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Moxidectin interference on motor activity of rats

RODRIGUES-ALVES, Patrícia de Sá e Benevides; FLÓRIO, Jorge Camilo; LEBRUN, Ivo; BERNARDI, Maria Martha; SPINOSA, Helenice de Souza
Fonte: Tecpar Publicador: Tecpar
Tipo: Artigo de Revista Científica
ENG
Relevância na Pesquisa
37.56%
The present study investigated the effects of t moxidectin (MXD) in some parameters of rat motor function and neurochemical. The general activity in the open field and the motor coordination in the wooden beam were employed to evaluate the MXD effects. The results showed that, in the open field, even at high doses (2.0 and 20.0 mg/kg), the MXD did not alter the locomotion and the rearing frequencies. However, MXD was able to impair the motor coordination of the animals at wooden beam. Neurochemical studies of striatal GABA and dopamine neurotransmitters showed a reduced levels of dopamine and its metabolite, homovanillic acid, without interference on striatal GABA levels. Since GABAergic receptor stimulation had an inhibitory effect on dopaminergic striatal system, the decreased motor coordination could be attributed to an action of MXD on dopamine system via GABA activation.; A moxidectina (MXD) é uma droga antiparasitária amplamente empregada em animais domésticos; seu mecanismo de ação, em mamíferos, envolve o neurotransmissor ácido gama-aminobutírico (GABA). Esse neurotransmissor tem papel importante na função motora. Assim, no presente trabalho estudaram-se os efeitos da MXD em alguns parâmetros comportamentais ligados a função motora de ratos e também em sistemas de neurotransmissão central. A atividade geral no campo aberto e a coordenação motora na trave elevada foram empregadas para avaliar os efeitos de diferentes doses de MXD. Os resultados mostraram que: no campo aberto...

Moxidectin interference on sexual behavior, penile erection and hypothalamic GABA levels of male rats

RODRIGUES-ALVES, Patricia S. B.; LEBRUN, Ivo; FLORIO, Jorge Camilo; BERNARDI, Maria M.; SPINOSA, Helenice de S.
Fonte: ELSEVIER SCI LTD Publicador: ELSEVIER SCI LTD
Tipo: Artigo de Revista Científica
ENG
Relevância na Pesquisa
37.56%
The moxidectin (MXD) is an antiparasitic drug used in domestic animals. The mechanism of action, in mammals, involves GABA, a neurotransmitter with an important role in the sexual behavior control. Presently, the effects of 0.2 mg/kg therapeutic dose were studied on sexual behavior, sexual motivation, penile erection and central GABA levels. Sexual behavior results showed increased latencies to the first mount and intromission as well as in inter-intromission interval; a reduction in total mounts was detected on the drug post-treatment. No difference was observed between sexual motivation of control and experimental animals. MXD treatment reduced penile erection and hypothalamic GABA levels. The results suggest that MXD reduced sexual behavior and penile erection by an action on the hypothalamic GABA system. Probably, the lack of effects in the motivational test and the increased mount and intromission latencies as well as decreased total mounts could be explained as a consequence of reduced male rat erection process. (C) 2007 Elsevier Ltd. All rights reserved.

Avaliação dos efeitos da moxidectina sobre as características reprodutivas de touros; Evaluation of effects of moxidectin on the reproductive characteristics of the bulls

Souza, Norma Lúcia de
Fonte: Biblioteca Digitais de Teses e Dissertações da USP Publicador: Biblioteca Digitais de Teses e Dissertações da USP
Tipo: Tese de Doutorado Formato: application/pdf
Publicado em 11/04/2007 PT
Relevância na Pesquisa
27.75%
Os parasitas nematóides afetam homens e animais, causando graves prejuízos à saúde pública e consideráveis perdas econômicas. A disponibilidade de anti-helmínticos de amplo espectro de ação tem auxiliado na redução de um grande número de perdas em decorrência das infestações parasitárias. Foram objetivos deste trabalho avaliar os efeitos do tratamento com moxidectina, na forma de longa-ação (LA), em sua dose terapêutica em touros, sobre a consistência e perímetro testicular, as características físicas (motilidade e vigor) e morfológicas do sêmen e o comportamento sexual. Foram utilizados 12 touros com idade de 48 ± 10 meses. Os animais foram alocados em 6 blocos com dois tratamentos. Os animais foram divididos nos grupos: controle (n=6), no qual cada animal recebeu 5 mL de solução fisiológica, via subcutânea, na orelha esquerda e grupo tratado (n=6), no qual cada animal recebeu 5 mL de moxidectina a 10% via subcutânea, na orelha esquerda. Os animais foram submetidos a exames andrológicos semanais, por um período de até 60 dias após o tratamento, sendo avaliadas as características testiculares (consistência e perímetro) e características seminais (motilidade, vigor e morfologia). Foram realizados testes de libido a cada 15 dias...

