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DIFLUCAN

(generic name: fluconazole)
Reviews

Diflucan

Bone Marrow Transplant. 2005 Mar;35(6):583-6.
Caspofungin as second-line therapy for fever of unknown origin or invasive fungal infection following allogeneic stem cell transplantation.
Trenschel R, Ditschkowski M, Elmaagacli AH, Koldehoff M, Ottinger H, Steckel N, Hlinka M, Peceny R, Rath PM, Dermoumi H, Beelen DW.
1Department of Bone Marrow Transplantation, University Hospital Essen, Essen, Germany.

Summary:Caspofungin (CAS) is the first of a new class of antifungal agents, the echinocandins, that interfere with fungal cell wall synthesis by inhibition of glucan synthesis. Here, we report the results of 31 patients treated with CAS following allogeneic SCT. CAS was administered as a second-line agent to patients with invasive fungal infection (IFI) (n=15) or fever of unknown origin (n=16) who were recalcitrant to or intolerant of prior antifungal therapy. Unsuccessful first-line regimes included amphotericin B (n=17), liposomal amphotericin B (n=5), fluconazole (n=3), itraconazole (n=1), and voriconazole (n=2). All patients received concomitant immunosuppressive therapy for graft-versus-host disease. In 23 patients, cyclosporin A (CSA) and CAS were administered concurrently without any major side effects detected. Observed increases in GPT were not clinically significant. Normalization of serum creatinine and significant reductions in C-reactive protein were observed in response to CAS. Favorable outcome to CAS were documented in eight of 15 patients with IFI and in 15 of 16 patients with fever of unknown origin. CAS is a promising alternative in patients with IFI and fever of unknown origin in the setting of allogeneic SCT.Bone Marrow Transplantation (2005) 35, 583-586. doi:10.1038/sj.bmt.1704859 Published online 31 January 2005.
Mycoses. 2005 Mar;48(2):126-31.
Molecular epidemiology of Candida species isolated from urine at an intensive care unit.
Ergon MC, Gulay Z.
Department of Microbiology and Clinical Microbiology, School of Medicine, Dokuz Eylul University, Izmir, Turkey.

Summary Candida spp. has been the leading microorganism isolated from the urine specimens of patients hospitalized at the Anesthesiology and Reanimation intensive care unit (ICU) of Dokuz Eylul University Hospital, Izmir, since 1998. This study was undertaken to investigate the clonal relationship of Candida urine isolates in order to find the mode of spread among the patients. Epidemiological surveillance of 38 Candida albicans, 15 Candida tropicalis and 12 Candida glabrata recovered from the urine specimens of patients who were hospitalized in the ICU between June 11, 2000 and October 15, 2001 was carried out by antifungal susceptibility testing and randomly amplified polymorphic DNA (RAPD) analysis. Two short primers [Cnd3 (5'-CCAGATGCAC-3') and Cnd4 (5'-ACGGTACACT-3')] were used for RAPD. None of the isolates had high minimal inhibitory concentration (MIC) values (>1 mug ml(-1)) against amphotericin B with MIC(50)values of 0.5 mug ml(-1), 0.5 mug ml(-1) and 0.125 mug ml(-1) for C. albicans, C. tropicalis and C. glabrata isolates, respectively. However, three C. glabrata isolates were resistant and one C. albicans and five C. glabrata isolates were dose-dependent susceptible (D-DS) to fluconazole. Among C. albicans isolates 19 and 20 patterns were detected with primers Cnd3 and Cnd4, respectively. When primers Cnd3 and Cnd4 were evaluated together, three and four genotypes were identified for C. tropicalis and C. glabrata isolates, respectively. Our results suggest that the source of C. albicans isolates was mostly endogenous. It is difficult to interpret the mode of spread of C. tropicalis and C. glabrata urine isolates as we obtained insufficient banding patterns for these species.

Br J Clin Pharmacol. 2005 Feb;59(2):160-6.
The effects of hepatic impairment on the pharmacokinetics of fosfluconazole and fluconazole following a single intravenous bolus injection of fosfluconazole.
Sobue S, Tan K, Haug-Pihale G.
Clinical Pharmacology, Pfizer Global R&D, Tokyo Laboratories, Pfizer Japan Inc., Tokyo, Japan. satoshi.sobue@japan.pfizer.com.

