Itraconazole capsules 100 mg

Instructions for use Itraconazole capsules 100 mg

Trade name: Itraconazole

International Nonproprietary Name (INN) - itraconazole

Dosage form – capsules

Composition per one capsule:

Active substance: itraconazole pellets - 464.00 mg, containing itraconazole - 100.00 mg.

Excipients included in the itraconazole pellets: sugar pellets - 207.44 mg (sucrose – 80.0 - 91.5 %, corn starch – 8.5 - 20.0 %, water – maximum 1.5 %), hypromellose - 130.11 mg, poloxamer 188 (Lutrol F68) – 25.94 mg, micronized poloxamer 188 (Lutrol Micro 68) - 0.51 mg.

Hard gelatin capsules: water – 13-16 %, sunset yellow FCF (E110) – 1 %, titanium dioxide – 1 %, gelatin – up to 100 %.

Description

Size No. 0 hard gelatin capsules, orange in color, containing spherical microgranules (pellets) from light yellow to yellowish-beige.

Pharmacotherapeutic group. Antifungal agent

ATC code  [J02AC02]

Pharmacological properties

Pharmacodynamics

Itraconazole, a triazole derivative, is active against infections caused by dermatophytes (Trichophyton spp., Microsporum spp., Epidermophyton floccosum), yeast-like fungi and yeasts (Candida spp., including C.albicans, C.glabrata and C.krusei, Cryptococcus neoformans, Pityrosporum spp., Trichosporon spp., Geotrichum spp.); Aspergillus spp., Histoplasma spp., Paracoccidioides brasiliensis, Sporothrix schenckii, Fonsecaea spp., Cladosporium spp., Blastomyces dermatitidis, Pseudallescheria boydii, Penicillium marneffei, as well as other yeasts and molds.

Itraconazole disrupts the synthesis of ergosterol, which is an important component of the fungal cell membrane, which determines the antifungal effect of the drug.

Pharmacokinetics

After oral administration, the maximum bioavailability of itraconazole is observed when capsules are taken immediately after a meal. The maximum plasma concentration is reached within 3-4 hours after oral intake. Elimination from plasma is biphasic with a terminal half-life of 24-36 hours. With long-term use, steady-state concentration is reached within 1-2 weeks. The steady-state plasma concentration of itraconazole 3-4 hours after administration is 0.4 µg/ml (100 mg taken once daily), 1.1 µg/ml (200 mg taken once daily), and 2.0 µg/ml (200 mg taken twice daily). Itraconazole is 99.8% bound to plasma proteins. The concentration of itraconazole in whole blood is about 60% of the concentration in plasma.

Accumulation of the drug in keratinous tissues, especially in the skin, is approximately 4 times higher than in plasma, and its elimination rate depends on epidermal regeneration.

Unlike plasma concentrations, which become undetectable within 7 days after cessation of therapy, therapeutic concentrations in the skin persist for 2-4 weeks after stopping a 4-week treatment course. Itraconazole is detected in nail keratin as early as one week after starting treatment and persists for at least 6 months after completing a 3-month course of therapy. Itraconazole is also found in sebum and, to a lesser extent, in sweat.

Itraconazole is well distributed in tissues prone to fungal infections. Concentrations in the lungs, kidneys, liver, bones, stomach, spleen, and muscles were two to three times higher than the corresponding plasma concentrations. Therapeutic concentrations in vaginal tissue persist for up to 2 days after the end of a 3-day course of treatment at a dose of 200 mg per day, and for 3 days after the end of a one-day course of treatment at a dose of 200 mg twice daily.

Itraconazole is metabolized in the liver to form a large number of metabolites. One such metabolite is hydroxy-itraconazole, which has comparable in vitro antifungal activity to itraconazole. Antifungal drug concentrations determined by microbiological assay were approximately 3 times higher than concentrations measured by HPLC. Excretion in feces ranges from 3 to 18% of the dose. Renal excretion accounts for less than 0.03% of the dose. Approximately 35% of the dose is excreted as metabolites in the urine within 1 week.

Since the total half-life and plasma concentration of itraconazole are somewhat increased in patients with renal failure, dose adjustment may be necessary (see "Special Instructions" section).

Since the total half-life and plasma concentration of itraconazole are somewhat increased in patients with cirrhosis, dose adjustment may be necessary (see "Special Instructions" section).

Indications for use

• Dermatomycoses;
• Fungal keratitis;
• Onychomycoses caused by dermatophytes and/or yeasts and molds;
• Systemic mycoses:
• Systemic aspergillosis and candidiasis,
• Cryptococcosis (including cryptococcal meningitis): in immunodeficient patients and in all patients with cryptococcosis of the central nervous system, Itraconazole capsules should be prescribed only in cases where first-line drugs are not applicable or are ineffective.
• Histoplasmosis,
• Sporotrichosis,
• Paracoccidioidomycosis,
• Blastomycosis
• Other rare systemic or tropical mycoses;
• Candidomycoses with skin or mucosal involvement, including vulvovaginal candidiasis;
• Pityriasis versicolor.

