The efficacy of orally applied terbinafine, itraconazole and fluconazole in models of experimental trichophytoses.

The antimycotic efficacy of terbinafine, itraconazole and fluconazole was evaluated in guinea-pig trichophytoses (Trichophyton mentagrophytes, Trichophyton rubrum) by use of the hair root invasion test (HIT) and the auricular skin temperature test (STT). In the prophylactic HIT model using T. mentagrophytes as the infective agent, statistical evaluation of the ratios of protected/inoculated animals revealed ED50 values of 2.

Preclinical antimycotic activity of SDZ 89-485: a new orally and topically effective triazole.

SDZ 89-485 is a new orally and topically active triazole antifungal with efficacy superior to reference compounds in most animal infection models used for preclinical comparison of antifungals. The compound inhibits mycelial transformation of Candida albicans in vitro at MIC50 concentrations of 0.006 and 0.

Preclinical evaluation of terbinafine in vivo.

The fungicidal activity of terbinafine which has been demonstrated in vitro for several strains of dermatophyte, filamentous and dimorphic fungi, has been demonstrated in vivo in model systems for dermatophytoses. This activity is accompanied by a fast onset of action which leads to superior antifungal efficacy when compared with fungistatic drugs.

Activity of terbinafine in experimental fungal infections of laboratory animals.

The allylamine derivative terbinafine is the first antifungal agent with primary fungicidal properties against dermatophytes which acts systemically after oral application as well as locally after topical application. Comparative oral studies carried out with griseofulvin and ketoconazole in model infections such as guinea pig trichophytosis and microsporosis revealed terbinafine to be superior to the reference compounds both clinically and mycologically. An excellent antimycotic activity of terbinafine was also demonstrable after topical treatment of guinea pig dermatophytoses caused by Trichophyton mentagrophytes or Microsporum canis.

Antifungal activity of the allylamine derivative terbinafine in vitro.

Terbinafine, an allylamine derivative, represents the most effective of this new chemical class of antimycotic compounds. Under in vitro conditions, terbinafine proved to be highly active against dermatophytes (MIC range, 0.001 to 0.

The "hair root invasion test", a semi-quantitative method for experimental evaluation of antimycotics in guinea-pigs.

The hair root invasion test is a new method for preclinical evaluation of the antimycotic efficacy of chemical compounds in vivo based on their antifungal activity against dermatophytes located at hair roots in the depth of the hair follicles of guinea-pigs. The test design allows for semi-quantitative assessment of the invasion density of the hair follicles in mycotic foci of treated and untreated animals. Conditions that must be met in order to yield satisfactory results are discussed and test results from standard antimycotics are presented.

In vivo antimycotic activity of naftifine.

Naftifine, a new antifungal agent belonging chemically to the allylamines, was tested for its in vivo activity after topical application against guinea pig skin infections caused by Trichophyton mentagrophytes, T. mentagrophytes var. quinckeanum, or Microsporum racemosum.

In vitro activity of naftifine, a new antifungal agent.

Naftifine exhibits an interesting in vitro spectrum of activity against dermatophytes (38 strains; minimal inhibitory concentration [MIC] range 0.1 to 0.2 microgram/ml), aspergilli (6 strains; MIC range, 0.

New chemotherapeutic nitroheterocycles active against 5-nitroimidazole-resistant strains of trichomonads.

The synthesis and the trichomonacidal activity of some 4-substituted 2-imidazolylquinazoline derivatives are described. The new compounds were highly active against metronidazole-sensitive and metronidazole-resistant strains of trichomonads. This was demonstrated in vitro as well as in various trichomoniasis models in mice and rats after oral treatment.

[The efficacy of pleuromutilins on Aegyptianella pullorum infections in chickens (author's transl)].

Pleuromutilins have an aegyptianellicidal efficacy. A significant chemotherapeutic influence on the course of the infection in chickens could only be achieved after repeated oral and intramuscular applications of at least 150 mg and 75 mg/kg body weight respectively. However, even at these concentrations the infections were not cleared.

Enhancement of the anticoccidial activity of polyether antibiotics in chickens by tiamulin.

The anticoccidial activities of monensin and lasalocid have been studied separately and in combination with tiamulin, a new pleuromutilin derivative. Combinations of constant tiamulin concentration (.0125%) in drinking water with various levels of polyether anticoccidials (6.

Studies on strain sensitivity of Trichomonas vaginalis to metronidazole.

Ninety-four strains of Trichomonas vaginalis isolated from unselected patients in Vienna during the period from November 1975 to November 1975 were subjected to sensitivity tests against metronidazole in vitro and in vivo. Nearly 90% of the isolates examined showed in vitro growth inhibition at concentrations of 0.4 to 1.

Assay conditions and the demonstration of nitroimidazole resistance in Tritrichomonas foetus.

Tritrichomonas foetus KV(1), a nitroimidazole-susceptible strain, and KV(1)/M100, its nitroimidazole-resistant daughter strain, differed markedly in their in vivo susceptibility to metronidazole. In vitro susceptibility testing in multiwell plates and tubes with different trichomonad media containing no, or low concentrations of, ascorbate demonstrated that the resistant strain behaves like the susceptible one, if tested under anaerobic conditions (deep cultures in tubes or multiwell plates in anaerobic jars), but shows resistance if tested in the presence of air (multiwell plates exposed to air). In media containing high concentrations of ascorbate, no resistance was observed even in air.

[Experimental studies on the schistosomicidal activity of the aminobenzaldehyde derivative 80.647 (author's transl)].

In a group of aminobenzaldehyde derivatives the 2-cholor-4-(1)-piperazinobenalazine showed to be highly active in golden hamsters (Mesocricetus auratus), Mastomys natalensis and capucine monkeys (Cebus capucinus capucinus) against Schistosoma mansoni, slightly active against S. mattheei and inactive against S. haematobium and S.

[The efficacy of established, systemically active trichomonacidal agents in the infection model tri-chomonas vaginalis/rat (author's transl)].

Experimental chemotherapeutical studies were carried out with metronidazole, tinidazole, nitrimidazine and ornidazole in rats infected with Trichomonas vaginalis intravaginally. All compounds tested showed a systemic trichomonacidal activity within rather a narrow dosage range after three oral doses and also after a single dose, i.e.

Mastomys natalensis as an experimental host for Brugia malaye subperiodic.

Infective larvae of Brugia malayi subperiodic obtained by dissection of infected Aedes togoi were injected subcutaneously into the scrotal region of Mastomys natalensis. From altogether 58 infected male M. natalensis 81% showed consistently or intermittently detectable microfilaraemia, whereas in 19% of the animals no microfilaraemia could be detected at any stage.