RESUMO
As the prevalence of drug-resistant Candida isolates continues to rise, the imperative for identifying novel compounds to enhance the arsenal of antifungal drugs becomes increasingly critical. Consequently, exploring new treatment strategies, including synthesizing molecular hybrids and applying combination therapy, is essential. For this reason, this study evaluated the efficacy of ten molecular hybrids of aza-bicyclic 2-isoxazoline-acylhydrazone belonging to two series 90 and 91 as possible anti-Candida agents. In addition, we also investigated the interaction between the hybrids and fluconazole, a commonly used antifungal drug. We evaluated the antifungal effect of aza-bicyclic 2-isoxazoline-acylhydrazone hybrid compounds against six Candida spp. strains that target planktonic cells. However, none of these new molecules were inhibitory active at the tested concentrations (2 to 1,024 µg/mL). Moreover, we analyzed the interaction between the ten new hybrid molecules and fluconazole using the checkerboard assay, employing two different methodologies for reading the plate. For this, one isolate fluconazole-resistant was selected. We observed that only one combination, 6-(4-tert-butylbenzoil)-4,5,6,6a-tetrahydro-3a-H-pirrole[3,2-d]isoxazole-3-carboxylic(furan-2-metilidene)-hydrazide (91e) and fluconazole, exhibited a synergistic interaction (FICI range 0.0781 to 0.4739). The combination successfully inhibited the growth of C. albicans CA2 fluconazole-resistant, and no interaction was observed in an isolate susceptible to fluconazole. Additionally, these results emphasize the continued need for research into new compounds and the importance of using combined approaches to increase their activity.
Assuntos
Antifúngicos , Candida albicans , Farmacorresistência Fúngica , Sinergismo Farmacológico , Fluconazol , Hidrazonas , Isoxazóis , Testes de Sensibilidade Microbiana , Antifúngicos/farmacologia , Antifúngicos/química , Fluconazol/farmacologia , Candida albicans/efeitos dos fármacos , Hidrazonas/farmacologia , Hidrazonas/química , Isoxazóis/farmacologia , Isoxazóis/química , HumanosRESUMO
BACKGROUND: In 2022, fluralaner was launched on the market for use in the control of the cattle tick Rhipicephalus microplus after showing 100% efficacy in registration trials against the causative agents of cattle tick fever (TFAs). The aim of the present study was to determine whether a strategic control regimen against R. microplus using fluralaner (FLU) in Holstein calves grazing in a tropical region would alter the enzootic stability status of cattle tick fever, triggering outbreaks in these animals up to 22 months age. METHODS: In this study, a group of calves treated with FLU was compared with a control group treated with the regimen currently being used on the farm, which consisted of the fipronil + fluazuron formulation (FIFLUA). In the first experiment, the efficacy of the FIFLUA pour-on formulation was evaluated in a field study. In the second experiment, which lasted 550 days, two experimental groups (n = 30/group) of Holstein calves naturally infested with R. microplus were analyzed. Calves aged 4 to 10 months received either a specific treatment regimen with FLU (experimental group) or FIFLUA (control group). During this period, tick counts, animal weight measurement, feces collection (to determine eggs and oocysts per gram of feces), tick fever monitoring, blood smears (to ascertain enzootic stability of the herd), PCR testing for TFAs and serology (indirect enzyme-linked immunosorbent assay [iELISA]) were performed. All calves were evaluated for signs of tick fever between ages 11 and 22 months. RESULTS: FIFLUA showed an acaricidal efficacy of > 90% from post-treatment days 14 to 35. Regarding treatments against the TFAs, the average number of treatments was similar between groups, but animals treated with FLU had a smaller reduction in packed cell volume on some of the evaluation dates of the second and third treatment against TFAs. In calves aged 10 months in the FLU group, B. bovis was not detected by PCR (0/15 samples), 40% of the samples had antibody titers and 33% (10/30) of the samples had positive blood smears. Regarding B. bigemina, > 86% of the samples in both groups tested positive for B. bigemina DNA and antibodies; there was no difference in the antibody titers between the groups. There were no clinical cases of cattle tick fever in calves aged 11 to 22 months. CONCLUSIONS: In comparison with the control treatment, the strategic control regimen against R. microplus with FLU that was implemented in the present study did not negatively affect the enzootic stability status of A. marginale and B. bigemina in the herd up to 22 months of age. The enzootic stability status of B. bovis was not reached by either group. These results likely represent a characteristic of the local tick population, so further studies should be performed.
