Diflucan

Diflucan (fluconazole) is a leading systemic antifungal medication prescribed for the treatment and prevention of a wide range of fungal infections. As a member of the triazole class of antifungals, it works by inhibiting the synthesis of ergosterol, a critical component of fungal cell membranes, leading to cell death. Its broad-spectrum activity, excellent bioavailability, and generally favorable safety profile have established it as a first-line agent in both outpatient and inpatient settings. Available in oral tablets, suspension, and intravenous formulations, Diflucan offers flexible dosing options tailored to specific clinical scenarios and patient needs.

Features

• Active ingredient: Fluconazole 50 mg, 100 mg, 150 mg, or 200 mg tablets
• Formulations: Oral tablets, powder for oral suspension, and intravenous solution
• Mechanism: Selective inhibition of fungal cytochrome P450-dependent enzyme lanosterol 14-α-demethylase
• Half-life: Approximately 30 hours, allowing for once-daily dosing
• Bioavailability: Over 90% following oral administration
• Excretion: Primarily renal, with 80% of dose excreted unchanged in urine

Benefits

• Provides rapid and effective resolution of symptomatic fungal infections
• Offers convenient once-daily dosing regimen for improved adherence
• Demonstrates excellent tissue penetration, including central nervous system and genitourinary tract
• Shows activity against a broad spectrum of pathogenic fungi, including Candida species and Cryptococcus neoformans
• Available in multiple formulations to accommodate various patient populations and clinical situations
• Generally well-tolerated with a predictable safety profile in appropriate patient populations

Common use

Diflucan is indicated for the treatment of mucosal candidiasis (oropharyngeal, esophageal, and vaginal candidiasis), systemic candidiasis (including candidemia, disseminated candidiasis, and pneumonia), cryptococcal meningitis, and prevention of fungal infections in immunocompromised patients. It is also used for fungal prophylaxis in patients undergoing bone marrow transplantation who receive cytotoxic chemotherapy and/or radiation therapy. Off-label uses include treatment of certain dermatophyte infections, fungal urinary tract infections, and prophylaxis in other immunocompromised populations.

Dosage and direction

Dosage varies significantly based on indication, patient factors, and renal function. For oropharyngeal candidiasis: 200 mg on first day, then 100 mg once daily for at least 14 days. For esophageal candidiasis: 200 mg on first day, then 100 mg once daily; may increase to 400 mg daily if needed. For vaginal candidiasis: single 150 mg oral dose. For systemic candidiasis: 400 mg on first day, then 200 mg once daily. For cryptococcal meningitis: 400 mg on first day, then 200-400 mg once daily. Dosage must be adjusted in patients with renal impairment (CrCl <50 mL/min). Administer with or without food; shake oral suspension well before use.

Precautions

Use with caution in patients with hepatic impairment, renal impairment, or electrolyte disturbances. Monitor hepatic function during prolonged therapy. QT prolongation may occur; use caution in patients with risk factors for arrhythmias. Avoid use in pregnancy unless potential benefit justifies potential risk to fetus (Pregnancy Category D). Breastfeeding should be discontinued during treatment. Superinfections with non-susceptible organisms may develop. Cross-resistance with other azole antifungals may occur. Photosensitivity reactions have been reported; advise patients to use sun protection.

Contraindications

Hypersensitivity to fluconazole, other azole antifungal agents, or any component of the formulation. Coadministration with cisapride, erythromycin, pimozide, or quinidine due to potential for serious cardiac adverse events. Use in patients with congenital or documented acquired QT prolongation. Severe hepatic impairment. Concurrent administration with drugs that are highly dependent on CYP3A4 for clearance and have narrow therapeutic windows.

Possible side effect

Common adverse reactions (≥1%) include headache, nausea, abdominal pain, diarrhea, dyspepsia, dizziness, and taste perversion. Less frequent but potentially serious side effects include hepatotoxicity (elevated liver enzymes, hepatitis, hepatic failure), QT prolongation, torsades de pointes, anaphylaxis, Stevens-Johnson syndrome, toxic epidermal necrolysis, leukopenia, thrombocytopenia, hypertriglyceridemia, and hypokalemia. Alopecia has been reported with prolonged use. Seizures have been reported in patients with serious underlying medical conditions.

Drug interaction

Diflucan is a moderate inhibitor of CYP3A4 and CYP2C9 and may increase concentrations of drugs metabolized by these enzymes. Significant interactions include: increased concentrations of warfarin (monitor INR), phenytoin, cyclosporine, tacrolimus, statins, sulfonylureas (risk of hypoglycemia), theophylline, and benzodiazepines. Rifampin decreases fluconazole concentrations. Hydrochlorothiazide increases fluconazole concentrations. Concomitant use with other QT-prolonging agents may have additive effects. Avoid concomitant use with cisapride, erythromycin, pimozide, or quinidine.

Missed dose

If a dose is missed, take it as soon as remembered unless it is almost time for the next dose. Do not double the dose to make up for a missed dose. Resume the regular dosing schedule. For once-weekly dosing regimens, contact healthcare provider for guidance if a dose is missed. Maintaining consistent blood levels is important for antifungal efficacy, particularly in serious infections.

Overdose

Symptoms of overdose may include hallucinations, paranoid behavior, and exaggerated side effects. In cases of massive overdose, seizures may occur. Treatment is supportive and symptomatic. Gastric lavage may be beneficial if performed soon after ingestion. Fluconazole is dialyzable; hemodialysis for three hours decreases plasma concentrations by approximately 50%. Monitor electrolyte balance, renal function, and hepatic function. No specific antidote exists.

Storage

Store at controlled room temperature (20-25°C/68-77°F). Keep container tightly closed. Protect from light and moisture. Do not freeze. Keep out of reach of children and pets. Do not use after expiration date. Oral suspension should be stored at room temperature; discard unused portion after 14 days. Intravenous solution should be inspected visually for particulate matter and discoloration before administration.

Disclaimer

This information is for educational purposes only and does not constitute medical advice. Diflucan is a prescription medication that should be used only under the supervision of a qualified healthcare professional. Individual response to treatment may vary. Always follow your healthcare provider’s instructions regarding dosage, administration, and monitoring. Report any adverse effects to your healthcare provider promptly. Do not share medication with others, even if they have similar symptoms.

Reviews

Clinical studies demonstrate Diflucan’s efficacy across multiple indications. In randomized trials for vaginal candidiasis, single-dose Diflucan showed clinical cure rates of 85-90% at 5-7 days and 75-80% at 30-35 days. For oropharyngeal candidiasis in immunocompromised patients, response rates of 80-90% have been reported. In cryptococcal meningitis trials, success rates of 60-70% were observed after 10 weeks of therapy. Most patients report satisfaction with the convenience of once-daily dosing and generally good tolerability. Healthcare providers appreciate its predictable pharmacokinetics and broad spectrum of activity.