Abstract The in vitro anthelmintic activity of essential oils from the Lamiaceae family species against Ancylostoma spp. eggs was evaluated, as well as the chemical composition by GC/MS of these essential oils. The major chemical compounds for O. vulgare were 4-terpineol, while for the essential oil of O. majorana, o 4-terpineol, and for the oil of R. officinalis it was observed cineole as major components. For this, hatchability tests were performed, where the parasite eggs were exposed to concentrations of 0.07% to 2.5% of the essential oils of Origanum vulgare, Origanum majorana and Rosmarinus officinalis. The assay was accompanied by a control with thiabendazole hydrochloride, a control with distilled water and a control with tween 80. The chemical composition of each essential oil sample was determined by gas chromatography. It was observed that all oils showed ovicidal action, and the percentage of inhibition of hatchability of R. officinalis oil was greater than 90% at concentrations from 0.62% to 2.5%. As for the essential oils of O. vulgare and O. majorana, the concentrations of 0.31% to 2.5% were those that presented an inhibitory percentage greater than 90%. Thus, this study showed that the essential oils of R. officinalis, O. vulgare and O. majorana inhibit the hatchability of Ancylostoma spp., being promising for the control of this helminth.

Resumo As infecções por nematódeos gastrintestinais (ING) constituem a maior limitação à produção de pequenos ruminantes. Na busca do controle desses parasitos, estudos com plantas medicinais têm sido uma importante alternativa. Visto isto, o estudo desenvolvido teve como objetivo avaliar a ação ovicida e larvicida in vitro do óleo essencial de Rosmarinus officinalis. O óleo foi extraído, analisado por cromatografia gasosa e testado sobre ovos e larvas de ING em seis concentrações, 227,5mg/mL; 113,7mg/mL; 56,8mg/mL; 28,4mg/mL; 14,2mg/mL; 7,1mg/mL. Para determinar a ação ovicida, ovos de ING foram recuperados de fezes de ovinos e incubados por 48h com as diferentes concentrações do óleo. Na avaliação da migração das larvas, as larvas de terceiro estágio (L3) foram obtidas por coprocultura, e associadas ao óleo essencial por 24h nas mesmas concentrações, permanecendo por mais 24h em microtamises, seguindo-se a contagem de larvas que migraram e que não migraram. Os testes in vitro com o óleo de R. officinalis mostraram o nível de significância (p<0.05) 97,4% a 100% na inibição da eclodibilidade e 20% a 74% na inibição da migração das larvas. Na análise por cromatografia gasosa o constituinte majoritário foi o eucaliptol. Os resultados apresentados mostram que o óleo essencial de R. officinalis possui ação ovicida e larvicida sobre ING de ovinos.

Abstract Gastrointestinal Nematode Infection (GIN) are the main constraint to the production of small ruminants. Studies of medicinal plants have been an important alternative in the effort to control these parasites. Therefore, the purpose of this study was to evaluate the in vitro ovicidal and larvicidal activity of essential oil of Rosmarinus officinalis. The oil was extracted, analyzed by gas chromatography and tested on GIN eggs and larvae in six concentrations, 227.5mg/mL, 113.7mg/mL, 56.8mg/mL, 28.4mg/mL, 14.2mg/mL and 7.1mg/mL. To determine the ovicidal activity, GIN eggs were recovered from sheep feces and incubated for 48h with different concentrations of the oil. For the evaluation of larval migration, third-stage larvae (L3) were obtained by fecal culture, and associated with the essential oil for 24h at the same concentrations, after which they were left for another 24 hours on microsieves, followed by the count of migrating and non-migrating larvae. The assays of R. officinalis oil showed a significant (p<0.05) 97.4% to 100% inhibition of egg hatching and a significant (p<0.05) 20% to 74% inhibition of larval migration. The main constituent revealed by gas chromatography was Eucalyptol. The results indicate that R. officinalis essential oil has ovicidal and larvicidal activity on sheep GINs.

