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M Plempel

Publications and source records attributed to M Plempel.

At least 37 records · Page 2Linked to original sources

On the action kinetics of clotrimazole.

The introduction of clotrimazole into the therapy of vaginal Candida and Torulopsis infections has significantly shortened the previously customary duration of treatment and reduced the frequency of dosage of the active ingredient. This simplification of therapy was based on the highly favorable antimycotic properties of clotrimazole. Since compliance problems arose among patients nevertheless, it was desired to shorten the length of treatment even further. This led us to carry out extensive studies on the basis, mechanisms and kinetics of the antimycotic action of azoles so that possibilities and limits to further reductions of the duration of treatment might be ascertained. The data presented below on the structure/activity relationships, mechanism of action, MIC values under special test conditions, fungicidal action, and active ingredient release in vitro and in vivo made it possible to propose a 1-day treatment for vaginal mycoses.

Candida albicans↗

Vaginal secretion levels after 6 days, 3 days and 1 day of treatment with 100, 200 and 500 mg vaginal tablets of clotrimazole and their therapeutic efficacy.

Patients with a mycologically confirmed vaginal mycosis were treated either with one 100-mg vaginal ovule of clotrimazole each for 6 days, or with one 200-mg vaginal ovule of clotrimazole each for 3 days, or with one 500-mg vaginal ovule of clotrimazole for 1 day, the ovule having been supplied in a novel, acid formulation. 24, 48 and 72 h after the last dose, samples of secretion were taken from the fornix vaginae. The intravaginal secretion levels were determined semiquantitatively on the basis of the measured inhibition zones obtained with Candida albicans growth on agar plates, and the levels obtained with the different treatment regimens were compared. The vaginal secretion levels after a single 500-mg dose of the new formulation were higher, even after 3 days, than those measured in the 6-day treatment, while administration of 200 mg clotrimazole on 3 days resulted in no increase of the secretion levels over those seen in 6-day treatment with 100 mg.

Candidiasis, Vulvovaginal↗

[New pharmaceuticals in systemic mycoses (author's transl)].

The chemotherapy of systemic fungal infections remains problematic due to a lack of alternative agents. There are only 3 drugs available: Amphotericin B, 5-Fluorcytosine and the new iv.-formulation of Miconazole. There are as yet limited experiences concerning one of the Imidazole-derivatives of the new generation, Ketoconazole. The main antimycotic and pharmacokinetic properties of these drugs will be discussed.

Amphotericin B↗

Pharmacokinetics of imidazole antimycotics.

According to data on the imidazole antimycotics at present on the market, none of these products satisfactorily fills the gaps which exist in the treatment for mycoses of internal organs, although they have brought considerable progress in the topical treatment of mycoses. On the basis of their very broad spectrum and high intensity of activity under suitable test conditions, and the comparatively tolerable amount of side effects in man, the present imidazole antimycotics are considered to be an encouraging start for future development of derivatives which will lead to products with considerably better pharmacokinetic, and therefore better therapeutic, properties.

Adult↗

Kidney homogenate, a test medium to determine the inhibitory effect of antimycotics on yeasts.

The test procedure described in this paper aims at assessing the effectiveness of antimycotics against yeasts. The inhibitory effect on Candida albicans growth is determined in the presence of kidney homogenate, an in vitro test medium offering fungal growth conditions similar to physiological conditions. The inoculum consists of kidney material from Candida-infected mice. By dilution with kidney material from uninfected mice the initial number of viable particles is standardised. Specimens withdrawn from this inoculum are mixed with different concentrations of the test substance and incubated for 24 hours. The inhibition of fungal growth is assessed on the basis of the number of colony-forming units in comparison with controls to which no test substance was added. The growth phase of C. albicans during incubation in vitro resembles that observed in the kidney in vivo, i.e. besides yeast cells, the fungus produces a great number of pseudomycelia and mycelia. The results of the tests conducted with the top-ranking antimycotics give good evidence of their therapeutic efficacy. The testing of further active substances revealed advantages of the new test model over existing test methods.

Animals↗

[Effect of 8-methoxypsoralen and blacklight on microorganisms in vitro and in experimental trichophytosis in guinea pigs].

The lack of experimental test models causes problems in comparative evaluation of photodynamic effects of 8-MOP and its possible derivatives after irradiation with blacklight or other irradiation sources. In our experiments in vitro, tests with various microorganisms and the in vivo model of experimental dermatophytosis in guinea pigs by Trichophyton mentagrophytes appeared to be suitable. In vivo, 8-MOP was applicated orally and topically in two formulations.

Administration, Oral↗