En DE FR ES PL
Itraconazole - instructions for use, reviews, analogs and formulations (capsules or tablets 100 mg, ointment or cream) of a drug for the treatment of candidiasis or thrush, multi-colored lichen and other mycoses in adults, children and pregnancy. Composition

Itraconazole - instructions for use, reviews, analogs and formulations (capsules or tablets 100 mg, ointment or cream) of a drug for the treatment of candidiasis or thrush, multi-colored lichen and other mycoses in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Itraconazole. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Itraconazole in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Itraconazole in the presence of existing structural analogues.Use for the treatment of candidiasis or thrush, multicolored lichen and other mycoses in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

 

Itraconazole - a synthetic antifungal agent of a wide spectrum of action. The triazole derivative. Suppresses the synthesis of ergosterol cell membrane of fungi. It is active against dermagophytes (Trichophyton spp., Microsporum spp., Epidermophyton floccosum), yeast fungi Candida spp. (Candida albicans, Candida parapsilosis), mold fungi (Cryptococcus neoformans, Aspergillus spp., Trichosporon spp., Geotrichum spp., Penicillium marneffei, Pseudallescheria boydii, Histoplasma spp., Coccidioides immitis, Paracoccidioides braziliensis., Sporothrix schenckii, Fonsecaea spp .. Cladosporium spp., Blastomyces dermatidis), Stalassezia spp.

 

Some strains may be resistant: Candida glabrata, Candida krusei, Candida tropicalis, Absidia spp., Fusarium spp., Mucor spp., Rhizomucor spp., Rhizopus spp., Scedosporium proliferans, Scopulariopsis spp.

 

The effectiveness of treatment is estimated after 2-4 weeks after discontinuation of therapy (with fungal infections), after 6-9 months - with onychomycosis (as the nails change).

 

Composition

 

Itraconazole + excipients.

 

Pharmacokinetics

 

It is absorbed from the gastrointestinal tract (GIT) quite full. Taking itraconazole in capsules immediately after meals increases bioavailability. It penetrates well into tissues and organs (including the mucous membrane of the vagina), is contained in the secretion of sebaceous and sweat glands. The concentration of itraconazole in the lungs, kidneys, liver, bones, stomach, spleen, skeletal muscles is 2-3 times higher than its concentration in plasma; in tissues containing keratin, 4-fold.The therapeutic concentration of itraconazole in the skin persists for 2-4 weeks after the cessation of the 4-week course of treatment. The therapeutic concentration in the nail keratin is reached 1 week after the start of treatment and is maintained for 6 months after the completion of the 3-month course of treatment. Low concentrations are determined in the sebaceous and sweat glands of the skin. Metabolised in the liver with the formation of active metabolites, including hydroxyitraconazole. Excretion from the plasma - biphasic: kidneys for 1 week (35% in the form of metabolites, 0.03% - unchanged) and through the intestine (3-18% unchanged).

 

Indications

  • vulvovaginal candidiasis;
  • dermatomycosis;
  • colored lichen;
  • Candidiasis of the oral mucosa;
  • keratomnosis;
  • onychomycosis caused by dermatophytes or yeast-like fungi;
  • systemic aspergillosis or candidiasis;
  • cryptococcosis (including cryptococcal meningitis) in immunocompromised individuals and cryptococcosis of the central nervous system irrespective of immune status with ineffective therapy of the 1st line;
  • histoplasmosis;
  • blastomycosis;
  • sporotrichosis;
  • paracoccidioidosis;
  • other rarely encountered systemic and tropical mycoses.

 

Forms of release

 

Capsules 100 mg.

 

Other dosage forms, be it pills, ointment or cream, exist.

 

Instructions for use and reception scheme

 

Inside. Immediately after eating. Capsules swallow whole.

 

The removal of itraconazole from the skin and nail tissue is slower than from the plasma. Thus, optimal clinical and mycological effects are achieved in 2-4 weeks after the end of treatment for skin infections and 6-9 months after the end of treatment for nail infections. The duration of treatment can be adjusted depending on the clinical picture of the treatment:

