Fluconazole is an effective remedy for combating candidiasis

Thrush or vaginal candidiasis is a disease that is encountered quite often today. Moreover, it occurs in both men and women. The difference is that in women it manifests itself with severe symptoms, while a man can only be a carrier, without characteristic signs. The causative agent of the disease is the diploid fungus Candida. This fungus exists in the body of every person, but favorable conditions, decreased immunity, and a number of other factors provoke its proliferation. The consequence of which is the disease thrush. In the article we talk about the causes, symptoms of thrush, as well as the popular treatment “Flucostat”.

Composition of Flucostat

Composition of 1 ml solution for parenteral administration:

• fluconazole – 2 mg;
• sodium chloride;
• water for injections.

capsule has the following components:

• fluconazole – 50 mg (or 150 mg);
• colloidal silicon dioxide (aerosil);
• corn starch;
• magnesium stearate;
• sodium lauryl sulfate;
• lactose.

capsule shell contains:

• gelatin;
• red dye iron oxide (E 172);
• methyl parahydroxybenzoate;
• propyl parahydroxybenzoate;
• titanium dioxide (E 171);
• acetic acid.

Release form

• Film-coated capsules are light pink or pink-brown in color, opaque. Inside there is a white or close to white powder. Packaged in 7 pieces in contour cell blisters. Cardboard packaging holds 1 plate.
• Tablets of 50 or 150 mg are white, oval in shape, secured in a contour-cell blister of 1 or 2. A cardboard pack contains only 1 plate with the drug.
• Solution for intravenous administration in the form of a clear, colorless liquid in 50 ml bottles. One bottle of medicine is placed in a cardboard package.
• White oval-shaped vaginal suppositories

pharmachologic effect

Flucostat is a strong antifungal pharmaceutical drug that, according to its chemical structure, belongs to the class of triazole compounds. Active against the following families of microorganisms:

• Candida spp;
• Cryptococcus neoformans;
• Microsporum spp;
• Trichphuton spp;
• Blastomyces dermatidis;
• Coccidioides immits;
• Histoplasma capsulatum.

The mechanism of the therapeutic action of the drug lies in the ability of the biologically active component to selectively inhibit the synthesis of sterols in the cells of sensitive fungi, due to which the cell wall of harmful or opportunistic microorganisms becomes untenable , since sterol is one of its main components.

Pharmacodynamics and pharmacokinetics

After oral administration of tablets or capsules, the active ingredients are well absorbed from the gastrointestinal tract. After 0.5-1.5 hours on an empty stomach, the maximum plasma concentration is achieved. The constituent elements of the drug penetrate well into all biological fluids of the body . There are certain properties for cumulation - six months after completion of conservative therapy, Fluconazole can be detected in the nails. About 80% of pharmaceutical drug metabolites are eliminated by the kidneys.

With intravenous administration of a parenteral solution of Flucostat, the active components are evenly distributed throughout biological fluids (the concentration in pulmonary sputum and saliva in the oral cavity corresponds to the amount of Fluconazole in the blood plasma). After several injections of 1 dose per day, the level of equilibrium concentration is reached by 4-5 days of conservative treatment, and with the initial use of a double amount of the drug - by 2 days.

In the bloodstream, about 11-12% of the total amount of Fluconazole binds to plasma proteins, which is why the half-life corresponds to 30 hours. The vast majority (about 80%) of the pharmaceutical drug is excreted in the urine. The clearance of the active component is directly proportional to the clearance of Creatinine.

How it works

Flucostat affects many microorganisms:

• candida;
• cryptococks;
• microspores;
• trichophytons;
• blastomycetes;
• coccidioides immitis;
• histoplasma.

The drug is well absorbed by the intestines. Half an hour after administration, the maximum concentration is already reached. The substance penetrates into all systems and organs. Excreted in urine.

Indications for use

• cryptococcosis (including cryptococcal meningitis);
• pityriasis versicolor;
• generalized or disseminated candidiasis, mainly affecting the skin and mucous membranes (for example, the oral cavity and esophagus);
• deep endemic mycoses (sporotrichosis, histoplasmosis, coccidioidomycosis);
• urogenital candidiasis in men (candidal balanitis) and women (vaginal candidiasis or thrush);
• prevention of fungal infections in patients with acquired immunodeficiency syndrome;
• mycoses of various etiologies;
• damage by pathogenic fungi during cytostatic, chemotherapy or radiation therapy;
• onychomycosis.