AIMS: Fosfluconazole is a phosphate pro-drug of fluconazole (FLCZ). This study was conducted to determine the pharmacokinetics of fosfluconazole and FLCZ following a single intravenous injection of fosfluconazole in subjects with hepatic impairment and to compare them with healthy subjects. METHODS: Twenty-four subjects (12 with normal hepatic function and 12 with chronic stable mild to moderate impaired hepatic function) received a single 1000-mg bolus intravenous injection of fosfluconazole. Concentrations of fosfluconazole and FLCZ were determined in plasma and urine samples taken up to 192 h and 48 h postdose, respectively. RESULTS: The total clearance of fosfluconazole was higher and the t(1/2,Z) and mean residence time were shorter in hepatically impaired subjects than in normal subjects. This may reflect more rapid conversion to FLCZ. The degree of protein binding of fosfluconazole (> 90%) and the amount of fosfluconazole excreted in the urine were similar in both groups. Slightly higher mean plasma concentrations of FLCZ were observed in the impaired group than in the normal group; however, hepatic impairment had no statistically significant effect on the FLCZ pharmacokinetic parameters apart from t(max). The t(max) values were 4.8 h and 3.1 h in the normal and impaired subjects, respectively. The shorter t(max) for FLCZ is also consistent with the more rapid conversion in the impaired subjects. The ratios (95% confidence intervals) for C(max) and AUC of FLCZ (impaired/normal) were 106.0% (92.8, 121.2) and 115.6% (86.4, 154.7), respectively. There were no serious adverse events, and no discontinuations due to adverse events or laboratory test abnormalities. The adverse events reported were mostly mild in severity and no trend could be discerned between the groups. CONCLUSIONS: Fosfluconazole was more rapidly converted to FLCZ in the hepatically impaired subjects but the FLCZ pharmacokinetic parameters (except t(max)) were not statistically significantly affected by hepatic impairment. Fosfluconazole was well tolerated by both groups. These results suggest that there is no requirement to adjust the dose of fosfluconazole when administered to subjects with mild to moderate hepatic impairment.

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Drug information

GENERIC NAME: fluconazole
BRAND NAME: Diflucan


DRUG CLASS AND MECHANISM: Antifungal (treatment of certain fungus infections).

PREPARATIONS: Suspension content per bottle is 350mg (when diluted 10mg per ml) and 1400mg (when diluted 40mg per ml). Tablets are available in 50mg, 100mg, and 200mg from Roerig Labs. Intravenous solutions are available.

STORAGE: Store tablets in a dry place at 20-25 degrees C (68-77 F), oral suspensions after dilution at 5-30 degrees C (41-86 F) the oral suspension should be discarded in 2 weeks after reconstituted.

PRESCRIBED FOR: Oral, esophageal, urinary, vaginal and possibly other organ infections caused by the fungus Candida. Fluconazole has also been used in the fungal infection Cryptococcus.

DOSING: Fluconazole is taken orally or by intravenous injection. Modified dosing is needed if the patient has impaired renal function or if taking certain other medications at the same time. Please consult your pharmacist or physician if taking other medications with fluconazole. This drug can be used in children and has been effective down to the age of 6 months of age. Fluconazole can cause liver damage in rare cases and the liver should be monitored if taken for several days.

DRUG INTERACTIONS: Caution if taking certain other medications with fluconazole such as phenytoin, cyclosporin, theophylline and coumadin. If a rash occurs while taking this medication notify your doctor.

PREGNANCY: Use of fluconazole in pregnancy is not usually recommended.

NURSING MOTHERS: Use of fluconazole in nursing mothers is not usually recommended.

SIDE EFFECTS: The incidence of side effects from this medication is relatively high (up to 25%) Many (13%) may get headaches. Some patients develop nausea, abdominal pain, diarrhea or dizziness. Severe skin rash may occur but is uncommon.

Caution! Before starting to take this medicine, it is vital that you should consult your doctor! Do not use it on your own initiative, without medical advice.

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DIFLUCAN
Substance: Fluconazole
Manufacturer: Pfizer
Dosage
Packing
Price
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50 mg
28 caps
USD 166.00
100 mg
28 tab
USD 314.00
150 mg
4 caps
USD 101.00
150 mg
16 caps
USD 395.00
 

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