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Description of the drug FLUCONAZOLE

When used simultaneously with warfarin, fluconazole increases prothrombin time (by 12%), and therefore bleeding may develop (hematomas, bleeding from the nose and gastrointestinal tract, hematuria, melena). In patients receiving coumarin anticoagulants, prothrombin time must be constantly monitored.

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 benzodiazepine therapy is necessary, patients taking fluconazole should be monitored for an appropriate benzodiazepine dose reduction.

With the simultaneous use of fluconazole and cisapride, adverse reactions from the heart are possible, incl. ventricular fibrillation/flutter (ari). The use of fluconazole at a dose of 200 mg 1 time / day and cisapride at a dose of 20 mg 4 times / day leads to a marked increase in plasma concentrations of cisapride and an increase in the QT interval on the ECG. Concomitant use of cisapride and fluconazole is contraindicated.

In patients after kidney transplantation, the use of fluconazole at a dose of 200 mg/day leads to a slow increase in cyclosporine concentrations. However, with repeated doses of fluconazole at a dose of 100 mg/day, no changes in cyclosporine concentrations were observed in bone marrow recipients. When using fluconazole and cyclosporine concomitantly, it is recommended to monitor the concentration of cyclosporine in the blood.

Repeated use of hydrochlorothiazide simultaneously with fluconazole leads to an increase in plasma concentrations of fluconazole by 40%. An effect of this magnitude does not require a change in the fluconazole dosage regimen in patients receiving concomitant diuretics, but this should be taken into account.

With the simultaneous use of a combined oral contraceptive with fluconazole at a dose of 50 mg, no significant effect on hormone levels has been established, while with daily intake of 200 mg of fluconazole, the AUC of ethinyl estradiol and levonorgestrel increases by 40% and 24%, respectively, and when taking 300 mg of fluconazole 1 time per day week - AUC of ethinyl estradiol and norethindrone increase 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.

Concomitant use of fluconazole and phenytoin may be accompanied by a clinically significant increase in phenytoin concentrations. With this combination, phenytoin concentrations should be monitored and the dose adjusted accordingly to ensure therapeutic serum concentrations.

Concomitant use of fluconazole and rifabutin may lead to increased serum concentrations of the latter. Cases of uveitis have been described with the simultaneous use of fluconazole and rifabutin. Patients receiving rifabutin and fluconazole concomitantly should be monitored closely.

The simultaneous use of fluconazole and rifampicin leads to a decrease in AUC by 25% and the duration of T1/2 of fluconazole by 20%. In patients concomitantly taking rifampicin, the advisability of increasing the dose of fluconazole must be considered.

Fluconazole, when taken simultaneously, leads to an increase in T1/2 of oral sulfonylurea drugs (chlorpropamide, glibenclamide, glipizide and tolbutamide). In patients with diabetes mellitus, fluconazole and oral sulfonylureas can be prescribed together, but the possibility of hypoglycemia should be taken into account.

The simultaneous use of fluconazole and tacrolimus leads to an increase in plasma concentrations of the latter. Cases of nephrotoxicity have been described. Patients with this combination should be carefully monitored.

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 at doses of 400 mg/day and above causes a significant increase in the concentration of terfenadine in 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.

When used simultaneously with fluconazole at a dose of 200 mg for 14 days, the average rate of plasma clearance of theophylline is reduced by 18%. When prescribing fluconazole to patients taking high doses of theophylline or to patients at increased risk of developing theophylline toxicity, monitor for symptoms of theophylline overdose and, if necessary, adjust therapy accordingly.

When used simultaneously with fluconazole, an increase in zidovudine concentrations is observed, which is likely due to 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.

When zidovudine 200 mg every 8 hours for 7 days was used in HIV-infected patients with or without fluconazole 400 mg/day with an interval of 21 days between the two regimens, a significant increase in zidovudine AUC was found (74%) when used simultaneously with fluconazole. Patients receiving this combination should be monitored for side effects of zidovudine.

