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FLUCONAZOLE TABLETS

DESCRIPTION

Fluconazole is the first of a new subclass of synthetic triazole antifungal agents. Fluconazole is designated chemically as 2,4-difluoro-α,α1-bis(1H-1,2,4-triazol-1-ylmethyl) benzyl alcohol and has the following structural formula:

C13H12F2N6O M.W. 306.3

Fluconazole is a white crystalline solid which is slightly soluble in water and saline.

Fluconazole tablets, for oral administration, contain 50, 100, 150, or 200 mg of fluconazole and have the following inactive ingredients: colloidal silicon dioxide, corn starch, croscarmellose sodium, FD&C red #40 aluminum lake, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and talc.

CLINICAL PHARMACOLOGY

Mode of Action

Fluconazole is a highly selective inhibitor of fungal cytochrome P-450 sterol C-14 alpha-demethylation. Mammalian cell demethylation is much less sensitive to fluconazole inhibition. The subsequent loss of normal sterols correlates with the accumulation of 14 alpha-methyl sterols in fungi and may be responsible for the fungistatic activity of fluconazole.

Pharmacokinetics and Metabolism

The pharmacokinetic properties 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 oral doses of 50 to 400 mg, fluconazole plasma concentrations and AUC (area under the plasma concentration-time curve) are dose proportional.

Administration of a single oral 150 mg tablet of fluconazole to ten lactating women resulted in a mean Cmax of 2.61 mcg/mL (range: 1.57 to 3.65 mcg/mL).

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 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.

*Relative to concurrent concentrations in plasma in subjects with normal renal function.

Independent of degree of meningeal inflammation.

Tissue or FluidRatio of Fluconazole Tissue (Fluid)/Plasma Concentration*
Cerebrospinal fluid0.5 to 0.9
Saliva1
Sputum1
Buler fluid1
Urine10
Normal Skin10
Nails1
Buler skin2
Vaginal tissue1
Vaginal fluid0.4 to 0.7

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 the dose is excreted in the urine as metabolites.

The pharmacokinetics of fluconazole are markedly affected by reduction in renal function. There is an inverse relationship between the elimination half-life and creatinine clearance. The dose of fluconazole may need to be reduced in patients with impaired renal function (see DOSAGE AND ADMINISTRATION). A 3-hour hemodialysis session decreases plasma concentrations by approximately 50%.

In normal volunteers, fluconazole administration (doses ranging from 200 mg to 400 mg once daily for up to 14 days) was associated with small and inconsistent effects on testosterone concentrations, endogenous corticosteroid concentrations, and the ACTH-stimulated cortisol response.

Pharmacokinetics in Children

In children, the following pharmacokinetic data {Mean(%cv)} have been reported:

Age StudiedDose (mg/kg)Clearance (mL/min/kg)Half-life (Hours)Cmax (mcg/mL)Vdss (L/kg)
9 Months to 13 yearsSingle-Oral 2 mg/kg0.40 (38%) N=1425.02.9 (22%) N=16-
9 Months to 13 yearsSingle-Oral 8 mg/kg0.51 (60%) N=1519.59.8 (20%) N=15-
5 to 15 yearsMultiple IV 2 mg/kg0.49 (40%) N=417.45.5 (25%) N=50.722 (36%) N=4
5 to 15 yearsMultiple IV 4 mg/kg0.59 (64%) N=515.211.4 (44%) N=60.729 (33%) N=5
5 to 15 yearsMultiple IV 8 mg/kg0.66 (31%) N=717.614.1 (22%) N=81.069 (37%) N=7

Clearance corrected for body weight was not affected by age in these studies. Mean body clearance in adults is reported to be 0.23 (17%) mL/min/kg.

In premature newborns (gestational age 26 to 29 weeks), the mean (%cv) clearance within 36 hours of birth was 0.180 (35%, N=7) mL/min/kg, which increased with time to a mean of 0.218 (31%, N=9) mL/min/kg six days later and 0.333 (56%, N=4) mL/min/kg 12 days later. Similarly, the half-life was 73.6 hours, which decreased with time to a mean of 53.2 hours six days later and 46.6 hours 12 days later.

