Dizole

Dizole - Uses | Warnings | Dosage

Dizole is a medicine that contains fluconazole as an active substance. The pharmacological classification of Dizole is antifungal drugs. According to its chemical structure it is classified into the triazoles. It works by inhibiting the fungal cytochrome P450-dependent enzyme, called lanosterol 14-alfa demethyllase. In this way it inhibits the fungal demethylation of 14-alfa lanosterol and prevents the synthesis of ergosterol. The accumulation of 14-alfa lanosterol in fungal cells leads to a fungistatic effect (preventing the reproduction and growth of fungi and thereby preventing spreading of infection), or fungicidal effect (killing fungi) - only if administered in high doses.

Uses

Dizole is used to treat the following fungal infections:

  • Oropharyngeal candidiasis (fungal infection that develops in the mouth or throat, also called thrush)
  • Esophageal candidiasis (fungal infection that develops in the esophagus)
  • Vaginal candidiasis
  • Coccidioidomycosis (fungal infection that develops in the lungs and bronchi)
  • Candidemia (a candida bloodstream infection)
  • Cryptococcal meningitis (fungal infection that develops in the brain)

Studies have shown that this drug is effective in treating urinary infections and pneumonia caused by Candida.

Doctors sometimes prescribe this medicine for the treatment of onychomycosis (fingernail and toenail infections), fungal skin infections, but also for the prevention of fungal infections.

Warnings

Dizole must be very carefully used in patients who have:

  • Heart disease (e.g. heart failure, angina, arrhythmia, and others).
  • Kidney disease.
  • Liver disease. Cases of severe hepatic impairment, some with a fatal outcome, have been reported!
  • High or low levels of minerals (potassium, calcium and magnesium) in the blood.

Skin allergic reactions have been reported, and in the event you notice rash on your skin, contact your doctor immediately.

Dizole, Pregnancy and Breastfeeding

FDA pregnancy category: D.

Data from the studies show the occurrence of congenital fetal anomalies in babies whose mothers have been exposed to high doses (400-800 mg daily) of this drug. Several epidemiological studies claim that this drug does not increase the risk of congenital anomalies if administered at low doses (150 mg daily).

AU TGA recommends that this medicine should be used during pregnancy only in case of serious, life-threatening fungal infection, and only if the benefit to the mother outweighs the risk for the fetus.

It is recommended to avoid using this medication during pregnancy, as well as during lactation (as it is excreted into the breast milk).

Dosage

Always follow your doctor's dosing instructions.

The recommended dosage for adults is shown in the table below:

Indication Dosage
Oropharyngeal candidiasis

Day 1: 200 mg once a day.

After the first day, the recommended dose is 100 mg once a day.

Duration of therapy: 2 weeks.

Esophageal candidiasis

Day 1: 200 mg once a day.

After the first day, the recommended dose is 100 mg once daily.

Duration of therapy: at least 3 weeks + 2 weeks (to prevent the recurrence).

Urinary infections caused by candida 50-200 mg once a day.
Cryptococcal meningitis

Day 1: 400 mg once a day.

After the first day, 200 mg once daily is recommended (although the dose can be increased to 800 mg in cases of severe infection).

Duration of therapy: 10-12 weeks after the cerebrospinal fluid culture is negative.

Coccidomycosis (fungal infection that develops in the lung) 400-800 mg once daily for 3-6 months in non-complicated infections or 200-400 mg once daily for 11-24 months, depending on the severity of the infection.
Fingernail infections 150-300 mg once a week for 3-6 months.
Toenail infections 150-300 mg once a week for 6-12 months.

In patients under 12 years of age, the dose should be calculated on the basis of body weight.

