Iconazole

Iconazole is an antifungal drug for systemic use. The active substance is itraconazole.

Indications Iconazole

It is indicated for the elimination of such disorders:

• pulmonary or other localized blastomycosis;
• Darling's disease (pulmonary cavitary form in chronic stage, disseminated, and also non-meningeal forms);
• pulmonary or other localized aspergillosis in people who are refractory or hypersensitive to treatment with amphotericin B;
• onychomycosis, which is caused by the action of dermatophytes (may or may not be accompanied by nail damage).

Release form

Available in capsules. One strip contains 4 pieces.

Pharmacodynamics

Itraconazole inhibits the activity of hemoprotein P450-dependent process of binding ergosterol, the most important element of fungal cell membranes.

The active component also inhibits the activity of Blastomyces dermatidis, Histoplasma capsulatum, Histoplasma duboisii, Aspergillus lutea, Aspergillus fuming, Candida albicans, and in addition to 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 breakdown 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 drug administration immediately after meals. With a single use, the peak plasma indicators of itraconazole are observed after 3-4 hours.

The component is metabolized in the liver, mainly via the CYP3A4 element, resulting in the formation of many derivatives, one of which (hydroxyitraconazole) has antifungal properties almost comparable to those of itraconazole.

The plasma protein synthesis of itraconazole is 99.8%, and that of hydroxyitraconazole is 99.5%.

The substance is excreted from plasma in 2 phases. The terminal half-life is 1-1.5 days. Excretion of the original active component via the kidneys is <0.03% of the dose taken. About 40% of the dosage is excreted in the form of inactive decay products in the urine. The total proportion of each of all excreted decay products is no more than 5%. The indicator of the original active component excreted in the feces is within 3-18% of the dosage taken.

Dosing and administration

To ensure the medicine is fully absorbed into the body, the capsule must be taken with food.

To eliminate blastomycosis, you should take the medicine in a dosage of 100 mg once a day to 200 mg twice a day. This course should last for six months.

When eliminating histoplasmosis, 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 - capsules are prescribed in the amount of 200 mg once a day, and in the development of disseminated or invasive form of pathology, the dosage is increased to twice daily use of the drug in the amount of 200 mg. The duration of therapy is 2-5 months.

For onychomycosis, the drug should be taken 200 mg once a day for 12 weeks, without taking breaks.

People with immune system disorders (for example, after an organ transplant or with AIDS or neutropenia) may need a higher dosage.

[ 1 ]

Use Iconazole during pregnancy

For the treatment of fungi, the drug is prescribed to pregnant women only if the need for its use is greater than the possible risk from its use.

During pregnancy, it is prohibited to use Iconazole to eliminate onychomycosis (and also during pregnancy planning). Before starting treatment for this disease, women of reproductive age should take care of effective contraception. The drug should be used from the 2nd-3rd day of the next normal menstrual cycle. Contraception should be used throughout the entire course of treatment with Iconazole, and then for another 2 months after its completion.

The medicine passes into breast milk, which is why breastfeeding must be discontinued during the course of treatment.

Contraindications

Among the contraindications:

• use together with certain drugs (cisapride, astemizole, as well as terfenadine, and in addition midazolam and triazolam for oral use);
• use with HMG-CoA reductase inhibitors (such as lovastatin or simvastatin), metabolized with the participation of the P450 ZA4 system (during their use, the use of Iconazole should be discontinued);
• childhood.

Side effects Iconazole

The most common side effects that develop from taking capsules are nausea, dyspeptic symptoms, constipation, abdominal pain, and in addition, increased activity of transaminases in the blood. Rarely, hepatitis may develop (as a result of prolonged treatment).

In addition, headaches, swelling, increased blood pressure, leukopenia or thrombocytopenia, heart failure, polyneuropathy, alopecia, and dysmenorrhea may occur. In addition, the lungs may swell.

The following allergic reactions may occur: itching, rashes, Quincke's edema, urticaria. There is information about rare cases of Stevens-Johnson syndrome, and also anaphylaxis.

Interactions with other drugs

Itraconazole prolongs the effect of digoxin with indirect anticoagulants, as well as cyclosporine A, warfarin, vincristine, and methylprednisolone with calcium channel blockers.

Itraconazole, together with its main breakdown product hydroxyitraconazole, are inhibitors of the hemoprotein P450 3A4 enzyme system. Combination with drugs that are also metabolized by the above system may increase or prolong the medicinal effect of these drugs and provoke the development of negative reactions. For this reason, it is necessary to discontinue the use of such drugs during the period of taking Iconazole.

Contraindicated in combination with astemizole, terfenadine, and cisapride.

When used in combination with phenytoin or rifampicin, the bioavailability of itraconazole decreases.

[ 2 ], [ 3 ]

Storage conditions

The medicine is kept in a dark place, inaccessible to children. The temperature regime is within 15-25ºC.

[ 4 ]

Shelf life

Iconazole is permitted to be used for 3 years from the date of release of the drug.