Itraconazole, 100 mg capsules 14 pcs
€13.70 €11.42
Vulvovaginal candidiasis;
Active ingredient
Itraconazole
Composition
Each capsule contains itraconazole pellets (22%) – 0.460 g.
Pellet composition:
How to take, the dosage
Internal. Immediately after a meal. Capsules are swallowed whole.
The elimination of the drug itraconazole from skin and nail tissue is slower than that from plasma. Thus, optimal clinical and mycological effects are achieved 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:
- for vulvovaginal candidiasis, 200 mg 2 times daily for 1 day or 200 mg once daily for 3 days;
- for dermatomycoses, 200 mg once daily for 7 days or 100 mg once daily for 15 days;
- in lesions of highlykeratinized skin areas (dermatophytosis of the feet and hands) – 200 mg 2 times a day for 7 days or 100 mg once a day for 30 days;
- with pityriasis – 200 mg once a day for 7 days;
- with chancroiditisIn oral candidiasis – 100 mg once daily for 15 days (in some cases in immunocompromised patients bioavailability of itraconazole may decrease, which sometimes requires doubling the dose);
- in keratomycosis – 200 mg once daily for 21 days (duration of therapy depends on the clinical response);
- in onychomycosis – 200 mg once daily for 3 months or 200 mg twice daily for 1 week per course;
- in nail lesions on the feet (regardless of the presence of nail lesions on the hands), 3 courses with an interval of 3 weeks.
- Intraconazole is slowly eliminated from skin and nails; optimal clinical response is achieved 2-4 months after treatment completion in dermatomycosis, 6-9 months in onychomycosis;
- with systemic aspergillosis – 200 mg/day for 2-5 months; In disease progression and dissemination the dose is increased to 200 mg 2 times a day;
- in systemic candidiasis – 100-200 mg once a day for 3 weeks to 7 months, in disease progression and dissemination the dose is increased to 200 mg 2 times a day;
- in systemic cryptococcosis without signs of meningitis – 200 mg once daily for 2-12 months. In cryptococcal meningitis – 200 mg 2 times a day for 2-12 months.
- Histoplasmosis treatment starts with 200 mg once daily, the maintenance dose is 200 mg twice daily for 8 months;
- with blastomycosis – 100 mg once daily, the maintenance dose is 200 mg twice daily for 6 months;
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- in paracoccidioidosis, 100 mg once daily for 6 months;
- in chromomycosis, 100-200 mg once daily for 6 months;
- children are indicated if the expected benefit exceeds the potential risk.
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Interaction
- Drugs affecting the absorption of itraconazole Drugs that reduce gastric acidity reduce the absorption of itraconazole, which is associated with the solubility of the capsule shells.
- Drugs affecting the metabolism of itraconazole. Itraconazole is mainly metabolized by CYP3A4 isoenzyme. The interaction of itraconazole with rifampicin, rifabutin and phenytoin, which are potent inducers of CYP3A4 isoenzyme, was studied. The study found that in these cases, the bioavailability of itraconazole and hydroxyitraconazole is significantly reduced, which leads to a significant reduction in the effectiveness of the drug. Concomitant use 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 conducted, however, similar results can be assumed. Powerful inhibitors of CYP3A4 isoenzyme, such as ritonavir, indinavir, clarithromycin and erythromycin, can increase the bioavailability of itraconazole.
- Itraconazole effect on metabolism of other drugs. Itraconazole may inhibit the metabolism of drugs cleaved by CYP3A4 isoenzyme. This can result in intensification or prolongation of their effects, including side effects. Before starting to take concomitant drugs, it is necessary to consult the attending physician about the metabolic pathway of this drug, specified in the instructions for medical use. After discontinuation of treatment, plasma concentrations of itraconazole decrease gradually, depending on the dose and duration of treatment (see section Pharmacokinetics). This must be taken into account when discussing the migratory effect of itraconazole on concomitant medications.
