Fluconazole

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Available since: 2019-09-19

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Clinical Pharmacology

Antifungal agent, has a highly specific effect, inhibiting the activity of enzymes of fungi, dependent on cytochrome P450. Blocks the conversion of lanosterol of fungal cells to ergosterol; increases the permeability of the cell membrane, violates its growth and replication.

Fluconazole, being highly selective for cytochrome P450 fungi, almost does not inhibit these enzymes in the human body (in comparison with itraconazole, clotrimazole, econazole and ketoconazole, to a lesser extent, it inhibits cytochrome P450-dependent oxidative processes in human liver microsomes). Does not possess antiandrogenic activity.

Active in opportunistic mycoses, incl. caused by candida spp. (including generalized forms of candidiasis in the presence of immunosuppression), Cryptococcus neoformans and Coccidioides immitis (including meningitis and encephalitis), Microsporum spp. and Trichophyton spp; with endemic mycoses caused by Blastomyces dermatidis, Histoplasma capsulatum (including immunosuppression).

Indications

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

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

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

- 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);

- Candida balanitis;

- prevention of fungal infections in patients with malignant neoplasms, which 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, groin;

- scaly (versicolor versicolor) versicolor;

- onychomycosis;

- skin candidiasis;

- deep endemic mycoses, including coccidiomycosis and histoplasmosis, in patients with normal immunity.

Composition

fluconazole 150 mg

excipients: lactose monohydrate; pregelatinized starch; silica colloidal anhydrous; magnesium stearate; sodium lauryl sulfate

the composition of the capsule shell for 150 mg: titanium dioxide E-171; sunset dye yellow T-110; dye "Ponso-4R" E-124; gelatin

Fluconazole is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Fluconazole	Vertex	Russia	capsules
Fluconazol-OBL	Obolensky OP	Russia	capsules
Fluconazole-Teva	Teva	Israel	capsules
Diflucan	Pfizer	USA	capsules
Flucostat	Pharmstandard	Russia	capsules
Fluconazole	Nizhpharm	Russia	capsules
Mycomax	Zentiva KS	Czech	capsules
Mycosyst®	Gedeon Richter	Hungary	capsules
Diflucan	Pfizer	USA	powder
Diflucan	Pfizer	USA	solution

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Dosage and Administration

For oral use.

Adults and children over 15 years of age (body weight over 50 kg) for cryptococcal meningitis and cryptococcal infections of other sites on the first day are usually prescribed 400 mg (8 capsules 50 mg), and then continue treatment at a dose of 200 mg (4 capsules 50 mg each ) - 400 mg (8 capsules 50 mg) 1 time / day. The duration of treatment for cryptococcal infections depends on the clinical efficacy confirmed by mycological examination; with cryptococcal meningitis, the treatment should be at least 6-8 weeks.

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

For candidemia, disseminated candidiasis and other invasive candidal infections, in the first 24 hours the dose is 400 mg (8 capsules 50 mg each), and then 200 mg (4 capsules 50 mg each) / day. With insufficient clinical efficacy, the dose of the drug can be increased to 400 mg (8 capsules of 50 mg) / day. The duration of therapy depends on the clinical efficacy of the drug (100% of the recommended dose).

When QA from 11 to 50 ml / min, 50% of the recommended dose is applied or the usual dose 1 time in 2 days.

Fluconazole is administered to patients with impaired renal function as follows.

Creatinine clearanceInterval / daily dose of more than 40 ml / min24 h (normal dosing regimen) 21-40 ml / min 48 h (1 time in two days) or half the usual daily dose (1 time in 24 h) 10-20 ml / min 72 h (1 once in three days) or 1/2 of the usual daily dose (1/3 per 24 h)

Patients on hemodialysis, a single dose of the drug is used after each session of hemodialysis.

Adverse reactions

The adverse events presented below are listed depending on the anatomical and physiological classification and frequency of occurrence. The frequency of occurrence is determined as follows: often - more than 1%; infrequently - 0.1-1%; rarely 0.01–0.1%; very rarely - less than 0.01%.

On the part of the digestive system: loss of appetite, change in taste, nausea, diarrhea, flatulence, abdominal pain, vomiting, abdominal pain; rarely, liver dysfunction (jaundice, hepatocellular necrosis, hyperbilirubinemia, increased alanine aminotransferase (ALT) activity, aspartate aminotransferase (ACT) and alkaline phosphatase (alkaline phosphatase), hepatitis, hepatonecrosis), including heavy

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

From the side of blood formation organs: rarely - leukopenia, thrombocytopenia (hemorrhage, petechiae), neutropenia, agranulocytosis.