Assuntos
Anaplasmose , Babesiose , Doenças dos Bovinos , Isoxazóis , Rhipicephalus , Infestações por Carrapato , Animais , Bovinos , Controle de Ácaros e Carrapatos , Infestações por Carrapato/tratamento farmacológico , Infestações por Carrapato/prevenção & controle , Infestações por Carrapato/veterinária , Doenças dos Bovinos/epidemiologia , Óvulo , Babesiose/epidemiologia , Anaplasmose/epidemiologiaRESUMO
Tungiasis is an endemic dermatological parasitic zoonosis in Latin America, caused by the sand flea Tunga spp. (Siphonaptera, Tungidae), which promotes intense discomfort, swelling, erythema, itching, pain, secondary bacterial infection, cellulitis and necrosis. Sarolaner has been used to control different ectoparasites, but there is no record of its use for the treatment of tungiasis in dogs. The objective of this study was to evaluate the effectiveness of sarolaner for the treatment dogs naturally infested by Tunga spp. kept in the same infested environment. Three of four animals were medicated with sarolaner orally with a single dose of 2 mg/kg, as recommended by the manufacturer, and one animal remained without medication. After 24 hours, the fleas from all four dogs were mechanically removed. The animals were reevaluated on days +15 and +30 to assess possible reinfestation. The medicated animals remained free of fleas, while the untreated animal had fleas on the days previously defined for reevaluation. We can thus conclude that the use of sarolaner is an effective choice for tungiasis treatment.
Tungíase é uma zoonose parasitária dermatológica endêmica na América Latina, causada pela pulga da areia Tunga spp. (Siphonaptera, Tungidae), que promove intenso desconforto, edema, eritema, prurido, dor, infecção bacteriana secundária, celulite e necrose. Sarolaner tem sido utilizado no controle de diversos ectoparasitas, mas não existem registros de seu uso no tratamento de tungíase em cães. O objetivo deste estudo foi avaliar a eficácia do sarolaner no tratamento de cães naturalmente infestados por Tunga spp. mantidos no mesmo ambiente infestado. Três dos quatro animais foram medicados com sarolaner por via oral em dose única de 2 mg/kg, conforme recomendação do fabricante, e um animal permaneceu sem medicação. Após 24 horas, as pulgas dos quatro cães foram removidas mecanicamente. Os animais foram reavaliados nos dias +15 e +30 para avaliar uma possível reinfestação. Os animais medicados permaneceram livres de pulgas, enquanto o animal não tratado apresentou pulgas nos dias previamente definidos para reavaliação. Podemos assim concluir que o uso do sarolaner é uma escolha eficaz para o tratamento da tungíase.
RESUMO
BACKGROUND: In Rio Grande do Sul, Brazil, a region with a subtropical climate, Rhipicephalus microplus is present in taurine cattle raised for beef and milk. In addition, ticks resistant to multiple acaricides are present in this region. Recently, fluralaner (isoxazoline) was launched on the market. Thus, there is a need to evaluate the effects of fluralaner for the control of R. microplus on taurine cattle. In addition, occurrence of myiasis by Cochliomyia hominivorax larvae after tick parasitism and weight gain of cattle during the experimental period were evaluated. METHODS: Thirty naturally infested cattle were divided into two experimental groups: T01, treated with fluralaner (2.5 mg/kg) pour-on; T02, control. T01 received fluralaner on Days 0 (early summer in January), 42 and 84 (early autumn), whereas T02, a control group, received palliative treatment with a spray formulation when the group mean was ≥ 30 ticks. Counts of R. microplus females and calculation of the efficacy of fluralaner were performed on Days 3, 7, 14, 28, 35, 42, 56, 70, 84, 98, 112 and 126. The occurrence of myiasis was assessed throughout the study period. In addition, the weight, weight gain and daily weight gain of the animals were evaluated. RESULTS: In the 12 evaluations performed, the parasitic load of T01 was near zero. Fluralaner showed 99.5% efficacy on the 3rd day after the first treatment and 100% efficacy from Day 7 to Day 126. Cochliomyia hominivorax larvae (n = 6; p = 0.0251) were found only in the control group (T02). At the end of the study, the animals subjected to treatments with fluralaner gained 32.8 kg more than the animals in the control group. CONCLUSIONS: Application of fluralaner in summer and autumn, with 42-day intervals between treatments, was effective to control R. microplus on taurine cattle, which also gained more weight than control cattle. Additionally, no cases of myasis were documented in animals treated with fluralaner.
