Medoflucon

Medoflucon has antimycotic activity.

Indications Medoflucona

It is used for the following disorders:

• candidiasis, affecting the mucous membranes in the digestive tract (mouth, pharynx and esophagus) or respiratory tract (candidiasis of the bronchopulmonary form), as well as oral candidiasis of an atrophic nature, affecting the mucous membranes and skin (arising from the use of dentures);
• generalized cryptococcal lesions in people with normal immune response and various types of immunosuppression;
• prevention of the development of generalized candidiasis or its therapy (disseminated candidiasis affecting various organs or candidemia);
• genital candidiasis (balanitis or vaginal), chronic or acute;
• mycoses affecting different parts of the epidermis: in the groin, on the feet and body; pityriasis versicolor, and also epidermal infections that have a candidal form;
• deep-seated mycoses of endemic type in individuals with healthy immunity: Darling's disease, coccidioidomycosis and Schenk's disease;
• prevention of the occurrence of fungal lesions in people with malignant tumors (during chemotherapy or radiation therapy).

Release form

The medicinal substance is released in capsules of 50, 100 or 150 mg. There are 7 or 10 capsules in a box.

It is also available as an infusion liquid of 2 mg/ml, in glass bottles with a capacity of 50 ml.

Pharmacodynamics

The drug has a strong, highly specific antimycotic effect and slows down the activity of enzymes of various fungi that depend on the hemoprotein P450. It acts by blocking the processes of converting lanosterol into the component ergosterol, and in addition to this, increasing the permeability of cell walls and disrupting the processes of reproduction and growth of fungi.

When compared with itraconazole, econazole, as well as ketoconazole and clotrimazole, fluconazole has a much weaker effect on oxidation occurring inside the liver with the participation of the enzyme hemoprotein P450. It does not have antiandrogenic activity. The drug works well in the treatment of opportunistic mycoses caused by the activity of coccidioides immitis, candida, Microsporum spp., trichophyton, Histoplasma capsulatum, as well as Cryptococcus neoformans and Blastomyces dermatidis (including generalized types of pathologies that occur with immunosuppression, intracranial lesions and endemic mycoses).

Pharmacokinetics

After oral administration, fluconazole is absorbed at high speed in the gastrointestinal tract; food intake does not change the nature of drug absorption. Bioavailability values are approximately 90%. Blood Cmax values are recorded after 60-90 minutes (directly proportional to the dosage size).

Fluconazole has a fairly low level of synthesis with blood protein - about 15%. The substance passes into almost all fluids and tissues of the body, and its values in breast milk, saliva, sputum, joint fluid and vaginal secretions are similar to blood.

The half-life is approximately 30 hours. In the liver, fluconazole slows the activity of the isoenzyme CYP2C9. Excretion occurs through the kidneys - mainly unchanged (a small part is excreted as metabolic products).

Dosing and administration

The medicine should be administered via a drip, intravenously, or taken orally in portions that are selected taking into account the nature and severity of mycotic lesions. Capsules should be taken once a day; the infusion should be administered at a low rate (less than 20 mg/minute), intravenously (supplemented with 20% dextrose liquid, Hartman or Ringer's solution, or NaCl and sodium bicarbonate).

In case of cryptococcal lesions, disseminated candidiasis or candidemia, intravenous or oral use is required - on the first day in a portion of 0.5 g, and then in a dosage of 0.2-0.4 g once a day. The duration of the course is selected taking into account the mycological and clinical effects of the drug.

People with candidal lesions of the mucous membranes need to use 50-100 mg of the substance per day, and the duration of the cycle is 15-30 days.

During thrush, the medicine is taken orally - 1 time in a portion of 0.15 g.

For epidermal infections (mycosis in the area of the feet, smooth skin or groin), 0.15 g of the drug should be used once a week or once a day in a dose of 50 mg. Duration of therapy is 0.5-1 month (if necessary, the cycle can be extended to 1.5 months).

During pityriasis versicolor, the medication is used in a dose of 0.3 g once a week (in a 2-week period). In severe stages of the disease, another weekly dosage of 0.3 g is needed.

In people with AIDS, to prevent exacerbations of the oropharyngeal form of candidiasis, Medoflucon is taken orally once a week in a dose of 0.15 g.

People with endemic mycosis of a deep nature require the administration of 0.2-0.4 g of the substance per day over a long period of time (up to 24 months).

Patients with severe liver dysfunction require dosage adjustments.

To prevent the occurrence of candidiasis, the oral dose of the drug varies depending on the degree of risk of contracting a mycotic infection and ranges from 50-400 mg once a day.

Use Medoflucona during pregnancy

It is prohibited to use the drug in pregnant or lactating women.

Contraindications

It is contraindicated for use in people with intolerance to the medication, as well as in combination with substances that have a strong hepatotoxic effect.

Caution is needed in the following situations:

• liver diseases;
• when rashes develop;
• persons with superficial fungal infections;
• disturbances in electrolyte balance indicators;
• organic cardiac pathologies.

Side effects Medoflucona

Side effects include:

• nausea, abdominal pain, loss of appetite, diarrhea or constipation and bloating; liver dysfunction is occasionally observed;
• headaches or dizziness, as well as rapid and severe fatigue;
• leukopenia or thrombocytopenia, as well as agranulocytosis;
• local signs of allergy (exudative erythema or epidermal rashes);
• hypokalemia, hair loss and hypercholesterolemia.

Overdose

Using too high doses of Medoflucon may cause paranoid behavior or hallucinations.

Interactions with other drugs

Combined use of the drug with terfenadine, astemizole or cisapride increases blood counts and increases the likelihood of severe arrhythmias (including paroxysms associated with ventricular tachycardia).

The combination of the drug with antidiabetic drugs for oral administration increases the half-life of the latter, which increases the risk of hypoglycemia.

The combination of Medoflucon and indirect anticoagulants potentiates and prolongs their effect by approximately 12% (on average).

Concomitant use with diuretics (eg, hydrochlorothiazide) may increase blood levels of fluconazole by up to 40%.

Use with theophylline increases its half-life and increases the likelihood of developing toxic symptoms.

Combination with the substance rifampicin reduces its half-life by 20%.

Use with zidovudine increases its plasma levels and the likelihood of developing its side effects.

The drug is prescribed with great caution in combination with medications whose metabolism is carried out with the participation of hemoprotein P450 isoenzymes.

Do not mix medicinal infusion with solutions of other substances.

Storage conditions

Medoflucon must be stored at temperatures in the range of 15-25°C.

Shelf life

Medoflucon capsules can be used within a 4-year period from the date of production of the drug, and the shelf life of the solution is 36 months.

Application for children

Medoflucon should not be used in pediatrics (under 18 years of age).

Analogues

The analogs of the drug are Difluzol, Mikosist, Flunol, as well as Nofung with Vero-Fluconazole and Mikomaks. In addition to this, the list includes Diflazon, Flucosan, Fluzol with Diflucan, Flucomicide with Flucostat, Prokanazol and Fluconazole. In addition to them, there are also Mikoflukan, Funzol, Fluconorm, Flucoside with Flusenil, Flucomabol and Forkan with Flukoral, as well as Tsiskan, Fungolon and Flucoric with Flumicon.