Fluconazole-Teva, 50 mg capsules 7 pcs.

Composition

1 capsule contains: 

Active ingredient:

fluconazole 50 mg;

Auxiliary substances:

lactose monohydrate;

pregelatinized starch;

colloidal anhydrous silicon dioxide;

magnesium stearate;

sodium lauryl sulfate.

Composition of the gelatin capsule body:

titanium dioxide (E171),

gelatin. Composition of the gelatin capsule cap:

titanium dioxide (E171),

diamond blue FCF (E133),

gelatin.

Pharmacological action

An antifungal agent derived from triazole. It is a selective inhibitor of sterol synthesis in fungal cells. Fluconazole is highly specific for cytochrome P450-dependent fungal enzymes.

When taken orally and when administered intravenously, fluconazole was active in various models of fungal infections in animals.

Fluconazole is active in opportunistic mycoses, including those caused by Candida spp., including generalized candidiasis in animals with reduced immunity; Cryptococcus neoformans, including intracranial infections; Microsporum spp. and Trychoptyton spp. Active in models of endemic mycoses in animals, including infections caused by Blastomyces dermatitidis, Coccidioides immitis, including intracranial infections, and Histoplasma capsulatum in animals with normal and reduced immunity.

Indications

• Cryptococcosis, including cryptococcal meningitis and other localization of the infection (including the lungs, skin), as in patients with normal immune response and in patients with various forms of immunosuppression (including patients with AIDS, organ transplant); the drug can be used for the prevention of cryptococcal infections in AIDS patients;
• generalized candidiasis, including candidemia, disseminated candidiasis and other forms of invasive Candida infections (infection of the peritoneum, endocardium, eyes, respiratory and urinary tract). The treatment may be performed in patients with malignant tumors, patients in the ICU, patients undergoing cytotoxic or immunosuppressive therapy, and the presence of other predisposing factors to the development of Candida;
• candidiasis of the mucous membranes, including the oral cavity and pharynx (including atrophic oral candidiasis associated with wearing dentures), esophagus, non-invasive bronchopulmonary candidiasis, candiduria, candidiasis of the skin; prevention of relapse of oropharyngeal candidiasis in patients with AIDS,
• genital candidiasis: vaginal candidiasis (acute and chronic recurrent), prophylactic use to reduce the frequency of recurrences of vaginal candidiasis (3 or more episodes per year); candidal balanitis;
• prevention of fungal infections in patients with malignancies who are predisposed to such infections as a result of chemotherapy with cytostatics or radiation therapy;
• fungal skin infections, including athlete’s foot, body, groin; tinea (colored) versicolor, onychomycosis; candidiasis of the skin;
• deep endemic mycoses, including coccidioidomycosis, paracoccidioidomycosis, sporotrichosis and histoplasmosis in patients with normal immune systems.

Contraindications

• Hypersensitivity to the drug (including other azole antifungal drugs in the anamnesis);
• concomitant use of terfenadine (against the background of constant use of fluconazole at a dose of 400 mg / day or more) or astemizole, as well as other drugs that extend the interval QT;
• children under 4 years of age.

With caution: hepatic and/or renal failure, rash associated with the use of fluconazole in patients with superficial fungal infection and invasive/systemic fungal infections, concomitant use of terfenadine and fluconazole at a dose of less than 400 mg / day, concomitant use of potentially hepatotoxic drugs, alcoholism, potentially proarrhythmogenic conditions in patients with multiple risk factors (organic heart disease, electrolyte imbalance, concomitant use of drugs that cause arrhythmias), pregnancy.

Side effects

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

Nervous system disorders: headache, dizziness, excessive fatigue, rarely-convulsions.

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

Allergic reactions: skin rash, rarely-erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), anaphylactoid reactions (including angioedema, facial edema, urticaria, pruritus of the skin).

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

Other services: rarely-impaired renal function, alopecia, hypercholesterolemia, hypertriglyceridemia, hypokalemia.

