Diflazon

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Diflazon: instructions for use and reviews

1. Release form and composition
2. Pharmacodynamics and pharmacokinetics
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Pregnancy and lactation
10. Renal dysfunction
11. Liver dysfunction
12. Drug interactions
13. Analogs
14. Terms and conditions of storage
15. Terms of dispensing from pharmacies
16. Reviews
17. Price in pharmacies

Latin name: Diflazon

ATX code: J02AC01

Active ingredient: Fluconazole (Fluconazole)

Manufacturer: KRKA (Slovenia)

Description and photo update: 2019-05-08

Prices in pharmacies: from 89 rubles.

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Diflazon is an antifungal agent.

Release form and composition

Dosage forms of Diflazon:

Hard gelatin capsules: No. 4 - with a white body and a light blue lid, No. 2 - with a white body and a blue lid, No. 1 - with a body and a light blue lid, No. 0 - with a white body and a dark purple lid; capsules contain almost white or white powder (No. 4 - 7 pcs. in blisters, in a cardboard box 1 blister; No. 2 - 7 pcs. in blisters, in a cardboard box 4 blisters; No. 1 - 1, 2 or 4 pcs in blisters, in a cardboard box 1 blister; No. 0 - 7 pcs. in blisters, in a cardboard box 1 blister, or 10 pcs. in blisters, in a cardboard box 2 blisters);
Solution for infusion: clear, colorless liquid, without visible inclusions (100 ml in vials, in a cardboard box 1 vial complete with a plastic holder).

The active ingredient of Diflazon is fluconazole:

1 capsule: No. 4 - 50 mg, No. 2 - 100 mg, No. 1 - 150 mg, No. 0 - 200 mg;
1 ml of solution - 2 mg.

Auxiliary components:

Capsules: corn starch, lactose monohydrate, anhydrous colloidal silicon dioxide, magnesium stearate, sodium lauryl sulfate;
Solution: sodium chloride, water for injection.

Capsule shell composition: gelatin, titanium dioxide (E171).

In addition, in addition to the capsule shell:

Capsules No. 4 and No. 2: cap - patented blue dye (E131);
Capsules No. 1: body and lid - patented blue dye (E131);
Capsules # 0: lid - indigo carmine FD&C dyes azorubin (E122), blue (E132).

Pharmacodynamics and pharmacokinetics

Diflazone belongs to the class of triazole antifungal drugs and is a potent selective inhibitor of the fungal enzyme 14-a-demethylase and other enzymes dependent on cytochrome P ₄₅₀. The drug prevents the conversion of lanosterol into ergosterol - the main element of the cell membranes of fungi. The effectiveness of Diflazon has been proven in opportunistic mycoses, including those caused by Trichophyton spp., Candida spp. (Candida tropicalis, Candida albicans), Microsporum spp., Cryptococcus neoformans. For endemic mycoses, including infectious diseases caused by Histoplasma capsulatum, Coccidioides immitis, Blastomyces dermatitidis, the use of fluconazole is also recommended.

After oral administration, fluconazole is well absorbed, and its bioavailability reaches 90%. The maximum concentration of the substance when taken orally on an empty stomach in an amount of 150 mg is 90% of the plasma level when infused at a dose of 2.5–3.5 mg / kg. The combination with food does not affect the absorption of Diflazon taken orally. The peak concentration of fluconazole in blood plasma is reached within 0.5-1.5 hours after administration. Plasma concentrations are directly proportional to the dose. A 90% level of equilibrium concentration is observed on the 4-5th day of drug therapy (when taken once a day).

Prescribing a dose twice the standard daily dose on the first day makes it possible to achieve a plasma level of fluconazole of 90% of the equilibrium concentration by the second day. The apparent volume of distribution is practically equal to the total volume of water in the body. The binding of the active substance to plasma proteins is insignificant and amounts to 11–12%.

Fluconazole largely penetrates into all body fluids, including the cerebrospinal fluid. The content of the drug in sputum and saliva is identical to its concentration in plasma. In patients with fungal meningitis, the level of fluconazole in the cerebrospinal fluid is approximately 80% of its plasma level.

