Orungamin, 100 mg capsules 14 pcs
€26.12 €21.77
Itraconazole is a synthetic broad-spectrum antifungal agent, a triazole derivative. It inhibits ergosterol synthesis of the cell membrane of fungi, which determines the antifungal effect of the drug.
Itraconazole is active against:
- dermatophytes (Trichophyton spp, Microsporum spp, Epidermophyton floccosum),
- dermatophyte fungi Candida spp. (including Candida albicans, Candida parapsilosis),
- Mould fungi (Cryptococcus neoformans, Aspergillus spp, Trichosporon spp., Geotrichum spp., Penicillium mameffei, Pseudallescheria boydii, Histoplasma spp., Coccidioides immitis, Paracoccidioides braziliensis, Sporothrix schenckii. Fonsecaea spp., Cladosporium spp., Blastomyces dermatidis), Malassezia spp..
Some strains may be resistant to itraconazole: C. glabrata, C. krusei, C. tropicalis, Absidia spp, Fusarium spp., Mucor spp., Rhizomucor spp. Rhizopus spp., Scedosporium proliferans, Scopulariopsis spp. The efficacy of treatment was evaluated in 2-4 weeks after cessation of therapy (for systemic mycoses), in 6-9 months. – for onychomycosis (as the nails change).
Pharmacokinetics
In oral administration the maximum bioavailability of itraconazole is observed when taking capsules immediately after meals. Maximal concentration in plasma is reached during 3-3.5 hours after oral administration and is 28.34 ng/ml. During prolonged use, the equilibrium concentration is reached within 1-2 weeks. Itraconazole is 99.8% bound to plasma proteins. The concentration of itraconazole in blood is 60% of the concentration in plasma. Accumulation of the drug in keratinous tissues, especially in the skin, is about 4 times higher than its accumulation in plasma, and its excretion rate depends on the regeneration of the epidermis.
In contrast to plasma concentrations, which are undetectable as early as 7 days after discontinuation of therapy, therapeutic concentrations in the skin persist for 2-4 weeks after discontinuation of a 4-week course of treatment. Itraconazole is detectable in nail keratin as early as 1 week after the start of treatment and persists for at least 6 months after the completion of the 3-month course of therapy. Itraconazole is also detected in skin fat and, to a lesser extent, in sweat.
Itraconazole is well distributed in tissues that are susceptible to fungal lesions. Concentrations in lungs, kidneys, liver, bones, stomach, spleen and muscles were 2-3 times higher than the corresponding concentrations in plasma. Therapeutic concentrations in vaginal tissues remained for 2 days after the end of 3 days’ treatment in a dose of 200 mg twice a day, and for 3 days after the end of one day’s treatment in a dose of 200 mg twice a day. Itraconazole is metabolized in the liver with the formation of active metabolites, including hydroxyitraconazole. It is an inhibitor of CYP3A4, CYP3A5 and CYP3A7 isoenzymes.
Extraction from plasma is biphasic: by kidney within 1 week (35% as metabolites). During 1 week (35% as metabolites, 0.03% – unchanged) and through intestine (3-18% unchanged). The elimination half-life is 1-1.5 days. It is not eliminated during dialysis.
Indications
– lesions of the skin and mucous membranes:
Active ingredient
How to take, the dosage
Interaction
Medicinal products affecting absorption of itraconazole.
Drugs that reduce the acidity of gastric juice interfere with the absorption of itraconazole, which is associated with the solubility of the capsule shells.
Drugs that affect the metabolism of itraconazole.
Itraconazole is mainly metabolized with participation of CYP3A4 isoenzyme. In concomitant use with rifampicin, rifabutin, phenytoin, which are potent inducers of CYP3A4 isoenzyme, bioavailability of itraconazole and hydroxyitraconazole decreases significantly that leads to a significant reduction of drug efficacy. Concomitant use of itraconazole with these drugs, which are potential inducers of microsomal hepatic enzymes, is not recommended.
Powerful inhibitors of CYP3A4 isoenzyme, such as ritonavir, indinavir, clarithromycin and erythromycin, may increase the bioavailability of itraconazole.
The effect of itraconazole on the metabolism of other drugs:
Itraconazole may inhibit the metabolism of drugs that are substrates of CYP3A isoenzymes. This may result in intensification or prolongation of their effects, including side effects. If concomitant drugs are used, it is necessary to study the information concerning their metabolism. After discontinuation of treatment, plasma concentrations of itraconazole decrease gradually, depending on the dose and duration of treatment (see section “Pharmacokinetics”). This should be taken into account when assessing the inhibitory effect of itraconazole on the metabolism of concomitantly administered drugs.