From drug repurposing studies, this work aimed to evaluate the activity of different pyrazinoic acid (POA) derivatives against Sporothrix brasiliensis. The POA esters were prepared and characterized as previously reported by classical esterification reactions, with good to excellent yields. Sporothrix brasiliensis isolates from cats (n=6) and standard strains of S. brasiliensis and S. schenckii were used to assess the antifungal activity of the POA derivatives through broth microdilution assay (CLSI M38-A2). Among the tested compounds, molecules 3 and 4 showed fungistatic and fungicidal activities against all Sporothrix spp. strains, and the obtained MIC and MFC values ranged from 2.12 to 4.24 mg/mL and from 1.29 to 5.15 mg/mL, respectively. Compound 2 and 5 were active as in vitro inhibitors of fungal growth, but showed weak fungicidal activity, while molecules 1 and POA itself were inactive. The results suggest the activity of POA derivatives against Sporothrix spp. may be dependent on the lipophilicity. In addition, the antifungal susceptibility of the isolates to itraconazole was performed, showing that two Sporothrix isolates from cats were itraconazole-resistant. Compounds 3 and 4 were also active against these itraconazole-resistant isolates, indicating a possible alternative route to the standard mode of action of itraconazole.

Resumo Dioctophyme renale é um nematódeo zoonótico que parasita principalmente o rim de carnívoros silvestres e domésticos, e tem sido relatado com frequência no Brasil. Objetivou-se registrar o número de casos de cães e gatos diagnosticados com dioctofimatose por necropsia (1981 a 2014) e exame ultrassonográfico (2010 a 2015) em Pelotas-RS. Nesse contexto, foi realizado um inquérito de casos de dioctofimatose em animais de companhia no Laboratório de Patologia Veterinária (LPV) e no Hospital de Clínicas Veterinária (HCV) da Universidade Federal de Pelotas (UFPel), e em uma clínica veterinária especializada em diagnóstico por imagem, totalizando 95 casos registrados. A elevada casuística da doença em cães pode estar relacionada à presença de um grande número de cães errantes e semi-domiciliados na cidade, e também devido à ingestão dos hospedeiros intermediários de D. renale parasitados com a larva infectante. Assim, conclui-se que Pelotas é uma cidade propícia para a ocorrência de dioctofimatose, com elevada casuística da doença nos últimos anos.

Abstract Dioctophyme renale is a zoonotic nematode that parasites the kidneys of wild and domestic carnivores, and it has been reported frequently in Brazil. The aim here was to register the number of cases of dogs and cats diagnosed with dioctophymosis by necropsy (1981 to 2014) and ultrasound examination (2010 to 2015) in Pelotas-RS. In this context, a survey was conducted on dioctophymosis cases diagnosed at the Veterinary Pathology Laboratory (LPV) and Veterinary Clinical Hospital (HCV) of the Federal University of Pelotas (UFPel), and at a specialist veterinary imaging diagnostics clinic. In total, 95 cases were registered. The high series of the disease in dogs can be related to the presence of a large number of stray and semi-domestic dogs in the city, and also due to the ingestion of intermediate hosts of D. renale parasitized with the infective larvae. Thus, it can be concluded that Pelotas is a city with favorable conditions for the occurrence of dioctophymosis with high rate of disease in recent years.

Resumo Dioctophyme renale é um parasito zoonótico com distribuição cosmopolita, entretanto sua ocorrência é pouco conhecida. Assim, o objetivo foi avaliar a presença de ovos do parasito no ambiente e na urina de cães e gatos de zona urbana. As amostras de solo e urina foram avaliadas, respectivamente, pela técnica de Caldwell e Caldwell e por urinálise. Das 100 amostras de solo, 3% apresentaram ovos de D. renale, e das 43 amostras de urina, 18,6% foram positivas, incluindo a de felino. Conclui-se que ovos de D. renale estão presentes no ambiente urbano, assim como os caninos e felinos apresentam-se parasitados, representando um risco para a saúde pública.

Abstract Dioctophyme renale is a zoonotic parasite with worldwide distribution, although its occurrence is little known. The objective here was to evaluate the presence of parasite eggs in the environment and in the urine of dogs and cats in an urban area. Soil samples and urine were evaluated respectively by means of the Caldwell-Caldwell technique and urinalysis. Out of the 100 soil samples, 3% presented D. renale eggs, and out of the 43 urine samples, 18.6% were positive, including the feline samples. Thus, D. renale eggs are present in the urban environment, and dogs and cats are parasitized by this nematode, which therefore represents a risk to public health.