In the sweat fluid, dermis, epidermis and stratum corneum, high concentrations of the active substance accumulate, which exceed serum concentrations. Less than 5% of fluconazole is metabolized during the first passage through the liver. Its half-life is approximately 30 hours. Due to this, it is enough to take the drug once in the treatment of vaginal candidiasis and apply it once a day for other indications. Excretion of fluconazole is carried out mainly through the kidneys, and approximately 80% of the dose taken is excreted unchanged. There is a proportional relationship between the clearance of fluconazole and the clearance of creatinine. Metabolites of the active substance Diflazon in the peripheral blood are not recorded.

Indications for use

Generalized candidiasis: candidemia, disseminated candidiasis, invasive candidal infections of the eyes, respiratory system, peritoneum, endocardium, urinary tract, including patients in intensive care units, patients with malignant neoplasms or being on cytotoxic or immunosuppressive therapy, with other factors predisposing development candidiasis;
Candidiasis of the mucous membranes of the mouth (superficial and chronic atrophic candidiasis), pharynx, esophagus, non-invasive bronchopulmonary candidiasis, candiduria, skin candidiasis, including prevention of recurrence of oropharyngeal candidiasis in AIDS patients;
Acute and chronic recurrent vaginal candidiasis;
Cryptococcal meningitis and other localizations of cryptococcosis (including skin, lungs), including in various forms of immunosuppression (AIDS, organ transplantation);
Dermatomycosis, especially with resistance to local therapy of severe fungal infections of the skin, mycoses of smooth skin, dermatophytosis of the feet, pityriasis (multicolored) lichen caused by dermatophytes and fungi of the genus Candida;
Prevention of fungal infections in malignant neoplasms in patients predisposed to the development of such infections as a result of radiation therapy and cytotoxic chemotherapy.

In addition, the use of capsules is shown:

Candidal balanitis, prevention of recurrence of vaginal candidiasis in the presence of three or more episodes per year;
Coccidioidomycosis, deep endemic mycoses, paracoccidioidomycosis, histoplasmosis, sporotrichosis (in patients with normal immunity);
Prevention of cryptococcosis in AIDS patients.

Also, Diflazon's solution is used to prevent candidiasis before bone marrow transplantation.

Contraindications

The simultaneous use of cisapride, astemizole or terfenadine (while taking fluconazole 400 mg per day or more) and other drugs that contribute to the lengthening of the QT interval and increase the risk of severe rhythm disturbances;
Breastfeeding period;
Hypersensitivity to azole compounds and drug components.

According to the instructions, Diflazon should be prescribed with caution: patients with invasive, systemic or superficial fungal infection with the appearance of a rash while taking the drug; with hepatic and renal failure, in combination with terfenadine fluconazole at a dose of less than 400 mg per day, potentially proarrhythmogenic conditions in patients simultaneously taking drugs that cause arrhythmias, patients with electrolyte imbalance, organic heart diseases and other risk factors.

The use of fluconazole during pregnancy is indicated only in case of a potential threat to the woman's life, if the expected therapeutic effect exceeds the harm to the fetus.

In addition, capsules are contraindicated for children under the age of 3 years.

Diflazon is used with caution in case of intolerance to acetylsalicylic acid.

Under the close supervision of a physician, the solution should be used for hypochlorhydria and achlorhydria, treating children under 6 months of age and patients suffering from alcoholism.

Instructions for the use of Diflazon: method and dosage

Diflazon solution is used for intravenous (IV) infusion in patients who cannot take the drug orally. The infusion rate is 200 mg per hour. As soon as the opportunity arises, the patient is transferred to take the drug inside, without changing the daily dose.

