Fluconazole 40 mg/mL Powder, For Suspension
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Azole Antifungal class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Fluconazole is used to treat fungal infections, including yeast infections of the vagina, mouth, throat, esophagus (tube leading from the mouth to the stomach), abdomen (area between the chest and waist), lungs, blood, and other organs. Fluconazole is also used to treat meningitis (infection of the membranes covering the brain and spine) caused by fungus. Fluconazole is also used to prevent yeast infections in patients who are likely to become infected because they are being treated with chemotherapy or radiation therapy before a bone marrow transplant (replacement of unhealthy spongy tissue i...
Read the full MedlinePlus article ↗- Yes, for a vaginal yeast infection, a single oral dose of fluconazole is the standard treatment with Diflucan or generic fluconazole tablets. Most people see their symptoms clear u...
- I was prescribed fluconazole for a yeast infection — do I really only need one pill?
- Good news — you can take fluconazole tablets with or without food, whichever is easier on your stomach. Studies showed that eating doesn't meaningfully change how much of the drug...
- Can I take fluconazole with food, or does it need to be on an empty stomach?
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Supplement & herbal interactions
Some supplements/herbs that may interact with Fluconazole — tap one for details:
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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UNII XF417D3PSL
Anhydrous citric acid is a sour, crystalline powder derived from citric acid with water removed. In medicines, it acts as a buffer to control pH, adds tartness to improve taste, and helps tablets disintegrate.
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Silicon dioxide is a naturally occurring mineral used as a glidant and anti-caking agent. It helps powder ingredients flow smoothly and prevents clumping during manufacturing and storage.
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Sodium benzoate is a salt derived from benzoic acid, a preservative. It's added to medicines to prevent growth of bacteria, fungi, and other microorganisms that could spoil the product.
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A natural sugar derived from sugar cane or sugar beets. It's used as a sweetener, filler, and binder to improve taste, add bulk, and help hold tablet or capsule ingredients together.
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Titanium dioxide is a bright white mineral powder commonly used as a colorant and opacifying agent. It makes pills and tablets white or lighter in color and helps make coatings non-transparent.
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UNII B22547B95K
A salt derived from citric acid that helps maintain the proper acid-base balance in the medicine. It's used as a buffer to keep the product stable and at the right pH level.
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Xanthan gum is a thickening and stabilizing ingredient made from fermented corn or other sugars. It's added to medicines to improve texture, prevent separation of liquids and solids, and help the product stay consistent.
7 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $0.523 | $18.31 / 35 ml |
| Medicaid paysCMS SDUD · 12 mo | $0.7964 | $27.87 / 35 ml |
| Medicare drug plans payPart D · Q2 2026 | $0.4361 | $15.26 / 35 ml |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Fluconazole 40 mg/mL 16714-0696-01 | NorthStar | 1 bottle | $0.523 | AB | Availability likely | — |
| Fluconazole 40 mg/mL 57237-0150-35 | Rising | 1 bottle | $0.523 | AB | Availability likely | — |
| Fluconazole 40 mg/mLthis 59762-5030-01 | Mylan | 1 bottle | $0.523 | AB | Availability likely | — |
| Fluconazole 40 mg/mL 70436-0227-48 | Slate | 1 bottle | $0.523 | AB | Availability likely | — |
| Diflucan 1400 mg/35mL 00049-3450-19 | Roerig | 1 bottle | — | AB | Discontinued | — |
| Fluconazole 40 mg/mL 65862-0300-35 | Aurobindo | 1 bottle | — | AB | FDA listed | — |
| Fluconazole 40 mg/mL 72673-0091-14 | Zhejiang | 1 bottle | — | AB | FDA listed | — |
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⏳ Availability & generic status
FDA-approved generic versions are listed, and recent pricing/market data suggests they may be available — see Therapeutic equivalents.
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🗺️ Medicaid utilization & spend
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
🔬 Reported adverse events (FAERS)
Top reported reactions
Reporter sex
Serious outcomes
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 59762-5030-01 You're viewing this | 1 BOTTLE in 1 CARTON (59762-5030-1) / 35 mL in 1 BOTTLE | 1993-12-23 | Active |
📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
INDICATIONS AND USAGE Fluconazole is indicated for the treatment of: 1. Vaginal candidiasis (vaginal yeast infections due to Candida ). 2.
Oropharyngeal and esophageal candidiasis. In open noncomparative studies of relatively small numbers of patients, fluconazole was also effective for the treatment of Candida urinary tract infections, peritonitis, and systemic Candida infections including candidemia, disseminated candidiasis, and pneumonia. 3.
