Mycosist caps. 150mg # 1

Dosage form

capsules

Structure

Active substance:

Fluconazole 150 mg

Excipients:

Colloidal silicon dioxide 0.9 mg, Magnesium stearate 3.6 mg, Talc 9.9 mg, Povidone 10.8 mg, Corn starch 36.3 mg, Lactose (anhydrous) 148.5 mg.

Composition of a hard gelatin capsule:

Lower part: Titanium dioxide Col.

I. 77891, E 171 2.0%, Gelatin up to 100%.

Upper part: Indigocarmine Tsv.

I. 73015, E 132 0.2513%, Titanium dioxide Tsv.

I. 77891, E 171 1.5%, Gelatin up to 100%.

pharmachologic effect

Fluconazole, a representative of the class of triazole derivatives, is a selective inhibitor of sterol synthesis in the fungal cell.

Blocks the transformation of fungal lanosterol into ergosterol

increases the permeability of the cell membrane.

Fluconazole, being highly selective for cytochrome P450 of fungi, practically does not inhibit the cytochrome P450 system in the human body (in comparison with itraconazole, clotrimazole, econazole and ketoconazole, to a lesser extent inhibits oxidative processes in human liver microsomes dependent on cytochrome P450).

Does not possess androgenic activity.

The drug is active in mycoses caused by Candida spp., Cryptococcus neoformans, Microsporum spp., Trichophyton spp., Blastomyces dermatidis, Coccidioides immitis and Histoplasma capsulatum.

Pharmacokinetics

After oral administration, fluconazole is well absorbed, its bioavailability is 90%.

The maximum concentration (Cmax) after oral administration on an empty stomach of 150 mg is achieved after 0.5-1.5 hours and is 90% of the plasma concentration when administered intravenously at a dose of 2.5-3.5 mg / kg.

Simultaneous food intake does not affect the absorption of the drug taken orally.

Plasma concentrations are directly proportional to the dose.

90% - I equilibrium concentration is achieved by 4-5 days of drug treatment (when taken 1 time per day).

Application on the first day of a dose 2 times higher than the usual daily dose, allows you to achieve a plasma concentration of fluconazole equal to 90% of the value of the equilibrium concentration by the second day.

The apparent volume of distribution approaches the total water content in the body.

Plasma protein binding - 11-12%.

Fluconazole penetrates well into all body fluids.

In the stratum corneum of the epidermis, dermis and sweat fluid, high concentrations are achieved, which exceed serum levels.

After oral administration of 150 mg on day 7, the concentration in the stratum corneum of the skin is 23.4 μg / g, and 1 week after taking the second dose - 7.1 μg / g

concentration in nails after 4 months of application at a dose of 150 mg once a week - 4.05 μg / g in healthy and 1.8 μg / g in affected nails.

The concentration of the drug in saliva, sputum, breast milk, joint and peritoneal fluid is similar to its concentration in blood plasma.

In patients with fungal meningitis, the content of fluconazole a in the cerebrospinal fluid reaches 80% of its plasma concentration.

Constant values ​​in vaginal secretions are reached 8 hours after oral administration and are kept at this value for at least 24 hours. It is an inhibitor of the CYP2C9 isoenzyme in the liver. Pharmacokinetics of fluconazole significantly depends on the functional state of the kidneys, with an inverse relationship between T1 / 2 and CC.

The half-life (T1 / 2) of fluconazole is about 30 hours. Fluconazole is excreted mainly by the kidneys

approximately 80% of the administered dose is excreted by the kidneys unchanged, 11% - in the form of metabolites.

Fluconazole clearance is proportional to creatinine clearance.

Fluconazole metabolites were not found in the peripheral blood.

After hemodialysis for 3 hours, the plasma concentration of fluconazole is reduced by 50%.

Side effects

From the digestive system: nausea, abdominal pain, diarrhea, flatulence.

From the side of the central nervous system: headache, dizziness.

Allergic reactions: skin rash, anaphylactic reactions.

Selling features

prescription

Special conditions

Fluconaso

Name ENG

MYCOSYST

Clinical and pharmacological group

Antifungal drug

ATX code

Fluconazole

Dosage

150mg

Structure

Active ingredient: Fluconazole 150 mg.

Excipients: Colloidal silicon dioxide 0.9 mg, Magnesium stearate 3.6 mg, Talc 9.9 mg, Povidone 10.8 mg, Corn starch 36.3 mg, Lactose (anhydrous) 148.5 mg.

Composition of a hard gelatin capsule: Lower part: Titanium dioxide Col.

I. 77891, E 171 2.0%, Gelatin up to 100%.

Upper part: Indigocarmine Tsv.

