DIFLUCAN POWDER FOR SUSPENSION 50MG/5ML 35ML BOTTLE

Dosage form

Powder for suspension for oral administration

Composition

5 ml ready slurry. contain <strong.Fluconazole 50 mg;
excipients: sucrose, colloidal silicon, titanium dioxide, xanthan gum, sodium citrate, citric acid, sodium benzoate, natural orange additive

Packaging

60 ml bottle (volume of the finished suspension 35 ml).

Mechanism of action

Diflucan - antifungal drug, a representative of a new class of triazole antifungal agents, is a powerful selective inhibitor of sterol synthesis in the cell of fungi.
When administered and with a / in the introduction of fluconazole has been effective in various models of fungal infections in animals. The activity of the drug was demonstrated in opportunistic mycoses, incl. caused by Candida spp., including generalized candidiasis in immunocompromised animals; Cryptococcus neoformans, including intracranial infections; Microsporum spp. and Trychoptyton spp. Fluconazole activity has also been shown in animal models of endemic mycoses, including infections caused by Blastomyces dermatitides, Coccidioides immitis, including intracranial infections, and Histoplasma capsulatum in animals with normal and reduced immunity.
Fluconazole therapy at 50 mg / day for up to 28 days did not affect the plasma testosterone concentration in men or the steroid concentration in women of childbearing age. Fluconazole at a dose of 200-400 mg / day did not have a clinically significant effect on the levels of endogenous steroids and their response to stimulation of ACTH in healthy male volunteers.
There have been reports of cases of superinfection caused by Candida albicans strains other than Candida albicans, which are often not sensitive to fluconazole (for example, Candida krusei). In such cases, alternative antifungal therapy may be required.

Indications and usage

- cryptococcosis, including cryptococcal meningitis and infections of other localization (for example, lungs, skin). Treatment can be carried out in patients with a normal immune response and in AIDS patients, recipients of transplanted organs and patients with other forms of immunodeficiency.Fluconazole can be used for maintenance therapy to prevent the recurrence of cryptococcosis in AIDS patients;
- generalized candidiasis, including candidaemia, disseminated candidiasis and other forms of invasive candidal infection. These include infections of the peritoneum, endocardium, eyes, respiratory and urinary tract. Treatment can be carried out in patients with malignant tumors, patients in intensive care units, patients receiving cytotoxic or immunosuppressive agents, as well as in the presence of other factors predisposing to the development of candidiasis;
- Candidiasis of mucous membranes, incl. oral cavity and pharynx, esophagus, non-invasive bronchopulmonary infections, candiduria, mucocutaneous and chronic oral atrophic candidiasis (associated with the wearing of dental prostheses). Treatment can be carried out in patients with normal and with reduced immunity. Prevention of recurrent oropharyngeal candidiasis in AIDS patients;
- genital candidiasis. vaginal candidiasis, acute or recurrent. Preventive use in order to reduce the frequency of recurrences of vaginal candidiasis (3 or more episodes per year). Candida balanitis;
- prevention of fungal infections in patients with malignant tumors that are predisposed to their development as a result of cytotoxic Chemotherapy or radiation therapy;
- mycoses of the skin, including mycoses of the feet, body, inguinal region, pityriasis versicolor, onychomycosis, and skin candidal infections;
- deep endemic mycoses, coccidioidomycosis, paracoccidioidomycosis, sporotrichosis and histoplasmosis in patients with normal immunity.

Contraindications

Simultaneous use of cisapride; simultaneous use of terfenadine and astemizole; Hypersensitivity to the drug or azole substances close to it in chemical structure.

Pregnancy and Breastfeeding

The use of fluconazole 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.
Fluconazole is found in breast milk in the same concentrations as in blood, therefore it is not recommended to use Diflucan during lactation (breastfeeding).

