Fluconazole
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Diflucan


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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Therapies for chronic bladder condition
From Saturday Evening Post, 5/1/05 by Cory SerVaas

Dear Dr. SerVaas:

I am writing to see if you or any of your readers know of anything that will help interstitial cystitis. I have a very dear relative who has this affliction and has suffered excruciating pain for many years. Her doctors have told her they do not know the cause nor the cure. She has learned that eating foods that are less acidic has helped some. However, the pain is exhausting. I thought perhaps you or some of your readers may have had some experience that would be helpful.

Mrs. Martin Zacha

Texarkana, Texas

For years, the late Dr. William Crook worked with Indianapolis urologist Dr. Phillip Mosbaugh to investigate whether the common yeast Candida albicans plays a role in interstitial cystitis (IC). At the time, it was quite unusual for a mainstream urologist like Dr. Mosbaugh to support such an unconventional theory.

In a 1998 pilot study, 15 patients with severe IC symptoms eliminated all sugars, wheat, yeast, beer, and al cohol from their diets and were given Diflucan (fluconazole) for treating systemic yeast infections. Although the diet was difficult to follow, six patients reported dramatic improvement and lapsed back to prior symptoms when the diet was gradually liberalized. Another six in the study were somewhat better, and three were unimproved.

"Expanded interest and research over the past 20 years has resulted in much greater awareness of interstitial cystitis, as well as more confidence and assurance in the diagnosis and better therapies," says Dr. Mosbaugh. We are sending you his summary of commonly used drug, dietary, and surgical strategies. If other readers would like to receive this information, please send a self addressed, stamped envelope to: "Medical Mailbox," Attn.: Cystitis.

Chelation for Chronic Pain

In the Mar./Apr. "Medical Mailbox," reader Byron King of Sonoma, California, requested information on using IV chelation for nondiabetic peripheral neuropathy (PN), adding that nearly every source of information he could locate is related to diabetics with the condition.

We asked Dr. Dale Guyer, a physician who utilizes complementary therapies in his clinical practice, to share his experiences with treating nondiabetic PN. His reply:

"I have observed good results with chelation therapy for nondiabetic peripheral neuropathy. In general, standard courses of chelation include 20 to 30 treatments. Improvement is often noted following 10 to 12 treatments, after which a maintenance program is advised.

"Optimum improvement is achieved when chelation is used synergistically with additional therapies. For example, I have seen excellent results with high-dose (about 10 mg daily) biotin supplementation. Acetyl 1-carnitine and good old-fashioned [B.sub.12] shots may also be beneficial.

"A good option for pain control--especially in light of the recent problems with systemic pain medicines--is pleuronic lecithin organogel (PLO gel). This is a prescription product that is manufactured by a compounding pharmacy. Anti-inflammatory agents can be mixed into the gel and rubbed on painful sites. The gel creates high levels of pain relief without being absorbed appreciably into the bloodstream. As a result, the compounded gel has no side effects for the most part. I have prescribed it for many patients, and they refer to it as "wonder' gel."

Dr. Guyer is currently participating in the NIH-funded study to test the effectiveness of chelation for coronary heart disease. See page 74 for more on the ongoing research.

COPYRIGHT 2005 Saturday Evening Post Society
COPYRIGHT 2005 Gale Group

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