinylpyrrolidone) - 0.0012 g or 0.00175 g, colloidal silicon dioxide (Aerosil) - 0.0048 g or 0.00035 g , magnesium stearate - 0.0024 g or 0.0035 g;

gelatin capsule composition: for a dosage of 50 mg - body: gelatin - 0.038102 g, titanium dioxide E 171 - 0.000778 g, cap: gelatin - 0.022513 g, titanium dioxide E 171 - 0.000462 g, iron oxide dye yellow E 172 - 0.000145 g; for a dosage of 150 mg - body: gelatin - 0.045408 g, titanium dioxide E 171 - 0.000461 g, iron dye yellow oxide E 172 - 0.000231 g; cap: gelatin - 0.029648 g, titanium dioxide E 171 - 0.000301 g, iron dye yellow oxide E 172 - 0.000151 g.

Description. Hard gelatin capsules No. 2 are opaque white with a yellow cap (for a dosage of 50 mg) or hard gelatin capsules No. 1 are opaque yellow with a yellow cap (for a dosage of 150 mg). The contents of the capsules are white or white powder with a yellowish tint.


Pharmacological properties:

Pharmacodynamics. Fluconazole, a representative of the class of triazole antifungal agents, is a powerful selective inhibitor of sterol synthesis in fungal cells. The drug is effective against opportunistic mycoses, incl. 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. After oral administration, fluconazole is well absorbed, its bioavailability is 90%. The maximum concentration after oral administration on an empty stomach of 150 mg is 90% of the plasma content when administered intravenously at a dose of 2.5 - 3.5 mg/l. Concomitant food intake does not affect the absorption of the drug taken orally. The maximum concentration is reached 0.5-1.5 hours after administration; the half-life of fluconazole is about 30 hours. Plasma concentrations are directly proportional to dose. 90% level of equilibrium concentration is achieved by 4-5 days of treatment with the drug (when taken 1 time / day).

The introduction of a “loading” dose (on the first day), 2 times higher than the usual daily dose, allows you to achieve a level corresponding to 90% of the equilibrium concentration by the second day. The apparent volume of distribution approximates the total body water content. Plasma protein binding - 11-12%.

Fluconazole penetrates well into all biological fluids of the body. Drug concentrations in saliva and sputum are similar to those in plasma. In patients with fungal meningitis, the fluconazole content in the cerebrospinal fluid reaches 80% of its plasma level.

In the stratum corneum, epidermis, dermis and sweat fluid, high concentrations are reached that exceed serum concentrations.

It is an inhibitor of the CYP2C9 isoenzyme in the liver.

The pharmacokinetics of fluconazole depends significantly on the functional state of the kidneys, and there is an inverse relationship between the half-life and creatinine clearance (CC). Fluconazole is excreted primarily by the kidneys; approximately 80% of the administered dose is excreted unchanged in the urine. No fluconazole metabolites were detected in peripheral blood.

Indications for use:

Cryptococcosis, including cryptococcal and other localizations of this infection (including lungs, skin), both in patients with a normal immune response and in patients with various forms of immunosuppression (including in patients with organ transplantation); the drug can be used to prevent cryptococcal infection in AIDS patients;

Generalized candidiasis, including candidemia, disseminated candidiasis and other forms of invasive candidal infections (infections of the peritoneum, endocardium, eyes, respiratory and urinary tract). Treatment can be carried out in patients with malignant neoplasms, patients in intensive care units, patients undergoing cytostatic or immunosuppressive therapy, as well as in the presence of other factors predisposing to the development of candidiasis;

Candidiasis of the mucous membranes, incl. oral cavity and pharynx (including atrophic associated with wearing dentures), esophagus, non-invasive bronchopulmonary candidiasis, skin candidiasis; prevention of relapse of oropharyngeal candidiasis in patients with AIDS;

Genital candidiasis: vaginal candidiasis (acute and chronic recurrent), prophylactic use to reduce the frequency of relapses of vaginal candidiasis (3 or more episodes per year); candida;

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;

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


Important! Get acquainted with the treatment, ,

Directions for use and dosage:

Method of application internally.

For adults with cryptococcal meningitis and cryptococcal infections of other localizations, 400 mg is usually prescribed on the first day, and then treatment is continued at a dose
200-400 mg 1 time/day. The duration of treatment for cryptococcal infections depends on clinical effectiveness confirmed by mycological examination; for cryptococcal meningitis it is usually continued for at least 6-8 weeks.