Abstract The study aimed to evaluate the anti-Sporothrix sp. activity of the essential oil of Origanum majorana Linn. (marjoram), its chemical analysis, and its cytotoxic activity. A total of 18 fungal isolates of Sporothrix brasiliensis (n: 17) from humans, dogs and cats, and a standard strain of Sporothrix schenckii (n: 1) were tested using the broth microdilution technique (Clinical and Laboratory Standard Institute - CLSI M27-A3) and the results were expressed in minimal inhibitory concentration (MIC) and minimal fungicidal concentration (MFC). The MIC50 and MIC90 of itraconazole against S. brasiliensis were 2 µg/mL and 8 µg/mL, respectively, and the MFC50 and MFC90 were 2 µg/mL and >16 µg/mL, respectively, with three S. brasiliensis isolates resistant to antifungal. S. schenckii was sensitive at MIC of 1 µg/mL and MFC of 8 µg/mL. For the oil of O. majorana L., all isolates were susceptible to MIC of ≤2.25-9 mg/mL and MFC of ≤2.25-18 mg/mL. The MIC50 and MIC90 were ≤2.25 mg/mL and 4.5 mg/mL, respectively, and the MFC50/90 values were twice more than the MIC. Twenty-two compounds were identified by gas chromatography with a flame ionization detector (CG-FID) and 1,8-cineole and 4-terpineol were the majority. Through the colorimetric (MTT) assay, the toxicity was observed in 70-80% of VERO cells between 0.078 and 5 mg/mL. For the first time, the study demonstrated the satisfactory in vitro anti-Sporothrix sp. activity of marjoram oil and further studies are needed to ensure its safe and effective use.

RESUMO Casos de esporotricose em humanos e animais sem resposta clínica satisfatória têm aumentado, sinal de alarme para o surgimento de cepas resistentes aos antifúngicos convencionais. A urgente busca por alternativas terapêuticas tem incentivado as pesquisas em plantas medicinais com atividade anti-Sporothrix spp. Um levantamento bibliográfico foi realizado com base em artigos científicos sobre a atividade antifúngica in vitro e in vivo de óleos essenciais e extratos de plantas preparados em diferentes solventes contra o complexo Sporothrix schenckii. A metodologia do estudo consistiu em uma revisão bibliográfica em Google Scholar, Science Direct, Pubmed, Bireme e Springer link com artigos desde 1986 até 2015. Foram encontradas 141 espécies de plantas já investigadas, das quais 100 espécies concentradas em 39 famílias botânicas apresentaram atividade anti-Sporothrix spp. confirmada. Combretaceae, Asteraceae e Lamiaceae representaram as famílias botânicas com maior número de espécies vegetais com potencial antifúngico, empregando diferentes metodologias. Entretanto, há poucos estudos com plantas medicinais em infecção experimental animal comprovando sua atividade no tratamento da esporotricose. Reforça-se a necessidade de mais pesquisas relacionadas à padronização de metodologias in vitro e a estudos in vivo relacionados à segurança e potencial tóxico dessas plantas com atividade anti-Sporothrix spp.

ABSTRACT Cases of sporotrichosis in humans and animals without satisfactory clinical response have increased, a warning sign of strains resistant to conventional antifungal agents. The urgent search for alternative therapies was an incentive for research on medicinal plants with anti-Sporothrix spp. properties. A bibliographic survey was performed based on scientific papers about in vitro and in vivo antifungal activity of essential oils and extracts of plants in differents solvents against the fungal of the Sporothrix schenckii complex. The study methodology consisted of a literature review in Google Scholar, Science Direct, Pubmed, Bireme and Springer link with papers from 1986 to 2015. We found 141 species of plants that were investigated, of which 100 species were concentrated in 39 botanical families that had confirmed anti-Sporothrix activity. Combretaceae, Asteraceae and Lamiaceae represented the botanical families with the greatest number of plants species with antifungal potential, using different methodologies. However, there are few studies with medicinal plants in experimental infection in animals that prove their activity in the treatment of sporotrichosis. It reinforces the need for further research related to standardization of in vitro methodologies and in vivo studies related to safety and to toxicity potential of these plants with anti-Sporothrix spp. activity.

