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PubMed2000

Comparison of oral fluconazole and itraconazole for progressive, nonmeningeal coccidioidomycosis. A randomized, double-blind trial. Mycoses Study Group.

BACKGROUND: In previous open-label noncomparative clinical trials, both fluconazole and itraconazole were effective therapy for progressive forms of coccidioidomycosis. OBJECTIVE: To determine whether fluconazole or itraconazole is superior for treatment of nonmeningeal progressive coccidioidal infections. DESIGN: Randomized, double-blind, placebo-controlled trial. SETTING: 7 treatment centers in California, Arizona, and Texas. PATIENTS: 198 patients with chronic pulmonary, soft tissue, or skeletal coccidioidal infections. INTERVENTION: Oral fluconazole, 400 mg/d, or itraconazole, 200 mg twice daily. MEASUREMENTS: After 4, 8, and 12 months, a predefined scoring system was used to assess severity of infection. Findings were compared with those at baseline. RESULTS: Overall, 50% of patients (47 of 94) and 63% of patients (61 of 97) responded to 8 months of treatment with fluconazole and itraconazole, respectively (difference, 13 percentage points [95% CI, -2 to 28 percentage points]; P = 0.08). Patients with skeletal infections responded twice as frequently to itraconazole as to fluconazole. By 12 months, 57% of patients had responded to fluconazole and 72% had responded to itraconazole (difference, 15 percentage points [CI, 0.003 to 30 percentage points]; P = 0.05). Soft tissue disease was associated with increased likelihood of response, as in previous studies. Azole drug was detected in serum specimens from all but 3 patients; however, drug concentrations were not helpful in predicting outcome. Relapse rates after discontinuation of therapy did not differ significantly between groups (28% after fluconazole treatment and 18% after itraconazole treatment). Both drugs were well tolerated. CONCLUSIONS: Neither fluconazole nor itraconazole showed statistically superior efficacy in nonmeningeal coccidioidomycosis, although there is a trend toward slightly greater efficacy with itraconazole at the doses studied.

Administration, Oral↗
PubMed1999

The effect of fluconazole on cyclophosphamide metabolism in children.

Fluconazole is increasingly used in children receiving chemotherapy. Many of these patients are being treated with cyclophosphamide, which must undergo hepatic metabolism to produce active alkylating species. As a consequence of the cytochrome P-450 inhibitory properties of fluconazole, a potential interaction exists between these two agents that could influence the therapeutic effect of cyclophosphamide. To investigate this interaction, a retrospective case series of patients was chosen from a population of children with a previously established profile of cyclophosphamide metabolism. Twenty-two children who were not receiving other therapy known to influence drug metabolism were selected and analyzed in terms of fluconazole treatment; of these, nine were receiving fluconazole and thirteen were identified as controls. Study design was not randomized. The plasma clearance of cyclophosphamide was lower in patients receiving fluconazole [mean(SD) 2.4(0.71) versus 4.2(1.2) l/h/m2, p =.001]. In vitro studies were performed to characterize the interaction between fluconazole and cyclophosphamide in six human liver microsomes. The concentration of fluconazole required to reduce the production of 4-hydroxycyclophosphamide to 50% of control values (IC50) varied between 9 and 80 microM (median 38 microM). Further studies of the effect of fluconazole on 4-hydroxycyclophosphamide production in vivo are warranted to determine whether this interaction reduces the therapeutic effect of cyclophosphamide in clinical practice.

Adolescent↗
PubMed2000

Treatment of candidal infections with fluconazole in neonates and infants.