Recommended dosage of Diflazon:

Cryptococcal meningitis and cryptococcal infections of other localization: on the first day - 400 mg, then at a dose of 200-400 mg once a day. Usually, therapy lasts 6-8 weeks, its duration depends on the clinical effect confirmed by mycological research. In AIDS patients, prophylaxis of relapse of cryptococcal meningitis is carried out at a dose of 200 mg per day for a long period;
Systemic candidiasis: on the first day - 400 mg, then 200-400 mg once a day, depending on the clinical efficacy and severity of the disease, it is possible to increase the daily dose to 800 mg. The treatment is continued after the complete disappearance of the symptoms of the disease and a negative blood culture for another 2 weeks;
Candidiasis of the mucous membranes: 50-100 mg 1 time per day for 1-2 weeks, in patients with immunodeficiency - 3 weeks. In severe forms of mucous candidiasis, 100-200 mg per day is prescribed with a duration of treatment up to 4 weeks. After completion of the course of primary therapy in AIDS patients, fluconazole at a dose of 150 mg once a week can be prescribed to prevent relapse;
Prevention of candidiasis: 50-400 mg per day (depending on the severity of neutropenia and the perceived risk of fungal infection after myelogenous transplantation and / or before cytostatic or radiation therapy for malignant neoplasms). Fluconazole should be prescribed several days before the expected development of neutropenia and continue to be used for at least 1 week after the neutrophil count exceeds 1000 / mm ³.

In addition, the dosage regimen for Diflazon capsules (capsules are taken orally):

Atrophic candidiasis of the oral cavity caused by wearing dentures: 50 mg once a day for 2 weeks with simultaneous treatment of the denture with antiseptic agents;
Vaginal candidiasis: single dose - 150 mg. For the prevention of relapses - 150 mg 1 time per 4 weeks. The duration of treatment is individual, varies within 4-12 courses;
Balanitis caused by Candida: single dose - 150 mg;
Mycosis of the skin, including candidiasis of the skin, mycoses of smooth skin, feet, groin area: 150 mg once a week or 50 mg once a day for 2-4 weeks, with mycoses of the feet - 6 weeks;
Pityriasis versicolor: 300 mg once a week, the course of treatment is 2-3 weeks, or 50 mg once a day for 2-4 weeks;
Onychomycosis: 150 mg once a week for the period necessary to completely replace the infected nail with a healthy one;
Deep endemic mycoses: 200-400 mg per day. The estimated duration of therapy for coccidioidomycosis is 11-24 months, for sporotrichosis - 1-16 months, for paracoccidioidomycosis - 2-17 months, with histoplasmosis - 3-17 months.

For children with candidiasis of the mucous membranes, the drug is prescribed on the first day at the rate of 6 mg per 1 kg of weight, then 3 mg per 1 kg per day.

For children, a dose of Diflazon is recommended to be prescribed taking into account the severity of the clinical condition and the weight of the child: with generalized candidiasis and cryptococcal infection - from 6 to 12 mg per 1 kg of the child's weight per day; for the prevention of fungal infections with reduced immunity after cytotoxic chemotherapy or radiation therapy - 3-12 mg per 1 kg per day.

At the age of 5-13 years, the daily dose should not exceed that in adult patients (up to 400 mg).

With a single dose of capsules, a dose change in patients with impaired renal function is not required.

Elderly patients do not require dosage adjustment.

When creatinine clearance (CC) is less than 50 ml / min, the dose of the drug in adults and children should be reduced depending on the degree of renal failure.

Patients on regular hemodialysis should receive one dose of the drug after each session.

Side effects

Cardiovascular system: lengthening on the electrocardiogram of the QT interval, flutter or fibrillation of the ventricles;
Digestive system: abdominal pain, nausea, flatulence, vomiting, diarrhea, change in taste; rarely - increased activity of hepatic enzymes, liver dysfunction (hyperbilirubinemia, jaundice, hepatocellular necrosis, hepatitis), including fatal ones;
Hematopoietic system: rarely - agranulocytosis, neutropenia; with severe fungal infections - thrombocytopenia, leukopenia;
Allergic reactions: skin rash, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), bronchial asthma (usually with intolerance to acetylsalicylic acid), anaphylactoid reactions, including pruritus, facial edema, urticaria, angioedema;
Nervous system: headache, dizziness; rarely - convulsions;
Others: rarely - alopecia, impaired renal function, hypercholesterolemia, hypokalemia, hypertriglyceridemia.

In addition, the use of the solution can cause decreased appetite and constipation.