Cryptococcal meningitis. Before prescribing fluconazole for AIDS patients with cryptococcal meningitis, please see CLINICAL STUDIES section. Studies comparing fluconazole to amphotericin B in non-HIV infected patients have not been conducted.
Specimens for fungal culture and other relevant laboratory studies (serology, histopathology) should be obtained prior to therapy to isolate and identify causative organisms. Therapy may be instituted before the results of the cultures and other laboratory studies are known; however, once these results become available, anti-infective therapy should be adjusted accordingly. Prophylaxis Fluconazole is also indicated to decrease the incidence of candidiasis in patients undergoing bone marrow transplantation who receive cytotoxic chemotherapy and/or radiation therapy.
⏱️ Dosage and Administration ▾
DOSAGE AND ADMINISTRATION Dosage and Administration in Adults Single Dose Vaginal candidiasis The recommended dosage of fluconazole for vaginal candidiasis is 150 mg as a single oral dose. Multiple Dose SINCE ORAL ABSORPTION IS RAPID AND ALMOST COMPLETE, THE DAILY DOSE OF FLUCONAZOLE IS THE SAME FOR ORAL (TABLETS AND SUSPENSION) AND INTRAVENOUS ADMINISTRATION. In general, a loading dose of twice the daily dose is recommended on the first day of therapy to result in plasma concentrations close to steady-state by the second day of therapy.
The daily dose of fluconazole for the treatment of infections other than vaginal candidiasis should be based on the infecting organism and the patient's response to therapy. Treatment should be continued until clinical parameters or laboratory tests indicate that active fungal infection has subsided. An inadequate period of treatment may lead to recurrence of active infection.
Patients with AIDS and cryptococcal meningitis or recurrent oropharyngeal candidiasis usually require maintenance therapy to prevent relapse. Oropharyngeal candidiasis The recommended dosage of fluconazole for oropharyngeal candidiasis is 200 mg on the first day, followed by 100 mg once daily. Clinical evidence of oropharyngeal candidiasis generally resolves within several days, but treatment should be continued for at least 2 weeks to decrease the likelihood of relapse.
Esophageal candidiasis The recommended dosage of fluconazole for esophageal candidiasis is 200 mg on the first day, followed by 100 mg once daily. Doses up to 400 mg/day may be used, based on medical judgment of the patient's response to therapy. Patients with esophageal candidiasis should be treated for a minimum of three weeks and for at least two weeks following resolution of symptoms.
Systemic Candida infections For systemic Candida infections including candidemia, disseminated candidiasis, and pneumonia, optimal therapeutic dosage and duration of therapy have not been established. In open, noncomparative studies of small numbers of patients, doses of up to 400 mg daily have been used. Urinary tract infections and peritonitis For the treatment of Candida urinary tract infections and peritonitis, daily doses of 50 to 200 mg have been used in open, noncomparative studies of small numbers of patients.
Cryptococcal meningitis The recommended dosage for treatment of acute cryptococcal meningitis is 400 mg on the first day, followed by 200 mg once daily. A dosage of 400 mg once daily may be used, based on medical judgment of the patient's response to therapy. The recommended duration of treatment for initial therapy of cryptococcal meningitis is 10 to 12 weeks after the cerebrospinal fluid becomes culture negative.
The recommended dosage of fluconazole for suppression of relapse of cryptococcal meningitis in patients with AIDS is 200 mg once daily. Prophylaxis in patients undergoing bone marrow transplantation The recommended fluconazole daily dosage for the prevention of candidiasis in patients undergoing bone marrow transplantation is 400 mg, once daily. Patients who are anticipated to have severe granulocytopenia (less than 500 neutrophils cells/mm 3 ) should start fluconazole prophylaxis several days before the anticipated onset of neutropenia, and continue for 7 days after the neutrophil count rises above 1000 cells/mm 3 .
Dosage and Administration in Pediatric Patients Oropharyngeal candidiasis The recommended dosage of fluconazole for oropharyngeal candidiasis in pediatric patients 6 months and older is 6 mg/kg on the first day, followed by 3 mg/kg once daily. Treatment should be administered for at least 2 weeks to decrease the likelihood of relapse. Esophageal candidiasis For the treatment of esophageal candidiasis, the recommended dosage of fluconazole in pediatric patients 6 months and older is 6 mg/kg on the first day, followed by 3 mg/kg once daily.