Allergic reactions: skin rash; rarely, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), anaphylactoid reactions (including angioedema, swelling of the face, urticaria, itchy skin).

Since the cardiovascular system: an increase in the duration of the QT interval, ventricular fibrillation / flutter.

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

Contraindications

- hypersensitivity to the drug (including to other azole antifungal drugs in history);

- simultaneous administration of terfenadine (against the background of continuous administration of fluconazole at a dose of 400 mg / day or more) or astemizole, as well as other drugs that extend the QT interval;

- children's age up to 4 years.

Carefully

Hepatic and / or renal failure, the appearance of a rash on the background of fluconazole use in patients with surface fungal infection and invasive / systemic fungal infections, simultaneous administration of potentially hepatotoxic drugs, potentially pro-arrhythmic conditions in patients with multiple risk factors (organic heart disease, electrolyte imbalance , simultaneous administration of drugs that cause arrhythmias), pregnancy.

Drug interactions

When fluconazole is used with warfarin, the prothrombin time increases (by an average of 12%). Recommended to control prothrombin time when fluconazole is combined with coumarin anticoagulants.

Fluconazole increases T1 / 2 from the plasma of oral hypoglycemic agents - sulfonylurea derivatives (chlorpropamide, glibenclamide, glipizide, tolbutamide) in healthy people. The combined use of fluconazole and oral hypoglycemic agents in patients with diabetes mellitus is allowed, but the physician must keep in mind the possibility of the development of hypoglycemia.

The simultaneous use of fluconazole and phenytoin can lead to an increase in plasma phenytoin concentration to a clinically significant extent. Therefore, if necessary, the joint use of these drugs is necessary to monitor the concentration of phenytoin with the correction of its dose in order to maintain the concentration of the drug within the therapeutic interval.

The combination with rifampicin reduces AUC by 25% and shortens T1 / 2 of fluconazole from plasma by 20%. Therefore, patients receiving rifampicin at the same time, it is advisable to increase the dose of fluconazole.

It is recommended to control the concentration of cyclosporine in the blood of patients receiving fluconazole, since with 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 plasma cyclosporine concentration.

Patients who receive high doses of theophylline or who are likely to develop theophylline intoxication should be monitored to identify symptoms of an overdose of theophylline, because simultaneous reception of fluconazole leads to a decrease in theophylline clearance from plasma.

There are reports of the interaction of fluconazole and rifabutin, accompanied by an increase in the serum concentration of the latter. With the simultaneous use of fluconazole and rifabutin, cases of uveitis are described. It is necessary to carefully monitor patients who simultaneously receive rifabutin and fluconazole.

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

With the simultaneous use of fluconazole, terfenadine and cisapride, cases of unwanted heart reactions, including pirouette arrhythmia, are described.

The simultaneous use of fluconazole and hydrochlorothiazide can lead to an increase in the concentration of fluconazole by 40%.

Increases the concentration of midazolam, and therefore increases the risk of psychomotor effects (more pronounced with the use of fluconazole orally than intravenously).

Increases the concentration of tacrolimus, and therefore increases the risk of nephrotoxic action.

Pregnancy and Lactation

The use of the drug in pregnant women is impractical, with the exception of severe or life-threatening forms of fungal infections, when the potential benefit from the use of fluconazole for the mother far exceeds the risk to the fetus.

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

Special instructions

Treatment should continue until clinical and hematologic remission. Premature discontinuation of treatment leads to relapse.

In rare cases, the use of fluconazole was accompanied by toxic changes in the liver, including fatal, mainly in patients with serious comorbidities. In the case of hepatotoxic effects, are associated with fluconazole, they are not markedly dependent on the total daily dose, duration of therapy, sex and age of the patient. The hepatotoxic effect of fluconazole has usually been reversible; his symptoms disappeared after cessation of therapy.If clinical signs of liver damage appear that may be associated with fluconazole, the drug should be withdrawn.

AIDS patients are more likely to develop severe skin reactions with the use of many drugs. In cases where a rash develops in patients with a surface fungal infection, and it is regarded as definitely associated with fluconazole, the drug should be discontinued. When a rash appears in patients with invasive systemic fungal infections, they should be carefully monitored and fluconazole should be canceled when a bullous change or erythema multiforme occurs.

Care must be taken when taking fluconazole with cisapride, rifabutin or other drugs metabolized by the cytochrome P450 system.