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Fluconazole

Fluconazole is an antifungal (or antifungal) drug of the azole type.

It is a drug used for different types of fungal infections, in fact, it is available in pharmaceutical formulations suitable both for oral administration and for parenteral and cutaneous administration.

Fluconazole - Chemical Structure

Indications

For what it uses

The use of fluconazole is indicated for:

  • Treatment and prevention of recurrence of cryptococcal meningitis (oral and parenteral administration);
  • Coccidioidomycosis (oral and parenteral administration);
  • Treatment of Candida infections found in the bloodstream, organs or urinary tract (oral and parenteral administration);
  • Treatment and prevention of recurrence of mucosal candidiasis (oral and parenteral administration);
  • Treatment and prevention of recurrences of genital candidiasis (oral administration);
  • Treatment of fungal infections of the skin and skin appendages, such as ringworm and fungal nail infections (oral administration);
  • Prevention of yeast infections caused by Candida in subjects with compromised immune systems (oral administration);
  • Treatment of dermatomycoses caused by dermatophytes, yeasts or molds, such as ringworm and candidiasis (dermal administration).

Warnings

Before starting treatment with fluconazole, it is good to inform your doctor if you are in one of the following conditions:

  • If you suffer from liver and / or kidney diseases;
  • If you suffer from heart disease;
  • If there is an alteration in the blood levels of potassium, calcium and / or magnesium.

If allergic reactions of any kind occur during fluconazole therapy, treatment with the drug should be stopped immediately.

Prolonged use of fluconazole for topical use may favor the onset of sensitization phenomena; in this case, treatment with the drug must be stopped immediately.

Fluconazole can cause side effects that are able to alter the ability to drive vehicles and / or use machinery, therefore, great care must be taken.

Interactions

At the moment there are no known drug interactions between topical fluconazole and other drugs.

On the contrary, pharmacological interactions are known between fluconazole for oral and parenteral use and other drugs. More in detail, the concomitant administration of fluconazole (both orally and parenterally) and of the following drugs should be avoided, due to the side effects that may arise:

  • Astemizole or terfenadine, antihistamine drugs;
  • Cisapride, a drug that is able to increase gastrointestinal motility;
  • Pimozide, an antipsychotic;
  • Quinidine, an antiarrhythmic;
  • Erythromycin, an antibiotic.

Also - due to the possible interactions that can occur - you need to tell your doctor if you are already taking any of the following medications:

  • Rifampicin or rifabutin, antibiotic drugs;
  • Fentanyl and other opioid analgesics;
  • Amitriptyline and nortriptyline, antidepressant drugs;
  • Amphotericin B and voriconazole, other antifungal drugs;
  • Oral anticoagulants such as, for example, warfarin;
  • Benzodiazepines ;
  • Carbamazepine and phenytoin, antiepileptic drugs;
  • Antihypertensive drugs;
  • Cyclosporine and other immunosuppressive drugs;
  • Anti- cancer drugs, such as, for example, vincristine and vinblastine;
  • Alofantrine, an antimalarial;
  • Statins ;
  • NSAIDs ;
  • Saquinavir and other antivirals used in the treatment of HIV;
  • Oral hypoglycemic agents ;
  • Theophylline, used in the treatment of asthma;
  • Vitamin A.

In any case, it is still advisable to inform your doctor if you are taking - or if you have recently been - drugs of any kind, including non-prescription medicines and herbal and / or homeopathic products.

Side effects

Fluconazole can cause various types of side effects, although not all patients experience them. This depends on each person's sensitivity to the drug. Therefore, it is not said that the adverse effects occur all with the same intensity in each individual.

Listed below are the main side effects that may occur during treatment with fluconazole.

Allergic reactions

Fluconazole can cause allergic reactions in sensitive individuals. These reactions can manifest as symptoms, such as:

  • Sudden wheezing;
  • Difficulty breathing and tightness in the chest;
  • Angioedema;
  • Skin eruptions;
  • Itch;
  • Formation of blisters in the oral cavity and on the tongue.

Hepatobiliary disorders

Treatment with fluconazole can cause liver damage that can occur with symptoms such as fatigue, vomiting and loss of appetite. Furthermore, the drug can promote the onset of jaundice and liver failure.

Nervous system disorders

Fluconazole therapy may cause:

  • Headache;
  • Drowsiness;
  • Decreased appetite;
  • dizziness;
  • Dizziness;
  • Pins and needles, tingling or numbness;
  • Alteration of the sense of taste;
  • Convulsions.

