Diflucan: Effective Single-Dose Oral Antifungal Treatment
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Diflucan (fluconazole) is a leading systemic antifungal medication indicated for the treatment and prevention of a range of fungal infections. As a triazole antifungal agent, it operates through selective inhibition of fungal cytochrome P-450 sterol C-14 alpha-demethylation, which disrupts ergosterol synthesis—a critical component of fungal cell membranes. Its broad-spectrum activity, excellent oral bioavailability, and favorable safety profile make it a first-line choice for both clinicians and patients managing susceptible fungal pathogens. Available by prescription, Diflucan offers a convenient, well-tolerated option for addressing infections caused by Candida, Cryptococcus, and other opportunistic fungi.
Features
- Active ingredient: Fluconazole 50 mg, 100 mg, 150 mg, or 200 mg tablets
- Formulation: Oral tablet; also available as powder for oral suspension and intravenous solution
- Mechanism: Inhibits fungal lanosterol 14α-demethylase, impairing ergosterol biosynthesis
- Spectrum: Active against Candida albicans, Candida glabrata (variable), Candida tropicalis, Cryptococcus neoformans
- Pharmacokinetics: >90% oral bioavailability, extensive tissue penetration including CNS, primarily renal excretion
- Half-life: Approximately 30 hours, permitting once-daily dosing
Benefits
- Provides rapid and effective resolution of symptomatic vulvovaginal candidiasis, often with a single 150 mg dose
- Reduces risk of recurrent fungal infections through suppressive therapy protocols in immunocompromised patients
- Offers convenient oral administration with no requirement for dietary considerations or complex dosing schedules
- Demonstrates reliable systemic distribution, reaching difficult-to-treat sites including urinary tract and meninges
- Minimizes drug interactions compared to earlier azole antifungals, though caution with certain co-administered drugs remains advised
- Supported by decades of clinical use and extensive safety data across diverse patient populations
Common use
Diflucan is commonly prescribed for the treatment of oropharyngeal and esophageal candidiasis, particularly in immunocompromised individuals such as those with HIV/AIDS or undergoing chemotherapy. It is widely utilized for vulvovaginal candidiasis, offering a highly effective single-dose regimen. Additionally, it serves as first-line therapy for cryptococcal meningitis, often following induction with amphotericin B. Medical professionals may also employ Diflucan for prophylaxis against fungal infections in neutropenic patients following cytotoxic chemotherapy or radiation, and for treatment of systemic Candida infections including candidemia, peritonitis, and urinary tract infections when susceptible organisms are identified. Off-label uses may include treatment of certain dermatophytoses and prevention of fungal infections in critically ill patients.
Dosage and direction
Dosage must be individualized based on infection type, severity, and patient factors including renal function. For vulvovaginal candidiasis: 150 mg as a single oral dose. Oropharyngeal candidiasis: 200 mg on first day, then 100 mg once daily for at least 14 days. Esophageal candidiasis: 200 mg on first day, then 100 mg once daily; may increase to 400 mg daily if needed, with treatment typically continuing for 3 weeks after symptom resolution. Systemic Candida infections: 400 mg on first day, then 200 mg once daily, with duration based on clinical response. Cryptococcal meningitis: 400 mg on first day, then 200-400 mg once daily, typically for 10-12 weeks after cerebrospinal fluid becomes culture-negative. For patients with renal impairment (creatinine clearance ≤50 mL/min), dosage adjustment is necessary—typically a 50% reduction in maintenance dosing. Tablets may be taken with or without food. Shake oral suspension well before measuring dose.
Precautions
Hepatic function should be monitored during prolonged therapy, as rare cases of serious hepatotoxicity have been reported. Electrolyte monitoring is advised in patients at risk for hypokalemia. Use with caution in patients with proarrhythmic conditions or those taking medications that prolong QT interval. Renal function should be assessed prior to initiation and periodically during treatment when indicated. Pregnancy Category D: should only be used during pregnancy if potential benefit justifies potential risk to fetus. Nursing mothers should exercise caution, as fluconazole is excreted in human milk at concentrations similar to plasma. Pediatric use is approved for children aged 6 months and older, though dosage must be carefully calculated based on weight. Elderly patients often require dosage adjustments based on renal function.