Contraindications

• Hypersensitivity to itraconazole or any component of the drug.
• Concurrent administration of Itraconazole capsules with the following drugs:
• Substrates of the CYP3A4 isoenzyme that prolong the Q-T interval (astemizole, bepridil, cisapride, dofetilide, levacetylmethadol, mizolastine, pimozide, quinidine, sertindole, terfenadine)
• HMG-CoA reductase inhibitors metabolized by the CYP3A4 isoenzyme (lovastatin, simvastatin);
• Concurrent oral administration of triazolam and midazolam, nisoldipine, eletriptan;
• Ergot alkaloid preparations such as  dihydroergotamine, ergometrine,
• Ergotamine and methylergometrine;
• Fructose intolerance, sucrase/isomaltase deficiency, glucose-galactose malabsorption;
• Children under 3 years of age;
• Pregnancy and lactation period

With caution – in liver cirrhosis, chronic renal failure, chronic  heart failure, hypersensitivity to other azoles, in children and elderly patients (see also "Special Instructions" section).

Use during pregnancy and lactation

Pregnancy is an absolute contraindication for the use of Itraconazole.

Since itraconazole may pass into breast milk, if use during lactation is necessary, women taking Itraconazole capsules should discontinue breastfeeding.

Itraconazole tablets are taken orally, swallowed whole with a small amount of water. The optimal time for administration is after a meal.

A detailed dosing regimen for Itraconazole should be sought in the instructions for use; the prescription of an individualized regimen and selection of dosages at the physician's discretion is also permitted.

Itraconazole is usually taken according to the following instructions:

• Vulvovaginal candidiasis – 200 mg twice daily for 1 day, OR 200 mg once daily for three days;
• Dermatomycosis – 200 mg once daily for seven days, OR 100 mg daily for 15 days;
• Skin lesions of feet and hands due to dermatophytosis – 200 mg twice daily for seven days, OR 100 mg once daily for one month;
• Pityriasis versicolor – 200 mg daily for at least seven days;
• Oral mucosal candidiasis – 100 mg of the drug once daily for 15 days (in some situations the dose may be increased to 200 mg);
• Keratinomycosis – 200 mg once daily for three weeks (the duration of Itraconazole intake may be increased at the physician's discretion);
• Onychomycosis – 200 mg once daily for three months, OR 200 mg twice daily for one week (if toenails are affected, three treatment courses are necessary; if fingernails are affected, the treatment course is repeated twice; in both cases, the interval between courses is at least three weeks);
• Systemic candidiasis – 100 or 200 mg once daily for a period ranging from three weeks to seven months;
• Systemic cryptococcal infection – 200 mg once daily for a period ranging from two months to one year; if cryptococcal meningitis is suspected: 200 mg twice daily for a period ranging from two months to one year;
• Histoplasmosis – 200 mg once daily for treatment and 200 mg twice daily for eight months for maintenance therapy.

Itraconazole tablets are prescribed to children under 12 years of age only if the importance of treatment outweighs all possible risks associated with taking this drug.

To reduce the risk of adverse reactions, it is recommended to drink plenty of fluids during treatment with Itraconazole and, if necessary, to use additional drugs as prescribed by a doctor.

If you miss a dose of the drug, do not double the next dose or restart the treatment regimen.

Dosage forms

Capsules 100 mg.

5, 6, or 7 capsules in a blister strip made of polyvinyl chloride film  and printed lacquered aluminum foil.

1, 2, or 3 blister packs, together with the instructions for use, are placed in a cardboard carton. 

Storage conditions

In a dry place, protected from light and moisture, at a temperature not exceeding 25 ^oC. Keep out of reach of children.

Shelf life

2 years. Do not use after the expiration date.

Prescription status

By prescription.

Name and address of the legal entity in whose name the registration certificate is issued / Organization accepting claims:

JSC "AVVA RUS", Russia, 121614,

Moscow, Krylatskie Kholmy st., 30, building 9.

Tel/Fax: +7 (495) 956-75-54.

avva.com.ru

Production site address:

JSC "AVVA RUS", Russia, 610044, Kirov region, Kirov, Luganskaya st., 53a.

Tel.: +7 (8332) 25-12-29; +7 (495) 956-75-54.

Where to Buy Itraconazole?

The drug is sold through pharmacies. In pharmacy chains, Itraconazole can only be purchased with a doctor's prescription. The price for Itraconazole is set individually by each pharmacy. Before use, it is necessary to carefully read the instructions for use, familiarize yourself with the indications and contraindications, special instructions for administration, and existing limitations. It is also recommended to thoroughly check the drug's expiration date and not to take Itraconazole after it has expired.

The drug should be taken strictly according to the instructions and the treatment regimen prescribed by the doctor.