Fluconazole-OBL, 150 mg capsules 2 pcs

Fluconazole, a member of the triazole antifungal class, is a potent selective inhibitor of the fungal 14-a-demethylase enzyme.

The drug prevents conversion of lanosterol into ergosterol, the main component of cell membranes of fungi.

The drug is effective against opportunistic mycoses, including those caused by Candida spp. (Candida albicans, Candida tropicalis), Cryptococcus neoformans, Microsporum spp.

Fluconazole activity has also been shown in models of endemic mycoses, including infections caused by Blastomyces dermatitidis, Coccidioides immitis and Histoplasma capsulatum.

Indications

Cryptococcosis, including cryptococcal meningitis and other localized infections (e.g., lung, skin), including in patients with normal immune response and in AIDS patients, transplant recipients and patients with other forms of immune deficiency; maintenance therapy to prevent relapse of cryptococcosis in AIDS patients.

Generalized candidiasis, including candidemia, disseminated candidiasis and other forms of invasive candidiasis infections such as peritoneal, endocardial, eye, respiratory and urinary tract infections, including in patients with malignant tumors, in the ICU and receiving cytotoxic or immunosuppressive agents, and in patients with other factors that predispose to candidiasis development.

Mucosal candidiasis, including oral and pharyngeal mucosa, esophagus, non-invasive bronchopulmonary infections, candiduria, dermal-mucosal and chronic atrophic oral candidiasis (associated with the wearing of dentures), including in patients with normal and abnormal oral candidiasis.including in patients with normal and suppressed immune function; prevention of relapse of oropharyngeal candidiasis in patients with AIDS.

Genital candidiasis; acute or recurrent vaginal candidiasis; prophylaxis to reduce the frequency of recurrent vaginal candidiasis (3 or more episodes per year); candidal balanitis.

Skin mycoses, including mycoses of the feet, body, inguinal area, pityriasis, onychomycosis and cutaneous candida infections.

Deep endemic mycoses in patients with normal immunity, coccidioidomycosis, paracoccidioidomycosis, sporotrichosis and histoplasmosis.

The prevention of fungal infections in patients with malignancies predisposed to develop such infections as a result of cytotoxic chemotherapy or radiation therapy.

Active ingredient

Composition

1 capsule contains:

Active ingredient:

fluconazole 150mg.

Associates:

corn starch,

povidone (polyvinylpyrrolidone low molecular weight),

calcium stearate.

Capsules are hard gelatin:

titanium dioxide,

patent blue dye,

p> gelatin,

preservatives – methyl hydroxybenzoate,

propyl hydroxybenzoate.

How to take, the dosage

Individual. It is intended for oral administration.

For adults, depending on the indication, treatment regimen and clinical situation, the daily dose is 50-400 mg, the frequency of administration is 1 time/day.

In children, the dose is 3-12 mg/kg/day and the frequency of use is 1 time/day.

In patients with impaired renal function the dose of fluconazole is reduced depending on CKD.

The duration of treatment depends on the clinical and mycological effect.

Interaction

In concomitant use with warfarin, fluconazole increases prothrombin time (by 12%), in connection with which bleeding may occur (hematoma, bleeding from the nose and gastrointestinal tract, hematuria, melena). In patients receiving coumarin anticoagulants prothrombin time should be constantly monitored.

Fluconazole significantly increases midazolam concentration and psychomotor effects after oral administration of midazolam, and this effect is more pronounced after fluconazole oral administration than when it is used intravenously. If concomitant therapy with benzodiazepines is necessary, patients taking fluconazole should be monitored to reduce the benzodiazepine dose accordingly.

In concomitant use of fluconazole and cisapride, adverse cardiac reactions, including ventricular fibrillation/tripping (pirouette-type arrhythmia) are possible. The use of fluconazole in dose 200 mg once daily and cisapride in dose 20 mg four times daily causes significant increase of plasma concentration of cisapride and prolongation of QT interval on ECG. Simultaneous administration 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 concentration of cyclosporine. However, no changes in cyclosporine concentrations were observed in bone marrow recipients when fluconazole was administered repeatedly at a dose of 100 mg/day. When concomitant use of fluconazole and cyclosporine it is recommended to monitor the concentration of cyclosporine in blood.

Multiple use of hydrochlorothiazide concomitantly with fluconazole leads to an increase in fluconazole plasma concentration by 40%. This increase does not require modification of the fluconazole dosing regimen in patients receiving concomitant diuretics, but this should be considered.