Examples of such medications are:
Drugs that should not be prescribed at the same time as itraconazole:
- .Terfenadine, astemizole, misolastin, cisapride, dofetilide, quinidine, pimozide, levacetylmetadol, sertindol: co-administration of these medicines with itraconazole may increase the plasma concentrations of these drugs and increase the risk of prolonged QT interval and in rare cases, the onset of ventricular torsade de pointes.
- CYP3A4 isoenzyme-metabolized HMG-CoA reductase inhibitors such as simvastatin and lovastatin,
- ergot alkaloids such as dihydroergotamine, ergometrine, ergotamine and methylergometrine,
- Slow” calcium channel blockers – in addition to the possible pharmacokinetic interaction associated with the common metabolic pathway involving the CYP3A4 isoenzyme, slow calcium channel blockers may have a negative inotropic effect that is enhanced when taken concurrently with itraconazole.
Drugs for which it is necessary to monitor their plasma concentrations, effects, side effects when prescribing. In case of concomitant administration with itraconazole, the dose of these drugs should be reduced, if necessary.
- Direct anticoagulants;
- HIV protease inhibitors such as ritonavir, indinavir, saquinavir;
- Some anticancer drugs, such as periwinkle alkaloids, busulfan, docetaxel, trimetrexate;
- CYP3A4 isoenzyme-metabolized calcium channel blockers such as verapamil and dihydropyridine derivatives;
- Some immunosuppressive agents: cyclosporine, tacrolimus, sirolimus (also known as rapamycin);
- Some CYP3A4 isoenzyme metabolized HMG-CoA reductase inhibitors such as atorvastatin;
- Some glucocorticosteroids, such as budesonide, dexamethasone, and methylprednisolone;
- Other drugs: Digoxin, carbamazepine, buspirone alfentanil, alprazolam, brotizolam, intravenous midazolam, rifabutin, ebastine, reboxetine, cilostazol, disoliramide, eletriptan, halofantrine, repaglinide.
The interaction between itraconazole and zidovudine and fluvastatin was not found.
There was no effect of itraconazole on the metabolism of ethinylestradiol and norethisterone.
The effect on plasma protein binding.
In vitro studies have demonstrated no interaction between itraconazole and drugs such as imipramine, propranolol, diazepam, cimetidine, indomethacin, tolbutamide and sulfamethazine in binding to plasma proteins.
Special Instructions
Women of childbearing age taking Itraconazole should use reliable methods of contraception throughout the course of treatment until their first menstrual period after completion of treatment.
Itraconazole has been found to have a negative inotropic effect. Caution should be exercised when concomitant administration of itraconazole and calcium channel blockers, which may have the same effect. There have been reported cases of chronic heart failure associated with taking Itraconazole.
Itraconazole should not be taken in patients with chronic heart failure or with the presence of this disease in the history, except in cases when the possible benefit significantly exceeds the potential risk. Factors such as severity of indications, dosing regimen, and individual risk factors for chronic heart failure should be taken into consideration when evaluating the benefit-risk ratio on an individual basis.
Risk factors include the presence of heart disease, such as coronary heart disease or valve lesions; serious lung disease, such as obstructive lung disease; and renal failure or other conditions accompanied by edema. Such patients should be informed about the signs and symptoms of congestive heart failure. Treatment should be performed with caution, and the patient should be monitored for signs of congestive heart failure. If they appear, Itraconazole should be discontinued.
In reduced gastric acidity: in this condition, absorption of Itraconazole from the capsules is impaired. Patients taking antacids (e.g., aluminum hydroxide) should use them not earlier than 2 hours after taking Itraconazole capsules. In patients with achlorhydria or who use H2-histamine receptor blockers and proton pump inhibitors, it is recommended to take Itraconazole capsules with drinks containing cola.
