Fluconazole
Find information on thousands of medical conditions and prescription drugs.

Fluconazole


Fluconazole is a synthetic antimycotic drug of the triazole class of compunds. The drug is sold under the brand name DiflucanĀ®. It is used orally and intravenously to treat yeast and other fungal infections. more...

Home
Diseases
Medicines
A
B
C
D
E
F
Captagon
Famohexal
Famotidine
Faslodex
Faslodex
Fasoracetam
Felbamate
Felbatol
Felodipine
Felypressin
Femara
Femara
Fempatch
Femring
Fenfluramine
Fenofibrate
Fentanyl
Fexofenadine
Filgrastim
Filipin
Finasteride
Fioricet
Fiorinal
Flagyl
Flarex
Flavoxate
Flecainide
Flexeril
Flomax
Flonase
Flovent
Floxuridine
Fluacizine
Flucloxacillin
Fluconazole
Flucytosine
Fludarabine
Fludrocortisone
Flumazenil
Flunisolide
Flunitrazepam
Fluocinonide
Fluohexal
Fluorometholone
Fluorouracil
Fluoxetine
Fluphenazine
Flurazepam
Flutamide
Fluticasone
Fluvastatin
Fluvoxamine
FML
Focalin
Folic acid
Follutein
Fomepizole
Formoterol
Fortamet
Fortovase
Fosamax
Fosinopril
Fosinoprilat
Fosmidomycin
Fosphenytoin
Frova
Frovatriptan
Frusehexal
Fulvestrant
Fumagillin
Furazolidone
Furosemide
Furoxone
Fusafungine
Fusidic acid
Fuzeon
G
H
I
J
K
L
M
N
O
P
Q
R
S
T
U
V
W
X
Y
Z

Mode of action

Fluconazole inhibits, much like the imidazole-antimycotics, the fungal P450-enzyme. The consequences are that Lanosterol can no longer be converted to Ergosterol. Ergosterol is an essential part of the fungal membrane and its deficit alters the permeability of the membrane and this eventually disrupts fungal growth. It acts fungistatic or fungizide depending on the susceptibility of the strain and the dose regime used. Fluconazole is theoretically capable of inhibiting demethylases in the human body, but this effect is not seem with therapeutic doses.

Susceptible fungi

Animal models (infection studies) showed that fluconazole is active against infections with strains of Candida, Cryptococcus, Aspergillus, Blastomyces, Coccidioides and Histoplasma. In vitro test systems are still inreliable.

Pharmacokinetic data

Following oral dosing, fluconazole is almost completely absorbed within two hours. The high bioavailability of over 90% is not significantly reduced by concomitant intake of meals and co-medication with H2-antagonists (e.g. cimetidine, ranitidine). Concentrations measured in urine, saliva, sputum and vaginal secrete are approximately equal to the plasma concentration measured following a wide dose range from 100 to 400 mg oral as a single dose. The half-life of fluconazole is approximately 30 hours and is increased in patients with impaired renal function.

Elimination and excretion

Fluconazol is renally eliminated and primarily (80%) excreted in the urine as unchanged drug.

Carcinogenicity

Male rats treated with 5 mg and 10 mg/kg weight respectively showed a higher incidence of hepatocelluar adenomas than expected. No data exists on human carcinogenity.

Uses

  • Infections with Candida in mouth and esophagus.
  • Recurrent vaginal infections, if local therapy is not sufficient.
  • Prophylaxis of infections with Candida in tumor patients receiving chemo- or radiotherapy.
  • Treatment of deep or recurrent fungal infection of the skin (dermatomycosis), if local treatment was not successful. The efficacy of fluconazole in the treatment of onchomycosis (fungal infection of the nails) has not been demonstrated.
  • Sepsis due to emergence of Candida in the blood (candidaemia).
  • Meningitis and prophylaxis of meningitis caused by cryptococcus in AIDS-Patients. In a subgroup of patients Fluconazole acts more slowly than amphotericin B alone or in combination with flucytosine. Nonetheless, response and curation rates were not significantly different.
  • Treatment of blastomycosis, histoplasmosis, coccidioidomycosis, sporotrichosis, and aspergillosis. Sometimes amphotericin B is the preferred agent.

Read more at Wikipedia.org


[List your site here Free!]


A comparison of fluconazole oral suspension and amphotericin B oral suspension in older patients with oropharyngeal candidosis - Statistical Data Included
From Age and Ageing, 3/1/00 by Jean Taillandier

Background: the optimum treatment for oropharyngeal candidosis, particularly in older patients, has not been established. Local treatment with nystatin and amphotericin B can be problematic. The oral suspension formulation of fluconazole may offer a good alternative to these conventional agents. Objective: to compare the safety and efficacy of fluconazole oral suspension with amphotericin B oral suspension in the treatment of older patients with oropharyngeal candidosis. Design: randomized open-label study. Patients: three hundred and five patients, aged 62 or older, with at least one sign or symptom of oropharyngeal candidosis. Methods: we evaluated patients for the signs and symptoms of candidosis before receiving the study drug and on days 4, 7 and 14. We assessed patients who were cured or improved after 7-14 days of treatment 2 weeks after the end of treatment (follow-up). We obtained specimens from buccal lesions for microscopic examination (baseline only) and culture at baseline and on days 7 and 14. Patients were evaluated for adverse events on days 4, 7 and 14. Results: one hundred and fifty patients received fluconazole and 155 received amphotericin B. There were no statistically significant differences in clinical or mycological response between fluconazole and amphotericin B at the end of treatment or at follow-up. At the end of treatment, 122 (81%) of 150 fluconazole-treated and 135 (87%) of 155 amphotericin B-treated patients were clinically cured or improved. Mycological cure rates were 35% and 46% for fluconazole and amphotericin B, respectively. The symptoms of burning sensation and buccal pain resolved significantly sooner (P < 0.05) in fluconazole-treated patients. The presence of dentures did not affect the response to antifungal therapy. The incidence of adverse events was 46% in the fluconazole group and 50% in the amphotericin B group (not statistically significant). Conclusion: fluconazole oral suspension is a good therapeutic alternative to amphotericin B oral suspension in the treatment of older patients with oropharyngeal candidosis.

COPYRIGHT 2000 Oxford University Press
COPYRIGHT 2000 Gale Group

Return to Fluconazole
Home Contact Resources Exchange Links ebay