UNLABELLED: To study the therapy, efficacy and safety of fluconazole in candidal mycoses during neonatal phase and infancy a case review in 53 newborns and infants was performed. The majority of these patients were premature with a median birth weight of 1120 g and born within gestational week 23-38. The median age at the onset of fluconazole treatment was 5 weeks. All patients had underlying diseases and several risk factors, which favored the occurence of a systemic candidal mycosis. Systemic candidiasis was the most frequent diagnosis (75.5%). Fluconazole was administered at a daily dosage of 5-6 mg/kg for a median duration of 21 days. The hepatic, renal and hematologic functions were assessed before, one, two, and three weeks after start of treatment. Yeasts were identified in 37 patients. The most common fungus isolated at baseline was Candida albicans (68%). Clinical cure or improvement was reported in 31 out of 38 patients (81.6%). Mycological cure was achieved in 25 out of 32 newborns and infants. Despite the limited number of patients with outcome data, these preliminary results of a small cohort clearly indicate the effective antifungal therapy with fluconazole in neonates and infants. No serious side effects were observed in fluconazole-treated patients. Two patients with megaureter-megacystis-hydronephrosis syndrome and severe meningoencephalitis showed a mild increase in liver enzymes. - CONCLUSION: Fluconazole seems to be an effective therapy for systemic and other forms of candidiasis in infants including very low birth weight infants (VLBWI; <1500 g). These favorable safety and efficacy data are similar to results obtained with fluconazole in older children and adults. These findings, however, must be supported by larger trials. The recommended daily dose is 5 mg/kg body weight. Only in VLBWI the dosage interval within the first two weeks of life should be prolonged up to 3 days and fluconazole serum levels should be monitored.

Antifungal Agents↗
PubMed2000

Prolonged fluconazole prophylaxis is associated with persistent protection against candidiasis-related death in allogeneic marrow transplant recipients: long-term follow-up of a randomized, placebo-controlled trial.

Two randomized, placebo-controlled trials previously showed that fluconazole (400 mg/d) administered prophylactically decreases the incidence of candidiasis in blood and marrow transplant (BMT) recipients. However, there exists conflicting data regarding the optimal duration of fluconazole administration, specifically whether prophylaxis through acute graft-versus-host disease (GVHD) results in improved survival in allograft recipients. Reported here are the results of long-term follow-up and a detailed analysis of invasive candidiasis and candidiasis-related death in 300 patients who received fluconazole (400 mg/d) or placebo for 75 days after BMT at the Fred Hutchinson Cancer Research Center. Patients in both treatment arms were compared for survival, causes of death, and the incidence of invasive fungal infections early (less than 110 days) and late (more than 110 days) after BMT. After 8 years of follow-up, survival is significantly better in fluconazole recipients compared with placebo recipients (68 of 152 vs 41 of 148, P =.0001). The overall incidence of invasive candidiasis was increased in patients who received placebo compared with fluconazole (30 of 148 vs 4 of 152, P <.001). More patients who received placebo died with candidiasis early (13 of 148 vs 1 of 152, P =.001) and late (8 of 96 vs 1 of 121, P =.0068) after BMT. The incidence of severe GVHD involving the gut was higher in patients who did not receive fluconazole (20 of 143 vs 8 of 145, P =.02), and fewer patients who received fluconazole died with this complication. Thus, administration of fluconazole (400 mg/d) for 75 days after BMT appears to be associated with decreased gut GVHD, a persistent protection against disseminated candidal infections and candidiasis-related death, resulting in an overall survival benefit in allogeneic BMT recipients.

Adult↗
PubMedDate not supplied

[The value of the agar dilution method as a screening test for determining the sensitivity of Candida albicans to fluconazole].

The aim of this study was to evaluate the performance of agar dilution method in the determination of fluconazole susceptibility of Candida albicans strains, by using different culture media. Hundred and seven C. albicans strains which were isolated from different clinical specimens were included to this study and fluconazole susceptibilities were determined by both of the microdilution method according to NCCLS M-27A standards, and an agar dilution based method by using CHROMagar Candida and Biggy agar. For this purpose, CHROMagar Candida and Biggy agar plates containing 0 (as control plate), 8 and 16 micrograms fluconazole per mililiter were prepared and inoculated with standard amounts of 24 hours culture suspansions of C. albicans strains. The culture media were evaluated after incubation at 30 degrees C for 48 hours, and the growth of strains in the fluconazole-containing and fluconazole-free plates were compared. C. albicans strains were accepted susceptible if there were no growth or the colonies were smaller than control media, and resistant if the colonies were the same size as in the control media. As a result, 106 (99.1%) of the strains were found susceptible and one (0.9%) was found dose-dependent susceptible to fluconazole by microdilution method, whereas none of the isolates grew on 8 and 16 micrograms/ml fluconazole containing CHROMagar Candida and Biggy agar media. Therefore, the agar dilution test results of 106 strains (99.1%) were in agreement with the reference microdilution method. In conclusion, it was thought that agar dilution screening tests using two different culture media, were rapid and practical for routine use in the determination of fluconazole susceptibilities of C. albicans strains.