In very rare cases during the use of Itraconazole severe toxic liver damage developed, including cases of acute hepatic failure with fatal outcome. In most cases this was observed in patients who already had liver disease, in patients with other severe diseases who received itraconazole therapy for systemic indications, as well as in patients who received other medicinal products 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 occurred in the first week of treatment. In this regard, it is recommended to monitor regularly the liver function in patients receiving itraconazole therapy. 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.
In case of appearance of these symptoms it is necessary to stop therapy immediately and conduct liver function tests. Patients with elevated concentration of “liver” enzymes or liver disease in active phase, or in patients with past toxic liver damage while taking other drugs should not be administered treatment with Itraconazole unless the expected benefits justify the risk of liver damage. In these cases it is necessary to monitor the concentration of “liver” enzymes during treatment.
Hepatic disorders: Itraconazole is metabolized mainly in the liver. As the total half-life of itraconazole is slightly prolonged in patients with hepatic impairment, it is recommended to monitor the concentration of itraconazole in plasma and adjust the dose of the drug, if necessary.
Renal disorders: Since in patients with renal impairment the total half-life of itraconazole is slightly prolonged, it is recommended to monitor the plasma concentration of itraconazole and adjust the dose of the drug, if necessary.
Patients with immunodeficiencies: bioavailability of itraconazole in per oral administration may be reduced in some patients with impaired immunity, such as patients with neutropenia, patients with AIDS or patients who underwent surgery for organ transplantation.
Patients with systemic fungal infections that are life-threatening: Due to the pharmacokinetic characteristics, Itraconazole in capsule form is not recommended for initiating treatment of systemic mycoses that are life-threatening in patients.
AIDS patients.
The treating physician should evaluate the need for maintenance therapy in AIDS patients previously treated for systemic fungal infections such as sporotrichosis, blastomycosis, histoplasmosis, or cryptococcosis (both meningeal and nonmeningeal) who are at risk for relapse.
The clinical data on the use of Itraconazole capsules in pediatric practice are limited. Itraconazole capsules should not be administered to children unless the expected benefit exceeds the possible risk.
The treatment should be stopped if peripheral neuropathy occurs, which may be associated with the intake of Itraconazole capsules.
There are no data on cross-sensitivity to itraconazole and other azole antifungal drugs.
Effects on ability to drive and operate machinery
Itraconazole may cause dizziness and other side effects that may affect ability to drive vehicles and other machinery that require extra attention at work.
Contraindications
Hypersensitivity, chronic heart failure, including history of heart failure. history (except for treatment of life-threatening conditions); concomitant use of CYP3A4 isoenzyme substrates that prolong the QT interval (astemizole, bepridil, cisapride, dofetilide, levacetylmetadol, misolastatin, pimozide, quinidine, sertindol, terfenadine); HMG-CoA reductase inhibitors, metabolized by CYP3A4 isoenzyme (lovastatin, simvastatin); simultaneous oral administration of triazolam and midazolam, ergot alkaloids (dihydroergotamine, ergometrine, ergotamine, methylergotamine), nisoldipine, eletriptan; pregnancy, lactation.
With caution
Renal and hepatic insufficiency, peripheral neuropathy, risk factors: chronic heart failure (coronary heart disease, heart valve lesions, severe lung diseases, includingincluding chronic obstructive pulmonary disease, conditions accompanied with edema syndrome), hearing impairment, simultaneous use of slow calcium channel blockers, children and elderly.
Side effects
– Gastrointestinal tract: dyspepsia (nausea, vomiting, diarrhea, constipation, decreased appetite), abdominal pain.
Similarities
Irunin, Rumicose, Itrazol, Orungamin, Itraconazole
Weight | 0.100 kg |
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Shelf life | 3 years. |
Conditions of storage | In a dry, light-protected place at a temperature not exceeding 25 ° C. |
Manufacturer | Avva Rus, Russia |
Medication form | capsules |
Brand | Avva Rus |
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