Pharmacokinetics in Elderly

A pharmacokinetic study was conducted in 22 subjects, 65 years of age or older receiving a single 50 mg oral dose of fluconazole. Ten of these patients were concomitantly receiving diuretics. The Cmax was 1.54 mcg/mL and occurred at 1.3 hours post dose. The mean AUC was 76.4+ 20.3 mcg∙h/mL, and the mean terminal half-life was 46.2 hours. These pharmacokinetic parameter values are higher than analogous values reported for normal young male volunteers. Coadministration of diuretics did not significantly alter AUC or Cmax. In addition, creatinine clearance (74 mL/min), the percent of drug recovered unchanged in urine (0-24 hr, 22%) and the fluconazole renal clearance estimates (0.124 mL/min/kg) for the elderly were generally lower than those of younger volunteers. Thus, the alteration of fluconazole disposition in the elderly appears to be related to reduced renal function characteristic of this group. A plot of each subject’s terminal elimination half-life versus creatinine clearance compared with the predicted half-life – creatinine clearance curve derived from normal subjects and subjects with varying degrees of renal insufficiency indicated that 21 of 22 subjects fell within the 95% confidence limit of the predicted half-life – creatinine clearance curves. These results are consistent with the hypothesis that higher values for the pharmacokinetic parameters observed in the elderly subjects compared with normal young male volunteers are due to the decreased kidney function that is expected in the elderly.

Drug Interaction Studies

Oral Hypoglycemics

The effects of fluconazole on the pharmacokinetics of the sulfonylurea oral hypoglycemic agents tolbutamide, glipizide, and glyburide were evaluated in three placebo-controlled studies in normal volunteers. All subjects received the sulfonylurea alone as a single dose and again as a single dose following the administration of fluconazole 100 mg daily for 7 days. In these three studies 22/46 (47.8%) of fluconazole treated patients and 9/22 (40.1%) of placebo treated patients experienced symptoms consistent with hypoglycemia (see PRECAUTIONS).

Microbiology

Fluconazole exhibits in vitro activity against Cryptococcus neoformans and Candida spp. Fungistatic activity has also been demonstrated in normal and immunocompromised animal models for systemic and intracranial fungal infections due to Cryptococcus neoformans and for systemic infections due to Candida albicans.

In common with other azole antifungal agents, most fungi show a higher apparent sensitivity to fluconazole in vivo than in vitro. Fluconazole administered orally and/or intravenously was active in a variety of animal models of fungal infection using standard laboratory strains of fungi. Activity has been demonstrated against fungal infections caused by Aspergillus flavus and Aspergillus fumigatus in normal mice. Fluconazole has also been shown to be active in animal models of endemic mycoses, including one model of Blastomyces dermatitidis pulmonary infections in normal mice; one model of Coccidioides immitis intracranial infections in normal mice; and several models of Histoplasma capsulatum pulmonary infection in normal and immunosuppressed mice. The clinical significance of results obtained in these studies is unknown.

Oral fluconazole has been shown to be active in an animal model of vaginal candidiasis.

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 C. albicans, no interaction in intracranial infection with Cr. neoformans, and antagonism of the two drugs in systemic infection with Asp. fumigatus. The clinical significance of results obtained in these studies is unknown.

There have been reports of cases of superinfection with Candida species other than C. albicans, which are often inherently not susceptible to fluconazole (e.g., Candida krusei). Such cases may require alternative antifungal therapy.

INDICATIONS AND USAGE

Fluconazole tablets are indicated for the treatment of:

  • Vaginal candidiasis (vaginal yeast infections due to Candida).
  • 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.
  • Cryptococcal meningitis. Before prescribing fluconazole for AIDS patients with cryptococcal meningitis, please see Clinical Studies. Studies comparing fluconazole to amphotericin B in non-HIV infected patients have not been conducted.

Prophylaxis

Fluconazole tablets are also indicated to decrease the incidence of candidiasis in patients undergoing bone marrow transplantation who receive cytotoxic chemotherapy and/or radiation therapy.

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

Clinical Studies

Pediatric Studies

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 terfenadine is contraindicated in patients receiving fluconazole at multiple doses of 400 mg or higher based upon results of a multiple dose interaction study. Coadministration of cisapride is contraindicated in patients receiving fluconazole (see CLINICAL PHARMACOLOGY, Drug Interaction Studies and PRECAUTIONS).

WARNINGS

1. Hepatic Injury

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

Patients have rarely developed exfoliative skin disorders during treatment with fluconazole. In patients with serious underlying diseases (predominantly AIDS and malignancy), these have rarely resulted in a fatal outcome. Patients who develop rashes during treatment with fluconazole should be monitored closely and the drug discontinued if lesions progress.

PRECAUTIONS

General

Some azoles, including fluconazole, have been associated with prolongation of the QT interval on the electrocardiogram. During postmarketing surveillance, there have been rare cases of QT prolongation and torsade de pointes in patients taking fluconazole. Most of these reports involved seriously ill patients with multiple confounding risk factors, such as structural heart disease, electrolyte abnormalities and concomitant medications that may have been contributory.