Antifungal Agents↗
PubMed2003

[In vitro activity of fluconazole, voriconazole and posaconazole against Candida spp].

Voriconazole and posaconazole are two new triazoles with broad-spectrum antifungal activity. The in vitro activity of these agents was compared with that of fluconazole against 113 clinical isolates of Candida spp. exhibiting a wide range of MICs for fluconazole (< or =0.125 to >64 mg/l). They included 22 C. albicans isolates, 22 C. glabrata, 20 C. tropicalis, 15 C. dubliniensis, 13 C. parapsilosis, 13 C. krusei, 4 C. lusitaniae, 3 C. guilliermondii and 1 C. famata. MICs were determined by broth microdilution test performed according to the National Committee for Clinical Laboratory Standards' M27-A document. Voriconazole and posaconazole were quite active against all Candida spp. isolates, with MIC(90) of 0.25 and 0.5 mg/l, respectively. Fluconazole MIC(50) and MIC(90) were 1 and 32 mg/l. Voriconazole and posaconazole showed in vitro activity against fluconazole-susceptible and -resistant Candida isolates. Higher voriconazole and posaconazole MICs were observed in isolates exhibiting higher fluconazole MICs (>/=16 mg/l) than in those of fluconazole-susceptible isolates (MIC(90) for voriconazole and posaconazole in the fluconazole-resistant isolates were 0.5 mg/l versus 0.06 mg/l for voriconazole and 0.25 mg/l for posaconazole in the fluconazole-susceptible strains). C. dubliniensis was the most susceptible species, and voriconazole the most active antifungal agent against all Candida spp. tested.

Antifungal Agents↗
PubMed2003

[Fluconazole resistance in Candida albicans assayed by PCR fingerprinting with M13 prime].

OBJECTIVE: To understand the molecular and genetic mechanism underlying fluconazole resistance in Candida albicans by PCR fingerprinting with M13 primer. METHODS: Paper disc diffusion method was employed for assay of fluconazole resistance in 41 clinical isolates of Candida albicans, followed by PCR fingerprinting with M13 primer to study the gel patterns with cluster analysis using neighbor joining (NJ) method performed with RAPD200 software. RESULTS: Of the 41 clinical isolates, 11 strains (26.8%) were fluconazole-sensitive, 8 (19.5%) fluconazole-dependent and 22 (53.7%) fluconazole-resistance. Two to twelve bands could be observed among these strains, and the gel patterns revealed by cluster analysis were associated with the reactions of the strains against fluconazole and the location of infection. CONCLUSION: There is high prevalence of fluconazole resistance in clinical Candida albicans isolates, and PCR fingerprinting with M13 primer is convenient for assay of fluconazole resistance and molecular epidemiological study of Candida albicans.

Antifungal Agents↗
PubMed1994

[Fluconazole sensitivity of Candida strains in vitro in the microdilution test and agar diffusion test].

The comparison of the in vitro-susceptibility of Candida isolates collected from the oral cavity of different groups of patients to fluconazole ist reported. The isolates of HIV-patients treated with fluconazole, HIV-patients and dermatological patients without fluconazole exposure were investigated. The in vitro-susceptibility of these isolates was determined by microdilution test and agar diffusion test. 88.7% of the 194 Candida isolates were susceptible in vitro, 6.7% less sensitive and 4.6% resistant to fluconazole. Comparing the susceptibility within the groups there was a higher number of isolates less sensitive (14.7%) and resistant (11.8%) to fluconazole in the group of HIV-patients treated with fluconazole than in the other 2 groups without treatment. The less sensitive isolates were 4 C. albicans and 6 C. glabrata. The resistant isolates were 2 C. albicans, 2 C. glabrata and 4 C. krusei. In the group of HIV-patients without fluconazole exposure there were only 2.7% of the isolates less sensitive (2 C. glabrata) and 1.4% resistant to fluconazole (1 C. glabrata). In dermatological patients there were 2% of the isolates less sensitive (2 C. glabrata) and no resistant isolate. Resistance both in vivo and in vitro was found in 2 patients.