Psychiatric disorders

Fluconazole treatment can cause insomnia.

Gastrointestinal disorders

Fluconazole therapy may cause:

  • Stomach disorders;
  • Nausea;
  • He retched;
  • Diarrhea;
  • Constipation;
  • Difficulty of digestion;
  • Flatulence.

Skin and subcutaneous tissue disorders

Treatment with fluconazole may promote the onset of:

  • Skin eruptions;
  • Urticaria;
  • Itch;
  • Increased sweating;
  • Hair loss.

Other side effects

Other side effects that may occur during fluconazole therapy are:

  • Temperature;
  • Fatigue;
  • General malaise;
  • Muscular pain;
  • Dry mouth;
  • Reduction in the number of red blood cells, white blood cells and platelets in the bloodstream;
  • Increased blood cholesterol levels;
  • Rhythm and heart rate alteration.

Overdose

Symptoms that may arise if excessive doses of fluconazole (both oral and parenteral) are taken consist of hallucinations and paranoid behavior. Therapy in case of overdosage is symptomatic and supportive. Gastric lavage could be useful.

In any case, if you suspect a fluconazole overdose, you must contact your doctor immediately and contact the nearest hospital.

As far as topical fluconazole is concerned, on the other hand, no cases of overdosage have been reported.

Action mechanism

Fluconazole performs its activity by interfering with the synthesis of ergosterol.

Ergosterol is a sterol that forms the plasma membrane of fungal cells; fluconazole is able to reduce its production by inhibiting a key enzyme involved in its synthesis: 14α-demethylase. By inhibiting this enzyme, there is an accumulation of ergosterol precursors inside the fungal cell.

The ergosterol precursors, when they reach too high levels in the cell, become toxic for the cell and cause alterations in the permeability of the cell membrane and in the functioning of the proteins contained in it. The fungal cell is thus condemned to certain death.

Mode of Use - Posology

Fluconazole is available for oral administration (in the form of capsules and oral suspension), for intravenous administration (in the form of a solution for infusion) and for topical administration (in the form of a cutaneous gel).

Regardless of the pharmaceutical formulation that you intend to use - for a successful outcome of the therapy - it is necessary to scrupulously follow the indications provided by the doctor, both as regards the amount of drug to be used, and as regards the duration of the therapy itself.

Below are some indications on the doses of fluconazole usually used in therapy.

Oral administration

In adults, the dose of fluconazole orally usually used varies from 50 to 800 mg a day depending on the type and severity of the infection to be treated. The duration of treatment also depends on the type of mycosis to be treated and its severity.

In children under 11 years of age, the oral dose of fluconazole is 3-12 mg / kg of body weight per day. Also in this case, the amount of drug to be used and the duration of treatment vary according to the type and severity of the infection to be treated. The maximum daily dose that can be administered in this category of patients is 400 mg.

Intravenous administration

Intravenous fluconazole should be administered by specialized personnel through an intravenous infusion.

In adults, the usual drug dose is 50-800 mg a day. The amount of drug to be used and the duration of treatment depend on the type and severity of the infection to be treated.

In children up to 11 years of age, the usual fluconazole dose is 3-12 mg / kg per day. The amount of drug to be administered, the frequency of administration and the duration of the therapy vary depending on the type and severity of the infection to be treated. It is important not to exceed the maximum daily dose of 400 mg of drug.

Topical administration

When using the fluconazole-based gel, it is recommended to carry out an application a day directly on the affected area. The duration of treatment depends on the type of fungus that caused the infection and on the site where the infection developed.

Pregnancy and breastfeeding

The use of fluconazole by pregnant women and by breast-feeding mothers should be avoided, except in the case where the doctor does not consider it absolutely necessary.

In any case, pregnant women and breastfeeding mothers should always seek medical advice before taking any type of medication.

Contraindications

The use of fluconazole is contraindicated in the following cases:

  • In patients with known hypersensitivity to fluconazole;
  • In patients with known hypersensitivity to other azole-type antifungals (such as, for example, econazole, ketoconazole, miconazole, voriconazole, itraconazole, etc.);
  • In patients already being treated with astemizole, terfenadine, cisapride, pimozide, quinidine or erythromycin.

Furthermore, fluconazole is generally contraindicated during pregnancy and lactation.

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