Itrazol, 100 mg capsules 42 pcs

Antifungal drug. Itraconazole is a synthetic broad-spectrum antifungal agent, a triazole derivative. It inhibits the synthesis of ergosterol of the cell membrane of fungi, which determines the antifungal effect of the drug.

Itraconazole is active against infections caused by dermatophytes (Trichophyton spp., Microsporum spp., Epidermophyton floccosum), yeast-like fungi and yeasts (Cryptococcus neoformans, Pityrosporum spp, Candida spp. including Candida albicans, Candida glabrata, Candida krusei), Aspergillus spp., Histoplasma spp., Paracoccidioides brasiliensis, Sporothrix schenckii, Fonsecaea spp., Cladosporium spp., Blastomyces dermatidis and other yeasts and molds.

Pharmacokinetics.

Indications

Fungal infections caused by pathogens sensitive to itraconazole:

damage to the skin and mucous membranes – vulvovaginal candidiasis, lichen versicolor, ringworm, candidiasis of the oral mucosa, fungal keratitis;
onychomycosis caused by dermatophytes and/or yeast-like fungi;
systemic mycoses – systemic aspergillosis and candidiasis, cryptococcosis, including cryptococcal meningitis (in patients with immunodeficiency and in all patients with cryptococcosis of the central nervous system, itraconazole should be used only in cases where first-line treatment drugs are not applicable or ineffective), histoplasmosis, blastomycosis, sporotrichosis, paracoccidioidomycosis, other rare systemic or tropical mycoses.

Pharmacological effect

Antifungal drug. Itraconazole is a synthetic broad-spectrum antifungal agent, a triazole derivative. Inhibits the synthesis of ergosterol in the cell membrane of fungi, which determines the antifungal effect of the drug.

Itraconazole is active against infections caused by dermatophytes (Trichophyton spp., Microsporum spp., Epidermophyton floccosum), yeast-like fungi and yeasts (Cryptococcus neoformans, Pityrosporum spp., Candida spp., including Candida albicans, Candida glabrata, Candida krusei), Aspergillus spp., Histoplasma spp., Paracoccidioides brasiliensis, Sporothrix schenckii, Fonsecaea spp., Cladosporium spp., Blastomyces dermatidis, as well as other yeasts and molds.

Pharmacokinetics

Special instructions

Women of childbearing potential taking Itrazol® must use adequate contraception throughout the course of treatment until the first menstrual period after its completion.

When studying the IV dosage form of itraconazole, a transient asymptomatic decrease in left ventricular ejection fraction was noted, which normalized until the next infusion of the drug.

Itraconazole has a negative inotropic effect. Cases of heart failure associated with itraconazole have been reported. Itraconazole should not be taken by patients with CHF or a history of this disease unless the possible benefit significantly outweighs the potential risk.

CCBs may have a negative inotropic effect, which may enhance this effect of itraconazole; itraconazole may reduce the metabolism of CCBs. Caution should be exercised when taking itraconazole and CCBs concomitantly.

With reduced gastric acidity, the absorption of itraconazole is impaired. For patients taking antacid medications (for example, aluminum hydroxide), it is recommended that they be used no earlier than 2 hours after taking Itrazol® capsules. Patients with achlorhydria or using H2-histamine blockers or proton pump inhibitors are recommended to take Itrazole® capsules with acidic drinks.

With long-term use of itraconazole (more than 1 month), when using itraconazole in patients receiving other drugs that have hepatotoxic effects, as well as in patients with liver diseases, it is recommended to regularly monitor liver function. Patients should be advised to contact their physician immediately if symptoms suggestive of hepatitis occur, such as anorexia, nausea, vomiting, weakness, abdominal pain, and dark urine. If such symptoms occur, you should immediately stop therapy and conduct a liver function test.

In patients with renal failure, the bioavailability of itraconazole may be reduced, and therefore dose adjustment is necessary.

Treatment should be discontinued if neuropathy occurs, which may be associated with taking Itrazole® capsules. There is no evidence of cross-hypersensitivity to itraconazole and other azole antifungals. Itrazole® capsules should be administered with caution to patients with hypersensitivity to other azoles.

In patients with compromised immunity (AIDS, after organ transplantation, neutropenia), an increase in the dose of Itrazole® may be required.

Active ingredient

Itraconazole

Composition

Active ingredient:

itraconazole 100 mg;

Excipients:

sugar pellets (sucrose – 80-91.5%, corn starch – 8.5-20%) – 207.44 mg;

poloxamer 188 (Lutrol) – 25.94 mg; Poloxamer 188 (Lutrol) micronized – 0.51 mg;

hypromellose – 130.11 mg.

Pregnancy

Itrazol® is contraindicated during pregnancy.

Women of childbearing age taking Itrazol® must use reliable methods of contraception throughout the course of treatment until the onset of the first menstruation after its completion.

Since itraconazole can pass into breast milk, breastfeeding should be discontinued if use of the drug is necessary.

