What is Diflucan, where is it used?
Diflucan is most often used for fungal skin diseases (affecting the legs, torso and other locations). It relieves well the symptoms of candidal damage to the oral cavity in adults. The drug is indicated to eliminate signs of cryptococcal meningitis.
The drug is actively used in gynecology for the treatment of fungal vaginosis in women. It is also in demand in the treatment of candidal balanitis (damage to the mucous membrane of the glans penis).
The medication for adult patients can be used as a prophylactic for cryptococcal meningitis, candidiasis of the skin and mucous membranes, including in people with neutropenia, reduced immune status (cancer patients, HIV-infected people, and so on).
In pediatrics, the drug is used for:
- Candidiasis of the oral mucosa;
- Inflammation of brain tissue caused by the fungus cryptococcus (more often occurs in patients with immunodeficiencies);
- Prevention of candidal damage to organs and tissues in patients with reduced immunity;
- Prevention of meningitis caused by cryptococcus.
For children, the drug is prescribed only by a doctor.
Diflucan capsules - instructions
Capsules are taken orally. It must be swallowed whole with liquid. The effectiveness of the medicine does not depend on food intake.
Adults
Depending on the disease, the drug should be used in different doses. How long can you take Diflucan, in what dosages:
- Meningitis and other diseases caused by cryptococcus - 200-400 mg per day; course therapy is 1.5-2 months. In some cases, you can increase the daily dosage to 800 mg;
- Prevention of relapse of cryptococcal infection - 200 mg per day; The duration of preventive therapy is determined by the doctor.
- Coccidioidomycosis - 200-400 mg per day (sometimes 800 mg). The duration of therapy in some cases reaches 2 years.
- Common candidiasis - 800 mg per day (1 day); further shown 400 mg per day. The course of therapy is up to 2 weeks after the disappearance of symptoms and the first negative blood culture.
The drug treats damage to the mucous membranes. Depending on the location of the damage, treatment tactics will differ:
- Fungal infection of the oral cavity and pharynx - 200-400 mg per day, then 100-200 mg/day. The duration of therapy is up to 3 weeks.
- Atrophic candidiasis of the oral cavity - 50 mg/day for 2 weeks.
- Fungal infection of mucous membranes and skin - 50-100 mg/day for a month.
- Damage to the esophagus - 200-400 mg initial dosage, on the second and subsequent days 100-200 mg/day; course therapy is 2-4 weeks;
- Prevention of candidiasis of the oral mucosa in patients with HIV - 100-200 mg/day or 200 mg three times a day; The duration of treatment is determined individually depending on the severity of HIV symptoms and the duration of the underlying disease.
- Vaginal infection with candida fungus - 150 mg once; then, to prevent the onset of the disease, drink 150 mg every three days (three dosages), then maintenance therapy - 150 mg/week. for 3-6 months.
The medicine effectively copes with fungal diseases of the skin. Treatment regimens for various skin diseases:
- Infectious pathologies of the skin, including dermatophytosis of the legs and torso - 150 mg per week or 50 mg once per day. The duration of course therapy is 14-28 days. If the patient's feet are affected, the duration of treatment is 1.5 months.
- Lichen versicolor - 300-400 mg per week for 1-3 weeks, or 50 mg once per day for 14-28 days.
- Onychomycosis - 150 mg once a week; Therapy continues until the entire nail is renewed.
- Prevention of the occurrence of fungal pathologies in patients with tumor processes - 200-400 mg per day. Therapy is carried out until neutropenia appears; as soon as the number of blood neutrophils has risen to 1000 mm3, treatment begins again for 7 days.
How should children take Diflucan?
For children, the drug is prescribed only by a pediatrician or a specialized specialist who is caring for the child. You should not take the medication yourself. The dosage of the medicine should not be higher than for an adult patient.
The prescribed dose is indicated to be taken once a day. Dosages:
- Damage to mucous membranes - 3 mg/kg/day; on the first day, a high dosage is allowed - 6 mg/kg/day;
- Invasive candidiasis, brain inflammation caused by cryptococcus - 6-12 mg/kg/day; re-exacerbation in HIV patients can be prevented with a dose of 6 mg/kg/day;
- Prevention of fungal infections in neutropenia, immunodeficiencies, cancer pathologies - 3-12 mg/kg/day.
The medication is prescribed only to those children who know how to take capsules. If the child is unable to swallow the encapsulated drug, another antifungal agent is selected for him (in the form of a powder for suspension).
Diflucan for children
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.
Interaction
Fluconazole interacts with a large number of drugs. It is prohibited to take it with the following medications: Cisapride, Pimozide, Terfenadine, Astemizole, Quinidine, Erythromycin, Amiodarone. The combination of these medications and fluconazole is life-threatening.
Fluconazole should be used very carefully with the following medications:
- Hydrochlorothiazide,
- Rifampicin,
- Alfentanil,
- Amitriptyline, nortriptyline,
- Amphotericin B,
- Anticoagulants,
- Azithromycin,
- Benzodiazepines,
- Calcium channel blockers,
- Cyclosporine,
- Cyclophosphamide,
- Fentanyl and other drugs, according to the instructions.
Restrictions on use
The medication has absolute and relative contraindications. The absolute ones include:
- Allergic reaction to the components of the product;
- Simultaneous use with Terfenadine, Cisapride, Astemizole, Erythromycin, Pimozide, Quinidine, Amiodarone;
- Lactase deficiency;
- Children under 3 years of age.