Em virtude da resistência dos nematódeos gastrintestinais aos antihelmínticos, diversas pesquisas têm sido desenvolvidas buscando-se alternativas de controle para essas parasitoses. Nesse contexto, o estudo avaliou a ação in vitro de Origanum vulgare sobre ovos de nematódeos gastrintestinais de bovinos. Para avaliar a capacidade de inibição da eclodibilidade dos ovos, diferentes formas de extratos das folhas secas desta planta foram testadas como tintura, extrato hidroalcoólico e extrato aquoso nas concentrações de 0,62 a 80 mg/mL. Cada ensaio foi acompanhado de controle contendo cloridrato de levamisol (0,2 mg/mL), água destilada e álcool de cereais 70° GL nas mesmas concentrações dos produtos. Os resultados dos testes demonstraram que os diferentes extratos de O. vulgare inibiram a eclodibilidade dos ovos de nematódeos gastrintestinais de bovinos com percentual de inibição variando de 8,8 a 100%, sendo a tintura e o extrato hidroalcoólico as formas mais promissoras. Frente a esta propriedade ovicida, o O. vulgare pode representar uma importante fonte de compostos antiparasitários viáveis para o controle das nematodioses em ruminantes.

Due to anthelmintic resistance in nematodes, several research studies have been developed seeking control alternatives to these parasites. This study evaluated the in vitro action of Origanum vulgare on gastrointestinal nematode eggs of cattle. In order to evaluate the ability to inhibit egg hatch, different dried leaves extracts of this plant were tested, such as dye, hydroalcoholic and aqueous extracts at concentrations varying from 0.62 to 80 mg/mL. Each assay was accompanied by control containing levamisole hydrochloride (0.2 mg/mL), distilled water and 70º GL grain alcohol at the same concentration of the extracts. Test results showed that the different O. vulgare extracts inhibited egg hatch of cattle gastrointestinal nematodes at a percentage that varied from 8.8 to 100%; dye and hydroalcoholic extract were the most promising inhibitors. In view of this ovicidal property, O. vulgare may be an important source of viable antiparasitic compounds for nematodiosis control in ruminants.

The oral microbiota of humans and animals is made up of a wide variety of yeasts and bacteria, but microbiota of dogs is not totally described. Although such identification is an important step to establish the etiopathogenesis and adequate therapy for the periodontal disease The aim of this study was to evaluate and correlate oral alterations with the presence of yeasts in oral cavity of female dogs. After clinical evaluation samples from healthy and from dogs with oral diseases were obtained from three different oral sites by swabs, curettes, millimeter periodontal probes and HA membrane tip in cellulose ester. Yeast identification was performed through macroscopic and microscopic colony features and biochemical tests. Dental calculus was the most prevalent occurrence in the oral cavity of 59 females. However, the isolation of yeasts was significantly higher (p < 0.05) in animals suffering from halitosis. Eleven yeast species were identified, namely: Malassezia pachydermatis, Rhodotorula spp., Candida albicans, C. catenulata, C. famata, C. guilliermondii, C. parapsilosis, C. intermedia, Trichosporon asahii, T. mucoides and Cryptococcus albidus. It could be concluded that the yeasts are part of the microbiota from the different sites of the oral cavity of the female canines studied without causing any significant alterations except halitosis.

INTRODUÇÃO: O Cryptococcus neoformans é uma levedura capsulada, agente etiológico da criptococose em humanos e animais, encontrado em fontes ambientais, incluindo excretas de pombos, é uma importante causa de mortalidade em indivíduos imunodeprimidos em todo o mundo. MÉTODOS: Com o objetivo de verificar a ocorrência do Cryptococcus neoformans, em excretas de pombos, na Cidade de Pelotas, pesquisou-se 70 ambientes, incluindo prédios, praças e locais ao ar livre, da Cidade de Pelotas, RS. Após a coleta, os excrementos foram adicionados de salina com cloranfenicol, homogeneizados, semeados em ágar Sabouraud com cloranfenicol e ágar Níger e incubados a 32ºC. Para identificação, realizou-se exame direto, prova da fenoloxidase, urease, assimilação de carboidratos e cultura em meio CGB. RESULTADOS: Dos locais estudados (nº =70), em 26 (37,1%) havia excretas de pombos. Estes lugares foram representados por prédios históricos (nº =8), torre de igreja (nº =1), engenhos e armazéns de arroz (nº =7), praça (nº =1) e locais ao ar livre (nº =9), o isolamento de Cryptococcus neoformans ocorreu em 26,9% (nº =7/26), destes locais. CONCLUSÕES: O estudo chama a atenção, para o isolamento do fungo em áreas urbanas, que apresentavam grande acúmulo de excretas, indicando um risco para a saúde pública, especialmente para indivíduos imunocomprometidos.