Contraindications

hypersensitivity to itraconazole or excipients;
simultaneous use of drugs that are substrates of the CYP3A4 isoenzyme (see “Interaction”), such as levacetylmethadone, methadone; disopyramide, dofetilide, dronedarone, quinidine; telithromycin in patients with severe renal or hepatic impairment; ticagrelor; halofantrine; astemizole, mizolastine, terfenadine; ergot alkaloids – dihydroergotamine, ergometrine (ergonovine), ergotamine, methylergometrine (methylergonovine), eletriptan; irinotecan; lurasidone, oral midazolam, pimozide, sertindole, triazolam; bepridil, felodipine, lercanidipine, nisoldipine; ivabradine, ranolazine; eplerenone; cisapride, domperidone; lovastatin, simvastatin, atorvastatin; fesoterodine in patients with moderate or severe renal or hepatic impairment, solifenacin in patients with severe renal impairment and moderate or severe hepatic impairment; colchicine in patients with impaired liver or kidney function;
chronic heart failure currently or in history (with the exception of treatment of life-threatening or other dangerous infections; see “Special Instructions”);
fructose intolerance, sucrase/isomaltase deficiency, glucose-galactose malabsorption;
children under 3 years of age;
pregnancy;
breast-feeding.

With caution: liver cirrhosis; severe dysfunction of the liver and kidneys; hypersensitivity to other azoles; simultaneous use with drugs that can increase or decrease the concentration of itraconazole in the blood plasma or simultaneous use with drugs whose concentration in the blood plasma can change (see “Interaction”); elderly patients; children over 3 years old (see “Special instructions”).

Side Effects

From the gastrointestinal tract: dyspepsia, nausea, abdominal pain and constipation, reversible increase in the activity of liver enzymes, cholestatic jaundice, hepatitis, anorexia. In very rare cases, when using the drug Itrazol®, severe toxic damage to the liver developed, incl. a case of acute liver failure with a fatal outcome.

From the central nervous system: headache, fatigue, dizziness, peripheral neuropathy.

From the cardiovascular system: congestive heart failure and pulmonary edema.

From other organs and systems: menstrual irregularities, allergic reactions (such as itching, rash, urticaria and angioedema), Stevens-Johnson syndrome, alopecia, hypokalemia, edema, dark urine discoloration, hypercreatininemia.

Interaction

Drugs that affect the metabolism of itraconazole

The interaction of itraconazole with rifampicin, rifabutin and phenytoin has been studied. The simultaneous use of itraconazole with these drugs, which are potential inducers of liver enzymes, is not recommended. Interaction studies with other hepatic enzyme inducers such as carbamazepine, phenobarbital and isoniazid have not been conducted, but similar results can be expected due to the fact that itraconazole is primarily metabolized by the enzyme CYP3A4; potent inhibitors of this enzyme may increase the bioavailability of itraconazole. Examples include ritonavir, indinavir, clarithromycin and erythromycin.

The effect of itraconazole on the metabolism of other drugs

Itraconazole may inhibit the metabolism of drugs metabolized by the CYP3A4 enzyme. The result of this may be an intensification or prolongation of their action, incl. and side effects.

Drugs that should not be given concomitantly with itraconazole

– terfenadine, astemizole, mizolastine, cisapride, triazolam and oral midazolam, dofetilide, quinidine, pimozide, HMG-CoA reductase inhibitors such as simvastatin and lovastatin;

– CCBs may have a negative inotropic effect, which may enhance the same effect exhibited by itraconazole. When taking itraconazole and CCBs simultaneously, caution must be exercised because CCB metabolism may be reduced.

Drugs, when prescribed, it is necessary to monitor their concentration in plasma and their effect, side effects

When co-administered with itraconazole, the dose of the following drugs should be reduced, if necessary:

– oral anticoagulants;

– HIV protease inhibitors, such as ritonavir, indinavir, saquinavir;

– some antitumor drugs, such as rose vinca alkaloids, busulfan, docetaxel, trimetrexate;

– CCBs cleaved by the CYP3A4 enzyme, such as verapamil;

– some immunosuppressive drugs: cyclosporine, tacrolimus, sirolimus;

– other drugs: digoxin, carbamazepine, buspirone, alfentanil, alprazolam, brotizolam, rifabutin, methylprednisolone, ebastine, reboxetine.

No interaction was found between itraconazole and zidovudine and fluvastatin.

There was no effect of itraconazole on the metabolism of ethinyl estradiol and norethisterone.

Effect on protein binding

In vitro studies have demonstrated the lack of competition between itraconazole and drugs such as imipramine, propranolol, diazepam, cimetidine, indomethacin, tolbutamide and sulfadimidine in binding to plasma proteins.

Overdose

No data available.

Treatment: during the first hour, perform gastric lavage and, if necessary, prescribe activated charcoal and symptomatic treatment. Itraconazole is not eliminated by hemodialysis. There is no specific antidote for the drug.

Storage conditions

In a dry place, protected from light, at a temperature below 25 °C.

Shelf life

2.5 years

Manufacturer

Vertex, Russia