Flucostat is an effective medicine for thrush.
Flucostat is an antifungal drug that is different from other similar drugs wide range actions. The greatest activity is observed in the treatment a separate type a fungus from a genus called Candida that causes thrush. But this triazole compound also fights other fungal infections very effectively.
The active substance of flucostat is fluconazole, which different dosages is the main component of tablets, solutions and suppositories. The drug, thanks to its thoughtful composition, does not harm the natural microflora of the intestines and the entire digestive tract, as well as the vagina. That is why it is used more often than other drugs to treat external and internal fungal infections.
Flucostat is available in different forms - there are suppositories and a solution for intravenous injections, but the most popular form is capsules. There are also several options here:
- 50 mg. active drug in the form of opaque pink capsules containing inside White powder; This option is packaged with seven tablets in each contour blister; one standard package contains only one such blister;
- 150 mg. the active drug is also in the form of capsules, but opaque white ones, containing the same white powder inside; standard packaging consists of only one blister pack with only one capsule; there is an option with two capsules in a box.
For full treatment The most popular dosage is 150 mg, since this amount of the active substance is just enough to rid the body.
Flucostat is domestic drug, produced in full compliance with all European standards. It really has a wide spectrum of action, and, despite its particular activity in the treatment of thrush, it is perfect for both women and the stronger sex, who can use capsules or an injection solution to get rid of any fungi. So, the indications for use are:
Photo: Candidiasis and mycosis - genital candidiasis, known to everyone under the “code” name “thrush; flucostat is used both to treat the first case of the disease and to get rid of relapses and their prevention;
- defeats mucous membranes, including lesions of the mouth and pharynx caused by wearing dentures, lesions of the esophagus when spores enter food, skin treatment and prevention of any fungal infections in people with weakened immune systems, including AIDS patients;
- treatment of any types of cryptococcosis, characterized by damage to important body systems, including the central nervous and respiratory;
- treatment of all types of generalized, including complex treatment malignant tumors, when restoring the body of patients intensive care and if there are other factors that predispose to the development of this type of fungus;
- prevention of any fungal formations in patients with malignant tumors, due to chemotherapy and radiation, those predisposed to the development of such infections;
- mycoses of any areas of the skin, the development of pityriasis versicolor and other variants of external fungal formations on the body;
- deep mycoses with pronounced symptoms, manifested even in patients with strong immunity.
Doses required for treatment
The degree of development of the disease and the risk of relapse significantly affects the amount of the drug required for treatment. In terms of treating thrush, there are three main options for using the drug. The instructions here are quite simple, and the amount of medicine needed is small.
Photo: Flucostat capsule It is usually used in the treatment of new symptoms of the disease and is often combined with the use of other forms of the drug, for example, with suppositories. This treatment is suitable for getting rid of mild signs of thrush that have manifested themselves for the first time. Single dose recommended only if exacerbations occur less than three times a year.
In the blood, a high concentration of the substance is observed within a few hours after taking the capsule, which allows you to begin getting rid of fungal formations immediately after the first symptoms appear. The active substance easily penetrates into all tissues and systems of the body.
2 tablets aimed at getting rid of more severe symptoms or from manifestations of a disease that appears as a result of other malfunctions in the body, for example, due to a sharp weakening of the immune system and other problems. A two-time dose is taken with a long break of 72 hours (the first capsule is drunk on the first day of treatment, the second - on the fourth)
Photo: triple dose of Flucostat - This is already a rather radical form of treatment. It is resorted to only if four or even more episodes of the disease have been observed in a year and there is still a threat of relapse.
In the most severe cases of the disease, prophylactic use of flucostat may additionally be recommended, which consists of using one capsule drug (150 mg.) once every seven days for six months.
When treating any other fungal infections, the exact dosages are usually prescribed by the doctor, usually combining the use of both forms of capsules (150 and 50 mg) for quality treatment and subsequent prevention. The use in this case is strictly regulated and controlled by the attending physician. Minimum term treatment is usually two weeks and can last up to six months or up to full recovery external tissues.
Photo: Skin lesions For skin lesions, the maximum dose for treatment is usually 50 mg., subsequently capsules with a dosage of 150 mg. become the basis for prevention.
For deep mycoses and other advanced variants of the disease, the daily dose of the drug usually varies between 200 and 400 mg., the duration of treatment in this case is usually several weeks or months.
In treatment, the dosage is calculated based on their weight - on the first day of treatment it is usually prescribed maximum dosage (5 mg per kilogram of body), on all subsequent days, prescribed by a doctor, the dose is reduced to 3 mg. for every kilogram of body.
There are several tips aimed at increasing the effectiveness of treatment with flucostat capsules. First of all, experts usually advise combining them with other forms, for example, suppositories in the case of treating the same thrush, and supplementing treatment of any duration with subsequent prophylaxis using the same or a lower dosage of the drug.
The drug is not tied to meals, so capsules can be taken before and after meals. But when long-term treatment It is better to observe the time of taking the tablets to ensure a sufficient positive effect. Contraindications for use
Flucostat has a very small list of contraindications, but do not forget about their existence. The main contraindications include:
- period of lactation and breastfeeding;
- young age (usually from the age of three children are already allowed to be treated with small doses of flucostat);
- individual intolerance to individual components of the drug included in the capsules.
A separate limitation for the use of the drug is the period of pregnancy. At this time, flucostat treatment can be prescribed only for fungal infections that are serious and dangerous to the health or even the life of the mother.
Photo: Flucostat during pregnancy - symptoms of poisoning, including banal nausea and changes in stool, as well as changes (exacerbation or dulling) in the functioning of taste buds;
- headaches, in especially severe, but very rare cases - convulsions;
- allergies and the appearance of skin rashes, redness and painful skin irritations;
- active influence on the central nervous system, expressed in inhibition of reaction or excessive excitement.
Photo: Medicinal capsules Flucostat capsules in a dosage of 150 mg. are considered a universal and effective remedy, among the advantages of which both doctors and people familiar with the effect of the drug will highlight a large number of unique advantages:
- For complex treatment it is necessary to remove fungal cells from all parts of the body and tissues where they can live. Superficial treatment of the affected areas of the body alone will not help to completely get rid of the problem, but additional dose capsules will lead to positive result treatment;
- the drug entering the body minimizes the chance of re-development of the disease;
- capsules can be taken at any time with virtually no restrictions - they have a very short list existing contraindications, and there is no connection between consumption and the time of day or combination with food;
- usually a full course of treatment consists of one or two capsules, a larger number is required only for worsened forms of fungal infections or re-infection;
- the spectrum of action of flucostat is very wide - a huge number of fungal infections and infections caused by pathogenic spores do not require the use of additional drugs.
Photo: Flucostat analogs Replace the flucostat yourself with existing analogues It is not advisable, and usually useless; it is better to do this only on the recommendation of a doctor. There is no particular point in choosing other medications. There are only two analogues of flucostat:
- diflucan;
- fluconazole.
The first option is an absolute analogue of the European-made flucostat. Accordingly, its properties are no different from Russian capsules, but the price is higher.
Fluconazole is the main active component of flucostat. There is no particular difference other than the price and manufacturer (both are produced in Russia), but it is worth considering that due to the simplified composition of fluconazole, some side effects and be indicated large quantity contraindications.
Video
Watch the video: Flucostat and thrush - misconceptions, reviews from doctors
Watch the video: Flucostat
Composition and release form
in blister packs 7 (50 mg) or 1 (150 mg) pcs.; 1 package in a box.
in bottles of 50 ml; 1 bottle in a cardboard pack.
Description of the dosage form
The solution for intravenous administration is a clear, colorless liquid.