When is it prescribed?

The drug is prescribed in the following conditions:

• mycosis;
• pityriasis versicolor;
• cryptococcosis;
• onychomycosis;
• candidiasis;
• prevention of fungal diseases;
• thrush;
• fungal infections after chemotherapy.

The drug is also prescribed as a prophylaxis during treatment with antibiotics.

Contraindications

Strict contraindications include the following conditions:

• increased individual sensitivity to the active ingredient or excipients;
• glucose-galactose malabsorption syndrome;
• lactose intolerance (including lactase deficiency);
• hereditary or acquired intolerance to the components of a pharmaceutical drug;
• children under 3 years of age;
• galactosemia;
• combined use of Flucostat with drugs that prolong the QT interval on the electrocardiogram (in particular astemizole or terfenadine ).

You should also outline a list of non-absolute contraindications when the medicine must be used with caution (conservative therapy under the supervision of qualified medical personnel is recommended):

• renal or liver failure;
• alcoholism;
• treatment with potentially dangerous pharmaceuticals with a high percentage of hepatotoxicity ;
• proarrhythmogenic conditions (especially if the patient has multiple risk factors for arrhythmia).

Who should not take it

The drug is contraindicated:

• children under three years old;
• with galactosemia;
• with increased sensitivity;
• with lactose intolerance;
• with renal failure;
• with liver failure;
• with alcohol addiction;
• during treatment with hepatoxic drugs;
• with extensive arrhythmia.

Sometimes unpleasant actions occur during treatment.

Side effects

When using capsules or tablets orally:

• From the digestive system: nausea, diarrhea, bloating and flatulence .
• Nervous system: headache and dizziness .
• From the hematopoietic system: thrombocytopenia, leukopenia, agranulocytosis .
• Allergic manifestations: anaphylactic reactions, skin rash .

Intravenous use of a pharmaceutical drug may cause the following side effects:

• From the gastrointestinal tract: nausea followed by vomiting, flatulence, abdominal pain, functional liver failure (increased levels of alkaline phosphatase, serum aminotransferases or bilirubin).
• Nervous system: headache, seizures .
• From the cardiovascular system: increased duration of the QT interval , ventricular fibrillation or even flutter .
• Allergic reactions: skin rash, Stevens-Jonas syndrome , toxic epidermal necrosis or Lyell's syndrome (an extreme manifestation of toxicoderma ), anaphylactic reactions.
• Metabolic processes: hypercholesterolemia, hypokalemia, hypertriglyceridemia.
• From other systems: alopecia, renal failure .

Flucostat 150 mg 2 pcs. capsules

pharmachologic effect

Antifungal agent.

Composition and release form Flucostat 150 mg 2 pcs. capsules

Capsules - 1 capsule:

• active substance: fluconazole - 150 mg;
• excipients: lactose (milk sugar) - 147.40 mg, corn starch - 49.00 mg, colloidal silicon dioxide (aerosil) - 0.36 mg, magnesium stearate - 2.88 mg, sodium lauryl sulfate - 0.36 mg;
• hard gelatin capsules (body and cap): titanium dioxide (E 171) - 2.0000%, gelatin - up to 100%.

1, 2, 3, 6 capsules of 150 mg each in a blister pack.

1 blister pack 4 blister packs of 6 capsules each along with instructions for use in a cardboard pack.

Description of the dosage form

Opaque capsules No. 0, white body and cap.

Characteristic

An antifungal agent from the group of triazole derivatives.

Directions for use and doses

Inside.

For adults with 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 200-400 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.

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

For vaginal candidiasis, fluconazole is taken:

• For newly diagnosed vaginal candidiasis - a single dose of 150 mg;
• For vaginal candidiasis with rare exacerbations or mild or moderately severe symptoms - a single dose of 150 mg;
• For severe vaginal candidiasis (with severe symptoms) - 150 mg once a day with an interval of 72 hours (on days 1 and 4 of therapy);
• For vaginal candidiasis with frequent relapses (4 or more times a year) - for the treatment of exacerbation: 150 mg 1 time per day with an interval of 72 hours (on days 1, 4 and 7 of therapy); to reduce the frequency of relapses: 150 mg once a week for 6 months.

