Mechanism of action
Antifungal. Diflucan is an inhibitor of sterol synthesis in the cell of fungi. Blocks a number of cytochrome P450 dependent enzymes and stops the synthesis of sterols in the cells of fungi.
Indications and usage
Candidiasis (generalized, disseminated, oropharyngeal, vaginal, mucous membranes, skin, nails), cryptococcosis, candidaemia, prevention of candidiasis in various groups of patients.
Diflucan therapy can be started before the results of seeding and other laboratory tests. However, anti-infective therapy needs to be changed accordingly, when the results of these studies become known.
The daily dose of Fluconazole depends on the nature and severity of the fungal infection. In vaginal candidiasis in most cases, a single dose of the drug is effective. In case of infections requiring repeated use of the antifungal drug, treatment should be continued until the clinical or laboratory signs of an active fungal infection disappear. Patients with AIDS and cryptococcal meningitis or recurrent oropharyngeal candidiasis usually need supportive therapy to prevent recurrence of the infection.
Inside or in / in by infusion at a rate of not more than 10 ml / min; the choice of route of administration depends on the clinical condition of the patient. For adults with cryptococcal meningitis and cryptococcal infections of other localization on the first day - usually 400 mg, and then - 200-400 mg 1 time per day. The duration of treatment of cryptococcal infections depends on the presence of clinical and mycological effect; with cryptococcal meningitis - 6-8 weeks.
To prevent the recurrence of cryptococcal meningitis in AIDS patients, after completing the full course of primary treatment, therapy with fluconazole at a dose of 200 mg / day can be continued for a very long time.
For candidemia, disseminated candidiasis and other invasive candidal infections - usually 400 mg in the first day, and then at 200 mg / day. Depending on the severity of the clinical effect, the dose may be increased to 400 mg / day. The duration of therapy depends on the clinical effectiveness.
When oropharyngeal candidiasis - usually 50–100 mg once a day for 7–14 days. If necessary, in patients with marked suppression of immune function, treatment can be continued for a longer time. In case of atrophic oral candidiasis associated with the wearing of dentures, 50 mg 1 time per day for 14 days in combination with local antiseptic agents for the treatment of the prosthesis.
For other candidal infections of the mucous membranes (with the exception of genital candidiasis, seebelow), for example, esophagitis, non-invasive bronchopulmonary infections, candiduria, candidiasis of the skin and mucous membranes, etc., the effective dose is usually 50–100 mg / day for a 14–30 day treatment.
For the prevention of recurrence of oropharyngeal candidiasis in patients with AIDS, after completing the full course of primary therapy, fluconazole may be given 150 mg once a week.
With vaginal candidiasis - once, by mouth, in a dose of 150 mg. To reduce the frequency of recurrences of vaginal candidiasis - 150 mg 1 time per month. Some patients may need more frequent use. The duration of therapy is 4–12 months.
With balanitis caused by Candida, - once in a dose of 150 mg orally.
For the prevention of candidiasis - 50-400 mg 1 time per day, depending on the degree of risk of a fungal infection. If there is a high risk of generalized infection, for example, in patients with expected severe or prolonged neutropenia, 400 mg 1 time per day. Fluconazole is prescribed a few days before the expected appearance of neutropenia; after increasing the number of neutrophils over 1000 in mm3 treatment continues for 7 days.
With infections of the skin, including mycoses of the feet, smooth skin, inguinal region and candidal infections - 150 mg once a week or 50 mg once a day. The duration of therapy in normal cases is 2–4 weeks, however, with mycoses of the feet, longer therapy may be required (up to 6 weeks). When pityriasis lichen - 300 mg 1 time per week for 2 weeks; some patients require a third dose of 300 mg per week, but in some cases, a single dose of 300–400 mg is sufficient. An alternative treatment regimen is the use of the drug 50 mg 1 time per day for 2-4 weeks.
With onychomycosis - 150 mg once a week. Treatment should be continued until the infected nail is replaced (the uninfected nail grows). Normally, it takes 3–6 months and 6–12 months to re-grow nails on the fingers and feet, respectively. However, the growth rate can vary widely among different people, as well as depending on age. After successful treatment of long-lasting chronic infections, a change in the shape of the nails is sometimes observed.
With deep endemic mycoses - at a dose of 200-400 mg / day for up to 2 years. The duration of therapy is determined individually: with coccidiomycosis - 11–24 months, with paracoccidioidomycosis - 2–17 months, with sporotrichosis - 1–16 months, with histoplasmosis - 3–17 months.
Children. As with similar infections in adults, the duration of treatment depends on the clinical and mycological effect. In children should not be used in a daily dose greater than that in adults. Fluconazole is used daily 1 time per day.
