Sporanox is a pharmacological agent with antifungal activity; its chemical structure is a triazole derivative. Available in capsules with a dosage of 100 mg. The capsules contain the active substance Itraconazole. Itraconazole has a wide degree of activity against many fungal diseases affecting the skin and the hair. The drug leads to a violation of the synthesis of the cell wall of the fungus. It happens due to inhibition of P450-dependent enzymes and, consequently, a violation of the synthesis of ergosterol, one of the wall's main components.
The medication is taken orally. The maximum concentration is observed 3.5-4 hours after administration. Itraconazole has a high bond with plasma proteins and high permeability into organs. The therapeutic dose of the drug remains in the skin three weeks after the completed course of treatment, which usually lasts about one month. Metabolism occurs in the liver, where the main metabolite is hydroxy itraconazole. Excretion of the drug occurs in 2 stages. The first stage is excretion through the kidneys, namely 35% of metabolites and only 0.03% of the unchanged substance. The second stage takes place through the intestines. Here, from 3 to 18% of the active substance is excreted. Dialysis does not help remove the drug.
Sporanox is effective against all types of mycoses.
These include cryptococcosis, aspergillosis, candidiasis of the skin and mucous membranes, blastomycosis, sporotrichosis, tinea versicolor, histoplasmosis, dermatomycosis caused by molds and yeasts, onychomycosis, fungal keratitis, and others. It is effective even against serious diseases such as meningitis, but it is recommended to use it only if the first line of drugs is ineffective.
The absorption of the drug increases when taken after meals. Therefore, the medicine is recommended to be taken orally, after meals, with water, without chewing. In some sources, it can be found that the drug is recommended to be taken with acidic drinks.
The dosage is selected individually for each patient, taking into account age, history, chronic diseases, and type of disease. On average, dosages of 100-200 mg are prescribed 2-3 times a day.
It is possible to assess the result of treatment only a month after the cessation of therapy for mycoses. In the case of onychomycosis, only after complete nail plate renewal, which lasts up to 9-10 months.
All side effects can be attributed to itraconazole overdose. The following actions can relieve an overdose: supportive therapy, gastric lavage with sodium bicarbonate solution, activated charcoal. Hemodialysis is not effective.
• Pregnancy and lactation; • Children under three years old; • Coadministration with lovastatin, simvastatin, triazolam, terfenadine, cisapride, quinidine, dofetilide, astemizole, mizolastine, methadone; • Individual intolerance to the components; • Taking methadone; • Pulmonary edema.
Sporanox is prohibited during pregnancy or breastfeeding. In the conducted clinical studies, congenital anomalies were noted: malformations, chromosomal mutations, pathology of the organs of vision and the bone-articular system, cardiovascular, urogenital.
During the period of treatment, women who may become pregnant must use reliable barrier contraception.
The drug passes into breast milk. Therefore, breastfeeding must be stopped during the treatment period.
The drug affects liver cells. Hence it can be observed: increased liver enzymes, jaundice, abdominal pain, nausea, vomiting, constipation. It rarely leads to the development of hepatitis.
Itraconazole reduces the ejection fraction of the heart from the left ventricle. Hence, during treatment, edema of the legs can appear, stagnation in the pulmonary circulation, and pulmonary edema.
Moreover, Sporanox can cause headaches and dizziness. In case of a reaction to the components, Sporanox can cause an allergic reaction in hives, rash, and itching.
With long-term treatment, the potassium level in the blood should be checked since the drug can cause hypokalemia and dysmenorrhea, and hair loss.
Sporanox capsules are metabolized in the liver and are an inhibitor of the CYP3A4 isoenzyme. It means that all drugs are metabolized by the same enzyme or have a specific effect on each other. The following list of drugs also affects the pharmacokinetics of itraconazole.
The following drugs reduce the concentration of Sporanox in the blood: • Medicines used to reduce gastric acidity (antacids, proton pump inhibitors, antagonists of H2-histamine receptors). All of them contribute to the malabsorption of itraconazole. Recommendation: apply 2 hours after or 1 hour before taking itraconazole. • Inducers of the P450 enzyme, specifically the CYP3A4 isoenzyme. • Antibiotics used to treat tuberculosis: rifampicin, isoniazid, rifabutin. • Medicines used for seizures: carbamazepine, phenobarbital, phenytoin. • Antiviral drugs: efavirenz, nevirapine.
Recommendations: avoid taking these drugs at once, and it is also not recommended to start intracostal treatment within 14 days after taking one of the drugs.
Drugs that can increase the concentration of Sporanox: • Antibiotics of the tetracycline series and fluoroquinolones: ciprofloxacin, clarithromycin, erythromycin. • Antiviral drugs: darunavir, ritonavir, fosamprenavir, indinavir, and telaprevir.
Itraconazole also affects the following drugs: terfenadine, astemizole, bepridil, mizolastine, cisapride, dofetilide, quinidine, pimozide, sertindole, levomethadone and can lead to an increase in the QT interval and ventricular tachyarrhythmias, including with ventricular tachycardia.