Relative restrictions include:
- Insufficient kidney and liver function;
- The appearance of rashes due to common fungal infections;
- Presence of heart pathologies, electrolyte disturbances;
- Use of fluconazole less than 400 mg and terfenadine simultaneously.
Attention! The drug should only be prescribed by a doctor; if the drug is used incorrectly, complications may occur.
Description of the drug FLUCONAZOLE
When used simultaneously with warfarin, fluconazole increases prothrombin time (by 12%), and therefore bleeding may develop (hematomas, bleeding from the nose and gastrointestinal tract, hematuria, melena). In patients receiving coumarin anticoagulants, prothrombin time must be constantly monitored.
After oral administration of midazolam, fluconazole significantly increases midazolam concentrations and psychomotor effects, and this effect is more pronounced after fluconazole is administered orally than when administered intravenously. If concomitant benzodiazepine therapy is necessary, patients taking fluconazole should be monitored for an appropriate benzodiazepine dose reduction.
With the simultaneous use of fluconazole and cisapride, adverse reactions from the heart are possible, incl. ventricular fibrillation/flutter (ari). The use of fluconazole at a dose of 200 mg 1 time / day and cisapride at a dose of 20 mg 4 times / day leads to a marked increase in plasma concentrations of cisapride and an increase in the QT interval on the ECG. Concomitant use of cisapride and fluconazole is contraindicated.
In patients after kidney transplantation, the use of fluconazole at a dose of 200 mg/day leads to a slow increase in cyclosporine concentrations. However, with repeated doses of fluconazole at a dose of 100 mg/day, no changes in cyclosporine concentrations were observed in bone marrow recipients. When using fluconazole and cyclosporine concomitantly, it is recommended to monitor the concentration of cyclosporine in the blood.
Repeated use of hydrochlorothiazide simultaneously with fluconazole leads to an increase in plasma concentrations of fluconazole by 40%. An effect of this magnitude does not require a change in the fluconazole dosage regimen in patients receiving concomitant diuretics, but this should be taken into account.
With the simultaneous use of a combined oral contraceptive with fluconazole at a dose of 50 mg, no significant effect on hormone levels has been established, while with daily intake of 200 mg of fluconazole, the AUC of ethinyl estradiol and levonorgestrel increases by 40% and 24%, respectively, and when taking 300 mg of fluconazole 1 time per day week - AUC of ethinyl estradiol and norethindrone increase by 24% and 13%, respectively. Thus, repeated use of fluconazole in the indicated doses is unlikely to affect the effectiveness of the combined oral contraceptive.
Concomitant use of fluconazole and phenytoin may be accompanied by a clinically significant increase in phenytoin concentrations. With this combination, phenytoin concentrations should be monitored and the dose adjusted accordingly to ensure therapeutic serum concentrations.
Concomitant use of fluconazole and rifabutin may lead to increased serum concentrations of the latter. Cases of uveitis have been described with the simultaneous use of fluconazole and rifabutin. Patients receiving rifabutin and fluconazole concomitantly should be monitored closely.
The simultaneous use of fluconazole and rifampicin leads to a decrease in AUC by 25% and the duration of T1/2 of fluconazole by 20%. In patients concomitantly taking rifampicin, the advisability of increasing the dose of fluconazole must be considered.
Fluconazole, when taken simultaneously, leads to an increase in T1/2 of oral sulfonylurea drugs (chlorpropamide, glibenclamide, glipizide and tolbutamide). In patients with diabetes mellitus, fluconazole and oral sulfonylureas can be prescribed together, but the possibility of hypoglycemia should be taken into account.
The simultaneous use of fluconazole and tacrolimus leads to an increase in plasma concentrations of the latter. Cases of nephrotoxicity have been described. Patients with this combination should be carefully monitored.
With the simultaneous use of azole antifungals and terfenadine, serious arrhythmias may occur as a result of an increase in the QT interval. When taking fluconazole at a dose of 200 mg/day, an increase in the QT interval has not been established, however, the use of fluconazole at doses of 400 mg/day and above causes a significant increase in the concentration of terfenadine in plasma. Concomitant use of fluconazole in doses of 400 mg/day or more with terfenadine is contraindicated. Treatment with fluconazole in doses less than 400 mg/day in combination with terfenadine should be carried out under close monitoring.
When used simultaneously with fluconazole at a dose of 200 mg for 14 days, the average rate of plasma clearance of theophylline is reduced by 18%. When prescribing fluconazole to patients taking high doses of theophylline or to patients at increased risk of developing theophylline toxicity, monitor for symptoms of theophylline overdose and, if necessary, adjust therapy accordingly.
When used simultaneously with fluconazole, an increase in zidovudine concentrations is observed, which is likely due to a decrease in the metabolism of the latter to its main metabolite. Before and after therapy with fluconazole at a dose of 200 mg/day for 15 days in patients with AIDS and ARC (AIDS-related complex), a significant increase in the AUC of zidovudine (20%) was found.
When zidovudine 200 mg every 8 hours for 7 days was used in HIV-infected patients with or without fluconazole 400 mg/day with an interval of 21 days between the two regimens, a significant increase in zidovudine AUC was found (74%) when used simultaneously with fluconazole. Patients receiving this combination should be monitored for side effects of zidovudine.
The simultaneous use of fluconazole with astemizole or other drugs whose metabolism is carried out by isoenzymes of the cytochrome P450 system may be accompanied by an increase in serum concentrations of these drugs. Patients with such combinations should be carefully monitored.