. No significant effects on hormone levels have been identified in concomitant administration of the combined oral contraceptive with fluconazole in a dose of 50 mg, while the AUCs of ethinylestradiol and levonorgestrel increase by 40% and 24% respectively when taking fluconazole 200 mg daily, and the AUCs of ethinylestradiol and norethindrone increase by 24% and 13% respectively when taking fluconazole 300 mg once a week. Thus, repeated use of fluconazole at the indicated doses is unlikely to affect the efficacy of the combined oral contraceptive.

The concomitant use of fluconazole and phenytoin may be accompanied by clinically significant increases in phenytoin concentrations. In this combination, phenytoin concentrations should be monitored and the dose should be adjusted accordingly to ensure therapeutic serum concentrations.

The concomitant use of fluconazole and rifabutin may lead to increased serum concentrations of the latter. In concomitant use of fluconazole and rifabutin there have been described cases of uveitis. Patients receiving rifabutin and fluconazole concomitantly should be monitored closely.

Special Instructions

Caution is used with caution in patients with hepatic dysfunction when using fluconazole, with the occurrence of rash on fluconazole in patients with superficial fungal infection and invasive/systemic fungal infections, with the simultaneous use of terfenadine and fluconazole at a dose less than 400 mg/day, in potentially proarrhythmic conditions in patients with multiple risk factors (organic heart disease, electrolyte imbalance and concomitant therapy that contributes to the development of such disorders).

Hepatotoxic effects of fluconazole were usually reversible; signs of these effects disappeared after discontinuation of therapy. Patients with impaired liver function during treatment with fluconazole should be monitored for signs of more serious liver damage. If there are clinical signs or symptoms of liver damage that may be associated with fluconazole, it should be discontinued.

AIDS patients are more prone to develop severe skin reactions with many drugs. If a patient treated for a superficial fungal infection presents with a rash that can be associated with fluconazole use, it should be discontinued. If rash appears in patients with invasive/systemic fungal infections, they should be closely monitored and fluconazole should be discontinued if bullous lesions or erythema multiforme appear.

The concomitant use of fluconazole in doses less than 400 mg/day and terfenadine should be monitored closely.

When using fluconazole, QT interval prolongation and ventricular fibrillation/rattling have been observed very rarely in patients with multiple risk factors, such as organic heart disease, electrolyte disturbances, and concomitant therapy contributing to these disorders.

The therapy can be started before the results of culture and other laboratory tests. However, anti-infective therapy should be adjusted accordingly when the results of these tests become available.

There have been reports of cases of superinfections caused by Candida strains other than Candida albicans, which often do not show sensitivity to fluconazole (e.g., Candida krusei). Alternative antifungal therapy may be necessary in such cases.

Contraindications

Simultaneous use of terfenadine during multiple use of fluconazole at a dose of 400 mg/day or more;

concomitant use of cisapride; hypersensitivity to fluconazole;

hypersensitivity to azole derivatives with a similar structure to fluconazole;

lactation; children under 3 years of age (for this dosage form).

Side effects

Nervous system disorders: headache, dizziness, seizures, change in taste.

Digestive system disorders: abdominal pain, diarrhea, flatulence, nausea, dyspepsia, vomiting, hepatotoxicity (including rare cases with lethal outcome), increased levels of alkaline phosphate, bilirubin, serum levels of aminotransferases (ALT and AST), liver function disorders, hepatitis, hepatocellular necrosis, jaundice.

Cardiovascular system: prolongation of the QT interval on ECG, ventricular fibrillation/tripping.

Dermatological reactions: rash, alopecia, exfoliative skin disorders including Stevens-Johnson syndrome and toxic epidermal necrolysis.

Hematopoietic system disorders: leukopenia, including neutropenia and agranulocytosis, thrombocytopenia.

Metabolism disorders: increase in plasma cholesterol and triglyceride levels, hypokalemia.

Allergic reactions: anaphylactic reactions (including angioedema, facial edema, urticaria, pruritus).

Overdose

Symptoms: nausea, vomiting, diarrhea, in severe cases seizures, hallucinations, paranoid behavior may be noted.

Treatment: symptomatic, gastric lavage; since fluconazole is excreted by the kidneys, forced diuresis is recommended. Hemodialysis within 3 hours reduces concentration in plasma by 2 times.

Similarities