Diflucan caps. 150mg No. 1

Release form, composition and packaging

Hard gelatin capsules, No. 1, with a turquoise lid and body, marked with the Pfizer" and "FLU-150" logo in black

the contents of the capsules are white to pale yellow powder.

1 caps.

fluconazole 150 mg

lactose - 149.123 mg, corn starch - 49.5 mg, colloidal silicon dioxide - 0.352 mg, magnesium stearate - 3.173 mg, sodium lauryl sulfate - 0.352 mg.

The composition of the capsule shell: titanium dioxide (E171) - 1.47%, patented blue dye (E131) - 0.03%, gelatin - up to 100%.

Ink composition: shellac glaze - 63%, black iron oxide (E172) - 25%, N-butyl alcohol - 8.995%, industrial methylated alcohol 74ОР - 2%, soy lecithin - 1%, antifoam component DC1510 - 0.005%.

1 PC.

- blisters (1) - cardboard packs.

4 things.

- blisters (1) - cardboard packs.

4 things.

- blisters (3) - cardboard packs.

pharmachologic effect

Antifungal drug of the triazole series, is a potent selective inhibitor of sterol synthesis in the fungal cell.

The activity of fluconazole in vitro and in clinical infections has been shown against most of the following microorganisms: Candida albicans, Candida glabrata (many strains are moderately sensitive), Candida parapsilosis, Candida tropicalis, Cryptococcus neoformans.

Fluconazole has been shown to be active against the following microorganisms in vitro, but the clinical significance of this is unknown: Candida dubliniensis, Candida guilliermondii, Candida kefyr, Candida lusitaniae.

Oral and intravenous administration fluconazole was active in various models of fungal infections in animals. Demonstrated the activity of the drug in opportunistic mycoses, incl. caused by Candida spp. (including generalized candidiasis in animals with reduced immunity), Cryptococcus neoformans (including intracranial infections), Microsporum spp. and Trychoptyton spp. The activity of fluconazole was also established 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.

Fluconazole is highly specific for cytochrome P450 dependent fungal enzymes.

Fluconazole therapy at 50 mg / day for up to 28 days does not affect the plasma testosterone concentration in men or the steroid concentration in women of childbearing age.

Fluconazole at a dose of 200-400 mg / day had no clinically significant effect on the levels of endogenous steroids and their response to ACTH stimulation in healthy male volunteers.

Mechanisms for the development of resistance to fluconazole

Resistance to fluconazole can develop in the following cases: a qualitative or quantitative change in the enzyme that is the target of fluconazole (lanosteril 14-alpha-demethylase), reduced access to the target of fluconazole, or a combination of these mechanisms.

Point mutations in the ERG11 gene encoding the target enzyme lead to a modification of the target and a decrease in the affinity for azoles.

An increase in the expression of the ERG11 gene leads to the production of high concentrations of the target enzyme, which creates the need to increase the concentration of fluconazole in the intracellular fluid to suppress all enzyme molecules in the cell.

The second significant mechanism of resistance is the active elimination of fluconazole from the intracellular space through the activation of two types of transporters involved in the active elimination (efflux) of drugs from the fungal cell.

These transporters include the main mediator encoded by the MDR (multidrug resistance) genes and the ATP-binding cassette transporter superfamily encoded by the CDR genes (genes for resistance of Candida spp. Fungi to azole antimycotics).

Overexpression of the MDR gene leads to resistance to fluconazole, while overexpression of the CDR genes

Name ENG

DIFLUCAN

Clinical and pharmacological group

Antifungal drug

ATX code

Fluconazole

Dosage

150mg

Structure

Each capsule contains: active substance: fluconazole 150 mg

excipients: lactose 149.123 mg, corn starch 49.5 mg, colloidal silicon dioxide 0.352 mg, magnesium stearate 3.173 mg, sodium lauryl sulfate 0.352 mg

capsule shell: titanium dioxide (E171) 1.47%, patented blue dye (E 131) 0.03%, gelatin up to 100%.

Ink for marking capsules 50 mg, 100 mg and 150 mg: shellac glaze 63%, iron oxide black (E172) 25%, N-butyl alcohol 8.995%, industrial methylated alcohol 74 OP 2%, soy lecithin 1%, antifoam component DC 1510 0.005%.

Indications

cryptococcosis, including cryptococcal meningitis and infections at other sites (eg, lungs, skin), incl.

in patients with a normal immune response and in AIDS patients, organ transplant recipients and patients with other forms of immunodeficiency

maintenance therapy to prevent relapse of cryptococcosis in AIDS patients

generalized candidiasis, including candidemia, disseminated candidiasis and other forms of invasive candidiasis, such as infections of the peritoneum, endocardium, eyes, respiratory and urinary tract, incl.

in patients with malignant tumors in intensive care units, patients receiving cytotoxic or immunosuppressive drugs, as well as in patients with other factors predisposing to the development of candidiasis

candidiasis of the mucous membranes, including the mucous membranes of the oral cavity and pharynx, esophagus, non-invasive bronchopulmonary infections, candiduria, mucocutaneous and chronic atrophic oral candidiasis (associated with wearing dentures), incl.

in patients with normal and suppressed immune function

prevention of recurrence of oropharyngeal candidiasis in AIDS patients

genital candidiasis

acute or recurrent vaginal candidiasis

prevention in order 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 tumors predisposed to the development of such infections as a result of cytotoxic chemotherapy or radiation therapy

mycoses of the skin, including mycoses of the feet, body, groin, pityriasis versicolor, onychomycosis and skin candidal infections

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

Storage conditions and periods

At a temperature not higher than 30 degrees.

Expiration date: 5 years

INN / Active ingredient

fluconazole

Contraindications

concomitant use of cisapride

simultaneous use of terfenadine during repeated use of fluconazole at a dose of 400 mg / day or more

hypersensitivity to fluconazole, other components of the drug, or azole substances with a structure similar to fluconazole.

The drug is prescribed with caution in case of violations of liver function indicators against the background of the use of fluconazole, with the appearance of a rash against the background of the use of fluconazole in patients with superficial fungal infection and invasive / systemic fungal infections, while using terfenadine and fluconazole at a dose of less than 400 mg / day, with the potential proarrhythmic conditions in patients with multiple risk factors (organic heart disease, electrolyte imbalance and concomitant therapy that promotes the development of such disorders).

Specifications

Category

Thrush

Scope of the drug

Gynecology

Release form

Capsules

Manufacturer country

France

Package quantity, pcs

one

Minimum age from

From birth

Way of introduction

Through the mouth

Vacation conditions

Without recipe

Brand name

Pfizer

The amount of the dosage form in the primary package

1 PC.

Primary packaging type

Blister

Type of consumer packaging

Pack of cardboard

Pharmaco-therapeutic group

Antifungal agent

Anatomical and therapeutic characteristics

J02AC01 Fluconazole

Dosage form

Capsules

Dosage (volume) of the substance in the preparation

fluconazole 150 mg

Expiration date in days

1825

The target audience

Children

Package weight, g

5

Mode of application

:

Inside.

In acute vaginal candidiasis, candidal balanitis, the drug is used 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 every three days - only 3 doses (on the 1st, 4th and 7th day), then a maintenance dose of 150 mg once a week.

A maintenance dose can be used for up to 6 months.

Information on technical characteristics, delivery set, country of manufacture "