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fluconazole
Commercial name
VIVOZOLE
Category
ANTI- INFECTION DRUGS
Chemical composition

Each 5 ml of the suspension after preparation contains 50 mg or 200 mg fluconazole.

Dosage Form
Granules for oral suspension
Pharmaceutical group
Antifungal drugs
Contraindications

- Hypersensitivity to the active substance, to related azoles, or to any of the excipients

- Coadministration of terfenadine is contraindicated in patients receiving fluconazole in multiple doses of 400 mg daily or higher based on the results of a multiple dose interaction study.

- Other drugs known to prolong the QT interval that are metabolized by cytochrome P450 (CYP) 3A4 such as cisapride, astemizole, pimozide, quinidine and erythromycin are contraindicated in patients receiving fluconazole

Drug interactions

- Cisapride: Increased plasma concentration of cisapride, therefore concomitant therapy is contraindicated.

- Terfenadine: Fluconazole at doses of 400 mg or more is contraindicated with terfenadine. Co-administration of fluconazole at doses less than 400 mg per day with terfenadine should be carefully monitored.

- Astemizole: administration of fluconazole with astemizole may increase serum levels/decrease clearance of astemizole.

- Pimozide: Concomitant administration of fluconazole with pimozide may lead to inhibition of pimozide metabolism.

- Quinidine: Fluconazole combined with quinidine may inhibit the metabolism of quinidine.

- Erythromycin: Concomitant use of fluconazole and erythromycin has the potential to increase the risk of cardiotoxicity (prolonged QT interval) and, consequently, sudden cardiac death.

- Rifampicin: Simultaneous administration leads to a decrease in the effectiveness of fluconazole and therefore the dose of fluconazole must be increased.

- Amitriptyline and Nortriptyline: Fluconazole increases the pharmacological effect of both compounds.

- Carbamazepine: Fluconazole inhibits the metabolism of carbamazepine and increases its serum levels

- Phenytoin: Fluconazole inhibits the hepatic metabolism of phenytoin and increases its serum levels.

Dosage and usage

 

Fluconazole is used in the treatment of onychomycosis caused by Candida, cryptococcus and other susceptible yeasts, in particular:

1- Mucosal candidiasis: includes oropharyngeal candidiasis, esophageal infections, non-invasive bronchopulmonary infections, candidiasis, mucocutaneous candidiasis, and chronic atrophic oral candidiasis (inflammation of the oral teeth).

2- Systemic candidiasis (including deep disseminated infection and peritonitis).

3- Acute malignant meningitis in adults, including AIDS patients, transplanted patients, or other patients with other causes of immunosuppression.

4- A genital candidiasis. Acute or recurrent vaginal candidiasis. Candida balanoposthitis.

5- Prevention of fungal infections for patients exposed to such infections as a result of chemotherapy or radiotherapy, including bone transplant patients.

6- Dermatophytosis, including infections such as tinea pedis, tinea corporis, tinea pedis, tinea versicolor.

- Fluconazole is not indicated for the treatment of nail infections and ringworm of the head

Dosage:

- The daily dose of fluconazole depends on the nature and severity of the fungal infection.

- Inadequate treatment period may cause relapses of active infection.

- Adults:

Candida vaginitis: 150 mg as a single daily dose.

Mucosal candidiasis: 50 mg as a single dose daily for 7-14 days

- Renal impairment: Fluconazole is mainly excreted in the urine as an unchanged drug. No adjustments are required in treatment with a single dose. In patients (including children) with impaired renal function who will receive multiple doses of fluconazole, the normal recommended dose should be administered on Day 1, followed by a daily dose based on creatinine clearance.

- Children: The maximum dose of 400 mg per day should not be exceeded

- Mucosal candidiasis: the daily dose is 3 mg/kg once daily

- Systemic candidiasis, cryptococcal infection: 6-12 mg/kg daily

-   Prevention of fungal infections in immunocompromised patients considered at risk of neutropenia after cytotoxic chemotherapy or radiotherapy: 3-12 mg/day

Side Effect

Anemia, agranulocytosis, facial edema, anorexia, hypertriglyceridemia, hypokalemia, headache, insomnia and drowsiness, arrhythmia, increase in serum activity of hepatic enzymes, cholestasis, pruritus, urticaria, exfoliative skin disorders, myalgia

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