Characteristic
An antifungal agent from the group of triazole derivatives.
pharmachologic effect
pharmachologic effect- antifungal.Selectively inhibits the synthesis of sterols in the cell wall of fungi.
Pharmacodynamics
Active regarding Candida spp., Cryptococcus neoformans, Microsporum spp., Trichoptyton spp., Blastomyces dermatitidis, Coccidioides immitis And Histoplasma capsulatum.
Pharmacokinetics
When taken orally, it is well absorbed from the gastrointestinal tract. Cmax is achieved 0.5-1.5 hours after administration on an empty stomach. Penetrates well into all body fluids and is detected in the nails 6 months after completion of therapy. Excreted by the kidneys up to 80%.
After intravenous administration, fluconazole penetrates well into body tissues and fluids. Concentrations of the drug in saliva and sputum correspond to concentrations in plasma. In patients with fungal meningitis, the content of fluconazole in the cerebrospinal fluid reaches 80% of the corresponding levels in plasma. After several administrations of 1 dose per day, 90% of the equilibrium concentration level is achieved by the 4-5th day; when administered on the 1st day, a dose 2 times higher than the usual daily dose is achieved by the 2nd day. The apparent volume of distribution approaches the total volume of water in the body. 11-12% of fluconazole is bound to plasma proteins. T 1/2 - 30 hours. 80% is excreted unchanged by the kidneys. Fluconazole clearance is directly proportional to creatinine clearance. No metabolites were detected in peripheral blood.
Indications of the drug Flucostat ®
Cryptococcosis, generalized candidiasis (including candidemia), disseminated (including in patients receiving immunosuppressive drugs), skin, mucous membranes (including oral cavity and pharynx, esophagus), acute or recurrent urogenital candidiasis (vaginal, candidal balanitis), bronchopulmonary candidiasis; prevention of relapses of oropharyngeal candidiasis in patients with AIDS, urogenital candidiasis, fungal infections during cytostatic chemotherapy or radiation therapy; mycosis of the skin, incl. mycosis of the feet, body, groin area, pityriasis versicolor
, onychomycosis, deep endemic mycoses.
Contraindications
Hypersensitivity (including to azole compounds that are similar in structure), simultaneous use of terfenadine, astemizole, cisapride.
Use during pregnancy and breastfeeding
Contraindicated during pregnancy (except for severe, generalized and potentially life-threatening fungal infections). Breastfeeding should be stopped during treatment.
Side effects
When taken orally. From the gastrointestinal tract:
nausea, diarrhea, flatulence. headache
, dizziness. Allergic reactions: skin rash
, anaphylactic reactions.
When taken orally. With intravenous administration. nausea, vomiting, diarrhea, flatulence, abdominal pain, liver failure (hepatitis, increased levels of alkaline phosphatase, bilirubin, serum level
aminotransferases). From the outside nervous system and sense organs:
, dizziness. headache, cramps.
skin rash, anaphylactic reactions, Stevens-Johnson syndrome, toxic epidermal necrolysis. Other:
alopecia, renal failure.
Interaction When combined with coumarin anticoagulants, an increase in prothrombin time is possible (it should be monitored); with terfenadine, there is a possible risk of developing arrhythmia; with cisapride, an increase adverse reactions from the outside of cardio-vascular system
, incl.
paroxysmal ventricular tachycardia. Prolongs T1/2 of sulfonylurea drugs from serum (increases the risk of developing hypoglycemia). Increases the concentration of phenytoin, cyclosporine, zidovudine in the blood. Rifampin shortens T1/2 of Flucostat.
Directions for use and doses Inside.
For cryptococcal infections, candidemia, disseminated candidiasis and other invasive candidal infections: on the 1st day - 400 mg, then - 200-400 mg 1 time per day.
For atrophic oral candidiasis associated with wearing dentures: 50 mg 1 time per day for 10-14 days.
For other candidal infections of the mucous membranes: 50-100 mg/day for 14-30 days.
To prevent relapses of oropharyngeal candidiasis in patients with AIDS after completing the full course of primary treatment: 150 mg once a week.
For vaginal candidiasis and balanitis: once 150 mg. To prevent relapses - 150 mg once a month for 4-12 months.
For the prevention of candidiasis in cancer patients during cytostatic chemotherapy or radiation therapy: 50-400 mg 1 time per day. If there is a high risk of developing a generalized infection: 400 mg 1 time per day a few 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 (feet, groin area, etc.), including candidiasis infections: 150 mg once a week or 50 mg once a day. The duration of therapy is 2-4 weeks, for mycoses of the feet - up to 6 weeks.
At pityriasis versicolor: 50 mg 1 time per day for 2-4 weeks.
For onychomycosis: 150 mg once a week until an uninfected nail grows out (3-6 and 6-12 months for fingernails and toenails, respectively).
For deep endemic mycoses: 200-400 mg/day for 11-24 months (coccidioidomycosis), 2-17 months (paracoccidioidomycosis), 1-16 months (sporotrichosis), 3-17 months (histoplasmosis).
For children for candidiasis of the mucous membranes on the 1st day - 6 mg/kg/day, then - 3 mg/kg/day, for systemic candidiasis or cryptococcosis- 6-12 mg/kg depending on the severity of the disease. For prophylaxis against the background of reduced immunity (depending on the severity of neutropenia) - 3-12 mg/kg/day.
IV drip (at a rate of no more than 20 mg/min (10 ml/min) for cryptococcal infections, candidemia, disseminated candidiasis and other invasive candidal infections: on the 1st day - 400 mg/day, then - 200-400 mg 1 time per day (for cryptococcal infections for 6-8 weeks).
When converting from intravenous administration to taking capsules and vice versa, there is no need to change the daily dose.
Overdose
In case of overdose, gastric lavage and symptomatic therapy, forced diuresis or hemodialysis (hemodialysis for 3 hours reduces the concentration of fluconazole by 50%).
Precautionary measures
Treatment should begin before culture and other laboratory results are available. In elderly patients with impaired renal function, adjustment of the dosage regimen is necessary. In case of renal failure (Cl creatinine 11-50 ml/min), a dose equal to 50% of the therapeutic dose is used. Patients constantly on dialysis need to take 100% of the dose after each dialysis procedure. When clinical signs liver damage, skin reactions the drug should be discontinued.
special instructions
The solution for infusion is compatible with solutions: 20% glucose, Ringer, Hartmann, potassium chloride in glucose, sodium bicarbonate 4.2%, isotonic sodium chloride solution and aminofusin.
Manufacturer
JSC "Dalkhimpharm" by order of JSC "Masterlek" (Russia) (size d/in. v/v).
EP MBP RK NPK Ministry of Health of the Russian Federation by order of JSC "Masterlek" (Russia) (caps.).
Storage conditions for the drug Flucostat ®
In a dry place, at a temperature not exceeding 25 °C.Keep out of the reach of children.
Shelf life of the drug Flucostat ®
solution for intravenous administration 2 mg/ml - 3 years.
capsules 50 mg - 2 years.
capsules 150 mg - 2 years.
Do not use after the expiration date stated on the package.
