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Icazolum
Iconazole is an antimycotic medicine for systemic use. The active substance is itraconazole.
Indications of the icazolum
It is shown for elimination of such violations:
- pulmonary or other localized blastomycosis;
- Darling's disease (pulmonary cavity in a chronic degree, disseminated, as well as non-meningeans);
- pulmonary or other localized aspergillosis in people who are unresponsive or hypersensitive to treatment with amphotericin B;
- onychomycosis, which is provoked by the action of dermatophytes (may be accompanied by a nail lesion or not).
Pharmacodynamics
Itraconazole inhibits the activity of hemoprotein P450 - a dependent process of binding of ergosterol, the most important element of membranes of fungal cells.
The active component also inhibits the activity of Blastomyces dermatidis, histoplasmus capsulatum, Histoplasma duboisii, aspergillus yellow, aspergillus smoking, Candida albicans, and in addition Cryptococcus neoformans. In addition, Sporothrix schenckii, fungi of the genus Trichophyton, Candida krusei and other bacteria of the genus Candida.
The effect of the bioactive decay product (hydroxyitraconazole) on the activity of Blastomyces dermatidis and histoplasma capsulatum has not been determined.
Pharmacokinetics
The peak bioavailability of the active substance is observed in the case of drugs immediately after ingestion. With a single use, the peak of the plasma values of itraconazole is observed after 3-4 hours.
Metabolism of the component occurs in the liver, mainly with the help of the element CYP3A4, resulting in the formation of a variety of derivatives, one of which (hydroxyitraconazole) has antimycotic properties almost comparable to the action of itraconazole.
Synthesis of itraconazole with plasma protein is 99.8%, and the value of hydroxyitraconazole is 99.5%.
From the plasma substance is excreted into 2 phases. The final half-life is 1-1.5 days. Excretion of the initial active component through the kidneys is <0.03% of the dose used. About 40% of the dosage is excreted in the form of inactive decay products along with urine. The total fraction of each of the deduced decay products is not more than 5%. The indicator of the initial active component output from the feces is within 3-18% of the dosage used.
Use of the icazolum during pregnancy
For the treatment of fungi, the drug is given to pregnant women only if the need for its use is higher than the possible risk from its use.
In pregnancy, it is forbidden to use Iconazole to eliminate onychomycosis (but also during pregnancy planning). Before starting treatment for this disease, women of reproductive age should take care of effective contraception. You need to use medicines from the 2-3rd day of the next normal cycle of menstruation. Use contraception should be the entire period of treatment Ikonazol, and then for another 2 months after its completion.
The drug enters the mother's milk, which means that for the period of the course of treatment it is required to refuse breastfeeding.
Contraindications
Among the contraindications:
- use together with individual drugs (cisapride, astemizole, as well as terfenadine, and in addition to midazolam and triazolam for oral use);
- use with HMG-CoA reductase inhibitors (eg, such as lovastatin or simvastatin) metabolized with the P450-ZA4 system (during the period of their use, Ikonazol should be discontinued);
- childhood.
Side effects of the icazolum
Most often, because of the capsules, such adverse reactions develop: nausea, dyspepsia, constipation, abdominal pain, and in addition an increase in the activity of transaminases inside the blood. Occasionally, hepatitis may develop (as a result of prolonged treatment).
In addition, headaches, swelling, rising blood pressure, leuko- or thrombocytopenia, heart failure, polyneuropathy, alopecia, and dysmenorrhea may occur. In addition, the lungs can swell.
Perhaps the emergence of such allergic manifestations: itching, rashes, edema Quincke, urticaria. There is information about the rare cases of the development of Stevens-Johnson syndrome, and besides this anaphylaxis.
Dosing and administration
To ensure that the drug is completely absorbed into the body, it is required to take the capsule along with the food.
To eliminate blastomycosis, you should drink the drug at a dosage of 100 mg once a day to 200 mg twice a day. This course should last for six months.
When histoplasmosis is eliminated, the dosage ranges from 200 mg once a day to 200 mg twice a day. The duration of the therapeutic course is 8 months.
Therapy for aspergillosis - appoint capsules at a rate of 200 mg once a day, and with the development of a disseminated or invasive form of the pathology, the dosage is increased to twice the use of drugs in the amount of 200 mg. The duration of therapy is 2-5 months.
With onychomycosis, you need to drink the drug 200 mg once a day for 12 weeks without taking breaks.
In people who have immune system disorders (eg, after organ transplantation, either with AIDS or neutropenia), there may be a need to increase the dosage size.
Interactions with other drugs
Itraconazole prolongs the action of digoxin with indirect anticoagulants, and in addition to cyclosporin A, warfarin, vincristine, and methylprednisolone with calcium channel blockers.
Itraconazole together with its main product of decomposition hydroxyitraconazole are inhibitors of the hemoprotein enzyme system P450 ZA4. The combination with drugs, the metabolism of which is also carried out with the help of the above system, can increase or prolong the medicinal effect of these drugs and provoke the development of negative reactions. Because of this, for the period of taking Ikonazol, it is necessary to cancel the use of such medications.
It is forbidden to combine with astemizole, terfenadine, and cisapride.
When combined with phenytoin or rifampicin, the level of bioavailability of itraconazole is reduced.