Assuntos
Doenças dos Bovinos , Isoxazóis , Miíase , Rhipicephalus , Infestações por Carrapato , Feminino , Bovinos , Animais , Infestações por Carrapato/tratamento farmacológico , Infestações por Carrapato/prevenção & controle , Infestações por Carrapato/veterinária , Miíase/veterinária , Larva , Calliphoridae , Aumento de Peso , Doenças dos Bovinos/tratamento farmacológico , Doenças dos Bovinos/prevenção & controle , Doenças dos Bovinos/epidemiologiaRESUMO
BACKGROUND: This study describes the effectiveness of a novel active pharmaceutical ingredient, fluralaner (isoxazoline class), against important ectoparasites infesting cattle in Brazil. METHODS: A total of 13 studies involving a 5% fluralaner-based pour-on formulation (Exzolt 5%; further referred to as Exzolt) were conducted. Specifically, the effectiveness of this formulation was studied against Rhipicephalus microplus (6 studies), Cochliomyia hominivorax larvae (4 studies), Dermatobia hominis larvae (1 study) and Haematobia irritans flies (2 studies). RESULTS: The therapeutic efficacy of Exzolt was found to exceed 98% at 4 days post treatment (DPT), while persistent efficacy (> 90% efficacy) against repeated infestations of R. microplus was observed for up to 79 DPT. In field studies, ≥ 98% therapeutic efficacy was demonstrated at all study sites by 7 DPT, and a persistent efficacy (> 90% efficacy) was observed for 42, 49 or 56 DPT. Exzolt prevented C. hominivorax eggs from developing to the larval stage, thus mitigating the development of myiasis in cattle naturally and artificially infested with this screworm. The efficacy of Exzolt against D. hominis larvae was 98% at 3 DPT, while persistent efficacy (> 90% effectiveness) was found to last for up to 70 DPT. Against H. irritans, Exzolt showed therapeutic efficacy (≥ 90%) within the first day of treatment at both study sites, while persistent efficacy (≥ 90%) was observed for 7 DPT at one site and for 21 DPT at the other site. CONCLUSIONS: Overall, the results from these studies confirm that Exzolt is therapeutically efficacious against the most important ectoparasites infesting cattle in Brazil. The novel active pharmaceutical ingredient, fluralaner, provides a new treatment option for farmers to control cattle ectoparasites, especially where there is resistance to other chemical classes. In addition, an effective control of ectoparasites will improve overall cattle health and well-being as well as production.
Assuntos
Doenças dos Bovinos , Muscidae , Infestações por Carrapato , Animais , Bovinos , Brasil/epidemiologia , Óvulo , Larva , Doenças dos Bovinos/tratamento farmacológico , Doenças dos Bovinos/prevenção & controle , Doenças dos Bovinos/parasitologia , Preparações Farmacêuticas , Infestações por Carrapato/tratamento farmacológico , Infestações por Carrapato/prevenção & controle , Infestações por Carrapato/veterináriaRESUMO
Fluralaner is a relatively new insecticide belonging to the isoxazoline group, whose action mechanism involves the blocking of GABAA-receptors in the insect nervous system. Because of its high hydrophobicity, fluralaner could bioaccumulate and reach toxic local concentrations. Since there are no data available about the penetration and persistence of isoxazolines in biological membranes, we intend to evaluate fluralaner permanence as a pollutant by using model membranes. We used experimental and in silico models to characterize the incorporation of fluralaner into the lipid phase at different packing states. We determined its impact in the membrane structure and organization. Our results confirm that fluralaner is capable of penetrating, holding, and accumulating in the lipid membrane and provide details on its precise location and orientation. These properties would allow fluralaner to reach high local concentrations in different membranes and organs, which could be dangerous for vertebrate organisms if its handling is not properly controlled.