Instructions for medical use
Synonyms of nosological groups
| ICD-10 rubric | Synonyms of diseases according to ICD-10 |
|---|---|
| B35-B49 Mycoses | Fungal infection |
| Fungal skin infections | |
| Fungal skin lesions | |
| Fungal infections | |
| Fungal skin infections | |
| B35.1 Nail mycosis | Fungal nail disease |
| Fungal nail infection | |
| Fungal nail diseases | |
| Fungal nail infections | |
| Dermatomycosis of nails | |
| Mycoses of nails | |
| Onychomycosis | |
| Onychomycosis | |
| Athlete's nails | |
| B35.2 Mycosis of the hands | |
| Mycoses of the hands | |
| Rubrophytosis of hands | |
| Trichophytosis of the palms | |
| Athlete's hand | |
| Athlete's palms | |
| B35.3 Mycosis of the feet | Foot fungus |
| Dermatophytosis of the feet | |
| Interdigital fungal erosion | |
| Mycosis of the feet | |
| Mycoses of the feet | |
| Athlete's foot | |
| B35.6 Athlete's foot | Fungal infections of skin folds |
| Dermatomycosis of the groin area and smooth skin | |
| Mycosis of the groin area | |
| Mycoses of the feet and large folds | |
| Dermatophytosis inguinalis | |
| Athlete's inguinal | |
| Inguinal ringworm | |
| B35.8 Other dermatophytosis | Dermatomycosis of the legs |
| Dermatophytosis of the genitals | |
| Rubromycosis | |
| Rubrophytia | |
| Trichophytosis of the skin of the lower extremities | |
| B36.0 Tinea versicolor | Pitirosporum orbiculare |
| Pityriasis versicolor | |
| Pityriasis furfuracea (pityriasis furfuracea) | |
| Ringworm multicolored | |
| Pityriasis versicolor | |
| Tinea versicolor | |
| B37.0 Candidal stomatitis | Atrophic candidiasis of the oral cavity |
| Fungal diseases of the oral cavity | |
| Fungal infections oral cavity | |
| Fungal infectious and inflammatory diseases of the oral cavity | |
| Candidiasis of the gastrointestinal tract | |
| Oral candidiasis | |
| Oral candidiasis | |
| Candidiasis of the oral mucosa | |
| Candidiasis of the mucous membranes | |
| Candidiasis of the mucous membranes of the oral cavity and pharynx | |
| Candidiasis of the oral cavity and pharynx | |
| Mucocutaneous candidiasis of the oral cavity | |
| Mycotic jam | |
| Oral thrush | |
| Oropharyngeal candidiasis | |
| Oropharyngeal candidiasis | |
| Chronic atrophic candidiasis of the oral cavity | |
| B37.1 Pulmonary candidiasis | Bronchopulmonary candidiasis |
| Candidiasis of internal organs | |
| B37.2 Candidiasis of the skin and nails | Fungal paronychia |
| Fungal eczema | |
| Fungal dermatoses | |
| Fungal diseases of smooth skin | |
| Fungal infections of smooth skin | |
| Fungal infections of smooth body skin | |
| Fungal nail infections | |
| Yeast skin infection | |
| Skin candidiasis | |
| Candidiasis of the skin and mucous membranes of the mouth and pharynx | |
| Candidiasis of the skin of the nail folds | |
| Candidiasis of the nail folds | |
| Nail candidiasis | |
| Candidiasis with damage to the skin and mucous membranes | |
| Candidiasis of mucous membranes and skin | |
| Candidal paronychia | |
| Candidomycosis of the skin | |
| Skin candidiasis infections | |
| Cutaneous candidiasis | |
| Interdigital fungal erosion | |
| Mycotic dermatitis | |
| Paronychia candidiasis | |
| Superficial form of skin candidiasis | |
| Superficial candidiasis | |
| Superficial nail candidiasis | |
| Superficial mycosis of the skin | |
| Chronic skin candidiasis | |
| B37.3 Candidiasis of the vulva and vagina (N77.1*) | Vaginal candidiasis |
| Vaginal candidiasis | |
| Vulval candidiasis | |
| Vulvovaginal candidiasis | |
| Vulvovaginal candidiasis | |
| Vulvovaginitis candidiasis | |
| Vulvovaginitis mycotic | |
| Fungal vaginitis | |
| Vaginal candidiasis | |
| Candidiasis of internal organs | |
| Genitourinary candidiasis | |
| Candidiasis genitourinary organs among women | |
| Candidiasis with damage to the skin and mucous membranes | |
| Candidiasis of the mucous membranes | |
| Candidiasis of mucous membranes and skin | |
| Candidal vaginitis | |
| Candidiasis vulvitis | |
| Vulvovaginal candidiasis | |
| Colpitis of fungal etiology | |
| Vaginal thrush | |
| Moniliasis vulvovaginitis | |
| Acute vaginal candidiasis | |
| Acute mycosis of the vagina | |
| Recurrent vaginal candidiasis | |
| Recurrent vaginal candidiasis | |
| Urogenital candidiasis | |
| Chronic vaginal candidiasis | |
| Chronic candidiasis of the mucous membranes | |
| Chronic recurrent vaginal candidiasis | |
| B37.4 Candidiasis of other urogenital sites | Genital candidiasis |
| Genitourinary candidiasis | |
| Candidiasis of the mucous membranes | |
| Candidal balanitis | |
| Candidiasis balanoposthitis | |
| Candiduria | |
| Superficial candidiasis of the genital mucosa | |
| Urogenital candidiasis | |
| B37.6 Candidal endocarditis (I39.8*) | Candidiasis of internal organs |
| B37.7 Candidal septicemia | Generalized candidiasis |
| Generalized candidiasis | |
| Candidemia | |
| Generalized candidiasis | |
| Systemic candidiasis | |
| Systemic candidiasis | |
| Heavy invasive forms candida infections | |
| B38 Coccidioidomycosis | California fever |
| Coccidiodomycosis | |
| Coccidioidosis | |
| Coccidioidosis (coccidioidomycosis) | |
| Coccidioidomycosis | |
| Desert rheumatism | |
| B41 Paracoccidioidomycosis | Paracoccidioidosis |
| B42 Sporotrichosis | Dory's disease |
| Rose Lovers Disease | |
| Schenck-Berman disease | |
| Rhinocladiasis | |
| B45 Cryptococcosis | Cryptococcus |
| B45.0 Pulmonary cryptococcosis | Torulez |
| B49 Mycosis, unspecified | Visceral mycosis |
| Deep endemic mycoses | |
| Fungal infection | |
| Fungal skin infections | |
| Fungal skin lesions | |
| Fungal infections of skin folds | |
| Fungal infections of the bronchial mucosa | |
| Fungal infections of the oral mucosa | |
| Fungal infections | |
| Fungal skin infections | |
| Keratomycosis | |
| Cutaneous mycosis | |
| Pulmonary mycosis | |
| Mycosis | |
| Mycoses of the eyes | |
| Mycoses of the gastrointestinal tract | |
| Skin mycoses | |
| Mycoses of large skin folds | |
| Systemic mycoses | |
| Mycoses of mucous membranes | |
| Mycoses with secondary bacterial infection | |
| Mycoses in patients with immunodeficiency | |
| Common mycoses | |
| Systemic mycoses | |
| Tropical mycoses | |
| N48.6 Balanitis | Balanitis dry obliterans |
| Fungal balanitis |
Included complex therapy Thrushes are prescribed the antifungal drug Flucostat. The medicine destroys fungal infections, the development of which is provoked by pathogens sensitive to its components. Before starting the course, you need to consult a gynecologist.
Composition and release form
The drug Flucostat is available in several dosage forms. Characteristics of each:
- Opaque capsules of light pink color with white powder in the composition. Packaged in blister packs of 1, 2 or 7 pcs. The pack contains 1 package, instructions for use.
- White oval tablets on a blister, 1 or 2 pcs. The package contains 1 plate, instructions for use.
- Transparent solution for intravenous administration. Pour into 50 ml bottles. The pack contains 1 bottle, instructions for use.
- Vaginal suppositories white. The medicine is distributed into aluminum foil blisters of 1 or 2 pieces.