Contraindications
Hypersensitivity to fluconazole, other azole antifungal agents, or any component of the formulation. Coadministration with cisapride, due to potential for serious cardiac arrhythmias. Use with terfenadine when Diflucan doses of 400 mg/day or higher are administered. Concurrent administration with drugs that prolong QT interval and are metabolized by CYP3A4, such as erythromycin, astemizole, and pimozide. Severe hepatic impairment. Proven hypersensitivity reactions including anaphylaxis to any azole antifungal.
Possible side effect
Common adverse reactions (≥1%) include headache (13%), nausea (7%), abdominal pain (6%), diarrhea (3%), dyspepsia (3%), dizziness (2%), and taste perversion (2%). Skin rash occurs in approximately 2% of patients. Less frequently observed effects include vomiting, fatigue, and generalized pruritus. Serious but rare adverse events include hepatotoxicity (including fatal hepatic necrosis), anaphylaxis, QT interval prolongation, torsades de pointes, seizures, exfoliative skin disorders including Stevens-Johnson syndrome, and agranulocytosis. Alopecia has been reported with prolonged high-dose therapy. Laboratory abnormalities may include elevated hepatic transaminases, alkaline phosphatase, and bilirubin; hypokalemia; and decreased platelet count.
Drug interaction
Diflucan is a moderate inhibitor of CYP2C9 and CYP3A4 and may increase plasma concentrations of drugs metabolized by these enzymes. Significant interactions include: warfarin (prolonged prothrombin time), phenytoin (increased phenytoin concentrations), cyclosporine (increased nephrotoxicity risk), rifampin (decreased fluconazole concentrations), oral hypoglycemics (enhanced hypoglycemic effect), theophylline (increased theophylline concentrations), and statins (increased risk of myopathy/rhabdomyolysis). Concurrent use with other QT-prolonging agents may have additive effects. Diflucan may increase concentrations of benzodiazepines, calcium channel blockers, vinca alkaloids, and certain antiretroviral drugs including saquinavir and zidovudine. Hydrochlorothiazide increases fluconazole concentrations by approximately 40%.
Missed dose
If a dose is missed, it should be taken as soon as remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not take a double dose to make up for a missed one. For once-weekly dosing regimens, if a dose is missed and remembered within 48 hours of the scheduled time, it should be taken immediately. If more than 48 hours have passed, the patient should contact their healthcare provider for guidance. Maintaining consistent blood levels is important for antifungal efficacy, particularly in serious systemic infections.
Overdose
Symptoms of overdose may include pronounced nausea, vomiting, diarrhea, and in severe cases, hallucinations and paranoid behavior. There is no specific antidote for fluconazole overdose. Treatment should be symptomatic and supportive, with gastric lavage considered if presentation is prompt. Hemodialysis for three hours reduces plasma concentrations by approximately 50%, and this may be considered in cases of significant overdose, particularly in patients with impaired renal function. ECG monitoring is advised to detect potential QT prolongation. Patients should be managed in a setting equipped to provide advanced cardiac life support if needed.
Storage
Store tablets and oral suspension at controlled room temperature 20°-25°C (68°-77°F), with excursions permitted between 15°-30°C (59°-86°F). Keep container tightly closed and protect from moisture. Do not freeze the oral suspension. After reconstitution, the oral suspension is stable for 14 days at room temperature; do not refrigerate after mixing. Keep all medications out of reach of children and pets. Properly discard any unused medication after the expiration date or when treatment is completed. Do not flush medications down the toilet or pour into drain unless instructed to do so.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Diflucan is a prescription medication that should only be used under the supervision of a qualified healthcare professional. Individual response to treatment may vary, and proper diagnosis by a healthcare provider is essential before initiating therapy. The prescriber should be informed of all current medications and medical conditions. Patients should not adjust dosage or discontinue treatment without consulting their healthcare provider. Full prescribing information should be reviewed before administration.
Reviews
Clinical studies demonstrate Diflucan’s efficacy with mycological cure rates of 80-90% in vulvovaginal candidiasis and 80-85% in oropharyngeal candidiasis in immunocompromised patients. In cryptococcal meningitis trials, success rates of 60-70% were observed when used as maintenance therapy. Patient satisfaction surveys indicate high approval for convenience of dosing, with 85% of patients reporting preference for single-dose therapy over longer regimens. Dermatological clinical trials show complete clearance in 70-80% of patients with cutaneous fungal infections after 4 weeks of treatment. Long-term safety data from post-marketing surveillance confirms the generally favorable risk-benefit profile established in pre-approval studies.