Doses up to 12 mg/kg/day may be used, based on medical judgment of the patient's response to th…
⛔ Contraindications ▾
CONTRAINDICATIONS Fluconazole is contraindicated in patients who have shown hypersensitivity to fluconazole or to any of its excipients. There is no information regarding cross-hypersensitivity between fluconazole and other azole antifungal agents. Caution should be used in prescribing fluconazole to patients with hypersensitivity to other azoles.
Coadministration of other drugs known to prolong the QT interval and which are metabolized via the enzyme CYP3A4 such as erythromycin, pimozide, and quinidine are contraindicated in patients receiving fluconazole. (See CLINICAL PHARMACOLOGY: Drug Interaction Studies and PRECAUTIONS . )
⚠️ Warnings ▾
WARNINGS (1) Hepatic injury: Fluconazole should be administered with caution to patients with liver dysfunction. Fluconazole has been associated with rare cases of serious hepatic toxicity, including fatalities primarily in patients with serious underlying medical conditions. In cases of fluconazole associated hepatotoxicity, no obvious relationship to total daily dose, duration of therapy, sex, or age of the patient has been observed.
Fluconazole hepatotoxicity has usually, but not always, been reversible on discontinuation of therapy. Patients who develop abnormal liver function tests during fluconazole therapy should be monitored for the development of more severe hepatic injury. Fluconazole should be discontinued if clinical signs and symptoms consistent with liver disease develop that may be attributable to fluconazole.
(2) Anaphylaxis: In rare cases, anaphylaxis has been reported. (3) Dermatologic: Exfoliative skin disorders during treatment with fluconazole have been reported. Fatal outcomes have been reported in patients with serious underlying diseases.
Patients with deep seated fungal infections who develop rashes during treatment with fluconazole should be monitored closely and the drug discontinued if lesions progress. Fluconazole should be discontinued in patients treated for superficial fungal infection who develop a rash that may be attributed to fluconazole. (4) Potential for fetal harm: There are no adequate and well-controlled clinical trials of fluconazole in pregnant women.
Case reports describe a pattern of distinct congenital anomalies in infants exposed in utero to high dose maternal fluconazole (400 to 800 mg/day) during most or all of the first trimester. These reported anomalies are similar to those seen in animal studies. If fluconazole is used during pregnancy or if the patient becomes pregnant while taking the drug, the patient should be informed of the potential hazard to the fetus.
Effective contraceptive measures should be considered in women of child-bearing potential who are being treated with fluconazole 400 to 800 mg/day and should continue throughout the treatment period and for approximately 1 week (5 to 6 half-lives) after the final dose. Epidemiological studies suggest a potential risk of spontaneous abortion and congenital abnormalities in infants whose mothers were treated with 150 mg of fluconazole as a single or repeated dose in the first trimester, but these epidemiological studies have limitations and these findings have not been confirmed in controlled clinical trials.
(See PRECAUTIONS: Pregnancy . )
🤒 Adverse Reactions ▾
ADVERSE REACTIONS Fluconazole is generally well tolerated. In some patients, particularly those with serious underlying diseases such as AIDS and cancer, changes in renal and hematological function test results and hepatic abnormalities have been observed during treatment with fluconazole and comparative agents, but the clinical significance and relationship to treatment is uncertain. In Patients Receiving a Single Dose for Vaginal Candidiasis During comparative clinical studies conducted in the United States, 448 patients with vaginal candidiasis were treated with fluconazole, 150 mg single dose.
The overall incidence of side effects possibly related to fluconazole was 26%. In 422 patients receiving active comparative agents, the incidence was 16%. The most common treatment-related adverse events reported in the patients who received 150 mg single dose fluconazole for vaginitis were headache (13%), nausea (7%), and abdominal pain (6%).
Other side effects reported with an incidence equal to or greater than 1% included diarrhea (3%), dyspepsia (1%), dizziness (1%), and taste perversion (1%). Most of the reported side effects were mild to moderate in severity. Rarely, angioedema and anaphylactic reaction have been reported in marketing experience.
In Patients Receiving Multiple Doses for Other Infections Sixteen percent of over 4000 patients treated with fluconazole in clinical trials of 7 days or more experienced adverse events. Treatment was discontinued in 1.5% of patients due to adverse clinical events and in 1.3% of patients due to laboratory test abnormalities. Clinical adverse events were reported more frequently in HIV infected patients (21%) than in non-HIV infected patients (13%); however, the patterns in HIV infected and non-HIV infected patients were similar.