The simultaneous use of fluconazole with astemizole or other drugs whose metabolism is carried out by isoenzymes of the cytochrome P450 system may be accompanied by an increase in serum concentrations of these drugs. Patients with such combinations should be carefully monitored.

Pharmacodynamics

Antifungal agent. A triazole derivative exhibits an antifungal effect by blocking the biosynthesis of ergosterol in the cell membrane of fungi. The “target” for the action of the drug is the enzyme 14-α-demethylase.

14-α-demethylase is part of a group of enzymes known collectively as cytochrome P450. All enzymes of the cytochrome P450 group contain hematinic iron-containing pigment. Fluconazole binds to the iron atom of the hematin group and inactivates 14-α-demethylase, which leads to disruption of ergosterol synthesis and accumulation of lanosterol and other sterols. Their inclusion in the membrane instead of ergosterol significantly disrupts the structure and function of the fungal cell membrane.

A decrease in ergosterol synthesis, as well as the accumulation of 14α-methylsterols, destroys the tightly packed acyl chains of fungal membrane phospholipids. Destabilization of the fungal membrane leads to dysfunction of membrane enzymes, including those involved in the electron transport chain, and ultimately to cell death.

Used for systemic mycoses: candidiasis, cryptococcosis, blastomycosis, histoplasmosis, coccidioidomycosis, as well as dermatomycosis. The relatively low toxic profile and high penetration into the cerebrospinal fluid make fluconazole the drug of choice for systemic candidiasis and cryptococcal meningitis. Because of complications associated with intrathecal amphotericin B, fluconazole is the first-line drug for coccidioidal meningitis. Although fluconazole is active against the causative agents of blastomycosis, histoplasmosis, and sporotrichosis, it is inferior in effectiveness against the causative agents of these infections to itraconazole. Fluconazole is not effective against aspergillosis.

Side effects

Side effects are possible when using the drug Fluconazole

From the immune system: hypersensitivity (cross with all azoles), other anaphylactic, anaphylactoid and allergic reactions (including Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria).
From the nervous system: headache, dizziness, peripheral neuropathy, paresthesia, excessive fatigue, rarely - convulsions.
From the digestive system: loss of appetite, dryness of the oral mucosa, 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 alkaline phosphatase activity, hepatocellular necrosis), including severe.
From the hematopoietic organs: rarely - leukopenia, thrombocytopenia (bleeding, petechiae), neutropenia, agranulocytosis.
From the cardiovascular system: increased duration of the QT interval, ventricular fibrillation/flutter, torsades de pointes.
Metabolism: hypercholesterolemia, hypertriglyceridemia, hypokalemia, hyperglycemia.
From the musculoskeletal system: myalgia.
Other: weakness, asthenia, peripheral edema, neutropenia, itching, pulmonary edema, fever, excessive sweating, vertigo.

Indications for use

Indications for the use of Fluconazole capsules are:

Cryptococcal infection, including specific damage to the membranes of the brain (cryptococcal meningitis) in patients with immunodeficiency or with a normal state of functional immune activity.
A severe form of candidiasis with generalization of the infectious process and damage to a significant amount of tissue (mucous membranes of various organs, skin, peritoneum, endocardium, eyes, respiratory and urinary tracts). In most cases, the infection develops against the background of a pronounced decrease in the functional activity of the immune system during malignant neoplasms, treatment with cytostatics, immunosuppressants, as well as in patients who have been in the intensive care unit for a long time.
Localized candidiasis, developing on the mucous membranes of the oral cavity and upper digestive tract, on the structures of the urogenital tract - the drug in dosage form for systemic use is used in case of insufficient effectiveness of ointment or cream for topical use.
Dermatomycosis, which is localized on the skin of the feet, torso, and groin area.
Pityriasis (multi-colored) lichen.
Fungal infection of the nail plates (onychomycosis).
Deep endemic mycoses, which may include paracoccidioidomycosis, coccidioidomycosis, histoplasmosis in patients with normal functional immune activity.

The drug is also used to prevent the development of fungal infections in patients with normal or impaired immunity.