INTRODUCTION: Cryptococcus neoformans is an encapsulated yeast and is the etiological agent for human and animal cryptococcosis. It is found in sources within the environment, including pigeon excrement, and is an important cause of mortality among immunocompromised individuals worldwide. METHODS: Seventy different environments in the city of Pelotas, Rio Grande do Sul, were surveyed for the purpose of investigating Cryptococcus neoformans occurrences in pigeon excreta. The environments included buildings, public squares and outdoor locations in the city. After collection, chloramphenicol saline solution was added to the excreta, which were then homogenized and seeded onto Sabouraud agar with chloramphenicol and onto Niger agar, and incubated at 32°C. Identification was performed by direct examination and by means of the phenoloxidase and urease tests, carbohydrate assimilation and culturing in CGB medium. RESULTS: Out of the sites investigated (n = 70), 26 (37.1%) of them contained pigeon excreta. These included historical buildings (n = 8), a church tower (n = 1), rice mills and warehouses (n = 7), a public square (n = 1) and outdoor locations (n = 9). Cryptococcus neoformans was isolated from 26.9% (n = 7/26) of these locations. CONCLUSIONS: This study draws attention to isolation of this fungus in urban areas that present large accumulations of pigeon excrement. This represents a risk to public health, especially for immunocompromised individuals.

The aim of this study was to evaluate the in vitro activity of the essential oil extracted from Origanum vulgare against sixteen Candida species isolates. Standard strains tested comprised C. albicans (ATCC strains 44858, 4053, 18804 and 3691), C. parapsilosis (ATCC 22019), C. krusei (ATCC 34135), C. lusitaniae (ATCC 34449) and C. dubliniensis (ATCC MY646). Six Candida albicans isolates from the vaginal mucous membrane of female dogs, one isolate from the cutaneous tegument of a dog and one isolate of a capuchin monkey were tested in parallel. A broth microdilution technique (CLSI) was used, and the inoculum concentration was adjusted to 5 x 10(6) CFU mL-1. The essential oil was obtained by hydrodistillation in a Clevenger apparatus and analyzed by gas chromatography. Susceptibility was expressed as Minimal Inhibitory Concentration (MIC) and Minimal Fungicidal Concentration (MFC). All isolates tested in vitro were sensitive to O. vulgare essential oil. The chromatographic analysis revealed that the main compounds present in the essential oil were 4-terpineol (47.95%), carvacrol (9.42%), thymol (8.42%) and □-terpineol (7.57%). C. albicans isolates obtained from animal mucous membranes exhibited MIC and MFC values of 2.72 µL mL-1 and 5 µL mL-1, respectively. MIC and MFC values for C. albicans standard strains were 2.97 µL mL-1 and 3.54 µL mL-1, respectively. The MIC and MFC for non-albicans species were 2.10 µL mL-1 and 2.97 µL mL-1, respectively. The antifungal activity of O. vulgare essential oil against Candida spp. observed in vitro suggests its administration may represent an alternative treatment for candidiasis.

