Fluconazole
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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...

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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


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Fluconazole keeps recurrent candidiasis at Bay - Maintenance Prophylaxis
From OB/GYN News, 6/1/03 by Miriam E. Tucker

WASHINGTON -- New data from two studies suggest that there is hope for women with complicated vulvovaginal candidiasis, Dr. Jack D. Sobel said at an update on sexually transmitted diseases sponsored by OB.GYN. NEWS and Boston University.

Maintenance prophylaxis with fluconazole appears to benefit women who typically relapse following what appears to be successful azole therapy. And women whose symptoms are caused by the nonalbicans strain Candida glabrata will probably respond to vaginal boric acid and/or flucytosine, said Dr. Sobel, professor and chief of the division of infectious diseases at Wayne State University, Detroit.

In the United States, 90% of vulvovaginal candidiasis cases in premenopausal women are uncomplicated, defined as mild to moderate in severity, with pseudohyphae, and occur infrequently or sporadically in women with normal immune systems. Nearly all of these cases will respond to one dose of fluconazole or single-dose azole therapy, Dr. Sobel said.

Complicated disease, on the other hand, may be moderate to severe and recurrent (at least four episodes a year). It may involve only budding yeast or it may occur in women with adverse risk factors such as uncontrolled diabetes, immunosuppression, and possibly pregnancy. In these women, prolonged treatment-lasting 7-14 days--is often required.

In some women, however, symptoms will return as soon as 1 month after what appears to be a complete mycologic cure. One theory is that these women are colonized with unique "adaptive strains" of Candida. Although susceptible to fluconazole, these strains remain alive--and detectable by polymerase chain reaction--despite negative cultures. "They are not new infections," Dr. Sobel noted.

Now even these women can potentially be cured. In a randomized, double-blind, multicenter study, 284 women with recurrent vaginal candidiasis infections first underwent an open-label induction period in which all were given a total of three doses of fluconazole at 72-hour intervals with the aim of achieving clinical remission. At 14 days, 95% were culture negative.

During the subsequent maintenance phase, the women took 150 mg fluconazole or placebo once a week for the next 6 months and were evaluated monthly. After that there was another 6-month period of observation during which patients were seen every 3 months.

At the end of the 6-month maintenance phase, 90% of 142 fluconazole patients remained in clinical remission, compared with just 34% of 142 who took placebo. Only 18% were culture positive at 6 months, compared with 72% of the placebo group. "It's an extraordinary difference, Dr. Sobel remarked.

After the next 6 months off the drug, 38% of the fluconazole group and 21% of the placebo group remained clinically cured. Mycologic remission remained at 12 months in 39% of the fluconazole patients and 27% of the placebo patients.

The median time for 50% of fluconazole-treated patients to have a clinical recurrence was 10.2 months, compared with 4.0 months with placebo. For mycologic recurrence, those times were 8.8 and 2.0 months, respectively Throughout the study there was no emergence of resistance or C. glabrata in vaginal isolates.

Another problematic version of recurrent vulvovaginal candidiasis--colonization with the C. glabrata species--also may be amenable to intervention, he said. C. glabrata, the most common of the nonalbicans strains, is 100 times less susceptible to most azoles than is C. albicans.

In a study of 73 women with C. glabrata vaginitis who failed azole therapy, vaginal application of boric acid (600 mg/day) produced clinical and mycologic cures in 67% treated for either 14 or 21 days.

COPYRIGHT 2003 International Medical News Group
COPYRIGHT 2003 Gale Group

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