AIDS-Related Opportunistic Infections↗
PubMed1993

Histoplasmosis in the acquired immunodeficiency syndrome (AIDS): treatment with itraconazole and fluconazole.

The manifestations of histoplasmosis in 20 patients with the acquired immunodeficiency syndrome are presented. In this series, patients were treated with either itraconazole or fluconazole. Twelve patients received treatment with itraconazole at 400 mg/day, including two patients who had not responded to treatment with fluconazole at 100 mg/day. Of the responses, seven were classified as remissions (mean treatment duration of 24 months), two as improvements, and three as failures. Ten patients received fluconazole. Of the responses, three were classified as remissions (mean treatment duration of 12 months), one as improvement, and six as failures. Of the 10 patients treated with fluconazole, five received doses of 100 mg/day, and five were given doses of 400 or 800 mg/day. The differences in outcome among the five patients receiving the lower dose of fluconazole (one remission, one improvement, and three failures) and the five patients given the higher doses of fluconazole (two remissions and three failures) were negligible. One other patient showed signs of histoplasmosis while receiving fluconazole at 50 mg/day for treatment of thrush. Three failures (two treated with itraconazole and one with fluconazole) followed lapses in azole therapy because of associated conditions. Azole therapy was well tolerated. The treatment responses in this pilot series appear promising in comparison with those reported in the literature with amphotericin B or ketoconazole.

Acquired Immunodeficiency Syndrome↗
PubMed1993

Low-dose fluconazole therapy potentiates the hypoprothrombinemic response of warfarin sodium.

BACKGROUND: Fluconazole has been reported to interact with many medications. This study examined the effect of low-dose fluconazole therapy on the hypoprothrombinemic response of warfarin sodium in patients. METHODS: Patients receiving low-intensity anticoagulation therapy with warfarin were recruited. All patients were taking stable doses of warfarin and had two baseline prothrombin times (PTs) within 10% of each other. Each patient received 100 mg of fluconazole daily for 7 days. Prothrombin times were measured on days 2, 5, and 8 during fluconazole administration. RESULTS: All patients had a progressive increase in PTs. Mean (+/- SD) of PTs increased from 15.8 +/- 1 seconds before the administration of fluconazole to 18.9 +/- 1.9 seconds on day 5 and 21.9 +/- 2.2 seconds on day 8. Fluconazole therapy was stopped early in the three patients due to high PTs. The largest change in PT was 9.7 seconds. No bleeding was noted during the study. CONCLUSION: Fluconazole predictably potentiates the hypoprothrombinemic response of warfarin. Prothrombin times must be monitored when fluconazole is administered to patients taking warfarin.

Aged↗
PubMed1997

Fluconazole as prophylaxis against fungal infection in patients with advanced HIV infection.

BACKGROUND: There is limited information regarding the usefulness of primary antifungal prophylaxis in patients with advanced human immunodeficiency virus (HIV) disease. OBJECTIVE: To evaluate the efficacy and safety of oral fluconazole treatment for the prevention of systemic fungal diseases related to the acquired immunodeficiency syndrome. METHODS: We evaluated the clinical records of more than 1300 HIV-infected patients followed up for 6 years to identify subjects with a CD4+ lymphocyte count less than 0.20 x 10(9)/L (200/microL) and no prior systemic fungal disease. We compared 128 patients who received oral fluconazole (100 mg/d every third week) with 121 subjects who received no antifungal treatment. MAIN OUTCOME MEASURES: The occurrence of visceral mycoses or death was considered an end point. The frequency of esophageal candidiasis and extrapulmonary cryptococcosis and their related clinical and laboratory features, as well as overall patient survival, were assessed and compared between the 2 study groups. RESULTS: Subjects not treated with fluconazole experienced a significantly higher incidence of systemic mycoses than patients who received fluconazole: 28.4 vs 8.8 cases per 100 patient-years (P < .001). Fluconazole treatment was more effective in preventing esophageal candidiasis than cryptococcosis and was more effective in subjects with a CD4+ cell count less than 0.10 x 10(9)/L. Moreover, fungal complications occurred later and were associated with a significantly lower CD4+ cell count among treated vs untreated patients, while the duration of antiretroviral therapy did not play a significant role. Although mortality rates were similar in the 2 study groups, the fatal outcome of disease was less frequently caused by a fungal disease in subjects who underwent fluconazole prophylaxis. Fluconazole had a favorable tolerability profile. CONCLUSIONS: In our experience, primary fluconazole prophylaxis proved safe and effective in the prevention of systemic candidiasis and cryptococcosis in patients with advanced HIV disease but it did not improve overall survival. Prospective controlled trials are advisable to confirm efficacy, to find the drug of choice and its best dosage and schedule of administration, to identify patient subgroups showing the most favorable cost-benefit ratios, and to evaluate the effects on overall life expectancy and the risk of emergence and spread of antifungal drug resistance.