To prevent relapse of cryptococcal meningitis in AIDS patients, after completing the full course of primary treatment, fluconazole is prescribed at a dose of 200 mg/day for a long period of time.

For candidemia, disseminated candidiasis and other invasive candidal infections, the dose is usually 400 mg on the first day, and then 200 mg each. If clinical effectiveness is insufficient, the dose of the drug can be increased to 400 mg/day. The duration of therapy depends on clinical effectiveness.

For oropharyngeal candidiasis, the drug is usually prescribed 50-100 mg 1 time / day; Duration of treatment is 7-14 days. If necessary, in patients with a pronounced decrease in immunity, treatment may be longer.

To prevent relapses of oropharyngeal candidiasis in patients with AIDS after completing the full course of primary therapy, the drug can be prescribed 150 mg once a week.

For atrophic candidiasis of the oral cavity associated with wearing dentures, fluconazole is usually prescribed 50 mg once a day for 14 days in combination with local antiseptics for the treatment of the denture.

For other localizations of candidiasis (except for genital candidiasis), for example, esophagitis, non-invasive bronchopulmonary lesions, candiduria, candidiasis of the skin and mucous membranes, etc., the effective dose is usually 50-100 mg/day with a treatment duration of 14-30 days.

For vaginal candidiasis, fluconazole is taken orally once at a dose of 150 mg. To reduce the frequency of relapses of vaginal candidiasis, the drug can be used at a dose of 150 mg once a month. The duration of therapy is determined individually; it varies from 4 to 12 months. Some patients may require more frequent use.

For balanitis caused by Candida, fluconazole is prescribed as a single 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 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/mm 3, treatment is continued for another 7 days.

For mycoses of the skin, including mycoses of the feet, skin of the groin area and skin candidiasis, the recommended dose is 150 mg once a week or 50 mg once a day. The duration of therapy in normal cases is 2-4 weeks, however, with mycoses of the feet, longer therapy (up to 6 weeks) may be required.

For pityriasis versicolor - 300 mg once a week for 2 weeks, some patients require a third dose of 300 mg per week, while in some cases a single dose of 300-400 mg is sufficient; An alternative treatment regimen is to use 50 mg once a day for 2-4 weeks.

For onychomycosis, the recommended dose is 150 mg once a week. Treatment should be continued until the infected nail is replaced (the uninfected nail regrows). It normally takes 3-6 months for fingernails and toenails to re-grow.
6-12 months respectively.

For 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; it can be 11-24 months for coccidioidomycosis; 2-17 months for paracoccidioidomycosis; 1-16 months for sporotrichosis and 3-17 months for histoplasmosis.

In children, as 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 that would exceed that in adults. The drug is used daily
1 time/day

For the treatment of generalized candidiasis or cryptococcal infection (including meningitis), the recommended dose is 6-12 mg/kg/day for 10-12 weeks (until laboratory confirmation of the absence of pathogens in the cerebrospinal fluid).

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

In children with impaired renal function, the daily dose of the drug should be reduced
(in the same proportion as in adults), in accordance with the severity of renal failure.

In elderly patients in the absence of renal dysfunction, the usual dosage regimen of the drug should be followed. In patients with renal failure (creatinine clearance less than 50 ml/min), the dosage regimen should be adjusted as indicated below.

Use of the drug in patients with impaired renal function.

Fluconazole is excreted mainly in the urine unchanged. When taken once, no dose change is required. When re-prescribing the drug to patients with impaired renal function, a “loading” dose of 50 mg to 400 mg should first be administered. If creatinine clearance (CC) is more than 50 ml/min, the usual dose of the drug is used (100% of the recommended dose). When CC is from 11 to 50 ml/min, a dose equal to 50% of the recommended dose is used. For patients regularly on dialysis, one dose of the drug is administered after each hemodialysis session.

Features of application:

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

Treatment can be started if culture or other laboratory test results are absent, but if they are available, appropriate adjustment of fungicidal therapy is recommended.

During treatment, it is necessary to monitor blood counts, kidney and liver function. If renal or liver dysfunction occurs, you should stop taking the drug.

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. In the case of hepatotoxic effects associated with fluconazole, there was no obvious dependence on the total daily dose, duration of therapy, gender and age of the patient. The hepatotoxic effects of fluconazole were usually reversible; its signs disappeared after cessation of therapy. If clinical signs of liver damage that may be associated with fluconazole appear, the drug should be discontinued.