  • with vulvovaginal candidiasis - 200 mg twice a day for 1 day or 200 mg once a day for 3 days;
  • with dermatomycosis - 200 mg once a day for 7 days or 100 mg once a day for 15 days;
  • lesions of highly keratinized skin areas (dermatophytosis of feet and brushes) - 200 mg twice a day for 7 days or 100 mg once a day for 30 days;
  • with pityriasis lichen - 200 mg once a day for 7 days;
  • when candidiasis of the oral mucosa - 100 mg once a day for 15 days (in some cases in immunocompromised individuals, the bioavailability of itraconazole may decrease, which sometimes requires a doubling of the dose);
  • in keratomycosis - 200 mg once a day for 21 days (the duration of treatment depends on the clinical response);
  • with onychomycosis - 200 mg once a day for 3 months or 200 mg 2 times a day for 1 week per course;
  • with the defeat of the nails on the legs (regardless of the presence of nail lesions on the hands) spend 3 courses at intervals of 3 weeks. If the nails are damaged only on the hands, 2 courses are carried out with an interval of 3 weeks;
  • elimination of itraconazole from the skin and nails is slow; the optimal clinical response for dermatomycosis is achieved 2-4 months after completion of treatment, with onychomycosis - 6-9 months;
  • with systemic aspergillosis - 200 mg per day for 2-5 months; when the disease progresses and disseminates, the dose is increased to 200 mg twice a day;
  • with systemic candidiasis - 100-200 mg once a day for 3 weeks - 7 months, with progression and dissemination of the disease, the dose is increased to 200 mg twice a day;
  • with systemic cryptococcosis without signs of meningitis - 200 mg once a day for 2-12 months. In cryptococcal meningitis, 200 mg twice a day for 2-12 months;
  • treatment of histoplasmosis begins with 200 mg once a day, maintaining a dose of 200 mg twice a day for 8 months;
  • with blastomycosis - 100 mg once a day, maintaining a dose of 200 mg twice a day for 6 months;
  • with sporotrichosis - 100 mg once a day for 3 months;
  • with paracoccidioidosis - 100 mg once a day for 6 months;
  • with chromomycosis -100-200 mg once a day for 6 months;
  • children are assigned if the expected benefit exceeds the potential risk.

 

Side effect

  • dyspepsia (nausea, vomiting, diarrhea, constipation, decreased appetite);
  • abdominal pain;
  • hepatitis;
  • severe toxic liver damage;
  • headache;
  • dizziness;
  • peripheral neuropathy;
  • anaphylactic, anaphylactoid and allergic reactions;
  • multiforme exudative erythema (Stevens-Johnson syndrome);
  • skin rash;
  • itching;
  • hives;
  • angioedema;
  • alopecia;
  • photosensitivity;
  • menstrual cycle disorders;
  • edematous syndrome;
  • chronic heart failure;
  • pulmonary edema.

 

Contraindications

  • hypersensitivity;
  • chronic heart failure, incl. in the anamnesis (except for therapy of life-threatening conditions);
  • Simultaneous reception of CYP3A4 isoenzyme substrates that extend the QT interval (astemizole, bepridil, cisapride, dofetilide, levacetylmetadol, misolastine, pimozide, quinidine, sertnidol, terfenadine);
  • HMG-CoA reductase inhibitors metabolized by the CYP3A4 isoenzyme (lovastatin, simvastatin);
  • simultaneous oral administration of triazolam and midazolam, ergot alkaloids (dihydroergotamine, ergometrine, ergotamine, methylergotamine), nisoldipine, eletriptan;
  • pregnancy;
  • lactation period.

 

Application in pregnancy and lactation

 

Contraindicated during pregnancy and lactation.

 

Application in elderly patients

 

With caution: the elderly.

 

Use in children

 

With caution: child age. Children are assigned if the expected benefit exceeds the potential risk.

 

special instructions

 

Women of childbearing age who are taking itraconazole should use reliable contraceptive methods throughout the course of treatment until the onset of the first menstrual period after it is completed.

 

Itraconazole has been found to have a negative inotropic effect. With the simultaneous administration of itraconazole and calcium channel blockers, which may have the same effect, care must be taken. Cases of chronic heart failure associated with taking Itraconazole have been reported.Itraconazole should not be taken to patients with chronic heart failure or having a history of the disease, unless the possible benefit far exceeds the potential risk. When assessing the benefit / risk ratio individually, factors such as the severity of the indications, the dosing regimen, and individual risk factors for chronic heart failure should be taken into account. Risk factors include the presence of heart disease, such as ischemic heart disease or lesion of the valves; serious lung diseases, such as obstructive pulmonary disease; renal failure or other diseases accompanied by edema. Such patients should be informed about the signs and symptoms of congestive heart failure. Treatment should be done with caution, while monitoring the patient for symptoms of congestive heart failure. When they appear, the intake of Itraconazole should be discontinued.