Multiple resistance to anthelmintics by Haemonchus contortus and Trichostrongylus colubriformis in sheep in Brazil

Almeida, F. A.; Garcia, K. C. O. D.; Torgerson, P. R.; Amarante, Alessandro Francisco Talamini do
Fonte: Elsevier B.V. Publicador: Elsevier B.V.
Tipo: Conferência ou Objeto de Conferência Formato: 622-625
ENG
Relevância na Pesquisa
27.89%
The objective of this study was to determine the level of resistance of Haemonchus contortus and Trichostrongylus colubriformis in sheep to levamisole albendazole ivermectin moxidectin closantel and trichlorfon The parasites were isolated from sheep naturally infected by gastrointestinal nematodes and were then kept in monospecifically infected lambs for production of infective larvae (L3) of both species Forty-two lambs at three months of age were simultaneously artificially infected with 4000 L3 of H contortus and 4000 L3 of T colubriformis The animals were allocated Into seven groups with six animals each that received one of the following treatments Group 1-control no treatment Group 2-moxidectin (0 2 mg/kg body weight (BW)) Group 3-closantel (10 mg/kg BW) Group 4-trichlorfon (100 mg/kg BW) Group 5-levamisole phosphate (4 7 mg/kg BW) Group 6-albendazole (5 0 mg/kg BW) and Group 7-ivermectin (0 2 mg/kg BW) Nematode fecal egg counts (FEC) were carried out on the day of treatment and again at 3 7 10 and 14 days post-treatment on the same occasions composite fecal cultures were prepared for each group for production of L3 which were identified into genus The animals were sacrificed for worm counts at 14 days after treatment The efficacy of each treatment was calculated from the arithmetic mean of the FEC or worm burden of the treated group compared with the values of the control group Only trichlorfon and moxidectin treatments resulted in a significant reduction of H contortus recorded at necropsy (73% and 45% respectively) Moxidectin reduced T colubriformis worm burdens by 82% and albendazole by 19% All other anthelmintics resulted in no significant reduction in the numbers of worms found at necropsy In conclusion the Isolates of H contortus and T colubriformis showed multiple resistance to all groups of anthelmintics tested This is the first report based on the controlled efficacy test to show resistance of T colubriformis to macrocyclic lactones in Brazil (C) 2010 Elsevier B.V. All rights reserved

Moxidectin-resistant nematodes in cattle in Brazil

Condi, G. K.; Soutello, R. G. V.; Amarante, Alessandro Francisco Talamini do
Fonte: Elsevier B.V. Publicador: Elsevier B.V.
Tipo: Artigo de Revista Científica Formato: 213-217
ENG
Relevância na Pesquisa
28.06%
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP); The frequent use of anthelmintics in cattle has contributed to the emergence of gastrointestinal nematode populations resistant to the drugs available in the market. This study aimed to evaluate moxidectin efficacy in a property with suspected presence of Oesophagostomum spp. resistant to such anthelmintic. The accuracy of fecal egg count reduction test (FECRT) was also assessed through comparison with the data obtained in the controlled efficacy test (worm burden determination after necropsy). Twenty worm free steers were placed together with cattle of the farm with suspected moxidectin resistance. They became naturally infected with the parasite species present in the farm, and when fecal egg counts (FEC) were higher than 200 eggs/g, the animals were randomly distributed into two groups. One group (n = 10) was treated with moxidectin (0.2 mg/kg; Cyclectin (R), Fort Dodge) and the other was the control group (n = 10). Fecal samples from each steer were collected on the treatment day and three, seven, 10 and 14 days later for FEC and fecal cultures. At 14 days after treatment, all animals were sacrificed and the gastrointestinal nematodes were recovered, identified and counted. Mean FEC reduction in the treated group (compared with control group) was of 88...

