Instructions for use DIFLOX

Instructions for use DIFLOX

Treatment can begin before receiving the results of the mycobiological study. However, it may be necessary to change therapy according to the results obtained.

For vaginal candidiasis

the drug is prescribed once at a dose of 150 mg.

For systemic candidiasis

patients without neutropenia and patients with stable condition with neutropenia are prescribed 400 mg/day on the first day of treatment, and 200-400 mg/day from the second day. The duration of treatment depends on the clinical picture and is at least 2 weeks after obtaining a negative culture result and disappearance of the clinical manifestations of the disease.

For candidiasis of the mucous membranes (including in patients with AIDS and other immunodeficiencies)

the drug is prescribed in a daily dose of 50-100 mg. For the first episode of the disease, treatment is continued for 7-14 days, in patients with immunodeficiency - 3 weeks. In extremely severe cases, the drug is prescribed at a dose of 100-200 mg/day for 1 month.

For cryptococcal meningitis and cryptococcal infections of other localizations

on the first day, 400 mg is prescribed, and then treatment is continued at a dose of 200-400 mg 1 time / day for 6-8 weeks.

To prevent relapse of cryptococcal meningitis in patients with AIDS

after completion of the full course of primary treatment, therapy can be continued at a dose of 200 mg/day for a long time.

For dermatomycosis

, especially those resistant to local therapy, the drug is prescribed at a dose of 50 mg/day or 150 mg once a week.
The course of treatment is 2-4 weeks, for mycosis of the feet
- up to 6 weeks.

For lichen versicolor

the drug is prescribed at 50 mg/day for 2-4 weeks.

For the prevention of candidiasis before bone marrow transplantation and before cytotoxic chemotherapy or radiation therapy in patients with malignant neoplasms

the drug is prescribed at a dose of 50-400 mg/day with further dose adjustment depending on the severity of neutropenia and the expected risk of fungal infection. Diflox is prescribed several days before the probable onset of neutropenia and treatment is continued for another 7 days after the number of neutrophils increases to 1000/μl.

In adults

in case of
impaired renal function,
the dose of the drug must be adjusted in accordance with the QC indicators.

Children with normal kidney function

for
life-threatening candidiasis,
the drug is prescribed in a daily dose of 6-12 mg/kg body weight.

For the prevention of mycoses

and
in the treatment of superficial mycoses,
the drug is prescribed in a daily dose of 3-6 mg/kg body weight. Depending on the effectiveness of the therapy, the daily dose can be increased to 12 mg/kg.

For children aged 5-13 years

the maximum daily dose is 400 mg.

Diflazon capsules 150 mg No. 1

Name

Diflazon capsules 150 mg in blisters in package No. 1

Description

Diflazone belongs to a group of medicines called "antifungal medicines". The active substance is fluconazole. The drug is used to treat fungal infections, as well as to prevent candida infections. The most common causative agents of fungal infections are yeast-like fungi - Candida.

Main active ingredient

Fluconazole

Release form

capsules

Dosage

150mg

special instructions

Treatment can be started in the absence of culture or other laboratory test results, but if they are available, appropriate adjustment of fungicidal therapy is recommended.

pharmachologic effect

Diflazon is an antifungal drug. Fluconazole, a member of the triazole antifungal class, is a powerful selective inhibitor of sterol synthesis in fungal cells. Active against pathogens of opportunistic mycoses, incl. caused by Candida spp., Cryptococcus neoformans, Microsporum spp., Trichophyton spp. Fluconazole has also been shown to be active in models of endemic mycoses, including infections caused by Blastomyces dermatitidis, Coccidioides immitis and Histoplasma capsulatum.

Pharmacodynamics

Absorption After oral administration, fluconazole is well absorbed. Bioavailability is 90%. After taking the drug orally on an empty stomach at a dose of 150 mg, Cmax is 90% of the plasma content with intravenous administration of the drug at a dose of 2.5-3.5 mg/l. Concomitant food intake does not affect oral absorption. Cmax is achieved 0.5-1.5 hours after taking fluconazole. Plasma concentration is directly proportional to the dose taken. The distribution of 90% of Css is achieved by the 4-5th day of treatment with the drug (when taken 1 time / day). Administration of a loading dose (on the 1st day), 2 times higher than the average daily dose, allows you to achieve a 90% Css level by the 2nd day. The apparent Vd approaches the total water content of the body. Protein binding - 11-12%. Fluconazole penetrates well into all body fluids. Concentrations of fluconazole in saliva and sputum are similar to its plasma levels. In patients with fungal meningitis, fluconazole levels in the cerebrospinal fluid are approximately 80% of plasma levels. In the stratum corneum, epidermis, dermis and sweat fluid, high concentrations are reached that exceed serum concentrations. Excretion Fluconazole is excreted mainly by the kidneys; approximately 80% of the administered dose is found unchanged in the urine. Fluconazole clearance is proportional to QC. No fluconazole metabolites were detected in the blood.

