Ozole

Ozole - Dosage | Interactions | Effects

Ozole contains an active substance called fluconazole and belongs to a group of azole antifungal drugs. It works by inhibiting cytochrome P450, which leads to accumulation of ergosterol in fungal cells and consequently to inhibition of reproduction which prevent the spread of infection. In vitro studies showed activity against the following fungi:

  • Candida albicans
  • Candida tropicalis
  • Candida glabrata
  • Candida parapsilosis
  • Cryptococcus neoformans

It is used in the treatment of the following infections:

  • Vaginal candidiasis.
  • Cryptococcal meningitis.
  • Candidaemia (fungal infection caused by Candida).
  • Peritonitis caused by Candida.
  • Disseminated candidiasis.
  • Fungal infections of the mouth, esophagus, pharynx and lungs caused by candida.

Ozole is also used to prevent fungal infections caused by candida in patients undergoing bone marrow transplantation and receive cytotoxic/radiation therapy.

Ozole is also indicated for the prevention of the recurrence of cryptococcal meningitis, vaginal candidiasis and other types of candidiasis.

Precautions

Ozole should not be used in patients who are allergic / hypersensitive to the active substance fluconazole or other azoles (e.g., ketoconazole, itraconazole, voriconazole and others).

Ozole inhibits enzymes that participate in the metabolism of many drugs, and therefore may enter a large number of major, clinically significant interactions, some of which may endanger your life! It is very important to inform your doctor about all medicines as well as the herbal preparations you are taking.

Cases of worsening liver function have been reported in one patient suffering from hepatitis and receiving fluconazole for the treatment of urinary fungal infections. Fatal cases of liver injury have also been reported. Damage occurs on the hepatocellular level and is often associated with symptoms of an allergic reaction (e.g. fever and skin rash).

Approximately 80% of the drug is excreted unchanged through urine, and patients with impaired renal function excrete this drug more slowly than healthy individuals and this may lead to Ozole accumulation in the body. It is therefore necessary to adjust the dose in patients with kidney problems.

There have been reported cases of torsades de pointes induced by the use of this drug. Torsades de pointes is a specific form of tachycardia (rapid heart rate) characterized by prolonged QT interval, and these types of arrhythmias are life-threatening (since the heart rate may increase up to 250 beats / min)! If you notice any symptoms of arrhythmia (eg palpitations), contact your doctor immediately.

The risk of torsades de pointes is higher in patients receiving other drugs that may also cause QT prolongation, such as:

  • Erythromycin and clarithromycin (macrolide antibiotics).
  • Moxifloxacin (fluoroquinolone antibiotic).
  • Astemizole and terfenadine (H2 antihistamines used in the treatment of allergic reactions).
  • Pimozide (medication used to treat motor tics).
  • Cisapride (medication used to treat heartburn in patients with gastroesophageal reflux disease - GERD).
  • Antiarrhythmic, such as:
    • ibutilide
    • amiodarone
    • procainamide
    • dronedarone
    • quinidine
    • sotalol
  • Bepridil (a calcium blocker used to treat angina).
  • Thioridazine (muscle relaxant).
  • Mesoridazine (a phenothiazine antipsychotic used to treat schizophrenia).
  • Halofantrine and lumefantrine (medications used to treat malaria).
  • Methadone (opioid analgesic).
  • Tricyclic antidepressants (amitriptyline and nortriptyline).

Concomitant use with these drugs is therefore absolutely contraindicated.

Ozole, Pregnancy and Breastfeeding

FDA pregnancy category: D. This means that its use during pregnancy is absolutely contraindicated.

AU TGA pregnancy category: C. This means that animal studies have confirmed the toxicity of this drug during pregnancy, but there is insufficient data on its use in pregnant women.

Ozole should not be used during pregnancy and breastfeeding unless advised by your doctor.

Dosage

The dose and duration of therapy will be determined by your doctor based on the type of fungus that caused the infection and clinical response to the therapy.

The usual dose for the treatment of vaginal candidiasis is 150 mg administered as a single dose.

The usual dose for the treatment of fungal infections of the mouth and throat is 200 mg on the first day followed by 100 mg once daily for at least 2 weeks. Symptoms and fungi are usually resolved within 3-7 days after starting the treatment, but therapy should continue for at least 2 weeks in order to prevent the recurrence of infection.

