Fluconazole

Fluconazole belongs to a group of medicines called antifungals. It works by stopping the growth of fungus and is used to treat infections of the mouth, throat, vagina and other parts of the body including fingernails and toenails. It kills fungi by destroying the fungal cell membrane.

Fluconazole is a triazole antifungal agent. It is a potent inhibitor of fungal cytochrome P-450 dependent enzymes. Cytochrome P-450 enzyme system is essential component of fungal cell membrane which is responsible for the synthesis of ergosterol.

• Vaginal Candidiasis: Used for treatment of vaginal fungal infections.
• Oropharyngeal Candidiasis: Used for treatment of mouth and throat fungal infections.
• Esophageal Candidiasis: Used for treatment of esophageal fungal infections.
• Tinea Infections: Used for treatment of skin fungal infections.
• Cryptococcal Meningitis: Used for treatment of brain fungal infections.

Drugs for subcutaneous and mycoses

Triazole Antifungal

Fluconazole is a triazole antifungal agent. It is a potent inhibitor of fungal cytochrome P-450 dependent enzymes. Cytochrome P-450 enzyme system is essential component of fungal cell membrane which is responsible for the synthesis of ergosterol.

Fluconazole decreases ergosterol synthesis by interfering with cytochrome P450 activity, thus inhibiting cell membrane formation of susceptible fungi.

Adult Dose (Oral/IV):

• Vaginal Candidiasis: 150 mg as a single dose.
• Oropharyngeal Candidiasis: Day 1: 200 mg, then 100 mg daily for 14 days.
• Esophageal Candidiasis: Day 1: 200 mg, then 100 mg daily for 14-30 days (up to 400 mg/day).
• Tinea Infections: 150 mg weekly for 4-6 weeks.
• Cryptococcal Meningitis: Day 1: 400 mg, then 200-400 mg daily; 6-8 weeks.

Child Dose (>1 year):

• Superficial Candidiasis: 1-2 mg/kg daily.
• Systemic Candidiasis: 3-6 mg/kg daily.

Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Fluconazole may be taken with or without food, but it is better to take it at a fixed time.

If you miss a dose of Fluconazole, take it as soon as possible; however, if it is almost time for your next dose, skip the missed dose.

Common Side Effects:

• Headache
• Nausea
• Rash
• Vomiting
• Abdominal discomfort
• Diarrhea

Precautions:

• Fluconazole may cause dizziness or seizures which may affect driving ability.
• Prescribed to cure infection and improve symptoms.
• Do not skip doses and finish the full course of treatment.
• Use a reliable method of contraception to prevent pregnancy while taking this medicine.
• Inform doctor if yellowing of eyes or skin, dark urine, or stomach pain occurs.
• Inform doctor if severe skin rash with fever develops.
• Liver function may be checked before and during treatment.

Contraindications: Hypersensitivity.

Drug Interactions:

• Oral hypoglycemics, phenytoin, theophylline, rifabutin: May increase plasma concentrations.
• Anticoagulants: May increase prothrombin time.
• Cyclosporine: May cause significant increase in levels.
• Rifampicin: Reduces fluconazole levels.
• Tacrolimus: May increase risk of nephrotoxicity.
• Potentially Fatal: Cardiac arrhythmias or QT prolongation with terfenadine, cisapride, astemizole, pimozide, quinidine.

Food Interactions: Caution is advised when consuming alcohol; consult your doctor. Take antacids 1 hour before or 2 hours after fluconazole.

Use in Pregnancy: Fluconazole is unsafe during pregnancy; definite evidence of risk to the developing baby; doctor may prescribe in life-threatening situations.

Use in Lactation: Fluconazole is safe during breastfeeding; does not pass into breastmilk in significant amount and is not harmful to the baby.

Pediatric Use: Child dosage provided above; dosage established for children over 1 year.

Geriatric Use: Normal dose should be used if there is no evidence of renal impairment.

Renal Impairment: Fluconazole is probably unsafe; caution required; adjust dosage intervals based on CrCl.

Hepatic Impairment: Use with caution; dose adjustment may be needed.

Overdose: Supportive measures and symptomatic treatment (gastric lavage if necessary); fluconazole is excreted largely in urine; hemodialysis decreases plasma levels by approximately 50%.

Storage: Keep in a dry place away from light and heat. Keep out of reach of children.

Fluconazole