Assuntos
Inseticidas , Inseticidas/química , Isoxazóis , Receptores de GABA-A , LipídeosRESUMO
In dogs, Rhipicephalus linnaei transmits pathogens such as Ehrlichia canis, Babesia vogeli, and Hepatozoon canis. The veterinary market has synthetic acaricides to ticks control. Esters derived from castor oil are efficient. However, there is little information about their effects on non-target organisms. This work consisted of a clinical (AST, ALT, and ALP) and histological and histochemical analysis (liver and spleen) of female rabbits exposed to these esters and afoxolaner. The rabbits were divided into three groups: control group (CG) received Bandeirante® rabbit feed; the afoxolaner treatment (TG1) received rabbit feed and two doses of afoxolaner; castor oil esters treatment (TG2) received rabbit feed enriched with esters (1.75 g esters/kg). No alterations were observed in the AST, ALT, and ALP enzymes in exposure to esters TG2. Rabbits from TG1 showed changes in AST. The liver of rabbits exposed to afoxolaner underwent histological and histochemical changes, such as steatosis and vacuolation, as well as poor protein labeling. Polysaccharides were intensely observed in the group exposed to esters. The spleen showed no changes in any of the exposure. Esters from castor oil caused fewer liver changes when incorporated into the feed and fed to rabbits than exposure to afoxolaner.(AU)
Carrapatos Rhipicephalus linnaei transmitem patógenos como Ehrlichia canis, Babesia vogeli e Hepatozoon canis, para os cães. O mercado veterinário dispõe de acaricidas sintéticos para o controle desses ectoparasitas. Ésteres derivados do óleo de mamona são eficientes, mas há pouca informação sobre seus efeitos em organismos não-alvos. Esse trabalho objetivou analisar clínica (AST, ALT e ALP), histológica e histoquímicamente (fígado e baço) coelhas expostas aos ésteres e ao afoxolaner, tendo sido as mesmas alocadas nos grupos: Controle (GC) que recebeu ração Bandeirante®; Tratamento 1 (TG1), além da ração foram expostas ao afoxolaner, Tratamento 2 (TG2) receberam ração enriquecida com os ésteres (1,75 g ésteres/kg). Não houve alterações nas enzimas AST, ALT e ALP na exposição aos ésteres (TG2). No TG1 houve alterações na AST. O fígado das coelhas do TG1 apresentou alterações histológicas e histoquímicas, tais como esteatose e vacuolização, bem como fraca marcação de proteínas. Polissacarídeos foi intensamente marcados no fígado do TG2. O baço não apresentou alterações em nenhum dos grupos. Os ésteres do óleo de mamona causaram menos alterações hepáticas nas coelhas do que quando elas foram expostas ao afoxolaner.(AU)
Assuntos
Animais , Feminino , Rhipicephalus/fisiologia , Acaricidas/efeitos adversos , Coelhos/parasitologia , Óleo de Rícino/químicaRESUMO
Isoxazoline is a 5-membered heterocycle present in the active compounds of many commercial veterinary anti-ectoparasitic products. The molecular target of isoxazolines is the inhibition of GABA-gated chloride channels in insects. These facts have inspired the use of the isoxazoline scaffold in the design of novel insecticide compounds. The main strategies used for isoxazoline synthesis are either the 1,3-dipolar cycloaddition between a nitrile oxide and an alkene or the reaction between hydroxylamine and an α,ß-unsaturated carbonyl compound. This review highlights the utilization of isoxazoline as insecticide: its mode of action, its commercial preparations and its consideration in the design of novel insecticides. Similarity analyses were performed with 235 isoxazoline derivatives in three different cheminformatic approaches - chemical property correlations, similarity network and compound clustering. The cheminformatic methodologies are interesting tools to use in evaluating the similarity between commercial isoxazolines and to clarify the main features explored within their derivatives.
Assuntos
Desenvolvimento de Medicamentos , Insetos/efeitos dos fármacos , Inseticidas/farmacologia , Isoxazóis/farmacologia , Animais , Inseticidas/síntese química , Inseticidas/química , Isoxazóis/síntese química , Isoxazóis/química , Estrutura Molecular , Receptores de GABA/metabolismoRESUMO
A series of novel thiourea and amide liquid crystals containing 5-membered isoxazoline and isoxazole rings were synthetized and the liquid crystal properties studied. Thioureas were obtained using a condensation reaction of benzoyl chlorides, arylamines and ammonium thiocyanate. The amides, on the other hand, were the byproduct of a quantitative reaction which used potassium cyanate as the starting material. Thiourea and amide derivatives were predominantly SmA mesophase inductors. A nematic mesophase was observed only for thioureas and amides containing an isoxazole ring. Additionaly, the liquid crystal behavior was also dependent on the relative position of nitrogen and oxygen atoms on the 5-membered heterocycle.