The usual dose for the treatment of fungal infection of the esophagus is 200 mg on the first day followed by 100 mg once daily for at least three weeks. The therapy should last at least two weeks after symptoms are resolved in order to prevent the recurrence of the infection.

The usual dose for the treatment of brain fungal infection caused by cryptococci is 400 mg on the first day followed by 200 mg once daily. The therapy should last at least 70-84 days after the cerebrospinal fluid culture becomes negative.

The usual dose for the prevention of fungal infections in patients undergoing bone marrow transplantation is 400 mg once daily. The therapy lasts for as long as your doctor estimates it is necessary based on the white blood cell count.

Dosages of 50-200 mg daily were used for the treatment of urinary fungal infections and peritonitis, but the dosing guide for these indications has not yet been established.

The usual dose for the treatment of fungal infections of the mouth, throat and esophagus in children under the age of 11 is 6 mg / kg on the first day, followed by 3 mg / kg once daily. The duration of therapy depends on the pediatrician's assessment and therapy usually lasts for at least two weeks (for fungal infections of the mouth and the throat) or 3 weeks (for fungal esophageal infections). In babies aged 3-4 weeks, the same dose should be administered but once every two days. In babies aged 0/2 weeks, the same dose should be administered but once every three days.

The usual dose for the treatment of fungal infections of the brain caused by cryptococci in children under the age of 11 is 12 mg / kg on the first day, followed by 6 mg / kg once daily. The therapy should last at least 70-84 days after the cerebrospinal fluid culture becomes negative. In babies aged 3-4 weeks, the same dose should be administered but once every two days. In babies aged 0/2 weeks, the same dose should be administered but once every three days.

Interactions

Ozole should not be administered concurrently with the following medicines:

  • Fentanyl and alfentanil (opioid analgesics). Ozole increases the concentration of these drugs in the blood which increases the risk of side effects (e.g. confusion, excess drowsiness, vertigo, bradycardia, and slow breathing).
  • Midazolam and triazolam (benzodiazepines). Ozole increases the concentration of these drugs in the blood, which increases the risk of side effects (e.g. excessive sedation).
  • Vincristine and vinblastine.
  • Nifedipine, felodipine (Felodil XR), amlodipine and nicardipine (dihydropyridine calcium antagonists used in the treatment of cardiovascular diseases). Ozole increases the concentration of these drugs in the blood and increases the risk of side effects.
  • Statins - medicines used to lower cholesterol, such as: Simultaneous administration increases the risk of hepatotoxicity and myopathy.
  • Antiepileptic medications, such as: carbamazepine and phenytoin.
  • Warfarin (anticoagulant drug). Simultaneous administration increases the risk of bleeding.
  • Non-steroidal anti-inflammatory drugs, such as:
  • Zidovudine (medication used to treat HIV).
  • Oral contraceptives (e.g., desogestrel / ethinyl estradiol, dienogest / estradiol valerate, ethynodiol / ethinyl estradiol, levonorgestrel / ethinyl estradiol, Yasmin and others).
  • Oral hypoglycemic medications, such as: glibenclamide and glipizide.
  • Corticosteroids (e.g. prednisone).
  • Medicines used to treat asthma (e.g. theophylline).

Side effects

Ozole is generally well tolerated. The most commonly reported adverse reactions are headache (13%), nausea (7%) and abdominal pain (6%).

The following adverse reactions have also been reported:

  • Dizziness.
  • Diarrhea.
  • Pain or discomfort in the epigastrium.
  • Loss of appetite, pain in the upper right part of the abdomen and jaundice (signs of liver injury).
  • Low red blood cell count associated with pale skin and shortness of breath.
  • Insomnia.
  • Drowsiness.
  • Pain in the muscles.
  • Fever.
  • Prolongation of QT interval.
  • Low blood potassium levels.
  • Hair loss.
  • Thrombocytopenia.
  • Asthenia.
  • Malaise.
  • Cholestasis.
  • Dry mouth.
  • Tremor.
  • Allergic reactions.

References

  • FDA
  • NCBI link
  • Livertox
  • Cousin L, Berre ML, Launay-Vacher V, and others. Dosing guidelines for fluconazole in patients with renal failure. Nephr Dial Trans. 2003: 2227-31.
  • NCBI link 2
  • PIL

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