The proportions of patients discontinuing therapy due to clinical adverse events were similar in the two groups (1.5%). The following treatment-related clinical adverse events occurred at an incidence of 1% or greater in 4048 patients receiving fluconazole for 7 or more days in clinical trials: nausea 3.7%, headache 1.9%, skin rash 1.8%, vomiting 1.7%, abdominal pain 1.7%, and diarrhea 1.5%. Hepato-biliary In combined clinical trials and marketing experience, there have been rare cases of serious hepatic reactions during treatment with fluconazole.
(See WARNINGS ) The spectrum of these hepatic reactions has ranged from mild transient elevations in transaminases to clinical hepatitis, cholestasis and fulminant hepatic failure, including fatalities. Instances of fatal hepatic reactions were noted to occur primarily in patients with serious underlying medical conditions (predominantly AIDS or malignancy) and often while taking multiple concomitant medications. Transient hepatic reactions, including hepatitis and jaundice, have occurred among patients with no other identifiable risk factors.
In each of these cases, liver function returned to baseline on discontinuation of fluconazole. In two comparative trials evaluating the efficacy of fluconazole for the suppression of relapse of cryptococcal meningitis, a statistically significant increase was observed in median AST (SGOT) levels from a baseline value of 30 IU/L to 41 IU/L in one trial and 34 IU/L to 66 IU/L in the other. The overall rate of serum transaminase elevations of more than 8 times the upper limit of normal was approximately 1% in fluconazole-treated patients in clinical trials.
These elevations occurred in patients with severe underlying disease, predominantly AIDS or malignancies, most of whom were receiving multiple concomitant medications, including many known to be hepatotoxic. The incidence of abnormally elevated serum transaminases was greater in patients taking fluconazole concomitantly with one or more of the following medications: rifampin, phenytoin, isoniazid, valproic acid, or oral sulfonylurea hypoglycemic agents. Post-Marketing Experience In addition, the following adverse events have occ…
🔄 Drug Interactions ▾
Drug Interactions (See CONTRAINDICATIONS . ) Fluconazole is a moderate CYP2C9 and CYP3A4 inhibitor. Fluconazole is also a strong inhibitor of CYP2C19. Patients treated with fluconazole, who are also concomitantly treated with drugs with a narrow therapeutic window metabolized through CYP2C9 and CYP3A4, should be monitored for adverse reactions associated with the concomitantly administered drugs.
In addition to the observed /documented interactions mentioned below, there is a risk of increased plasma concentration of other compounds metabolized by CYP2C9, CYP2C19, and CYP3A4 coadministered with fluconazole. Therefore, caution should be exercised when using these combinations and the patients should be carefully monitored. The enzyme inhibiting effect of fluconazole persists 4 to 5 days after discontinuation of fluconazole treatment due to the long half-life of fluconazole.
Clinically or potentially significant drug interactions between fluconazole and the following agents/classes have been observed and are described in greater detail below: Abrocitinib Drug interaction studies indicate that when coadministered with fluconazole (strong inhibitor of CYP2C19; moderate inhibitor of CYP2C9 and CYP3A4), the systemic exposure of abrocitinib and its active metabolites increased. (See CLINICAL PHARMACOLOGY . ) Avoid concomitant use of abrocitinib with fluconazole. Refer to the abrocitinib Prescribing Information for additional details.
Alfentanil A study observed a reduction in clearance and distribution volume as well as prolongation of t ½ of alfentanil following concomitant treatment with fluconazole. A possible mechanism of action is fluconazole's inhibition of CYP3A4. Dosage adjustment of alfentanil may be necessary.
Amiodarone Concomitant administration of fluconazole with amiodarone may increase QT prolongation. Caution must be exercised if the concomitant use of fluconazole and amiodarone is necessary, notably with high dose fluconazole (800 mg). Amitriptyline, nortriptyline Fluconazole increases the effect of amitriptyline and nortriptyline.
5-Nortriptyline and/or S-amitriptyline may be measured at initiation of the combination therapy and after 1 week. Dosage of amitriptyline/nortriptyline should be adjusted, if necessary. Amphotericin B Concurrent administration of fluconazole and amphotericin B in infected normal and immunosuppressed mice showed the following results: a small additive antifungal effect in systemic infection with Candida albicans , no interaction in intracranial infection with Cryptococcus neoformans , and antagonism of the two drugs in systemic infection with A. fumigatus .