With candidiasis of the mucous membranes - 3 mg / kg / day. On the first day, a loading dose of 6 mg / kg can be given in order to more quickly achieve a constant equilibrium concentration.
For the treatment of generalized candidiasis and cryptococcal infection - 6–12 mg / kg / day, depending on the severity of the disease.
For the prevention of fungal infections in immunocompromised patients, in whom the risk of developing an infection is associated with neutropenia developing as a result of cytotoxic Chemotherapy or radiation therapy - 3–12 mg / kg / day depending on the severity and duration of persistence of induced neutropenia (see adult dosage).
Children aged 4 weeks or less. In the first 2 weeks of life - the same dose (in mg / kg) as in older children, but with an interval of 72 hours; 3-4 weeks - the same dose with an interval of 48 hours.
Patients with renal insufficiency. With a single dose change is not required. In patients (including children) with impaired renal function, with repeated use of the drug, a loading dose of from 50 to 400 mg should be initially administered. After the administration of the loading dose, the daily dose (depending on the indication) is determined according to the following table.
|Creatinine clearance, ml / min
||The percentage of the recommended dose
|<50 (without dialysis)
|Patients who are constantly on dialysis
||100% after each dialysis
To prepare the oral suspension, shake the bottle to loosen the powder, add 24 ml of water and shake well. Before each use, the vial with suspension for oral administration must be shaken.
When transferring a patient from intravenous administration to oral administration of the drug or vice versa, a change in daily dose is not required. Fluconazole for iv administration is contained in a 0.9% solution of sodium chloride; every 200 mg (100 ml bottle) contains 15 mmol of Na+ and Cl-. Since fluconazole is available as an isotonic saline solution, in patients who need to limit sodium or fluid intake, it is necessary to consider the rate of fluid administration.
Nausea, vomiting, abdominal pain, flatulence, diarrhea, rash, headache; in very rare cases, against the background of other serious diseases - changes in liver and kidney function, convulsions, leukopenia, thrombocytopenia, alopecia, exfoliative skin (Stevens-Johnson syndrome, toxic epidermal necrolysis) and Anaphylactic reactions .
- simultaneous use of cisapride;
- simultaneous use of terfenadine and astemizole;
- Hypersensitivity to the drug or azole substances close to it in chemical structure.
The use of Diflucan during pregnancy should be avoided, except in cases of severe and potentially life-threatening fungal infections, when the expected benefit of treatment outweighs the possible risk to the fetus.
Diflucan (Fluconazole) is found in breast milk in the same concentrations as in the blood, so it is not recommended to use Diflucan during lactation (breastfeeding).
In rare cases, the use of fluconazole was accompanied by toxic changes in the liver, including fatal, mainly in patients with serious concomitant diseases. In the case of the development of hepatotoxic effects associated with fluconazole, they are not marked by an obvious dependence on the total daily dose, duration of therapy, sex and age of the patient.The hepatotoxic effect of fluconazole has usually been reversible; his symptoms disappeared after cessation of therapy. It is necessary to observe patients in whom indicators of liver function are disturbed during treatment with fluconazole in order to detect signs of more serious liver damage. If clinical signs of liver damage appear that may be associated with fluconazole, the drug should be withdrawn.
During treatment with fluconazole, patients rarely developed exfoliative skin reactions, such as Stevens-Johnson syndrome and toxic epidermal necrolysis. AIDS patients are more likely to develop severe skin reactions with the use of many drugs. When a rash appears to be associated with fluconazole in a patient receiving treatment for a superficial fungal infection, the drug should be discontinued. When a rash appears in patients with invasive / systemic fungal infections, they should be carefully monitored and fluconazole should be canceled when there is a bullous lesion or erythema multiforme.
It should be borne in mind that the use of the drug in rare cases anaphylactic reactions were noted.
In the treatment of vaginal candidiasis Diflucan in the form of capsules 150 mg may be dispensed from pharmacies without a prescription.
Influence on ability to drive motor transport and control mechanisms
Experience with fluconazole suggests that the deterioration of the ability to drive and mechanisms associated with the drug, it is unlikely.
Enhances the effects of anticoagulants, sulfonylurea drugs, hydrochlorothiazide, phenytoin, increases plasma concentrations of cyclosporine, theophylline, zidovudine; elimination of Diflucan accelerates rifampicin.
The drug should be stored at a temperature not exceeding 30 ° C, out of the reach of children.
Shelf life of capsules and solution for intravenous administration - 5 years. The shelf life of the powder for the preparation of suspensions for oral administration is 3 years. The shelf life of the finished suspension is 14 days; the suspension should be protected from freezing.
Pharmacy sales terms
The drug is available by prescription, 150 mg capsules - without a doctor's prescription (only in the treatment of vaginal candidiasis).