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Antifungal Fluconazole : Definition, Mechanism, Objectives, Indications, Precautions and Interactions

Friday, September 7th 2012. | Medical Treatment

Antifungal Fluconazole Definition

Antifungals or fungicides are drugs having the capacity to treat fungal infections, it is to statements of infections caused by fungi.

Fluconazole is a derivative of triazole with antifungal properties. It is administered systemically, capsules or oral suspension, injectable form being reserved for hospitals.

Antifungal Fluconazole Mechanism

Fluconazole inhibits the synthesis of ergosterol in the fungal cell. Ergosterol is an essential component of the fungal membrane. The antifungal effect results from this inhibition.Stopping the growth of fungus, fluconazole is fungistatic.

fungicides

For an antifungal effective, it must happen in sufficient quantity at the site of infection to reach the MIC (which is the minimum inhibitory concentration able to inhibit any culture of bacteria and fungi) and the fungus is sensitive to this antifungal agent. The diffusion of the antifungal in the body is an important parameter to know when prescribing.

After oral administration, the digestive absorption of fluconazole is important (within 90%) and absolute bioavailability is 90%. Its absorption is not affected by food. The peak plasma levels occur between 0.5 and 1, 5:00, and are proportional to the dose.

Fluconazole penetrates into all body fluids, thus in people with fungal meningitis, the rates found in the CSF are equivalent to about 80% in blood. And salivary concentrations in bronchial secretions are similar plasma concentrations.

Fluconazole is poorly metabolized in the liver and its elimination is via the urine mainly as active (80%). Its half-life is 20 to 30 hours.

All these pharmacokinetic parameters allow a daily prescription of one tablet.

Antifungal Fluconazole Objectives

Curb and combat yeast infections and fungi sensitive to their locations.

What are fungi susceptible and resistant?

Fluconazole is active on Candida albicans, Cryptococcus neoformans and with an activity comparable to amphotericin B injection, also on dermatidis Blastomyces, Histoplasma capsulatum and the dermatophytes (Trichophyton, microsporum, epidermophyton).

Resistance was usual candidaa krusei, Aspergillus fumigalus, asprgillus flavus.

Antifungal Fluconazole Indications

Fluconazole is indicated for:

  • Neuro-meningeal cryptococcosis, with an efficiency comparable to that of amphotericin B injection.
  • Oropharyngeal candidiasis, esophageal, urinary, systemic particularly in immunocompromised patients with AIDS, perineal and vaginal candidiasis recurrent oral candidiasis associated with dentures.

Off-label indications, such as onychomicoses dermatophyte, with healing in about 75% of cases, and in dermatomycoses.

Antifungal Fluconazole Adverse

These are some complications that can occur when taking the drug, knowing that induced side effects vary among individuals.

When taking fluconazole have been reported:

Nausea, abdominal pain, headache, and more rarely diarrhea, vomiting, allergic skin reactions.

Antifungal Fluconazole Precautions

In case of renal impairment, the dose should be reduced and adjusted according to the creatinine clearance.

hemodialysis patients, administration of the product will be after each dialysis session.

Pregnancy and lactation

Prescription fluconazole is against-indicated during pregnancy except in patients with severe fungal infections or potentially lethal, will be established the principle of benefit compared to risk.

Fluconazole is cons-indicated during lactation.

Lifestyle

Fungal infections are contagious, the person transmission occurs directly.

Fungal infections of the skin, mucous membranes and nails are favored by maceration, humidity, poor hygiene.

Interactions

Associations with pimozide, halofantrine, are cons-indicated because of the risk of torsades de pointes.

Associations with AVK, cyclosporine, phenytoin, sulfonylureas, theophylline due to a potentiation of these products should be used with caution.

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