RESUMO
Lice are ectoparasites capable of affecting birds, and can result in direct and indirect damage to their host. Afoxolaner is an isoxazoline that has been shown to be effective against these ectoparasites without known adverse effects. The objective of this research was to evaluate the effect of afoxolaner on lice in pheasants and plain chachalacas. A total of 29 pheasants of different genera and species (Chrysolophus pictus, C. amherstiae, Lophura swinghoii, L. nycthemera, Phasianus colchicus, and Syrmaticus reevesii) and 18 West Mexican Chachalacas (Ortalis poliocephala) naturally infested with Goniodes pavonis were used. The birds were allocated to one of two groups: group 1 treated with 2.50â¯mg/kg of afoxolaner, and group 2 given no treatment. Ectoparasites were collected using the adhesive tape technique and identified. Afoxolaner was administered later as a single dose to group 1, and the clinical assessment to detect ectoparasites was repeated 28 days post-treatment. On day 28 post-treatment, group 1 was found to be negative for the presence of lice. The body weights were compared at the beginning and end of the clinical assessment in both groups and a significant difference in weight of treated birds was found. The mean body weight decreased by 0.017â¯g in control group, whereas it increased by 0.016â¯g in treated group. Oral administration of afoxolaner is an effective option for the treatment of Goniodes pavonis infestations in zoo birds.
Assuntos
Doenças das Aves/prevenção & controle , Galliformes , Controle de Insetos , Inseticidas , Iscnóceros , Isoxazóis , Infestações por Piolhos/veterinária , Naftalenos , Animais , Doenças das Aves/parasitologia , Infestações por Piolhos/parasitologia , Infestações por Piolhos/prevenção & controleRESUMO
BACKGROUND: The ixodid tick Amblyomma cajennense (sensu lato) complex, widespread throughout South and Central America, is also present in Mexico, Texas and Florida. As a vector of Rickettsia rickettsii, and potentially of other pathogens, infestations with A. cajennense present a substantial health risk to humans, dogs and other mammals. Oral administration of lotilaner flavored chewable tablets (CredelioTM, Elanco) to dogs was previously shown to rapidly provide killing activity of infesting ticks. This study investigated lotilaner's efficacy against A. cajennense (s.l.). METHODS: Twenty purpose-bred Beagles (10 male and 10 female) were ranked by Day -5 burdens of nymphal A. cajennense (s.l.) and randomized to either treatment with lotilaner or to a sham-treated control group. On Day 0, dogs were fed within approximately 30 min prior to oral lotilaner administration at as close as possible to 20 mg/kg, the minimum dose rate. For efficacy assessments, tick counts were completed 48 h post-treatment or 48 h after experimental challenge infestations with 200 nymphal A. cajennense (s.l.) on Days -7, -2, 7, 14, 21 and 28. RESULTS: Tick infestations in the control group dogs ranged from a low of 43 to 95, with the average infestation remaining above 25% at each assessment, thereby meeting the requirement for efficacy comparison with the treated group. Lotilaner efficacy was 100% within 48 h post-treatment, and at nine days post-treatment. Efficacy was greater than 99% at all subsequent assessments through Day 30. No treatment-related adverse events were observed. CONCLUSION: The results demonstrate that lotilaner, administered orally to dogs at a minimum dose of 20 mg/kg is well tolerated, provides rapid reduction of existing A. cajennense (s.l.) tick infestations, and provides sustained residual protection for at least 30 days against subsequent infestation by A. cajennense (s.l.).