Interaction

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

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

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

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

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

Patients who are receiving high doses of theophylline or who are likely to develop theophylline intoxication should be monitored for early detection of symptoms of overdose of theophylline, since taking fluconazole leads to a decrease in the average rate of clearance of theophylline from plasma.

Concomitant use of fluconazole with terfenadine and cisapride has been associated with cases of adverse cardiac reactions, including paroxysms of ventricular tachycardia (torsades de points).

Concomitant administration of fluconazole and hydrochlorothiazide may increase the plasma concentration of fluconazole by 40%.

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

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

Increases the concentration of midazolam, and therefore increases the risk of psychomotor effects (most pronounced when using fluconazole inside, than IV).

Increases the concentration of tacrolimus, which increases the risk of nephrotoxic effects.

How to take it, course of administration and dosage

Inside.

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

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

For candidaemia, disseminated candidiasis and other invasive candida infections, the dose is 400 mg (8 capsules of 50 mg) on the first day, and then 200 mg (4 capsules of 50 mg) per day. In case of insufficient clinical efficacy, the dose of the drug can be increased to 400 mg (8 capsules of 50 mg) per day. The duration of therapy depends on the clinical efficacy.

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

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

For atrophic oral candidiasis associated with wearing dentures — 50 mg once a day for 14 days in combination with local antiseptic drugs for the treatment of the prosthesis.

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

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

When balanitis caused by Candida, fluconazole is administered orally once at a dose of 150 mg / day.

For the prevention of candidiasis, the recommended dose is 50-400 mg once a day, depending on the degree of risk of developing a fungal infection. For the prevention of candidiasis in patients with malignant neoplasms, the recommended dose of fluconazole is 150-400 mg once a day, depending on the degree of risk of fungal infection. If there is a high risk of generalized infection, for example, in patients with expected severe or long-term persistent neutropenia, the recommended dose is 400 mg / day. Fluconazole is prescribed a few days before the expected appearance of neutropenia; after an increase in the number of neutrophils more than 1 thousand/µl, treatment is continued for another 7 days.

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

With pityriasis versicolor — 300 mg (2 capsules of 150 mg) 1 time 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 the use of 50 mg 1 time a day for 2-4 weeks.

For onychomycosis, the recommended dose is 150 mg once a week. Treatment should be continued until the infected nail is replaced (uninfected nail regrowth). It normally takes 3-6 months and 6-12 months, respectively, for the nails to regrow on the fingers and feet.

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

In children, as with similar infections in adults, the duration of treatment depends on the clinical and mycological effect. In children, the drug should not be used in a daily dose that would exceed that of adults, i. e. no more than 400 mg / day. The drug is used daily 1 time a day.

Overdose

Symptoms: hallucinations, paranoid behavior.

Treatment: symptomatic — gastric lavage, forced diuresis. Hemodialysis for 3 hours reduces the plasma concentration by approximately 50%.

Special instructions

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

During treatment, it is necessary to monitor blood parameters, kidney and liver function. If you experience impaired renal and hepatic function, you should stop taking the drug.

In rare cases, the use of fluconazole was accompanied by toxic changes in the liver, including 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 effect of fluconazole was usually reversible; signs of it disappeared after discontinuation of therapy. If there are clinical signs of liver damage that may be associated with fluconazole, the drug should be discontinued.

Patients People with AIDS are more likely to develop severe skin reactions when using many medications. In cases where patients with a superficial fungal infection develop a rash and it is considered definitely associated with fluconazole, the drug should be discontinued. If a rash appears in patients with invasive / systemic fungal infections, they should be carefully monitored and discontinue fluconazole if bullous changes or erythema multiforme occur.

Caution should be exercised when taking fluconazole concomitantly with cisapride, rifabutin, or other drugs that are metabolized by the cytochrome P450 system.

Storage conditions

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

Active ingredient

Fluconazole

Conditions of release from pharmacies

By prescription

Dosage form

of the capsule

Purpose

For adults, Children as prescribed by a doctor, Children over 3 years of age

Indications

Fungus, Thrush

Weight

Weight: 14 gr.