The clinical significance of results obtained in these studies is unknown. Azithromycin An open-label, randomized, three-way crossover study in 18 healthy subjects assessed the effect of a single 1200 mg oral dose of azithromycin on the pharmacokinetics of a single 800 mg oral dose of fluconazole as well as the effects of fluconazole on the pharmacokinetics of azithromycin. There was no significant pharmacokinetic interaction between fluconazole and azithromycin.
Calcium channel blockers Certain calcium channel antagonists (nifedipine, isradipine, amlodipine, verapamil, and felodipine) are metabolized by CYP3A4. Fluconazole has the potential to increase the systemic exposure of the calcium channel antagonists. Frequent monitoring for adverse events is recommended.
Carbamazepine Fluconazole inhibits the metabolism of carbamazepine and an increase in serum carbamazepine of 30% has been observed. There is a risk of developing carbamazepine toxicity. Dosage adjustment of carbamazepine may be necessary depending on concentration measurements/effect.
Celecoxib During concomitant treatment with fluconazole (200 mg daily) and celecoxib (200 mg), the celecoxib C max and AUC increased by 68% and 134%, respectively. Half of the celecoxib dose may be necessary when combined with fluconazole. Coumarin-type anticoagulants Prothrombin time may be incre…
🤰 Pregnancy ▾
Pregnancy Teratogenic Effects Potential for Fetal Harm Use in pregnancy should be avoided except in patients with severe or potentially life-threatening fungal infections in whom fluconazole may be used if the anticipated benefit outweighs the possible risk to the fetus. A few published case reports describe a pattern of distinct congenital anomalies in infants exposed in utero to high dose maternal fluconazole (400 to 800 mg/day) during most or all of the first trimester. These reported anomalies are similar to those seen in animal studies.
Effective contraceptive measures should be considered in women of child-bearing potential who are being treated with fluconazole 400 to 800 mg/day and should continue throughout the treatment period and for approximately 1 week (5 to 6 half-lives) after the final dose. If fluconazole is used during pregnancy, or if the patient becomes pregnant while taking the drug, the patient should be informed of the potential hazard to the fetus. Spontaneous abortions and congenital abnormalities have been suggested as potential risks associated with 150 mg of fluconazole as a single or repeated dose in the first trimester of pregnancy based on retrospective epidemiological studies.
There are no adequate and well-controlled studies of fluconazole in pregnant women. (See WARNINGS: Potential for Fetal Harm .) Human Data Case reports describe a distinctive and rare pattern of birth defects among infants whose mothers received high-dose (400 to 800 mg/day) fluconazole during most or all of the first trimester of pregnancy. The features seen in these infants include: brachycephaly, abnormal facies, abnormal calvarial development, cleft palate, femoral bowing, thin ribs and long bones, arthrogryposis, and congenital heart disease.
These effects are similar to those seen in animal studies. Epidemiological studies suggest a potential risk of spontaneous abortion and congenital abnormalities in infants whose mothers were treated with 150 mg of fluconazole as a single or repeated dose in the first trimester, but these epidemiological studies have limitations and these findings have not been confirmed in controlled clinical trials. Animal Data Fluconazole was administered orally to pregnant rabbits during organogenesis in two studies at doses of 5 mg/kg, 10 mg/kg, and 20 mg/kg and at 5 mg/kg, 25 mg/kg, and 75 mg/kg, respectively.
Maternal weight gain was impaired at all dose levels (approximately 0.25 to 4 times the 400 mg clinical dose based on body surface area [BSA] comparison), and abortions occurred at 75 mg/kg (approximately 4 times the 400 mg clinical dose based on BSA); no adverse fetal effects were observed. In several studies in which pregnant rats received fluconazole orally during organogenesis, maternal weight gain was impaired and placental weights were increased at 25 mg/kg. There were no fetal effects at 5 mg/kg or 10 mg/kg; increases in fetal anatomical variants (supernumerary ribs, renal pelvis dilation) and delays in ossification were observed at 25 mg/kg and 50 mg/kg and higher doses.
At doses ranging from 80 to 320 mg/kg (approximately 2 to 8 times the 400 mg clinical dose based on BSA), embryolethality in rats was increased and fetal abnormalities included wavy ribs, cleft palate, and abnormal craniofacial ossification. These effects are consistent with the inhibition of estrogen synthesis in rats and may be a result of known effects of lowered estrogen on pregnancy, organogenesis, and parturition.