The active ingredient is fluconazole. Chemical composition Flucostat:
| Release form | Active ingredient | Auxiliary components | Shell composition |
| Capsules, 1 pc. | fluconazole (50 and 150 mg) | corn starch; magnesium stearate; silicon dioxide; sodium lauryl sulfate; | methyl parahydroxybenzoate; iron dye E172; titanium dioxide (E171); propyl parahydroxybenzoate. |
| Solution, 1 ml | fluconazole | sodium chloride; water for injections | |
| Tablets, 1 pc. | fluconazole (50 and 150 mg) | silica; Magnesium stearate. | |
| Vaginal suppositories, | fluconazole | polyglycerides |
Pharmacological properties
Flucostat for thrush is an antifungal drug that belongs to the group of triazole compounds. Active against fungi localized after infection in the urethra:
- Candida spp;
- Blastomyces dermatidis;
- Microsporum spp;
- Cryptococcus neoformans;
- Trichophyton spp;
- Coccidioides immits;
- Histoplasma capsulatum.
Fluconazole inhibits the synthesis of sterols (structural components of fungal cells), thereby reducing the activity of pathogenic flora. Upon penetration into the body, it is evenly distributed in the tissues. Sterol deficiency increases the permeability of the fungal membrane, destroys it, which leads to the death of the pathogenic pathogen. Information on pharmacokinetics depending on the dosage form:
- When a single dose is administered orally on an empty stomach, Flucostat is absorbed from the digestive tract. The maximum concentration in plasma is reached after 1–1.5 hours. The half-life is 30 hours. 80% of metabolites are eliminated in urine.
- At intravenous administration fluconazole is evenly distributed throughout biological fluids. Therapeutic effect observed on days 4–5 of use injection solution. Excreted by the kidneys.
Indications for use
Flucostat tablets are prescribed for fungal infections that are sensitive to the components of the medication. The instructions describe medical indications:
- mycoses of various etiologies;
- cryptococcosis, including cryptococcal meningitis;
- pityriasis versicolor;
- sporotrichosis, histoplasmosis, coccidioidomycosis;
- prevention of fungal infection in patients with AIDS;
- generalized or disseminated candidiasis;
- prevention of fungal infection after cytostatic, chemotherapy or radiation therapy;
- genital candidiasis (thrush);
- candidiasis of the mucous membranes of the oral cavity, pharynx, esophagus, trachea, urinary system.
How to take Flucostat
The method of administration and daily doses depend on the release form of Flucostat. Capsules and tablets are intended for oral use, suppositories are used vaginally. It is allowed to combine several forms of Flucostat at once. The course of treatment varies from several days to 3–4 weeks.
Capsules and tablets
Flucostat is taken orally. Daily dosages of capsules depend on the disease and are described in the instructions for use:
| Daily doses, mg/day | Course of treatment, days |
|
| Prevention of cryptococcal meningitis in patients with AIDS | individual |
|
| Atrophic candidiasis of the oral cavity | ||
| Cryptococcal infection, generalized candidiasis | individual |
|
| Mycosis of the skin | ||
| Candidiasis of the mucous membranes of the reproductive system, balanitis | once |
|
| Pityriasis versicolor | ||
| Deep endemic mycoses | ||
| Onychomycosis | 150 once a week | until complete recovery nail plate |
| Esophagitis, candiduria |
Flucostat tablets are intended for intravaginal administration. To suppress relapse, 1 tablet is injected into the vagina. For a chronic disease, the dosage and course of treatment are determined individually.
Flucostat - before or after meals
Since the absorption of the active substances of Flucostat does not depend on filling the lumen digestive tube, the antifungal drug can be taken orally before or after meals. Therapeutic effect does not weaken.
Solution in ampoules
Flucostat in this release form is intended for intravenous drip administration. According to the instructions, the maximum dosage is 10 ml. For cryptococcal and candida infections, the initial dose is 400 mg, then reduced to 200-400 mg/day for 6-8 weeks. The drug is allowed to be combined with solutions of glucose, Ringer, Hartmann, potassium chloride in glucose, sodium bicarbonate, isotonic sodium chloride and aminofusin.
Flucostat suppositories
Suppositories are intended for vaginal administration (deep into the vagina at night). For thrush, 1 suppository is prescribed for a course of 7 days. It is first necessary to carry out hygienic procedures for the genital organs. The doctor determines the course of treatment individually.
special instructions
Before using Flucostat for its intended purpose, it is necessary to determine the nature of the pathogen and its sensitivity to fluconazole. Other specialist instructions:
- For chronic kidney disease, it is necessary to prescribe an average therapeutic dose depending on the level of creatinine in the blood.
- If treatment with an antifungal drug is accompanied by liver dysfunction or skin rashes, you need to stop taking Flucostat.
- When undergoing parallel hemodialysis, the maximum dose of fluconazole is prescribed after each procedure.
- The drug inhibits the functions of the nervous system, therefore, if a headache occurs, or frequent attacks of dizziness and drowsiness occur, it is not recommended to operate power mechanisms or exercise intellectual activity.
- For vaginal candidiasis, both sexual partners should be treated with Flucostat.
- When used simultaneously with alcohol, nausea, vomiting, and severe headache may occur. The load on the liver increases, the concentration of leukocytes and platelets in the blood decreases, and the heart rhythm is disturbed.
During pregnancy
When carrying a fetus, Flucostat is prescribed for health reasons, since the drug component in a small concentration penetrates the placental barrier and is excreted in breast milk. In the latter case, if treatment is necessary, it is necessary to temporarily stop lactation and transfer the baby to adapted formulas.
Flucostat for children
In childhood, the antifungal drug is allowed for patients over 3 years of age on the recommendation of a pediatrician. According to the instructions, daily dosage varies from 3 to 12 mg per 1 kg of body weight. On an individual basis, for example, with reduced immunity, it is increased. The course of treatment depends on the disease, stage pathological process.
Drug interactions
Flucostat is involved in a complex therapy regimen. The instructions provide information about drug interactions:
- fluconazole is carefully combined with Cisapride, Astemizole, Rifabutin, Tacrolimus;
- when used simultaneously with Terfenadine and Cisapride, it develops ventricular tachycardia, arrhythmia, in combination with Rifabutin, uveitis progresses;
- fluconazole increases the effectiveness of antibiotics and the half-life of hypoglycemic agents, increases the concentration of Phenytoin, Cyclosporine and Zidovudine;
- Warfarin and coumarin anticoagulants increase prothrombin time;
- Tacrolimus increases the risk of nephrotoxicity, Midozolam disrupts the body's psychomotor reactions.
Side effects of Flucostat
When using an antifungal drug, the patient's health may deteriorate sharply. When side effects further treatment Flucostat is stopped:
- digestive system: flatulence, nausea, vomiting, loss of taste, bloating, gastralgia, diarrhea syndrome;
- nervous system: headache, dizziness, convulsions, auditory, visual hallucinations;
- urinary system and liver: cholestatic jaundice, hepatitis, renal failure, hyperbilirubinemia;
- hematopoietic organs: leukopenia, thrombocytopenia, agranulocytosis;
- metabolic processes: hypokalemia, hypercholesterolemia, hypertriglyceridemia;
- skin: erythema, urticaria, necrosis, urticaria, skin itching, redness and swelling, Stevens-Jonas syndrome;
- other: alopecia, vaginal irritation, anaphylactic shock.
Overdose
When daily doses of Flucostat are systematically exceeded, the side effects. The patient is prescribed gastric lavage, then symptomatic treatment. On the recommendation of the doctor, the patient is given forced diuresis and three-hour hemodialysis.
, onychomycosis, deep endemic mycoses.
Absolute contraindications to the use of Flucostat are hypersensitivity of the body to the active ingredients of the drug, galactosemia, and childhood. The drug is prescribed with caution for:
- pregnancy, lactation;
- organic lesions myocardium;
- chronic alcoholism;
- electrolyte imbalance;
- renal, liver failure.