People with AIDS are more likely to develop severe skin reactions when taking many drugs. In cases where a rash develops in patients with a superficial fungal infection and is assessed as definitely related to fluconazole, the drug should be discontinued. If a rash appears in patients with invasive/systemic fungal infections, they should be carefully monitored and fluconazole should be discontinued if bullous changes or erythema multiforme occur.

Caution must be exercised when taking fluconazole concomitantly with cisapride, rifabutin or other drugs metabolized by the cytochrome P 450 system.

Influence on the ability to drive vehicles and machinery.

Fluconazole does not affect the ability to drive vehicles or engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Side effects:

From the digestive system: changes in taste, abdominal pain, impaired liver function (jaundice, hyperbilirubinemia, increased activity of alanine aminotransferases, aspartate aminotransferases, increased activity of alkaline phosphatase, hepatonecrosis), incl. with fatal outcome.

From the nervous system: headache,.

From the hematopoietic organs: , .

From the cardiovascular system: increased duration of the interval
Q-T, ventricular fibrillation/flutter.

Allergic reactions: skin rash, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), anaphylactoid reactions (including angioedema, facial swelling, skin itching).

Other: renal dysfunction, .

Interaction with other drugs:

When fluconazole is used with warfarin, the prothrombin time increases
(on average by 12%). In this regard, it is recommended to carefully monitor prothrombin time in patients receiving the drug in combination with coumarin anticoagulants.

Fluconazole increases the plasma half-life of oral hypoglycemic agents - sulfonylurea derivatives (chlorpropamide, glibenclamide, glipizide, tolbutamide) in healthy people. The combined use of fluconazole and oral hypoglycemic agents in patients with diabetes is allowed, however, the doctor must be aware of the possibility of developing hypoglycemia.

Concomitant use of fluconazole and phenytoin may lead to an increase in plasma phenytoin concentrations to a clinically significant extent. Therefore, if it is necessary to use these drugs together, it is necessary to monitor phenytoin concentrations with dose adjustment in order to maintain drug levels within the therapeutic interval.

Combination with rifampicin leads to a decrease in AUC by 25% and a shortening of the plasma half-life of fluconazole by 20%. Therefore, in patients receiving rifampicin at the same time, it is advisable to increase the dose of fluconazole.

It is recommended to monitor the concentration of cyclosporine in the blood in patients receiving fluconazole, because the use of fluconazole and cyclosporine in patients with a kidney transplant; taking fluconazole at a dose of 200 mg/day leads to a slow increase in the concentration of cyclosporine in plasma.

Patients who receive high doses of theophylline or who are at risk of developing theophylline toxicity should be monitored for early detection of symptoms of theophylline overdose, because taking fluconazole leads to a decrease in the average rate of clearance of theophylline from plasma.

With the simultaneous use of fluconazole and cisapride, cases of adverse reactions from the heart, including paroxysms of ventricular tachycardia (torsades de points), have been described.

There are reports of interaction between fluconazole and rifabutin, accompanied by an increase in serum levels of the latter. Cases of uveitis have been described with the simultaneous use of fluconazole and rifabutin. Patients receiving rifabutin and fluconazole simultaneously should be carefully monitored.

In patients receiving a combination of fluconazole and zidovudine, an increase in the concentration of zidovudine is observed, which is caused by a decrease in the conversion of the latter to its main metabolite, so an increase in the side effects of zidovudine should be expected.

Fluconazole increases the concentration of midazolam - increasing the risk of psychomotor effects (more pronounced when fluconazole is used orally); tacrolimus - risk of nephrotoxicity.

Hydrochlorothiazide increases the plasma concentration of fluconazole by 40%.

Contraindications:

Simultaneous use of terfenadine (while constantly taking fluconazole at a dose of 400 mg/day or more) or astemizole and other drugs that prolong the QT interval;

Hypersensitivity to the drug or azole compounds similar in structure;

Lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

Children's age (up to 3 years).

Overdose:

Symptoms:, paranoid behavior.

Treatment: symptomatic, . within 3 hours reduces plasma concentrations by approximately 50%.

Storage conditions:

In a dry place, protected from light, at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Vacation conditions:

Over the counter

Package:

Capsules 50 mg and 150 mg. 1, 4, 7 or 10 capsules per blister pack. 1, 2 or 4 blister packs along with instructions for use in a cardboard pack.