Some patients may require more frequent use.

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

Pharmacodynamics

Fluconazole, a member of the triazole antifungal class, is a 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, 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 all biological fluids of the body. Concentrations of the drug in saliva and sputum are similar to its levels 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. 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 Flucostat 150 mg 2 pcs. capsules

• 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;
• in 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; in 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 (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, onychomycosis; skin candidiasis;
• in deep endemic mycoses, including coccidioidomycosis, paracoccidioidomycosis, sporotrichosis and histoplasmosis in patients with normal immunity.

Contraindications

• Simultaneous use of terfenadine (against the background of repeated doses of fluconazole at a dose of 400 mg/day or more);
• 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;
• Concomitant use with drugs that increase the Q-interval and are metabolized by isoenzyme CY3A4, such as cisapride, astemizole, erythromycin, pimozide and quinidine;
• 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 terfeiadine and fluconazole at a dose of less than 400 mg/day.

Application of Flucostat 150 mg 2 pcs. capsules during pregnancy and breastfeeding

There have been no adequate and controlled studies of the use of flucopazole in pregnant women.

Currently, there is no evidence of the effect of low doses of flucopazole (150 mg once for the treatment of vulvovaginal candidiasis) on an increase in the incidence of adverse pregnancy outcomes, 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, with the exception of severe or life-threatening forms of fungal infections, if the expected benefit to the mother outweighs the possible risk to 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.

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 hematological remission occurs, since its premature transformation leads to relapses.

Impact on the ability to drive vehicles and operate 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 hazardous activities that require increased concentration, speed of psychomotor and motor reactions.

Overdose

Symptoms: hallucinations, paranoid behavior.

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

Side effects Flucostat 150 mg 2 pcs. capsules

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, hepatonecrosis, hyperbilirubipemia, increased activity of alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase), hepatotoxicity, in some cases fatal, cholesgas, genocellular damage.

From the nervous system: headache, dizziness, change in taste, paresthesia. insomnia, drowsiness, tremor; rarely - convulsions.

From the blood and lymphatic system: anemia; rarely - leukopenia, thrombocytopenia, eutropenia, agranulocytosis.

From the cardiovascular system: increased duration of the 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 metabolic side: increased concentrations of cholesterol and triglycerides in the blood plasma, hypokalemia.

From the musculoskeletal system, myalgia.

Other: weakness, asthenia, increased fatigue, fever, increased sweating, vertigo; rarely - renal dysfunction.

Drug interactions

Single or multiple doses of fluconazole at a dose of 50 mg do not affect the metabolism of phenazone (Antipyrine) when taken simultaneously.

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 dc 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 terfinadine, 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. 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 plasma concentrations of astemizole may lead to prolongation of the QT interval and, in some cases, to the development of torsade dc pointes. The simultaneous use of astemizole and fluconazole is contraindicated.

Pimozide. Although appropriate in vitro or in vivo studies have not been conducted, the simultaneous use of fluconazole and pimozide may lead to inhibition of the metabolism of pimozide. 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. Despite. Although appropriate in vitro or in vivo studies have not been conducted, the simultaneous use of flucoiazole and quinidine may also lead to inhibition of quinidine metabolism. The use of quinidine is associated with prolongation of the QT interval and, in some cases, with the development of torsade dc pointes. The simultaneous use of quinidine and fluconazole is contraindicated.

Erythromycin. Concomitant use of fluconazole and erythromycin potentially leads to an increased risk of cardiotoxicity (QT prolongation, torsade de pointes) and, consequently, 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 flucoiazole: Hydrochlorothiazide. Simultaneous repeated use of flucoiazole 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. Combination with rifampicin leads to a decrease in AUC (area under the competition curve), 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 (fluvastagin), 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. Flucopazole inhibits the metabolism of losartan to its active metabolite (E-31 74), which is responsible for most of the effects associated with angiotensin-II receptor antagonism. Regular monitoring of blood pressure is necessary.