Terms of sale and storage
Flucostat in any form of release is sold in pharmacies without a prescription. The medicine must be stored in a cool place out of reach of children. Shelf life – 2 years.
Analogs
If the medicine does not help or worsens the patient’s well-being, it is replaced with an analogue:
- Mikosist. These are capsules that are effective against fungal infections. During treatment, dysbiosis may develop with disruption of the intestinal microflora, so self-medication is contraindicated.
- Mycomax. A fluconazole-based drug in capsule form recommended for fungal infections. The medication is contraindicated in children weighing up to 40 kg.
- Microflucan. This is an antimycotic agent in the form of tablets and solution. The drug is prescribed for the treatment and prevention of fungal infections.
- Diflucan. 4 capsules per package, each containing 50 or 150 ml of fluconazole. Other forms are powder for preparing a suspension, solution in bottles.
A distinctive feature of the flucostat is the precise direction of its action. The drug “hits” only fungal cells, keeping bacteria “intact”, which are needed to maintain healthy microflora gastrointestinal tract or vagina. So in the fight against thrush you cannot find a better “helper” than flucostat. After all, it perfectly helps in suppressing the activity of fungi of the genus Candida.
Flucostat is available in the form of capsules and a solution, which is used when the drug must be administered through a syringe. In both cases, the active substance is fluconazole, but its concentration varies. Tablets are available in three types: fluconazole 50, 100 or 150 mg. On the shelves of pharmacies you can find bottles of 0.2 percent injection solution of 50 and 100 ml. They contain 200 mg of fluconazole.
According to experts, Flucostat capsules are very well absorbed. Their bioavailability is ninety percent, so exceeding the dosage is not recommended. Most often, one tablet per day is enough, and in the early stages, one dose is enough. It does not matter whether you took the tablet with food or not. It is absorbed equally well. Fluconazole is excreted from the body through the kidneys. Almost 80 percent is excreted in urine.
Indications
Fluxstat will be a lifeline for those who have been diagnosed with cryptococcosis (including cryptococcal meningitis, as well as its analogues). With the help of Flucostat, generalized candidiasis can be cured.
It will even help those who have contracted candidemia, disseminated candidiasis, or some other form of invasive candidal infections. Simply put, it will be effective in combating infections of the peritoneum, endocardium, as well as the eyes, respiratory and urinary tract.
Flucostat will also “come to the rescue” for those who are faced with candidiasis of the mucous membranes, esophagus, as well as non-invasive bronchopulmonary candidiasis, candiduria and skin candidiasis.
It can also be used to prevent fungal infections in patients with malignant neoplasms, predisposition to such infections sometimes appears as a side effect of chemotherapy or radiation therapy.
However, most often the drug is used to combat “thrush” (or genital candidiasis, as experts call it). With its help, you can treat vaginal candidiasis, carry out prevention and even treat candidal balanitis, the so-called “male thrush”. In addition, Flucostat is able to quickly and effectively relieve a person from skin mycoses; it is used to treat pityriasis versicolor and onychomycosis, as well as deep endemic mycoses, including coccidioidomycosis, paracoccidioidomycosis, sporotrichosis and histoplasmosis in patients with normal immunity.
If your immune system is weakened
Most often, the drug can be taken by both people with normal immunity and those who suffer from immunosuppression (for example, those who have undergone organ transplantation or have AIDS). By the way, in the second case it is also used as a means of maintenance therapy for the prevention of cryptococcal infection.
It is noteworthy that 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.
, onychomycosis, deep endemic mycoses.
Fluxstat “conflicts” with some drugs. It should not be mixed with terfenadine or astemizole, as well as other drugs that prolong the QT interval.
Hypersensitivity to the components of Flucostat or azole compounds similar in structure may also be a contraindication. It should not be given to children under the age of three years, as well as pregnant and nursing mothers. For those who are preparing to experience the joys of motherhood, flucostat is prescribed only when fungal infections threaten their life or the life of their unborn child.
It is worth treating with caution if there is a history of liver or kidney failure. Doctors try not to prescribe it to alcoholics and those who suffer from organic heart disease and electrolyte imbalance. In addition, you should not take Flucostat together with medications that cause arrhythmia.
Dosage for adults
People experiencing cryptococcal infections should take 400 mg on the first day, then 200-400 mg will be sufficient. This should be done once a day for about seven weeks.
To prevent cryptococcal meningitis in AIDS patients, it is recommended to take 200 mg per day. And for candidemia, disseminated candidiasis, as well as other similar infections, on the first day the dose is 400 mg, then it should be halved.
For oropharyngeal candidiasis, 50-100 mg is prescribed once a day. It is recommended to take the drug for at least a week. In cases where a person also suffers from suppressed immunity, treatment should be longer.
If problems arose due to wearing dentures, then 50 mg once a day is enough. True, you will have to take Flucostat for two weeks. The same or even longer course of the drug is prescribed for candidiasis infections of the mucous membranes. To get rid of this disease, Flucostat should be taken in a dosage of 50-100 mg, every day for two weeks to a month.
To prevent relapses of oropharyngeal candidiasis in patients with AIDS, after completing the full course of primary therapy, 150 mg can be prescribed once a week.
For vaginal candidiasis, the drug is taken in a dose of 150 mg. As a rule, one dose is enough. In the same way, they combat the frequency of relapses. To reduce it, the drug is used once a month.
The same dosage is prescribed for skin infections. To get rid of itching and forget about the fungus, 150 mg of Flucostat once a week or 50 mg once a day for two to four weeks is enough. In some cases, treatment is delayed for eight weeks.
Onychomycosis should be treated until a new nail grows. It will be enough to take 150 mg of the drug once a week. And for deep endemic mycoses, the dosage is increased to 200-400 mg per day. The duration of treatment in this case is determined individually.
Treatment of children
Under no circumstances should you “prescribe” pills to your child on your own; consult your doctor!
For candidiasis of the mucous membranes, the dose is 3 mg per kilogram of weight; on the first day, a loading dose of 6 mg/kg can be prescribed. The dosage is increased when it comes to the treatment of generalized candidiasis and cryptococcal infections. Therapy will be effective if you give the child 6-12 mg/kg every day.
To prevent fungal infections, a daily dosage of 3 to 12 mg/kg will be sufficient. It should be taken into account that for those who have just been born, the interval between administrations of the drug is 72 hours, and when the child grows up (at the age of two to four weeks), the same dose is administered at a shorter interval. Flucostat is given once every two days.
In children who have learned about kidney problems at a tender age, the dose should be reduced (in the same proportion as in adults). To calculate it, you need to understand how severe the kidney failure is. This can only be done by a practicing doctor.
*registered by the Ministry of Health of the Russian Federation (according to grls.rosminzdrav.ru)
INSTRUCTIONS
By medical use drug
Registration number:
Р N001361/01-310308
Trade name of the drug:
Flucostat ®
INN:
fluconazole
Dosage form:
Composition of contents per capsule:
active substance: fluconazole 50 mg or 150 mg;
Excipients: lactose (milk sugar) 49.40 mg or 147.40 mg, corn starch 16.40 mg or 49.00 mg, colloidal silicon dioxide (aerosil) 0.12 mg or 0.36 mg, magnesium stearate 0.96 mg or 2.88 mg, sodium lauryl sulfate 0.12 mg or 0.36 mg;
hard gelatin capsules:
(for 50 mg dosage) body: titanium dioxide (E 171) – 3.0000%, red iron oxide (E 172) – 0.0857%, gelatin – up to 100%; cap: titanium dioxide (E 171) – 2.0000%, red iron oxide (E 172) – 0.7286%, gelatin – up to 100%;
(for 150 mg dosage) body and cap: titanium dioxide (E 171) – 2.0000%, gelatin – up to 100%.