Assuntos
Acaricidas/farmacologia , Acaricidas/uso terapêutico , Doenças do Cão/tratamento farmacológico , Ixodidae/efeitos dos fármacos , Controle de Ácaros e Carrapatos/métodos , Infestações por Carrapato/veterinária , Acaricidas/administração & dosagem , Administração Oral , Animais , Doenças do Cão/parasitologia , Cães , Feminino , Masculino , Ninfa/efeitos dos fármacos , Infestações por Carrapato/tratamento farmacológico , Infestações por Carrapato/parasitologia , Resultado do TratamentoRESUMO
O objetivo do presente trabalho foi relatar a eficácia do fluralaner no tratamento da demodicidose juvenil generalizada canina. Dois caninos, apresentando dois e três meses de idade, com diagnóstico clínico e parasitológico de demodicidose generalizada, foram tratados com administração única de fluralaner, na dose recomendada em bula pelo fabricante. Além disso, foi realizada a terapia adjuvante à base de xampu de peróxido de benzoíla e domperidona. Observou-se uma resposta terapêutica satisfatória, com repilação completa ao 30º dia após a administração do fármaco. Para cada paciente, foi realizado exame parasitológico do raspado cutâneo aos 75 e 90 dias seguintes ao início do tratamento, e todos foram negativos. Tendo em vista a elevada eficácia do tratamento proposto, sugere-se a inclusão do fluralaner nos protocolos terapêuticos destinados à demodicidose canina, particularmente nos pacientes pediátricos e com a forma generalizada da doença.(AU)
The aim of the present study was to report the efficiency of fluralaner on the treatment of two cases of canine generalized juvenile demodicosis. Two puppies, aging two and three months old, with the clinic and parasitological diagnosis of generalized demodicosis were treated with single administration of fluralaner. according to the dose recommended by the responsible laboratory. Additionally, adjuvant therapy was applied using benzoyl peroxide shampoo and domperidone. A satisfactory therapeutic response was observed, and complete repilation was present at the 30th day after drug administration. For each patient, at the 75th and 90th day after the treatment began, skin scrapings were performed in order to investigate the presence of Demodex sp; and all were negative. Considering the high efficiency of the treatment used, we suggest the inclusion of fluralaner on the therapeutic protocol for canine demodicosis, particularly in pediatric patients and with the generalized form of the disease.(AU)
Assuntos
Animais , Cães , Antiparasitários/uso terapêutico , Peróxido de Benzoíla/uso terapêutico , Domperidona/uso terapêutico , Dermatopatias Parasitárias/tratamento farmacológico , Dermatopatias Parasitárias/veterináriaRESUMO
O objetivo do presente trabalho foi relatar a eficácia do fluralaner no tratamento da demodicidose juvenil generalizada canina. Dois caninos, apresentando dois e três meses de idade, com diagnóstico clínico e parasitológico de demodicidose generalizada, foram tratados com administração única de fluralaner, na dose recomendada em bula pelo fabricante. Além disso, foi realizada a terapia adjuvante à base de xampu de peróxido de benzoíla e domperidona. Observou-se uma resposta terapêutica satisfatória, com repilação completa ao 30º dia após a administração do fármaco. Para cada paciente, foi realizado exame parasitológico do raspado cutâneo aos 75 e 90 dias seguintes ao início do tratamento, e todos foram negativos. Tendo em vista a elevada eficácia do tratamento proposto, sugere-se a inclusão do fluralaner nos protocolos terapêuticos destinados à demodicidose canina, particularmente nos pacientes pediátricos e com a forma generalizada da doença.(AU)
The aim of the present study was to report the efficiency of fluralaner on the treatment of two cases of canine generalized juvenile demodicosis. Two puppies, aging two and three months old, with the clinic and parasitological diagnosis of generalized demodicosis were treated with single administration of fluralaner. according to the dose recommended by the responsible laboratory. Additionally, adjuvant therapy was applied using benzoyl peroxide shampoo and domperidone. A satisfactory therapeutic response was observed, and complete repilation was present at the 30th day after drug administration. For each patient, at the 75th and 90th day after the treatment began, skin scrapings were performed in order to investigate the presence of Demodex sp; and all were negative. Considering the high efficiency of the treatment used, we suggest the inclusion of fluralaner on the therapeutic protocol for canine demodicosis, particularly in pediatric patients and with the generalized form of the disease.(AU)
