Itraconazole
What is it?
Itraconazole is an azole antifungal that is used in the treatment of various types of fungal infections, both superficial and systemic. Itraconazole is an azole-type antifungal that performs its fungicidal activity by interfering with the synthesis of ergosterol.
Ergosterol is a sterol that makes up the plasma membrane of fungal cells.
Itraconazole - like all azole antifungals - inhibits one of the key enzymes in the synthesis of the aforementioned ergosterol: 14α-demethylase. Inhibiting this enzyme results in an accumulation of ergosterol precursors within the fungal cell.
The ergosterol precursors - when they reach too high levels in the cell - become toxic to the cell itself and cause alterations in the permeability of the cell membrane and in the functioning of the proteins it contains. In this way, the fungal cell is condemned to death.
When is this procedure indicated?
The use of itraconazole is indicated for the treatment of:
- candidiasis of the mouth, throat, and genitals;
- fungal infections of the skin and nails;
- lymphocutaneous sporotrichosis;
- paracoccidioidomycosis;
- blastomycosis;
- histoplasmosis;
- invasive aspergillosis in cases where amphotericin B (another antifungal) cannot be administered.
How is it performed?
Itraconazole is available for oral administration (as capsules and oral solution) and for intravenous administration (as concentrate for solution for infusion). For the success of the therapy, it is recommended to scrupulously follow the indications provided by the doctor, both with regard to the quantity of drug to be taken, and with regard to the duration of therapy itself.
Generally, the usual orally administered dose of itraconazole is 100-400 mg, taken once or twice a day. The amount of medication to be administered, the frequency of administration and the duration of treatment depend on the type of fungal infection to be treated and its severity.
Contraindications
Itraconazole can cause various types of side effects, although not all patients experience them. This is due to the different sensitivity each individual has to the drug. Therefore, it is not necessarily the case that all adverse effects occur with the same intensity in each person. Below are the main side effects that may occur during treatment with the drug.
Allergic reactions:
- Angioedema;
- Skin rashes;
- Eye disorders;
- Serum sickness;
Hemolymphopoietic system disorders
Treatment with itraconazole may cause:
- Leukopenia, which is a decrease in the number of leukocytes in the bloodstream;
- Neutropenia, which is the decrease in the number of neutrophils in the bloodstream;
- Plateletopenia, which is a decrease in the number of platelets in the bloodstream.
Nervous system disorders
Itraconazole therapy may lead to the onset of:
- Headaches;
- Dizziness;
- Paresthesia;
- Hypoesthesia;
- Peripheral neuropathy;
- Alterations of the sense of taste.
Eye diseases
Treatment with itraconazole may cause visual disturbances, such as blurred vision and diplopia.
Ear Diseases
Therapy with itraconazole may cause tinnitus (i.e., a hearing disorder characterized by the perception of buzzing, whistling, rattling, etc.) and may cause temporary or permanent hearing loss.
Gastrointestinal disorders
Treatment with itraconazole may cause:
- Stomach Pain;
- Nausea;
- Vomiting;
- Diarrhea or constipation;
- Indigestion;
- Flatulence;
- Pancreatitis.
Skin and subcutaneous tissue disorders
During itraconazole therapy, the following may occur:
- Skin rashes;
- Photosensitivity reactions;
- Hair loss;
- Ulcerations of the oral cavity;
- Stevens-Johnson Syndrome;
- Toxic Epidermal Necrolysis.
Kidney and urinary tract disorders
Treatment with itraconazole may cause an increase in the frequency of urination and may lead to urinary incontinence.
Reproductive system disorders
Therapy with itraconazole may cause menstrual cycle alterations and erectile dysfunction.
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