Description: dosage 50 mg: opaque capsules No. 2, light pink body, pinkish-brown cap; dosage 150 mg: opaque capsules No. 0, white body and cap.
Pharmacotherapeutic group:
antifungal agent
ATX code
Pharmacological properties
Pharmacodynamics:
Fluconazole, a member of the triazole antifungal class, is selective inhibitor synthesis of sterols 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, Coccidiodes immitis and Histoplasma capsulatum.
Pharmacokinetics:
After oral administration, fluconazole is well absorbed, its bioavailability is 90%. The maximum concentration after oral administration, 150 mg on an empty stomach, is 90% of the content in. plasma 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. Plasma concentrations reach a peak 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).
Administration of a loading dose (on the first day), 2 times higher than the usual daily dose, allows one 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 everything biological fluids body. Concentrations of the drug in saliva and sputum are similar to its levels in plasma. In patients with fungal meningitis, the content of fluconazole in cerebrospinal fluid reaches 80% of its level in plasma.
In the stratum corneum, epidermis, dermis and sweat fluid, high concentrations are reached that exceed serum concentrations.
Fluconazole is excreted primarily by the kidneys; approximately 80% of the administered dose is excreted unchanged. Fluconazole clearance is proportional to creatinine clearance. No fluconazole metabolites were detected in peripheral blood.
Indications for use
- 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 immunosuppression (including in patients with AIDS, during 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 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 candidiasis of the oral cavity associated with wearing dentures), esophagus, non-invasive bronchopulmonary candidiasis, candiduria, skin candidiasis; prevention of relapse of oropharyngeal candidiasis in patients with AIDS;
- genital candidiasis: treatment of vaginal candidiasis, prophylactic use to reduce the frequency of relapses of vaginal candidiasis, 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;
- skin mycoses, including mycoses of the feet, body, and groin area; pityriasis versicolor, onychomycosis; skin candidiasis;
- deep endemic mycoses, including coccidioidomycosis, paracoccidioidomycosis, sporotrichosis and histoplasmosis in patients with normal immunity.
, onychomycosis, deep endemic mycoses.
- Simultaneous use of terfenadine (against the background of repeated use of fluconazole at a dose of 400 mg / day or more) (see section “Interaction with other medicines»);
- Hypersensitivity to fluconazole and other components of the drug or azole compounds similar in structure;
- Children under 3 years of age (for this dosage form);
- Lactation period (see section “Use during pregnancy and breastfeeding”);
- Concomitant use with drugs that increase the QT interval and are metabolized by the CY3A4 isoenzyme, such as cisapride, astemizole, erythromycin, pimozide and quinidine (see section “Interaction with other drugs”);
- Lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
Carefully
- Impaired liver function tests;
- Concomitant use of potentially hepatotoxic drugs;
- Alcoholism;
- Proarrhythmic conditions in patients with multiple risk factors (organic heart disease, electrolyte imbalance, concomitant use of medications that cause arrhythmias);
- Renal dysfunction;
- 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 flucopazole at a dose of less than 400 mg/day.
Use during pregnancy and breastfeeding
There have been no adequate and controlled studies of the use of fluconazole in pregnant women.
There is currently no evidence that low doses of fluconazole (150 mg once for the treatment of vulvovaginal candidiasis) increase the incidence of adverse outcomes pregnancy, as well as the relationship with the occurrence of any specific malformations in the child.
When using high doses (400-800 mg/day) of fluconazole, several cases of multiple congenital defects have been described in newborns whose mothers received fluconazole therapy for most or all of the first trimester.
The use of the drug in pregnant women is not advisable, except for severe or life-threatening forms of fungal infections if the expected benefit to the mother exceeds possible risk for the fetus.
Women of childbearing age should use contraception.
Fluconazole is found in breast milk in the same concentration as in plasma, so its use during lactation is contraindicated.
, incl.
Inside.
For adults at cryptococcal meningitis and cryptococcal infections of other localizations on the first day, 400 mg (8 capsules of 50 mg each) is usually prescribed, and then treatment is continued at a dose of 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.
At candidemia, disseminated candidiasis and other invasive candidal infections the dose is usually 400 mg on the first day, and then 200 mg. 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.
At 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.
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 topical antiseptics for processing the prosthesis.
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. 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 vaginal candidiasis, fluconazole is taken:
At 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/mm3, treatment is continued for another 7 days.
At 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, more may be required. long-term therapy(up to 6 weeks).
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.
At 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.
At 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.
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 constant equilibrium concentrations.
For treatment generalized candidiasis or cryptococcal infection The recommended dose is 6-12 mg/kg/day depending on the severity of the disease.
For 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/day, depending on the severity and duration of persistence of induced neutropenia, the maximum daily dose no more than 600 mg.
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.
Use of the drug in patients with impaired renal function.
With a single dose, no dose change is required. When administering the drug multiple times, if the creatinine clearance (CC) is more than 50 ml/min, the usual dose of the drug is used; if the creatinine clearance (CC) is from 11 to 50 ml/min, the drug should be administered first loading dose from 50 mg to 400 mg, then a dose equal to 50% of the recommended dose is applied. For patients regularly on dialysis, one dose of the drug is administered after each hemodialysis session.
Side effect
From the gastrointestinal tract: dryness of the oral mucosa, vomiting, nausea, diarrhea, constipation, flatulence, abdominal pain.From the liver and biliary tract: rarely - impaired liver function (jaundice, hepatitis, hepatitis, hyperbilirubinemia, increased activity of alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase), hepatotoxicity, in some cases fatal, cholestasis, hepatocellular damage.
From the nervous system: headache, dizziness, change in taste, paresthesia, insomnia, drowsiness, tremor; rarely – convulsions.
From the side of blood and lymphatic system: anemia; rarely – leukopenia, thrombocytopenia, neutropenia, agranulocytosis.
From the cardiovascular system: increase in duration QT interval; fibrillation, ventricular flutter, ventricular tachysystolic arrhythmia of the “pirouette” type (torsade de pointes).
From the skin: rash, alopecia, exfoliative skin lesions, including Stevens-Johnson syndrome and toxic epidermal necrolysis, acute generalized exanthematous pustulosis, increased sweating, drug rash.
From the side of metabolism: increased concentrations of cholesterol and triglycerides in the blood plasma, hypokalemia.
From the musculoskeletal system: myalgia.
skin rash, anaphylactic reactions, Stevens-Johnson syndrome, toxic epidermal necrolysis. weakness, asthenia, increased fatigue, fever, increased sweating, vertigo; rarely – renal dysfunction.
Overdose
Symptoms: hallucinations, paranoid behavior.
Treatment: symptomatic, gastric lavage, forced diuresis. Hemodialysis within 3 hours reduces plasma concentrations by approximately 50%.
Interaction with other drugs
Single or multiple doses of fluconazole at a dose of 50 mg do not affect the metabolism of phenazone (Antipyrine) in their simultaneous administration.
Concomitant use of fluconazole with the following drugs is contraindicated
Cisapride. With the simultaneous use of fluconazole and cisapride, adverse reactions from the heart are possible, including ventricular tachysystolic arrhythmia of the “pirouette” type (torsade de pointes). The use of fluconazole at a dose of 200 mg once a day and cisapride at a dose of 20 mg 4 times a day leads to a marked increase in plasma concentrations of cisapride and an increase in the QT interval on the ECG.