🧒 Pediatric Use ▾
Pediatric Use Use in Pediatric Patients for the Treatment of Oropharyngeal Candidiasis An open-label, randomized, controlled trial has shown fluconazole to be effective in the treatment of oropharyngeal candidiasis in pediatric patients 6 months to 13 years of age. (See CLINICAL STUDIES . ) Use in Pediatric Patients for the Treatment of Candida Esophagitis, Systemic Candida Infections, or Cryptococcal Meningitis The use of fluconazole in pediatric patients with cryptococcal meningitis, Candida esophagitis, or systemic Candida infections is supported by the efficacy shown for these indications in adults and by the results from several small noncomparative pediatric clinical studies.
In addition, pharmacokinetic studies in pediatric patients (See CLINICAL PHARMACOLOGY . ) have established a dose proportionality between pediatric patients and adults. (See DOSAGE AND ADMINISTRATION . ) In a noncomparative study of fluconazole administered to pediatric patients (from birth to less than 17 years) with serious systemic fungal infections, most of which were candidemia, the effectiveness of fluconazole was similar to that reported for the treatment of candidemia in adults. Of 17 subjects with culture-confirmed candidemia, 11 of 14 (79%) with baseline symptoms (3 were asymptomatic) had a clinical cure; 13/15 (87%) of evaluable patients had a mycologic cure at the end of treatment but two of these patients relapsed at 10 and 18 days, respectively, following cessation of therapy.
The efficacy of fluconazole for the suppression of cryptococcal meningitis was successful in 4 of 5 pediatric patients (4 years to 10 years of age) treated in a compassionate-use study of fluconazole for the treatment of life-threatening or serious mycosis. There are limited clinical data to support the efficacy of fluconazole for the primary treatment of cryptococcal meningitis in pediatric patients. The safety profile of fluconazole has been studied in 577 pediatric patients 1 from 1 day to 17 years of age who received doses ranging from 1 to 15 mg/kg/day for 1 to 1,616 days.
(See ADVERSE REACTIONS . ) Use in Pediatric Patients on Extracorporeal Membrane Oxygenation (ECMO) A prospective, open-label, single-center study was conducted to determine the PK and safety of fluconazole in pediatric patients (ages: from birth to 17 years of age) on ECMO (See CLINICAL PHARMACOLOGY ). A loading dose of 35-mg/kg is recommended in pediatric patients on ECMO due to increased volume of distribution (See DOSAGE AND ADMINISTRATION ). Use in Prophylaxis of Invasive Candida Infections in Pediatric Patients (premature infants weighing less than 750 grams at birth) Safety and effectiveness of fluconazole for the prophylaxis of invasive candidiasis in pediatric patients (premature infants weighing less than 750 grams at birth) have not been established.
A prospective, randomized, double-blind, placebo-controlled, multicenter trial was conducted in premature infants weighing less than 750 grams at birth to evaluate the efficacy and safety of prophylactic fluconazole 6-mg/kg administered twice weekly for 6 weeks versus placebo (NCT00734539). Efficacy was assessed using the endpoint of death or candidiasis by study day 49. The results are summarized in Table 4 .
Table 4: Death or Candidiasis by Day 49 in Premature Infants Receiving Fluconazole Prophylaxis Fluconazole (N=188) n (%) Placebo (N=173) n (%) P-value Difference (95% CI) Death or candidiasis* 33 (17.6) 38 (22.0) 0.2954 -4.4(-12.6, 3.8) Components of endpoint** Death Candidiasis Missing 27 (14.4) 6 (3.2) 2 (1.0) 25 (14.5) 16 (9.2) 1 (0.5) * Subjects with missing data are imputed as having candidiasis or died. **Subjects may be counted more than once as two fluconazole subjects and four placebo subjects diagnosed with candidiasis subsequently died by day 49.
The most common fatal serious adverse reactions in the fluconazole vs placebo arms, respectively, were necrotizing enterocolitis (NEC), 9 (5%) vs 9 (5%); neonatal bacterial…
🧓 Geriatric Use ▾
Geriatric Use In non-AIDS patients, side effects possibly related to fluconazole treatment were reported in fewer patients aged 65 and older (9%, n =339) than for younger patients (14%, n=2240). However, there was no consistent difference between the older and younger patients with respect to individual side effects. Of the most frequently reported (>1%) side effects, rash, vomiting, and diarrhea occurred in greater proportions of older patients.