Fluconazole should be administered with caution to patients with these potentially proarrhythmic conditions.

Drug Interactions

(See CLINICAL PHARMACOLOGY, Drug Interaction Studies and CONTRAINDICATIONS). Clinically or potentially significant drug interactions between fluconazole and the following agents/classes have been observed. These are described in greater detail below:

Oral hypoglycemicsRifampinAstemizole
Coumarin-type anticoagulantsTheophyllineRifabutin
PhenytoinTerfenadineTacrolimus
CyclosporineCisaprideShort-acting benzodiazepines

Carcinogenesis, Mutagenesis and Impairment of Fertility

Fluconazole showed no evidence of carcinogenic potential in mice and rats treated orally for 24 months at doses of 2.5, 5 or 10 mg/kg/day (approximately 2 to 7 x the recommended human dose). Male rats treated with 5 and 10 mg/kg/day had an increased incidence of hepatocellular adenomas.

Fluconazole, with or without metabolic activation, was negative in tests for mutagenicicty in 4 strains of S. typhimurium, and in the mouse lymphoma L5178Y system. Cytogenetic studies in vivo (murine bone marrow cells, following oral administration of fluconazole) and in vitro (human lymphocytes exposed to fluconazole at 1000 mcg/mL) showed no evidence of chromosomal mutations.

Fluconazole did not affect the fertility of male or female rats treated orally with daily doses of 5, 10 or 20 mg/kg or with parenteral doses of 5, 25 or 75 mg/kg, although the onset of parturition was slightly delayed at 20 mg/kg PO. In an intravenous perinatal study in rats at 5, 20 and 40 mg/kg, dystocia and prolongation of parturition were observed in a few dams at 20 mg/kg (approximately 5 to 15 x the recommended human dose) and 40 mg/kg, but not at 5 mg/kg. The disturbances in parturition were reflected by a slight increase in the number of still-born pups and decrease of neonatal survival at these dose levels. The effects on parturition in rats are consistent with the species specific estrogen-lowering property produced by high doses of fluconazole. Such a hormone change has not been observed in women treated with fluconazole (see CLINICAL PHARMACOLOGY).

Pregnancy

Teratogenic Effects

Nursing Mothers

Fluconazole is secreted in human milk at concentrations similar to plasma. Therefore, the use of fluconazole in nursing mothers is not recommended.

Pediatric Use

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).

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 pediatric patients 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 treated in a compassionate-use study of fluconazole for the treatment of life-threatening or serious mycosis. There is no information regarding the efficacy of fluconazole for primary treatment of cryptococcal meningitis in pediatric patients.

The safety profile of fluconazole in pediatric patients has been studied in 577 pediatric patients ages 1 day to 17 years who received doses ranging from 1 to 15 mg/kg/day for 1 to 1,616 days (see ADVERSE REACTIONS).

Efficacy of fluconazole has not been established in infants less than 6 months of age (see CLINICAL PHARMACOLOGY). A small number of patients (29) ranging in age from 1 day to 6 months have been treated safely with fluconazole.

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 casual 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.)

ADVERSE REACTIONS

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 side 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%.

Post-Marketing Experience

In addition, the following adverse events have occurred during post-marketing experience.

Adverse Reactions in Pediatric Patients

In Phase II/III clinical trials conducted in the United States and in Europe, 577 pediatric patients, ages 1 day to 17 years were treated with fluconazole at doses up to 15 mg/kg/day for up to 1,616 days. Thirteen percent of pediatric patients experienced treatment related adverse events. The most commonly reported events were vomiting (5%), abdominal pain (3%), nausea (2%), and diarrhea (2%). Treatment was discontinued in 2.3% of patients due to adverse clinical events and in 1.4% of patients due to laboratory test abnormalities. The majority of treatment-related laboratory abnormalities were elevations of transaminases or alkaline phosphatase.

Percentage of Patients With Treatment-Related Side Effects
Fluconazole(N=577)Comparative Agents(N=451)
With any side effect13.09.3
Vomiting5.45.1
Abdominal pain2.81.6
Nausea2.31.6
Diarrhea2.12.2

OVERDOSAGE

There have been reports of overdosage with fluconazole. A 42-year-old patient infected with human immunodeficiency virus developed hallucinations and exhibited paranoid behavior after reportedly ingesting 8200 mg of fluconazole. The patient was admitted to the hospital, and his condition resolved within 48 hours.

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 three-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.

DOSAGE AND ADMINISTRATION

Dosage and Administration in Adults

Single Dose

Multiple Dose

SINCE ORAL ABSORPTION IS RAPID AND ALMOST COMPLETE, THE DAILY DOSE OF FLUCONAZOLE IS THE SAME FOR ORAL 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.