Methadone. Flucopazole may increase plasma concentrations of methadone. Methadone dose adjustment may be necessary.

Non-steroidal anti-inflammatory drugs (NSAIDs). Flurbiprofen Cmax and AUC increased by 23% and 81%, respectively. Similarly, Cmax and AUC of the pharmacologically active isomer [S-(+)-ibuprofen] increased by 15% and 82%, respectively, when fluconazole was administered simultaneously 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 PIVPs metabolized by the CYP2C9 isoenzyme (naproxen, lornoxicam, meloxicam, diclofenac). The dose of PIVP may need to be adjusted.

When using NSAIDs and fluconazole 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 at 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 report of the development of acute adrenal insufficiency in a patient after liver transplantation when fluconazole was discontinued 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 with prednisone and fluconazole should be under close medical supervision when discontinuing fluconazole 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 the CYP3A4 isoenzyme and P-glycoprotsin. 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 isphrotoxicity 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 using fluconazole at a dose of 200 mg for 14 days simultaneously (or in combination) with theophylline, the average rate of plasma clearance of theophylline is reduced by 18%. When prescribing fluconazole to patients taking high doses of tsophylline, or to patients at increased risk of developing theophylline toxicity, 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 isrotoxicity, which may be due to inhibition of the CYP3A4 isoenzyme.

Vitamin A. There is a report of one case of the development of adverse reactions from the central nervous system (CNS) in the form of pseudotumor cerebri with the simultaneous use of all-trans retinoic 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 is increased when coadministered with drugs that are both moderate CYP3A4 inhibitors and strong CYP2C19 inhibitors (eg, fluconazole). 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 flucopazole; 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.

Flucostat, instructions for use (Method and dosage)

Flucostat tablets, instructions for use

Film-coated capsules and tablets are used enterally , that is, orally. They should be swallowed whole without breaking the integrity, this may affect the therapeutic effectiveness of the treatment. How to take it - before or after a meal - does not matter, since the absorption of the active components of Flucostat does not depend on filling the lumen of the digestive tube. The duration of treatment is selected individually; as a rule, conservative therapy is carried out until the results of microbiological studies of the pathological focus are completely negative.

The dosage of the pharmaceutical drug and the treatment regimen depend on the clinical diagnosis:

• atrophic oral candidiasis and similar infections of the mucous membranes – 50-100 mg/day for 14-30 days;
• cryptococcal infections , disseminated candidiasis and fungi entering the blood - 1st day 400 mg, and then 200-400 mg once a day for a long period;
• vaginal candidiasis and balanitis - 150 mg once, and then to prevent relapse 150 mg once a month for 4-12 months;
• skin mycoses - 150 mg once a week or 50 mg once a day for 2-6 weeks, depending on the sensitivity of the pathogen to therapy;
• pityriasis versicolor – 50 mg once a day for 2-4 weeks;
• deep endemic mycoses - 200-400 mg per day (duration depends on the pathogenic fungus that caused the disease);
• onychomycosis - 150 mg once a week until the unaffected nail plate is completely restored (nails on the hands grow in 3-6 months, and on the feet in 6-12 months).

antibiotics are often added to the treatment regimen . Solutab , a beta-lactam penicillin , which is used to prevent the development of generalized infectious diseases with local or general decrease in immunity due to toxins of pathogenic fungal colonies, has received especially widespread use in this vein You should find out from your doctor how to take antibiotics, because their incorrect use can lead to such adverse consequences as dysbacteriosis or the development of microflora resistance to the penicillin group of drugs.

Antifungal medicine for children

The tablet form of Flucostat can also be used in pediatric practice, since fungal infections in children develop and occur even more often than in adults. The dosage is selected individually for each child, based on his anthropometric indicators (in particular weight) and clinical diagnosis, which should be confirmed by microscopic examination. treatment regimens for pediatricians exist

• candidiasis of the mucous membranes - 6 mg per 1 kg of patient weight on day 1, and then 3 mg per kg until the results of microbiological studies are negative;
• cryptococcosis and systemic candidiasis – 6-12 mg/kg, depending on the severity of the disease;
• for preventive purposes against the background of reduced immune abilities of the body - 3-12 mg per 1 kg of weight per day (the exact amount of the pharmaceutical drug should be calculated based on the level of leukopenia in a blood test).