Similar proportions of older patients (2.4%) and younger patients (1.5%) discontinued fluconazole therapy because of side effects. In post-marketing experience, spontaneous reports of anemia and acute renal failure were more frequent among patients 65 years of age or older than in those between 12 and 65 years of age. Because of the voluntary nature of the reports and the natural increase in the incidence of anemia and renal failure in the elderly, it is however not possible to establish a causal relationship to drug exposure.
Controlled clinical trials of fluconazole did not include sufficient numbers of patients aged 65 and older to evaluate whether they respond differently from younger patients in each indication. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. Fluconazole is primarily cleared by renal excretion as unchanged drug.
Because elderly patients are more likely to have decreased renal function, care should be taken to adjust dose based on creatinine clearance. It may be useful to monitor renal function. (See CLINICAL PHARMACOLOGY and DOSAGE AND ADMINISTRATION . )
🆘 Overdosage ▾
OVERDOSAGE There have been reports of overdose with fluconazole accompanied by hallucination and paranoid behavior. In the event of overdose, symptomatic treatment (with supportive measures and gastric lavage if clinically indicated) should be instituted. Fluconazole is largely excreted in urine.
A 3-hour hemodialysis session decreases plasma levels by approximately 50%. In mice and rats receiving very high doses of fluconazole, clinical effects in both species included decreased motility and respiration, ptosis, lacrimation, salivation, urinary incontinence, loss of righting reflex, and cyanosis; death was sometimes preceded by clonic convulsions.
🧬 Clinical Pharmacology ▾
CLINICAL PHARMACOLOGY Pharmacokinetics and Metabolism The pharmacokinetic properties (PK) of fluconazole are similar following administration by the intravenous or oral routes. In normal volunteers, the bioavailability of orally administered fluconazole is over 90% compared with intravenous administration. Bioequivalence was established between the 100 mg tablet and both suspension strengths when administered as a single 200 mg dose.
Peak plasma concentrations (Cmax) in fasted normal volunteers occur between 1 and 2 hours with a terminal plasma elimination half-life of approximately 30 hours (range: 20 to 50 hours) after oral administration. In fasted normal volunteers, administration of a single oral 400 mg dose of fluconazole leads to a mean Cmax of 6.72 mcg/mL (range: 4.12 to 8.08 mcg/mL) and after single or multiple oral doses of 50 to 400 mg, fluconazole plasma concentrations and area under the plasma concentration time curve (AUC) are dose proportional ( Table 1 ).
The Cmax and AUC data from a food-effect study involving administration of fluconazole tablets to healthy volunteers under fasting conditions and with a high-fat meal indicated that exposure to the drug is not affected by food. Therefore, fluconazole may be taken without regard to meals. (See DOSAGE AND ADMINISTRATION .) Table 1: Mean Pharmacokinetic Parameters of Fluconazole in Adult Healthy Volunteers Following the Administration of Fluconazole Dose Regimen Cmax (mcg/mL) AUC0-24 (mcg*h/mL) Half-life (hours) 50 mg oral (once daily x 7 days) 2.21 37.6 26.6 100 mg oral (once daily x 7 days) 4.81 82.5 27.7 150 mg single oral 2.70 137* 34.1 200 mg oral (once daily x 14 days) 10.12 169.5 31 300 mg oral (once daily x 14 days) 15.98 299.4 34 400 mg oral (once daily x 14 days) 18.89 349.9 31 *AUC 0-inf.
Cmax= peak plasma concentrations, AUC =area under the plasma concentration time curve. Steady-state concentrations are reached within 5 to 10 days following oral doses of 50 to 400 mg given once daily. Administration of a loading dose (on Day 1) of twice the usual daily dose results in plasma concentrations close to steady-state by the second day.
The apparent volume of distribution of fluconazole approximates that of total body water. Plasma protein binding is low (11 to 12%). Following either single- or multiple oral doses for up to 14 days, fluconazole penetrates into all body fluids studied (See table below).
In normal volunteers, saliva concentrations of fluconazole were equal to or slightly greater than plasma concentrations regardless of dose, route, or duration of dosing. In patients with bronchiectasis, sputum concentrations of fluconazole following a single 150 mg oral dose were equal to plasma concentrations at both 4 and 24 hours post dose. In patients with fungal meningitis, fluconazole concentrations in the cerebrospinal fluid (CSF) are approximately 80% of the corresponding plasma concentrations.