Dosage and Administration in Pediatric Patients

The following dose equivalency scheme should generally provide equivalent exposure in pediatric and adult patients:

Pediatric PatientsAdults

* Some older children may have clearances similar to that of adults. Absolute doses exceeding 600 mg/day are not recommended.

3 mg/kg100 mg
6 mg/kg200 mg
12* mg/kg400 mg

Experience with fluconazole in neonates is limited to pharmacokinetic studies in premature newborns (see CLINICAL PHARMACOLOGY). Based on the prolonged half-life seen in premature newborns (gestational age 26 to 29 weeks), these children, in the first two weeks of life, should receive the same dosage (mg/kg) as in older children, but administered every 72 hours. After the first two weeks, these children should be dosed once daily. No information regarding fluconazole pharmacokinetics in full-term newborns is available.

Dosage in Patients With Impaired Renal Function

Fluconazole is cleared primarily by renal excretion as unchanged drug. There is no need to adjust single dose therapy for vaginal candidiasis because of impaired renal function. In patients with impaired renal function who will receive multiple doses of fluconazole, an initial loading dose of 50 to 400 mg should be given. After the loading dose, the daily dose (according to indication) should be based on the following table:

Creatinine Clearance (mL/min)Percent of Recommended Dose
>50100%
≤50 (no dialysis)50%
Regular dialysis100% after each dialysis

These are suggested dose adjustments based on pharmacokinetics following administration of multiple doses. Further adjustment may be needed depending upon clinical condition.

When serum creatinine is the only measure of renal function available, the following formula (based on sex, weight, and age of the patient) should be used to estimate the creatinine clearance in adults:

Males:Weight (kg) x (140-age)
72 x serum creatinine (mg/100 mL)
Females:0.85 x above value

Although the pharmacokinetics of fluconazole has not been studied in children with renal insufficiency, dosage reduction in children with renal insufficiency should parallel that recommended for adults. The following formula may be used to estimate creatinine clearance in children:

K xlinear length or height (cm)
serum creatinine (mg/100mL)

(Where K=0.55 for children older than 1 year and 0.45 for infants.)

HOW SUPPLIED

Fluconazole Tablets, 50 mg are available as pink, modified oval-shaped, unscored tablets, debossed “5410” on one side and

“50” on the other side and packaged in bottles of 30, 100 and unit-dose boxes of 100 tablets.

Fluconazole Tablets, 100 mg are available as pink, modified oval-shaped, unscored tablets, debossed “5411” on one side and

“100” on the other side and packaged in bottles of 30, 100 and unit-dose boxes of 100 tablets.

Fluconazole Tablets, 150 mg are available as pink, modified oval-shaped, unscored tablets, debossed “5412” on one side and

“150” on the other side and packaged in unit-of-use cards of 1 tablet.

Fluconazole Tablets, 200 mg are available as pink, modified oval-shaped, unscored tablets, debossed “5413” on one side and

“200” on the other side and packaged in bottles of 30, 100 and unit-dose boxes of 100 tablets.

PHARMACIST: Dispense in a tight container as defined in the USP. Use child-resistant closure (as required).

Store at 20°-25°C (68°-77°F) [See USP Controlled Room Temperature].

PATIENT INFORMATION

Fluconazole Tablets

This leaflet contains important information about fluconazole. It is not meant to take the place of your doctor’s instructions. Read this information carefully before you take fluconazole. Ask your doctor or pharmacist if you do not understand any of this information or if you want to know more about fluconazole.

What is Fluconazole?

Fluconazole is a tablet you swallow to treat vaginal yeast infections caused by a yeast called Candida. Fluconazole helps stop too much yeast from growing in the vagina so the yeast infection goes away.

Fluconazole is different from other treatments for vaginal yeast infections because it is a tablet taken by mouth. Fluconazole is used for other conditions. However, this leaflet is only about using fluconazole for vaginal yeast infections. For information about using fluconazole for other reasons, ask your doctor or pharmacist. See the section of this leaflet for information about vaginal yeast infections.

What is a Vaginal Yeast Infection?

It is normal for a certain amount of yeast to be found in the vagina. Sometimes too much yeast starts to grow in the vagina and this can cause a yeast infection. Vaginal yeast infections are common. About three out of every four adult women will have at least one vaginal yeast infection during their life.

Some medicines and medical conditions can increase your chance of getting a yeast infection. If you are pregnant, have diabetes, use birth control pills, or take antibiotics you may get yeast infections more often than other women. Personal hygiene and certain types of clothing may increase your chances of getting a yeast infection. Ask your doctor for tips on what you can do to help prevent vaginal yeast infections.