How to take medicine for thrush

How to take Flucostat for thrush , each patient can decide independently or find out in consultation with a qualified specialist, since there are different treatment regimens for fungal infections of the urogenital area in women. The quantity and frequency of application depends on the manifestations of the pathological process, the form of the disease and associated complications:

• An uncomplicated form of candidiasis that occurs for the first time with mild or moderate symptoms - 1 capsule (150 mg of Flucostat) once.
• Complicated form of thrush with severe symptoms or against the background of concomitant chronic diseases - 150 mg of the drug on days 1 and 4 of conservative therapy.
• A recurrent form of candidiasis in women, which manifests itself at least 4 times during the year - 150 mg in three doses, on the 1st, 4th and 7th day of sanitation. It is also necessary to treat the sexual partner - 150 mg once. This form of fungal pathology requires maintenance therapy to prevent repeated episodes of the disease. For this purpose, 150 mg tablets are used once a week for 6 months.

How long does it take for a pharmaceutical drug to help?

Whether the medicine for thrush helps and how long to wait for the therapeutic effect can be found out after two weeks in case of a severe form of the disease or in a week if the nosological unit manifests itself with mild symptoms without adverse consequences, because this is how long the course of conservative treatment usually lasts, after which the following symptoms disappear without a trace:

• annoying itching and burning in the external genitalia and vagina;
• copious curdled discharge ;
• pain during intercourse or urination.

Flucostat suppositories

It should be noted that the instructions for using Flucostat for thrush may also include suppositories as a local means of combating harmful fungi, which from the point of view of the medical community is much more favorable for a number of reasons:

• the use of vaginal suppositories is not accompanied by unpleasant sensations or inconvenience;
• a course of conservative therapy can be started immediately from the moment the characteristic symptoms of a given nosological unit are detected, without even waiting for the end of the menstrual cycle;
• side effects from pharmaceutical treatment are less ;
• the therapeutic effectiveness of suppositories does not depend on food intake, time of day and in no way affects the usual routine of things.

To make sure how to take Flucostat for thrush in the form of suppositories, the exact dosages of this pharmaceutical form of the drug, the duration of the course of therapy, you should contact the antenatal clinic or the gynecological department, however, as a rule, the treatment regimen does not differ from that when using the enteral form of the antifungal drug facilities.

Instructions for Flucostat for men

Thrush is a disease that affects predominantly the female half of the population, but the widespread belief is that genital candidiasis is their exclusive lot. is erroneous. Of course, yeast-like fungi of the genus Candida do not take root well in the urethra of most of our planet, since they are regularly washed out with urine , but with a local weakening of immune mechanisms, favorable conditions are created for the development of urogenital candidiasis , and therefore the question is increasingly being asked whether men can take Flucostat to eliminate thrush.

antifungal pharmaceutical drug is absorbed into the main bloodstream and is evenly distributed in the biological fluids and environments of the male body in the same way as in women. But biologically active components have no effect on hormonal levels and are not capable of changing it in any way, so can men Flucostat to get rid of an unpleasant pathology - of course, yes. Such therapeutic measures will be regarded as etiological therapy aimed at eradicating the causative agent of thrush.

Reasons for the development of thrush

There are many reasons for the development of thrush. At the same time, there are a number of main factors that have a strong influence on the microflora and thereby provoke the appearance of thrush:

• Antibiotics;
• acute respiratory viral infections and food poisoning;
• stressful conditions;
• chronic diseases of the reproductive system;
• hormonal changes;
• endocrine diseases;
• reaction to underwear and intimate hygiene products;
• poor nutrition;
• sudden climate change.

Symptoms of thrush

You can notice thrush in the early stages of the disease:

• the discharge becomes more abundant and acquires a cheesy consistency;
• irritation and swelling of the genital mucosa appears;
• During sexual intercourse and urination, discomfort is clearly felt - burning, itching.

