Fluconazole - a drug that has a pronounced anti-fungal effect. The mechanism of action of the drug fluconazole is to inhibit the enzymatic activity of fungal cytochrome P450-dependent.
As a result, blocks the process of transformation of fungal cells in the lanosterol ergosterol, increased permeability of the membrane of the cell wall, it inhibited the replication and growth
. However Fluconazole has selective activity and inhibits enzymes similar to human cells, so the treatment is safe enough fluconazole
. The drug has no anti-androgenic action
. It has high activity in the case of opportunistic fungal infections
. Perhaps the use of fluconazole prophylaxis of fungal complications in cancer patients treated with cytotoxic drugs, as well as in transplantation and other situations when the background of reduced immunity may join a fungal infection
. When applied according to the instructions Fluconazole has a very powerful anti-fungal exposure
. The high efficiency of the preparation and reviews of saying fluconazole by general practitioners
Fluconazole has a high absorption. Eating does not affect the absorption of the drug. Bioavailability - 90%. The amount of 11-12% bound to plasma proteins. Fluconazole concentration in plasma is directly proportional to dose. The drug penetrates well into all body fluid. Fluconazole concentration in synovial fluid, breast milk, peritoneal fluid, sputum, saliva similar to that in plasma. The high concentration of the drug in the vaginal secretions is achieved after 8 hours after administration and maintained at therapeutic levels for at least a day, that allows to apply Fluconazole treatment of vaginal candidiasis.
The pharmacokinetics of the drug depends on the state of the glomerular apparatus of the kidneys, and the half-life of Fluconazole is inversely proportional to creatinine clearance.
Indications for fluconazole
The instructions are listed to fluconazole indications for its use:
- various fungal infections: Cryptococcosis, including cryptococcal meningitis, systemic candidiasis, and mucosal candidiasis, vaginal candidiasis;
- prevention of fungal complications in patients on the background of immunosuppression (cytostatic treatment, radiotherapy, receiving immunosuppressive drugs).
Contraindications to fluconazole
According to the instructions Fluconazole should not be used under the following conditions:
- pregnancy, lactation;
- age up to 16 years;
- hypersensitivity to antifungal drugs in history.
Caution should be used when Fluconazole liver failure, simultaneous reception terfinadina potentially proaritmogennoe conditions caused by organic cardiac disorders, electrolyte imbalance, taking medications that can cause an arrhythmia.
In the treatment of fluconazole side effects are rare. This phenomena such as nausea, bloating, diarrhea, hyperbilirubinemia, dizziness, headache, leukopenia, neutropenia, agranulocytosis, skin rash, atrial fibrillation / ventricular flutter.
At fluconazole for instructions overdose is unlikely. In overdose developing paranoid behavior, hallucinations.
The dosage and mode of administration of fluconazole
According to the instructions Fluconazole is used for oral and intravenous administration.
A preparation for parenteral administration is in the form 0, 2% solution for oral application - in the form of capsules containing 50, 100, 150 and 200 mg of active substance. Fluconazole long half-life, in connection with which the drug is used 1 time per day. The therapeutic dose varies 200-400mg. When Candida lesions of the mucous membranes of the dose is 50-100mg per day in the case of bacterial candidiasis - 150mg. In each clinical situation, the dosage of the drug selects only the doctor.
In the treatment of fluconazole is necessary to monitor hematologic parameters. Treatment should be continued until the condition of clinical remission. Initiate therapy with fluconazole can be no culture results, but with the results of the survey method, if necessary, the adjustment of the fungicidal treatment.
Fluconazole Interaction with other drugs
Fluconazole increases the activity of coumarin anticoagulants, the concentration of zidovudine, cyclosporine, rifabutin, prolongs the half-life of theophylline, increases the plasma concentration of midazolam. This should be considered in the appointment of the drug.
Reviews of fluconazole
Due to the high fungicidal activity reviews of fluconazole by physicians and patients taking it are positive. The efficacy demonstrated in several clinical trials. The drug has minimal liver toxicity, and caused them to cease hyperbilirubinemia after drug treatment, that is completely reversible.
Fluconazole drug should be stored at room temperature, protected from sunlight place.
Be sure to read the instructions in detail to fluconazole before starting treatment with this drug.