Medoflucon

Medoflucon possesses antimycotic activity.

Indications Medoflyukon

It is used for the following violations:

• candidiasis affecting the mucous membranes in the area of the alimentary tract (mouth, throat and esophagus) or respiratory tract (candidiasis with a bronchopulmonary form), as well as oral atrophic candidiasis, affecting the mucous membranes and skin (resulting from the use of dental prostheses);
• general cryptococcal lesions in people with normal immune response and various types of immunosuppression;
• prevention of the development of candidiasis of a generalized nature or its therapy (which affects a variety of organs of candidiasis of disseminated nature or candidemia);
• Candidiasis of the genital location (balanitis or vaginal), having a chronic or acute nature;
• affecting different parts of the epidermis of mycosis: in the groin, on the feet and body; deprive of scaly form, and besides this, the candidal form of epidermal infections;
• deep-seated mycosis of the endemic type in individuals with healthy immunity: Darling's disease, coccidioidosis, and Schenk's disease;
• preventing the appearance of fungal infections in people with malignant tumors (during chemotherapy or radiotherapy).

Release form

The release of the drug substance is produced in capsules with a volume of 50, as well as 100 or 150 mg. In the box - 7 or 10 capsules.

It is also sold in the form of an infusion fluid of 2 mg / ml, inside a bottle of glass, having 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 conversion of lanosterol to the ergosterol component, and in addition to this increase in the permeability of the cell walls and the breakdown of the processes of reproduction and growth of fungi.

If you compare fluconazole with itraconazole, econazole, and ketoconazole and clotrimazole, it has a much weaker effect on oxidation that occurs inside the liver with the participation of the enzyme hemoprotein P450. Does not possess antiadrogenic activity. The drug works well in the treatment of opportunistic mycosis, triggered by the activities of coccidioids immitis, dextr, non-destructive, abstr. Character).

Pharmacokinetics

After ingestion, fluconazole is absorbed at high speed inside the gastrointestinal tract; eating food 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 size of the dosage).

Fluconazole has a rather low level of synthesis with blood protein - about 15%. The substance passes inside almost all body fluids and tissues, and its values inside mother's milk, saliva, sputum, joint fluid and vaginal secretions are similar to blood.

The half-life is approximately 30 hours. Inside the liver, fluconazole slows down the activity of CYP2C9 isoenzyme. Excretion is carried out through the kidneys - mostly in an unchanged state (a small part is displayed under the guise of metabolic products).

Dosing and administration

The drug should be administered through an IV drip, intravenously, or taken orally in portions, which are selected based on the nature and severity of mycotic lesions. It is necessary to use capsules once a day; infusion administered at low speed (less than 20 mg / minute), intravenously (supplemented with 20% dextrose liquid, Hartman solution or Ringer, or NaCl and sodium bicarbonate).

In the case of cryptococcal lesions, candidiasis of disseminated nature or candidemia, intravenous or oral use is required - on the first day in a dose of 0.5 g, and then at a dosage of 0.2-0.4 g 1 time per day. The course duration is selected, taking into account the mycological and clinical effects of drugs.

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

During thrush, the medicine is taken orally - 1 time per dose of 0.15 g.

For epidermal infections (mycoses in the area of the feet, smooth skin or groin), it is necessary to apply 0.15 g of drug 1 time per week or 1 time per day in a 50 mg dose. The duration of therapy is 0.5-1 month (if necessary, the cycle can be extended up to 1.5 months).

During the depriving of the scaly form, the drug is used in a portion of 0.3 g 1-fold per week (in a 2-week period). With severe stages of the disease need another weekly dosage of 0.3 g.

In people with AIDS, in order to prevent exacerbations of the oropharyngeal form of candidiasis, Medoflucon is taken orally 1 times a week in a portion of 0.15 g.

Persons with an endemic form of mycosis, which has a deep character, require the introduction of 0.2-0.4 g of the substance per day for a long time (up to 24 months).

Patients with liver disorders in severe need to adjust the dosage portions.

To prevent the occurrence of candidiasis, the oral dose of drugs varies depending on the severity of the risk of infection with mycotic infection and ranges from 50-400 mg 1 time per day.

Use Medoflyukon during pregnancy

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

Contraindications

It is contraindicated for people with intolerance regarding the drug, as well as in combination with substances with a strong hepatotoxic effect.

Caution is needed in the following situations:

• liver disease;
• with the development of rashes;
• persons with fungal lesions of a superficial nature;
• electrolyte balance disorder;
• cardiac pathologies of organic type.

Side effects Medoflyukon

Among the side effects are:

• nausea, abdominal pain, loss of appetite, diarrhea or obstipation and bloating; occasionally there are disorders in the liver;
• headaches or dizziness, as well as fast and severe fatigue;
• leuko- or thrombocytopenia, and in addition agranulocytosis;
• local signs of allergy (erythema of an exudative nature or epidermal rashes);
• hypokalemia, hair loss and hypercholesterolemia.

Overdose

Using too high dosages of Medoflucon can cause paranoid behavior or hallucinations.

Interactions with other drugs

The combined use of the drug with terfenadine, astemizole or cisapride increases blood parameters and increases the likelihood of severe arrhythmias (among them, paroxysms associated with ventricular tachycardia).

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

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

Simultaneous use with diuretics (for example, hydrochlorothiazide) can increase the blood values of fluconazole by up to 40%.

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

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

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

Very carefully the drug is prescribed in combination with medicines, whose metabolism is carried out with the participation of hemoprotein P450 isoenzymes.

Do not mix drug infusion with solutions of other substances.

Storage conditions

Medoflucon must be maintained at temperature elevations in the range of 15-25 ° C.

Shelf life

Medoflucon capsules can be used within a 4-year term from the time of manufacture of the drug, and the solution has a shelf life of 36 months.

Application for children

Do not use Medoflucon in pediatrics (up to the 18th anniversary).

Analogs

Analogues of the drug are the substances Difluzol, Mikosist, Flunol, as well as Nofung with Vero-Fluconazole and Mikomax. In addition, Diflazon, Flucosan, Fluzol with Diflucan, Flucomycide with Flucostat, Procanazole and Fluconazole are on the list. In addition to them, Mikoflukan, Funzol, Flukonorm, Flukozid with Flusenil, Flucomabol and Forkan with Fluoral, as well as Tsiskan, Fungolon and Flucoric with Flumicon.