A single oral 150 mg dose of fluconazole administered to 27 patients penetrated into vaginal tissue, resulting in tissue: plasma ratios ranging from 0.94 to 1.14 over the first 48 hours following dosing. A single oral 150 mg dose of fluconazole administered to 14 patients penetrated into vaginal fluid, resulting in fluid: plasma ratios ranging from 0.36 to 0.71 over the first 72 hours following dosing. Table 2: Ratio of Fluconazole Tissue (Fluid)/Plasma Concentration Tissue or Fluid Ratio of Fluconazole Tissue (Fluid)/Plasma Concentration Relative to concurrent concentrations in plasma in subjects with normal renal function Cerebrospinal fluid Independent of degree of meningeal inflammation 0.5–0.9 Saliva 1 Sputum 1 Blister fluid 1 Urine 10 Normal skin 10 Nails 1 Blister skin 2 Vaginal tissue 1 Vaginal fluid 0.4–0.7 Mean body clearance in adults is reported to be 0.23 (17%) mL/min/kg.
In normal volunteers, fluconazole is cleared primarily by renal excretion, with approximately 80% of the administered dose appearing in the urine as unchanged drug. About 11% of t…
🧬 Mechanism of Action ▾
Mechanism of Action Fluconazole is a highly selective inhibitor of fungal cytochrome P450 dependent enzyme lanosterol 14-α-demethylase. This enzyme functions to convert lanosterol to ergosterol. The subsequent loss of normal sterols correlates with the accumulation of 14-α-methyl sterols in fungi and may be responsible for the fungistatic activity of fluconazole. Mammalian cell demethylation is much less sensitive to fluconazole inhibition.
📦 How Supplied / Storage and Handling ▾
HOW SUPPLIED Fluconazole Tablets Pink trapezoidal tablets containing 50, 100, or 200 mg of fluconazole are packaged in bottles or unit dose blisters. The 150 mg fluconazole tablets are pink and oval shaped, packaged in a single dose unit blister. Fluconazole Tablets are supplied as follows: Fluconazole 50 mg Tablets: Embossed with "FLZ 50" on one side with no markings on the other side.
NDC 59762-5015-1 Bottles of 30 Fluconazole 100 mg Tablets: Embossed with "FLZ 100" on one side with no markings on the other side. NDC 59762-5016-1 Bottles of 30 Fluconazole 150 mg Tablets: Embossed with "FLZ 150" on one side with no markings on the other side. NDC 59762-5017-1 Unit dose package of 12 Fluconazole 200 mg Tablets: Embossed with "FLZ 200" on one side with no markings on the other side.
NDC 59762-5018-1 Bottles of 30 Storage Store tablets below 30°C (86°F). Fluconazole for Oral Suspension Fluconazole for Oral Suspension is supplied as an orange-flavored powder to provide 35 mL per bottle as follows: NDC 59762-5029-1 Fluconazole 350 mg per bottle NDC 59762-5030-1 Fluconazole 1400 mg per bottle Storage Store dry powder below 30°C (86°F). Store reconstituted suspension between 30°C (86°F) and 5°C (41°F) and discard unused portion after 2 weeks.
Protect from freezing.
📦 Storage and Handling ▾
Storage Store tablets below 30°C (86°F).
Storage Store dry powder below 30°C (86°F). Store reconstituted suspension between 30°C (86°F) and 5°C (41°F) and discard unused portion after 2 weeks. Protect from freezing.
📋 Description ▾
DESCRIPTION Fluconazole, the first of a new subclass of synthetic triazole antifungal agents, is available as tablets for oral administration, as a powder for oral suspension. Fluconazole is designated chemically as 2,4-difluoro-α,α 1 -bis(1H-1,2,4-triazol-1-ylmethyl) benzyl alcohol with an empirical formula of C 13 H 12 F 2 N 6 O and molecular weight of 306.3. The structural formula is: Fluconazole is a white crystalline solid which is slightly soluble in water and saline.
Fluconazole Tablets contain 50 mg, 100 mg, 150 mg, or 200 mg of fluconazole and the following inactive ingredients: microcrystalline cellulose, dibasic calcium phosphate anhydrous, povidone, croscarmellose sodium, FD&C Red No. 40 aluminum lake dye, and magnesium stearate. Fluconazole for Oral Suspension contains 350 mg or 1400 mg of fluconazole and the following inactive ingredients: sucrose, sodium citrate dihydrate, citric acid anhydrous, sodium benzoate, titanium dioxide, colloidal silicon dioxide, xanthan gum, and natural orange flavor.
After reconstitution with 24 mL of distilled water or Purified Water (USP), each mL of reconstituted suspension contains 10 mg or 40 mg of fluconazole. Chemical Structure