O estudo objetivou avaliar a atividade in vivo do itraconazol e terbinafina no tratamento da esporotricose cutânea experimental. Foram utilizados 80 ratos Wistar divididos em quatro grupos (TERB20, TERB30, ITRA e CONT) inoculados no coxim plantar esquerdo com 0,2ml de solução contendo 2x103 células de Sporothrix schenckii/ml e tratados com terbinafina (20 e 30mg/kg), itraconazol (10mg/kg) e placebo durante 13 semanas. As lesões do sítio de inoculação foram avaliadas e mensuradas semanalmente, assim como a disseminação das mesmas. Após foi realizada análise micológica e histopatológica. Os resultados demonstraram que os animais do grupo ITRA diferiram estatisticamente em todos os parâmetros avaliados em relação ao CONT. Em relação à terbinafina, não houve diferenças estatísticas entre os grupos tratados e controle. Pode-se confirmar a boa atividade do itraconazol no tratamento da esporotricose e a pouca eficácia da terbinafina nas doses utilizadas, sendo necessários mais estudos com este antifúngico.

The aim of this study was to evaluate the in vivo activity of itraconazole and terbinafine for treating experimental cutaneous sporotrichosis. Eighty Wistar rats were used, divided into four groups (TERB20, TERB30, ITRA and CONT). They were inoculated in the left plantar pad with 0.2 ml of solution containing 2x10³ cell/ml of Sporothrix schenckii and treated with terbinafine (20 and 30 mg/kg), itraconazole (10 mg/kg) or placebo for 13 weeks. The lesions at the inoculation site were evaluated and measured weekly, along with their dissemination. Mycological and histopathological analyses were performed subsequently. The results showed that the animals in the ITRA group differed statistically in all parameters evaluated, in relation to CONT. For terbinafine, there were no statistical differences between the treated and control groups. It could be confirmed that itraconazole presented good activity for treating sporotrichosis, while terbinafine was ineffective for this disease at the doses used. However, more studies on the latter antifungal agent are needed.

Itraconazol é atualmente considerado a droga de escolha para o tratamento das diferentes formas clínicas da esporotricose. Por outro lado a terbinafina devido a sua excelente atividade in vitro está sendo avaliada quanto ao seu potencial terapêutico frente a diversas infecções fúngicas. O objetivo deste estudo foi determinar a eficácia in vivo da terbinafina e itraconazol em um modelo de esporotricose experimental sistêmica. 120 ratos Wistar receberam uma injeção de 2x10³ células de S. schenckii pela veia lateral da cauda. Após 3 dias os animais foram tratados com terbinafina (250mg/kg) e itraconazol (100mg/kg) e os seus respectivos diluentes. No modelo experimental estudado, a terbinafina e itraconazol se mostraram efetivos reduzindo o número de sintomas clínicos e retroisolamento positivo para o agente. Houve diferenças estatísticas entre os grupos tratados com os antifúngicos em relação aos grupos controle (p<0,05) nas alterações clínicas, achados anatomopatológicos e no retroisolamento do agente, sendo que os animais tratados resultaram na ausência e/ou diminuição de todos os parâmetros avaliados. Quanto aos tratamentos a terbinafina se mostrou com atividade similar ou superior ao itraconazol quando avaliado as alterações anatomopatológicos do testículo (p=0,0004), assim como no retoisolamento do órgão (p=0,0142). Com estes resultados permite-se concluir que os antifúngicos estudados são efetivos no tratamento da esporotricose sistêmica experimental.

Itraconazole is currently considered the drug of choice to treat the diverse clinical presentation of sporotrichosis. On the other hand terbinafine by virtue of its excellent in vitro activity is under comparative evaluation for its therapeutic potential for a wide range of fungal infections. In this study, our aim was to determine the in vivo efficacy of terbinafine and itraconazole on a experimental model of systemic sporotrichosis. 120 rats Wistar received an injection of 2x10³ S. schenckii cells by via the lateral tail vein. After 3 days the animals were treated with terbinafine (250mg/kg) and itraconazole (100 mg/kg) and their respective diluents. In our model, terbinafine and itraconazole were effective in reducing the number of clinical lesions and positive organ cultures. There was statistical difference between the groups treated with the antifungals in relation to the control groups (p<0,05) concerning the clinical alterations, anatomic-pathological findings and in the positive organ cultures of the agent, being that the treated animals resulted in the absence and/or reduction of all the evaluated parameters. As for the treatments, terbinafine showed similar or higher activity that itraconazole in the evaluation of the testicle alteration (p=0,0004), as well as in the positive organ cultures of microorganism from the organ (p=0,0142). With these results it is possible to conclude that the antifungals studied are effective in the treatment of experimental systemic sporotrichosis.