AIDS-Related Opportunistic Infections↗
PubMed1997

[Current treatment of candidemia in non-neutropenic patients. Amphotericin B or fluconazole? A retrospective study of 62 consecutive patients].

BACKGROUND: To analyze the epidemiologic characteristics of non-neutropenic patients with candidemia in a general hospital and the advantages and disadvantages of treatment with amphotericin B or fluconazole. PATIENTS AND METHODS: A total of 62 adult non-neutropenic patients with candidemia and treated with amphotericin B (n = 35) or fluconazole (n = 27) were studied. All episodes were considered to be associated with infection in a vein catheter. The demographic characteristics, risk factors for the development of candidemia, Candida species recovered from blood culture, underlying diseases, and clinical manifestations in both groups were compared. The evolution regarding secondary effects developed with both drugs, therapy failures, long term complications, and overall mortality rate associated with candidemia were analyzed. RESULTS: Both groups were comparable with the exception of the percentage of patients infected with species different from Candida albicans, which was higher in the group of patients who received amphotericin B (57%) than in the fluconazole group (26%) (p = 0.02), and in that patients with severe renal failure or AIDS had received preferentially fluconazole. There were no statistically significant differences regarding the evolution of patients treated with amphotericin B or fluconazole with the following factors: therapy failure (27% versus 19%; p = 0.7), overall mortality rate (40% versus 44%; p = 0.6), and mortality directly related to candidemia (33% versus 30%). Mortality was significantly higher among patients who had not their vein catheters removed early (78%) compared with those who had their vein catheters removed early (34%) (p = 0.01). Sixty-six percent of patients treated with amphotericin developed some severe secondary effect, whereas no patient in the fluconazole group developed such effects. CONCLUSIONS: Both amphotericin B and fluconazole seem to be effective drugs for the treatment of vein catheter related candidemia in the non-neutropenic patient, although fluconazole is far less toxic. The early removal of the vein catheter plays a prognostic role with at least the same relevance than the type of antifungal therapy chosen.

Adult↗
PubMed1998

Analysis of fluconazole effect on Candida albicans viability during extended incubations.

Fluconazole is an azole agent with primarily fungistatic activity in standard in vitro susceptibility tests. However, recent work has demonstrated that this drug can reduce Candida albicans viability during prolonged incubations under non-growing conditions. The present study was undertaken to examine more closely some of the parameters of this killing activity. Fungicidal effects of 1.0 microg ml-1 of fluconazole were found during 7-14-day exposures in each of two media that prevented proliferation, distilled water and metal-depleted RPMI 1640 tissue-culture medium. Fluconazole appeared to be stable after being incubated at 37 degreesC for either 7 or 14 days. Strains of C. albicans resistant to fluconazole in standard short-term growth-inhibition assays were also found to be resistant to fluconazole's effect on viability in prolonged culture, suggesting similar mechanisms of action for these effects. C. albicans yeast cells pre-incubated for 7 days in distilled water were not more sensitive to the drug in short-term susceptibility assays. Although all proliferation of the organisms in distilled water cultures appeared to cease after 3 days, fluconazole added at 7 days still reduced C. albicans viability. Therefore, the drug appeared to kill the non-proliferating organisms directly rather than preventing growth and thereby the emergence of younger organisms that would live longer. Transmission electron microscopy demonstrated damage to the cell wall-cell membrane complex and interior contents of yeast cells incubated in distilled water alone; fluconazole appeared to increase the percentages of cells so affected. In summary, extended-incubation susceptibility tests demonstrated that fluconazole has direct fungicidal activity of non-proliferating C. albicans yeast cells. These results may be relevant to the manner in which this drug promotes clearance of chronic fungal infections.