Dosage and administration

Treatment can begin before the results of seeding and other laboratory tests. However, the 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.
With vaginal candidiasis in most cases, a single dose of the drug is effective.
For infections that require repeated use of an antifungal drug, treatment should be continued until the clinical or laboratory signs of a fungal infection disappear. Patients with AIDS and cryptococcal meningitis or recurrent oropharyngeal candidiasis usually need supportive therapy to prevent recurrence of the infection.
Adults with cryptococcal meningitis and cryptococcal infections another localization on the first day is prescribed on average 400 mg, and then continue the treatment in a dose of 200-400 mg 1 time / day. The duration of treatment of cryptococcal infections depends on the presence of clinical and mycological effect; with cryptococcal meningitis, it is usually continued for at least 6-8 weeks.
To prevent the recurrence of cryptococcal meningitis in AIDS patientsAfter completion of the full course of primary treatment, therapy with fluconazole at a dose of 200 mg / day can be continued for a very long time.
In candidaemia, disseminated candidiasis and other invasive candidal infections, the dose averages 400 mg on the first day, and then 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 the drug is prescribed on average 50-100 mg 1 time / day for 7-14 days. If necessary, in patients with a pronounced decrease in immunity, treatment can be continued for a longer time. In case of atrophic oral candidiasis associated with the wearing of dentures, the drug is prescribed in an average dose of 50 mg 1 time / 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), for example, esophagitis, non-invasive bronchopulmonary infections, candiduria, candidiasis of the skin and mucous membranes, the effective dose averages 50-100 mg / day for a duration of treatment of 14-30 days.
For the prevention of recurrence of oropharyngeal candidiasis in AIDS patients After completion of the full course of primary therapy, fluconazole can be administered 150 mg 1 time / week.
With vaginal candidiasis Fluconazole is taken once by mouth in a dose of 150 mg.
To reduce the frequency of recurrences of vaginal candidiasis the drug can be used in a dose of 150 mg 1 time / month. The duration of therapy is determined individually; it varies from 4 to 12 months. Some patients may need more frequent use.
With balanitis caused by Candida, fluconazole administered once a dose of 150 mg orally.
For the prevention of candidiasis The recommended dose of fluconazole is 50-400 mg 1 time / day, depending on the degree of risk of developing a fungal infection. If there is a high risk of generalized infection, for example, in patients with expected severe or prolonged neutropenia, the recommended dose is 400 mg 1 time / day. Fluconazole is prescribed a few days before the expected appearance of neutropenia; after an increase in the number of neutrophils of more than 1000 / μl, the treatment is continued for another 7 days.
With skin infections, including mycoses of the feet, smooth skin, inguinal area and candidal infections, the recommended dose is 150 mg 1 time / week. or 50 mg 1 time / 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).
With pityriasis versicolor The recommended dose is 300 mg 1 time / week. within 2 weeks; some patients require a third dose of 300 mg / week, while 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 / day for 2-4 weeks.
With onychomycosis The recommended dose is 150 mg 1 time / 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, respectively, to re-grow nails on the fingers and feet. 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 may require the use of the drug in a dose of 200-400 mg / day for up to 2 years. The duration of therapy is determined individually; it is 11–24 months for coccidioidomycosis, 2–17 months for paracoccidiomycosis, 1–16 months for sporotrichosis and 3–17 months for histoplasmosis.

In children, as with similar infections in adults, the duration of treatment depends on the clinical and mycological effect. In children, the drug should not be used in a daily dose in excess of that in adults.Fluconazole is used daily 1 time / day.
With candidiasis of the mucous membranes The recommended dose of fluconazole is 3 mg / kg / day. On the first day, a loading dose of 6 mg / kg can be given in order to more quickly achieve constant equilibrium concentrations.
For treatmentgeneralized candidiasis and cryptococcal infection The recommended dose is 6-12 mg / kg / day, depending on the severity of the disease.
For the prevention of fungal infections in patients with reduced immunity, in which the risk of developing an infection is associated with neutropenia, developing as a result of cytotoxic chemotherapy or radiation therapy, the drug is prescribed at 3-12 mg / kg / day, depending on the severity and duration of persistence of induced neutropenia.
When using the drug in children aged 4 weeks or less, it should be borne in mind that in newborns fluconazole is eliminated slowly. In the first 2 weeks of life, the drug is prescribed in the same dose (in mg / kg) as the older children, but with an interval of 72 hours. Children at the age of 3 and 4 weeks of life are given the same dose with an interval of 48 hours.
In elderly patients, in the absence of signs of renal failure, the drug is used in an average dose.

Diflucan can be taken orally or administered intravenously 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. When transferring a patient with a / in the introduction to the reception of the drug inside or vice versa, the change in daily dose is not required.
Capsules should be swallowed whole.
When preparing the suspension for ingestion, shake the bottle first to loosen the powder, then add 24 ml of water, then shake the bottle thoroughly again. Immediately before use, the suspension should be shaken.

The most common side effects that have been reported in fluconazole clinical trials.
From the side of the central nervous system: headache.
Dermatological reactions: rash.
From the digestive system: abdominal pain, diarrhea, flatulence, nausea, toxic effect on the liver (including rare cases with fatal outcome), increased levels of alkaline phosphatase, bilirubin, increased serum levels of aminotransferases (ALT and AST).
In some patients, especially with serious diseases (AIDS, malignant neoplasms), with treatment with fluconazole and similar drugs, changes in blood parameters, kidney and liver function were observed, however, the clinical significance of these changes and their relationship to treatment have not been established.
In the process of widespread use the following side effects are additionally registered.
From the side of the central nervous system and peripheral nervous system: dizziness, convulsions.
Dermatological reactions: alopecia, exfoliative skin diseases, including Stevens-Johnson syndrome, Lyell's syndrome (toxic epidermal necrolysis).
From the digestive system: dyspepsia, vomiting, abnormal liver function, hepatitis, hepatocyte necrosis, jaundice, increased serum ALT and AST levels.
From the hemopoietic system: leukopenia, including neutropenia and agranulocytosis, thrombocytopenia.
Metabolism: increased plasma cholesterol and triglycerides, hypokalemia.
Allergic reactions: Anaphylactic reactions, angioedema, swelling of the face, itching.
Other: change in taste.

In rare cases, the use of fluconazole was accompanied by toxic changes in the liver, including fatal, mainly in patients with serious concomitant diseases. There is no marked dependence of the incidence of hepatotoxic effects of fluconazole 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.
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.

The drug should be stored at a temperature not exceeding 30 ° C, out of the reach of children.