Overdose

Symptoms of an overdose of Diflazon are hallucinations, paranoid behavior, hyperglyceridemia, increased severity of side effects. In this case, they resort to urgent gastric lavage and emergency forced diuresis. When using hemodialysis, the concentration of the drug in the body is reduced by half in 3 hours.

special instructions

Taking capsules is possible before the results of laboratory tests are received, however, after receiving them, it is recommended to adjust the dosage regimen.

Treatment with multiple doses of Diflazon should be accompanied by monitoring of renal function; in renal insufficiency, the dosing regimen should be prescribed taking into account QC.

It is necessary to monitor patients with a functional disorder of the liver, regularly monitor the level of liver enzymes. With an increase in their activity, the doctor must compare the benefits of therapy and the risk of possible toxic liver damage in a severe form. The hepatotoxic effect is usually reversible and after discontinuation of therapy, its symptoms disappear.

If a rash caused by taking fluconazole develops in patients with superficial fungal infection, the drug should be discontinued. In patients with systemic or invasive fungal pathologies, the rash should be observed and therapy should be discontinued in case of erythema multiforme or the appearance of bullous changes.

With the simultaneous use of fluconazole and coumarin anticoagulants, prothrombin time should be carefully monitored. It is necessary to continue treatment until the onset of clinical and hematological remission; premature termination of therapy may lead to relapses.

The E122 dye contained in capsules No. 0 (200 mg) can cause allergies, including bronchial asthma.

In patients with acetylsalicylic acid intolerance, allergic reactions appear more often.

The negative effect of Diflazon on the patient's ability to drive vehicles and mechanisms has not been established.

Pregnancy and lactation

The use of Diflazon in pregnant women is inappropriate, except for severe or life-threatening forms of fungal infections, when the intended benefit to the mother outweighs the potential risk to the fetus.

The content of fluconazole in breast milk coincides with its concentration in the blood plasma; therefore, it is not recommended to prescribe it during breastfeeding.

Renal dysfunction

Patients with renal insufficiency (CC less than 50 ml / min) need correction of the dosage regimen. When CC is more than 50 ml / min, the average recommended dose of Diflazon is prescribed, with CC of 11-50 ml / min, the dose of the drug is reduced to 50% of the recommended dose.

In children with renal dysfunction, the daily dose of Diflazon should be reduced in the same proportional relationship as in adult patients, given the severity of renal failure.

Liver dysfunction

In isolated cases, when using Diflazon, toxic changes in the liver were noted, sometimes leading to death, mainly in patients with serious concomitant diseases. The hepatotoxic effect of fluconazole is predominantly reversible, and its symptoms disappear after stopping treatment. If there are clinical signs of liver damage associated with taking the drug, Diflazon is canceled.

Drug interactions

During the period of treatment with Diflazon, the simultaneous use of any medications must be agreed with the attending physician.

Analogs

Diflazon's analogs are: Diaflu, Difluzol, Diflucan, Candizol, Medoflucon, Mikomax, Mikosist, Tierlit, Flugal, Fluzamed, Fluzon, Fluconaz, Fluconazole, Flucorus, Flucomabol, Flunol, Flucan, Fluciostat, Flucostat, Flunol, Flucan.

Terms and conditions of storage

Keep out of the reach of children.

Store at temperature: capsules - up to 25 ° C, solution - up to 30 ° C.

Shelf life: capsules - 5 years, solution - 3 years.

Terms of dispensing from pharmacies

The solution is available by prescription, capsules are dispensed without a prescription.

Reviews of Diflazon

According to reviews, Diflazon is well tolerated and is considered an effective drug when used strictly according to indications and subject to the rules contained in the instructions for use.

Diflazon price in pharmacies

The price for Diflazon is on average 170–240 rubles per package containing 1 capsule of 150 mg. A package of the drug, including 7 capsules, will cost about 470-500 rubles. The cost of the solution for infusion Diflazon in pharmacies varies in the range from 680 to 770 rubles.

Diflazon: prices in online pharmacies

Drug name

Price

Pharmacy

Diflazon 150 mg capsule 1 pc.

89 RUB

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Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!