Diflucan

Diflucan, the main ingredient – Fluconazole, is a representative of the class of triazole antifungal agents. It is a potent selective inhibitor of sterol synthesis in the fungal cell. Fluconazole has shown activity in vitro and in clinical infections against most of the following microorganisms: Candida albicans, Candida glabrata (many strains are moderately susceptible), Candida parapsilosis, Candida tropicalis, Cryptococcus neoformans.

Indications

It is applied for the treatment of the following diseases in adults:

  • cryptococcal meningitis;
  • coccidioidomycosis;
  • invasive candidiasis;
  • mucous candidiasis, incl. oropharyngeal candidiasis, esophageal candidiasis, candiduria and chronic mucocutaneous candidiasis;
  • chronic atrophic candidiasis of the oral cavity (associated with wearing dentures), when oral hygiene or local treatment is not enough;
  • vaginal candidiasis, acute or recurrent, when local therapy is not applicable;
  • candidal balanitis when local therapy is not applicable;
  • dermatomycosis, incl. dermatophytosis of the feet, dermatophytosis of the corp, inguinal dermatophytosis, versicolor and cutaneous candidiasis, when systemic treatment is indicated;
  • dermatophytosis of the nails (onychomycosis), when treatment with other drugs is not acceptable.

Diflucan is used for the prevention of the following diseases in adults:

  • relapse of cryptococcal meningitis in patients at high risk of relapse;
  • outbreak of candidiasis and esophageal candidiasis in HIV-infected patients with a high risk of recurrence;
  • to reduce the frequency of relapse of vaginal candidiasis (4 or more episodes per year);
  • for the prevention of candidal infections in patients with prolonged neutropenia (such as patients with hematological malignancies undergoing chemotherapy or patients undergoing hematopoietic stem cell transplantation).

Fluconazole, the main Diflucan component, is indicated for the treatment of children. It is used to treat mucous candidiasis (oropharyngeal and esophageal candidiasis), invasive candidiasis, cryptococcal meningitis, and the prevention of candidal infections in patients with weakened immune systems. This antibiotic can be used as maintenance therapy to prevent relapse of cryptococcal meningitis in children at high risk of recurrence.

Dosage regimen

Oral administration. The pills are swallowed whole. Therapy should be changed when other laboratory test results will be done. However, antifungal therapy must be modified accordingly when the results of these studies become known. When transferring a patient from intravenous to oral administration of the drug, or vice versa, no change in the daily dose is required.

The daily dose of this drug depends on the nature and severity of the fungal infection. For infections requiring repeated administration of the drug, treatment should be continued until the disappearance of clinical or laboratory signs of active fungal infection. Patients with AIDS and cryptococcal meningitis or recurrent oropharyngeal candidiasis usually require supportive care to prevent recurrent infection.

Side effects

  • The nervous system: often – headache; infrequently – dizziness, convulsions, taste changes, paresthesia, insomnia, drowsiness; rarely – tremor.
  • The digestive system: often – abdominal pain, diarrhea, nausea, vomiting; infrequently – flatulence, dyspepsia, dryness of the oral mucosa, constipation.
  • The hepatobiliary system: often – increased serum activity of aminotransferases, alkaline phosphatase; infrequently – cholestasis, jaundice, increased bilirubin concentration; rarely – hepatotoxicity, in some cases fatal, liver dysfunction, hepatitis, hepatocellular necrosis, hepatocellular damage.
  • The side of the skin: often – a rash; infrequently – itchy skin, hives, increased sweating, drug rash (including persistent drug rash); rarely – exfoliative skin lesions, including Stevens-Johnson syndrome and toxic epidermal necrolysis, acute generalized exanthematous pustulosis, facial edema, alopecia; frequency unknown – drug rash with eosinophilia and systemic symptoms (DRESS-syndrome).
  • The hematopoietic system: rarely – leukopenia, including neutropenia and agranulocytosis, thrombocytopenia, anemia.
  • The immune system: anaphylaxis (including angioedema).
  • The cardiovascular system: rarely – an increase in the QT interval on the ECG, ventricular tachysystolic arrhythmia of the “pirouette” type (torsade de pointes).
  • The side of metabolism: rarely – an increase in the concentration of cholesterol and triglycerides in the blood plasma, hypokalemia.
  • The musculoskeletal system: infrequently – myalgia.
  • Others: infrequently – weakness, asthenia, increased fatigue, fever, vertigo.

Contraindications

  • Simultaneous use of terfenadine during repeated use of fluconazole at a dose of 400 mg / day or over;
  • Simultaneous use with drugs that increase the QT interval and are metabolized by the CYP3A4 isoenzyme, such as cisapride, astemizole, erythromycin, pimozide and quinidine;
  • Lactase deficiency, galactose intolerance, glucose-galactose malabsorption;
  • Children under 3 years of age;
  • Hypersensitivity to fluconazole, other components of the drug, or azole substances with a structure similar to fluconazole.

Take this drug with care in the following cases: liver failure; renal failure; the appearance of a rash against the background of the fluconazole use in patients with superficial fungal infection and invasive/systemic fungal infections; simultaneous use of terfenadine and fluconazole at a dose of less than 400 mg per day; potentially proarrhythmic conditions in patients with multiple risk factors (organic heart disease, electrolyte imbalance and concomitant therapy that promotes the development of such disorders).

Overdose

In one case of a fluconazole overdose, a 42-year-old patient infected with HIV developed hallucinations and paranoid behavior after taking 8200 mg of fluconazole. The patient was hospitalized, his condition returned to normal within 48 hours.

Treatment: in case of an overdose, symptomatic therapy is performed (including supportive measures and gastric lavage). Fluconazole is excreted mainly in the urine, so forced diuresis is likely to accelerate its excretion. A 3-hour hemodialysis session reduces plasma fluconazole levels by about 50%.