Medicinal products which are not recommended to be prescribed concomitantly with itraconazole:
– Terfenadine, astemizole, bepridil, misolastin, cisapride, dofetilide, quinidine, pimozide, sertindol, levacetylmetadol, HMG-CoA reductase inhibitors such as simvastatin and lovastatin.
– Oral midazolam and triazolam.
– Drugs with ergot alkaloids such as dihydroergotamine, ergometrine, ergotamine and methylergometrine.
– Nisoldipine
– Slow calcium channel blockers may have a negative inotropic effect, which is enhanced when taken simultaneously with itraconazole. Concomitant use of itraconazole and “slow” calcium channel blockers requires caution, because metabolism of “slow” calcium channel blockers may be reduced.
Drugs in concomitant administration of which it is recommended to monitor their plasma concentrations, effects, side effects.
The dose of these drugs should be reduced if necessary.
– indirect anticoagulants;
– HIV protease inhibitors (ritonavir, indinavir, saquinavir);
– some anticancer drugs (alkaloids of periwinkle pink, including vincristine and vinblastine; Busulfan, docetaxel, trimetrexate);
– slow calcium channel blockers metabolized by CYP3A4 isoenzyme (verapamil and dihydropyridine derivatives);
– some immunosuppressive agents (cyclosporine, tacrolimus, sirolimus);
– some HMG-CoA reductase inhibitors metabolized by CYP3A4 isoenzyme (atorvastatin);
– some glucocorticosteroids (budesonide, dexamethasone, fluticasone and methylprednisolone);
Special Instructions
– To prevent reinfection it is necessary to simultaneously treat sexual partners and observe personal hygiene. It is recommended to abstain from sexual intercourse during the treatment period. If signs of infection persist after completion of treatment, repeat microbiological examination to confirm the diagnosis.
– The effectiveness of itraconazole for the treatment of fungal infections with severe neutropenia is unknown, so in these cases the drug should be used only if 1st-line therapy is ineffective.
If risk factors for chronic heart failure occur (coronary heart disease, heart valve disease, severe lung disease including chronic obstructive pulmonary disease, conditions accompanied by edema) during itraconazole therapy should be stopped.
– Transient and permanent deafness has been reported in some patients while taking itraconazole.
– 1 orongamin capsule contains 4 bread units (BE).
Contraindications
1. Hypersensitivity to itraconazole or excipients.
2. Chronic heart failure, including a history of heart failure (except for treatment of life-threatening conditions).
3. Concurrent use of the following medications:
4. children under 3 years of age.
5. fructose intolerance, sugar/isomaltase deficiency, glucose-galactose malabsorption.
WARNING – renal/liver failure, peripheral neuropathy, risk factors for chronic heart failure (coronary heart disease, heart valve defects, severe lung disease including chronic obstructive pulmonary disease, conditions accompanied with edema syndrome), hearing impairment, concurrent use of “slow” calcium channel blockers, childhood and old age.
Side effects
Blood organs: leukopenia, neutropenia, thrombocytopenia.
Allergic reactions: serum sickness, angioedema, anaphylactic and anaphylactoid reactions, hypersensitivity.
Skin disorders: toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis, leukoclastic vasculitis, alopecia, photosensitization, urticaria, rash, itching.
Metabolism disorders: hypertriglyceridemia, hypokalemia.
Nervous system disorders: peripheral neuropathy, paresthesia, hypoesthesia, dizziness.
Sight and hearing disorders: visual disturbances including blurring and diplopia, tinnitus, transient or permanent deafness.
Cardiovascular system disorders: congestive heart failure.
Respiratory system: pulmonary edema.
Digestive system disorders: abdominal pain, vomiting, nausea, diarrhea, impaired sense of taste, increased activity of “liver” enzymes; dyspepsia, constipation, hepatitis, hyperbilirubinemia; hepatotoxicity, acute liver failure.
Motor system disorders: myalgia, arthralgia.
Urogenital system disorders: pollakiuria, urinary incontinence, menstrual cycle disorders, erectile dysfunction.
Others: edema.
Overdose
There are no data available. In case of accidental overdose, gastric lavage should be performed within the first hour after taking the drug, take activated charcoal.
Symptomatic treatment. Hemodialysis is not effective. There is no specific antidote.
Similarities
Weight | 0.021 kg |
---|---|
Shelf life | 3 years. Do not use after the expiry date |
Conditions of storage | Store in a dry, light-protected place at a temperature not exceeding 25°C. Store in a place out of the reach of children. |
Manufacturer | Ozon, Russia |
Medication form | capsules |
Brand | Ozon |
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