Antifungal Agents↗
PubMedDate not supplied

Fluconazole therapy in coccidioidal meningitis maintained with intrathecal amphotericin B.

BACKGROUND: Meningitis follows approximately 0.15% to 0.75% of cases of extrapulmonary coccidioidomycosis. Successful treatment of coccidioidal meningitis (CM) has generally required intrathecal therapy with amphotericin B, which often causes significant toxic effects and discomfort to the patient. Prior to fluconazole, azoles had not been efficacious in CM either because of toxicity at elevated doses or because of poor cerebrospinal fluid distribution. Fluconazole however, has been found to have both good cerebrospinal fluid penetration and a favorable side effect profile. METHODS: We studied 11 patients with CM who were maintained with amphotericin B and were then switched to oral fluconazole therapy alone at a dosage of 400 mg/d for a period of up to 19 months. The patients were evaluated clinically for evidence of deterioration measured by need for hospitalization, development of extrameningeal disease during the study period, need to reinstitute intrathecal amphotericin B therapy because of worsening disease, cerebrospinal fluid leukocyte count, protein level, and serologic tests for complement-fixing antibody. RESULTS: Three patients required hospitalization during the study, two patients for reasons unrelated to CM. No patient developed extrameningeal disease or required discontinuation of fluconazole therapy because of deteriorating disease. Patients at exit reported no symptoms related to meningitis or adverse effects related to fluconazole therapy. There was no deterioration in general health or neurologic status. CONCLUSIONS: Our study demonstrates that conversion from amphotericin B to fluconazole was associated with a stable disease course of CM for up to 19 months. Further studies delineating both optimal dosage and characteristics of patients likely to respond to fluconazole therapy alone are needed.

Administration, Oral↗
PubMed1997

The effect of empiric and prophylactic treatment with fluconazole on yeast isolates in a surgical trauma intensive care unit.

OBJECTIVE: To assess the effect of aggressive antifungal prophylaxis and empiric antifungal therapy using fluconazole on the mycotic microbiology and associated infectious complications in a surgical intensive care unit. DESIGN: Retrospective review of a cohort of critically ill surgical patients treated during an 11-month period. SETTING: Surgical intensive care unit, university hospital, state-designated level I trauma center. PATIENTS: All patients treated with fluconazole during the study. MAIN OUTCOME MEASURES: Positive fungal cultures obtained after commencement of antifungal prophylaxis or antifungal treatment with fluconazole. Overall and infectious mortality rates for patients with positive cultures were also measured. RESULTS: Of 72 surgical patients who were treated with fluconazole; 16 (22%) had secondary mycoses. Fourteen (88%) of these patients were receiving fluconazole as antifungal prophylaxis or as empiric treatment of suspected but unproved infection. The predominant organisms isolated from these 16 patients were Candida glabrata (41%) and Candida parapsilosis (41%). Overall mortality for this group was 44%, and infectious mortality was 38%. The infectious mortality rate was significantly higher than the rate found in patients who were successfully treated with fluconazole for primary mycoses, and who did not have secondary infections with resistant organisms (mortality, 9%; P < .01, chi 2). CONCLUSIONS: Emergence of resistant species after treatment with fluconazole does occur in surgical patients, and suggests that the development of a secondary fungal infection with a resistant organism may be associated with a poor prognosis.

Antifungal Agents↗
PubMed2002

Absence of clinically relevant drug interactions following simultaneous administration of didanosine-encapsulated, enteric-coated bead formulation with either itraconazole or fluconazole.