Levando em consideração a importância do itraconazol e da terbinafina na terapia antifúngica, o estudo tem como objetivo avaliar os efeitos de altas doses de itraconazol (100 mg/kg) e terbinafina (250 mg/kg) em ratos albinos wistar através das análises das enzimas hepáticas (ALT e ALP), hemograma completo e estudo histopatológico de diferentes órgãos. Os fármacos foram administrados pela via oral, uma vez ao dia, por um período de 30 dias, quando foi coletado sangue e realizado a necrópsia dos animais experimentais. Os valores detectados das enzimas hepáticas e do hemograma foram compatíveis aos índices fisiológicos para a espécie estudada não sendo observadas diferenças estatísticas entre os grupos experimentais. A histopatologia não revelou nenhuma anormalidade, porém 25% dos animas tratados com terbinafina morreram imediatamente após a administração do fármaco. Com esses resultados concluiu-se que as doses administradas dos fármacos não alteraram as enzimas hepáticas avaliadas, assim como o hemograma, sendo, no entanto, necessários mais estudos que possibilitem considerar doses elevadas da terbinafina e itraconazol como alternativa terapêutica viável para o tratamento de micoses sistêmicas.

Taking into account the importance of the itraconazole and terbinafine in the antifungal therapy, the study has as objective evaluate the effects of high itraconazole doses (100 mg/kg) and terbinafine (250 mg/kg) in rats albino Wistar through the analyses of the hepatic enzymes (ALT and ALP), complete blood count and histopathologic study of different organs. The drugs were administered orally once a day, for a period of 30 days, when blood was collected and accomplished the necropsy of the experimental animals. The detected values of the hepatic enzymes and of the blood count were compatible to the physiologic indexes for the studied species with no statistical differences among the experimental groups. The histopathologic exam did not reveal any abnormality, however 25% of the treated with terbinafine died immediately after the administration of the drug. With those results we concluded that the administered doses of the drugs did not alter the appraised hepatic enzymes, as well as the blood count. However, more studies are needed to consider high doses of the terbinafine and itraconazole as viable treatment alternative for systemic mycosis.

O estudo objetiva determinar a atividade in vitro da terbinafina e itraconazol através da técnica de microdiluição em caldo (NCCLSM27-A2) adaptado para um fungo dimórfico frente a 12 isolados de Sporothrix schenckii, sendo seis de esporotricose felina, três de esporotricose humana, um isolado de cão e dois isolados humanos provenientes do Instituto Oswaldo Cruz (IOC). O inóculo e as concentrações antifúngicas foram distribuídas em microplacas, as quais foram incubadas a 35°C por cinco dias, quando foi realizada a leitura da concentração inibitória mínima. A concentração inibitória mínima para a terbinafina variou de 0,055µg/ml a 0,109µg/ml e para o itraconazol de 0,219µg/ml a 1,75µg/ml, sendo que para ambos os fármacos as CIMs entre os isolados do IOC foi de 0,875µg/ml. O estudo demonstrou uma alta suscetibilidade do Sporothrix schenckii frente à terbinafina, necessitando mais estudos que correlacionem os testes in vitro frente ao fármaco com a resposta clínica em pacientes com esporotricose.

The study objective was to determine the in vitro activity of terbinafine and itraconazole through the microdilution technique in broth (NCCLSM27-A2), adapted for dimorphic fungus, in relation to 12 isolates of Sporothrix schenckii. Six were from feline sporotrichosis, three from human sporotrichosis, one from a dog and two from human isolates originating from Instituto Oswaldo Cruz. The inoculum and antifungal concentrates were distributed on microplates that were incubated at 35°C for five days. Minimum inhibitory concentration readings were made at the end of this period. The MIC for terbinafine ranged from 0.055µg/ml to 0.109µg/ml, and the MIC for itraconazole ranged from 0.219µg/ml to 1.75µg/ml. For both drugs, the MIC from the isolates from IOC was 0.875µg/ml. The present study demonstrates the high susceptibility of Sporothrix schenckii to terbinafine. Further studies to correlate the in vitro susceptibility tests with the clinical response of patients with sporotrichosis are needed.