Indications for use

Cryptococcosis, including cryptococcal meningitis and other localizations of this infection (including lungs, skin), both in patients with a normal immune response and in patients with various forms of immunosuppression (including AIDS patients, organ transplants ); prevention of cryptococcal infection in patients with AIDS; generalized candidiasis, including candidemia, disseminated candidiasis and other forms of invasive candidal infections (infections of the peritoneum, endocardium, eyes, respiratory and urinary tract). Treatment can be carried out in patients with malignant neoplasms, patients in intensive care units and undergoing cytostatic or immunosuppressive therapy, as well as in the presence of other factors predisposing to the development of candidiasis; candidiasis of the mucous membranes, incl. oral cavity and pharynx (including atrophic candidiasis of the oral cavity associated with wearing dentures), esophagus, non-invasive bronchopulmonary candidiasis, candiduria, skin candidiasis; prevention of relapse of oropharyngeal candidiasis in patients with AIDS; genital candidiasis: vaginal candidiasis (acute and chronic recurrent), prophylactic use to reduce the frequency of relapses of vaginal candidiasis (3 or more episodes per year); candidal balanitis; prevention of fungal infections in patients with malignant neoplasms who are predisposed to such infections as a result of chemotherapy with cytostatics or radiation therapy; mycoses of the skin, including mycoses of the feet, body, and groin area; pityriasis versicolor; onychomycosis; skin candidiasis; deep endemic mycoses, including coccidioidomycosis, paracoccidioidomycosis, sporotrichosis and histoplasmosis in patients with normal immunity.

Directions for use and doses

For adults with cryptococcal meningitis and cryptococcal infections of other localization, 400 mg is prescribed on the first day, and then treatment is continued at a dose of 200-400 mg once a day. The duration of treatment for cryptococcal infections depends on clinical effectiveness confirmed by mycological research; for cryptococcal meningitis, therapy is usually continued for at least 6-8 weeks. To prevent relapse of cryptococcal meningitis in patients with AIDS, after 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 period of time. For candidemia, disseminated candidiasis and other invasive candidal infections, the dose averages 400 mg on the first day, and then 200 mg/day. If clinical effectiveness is insufficient, the dose may be increased to 400 mg/day. The duration of therapy depends on clinical effectiveness. For oropharyngeal candidiasis, the drug is prescribed on average 50-100 mg once a day; Duration of therapy is 7-14 days. If necessary, in patients with a pronounced decrease in immunity, treatment may be longer. For atrophic candidiasis of the oral cavity associated with wearing dentures, the drug is prescribed at an average dose of 50 mg once a day for 14 days in combination with local antiseptics for treating the denture. For other candidal infections (with the exception of genital candidiasis), such as esophagitis, non-invasive bronchopulmonary lesions, candiduria, candidiasis of the skin and mucous membranes, the effective dose averages 50-100 mg/day with a treatment duration of 14-30 days. To prevent relapses of oropharyngeal candidiasis in AIDS patients after completing the full course of primary therapy, fluconazole can be prescribed 150 mg once a week. For vaginal candidiasis, fluconazole is taken orally once at a dose of 150 mg. To reduce the frequency of relapses of vaginal candidiasis, the drug can be used at a dose of 150 mg once a month. The duration of therapy is determined individually; it varies from 4 to 12 months. Some patients may require more frequent use. For balanitis caused by Candida, fluconazole is prescribed as a single dose of 150 mg orally. For the prevention of candidiasis, the recommended dose of fluconazole is 50-400 mg once a 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 long-lasting neutropenia, the recommended dose is 400 mg 1 time per day. Fluconazole is prescribed several days before the expected onset of neutropenia; after the number of neutrophils increases to more than 1000/μl, treatment is continued for another 7 days. For mycoses of the skin, including mycoses of the feet, smooth skin, groin area and skin candidiasis, the recommended dose is 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 (up to 6 weeks) may be required. For pityriasis versicolor, the recommended dose is 300 mg once a week for 2 weeks; some patients require a third dose of 300 mg per week, while in some cases a single dose of 300-400 mg is sufficient. An alternative treatment regimen is to use the drug 50 mg once a day for 2-4 weeks. For onychomycosis, the recommended dose is 150 mg once a week. Treatment should be continued until the infected nail is replaced (the uninfected nail regrows). It normally takes 3-6 months and 6-12 months for fingernails and toenails to re-grow, respectively. For deep endemic mycoses, it may be necessary to use the drug at 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 paracoccidioidomycosis, 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 higher than that in adults. Diflazon is used daily 1 time/day. For 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 may be prescribed in order to more quickly achieve constant equilibrium concentrations. For the treatment of generalized 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 children with reduced immunity, in whom the risk of developing infection is associated with neutropenia developing as a result of cytotoxic chemotherapy or radiation therapy, the drug is prescribed at a dose of 3-12 mg/kg/day, depending on the severity and duration of persistence of induced neutropenia. In children with impaired renal function, the daily dose of the drug should be reduced (in the same proportion as in adults), in accordance with the severity of renal failure. In elderly patients in the absence of signs of renal failure, the usual dosage regimen should be followed. Patients with renal failure (QC Fluconazole is excreted mainly in the urine unchanged. With a single dose, no dose change is required. When re-administered to patients with impaired renal function, a loading dose of 50 mg to 400 mg should be administered. For QC>50 ml/ min, the average recommended dose of the drug is used; for CC from 11 to 50 ml/min, a dose of 50% of the recommended is used. For patients regularly on hemodialysis, one dose of the drug is administered after each hemodialysis session.