Terfenadine. With the simultaneous use of azole antifungals and terfenadine, serious arrhythmias may occur as a result of an increase in the QT interval. When taking fluconazole at a dose of 200 mg/day, an increase in the QT interval has not been established. However, the use of fluconazole in doses of 400 mg/day and above causes a significant increase in the concentration of terfenadine in the blood plasma. Concomitant use of fluconazole in doses of 400 mg/day or more with terfenadine is contraindicated (see section “Contraindications”). Treatment with fluconazole in doses less than 400 mg/day in combination with terfenadine should be carried out under close monitoring.
Astemizole. The simultaneous use of fluconazole with astemizole or other drugs whose metabolism is carried out by the cytochrome P450 system may be accompanied by an increase in serum concentrations of these drugs. Elevated concentrations of astemizole in blood plasma can lead to prolongation of the QT interval and, in some cases, to the development of ventricular tachysystolic arrhythmia of the “pirouette” type (torsade de pointes). The simultaneous use of astemizole and fluconazole is contraindicated.
Pimozide. Although adequate in vitro or in vivo studies have not been conducted, concomitant use of fluconazole and pimozide may result in inhibition of pimozide metabolism. In turn, an increase in plasma concentrations of pimozide can lead to a prolongation of the QT interval and, in some cases, the development of ventricular tachysystolic arrhythmia of the “pirouette” type (torsade de pointes). The simultaneous use of pimozide and fluconazole is contraindicated.
Quinidine. Although adequate in vitro or in vivo studies have not been conducted, concomitant use of fluconazole and quinidine may also result in inhibition of quinidine metabolism. The use of quinidine is associated with prolongation of the QT interval and, in some cases, with the development of ventricular tachysystolic arrhythmia of the “torsade de pointes” type. The simultaneous use of quinidine and fluconazole is contraindicated.
Erythromycin.
Concomitant use of fluconazole and erythromycin potentially leads to increased risk development of cardiotoxicity (prolongation of the Q-T interval, torsade de pointes) and, as a result, sudden cardiac death. The simultaneous use of fluconazole and erythromycin is contraindicated.
Caution and possible dosage adjustments should be used when the following drugs are used concomitantly with fluconazole:
Hydrochlorothiazide.
Simultaneous repeated use of fluconazole and hydrochlorothiazide can lead to an increase in the concentration of fluconazole in the blood plasma by 40%. An effect of this severity does not require a change in the fluconazole dosage regimen in patients receiving concomitant diuretics, but the doctor should take this into account.
Rifampicin. The combination with rifampicin leads to a decrease in AUC (area under the concentration-time curve) 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.
Fluconazole is a potent inhibitor isoenzyme CYP2C9 and CYP2C19 cytochrome P450 and a moderate isoenzyme inhibitor CYP3A4. In addition to the effects listed below, there is a risk of increased plasma concentrations of other drugs that are metabolized by the isoenzymes CYP2C9, CYP2C19 and CYP3A4 when taken simultaneously with flucoiazole.
In this regard, caution should be exercised when using the following drugs simultaneously, and if such combinations are necessary, patients should be under close medical supervision. It should be taken into account that the inhibitory effect of fluconazole persists for 4-5 days after discontinuation of the drug due to long period half-life.
Alfentanil. There is a decrease in clearance and volume of distribution, and an increase in the half-life of alfentanil. This may be due to inhibition of the CYP3A4 isoenzyme by flucoiazole. Alfentanil dosage adjustment may be required.
Amitriptyline, nortriptyline.
Increase the effect. Concentrations of 5-nortriptyline and/or S-amitriptyline can be measured at the start of combination therapy with fluconazole and one week after the start of treatment. If necessary, the dose of amitriptyline/nortriptyline should be adjusted.
Amphotericin B.
In studies in mice (including immunosuppressed mice), the following results were observed: a small additive antifungal effect in systemic infection with C. albicans, no interaction in intracranial infection with Cryplococcus neoformans, and antagonism in systemic infection with A. fimigatus. Clinical significance these results are not clear.
When using fluconazole and other antifungal agents (azole derivatives) with warfarin, the prothrombin time increases (on average by 12%). Bleeding may develop (hematomas, bleeding from the nose and gastrointestinal tract, hematuria, melena). In patients receiving coumarial anticoagulants, prothrombin time must be constantly monitored during therapy and for 8 days after simultaneous use. The advisability of adjusting the warfarin dose should also be assessed.
Azithromycin.
With simultaneous oral use of fluconazole in a single dose of 800 mg with azithromycin in a single dose of 1200 mg, no pronounced pharmacokinetic interaction has been established between both drugs.
Benzodiazepines.
(short acting). After oral administration of midazolam, fluconazole significantly increases midazolam concentrations and psychomotor effects, and this effect is more pronounced after fluconazole is administered orally than when administered intravenously. If concomitant therapy with benzodiazepines is necessary, patients taking fluconazole should be monitored to assess the appropriateness of an appropriate reduction in the benzodiazepine dose.
When coadministered with a single dose of triazolam, fluconazole increases the AUC of triazolam by approximately 50%, Cmax by 25-50% and half-life by 25-50% due to inhibition of triazolam metabolism. Triazolam dose adjustment may be necessary.
Carbamazepine.
Fluconazole inhibits the metabolism of carbamazepine and increases its serum concentration by 30%. The risk of carbamazepine toxicity must be taken into account. The need for carbamazepine dose adjustment based on concentration/effect should be assessed.
Calcium channel blockers.
Some calcium channel antagonists (nifedipine, isradipine, amlodipine, verapamil and felodipine) are metabolized by the CYP3A4 isoenzyme. Fluconazole increases the systemic exposure of calcium channel antagonists. Monitoring for side effects is recommended.
Cyclosporine.
It is recommended to monitor the concentration of cyclosporine in the blood in patients receiving fluconazole, since 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. However, with repeated administration of fluconazole at a dose of 100 mg/day, changes in the concentration of cyclosporine in recipients bone marrow was not observed.
Cyclophosphamide.
With the simultaneous use of cyclophosphamide and fluconazole, an increase in serum concentrations of bilirubin and creatinine is observed. A combination of drugs is possible taking into account the risk of these disorders.
Fentanyl. There has been a report of one death possibly related to the concomitant use of fentanyl and fluconazole. The disturbances are believed to be related to fentanyl intoxication. Fluconazole has been shown to significantly prolong the clearance time of fentanyl. It should be taken into account that increasing the concentration of fentanyl can lead to depression respiratory function.
Halofantrine.
Fluconazole may increase plasma concentrations of halofantine due to inhibition of the CYP3A4 isoenzyme. When used simultaneously with fluconazole, as well as with other azole antifungal drugs, the development of ventricular tachysystolic arrhythmia of the “pirouette” type is possible, so their combined use is not recommended.
HMC-CoA reductase inhibitors.
When fluconazole is used concomitantly with HMC-CoA reductase inhibitors metabolized by the CYP3A4 isoenzyme (such as atorvastatin and simvastatin) or the CYP2D6 isoenzyme (fluvastatin), the risk of developing myopathy and rhabdomyolysis increases. If simultaneous therapy with these drugs is necessary, patients should be monitored to identify symptoms of myopathy and rhabdomyolysis. It is necessary to monitor the concentration of creatinine kinase
If there is a significant increase in creatinine kinase concentrations or if myopathy or rhabdomyolysis is diagnosed or suspected, therapy with HMC-CoA reductase inhibitors should be discontinued.
Losartan. Fluconazole inhibits the metabolism of losartan to its active metabolite (E-3I 74), which is responsible for most of the effects associated with antagonism angiotensin-II receptor. Regular monitoring required blood pressure.
Methadone. Fluconazole may increase plasma concentrations of methadone. Methadone dosage adjustment may be necessary.