Overdose

Symptoms that are observed with a drug overdose:

• hallucinations;
• maximum manifestation of side effects (see list above);
• paranoid behavior.

There is no specific pharmaceutical antidote for reversing an overdose of Flucostat. Gastric lavage and symptomatic treatment of individual manifestations should be performed. Forced diuresis is also indicated , since the main route of excretion of metabolites of the active ingredient is in the urine. Hemodialysis works well, since within three hours of manipulation the plasma concentration of Fluconazole is reduced by half.

special instructions

Flucostat has the property of somewhat lowering local immunity , acting in a specific way on the microflora of the urogenital area. As a result of this side effect, additional gates are opened for the invasion of infectious pathogens of a non-fungal nature, and accordingly, conditions are created for the development of unpleasant diseases of the genitourinary system. In order to eliminate possible adverse effects of conservative therapy, antibiotics .

Qualified specialists agree that no ordinary pharmaceutical drug should be used, so as not to develop resistance to the main chemical components of drugs that affect harmful microflora. In this vein, Solutab 30 , a reserve antibiotic, is often used, which reduces the risk of the above-mentioned complications of treating fungal pathology.

Flucostat's analogs

Level 4 ATC code matches:
Medoflucon

Vfend

Itracon

Mikosist

Irunin

Mikomax

Orungal

Mycoflucan

Fluconazole

Sporagal

Orungamin

Difluzol

Rumicosis

Futsis

Vero-Fluconazole

Kandizol

Kanditral

Itraconazole

Diflazon

Contraindications to the use of Flucostat are common metabolic disorders, therefore there is a whole group of foreign pharmaceuticals that, under certain conditions, can be used as an analogue of Flucostat for thrush or other nosological units of fungal origin. Mikosist, Mikomax, Microflucan have received wide recognition among patients, but Diflucan as a high-quality substitute for an antifungal drug.

Diflucan and Flucostat: the difference between antifungal agents

• Diflucan is an imported drug that is produced in such advanced countries as the United States of America and France, in contrast to the domestic Flucostat;
• Flucostat is an original drug that appeared on the pharmaceutical market at the end of the last century;
• Flucostat contains some chemical components that are not found in Diflucan.

Based on the differences between these pharmaceuticals, it is difficult to definitively answer which is better—Flucostat or Diflucan. Of course, the credibility of an imported drug is greater, especially since production in such large countries allows you to be confident in the high quality of medicinal products. On the other hand, the price of Flucostat is 10, and sometimes more, times less than the cost of Diflucan, which in our mentality is also valued very highly, so the choice: what to use - Flucostat or Diflucan - should be made independently.

Domestic analogues

Since the price of analogues produced abroad is significantly higher than the cost of domestic drugs, patients try to avoid purchasing them and are increasingly seeking to find cheap Russian analogues of Flucostat. But this group of pharmaceuticals is presented extremely poorly on pharmacy shelves; moreover, we can say that there is only one analogue of Flucostat that is not inferior in therapeutic effectiveness, but cheaper - Fluconazole, the capsules of which use an identical active substance in the same dosages (50 and 150 mg), as in Flucostat, but the price of cardboard packages is sometimes 10 times lower, which, undoubtedly, makes the choice to the domestic analogue.

Analogs

There are drugs with similar effects:

• medoflucon;
• Vfend;
• itracon;
• mycosist;
• mycomax;
• irunin;
• orungal;
• mycoflucan;
• fluconazole.

All of these medications have antifungal effects. The only difference is the price, auxiliary components, and country of production. Among domestic drugs – Fluconazole. It is cheaper than Flucostat, but the effect is similar.

Flucostat and alcohol

Exposure to any pharmaceutical drug while drinking alcohol leads, as a rule, to the development of adverse consequences of conservative therapy. Flucostat, in turn, is not just an ordinary drug, but its active components have antibiotic properties, therefore combining alcohol with a course of conservative sanitation with an antifungal drug is strictly prohibited in order to avoid the development of the following pathological conditions:

• toxic and necrotic liver damage;
• inadequate functioning of the central nervous system with the development of increased sensitivity of various structures to afferent and efferent impulses;
• increased load on the heart muscle;
• high risk of developing arterial hypertension , up to rapid hypertensive crisis;
• a significant decrease in the therapeutic effectiveness of the drug.