Due to the negative inotropic effect, the drug can lead to chronic heart failure (HF), especially at a dosage of 400 mg/day. The higher the dose, the higher the likelihood of developing HF. For the same reason, the use in persons with a history of heart failure is not recommended. Risk factors for developing heart failures such as coronary artery disease, obstructive pulmonary disease, renal disease and myocardial infarction should also be taken into account. In the case of existing risk factors, the patient must be informed about the signs and symptoms of the disease. When the first signs appear, stop treatment immediately.
It should also be noted that the reduced acidity of gastric juice (achlorhydria) interferes with the absorption of the drug.
Use of medication for liver failure. The drug, in rare cases, has a toxic effect on patients who already have damaged liver. Most often, problems began after a month of therapy. In this case, control over the liver functions is imperative, and if symptoms of hepatitis occur, such as weakness, abdominal pain, nausea, vomiting, anorexia, dark urine, yellowness of the sclera, it is necessary to stop treatment.
Use for renal failure. When using Sporanox, patients with renal insufficiency require medical supervision to control the concentration of the drug in the blood plasma and dose adjustment.
The drug concentration decreases in patients with an immunodeficiency state and those who have undergone surgery for organ transplantation.
Use of the drug in pediatric practice. There are not enough data from clinical trials. Usage is not recommended.
There was evidence of hearing loss in patients taking itraconazole, especially often against the background of joint administration with quinidine. In some cases, the hearing restores after completion of therapy, but there were also irreversible cases.
Effects on vehicle driving. However, dizziness, visual impairment, and hearing loss happen. Therefore, if unwanted symptoms appear, the patient should refuse to drive a vehicle.
Aspergillosis is a type of mycosis caused by Aspergillus molds. A person becomes infected through inhalation of fungal spores, hyphae are formed, and germination into blood vessels occurs. The disease transmits through the air.
It can enter the human body through damaged skin. The disease ranks first among all mycoses. Molds are found in soil, air, and even distilled water. The pathogen gets inside through ventilation, air conditioners, humidifiers, books, pillows, showers, inhalers, construction dust, spices, herbs, and much more.
The disease affects the internal organs, manifests itself as an allergic reaction, but also is asymptomatic. The reaction in all patients is different and depends on the immune system, chronic diseases, Etc. Symptoms are similar to bronchial asthma, pneumonia, sinusitis, and even rapidly progressing systemic diseases. Patients may complain of nasal congestion, epistaxis, asthma, nasal polyps, allergic rhinitis, chest pain, cough, wheezing, headaches, and fever without antipyretics.
Types of disease: • Aspergillosis of the skin; • Aspergillosis of the bones; • Bronchopulmonary; • ENT organs; • Invasive; • Eye; • Allergic; • Septic.
Chronic forms are secondary. The disease often lies on already having lung lesions, such as abscesses or bronchiectasis.
Sometimes patients notice the smell of mold from the mouth, green lumps in the sputum. On x-ray, it seems like a filled cavity in the form of a shadow with a spherical shape.
Risk factors: • Neutropenia (decrease in neutrophils for more than a week); • Long-term corticosteroid therapy; • Transplantation; • Chronic granulomatosis and other hereditary diseases are associated with a decrease in neutrophils.
The disease is widespread in AIDS patients. It develops most often already in the expanded stage. Most often, it starts with a pulmonary form, which then turns into a septic form. The disease has a severe course and is fatal. It is possible to save only those patients who retain at least some immune function.
Aspergillosis is diagnosed clinically by topography, chest x-ray, histopathology of tissue samples, and determination of galactomannan antigen in serum and bronchoalveolar lavage samples.
A person with aspergillosis poses no danger to other people. A person who has recovered develops immunity, but it is not persistent.
Antifungal therapy is essential. The following drugs are used: voriconazole, amphotericin B, itraconazole, etc. Aspergillomas do not respond to systemic antifungal therapy, so surgical treatment is required.
As for the treatment of aspergillosis with folk remedies, there is evidence that herbs can be used as an additional treatment. If you open sources for herbal medicine, it is possible to find data on the successful cure of birch tar. Healers recommend the use of flax seeds, birch leaves, cherry branches, wormwood.
Treatment of pulmonary and generalized septic forms of the disease is difficult to treat. If there is a limited infiltration, then lobectomy is successfully applied. In most cases, the operation takes place without complications with good long-term results without relapses. When distributed, they are used in conjunction with conservative therapy, prescribing iodine preparations with increasing doses.
• Maintaining an optimal humidity level; • Particular attention to cleanliness in bathrooms and toilets, since it is here that high humidity is observed; • Keep the refrigerator clean, regularly clean it of spoiled food, wash the shelves and sections. Aspergillosis of the skin and mucous membranes is the most favorable form. The pulmonary form of the disease is hazardous, and in 30% of cases, it is fatal. If the patient has an immunodeficiency in addition to the disease, the statistics grow to 50%. The septic form is the most unfavorable.
Aspergillosis is a disease that requires special attention, especially against the background of reduced immunity. It can often be confused with allergic diseases. A thorough medical examination by a specialist is necessary. It should also be noted that people who work with pigeons are especially susceptible to the disease. It is also necessary to consider the appearance of dampness and try to prevent it by monitoring the optimal humidity in the house. Optimum humidity ranges from 40% to 60%. Aspergillus is found everywhere, but if a person has good immunity, the usual concentrations will not be enough for infection.