 

With reduced acidity of the stomach: with this condition, the absorption of itraconazole from the capsules is impaired.Patients taking antacid preparations (for example, aluminum hydroxide), it is recommended to use them not earlier than 2 hours after taking Itraconazole capsules. Patients with achlorhydria or using H1 histamine receptor blockers and proton pump inhibitors are advised to take itraconazole capsules with drinks containing cola.

 

In very rare cases, with the use of Itraconazole, severe toxic liver damage developed, including cases of acute hepatic insufficiency with a fatal outcome. In most cases, this was noted in patients who already had liver disease, in patients with other serious diseases who received itraconazole therapy for systemic indications, as well as for patients receiving other drugs with hepatotoxic effect. In some patients, there were no obvious risk factors for liver damage. Several such cases occurred in the first month of therapy, and some in the first week of treatment. In this regard, it is recommended to regularly monitor liver function in patients receiving itraconazole therapy.Patients should be warned about the need to immediately contact their doctor if symptoms occur that suggest hepatitis, namely: anorexia, nausea, vomiting, weakness, abdominal pain and darkening of the urine. In case of such symptoms it is necessary to immediately stop therapy and conduct a study of liver function. Patients with a high concentration of liver enzymes or liver disease in the active phase, or with a transferred toxic liver injury with other medications should not be treated with Itraconazole, unless the expected benefit justifies the risk of liver damage. In these cases, it is necessary to control the concentration of "hepatic" enzymes during the treatment.

 

Disorders of liver function: itraconazole is metabolized predominantly in the liver. Since in patients with impaired liver function the full half-life of itraconazole is slightly increased, it is recommended to monitor the concentration of itraconazole in the plasma and, if necessary, adjust the dose of the drug.

 

Kidney Dysfunction: Since the full half-life of itraconazole is slightly increased in patients with renal insufficiency, it is recommended to monitor the concentration of itraconazole in the plasma and, if necessary, adjust the dose of the drug.

 

Patients with immunodeficiency: the bioavailability of itraconazole for oral administration may be reduced in some patients with impaired immunity, for example, in patients with neutropenia, AIDS patients or undergoing organ transplant surgery.

 

Patients with systemic fungal infections that pose a life threat: due to pharmacokinetic characteristics Itraconazole in the form of capsules is not recommended for the initiation of treatment of systemic mycoses that pose a threat to the lives of patients.

 

AIDS patients

 

The attending physician should evaluate the need to prescribe supportive therapy for people with AIDS who have previously been treated for systemic fungal infections, such as sporotrichosis, blastomycosis, histoplasmosis, or cryptococcosis (both meningeal and non-meningeal) who are at risk of recurrence.

 

Clinical data on the use of capsules Itraconazole in pediatric practice are limited.Capsules Itraconazole should not be given to children unless the expected benefit exceeds the possible risk.

 

Treatment should be discontinued if peripheral neuropathy occurs, which may be associated with the administration of Itraconazole capsules.

 

There is no evidence of cross-sensitivity to itraconazole and other azole antifungal agents.

 

Impact on the ability to drive a car and work with machinery

 

Itraconazole may cause dizziness and other side effects that may affect the ability to drive vehicles and other techniques that require increased attention during work.

 

Drug Interactions

 

1. Medicines that affect the absorption of itraconazole Drugs that reduce the acidity of the stomach, reduce the absorption of itraconazole, which is due to the solubility of capsule shells.

 

2. Medicines that affect the metabolism of itraconazole. Itraconazole is mainly metabolized by the CYP3A4 isoenzyme. The interaction of itraconazole with rifampicin, rifabutin and phenytoin, which are potent inducers of the isoenzyme CYP3A4, was studied.The study found that in these cases the bioavailability of itraconazole and pyroxytraconazole is significantly reduced, which leads to a significant decrease in the effectiveness of the drug. Simultaneous application of itraconazole with these drugs, which are potential inducers of microsomal liver enzymes, is not recommended. Studies of interaction with other inducers of microsomal liver enzymes, such as carbamazepine, Phenobarbital and isoniazid, have not been carried out, however, similar results can be assumed.

 

Powerful inhibitors of the CYP3A4 isoenzyme, such as ritonavir, indinavir, Clarithromycin and erythromycin, can increase the bioavailability of itraconazole.