Non-steroidal anti-inflammatory drugs (NSAIDs).
Cmax and AUC of flurbiprofen increased by 23% and 81%, respectively. Similarly, the Cmax and AUC of the pharmacologically active isomer increased by 15% and 82%, respectively, when fluconazole was co-administered with racemic ibuprofen (400 mg).
With simultaneous use of fluconazole at a dose of 200 mg/day and celecoxib at a dose of 200 mg, the Cmax and AUC of celecoxib increase by 68% and 134%, respectively. In this combination, it is possible to reduce the dose of celecoxib by half.
Despite the lack of targeted studies, fluconazole may increase the systemic exposure of other NSAIDs metabolized by the CYP2C9 isoenzyme (naproxen, lornoxicam, meloxicam, diclofenac). NSAID dose adjustment may be necessary.
When NSAIDs and fluconazole are used concomitantly, patients should be closely monitored medically to identify and monitor NSAID-related adverse events and toxicities.
Oral contraceptives.
With simultaneous use of a combined oral contraceptive with fluconazole at a dose of 50 mg, no significant effect on hormone levels has been established. When taking 200 mg fluconazole daily, the AUCs of ethinyl estradiol and levonorgestrel increase by 40% and 24%, respectively. When fluconazole 300 mg was administered once weekly, the AUCs of ethinyl estradiol and norethindrone increased by 24% and 13%, respectively. Thus, repeated use of fluconazole in the indicated doses is unlikely to affect the effectiveness of the combined oral contraceptive.
Phenytoin. 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.
Prednisone. There is a development report acute failure adrenal cortex in a patient after liver transplantation against the background of fluconazole withdrawal after a three-month course of therapy. Presumably, discontinuation of fluconazole therapy caused an increase in the activity of the CYP3A4 isoenzyme, which led to increased metabolism of prednisone.
Patients receiving combination therapy prednisone and fluconazole should be under close medical supervision when discontinuing fluconazole in order to assess the condition of the adrenal cortex.
Rifabutin. There are reports of interaction between fluconazole and rifabutin, accompanied by an increase in serum concentrations of the latter up to 80%. Cases of uveitis have been described with the simultaneous use of fluconazole and rifabutin. Patients receiving rifabutin and fluconazole simultaneously should be carefully monitored.
Saquinavir. AUC increases by approximately 50%, Cmax by 55%. The clearance of saquinavir is reduced by approximately 50% due to inhibition of the hepatic metabolism of CYP3A4 and P-glycoprotein. Dose adjustment of saquinavir may be necessary.
Sirolimus. An increase in the concentration of sirolimus in the blood plasma is presumably due to inhibition of the metabolism of sirolimus through inhibition of the CYP3A4 isoenzyme and P-glycoprotein. This combination can be used with appropriate dose adjustment of sirolimus depending on the effect/concentration.
Oral hypoglycemic agents.
Fluconazole increases the plasma half-life of oral hypoglycemic agents - sulfonylurea derivatives (chlorpropamide, glibenclamide, glipizide, tolbutamide). The combined use of fluconazole and oral hypoglycemic agents is allowed, but the doctor must keep in mind the possibility of developing hypoglycemia. Regular monitoring of blood glucose and, if necessary, dose adjustment of sulfonylurea drugs are necessary.
Tacrolimus. The use of fluconazole and tacrolimus (orally) leads to an increase in serum concentrations of the latter by 5 times due to inhibition of the metabolism of tacrolimus occurring in the intestine through the CYP3A4 isoenzyme. No significant changes in the pharmacokinetics of the drugs were observed when tacrolimus was administered intravenously. Cases of nephrotoxicity have been described. Patients receiving oral tacrolimus and fluconazole concomitantly should be monitored closely. The dose of tacrolimus should be adjusted depending on the degree of increase in its concentration in the blood.
Theophylline. When fluconazole is used at a dose of 200 mg for 14 days simultaneously (or in combination) with theophylline, the average rate of plasma clearance of tsophylline is reduced by 18%. When prescribing fluconazole to patients taking high doses of theophylline or to patients with increased risk development of theophylline toxicity, the appearance of symptoms of theophylline overdose should be monitored and, if necessary, therapy should be adjusted accordingly.
Vinca alkaloid.
Although targeted studies are lacking, it is suspected that fluconazole may increase plasma concentrations of vinca alkaloids (eg, vincristine and vinblastine) and thus lead to neurotoxicity, which may be due to inhibition of CYP3A4.
Vitamin A. There is a report of one case of development adverse reactions from the central nervous system (CNS) in the form of pseudotumor cerebri with simultaneous use of all-transretinoic acid and fluconazole, which disappeared after discontinuation of fluconazole. The use of this combination is possible, but one should remember the possibility of adverse reactions from the central nervous system.
Zidovudine. In patients receiving a combination of fluconazole and zidovudine, there is an increase in the Cmax and AUC of zidovudine by 84% and 74%, respectively, which is caused by a decrease in the metabolism of the latter to its main metabolite. Before and after therapy with fluconazole at a dose of 200 mg/day for 15 days in patients with AIDS and ARC (AIDS-related complex), a significant increase in the AUC of zidovudine (20%) was found. Patients receiving this combination should be monitored for side effects of zidovudine.
Voriconazole (inhibitor of the isoenzyme CYP2C9, CYP2C19 and CYP3A4).
Concomitant use of voriconazole (400 mg twice daily on the first day, then 200 mg twice daily for 2.5 days) and fluconazole (400 mg on the first day, then 200 mg daily for 4 days) , leads to an increase in voriconazole concentration and AUC by 57% and 79%, respectively. It has been shown that this effect persists when the dose and/or frequency of administration of any of the drugs is reduced. Concomitant use of voriconazole and fluconazole is not recommended.
Tofacitinib:
Tofacitinib exposure increases when co-administered with drugs that are both moderate CYP3A4 inhibitors and strong CYP2C19 inhibitors (for example, fluconazole). A dose adjustment of tofacitinib may be necessary.
Studies of the interaction of oral forms of fluconazole when taken simultaneously with food, cimetidine, antacids, as well as after total body irradiation in preparation for bone marrow transplantation showed that these factors do not have a clinically significant effect on the absorption of fluconazole.
The listed interactions were established with repeated use of fluconazole; There are no known drug interactions resulting from a single dose of fluconazole.
Doctors should note that interactions with other drugs have not been specifically studied, but are possible.
special instructions
In rare cases, the use of fluconazole was accompanied by toxic changes in the liver, incl. with a fatal outcome, mainly in patients with serious concomitant diseases. 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.
Treatment must be continued until clinical and hematological remission occurs, since premature cessation leads to relapses.
Impact on the ability to drive vehicles and machinery
Due to the possibility of dizziness and other side effects associated with taking the drug, during the treatment period patients are advised to refrain from driving vehicles and engaging in other potentially dangerous activities. dangerous species activities requiring increased concentration attention, speed of psychomotor and motor reactions.
Release form
Capsules 50 mg and 150 mg.
7 capsules of 50 mg or 1, 2, 3, 6 capsules of 150 mg in a blister pack.
1 blister pack of 7 capsules (for a dosage of 50 mg) or 1 blister pack of 1, 2, 3 capsules or 4 blister packs of 6 capsules (for a dosage of 150 mg) along with instructions for use in a cardboard pack.
Storage conditions
Store at a temperature not exceeding 25 °C.
Keep out of the reach of children.
Best before date
3 years. Do not use after the expiration date stated on the package.
Vacation conditions
Over the counter.
Name and address of the manufacturer/organization receiving claims:
OJSC "Pharmstandard-Leksredstva", 305022, Russia, Kursk, st. 2nd Aggregate. 1 a/18.
www.pharmstd.ru