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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 Diflucan®. 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.

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South Africa: Historic "Defiance Campaign" Imports Generic Fluconazole - Treatment Action Committee imports fluconazole for HIV treatment
From AIDS Treatment News, 10/20/00 by John S. James

This week South Africa's Treatment Action Committee (TAC), the major HIV treatment activist group in the country, defied patent laws by importing generic fluconazole from Thailand, where TAG purchased it more than 50 times cheaper than the South African retail price, according to news reports in the country. Many people in Africa have died because they could not afford the drug-including activist and TAC member Christopher Moraka, who had testified to a committee of parliament about the need for fluconazole and about its inflated price. The campaign to import the drug and raise this issue has been named after him.

For months patent holder Pfizer has been negotiating with the South African government to provide fluconazole free to the government for treating cryptococcal meningitis-but apparently not for major candidiasis (thrush) infections, which killed Christopher Moraka, and apparently with no price reduction for patients who cannot get the drug through the government program but have to purchase it privately. Pfizer made the donation announcement after TAG had raised the issue by asking the company to either reduce its price to twice the generic price, or license someone else to do so. The company's press release reaped great international publicity, but in the months since, not one capsule has reached a single patient.

TAC has applied to the South African government for a humanitarian exemption to import the generic-an exemption recognized under the country's law. Instead, the government charged organizer Zackie Achmat with a criminal offense. He turned himself in to the police, providing documentation on the Thai product (called Biozole) and a sample of the drug, and was not arrested at that time.

The Defiance Campaign is supported by many doctors and nurses, by Jubilee 2000, by trade unions, by the AIDS Consortium and AIDS Law Project, and by children's rights organizations throughout the country.

TAC has asked for international awareness and support. More information will be available at http://www.tac.org.za/ or at http://www.healthgap.org/

In North America, financial contributions can be made through the South Africa Development Fund, 555 Amory St., Boston MA 02130, 617-522-5511, freesa@igc.org; make checks payable to the South Africa Development Fund, and indicate the funds are for the TAC Christopher Moraka Defiance Campaign. According to TAC's October 17 press release, "100% of the, donation will go to purchasing and distributing medication via qualified health professionals only, free of charge to patients."

Comment

It's time to call an end to the current system where tens of thousands of people must die routinely to protect the profits of giant corporations with the political influence money can buy. We do need patent protection to provide incentive for drug development, but the rules must be changed so that they do not have horrible consequences. That's what the Christopher Moraka Defiance Campaign Against Patent Abuse is about.

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