 

3. Effect of itraconazole on the metabolism of other drugs. Itraconazole can inhibit the metabolism of drugs cleaved by the CYP3A4 isoenzyme. The result of this may be an increase or prolongation of their action, including side effects. Before starting to take concomitant medications, you should consult your doctor about the ways of metabolism of this drug, indicated in the instructions for medical use.After discontinuation of treatment, the concentrations of itraconazole in plasma

decrease gradually depending on the dose and duration. This need to be taken into account when discussing the migrating effect of itraconazole on concomitant medications.

 

Examples of such medicines are:

 

Drugs that can not be administered simultaneously with itraconazole:

  • terfenadine, astemizole, misolastine, cisapride, dofetilide, quinidine, pimozide, levacetylmetadol, sertindole - the combined use of these drugs with itraconazole may cause an increase in plasma concentrations of these substances and increase the risk of prolonging the QT interval and, in rare cases, the occurrence of atrial fibrillation (torsade des pointes);
  • metabolized by the CYP3A4 isoenzyme, HMG-CoA reductase inhibitors such as simvastatin and lovastatin;
  • midazolam for oral administration and triazolam;
  • ergot alkaloids such as dihydroergotamine, ergometrine, ergotamine and methylergometrine;
  • blockers of "slow" calcium channels - in addition to the possible pharmacokinetic interaction associated with a common metabolic pathway involving the isoenzyme CYP3A4,blockers of "slow" calcium channels may have a negative inotropic effect, which is enhanced by simultaneous administration with itraconazole.

 

Preparations, in the appointment of which it is necessary to monitor their concentrations in plasma, action, side effects. In the case of simultaneous administration with itraconazole dose of these drugs, if necessary, should be reduced:

  • indirect anticoagulants;
  • HIV protease inhibitors such as ritonavir, indinavir, saquinavir;
  • some antineoplastic agents, such as vinca alkaloids pink, busulfan, docetaxel, trimetrexate;
  • metabolized by the isoenzyme CYP3A4 blockers of "slow" calcium channels, such as verapamil and dihydropyridine derivatives;
  • Some immunosuppressive agents: cyclosporine, tacrolimus, sirolimus (also known as rapamycin);
  • some metabolized by the CYP3A4 isoenzyme HMG-CoA reductase inhibitors such as atorvastatin;
  • some glucocorticosteroids, such as budesonide, dexamethasone and methylprednisolone;
  • other drugs: digoxin, carbamazepine, buspirone alfentanil, alprazolam, brothiol, midazolam for intravenous administration, rifabutin, ebastin, reboxetine, cilostazol, disopyramide, eletriptan, halofatrine, repaglinide.

 

Interactions between itraconazole and zidovudine and fluvastatin were not detected. There was no effect of itraconazole on the metabolism of ethinylestradiol and norethisterone.

 

4. Effect on plasma protein binding.

 

Studies have demonstrated a lack of interaction between itraconazole and such drugs as imipramine, propranolol, diazepam, cimetidine, indomethacin, tolbutamide and sulfamethazine when bound to plasma proteins.

 

Analogs of medicinal product Itraconazole

 

Structural analogs for the active substance:

  • Irunin;
  • Itrazole;
  • Itraconazole ratopharm;
  • Itramikol;
  • Canditral;
  • Miconiol;
  • Orungal;
  • Orungamine;
  • Orunite;
  • Rumikoz;
  • Tecnazol.

 

Analogues on the curative effect (the means for treating varicolored lichen):

  • Acriderm;
  • Amicon;
  • Atitis;
  • Binafin;
  • Diflason;
  • Diflucan;
  • Zalain;
  • Imidil;
  • Irunin;
  • Itrazole;
  • Iphenec;
  • Candide;
  • Canison;
  • Ketoconazole;
  • Keto plus;
  • Clotrimazole;
  • Lamisyl;
  • Lamizil Dermgel;
  • Lamella;
  • Mikogal;
  • Mycosorrhal;
  • Mycomomax;
  • Nizoral;
  • Nofung;
  • Orungal;
  • Rumikoz;
  • Terbisyl;
  • Terbiks;
  • Triderm;
  • Fluconazole;
  • Flucostat;
  • Friederm;
  • Fungolon;
  • Fungoterbine;
  • Fungoterbine Neo;
  • Exifin;
  • Exodermil.

Similar medicines:

Other medicines:

Reviews (1):
Guests
Galina
Drank a drug with the same active substance - itraconazole, called Orungamin, a good analog.

Rules for publishing reviews and visitor questions