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:

Active ingredient

Composition

Active ingredient:

itraconazole 100 mg;

Associates:

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.

How to take, the dosage

Itrazol capsules are taken orally after meals.

Onychomycosis – 200 mg once daily for 3 months or 200 mg twice daily for 1 week with a 3 week break; In case of onychomycosis of feet – 3 courses of treatment, of hands – 2 courses;

Vulvovaginal candidiasis – 200 mg 2 times daily for 1 day or 200 mg 1 time per day for 3 days; Scrofulous ulcer – 200 mg 1 time per day for 7 days;

Dermatomycosis and oral candidiasis – 100-200 mg 1 time per day for 7-15 days (repeat course if necessary);

Fungal keratitis – 200 mg once daily for 21 days; systemic mycoses – 100-200 mg 1-2 times daily for 2-12 months (depending on the causative agent).

Interaction

Preventive drugs affecting the metabolism of itraconazole

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

Influence of itraconazole on the metabolism of other drugs

Itraconazole may inhibit the metabolism of drugs cleaved by CYP3A4 enzyme. This may result in strengthening or prolongation of their effects, including side effects.

Drugs that should not be taken at the same time as itraconazole

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

– BCAAs may have a negative inotropic effect, which may exacerbate the same effect exhibited by itraconazole. Caution should be exercised when concomitant administration of itraconazole and BCAA, as metabolism of BCAA may be reduced.

Pdrugs whose plasma concentrations and effects, side effects

If prescribed concomitantly with itraconazole, the dose of the following drugs should be reduced if necessary:

– oral anticoagulants;

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

– Certain anticancer drugs, such as periwinkle pink alkaloids, busulfan, docetaxel, trimetrexate;

– BCAs that are cleaved by the CYP3A4 enzyme, such as verapamil;

– Certain immunosuppressive drugs: cyclosporine, tacrolimus, sirolimus;

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

The interaction between itraconazole and zidovudine and fluvastatin has not been found.

The effect of itraconazole on the metabolism of ethinylestradiol and norethisterone was not observed.

Influence on protein binding

In vitro studies have demonstrated no competition between itraconazole and such drugs as imipramine, propranolol, diazepam, cimetidine, indomethacin, tolbutamide and sulfadimidine in binding to plasma proteins.

Special Instructions

Women of childbearing age taking Itrazol® should use adequate contraceptive measures throughout the course of treatment until the first menstrual period after completion.

In an IV study of itraconazole, a transient asymptomatic decrease in left ventricular ejection fraction was observed, which normalized before the next infusion of the drug.

Itraconazole has a negative inotropic effect. Cases of heart failure associated with itraconazole administration have been reported. Itraconazole should not be taken in patients with CHF or with a history of this disease, except in cases when the possible benefit significantly exceeds the potential risk.

The BCCs may have a negative inotropic effect, which may increase the similar effect of itraconazole; itraconazole may decrease metabolism of BCCs. Caution should be exercised when concomitant administration of itraconazole and BCAA.

In low gastric acidity, absorption of itraconazole is impaired. Patients taking antacids (e.g., aluminum hydroxide), it is recommended to use them not earlier than 2 hours after taking Itrazol® capsules. Patients with achlorhydria or who use H2-histamine receptor blockers or proton pump inhibitors are recommended to take Itrazol® capsules with acidic beverages.

When itraconazole is used for a long time (more than 1 month), when itraconazole is used by patients receiving other drugs with hepatotoxic effect, as well as by patients with liver diseases it is recommended to monitor the liver function regularly. Patients should be warned to contact their physician immediately in case of symptoms suggestive of hepatitis, namely: anorexia, nausea, vomiting, weakness, abdominal pain and darkened urine. If these symptoms occur, therapy should be stopped immediately and liver function tests should be performed.

The bioavailability of itraconazole may be reduced in patients with renal impairment; therefore, the dose should be adjusted.

The treatment should be stopped if neuropathy occurs, which may be associated with the intake of Itrazol® capsules. There are no data on cross-sensitivity to itraconazole and other azole antifungal drugs. Itrazol® capsules should be used with caution in patients with hypersensitivity to other azoles.

In patients with impaired immunity (AIDS, after organ transplantation, neutropenia) the dose of Itrazol® may require increasing.

Contraindications

With caution: Hepatic cirrhosis; severe hepatic and renal dysfunction; hypersensitivity to other azoles; simultaneous use with drugs that may increase or decrease the plasma concentration of itraconazole or simultaneous use with drugs whose plasma concentrations may change (see “Interactions”); elderly patients; children over 3 years (see “Special Indications”).

Side effects

Gastrointestinal disorders:dyspepsia, nausea, abdominal pain and constipation, reversible increase in liver enzyme activity, cholestatic jaundice, hepatitis, anorexia. In very rare cases during the use of Itrazol® preparation severe toxic liver injury occurred, including a case of acute hepatic failure with fatal outcome.

CNS disorders: headache, fatigue, dizziness, peripheral neuropathy.

CCS: constrictive heart failure and pulmonary edema.

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

Overdose

No data available.

Treatment:In the first hour, gastric lavage and, if necessary, administration of activated charcoal, symptomatic treatment. Itraconazole is not excreted by hemodialysis. There is no specific antidote to the drug.

Pregnancy use

Itrazol® is contraindicated in pregnancy.

Women of childbearing age who take the drug Itrazol® should use reliable contraceptive methods for the duration of treatment until the first menstrual period after its completion.

Because itraconazole may pass into breast milk, breast-feeding should be stopped if therapy is required.

Similarities