Itrazol capsules 100 mg, 42 pcs. (Itraconazole)

packaging 42 pcs

Pharmacological action

Intrazole - antifungal.

Pharmacodynamics

Itraconazole is a synthetic broad-spectrum antifungal agent derived from triazole. It 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 yeast (Cryptococcus neoformans, Pityrosporum spp., Candida albisans, C. C. albratans C. ) Aspergillus spp., Histoplasma spp., Paracoccidioides brasiliensis, Sporothrix schenckii, Fonsecaea spp., Cladosporium spp., Blastomyces dermatidis, as well as other yeast and mold fungi.

Pharmacokinetics

Absorbed from the gastrointestinal tract completely enough. Taking itraconazole in capsules immediately after a meal increases bioavailability. Cmax in plasma is reached within 3-4 hours after ingestion. Css when taking 100 mg of the drug 1 time per day - 0.4 μg / ml when taking 200 mg 1 time per day - 1.1 μg / ml, 200 mg 2 times a day - 2 μg / ml.

The time of onset of Css in plasma with prolonged use is 1-2 weeks. Communication with plasma proteins - 99.8%.

It penetrates well into tissues and organs (including the mucous membrane of the vagina), is contained in the secretion of the sebaceous and sweat glands. The concentration of itraconazole in the lungs, kidneys, liver, bones, stomach, spleen, and skeletal muscle is 2–3 times higher than its concentration in plasma in tissues containing keratin — 4 times.

The therapeutic concentration of itraconazole in the skin persists for 2–4 weeks after discontinuation of the 4-week course of treatment. The therapeutic concentration in nail keratin is achieved 1 week after the start of treatment and persists for 6 months after completion of a 3-month course of treatment. Low concentrations are detected in the sebaceous and sweat glands of the skin.

Metabolized in the liver with the formation of active metabolites, including hydroxyitraconazole. It is an inhibitor of isoenzymes CYP3A4, CYP3A5 and CYP3A7.

Excretion from plasma is two-phase: by the kidneys for 1 week (35% - in the form of metabolites, 0.03% - unchanged) and through the intestines (3-18% - unchanged). T1 / 2 - 1-1.5 days. It is not removed during dialysis.

Indications

dermatomycosis

fungal keratitis

onychomycosis caused by dermatophytes and / or yeast and mold

systemic mycoses: systemic aspergillosis and candidiasis, cryptococcosis (including cryptococcal meningitis), histoplasmosis, sporotrichosis, paracoccidioidomycosis, blastomycosis and other systemic or tropical mycoses

candidomycosis with lesions of the skin or mucous membranes, including vulvovaginal candidiasis

pityriasis versicolor.

Contraindications

individual hypersensitivity to the drug or its components

simultaneous administration of drugs metabolized with the participation of the CYP3A4 enzyme: terfenadine, astemizole, misolastine, cisapride, dofetilide, quinidine, pimozimstin inhibit, , triazolam and midazolam (see “Interaction”)

pregnancy

lactation period

childhood (up to 3 years).

Precautions: severe heart failure of a liver disease (including those accompanied by liver failure). Itrazol® is recommended for use in children over 3 years old only if the potential benefit outweighs the potential risk.

Special instructions

Women of childbearing age who take ItrazolВ® must use adequate contraceptive measures throughout the course of treatment until the onset of the first menstruation after its completion.

When examining the iv dosage form of itraconazole, a transient asymptomatic decrease in the ejection fraction of the left ventricle was observed, normalizing 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 in patients with chronic heart failure or a history of the disease, unless the potential benefit significantly exceeds the potential risk.

BKK can have a negative inotropic effect, which can enhance the similar effect of itraconazole, itraconazole can reduce the metabolism of BKK. With the simultaneous administration of itraconazole and BCC, caution must be exercised.

With reduced gastric acidity, absorption of itraconazole is impaired. Patients taking antacids (e.g. aluminum hydroxide) are advised to use them no earlier than 2 hours after taking ItrazoleВ® capsules. Patients with achlorhydria or those using H2 histamine receptor blockers or proton pump inhibitors are advised to take ItrazoleВ® capsules with acidic drinks.

With prolonged use of itraconazole (more than 1 month), with itraconazole, it is recommended that patients receiving other drugs with hepatotoxic effects, as well as patients with liver diseases, regularly monitor liver function. Patients should be warned about the need to immediately contact their doctor in case of symptoms suggesting the onset of hepatitis, namely: anorexia, nausea, vomiting, weakness, abdominal pain and dark urine. In the event of such symptoms, it is necessary to immediately stop therapy and conduct a liver function test.

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

Treatment should be discontinued if a neuropathy occurs that may be associated with taking ItrazoleВ® capsules. There is no evidence of cross-sensitivity to itraconazole and other azole antifungal drugs. ItrazolВ® in capsules should be used with caution in patients with hypersensitivity to other azoles.

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

Composition

1 capsule contains:

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.

Side effects of

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, with the use of Itrazol®, severe toxic liver damage developed, including a case of acute liver failure with a fatal outcome.

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

From the CCC side: 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, hypercreatininemia.

Drug interactions

drugs that affect the metabolism of itraconazole

The interaction of itraconazole with rifampicin, rifabutin and phenytoin was studied. The simultaneous use of itraconazole with these drugs, which are potential inducers of liver enzymes, is not recommended.

Interaction studies with other liver enzyme inducers such as carbamazepine, phenobarbital and isoniazid have not been conducted, however, similar results can be assumed due to the fact that itraconazole is mainly metabolized by the enzyme CYP3A4, powerful inhibitors of this enzyme can increase the bioavailability of itraconazole. Examples include ritonavir, indinavir, clarithromycin, and erythromycin.

Effect of itraconazole on the metabolism of other drugs

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

Drugs that should not be administered concomitantly with itraconazole

- terfenadine, astemizole, misolastine, cisapride, triazolam and oral midazolam, dofetilide, quinidine, pimozide, HMG-CoA reductase inhibitors such as simvastatin Bt and , which can enhance the same effect shown by itraconazole. With the simultaneous administration of itraconazole and BCC, caution must be exercised, as BCK metabolism can be reduced.

Drugs for which it is necessary to monitor their plasma concentration and effect, side effects

In case of simultaneous administration 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 pink vinca alkaloids, busulfan, docetaxel,

trimerexate - cleaved by the CYP3A4 BKK enzyme, such as verapamil

- some immun suppressants: 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.

No effect of itraconazole on the metabolism of ethinyl estradiol and norethisterone was observed.

Effect on protein binding

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

Overdose

No data available.

Treatment: Within the first hour, gastric lavage and, if necessary, prescribed activated charcoal, symptomatic treatment. Itraconazole is not excreted in hemodialysis. There is no specific antidote for the drug.

Storage Conditions

In a dry, dark place at temperatures below 25 ° C.

Deystvuyushtee substance

Itraconazole

Terms and conditions

prescription

Prescription

Prescription

Prescribed by a doctor, Pregnant women as prescribed by a doctor Adults prescribed by a doctor

Vertex, Russia



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