Interactions

Studies have shown that Dizole is highly selective for fungal cytochrome P450 but still acts as an inhibitor of this enzyme in humans (a potent inhibitor of CYP2C9 and a moderate inhibitor of CYP3A4). Since CYP2C9 and CYP3A4 are responsible for the metabolism of a large number of drugs, Dizole can interact with many drugs, but the following interactions are classified as clinically significant (major):

  • Terfenadine and astemizole (a new generation of antihistamines) that are used to treat allergies. Concomitant administration with these drugs increases the risk of QT prolongation and severe arrhythmias.
  • Fentanyl, hydrocodone, oxycodone, alfentanyl and other narcotic analgesics. Dizole significantly increases the concentration of these drugs in the blood which can cause severe dizziness, bradycardia (slow heart rate), hypotension and difficulty breathing.
  • Atorvastatin, lovastatin, rosuvastatin (Crestor), pravastatin (PravaCor), simvastatin (Zocor), niacin, ezetimibe, Atozet and other medicines used to lower blood cholesterol. Dizole increases the concentration of these drugs in the blood and increases the risk of liver damage and rhabdomyolysis (breakdown of muscle tissue leading to kidney failure and may have fatal outcome)!
  • Ciprofloxacin, moxifloxacin, norfloxacin, ofloxacin and other fluoroquinolones (antibiotics). Dizole increases the concentration of these drugs in the blood which increases the risk of QT prolongation and serious cardiac arrhythmias.
  • Anisindione (a medicine used to treat thromboembolic disorders). Simultaneous administration with this medicine increases the risk of bleeding. It is necessary to adjust the dose of the anisindione according to the INR (International Normalized Ratio).
  • Leflunomide and teriflunomide (medicines used to treat moderate and severe forms of rheumatoid arthritis). Simultaneous administration increases the risk of liver damage.
  • Ergotamine (a medicine used to treat migraine). Dizole increases the concentration of ergotamine in the blood which can cause severe vasoconstriction and consequently high blood pressure, gangrene, heart attack and stroke!
  • Colchicine (a medicine used to treat gout). Simultaneous administration with this medicine increases the risk of side effects that affect nervous system and liver.
  • Citalopram and escitalopram (antidepressants). Simultaneous administration with these medicines increases the risk of severe arrhythmias.
  • Warfarin, dicumarol and acenocoumarol (anticoagulants). Simultaneous administration with these medicines increases the risk of bleeding.
  • Ceritinib (a medicine used to treat lung cancer). Simultaneous administration increases the risk of arrhythmias.
  • Cilostazole (a medicine used in the treatment of intermittent claudication - occlusive disease of the arteries and veins of the lower extremities). Simultaneous administration increases the risk of side effects, such as:
    • nausea
    • vomiting
    • diarrhea
    • dizziness
    • palpitations
    • bleeding
    • arrhythmias
  • Amiodarone, quinidine, dronedarone and ibutilide (antiarrhythmic agents). Simultaneous administration with these medicines increases the risk of arrhythmias.
  • Everolimus (a medicine used to treat advanced kidney cancer). Simultaneous administration increases the risk of lung inflammation and bleeding.
  • Efavirenz (a medicine used to treat HIV). Simultaneous administration increases the risk of arrhythmias.
  • Erythromycin (antibiotic). Simultaneous administration increases the risk of QT prolongation and serious cardiac arrhythmias.
  • Haloperidol and droperidol (antipsychotics). Concomitant use with these medicines increases the risk of cardiac arrhythmias.
  • Pimozide.
  • Cisapride.
  • Oral contraceptives.
  • Benzodiazepines (diazepam, bromazepam, lorazepam, alprazolam, midazolam and others).
  • Tricyclic antidepressants (nortriptylin, amitriptyline and imipramine).

Note: Not all major interactions are listed above. Consult your doctor if you are taking any other medicines.

Side effects

Dizole can cause the following side effects:

  • Diarrhea
  • Nausea
  • Vomiting
  • Anemia
  • Skin rash
  • Difficulty breathing
  • Liver damage (fatigue, loss of appetite, elevated blood transaminase levels, vomiting and jaundice)
  • Paresthesia
  • Pain in the muscles
  • Insomnia
  • Drowsiness
  • Alopecia
  • Hypokalemia
  • Increased cholesterol levels
  • Allergic reactions

Reference

  1. FDA
  2. PIL

Information on this website are provided for educational purposes only and are not intended for medical advice, diagnosis or treatment.

If you have any concerns or questions about your health, you should always consult with a physician or other health-care professional.