Assuntos
Animais , Cães , Antiparasitários/uso terapêutico , Peróxido de Benzoíla/uso terapêutico , Domperidona/uso terapêutico , Dermatopatias Parasitárias/tratamento farmacológico , Dermatopatias Parasitárias/veterináriaRESUMO
BACKGROUND: Amblyomma cajennense is the main vector of Rickettsia rickettsii which causes Brazilian spotted fever. This adult tick preferably infests horses and capybaras, but has low host specificity during its immature stages, thus posing a threat to humans and dogs. In this study, the efficacy of sarolaner (Simparic™/Simparica®, Zoetis) when administered once orally to dogs at 2 mg/kg was evaluated against induced infestations of A. cajennense nymphs for up to 35 days after treatment. METHODS: Based on pretreatment tick counts, 20 dogs were randomly allocated to treatment with sarolaner (Simparic™) dosed at 2 mg/kg of body weight or a placebo on Day 0 of the study. Artificial infestations were performed using laboratory raised A. cajennense nymphs on study days -2, 5, 12, 19, 26 and 33. Efficacy was determined at 48 h post-treatment or post-infestation at each time point relative to the counts for dogs that received placebo. RESULTS: There were no adverse reactions to treatment. A single dose of sarolaner (Simparic™) provided 100% efficacy on study days 2, 7 and 14; and ≥ 99.6% on days 21, 28 and 35. Geometric mean live tick counts for sarolaner were significantly lower than those for placebo on all days (P < 0.0001). CONCLUSIONS: Under the conditions of the present study, sarolaner (Simparic™) administered once orally at 2 mg/kg provided 100% efficacy against existing infestations and ≥ 99.6% efficacy within 48 h against weekly challenges of A. cajennense for at least 35 days after treatment.
Assuntos
Vetores Aracnídeos/efeitos dos fármacos , Azetidinas/uso terapêutico , Doenças do Cão/tratamento farmacológico , Ixodidae/efeitos dos fármacos , Compostos de Espiro/uso terapêutico , Infestações por Carrapato/veterinária , Administração Oral , Animais , Vetores Aracnídeos/fisiologia , Azetidinas/administração & dosagem , Azetidinas/efeitos adversos , Brasil , Doenças do Cão/parasitologia , Cães , Ixodidae/fisiologia , Ninfa/efeitos dos fármacos , Ninfa/fisiologia , Carga Parasitária , Febre Maculosa das Montanhas Rochosas/transmissão , Compostos de Espiro/administração & dosagem , Compostos de Espiro/efeitos adversos , Infestações por Carrapato/tratamento farmacológico , Infestações por Carrapato/parasitologia , Fatores de Tempo , Resultado do TratamentoRESUMO
ABSTRACT The aim of the present study was to report the efficiency of fluralaner on the treatment of two cases of canine generalized juvenile demodicosis. Two puppies, aging two and three months old, with the clinic and parasitological diagnosis of generalized demodicosis were treated with single administration of fluralaner. according to the dose recommended by the responsible laboratory. Additionally, adjuvant therapy was applied using benzoyl peroxide shampoo and domperidone. A satisfactory therapeutic response was observed, and complete repilation was present at the 30th day after drug administration. For each patient, at the 75th and 90th day after the treatment began, skin scrapings were performed in order to investigate the presence of Demodex sp; and all were negative. Considering the high efficiency of the treatment used, we suggest the inclusion of fluralaner on the therapeutic protocol for canine demodicosis, particularly in pediatric patients and with the generalized form of the disease.
RESUMO O objetivo do presente trabalho foi relatar a eficácia do fluralaner no tratamento da demodicidose juvenil generalizada canina. Dois caninos, apresentando dois e três meses de idade, com diagnóstico clínico e parasitológico de demodicidose generalizada, foram tratados com administração única de fluralaner, na dose recomendada em bula pelo fabricante. Além disso, foi realizada a terapia adjuvante à base de xampu de peróxido de benzoíla e domperidona. Observou-se uma resposta terapêutica satisfatória, com repilação completa ao 30º dia após a administração do fármaco. Para cada paciente, foi realizado exame parasitológico do raspado cutâneo aos 75 e 90 dias seguintes ao início do tratamento, e todos foram negativos. Tendo em vista a elevada eficácia do tratamento proposto, sugere-se a inclusão do fluralaner nos protocolos terapêuticos destinados à demodicidose canina, particularmente nos pacientes pediátricos e com a forma generalizada da doença.