Generic

Fluconazole

Indication

Canazole is indicated for acute or recurrent vaginal candidiasis and mucosal candidiasis e.g. oropharyngeal, esophageal, and noninvasive bronchopulmonary infections. Dermal tinea infections e.g. tinea pedis, tinea corporis, tinea cruris, tinea versicolor. Systemic candidiasis e.g. candidaemia, disseminated candidiasis. Cryptococcosis including cryptococcal meningitis and infections of other sites (e.g. pulmonary, cutaneous). For the prevention of fungal infections in patients with compromised immune function, patients with AIDS, organ transplants, or other causes of immunosuppression.

Pharmacology

Fluconazole is a triazole antifungal that is used to treat fungal infections. It’s a strong inhibitor of cytochrome P-450-dependent enzymes in fungi. The ergosterol synthesis is carried out by the Cytochrome P-450 enzyme system, which is an important component of the fungal cell membrane.

Dosage and administration

Adult (oral)-

• Vaginal candidiasis: 150 mg as a single dose.
• Oropharyngeal candidiasis: 200 mg on the first day, followed by 100 mg once daily. Clinical evidence of this infection generally resolves within several days, but treatment should be continued for at least 2 weeks to decrease the likelihood of relapse.
• Esophageal candidiasis: 200 mg on the first day, followed by 100 mg once daily. Doses up to 400 mg/day may be used. Patients should be treated for a minimum of three weeks and for at least two weeks following resolution of symptoms.
• Systemic candida infections: Optimal therapeutic dosage and duration of therapy have not been established. Sometimes, doses of up to 400 mg daily have been used.
• Urinary tract infections caused by candida and peritonitis: 50-200 mg daily have been used.
• Cryptococcal meningitis: 400 mg on the first day, followed by 200 mg once daily.
• Prophylaxis in patients undergoing bone marrow transplantation: 400 mg once daily.

Child (oral):

• Doses of 3-6 mg/kg daily have been used. Doses up to 12 mg/kg are recommended.

Intravenous-

• Adult: Invasive candidal infections including candidaemia and disseminated candidiasis and cryptococcal infections including meningitis, by IV, 400 mg initially then 200 mg daily, increased if necessary to 400 mg daily, treatment continued according to response (at least 6-8 weeks for cryptococcal meningitis)
• Child: 6-12 mg/kg daily (every 72 hours in neonate up to 2 weeks old, every 48 hours in neonate 2-4 weeks old); maximum 400 mg daily. Prevention of relapse of cryptococcal meningitis, by IV, 100-200 mg daily.

Interaction

Fluconazole concentration in plasma reduces by rifampicin but the effect of nicoumalone, phenytoin, and warfarin is enhanced. Plasma concentration of sulphonylureas and theophylline is possibly increased.

Contraindications

Fluconazole is contraindicated in patients who have known hypersensitivity to Fluconazole or to any of its excipients. There is no information regarding cross-hypersensitivity between Fluconazole and other azole antifungal agents.

Side effects

Fluconazole is generally well tolerated. The most common side effects associated with Fluconazole are symptoms associated with the gastrointestinal tract e.g. nausea, abdominal discomfort, diarrhea, headache, vomiting and flatulence. Other adverse effects such as rash are rarely encountered (incidence less than 1%).

Pregnancy & Lactation

US FDA Pregnancy category of Fluconazole is C. So, Fluconazole should be avoided in pregnancy and lactation unless the potential benefits to the other outweigh the possible risks to the fetus.

Precautions & Warnings

Fluconazole should be administered with caution to patients having proarrhythmic conditions.

Therapeutic Class

Drugs for subcutaneous and mycoses

Storage Conditions

Keep away from light and heat in a dry location. Keep out of children’s reach.

Pharmaceutical Name

Opsonin Pharma Ltd.