Compatibility

During treatment with flucostat, you should not drink alcohol. Violation of this condition can lead to serious consequences, including death. You should not take flucostat simultaneously with drugs that are hard on the liver. This can cause serious poisoning and liver dysfunction.

Do not take the drug simultaneously with blood thinning medications. Oral contraceptives reduce the effect of flucostat.

During pregnancy, the drug is prescribed only if the benefit to the mother outweighs the risk to the fetus. Because the drug affects the liver and is absorbed into the blood, penetrating the placenta. A similar effect is observed in nursing mothers. The substance passes easily into breast milk. Therefore, it is not recommended to take the drug during breastfeeding.

Flucostat during pregnancy (and lactation)

During the use of the drug, the active ingredients are absorbed into the main bloodstream and distributed throughout the woman’s body, evenly deposited in biological fluids. That is why the use of the antifungal drug Flucostat during pregnancy is allowed only for health reasons (for example, in the case of severe, generalized infections that threaten the life of the expectant mother and fetus).

If there is a need to undergo a course of conservative therapy during breastfeeding, then the child should be weaned from the breast and mother’s milk, because even in such a specific secretion traces of biologically active substances that are part of the enteral and parneteral forms of Flucostat are found.

Can I take Fluconazole while taking antibiotics?

Combinations of antibiotics and antifungal agents are determined only by a doctor. If after treatment with antibiotics the patient develops candidiasis, the use of Fluconazole is possible. But simultaneous use is not always possible due to the fact that the medicine actively interacts with other substances. Some antibiotics, cardiovascular drugs, psychotropic drugs and many others are at risk. Therefore, the patient must be informed about all his concomitant diseases and medications taken.

Reviews of Flucostat

Reviews about Flucostat on the Internet are full of positive emotions and grateful words, because the drug in a short time allows you to eliminate very unpleasant pathological conditions associated not only with adverse consequences in the physical sense, but also with special psycho-emotional factors. Reviews from women vying with each other insist that diseases of the urogenital area, as a rule, are associated with stress, and this entails a deterioration in the functioning of all organs and systems in the body. Flucostat, in turn, not only eliminates the main cause of the unpleasant disease, but also allows you to “take a deep breath” when starting a new day.

Therefore, reviews of Flucostat for thrush recommend the use of the pharmaceutical drug everywhere, even only if a nosological entity caused by fungal invasion in the genitourinary system is suspected. Patients who have undergone a course of conservative therapy note that the drug allows for effective eradication of the pathogen even in the complicated form of thrush and with a recurrent course, which is not feasible for every antifungal drug.

Flucostat for men is no less useful a drug than for women, since, contrary to popular belief, the causative agent of thrush, the yeast-like fungus Candida albicans, can also infect the genitourinary system of the stronger sex. In this case, the therapeutic effect of the pharmaceutical drug makes it possible to eliminate unpleasant manifestations within a short period of sanitation. Also, film-coated capsules or a solution for parenteral administration of Flucostat are used to prevent asymptomatic carriage of fungi in men, because during sexual intercourse women are infected, in whose vagina the optimal environment for the development of a pathological focus is constantly maintained.

Special Recommendations

Patients diagnosed with AIDS may develop a rash from taking Flucostat. In this case, you should immediately stop taking the drug, since in such patients the skin reactions are more severe. If the rash appears in other people, close monitoring should be initiated. If the rash does not progress to the stage of formation of bullous lesions, treatment can be continued. In addition, Flucostat should be taken with extreme caution when taking drugs that are metabolized by isoenzymes of the cytochrome P450 system.

Flucostat and antibiotics

Although antibiotics can cause thrush, they may also be necessary for treatment. The dosage and duration of the course are determined based on an analysis of the patient’s condition and the stage of the disease.

Antibiotics are prescribed to completely eradicate the infection. At the same time, it is important to strictly adhere to the course of taking medications. Taking Fluyucostat should be started no earlier than 2-5 days after starting the antibiotic. It is also important to maintain a certain hourly interval between taking antibiotics and Flucostat.