This open-label, two-way crossover study was undertaken to determine whether the enteric formulation of didanosine influences the pharmacokinetics of itraconazole or fluconazole, two agents frequently used to treat fungal infections that occur with HIV infection, and whose bioavailability may be influenced by changes in gastric pH. Healthy subjects were randomized to Treatment A (200-mg itraconazole or 200-mg fluconazole) or Treatment B (same dose of itraconazole or fluconazole with 400 mg of didanosine as an encapsulated, enteric-coated bead formulation). In the itraconazole study, a lack of interaction was concluded if the 90% confidence interval (CI) of the ratio of the geometric means of log-transformed C(max) and AUC(0-T) values of itraconazole and hydroxyitraconazole, the active metabolite of itraconazole, were contained entirely between 0.75 and 1.33. In the fluconazole study, the equivalence interval for C(max) and AUC(0-T) was 0.80-1.25. The data showed that for itraconazole the point estimate and 90% CI of the ratios of C(max) and AUC(0-T) values were 0.98 (0.79, 1.20) and 0.88 (0.71, 1.09), respectively; for hydroxyitraconazole the respective values were 0.91 (0.76, 1.08) and 0.85 (0.68, 1.06). In the fluconazole study, the point estimate and 90% CI of the ratios of C(max) and AUC(0-T) values were 0.98 (0.93, 1.03) and 1.01 (0.99, 1.03), respectively. The T(max) for itraconazole, hydroxyitraconazole, and fluconazole were similar between treatments. Both studies indicated a lack of clinically significant interactions of the didanosine formulation with itraconazole or fluconazole. These results showed that the encapsulated, enteric-coated bead formulation of didanosine can be concomitantly administered with drugs, such as the azole antifungal agents, whose bioavailability may be influenced by interaction with antacids.

Adolescent↗
PubMed2005

Prenatal exposure to fluconazole: an identifiable dysmorphic phenotype.

BACKGROUND: Fluconazole is a triazole antifungal used to treat mycotic infections. Fluconazole is reported to act as a teratogen when used continuously at a dosage of 400-800 mg daily. Fluconazole embryopathy was previously reported in 4 cases. The common features that were also seen in the current case include multiple synostosis (including craniosynostosis and digital synostosis), congenital heart defects, skeletal anomalies, and recognizable dysmorphic facial features. CASE: We report the case of a 9-month-old male born to a 30-year-old woman following a 37-week pregnancy. The pregnancy was complicated by maternal human immunodeficiency virus (HIV) infection and multiple drug exposures, including fluconazole (400 mg/day) until the fifth month and then from 6 months to term, efavirenz, nevirapine, methadone, dapsone, pentamidine, and trimethoprim-sulfamethoxazole. At birth the infant had seizures related to neonatal abstinence syndrome and was noted to have multiple congenital anomalies. On examination at age 9 months, he had craniosynostosis secondary to coronal and lambdoidal suture closures, shallow orbital region, hypoplastic supraorbital ridges, hypertelorism, and mild ptosis. He had radioulnar synostosis and metacarpophalangeal-proximal interphalangeal symphalangism of D2-D5 bilaterally. CONCLUSIONS: The findings of cranial synostosis, multiple symphalangism, and long-bone abnormalities in our case are typical of other reported cases of fluconazole embryopathy. Our patient showed no evidence of embryopathy due to efavirenz, and he did not have the features of Antley-Bixler or other craniosynostosis syndromes. We review the literature regarding the teratogenic effects of prenatal exposure to fluconazole and provide additional evidence that prenatal fluconazole exposure has a clearly identifiable phenotype.

Abnormalities, Drug-Induced↗
PubMed1996

Correlation between in vitro resistance to fluconazole and clinical outcome of oropharyngeal candidiasis in HIV-infected patients.

Fifty episodes of oropharyngeal candidiasis in HIV-infected patients were analyzed prospectively in order to evaluate the clinical response to fluconazole. The minimum inhibitory concentrations (MICs) of fluconazole for the Candida strains isolated from the pharynx were correlated with the clinical response. Treatment with fluconazole (100 mg/day) was successful in 86% of the cases. A good clinical outcome followed in 97% of the cases when a strain sensitive to fluconazole was isolated. This figure fell to 22% when the strain was resistant to fluconazole (p < 0.001). The rate of post-treatment colonization was high (87%), and selection of non-albicans Candida species occurred in 23% of the cases. In conclusion, fluconazole treatment for oropharyngeal candidiasis of HIV-infected patients was useful in most cases, but less sensitive non-albicans species can be selected. Most treatment failures were associated with increased MICs of fluconazole for the strains isolated before treatment; therefore, susceptibility testing is recommended as an aid in clinical decision-making for the use of the azole group of drugs.

Antifungal Agents↗