Use during pregnancy and lactation

The use of Diflazon during pregnancy is not advisable, with the exception of severe or life-threatening forms of fungal infections, if the expected benefit to the mother outweighs the possible risk to the fetus. Fluconazole is found in breast milk in the same concentration as in plasma, so the use of the drug during lactation is not recommended.

Precautionary measures

Before taking Diflazon®, tell your doctor that:

• you have problems with the liver or kidneys;
• you suffer from cardiovascular diseases, including heart rhythm disturbances;
• your blood levels of potassium, calcium and magnesium are abnormal;
• you have developed severe skin reactions (itching, redness of the skin) or difficulty breathing.

If you are not sure whether the above applies to you, consult your doctor before starting to take this drug. In some cases, your doctor may order a test to determine the type of bacteria causing the disease. Depending on the results obtained, different dosages of Diflazon® or another medicine may be prescribed.

Interaction with other drugs

When fluconazole was used with warfarin, an increase in prothrombin time by 12% was observed. In this regard, it is recommended to monitor prothrombin time in patients receiving Diflazon in combination with coumarin anticoagulants. With simultaneous use, fluconazole increases T1/2 of oral hypoglycemic drugs - sulfonylurea derivatives (chlorpropamide, glibenclamide, glipizide and tolbutamide) in healthy volunteers. Co-administration of fluconazole and oral hypoglycemic drugs is allowed, but the possibility of developing hypoglycemia should be taken into account. Concomitant use of fluconazole and phenytoin may be accompanied by an increase in phenytoin concentrations to a clinically significant extent. If concomitant use of two drugs is required, phenytoin levels should be monitored and the dose adjusted to ensure therapeutic serum concentrations. The simultaneous use of fluconazole and rifampicin leads to a decrease in AUC by 25% and a shortening of half-life of fluconazole by 20%. In patients receiving concomitant rifampicin, it is necessary to consider the advisability of increasing the dose of fluconazole. It is recommended to monitor the concentration of cyclosporine in the blood in patients receiving fluconazole, because When using fluconazole and cyclosporine in patients with a kidney transplant, taking fluconazole at a dose of 200 mg/day slowly increased the concentration of cyclosporine. Patients receiving high doses of theophylline, or who are at risk of developing theophylline toxicity, should be monitored for early detection of symptoms of theophylline overdose, as simultaneous administration of fluconazole leads to a decrease in the average rate of clearance of theophylline from plasma. With the simultaneous use of fluconazole and cisapride, cases of adverse reactions from the heart, including paroxysms of ventricular tachycardia (AR), have been described. There are reports of interaction between fluconazole and rifabutin, accompanied by an increase in serum levels of the latter. With the simultaneous use of fluconazole and rifabutin, cases of uveitis have been described. Patients receiving rifabutin and fluconazole simultaneously should be carefully monitored. With the simultaneous use of zidovudine and fluconazole, an increase in the concentration of zidovudine in plasma is observed, which is caused by a decrease in the conversion of the latter into the main metabolite, so an increase in the side effects of zidovudine should be expected.

Contraindications

Hypersensitivity to fluconazole, other components of Diflazon or other azole compounds; simultaneous use of terfenadine (while constantly taking fluconazole at a dose of 400 mg/day or more), cisapride or astemizole and other drugs that prolong the QT interval and increase the risk of developing severe arrhythmias; lactation period.

Compound

1 capsule contains: Active substance: fluconazole 150 mg; Excipients: lactose monohydrate; corn starch; anhydrous colloidal silicon dioxide; sodium lauryl sulfate; magnesium stearate.

Overdose

Symptoms: hallucinations, paranoid behavior. Treatment: gastric lavage and symptomatic therapy are recommended. Since fluconazole is excreted in the urine, forced diuresis increases its excretion. Hemodialysis for 3 hours reduces the concentration of fluconazole in plasma by 50%.

Side effect

From the digestive system: nausea, diarrhea, flatulence, vomiting, abdominal pain, change in taste, rarely - increased activity of liver enzymes and impaired liver function (jaundice, hyperbilirubinemia, increased activity of ALT, AST and alkaline phosphatase, hepatitis, hepatocellular necrosis, including .ch. with fatal outcome). From the nervous system: headache, dizziness; rarely - convulsions. From the hematopoietic organs: rarely - agranulocytosis, neutropenia. Patients with severe fungal infections may experience hematological changes (leukopenia and thrombocytopenia). From the cardiovascular system: increased duration of the QT interval on the electrocardiogram (ECG), ventricular fibrillation/flutter. Allergic reactions: skin rash, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), bronchial asthma (more often with intolerance to acetylsalicylic acid), anaphylactoid reactions (including angioedema, swelling of the face, urticaria, itching).

Storage conditions

Store out of the reach of children at a temperature not exceeding 25°C.