Flucostat can also be prescribed after a course of antibiotics as a prophylactic agent. The preventive course lasts no more than 2 weeks. Usually 150-250 mg of the drug is prescribed.

Flucostat and its effect on the body

In addition to the fact that Flucostat negatively affects the functioning of the kidneys and liver, the negative effects of the drug can also affect the patient’s general well-being. This can be expressed in gastrointestinal disorders, dizziness, and the appearance of a rash. In addition, the drug has a strong effect on the hematopoietic system, which can lead to blood diseases.

Flucostat and its effect on sexual intercourse

The effect of the drug is usually observed within 2 days after administration. However, it is not recommended to resume sexual activity earlier than after a month. The best solution would be to have repeat smears and return to sexual activity after receiving a positive smear test result.

Flucostat and menstruation

Menstruation with thrush can cause the condition to worsen. During menstruation, the vaginal microflora becomes favorable for the development of fungus. This is why it is important to continue taking the drug during this time. Flucostat does not affect the cycle in any way. It does not apply to hormonal drugs. Increased discharge is possible, as the product provokes a decrease in potassium content.

Flucostat today is one of the most effective means in the fight against thrush and other fungal infections. But it should be taken strictly as prescribed by a specialist.

Flucostat price, where to buy

The price of Flucostat largely depends on the form of release of the pharmaceutical drug and the country where you want to buy the antifungal agent. For example, Ukraine offers the most optimal price for pharmaceutical products, Kharkov is especially pleasing, because in the first capital the price of Flucostat tablets is 27 hryvnia, and the price of candles is less - 10-15 hryvnia.

In Russia, how much Flucostat costs in the pharmacy located closest to you must be found out taking into account the prescribed dosage of the drug, since the price of Flucostat 150 mg is 350 rubles, and capsules containing 50 mg of antifungal powder can be purchased for 270 rubles.

The price of Flucostat for thrush in other nearby countries can be calculated at the local exchange rate, because competition for the import of pharmaceutical products extends far beyond the borders of the CIS countries. For example, in Belarus, 150 mg tablets can be bought for between 10-40 thousand rubles, which reflects the exact cost of the drug in Kharkov, and the price of ointment in Kazakhstan is equivalent to its cost in Omsk.

• Online pharmacies in RussiaRussia

ZdravCity

• Flucostat capsules 50 mg 7 pcs. Pharmstandard-Leksredstva OJSC
  356 rub. order

How to take Fluconazole for thrush?

With this pathology, patients can purchase medicine without a prescription and on the advice of a pharmacist. If you visit a doctor, he will confidently prescribe Fluconazole even before receiving test results for pathogens. Later, if the examination results are available, the doctor will only need to adjust the treatment regimen, or continue the chosen tactics. Fluconazole capsules help very quickly.

When taken orally, the level of bioavailability of the drug is as high as when administered intravenously, so it is enough to take one 150 mg capsule once with water. To prevent symptoms from returning, it is possible to take the drug every three days, with a total of 3 doses - on days 1, 4 and 7.

Fluconazole can begin to work within a day. In particular, the manufacturer of the original drug Pfizer (Diflucan) specifically reports that relief occurs within 24 hours. However, it is necessary to consult a doctor in order to exclude the presence of other pathogenic agents.

Fluconazole 150 mg

Thrush itself is not a sexually transmitted infection. Candidiasis develops against a background of reduced immunity, for example, after using antibiotics, when wearing synthetic underwear, during periods of very hot weather and even under stress. During a visit to the doctor, patients must be informed about the presence of a sexual partner so that preventive or therapeutic measures can be prescribed.

Women often ask the question: can cystitis appear from thrush? In this case, only the doctor can give an objective answer. The development of cystitis against the background of thrush is a very real scenario if the patient ignores visiting a specialist. Yeast-like fungi travel from the urethra to the bladder and cause inflammation there. Symptoms of vaginal candidiasis and cystitis may be similar. In the future, the infection from the bladder can reach the kidneys and there lead to acute renal failure. Therefore, therapy must be started on time. Sometimes women do not have candidiasis, but it develops after treating cystitis with antibiotics. A doctor will help correct the unpleasant effect.