I. 73015, E 132 0.2513%, Titanium dioxide Tsv.

I. 77891, E 171 1.5%, Gelatin up to 100%.

Indications

Cryptococcosis cryptococcal meningitis

cryptococcal infections of the lungs and skin

cryptococcal sepsis

prevention of recurrence of cryptococcosis in AIDS patients

with organ transplantation or other cases of immunodeficiency

generalized candidiasis candidemia, disseminated candidiasis and other forms of invasive candidiasis infections (infections of the abdominal cavity, endocardium, eyes, respiratory and urinary tract), incl.

in patients receiving a course of cytostatic or immunosuppressive therapy, as well as in the presence of other factors predisposing to the development of candidiasis, treatment and prevention

candidiasis of the mucous membranes of the oral cavity, incl.

atrophic candidiasis of the oral cavity associated with wearing dentures, pharynx, esophagus and non-invasive bronchopulmonary infections, candiduria

genital vaginal candidiasis (acute or chronic recurrent form)

candidal balanitis (capsules)

prevention of fungal infections in patients with malignant neoplasms who are predisposed to such infections as a result of chemotherapy with cytostatics or radiation therapy

prevention of recurrence of oropharyngeal candidiasis in AIDS patients

mycoses of the skin, including mycoses of the trunk, groin

capsules: pityriasis versicolor, onychomycosis, mycoses of the feet

deep endemic mycoses, including coccidioidosis, paracoccidioidosis and histoplasmosis in patients with normal immunity.

Storage conditions and periods

At a temperature not higher than 30 degrees.

Expiration date: 5 years

INN / Active ingredient

Fluconazole

Contraindications

Hypersensitivity to fluconazole, other components of the drug or other azole compounds similar in structure

simultaneous use of terfenadine (against the background of constant intake of fluconazole at a dose of 400 mg / day and above) and cisapride, because

both drugs lengthen the QT interval and increase the risk of developing severe heart rhythm disturbances

simultaneous use of astemizole

lactose intolerance, lactase deficiency, glucose-galactose malabsorption (capsules)

lactation period.,

With care: hepatic and / or renal failure

the appearance of a rash during the use of fluconazole in patients with superficial fungal infection and invasive / systemic fungal infections

simultaneous use of fluconazole with rifabutin or other drugs metabolized by the cytochrome P450 system

simultaneous use of terfenadine and fluconazole at a dose of less than 400 mg / day

potentially proarrhythmogenic conditions in patients with multiple risk factors (organic heart disease, electrolyte imbalance, concomitant use of drugs that cause arrhythmias)

patients with acetylsalicylic acid intolerance

pregnancy.

Specifications

Category

Antifungal

Scope of the drug

General

Release form

Capsules

Manufacturer country

Hungary

Package quantity, pcs

one

Scope of application

Dermatology

Way of introduction

Through the mouth

Vacation conditions

Without recipe

Brand name

Gedeon richter

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

The target audience

Children

Expiration date in days

1826

Package weight, g

5

Mode of application

:

The drug is taken orally. < br> When transferring from intravenous administration to taking capsules and vice versa, there is no need to change the daily dose. < br> Use in adults < br> For cryptococcal infections, the usual dose of fluconazole is 400 mg once a day on the first day of treatment, then 200-400 mg once a day. The duration of treatment for cryptococcal infections depends on the clinical efficacy confirmed by mycological study and is usually 6 to 8 weeks. < br> The recommended duration of treatment for cryptococcal meningitis is 10-12 weeks after a negative microbiological examination of a cerebrospinal fluid sample. < br> For the prevention of recurrence of cryptococcal meningitis in AIDS patients, after the completion of the full course of primary therapy, fluconazole is prescribed to the patient at a dose of at least 200 mg per day for a long period. < br> For candidemia, disseminated candidiasis and other invasive candidal infections, the daily dose of fluconazole is 400 mg on the first day and 200 mg on the following days. If necessary, the dose of the drug can be increased to 400 mg / day. The duration of treatment depends on the clinical effectiveness. < br> In case of severe systemic candidiasis, it is possible to increase the dose to 800 mg per day. The duration of therapy depends on the clinical effectiveness. Should continue for at least 2 weeks after receiving a negative blood culture or after the disappearance of symptoms. < br> With oropharyngeal candidiasis,including patients with impaired immunity, the usual dose of fluconazole is 50-100 mg once a day for 7-14 days. For the prevention of recurrence of oropharyngeal candidiasis in AIDS patients after completing a full course of primary therapy - 150 mg once a week. If necessary, treatment can be extended, especially in severe immunity disorders. < br> In case of atrophic candidiasis of the oral cavity associated with wearing dentures, fluconazole is usually prescribed 50 mg once a day for 14 days in combination with antiseptic agents for processing the prosthesis. < br> For other candidal infections, for example, with esophagitis, non-invasive bronchopulmonary infections, candiduria, candidiasis of the skin and mucous membranes, the daily dose is 50-100 mg for 14-30 days. < br> With severe candidiasis of the mucous membranes - 100-200 mg per day. < br> For the prevention of fungal infections in patients with malignant neoplasms, the dose of fluconazole should be 50 mg once a day until the patient is at increased risk due to cytostatic or radiation therapy. < br> For vaginal candidiasis - 150 mg once. To reduce the frequency of relapses, 150 mg is used once a month for 4-12 months, sometimes more frequent use may be required.For vaginal candidiasis - 150 mg once. To reduce the frequency of relapses, 150 mg is used once a month for 4-12 months, sometimes more frequent use may be required.For vaginal candidiasis - 150 mg once. To reduce the frequency of relapses, 150 mg is used once a month for 4-12 months, sometimes more frequent use may be required.

Information on technical characteristics, delivery set, country of manufacture