If you get a vaginal yeast infection, you may have any of the following symptoms:

  • itching
  • a burning feeling when you urinate
  • redness
  • soreness
  • a thick white vaginal discharge that looks like cottage cheese

What To Tell Your Doctor Before You Start Fluconazole?

Do not take fluconazole if you take certain medicines. They can cause serious problems.

Therefore, tell your doctor about all the medicines you take including:

  • diabetes medicines you take by mouth such as glyburide, tolbutamide, glipizide
  • blood thinners such as warfarin
  • cyclosporine (used to prevent rejection of organ transplants)
  • rifampin or rifabutin (used for tuberculosis)
  • astemizole (used for allergies)
  • tacrolimus (used to prevent rejection of organ transplants)
  • phenytoin (used for seizures)
  • theophylline (used for asthma)
  • cisapride (Propulsid®; used for stomach acid problems)
  • terfenadine (Seldane®; used for allergies)

Since there are many brand names for these medicines, check with your doctor or pharmacist if you have any questions.

  • are taking any over-the-counter medicines you can buy without a prescription, including natural or herbal remedies
  • have any liver problems.
  • have any other medical conditions
  • are pregnant, plan to become pregnant, or think you might be pregnant. Your doctor will discuss whether fluconazole is right for you.
  • are breast-feeding. Fluconazole can pass through breast milk to the baby.
  • are allergic to any other medicines including those used to treat yeast and other fungal infections.
  • are allergic to any of the ingredients in fluconazole. If you need to know the inactive ingredients, ask your doctor or pharmacist.

Who Should Not Take Fluconazole?

To avoid a possible serious reaction, do NOT take fluconazole if you are taking cisapride (Propulsid®)* since it can cause changes in heartbeat in some people if taken with fluconazole.

How Should I Take Fluconazole?

Take fluconazole by mouth with or without food. You can take fluconazole any time of the day.

Fluconazole keeps working for several days to treat the infection. Generally the symptoms start to go away after 24 hours. However, it may take several days for your symptoms to go away completely. If there is no change in your symptom after a few days, call your doctor.

Just swallow 1 fluconazole tablet to treat your vaginal yeast infection.

What Should I Avoid While Taking Fluconazole?

Some medicines can affect how well fluconazole works. Check with your doctor before starting any new medicines within seven days of taking fluconazole.

What Are The Possible Side Effects of Fluconazole?

Like all medicines, fluconazole may cause some side effects that are usually mild to moderate.

The most common side effects of fluconazole are:

  • headache
  • diarrhea
  • nausea or upset stomach
  • dizziness
  • stomach pain
  • changes in the way food tastes

Allergic reactions to fluconazole are rare, but they can be very serious if not treated right away by a doctor. If you cannot reach your doctor, go to the nearest hospital emergency room. Signs of an allergic reaction can include shortness of breath; coughing; wheezing; fever; chills; throbbing of the heart or ears; swelling of the eyelids, face, mouth, neck, or any other part of the body; or skin rash, hives, bulers or skin peeling.

Fluconazole has been linked to rare cases of serious liver damage, including deaths, mostly in patients with serious medical problems. Call your doctor if your skin or eyes become yellow, your urine turns a darker color, your stools (bowel movements) are light-colored, or if you vomit or feel like vomiting or if you have severe skin itching.

In patients with serious conditions such as AIDS or cancer, rare cases of severe rashes with skin peeling have been reported. Tell your doctor right away if you get a rash while taking fluconazole.

Fluconazole may cause other less common side effects besides those uled here. If you develop any side effects that concern you, call your doctor. For a ul of all side effects, ask your doctor or pharmacist.

What To Do For An Overdose

In case of an accidental overdose, call your doctor right away or go to the nearest emergency room.

How To Store Fluconazole

Keep fluconazole and all medicines out of the reach of children.

General Advice About Prescription Medicines

Medicines are sometimes prescribed for conditions that are not mentioned in patient information leaflets. Do not use fluconazole for a condition for which it was not prescribed. Do not give fluconazole to other people, even if they have the same symptoms you have. It may harm them.

This leaflet summarizes the most important information about fluconazole. If you would like more information, talk with your doctor. You can ask your pharmacist or doctor for information about fluconazole that is written for health professionals.

* Propulsid (cisapride) is a registered trademark of Janssen Pharmaceutica.

Manufactured for: 0172

Ivax Pharmaceuticals, Inc. 06/05

Miami, FL 33137 B3

by: Cipla Ltd.

Kurkumbh, India

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