Comparative efficacy evaluation of moxidectin gel and ivermectin paste against internal parasites of equines in Brazil

Costa, A. J.; Barbosa, O. F.; Moraes, F. R.; Acuna, A. H.; Rocha, U. F.; Soares, V. E.; Paullilo, A. C.; Sanches, A.
Fonte: Elsevier B.V. Publicador: Elsevier B.V.
Tipo: Artigo de Revista Científica Formato: 29-36
ENG
Relevância na Pesquisa
38.2%
A total of 24 male and female equines of mixed breed, 10-20 months of age and naturally infected with internal parasites was utilized in a controlled test to evaluate the efficacy of a moxidectin 2% gel formulation at the dosage of 0.4 mg moxidectin per kg of live weight and an ivermectin 1.87% commercial paste formulation at the dosage 0.2 mg ivermectin per kg applied orally Animals were allocated into three groups of eight horses each based on pre-treatment eggs per gram (EPG) counts and treatments were randomized among the groups. One group was kept as untreated controls. One animal in the moxidectin-treated group died before the end of the trial from a cause unrelated to treatment leaving a total of seven animals in this group. Fecal egg counts were performed three times post-treatment and the number of parasites remaining in each animal was determined. Statistical analyses using geometric means were performed at the 1% level of significance. Both moxidectin and ivermectin preparations reduced initial EPG from a mean of 1600 to 0 on Days 5, 7 and at the end of the trial on Day 14. Efficacy percentages of moxidectin and ivermectin against immature and adult nematodes were as follows: Trichostrongylus axel, Parascaris equorum, Strongylus edentatus...

Effects of macrocyclic lactones on the reproductive parameters of engorged Rhipicephalus (Boophilus) microplus females detached from experimentally infested cattle

Lopes, Welber Daniel Zanetti; Teixeira, Weslen Fabricio Pires; de Matos, Lucas Vinicius Shigaki; Felippelli, Gustavo; Cruz, Breno Cayeiro; Maciel, Willian Giquelin; Buzzulini, Carolina; Fávero, Flávia Carolina; Soares, Vando Edésio; Oliveira, Gilson Pe
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 72-78
ENG
Relevância na Pesquisa
28.06%
The present study therefore assessed the deleterious effects of MLs (ivermectin, abamectin, doramectin and moxidectin) on the reproductive parameters of engorged Rhipicephalus (Boophilus) microplus females that naturally detached from experimentally infested cattle in two experiments. The following reproductive parameters of engorged female ticks were analyzed: female weight, egg mass weight, percentage of hatchability, percentage of reduction in oviposition, percentage of reduction in hatchability, reproductive efficiency and percent control/efficacy of formulations with respect to reproductive parameters. In the experiment I, statistical analysis of the data grouped into 5-days intervals revealed that pour-on application of abamectin (500. mcg/kg) had significantly (p≤. 0.05) reduced engorged female weight, egg mass weight and percent hatchability on days 6-15, 6-20 and 11-20 post-treatment (p. t.) compared to the respective data for detached and pre-selected engorged females in the control group. The abamectin, demonstrated 33.41% of reduction in oviposition, 6.77% in hatchability and abamectin efficacy was of 13.99%. In the experiment II, statistically significant reductions (p≥. 0.05) were observed in animals treated subcutaneous with ivermectin (630. mcg/kg)...

Assessing resistance of ivermectin and moxidectin against nematodes in cattle naturally infected using three different methodologies

Zanetti Lopes, Welber Daniel; Pires Teixeira, Weslen Fabricio; Felippelli, Gustavo; Cruz, Breno Cayeiro; Maciel, Willian Giquelin; Soares, Vando Edesio; Santos, Thais Rabelo dos; Shigald de Matos, Lucas Vinicius; Favero, Flavia Carolina; Costa, Alvimar Jo
Fonte: Elsevier B.V. Publicador: Elsevier B.V.
Tipo: Artigo de Revista Científica Formato: 133-138
ENG
Relevância na Pesquisa
37.89%
The objective of this study was to evaluate the accuracy of the faecal egg count reduction test (FECRT) and the faecal egg count efficacy test (FECET) to assess the resistance status of ivermectin (630 mu g/g) and moxidectin (200 mu g/kg), using the controlled efficacy test as a reference, and whether the results of the EPG are equivalent to the efficacy results from the parasitological necropsies. Two experiments were conducted. The results demonstrate that it was not possible to demonstrate that the EPG values were equivalent with the ivermectin and moxidectin efficacy obtained by parasitological necropsies, mainly if the phenomenon of parasites resistance is not advanced in a determined field population. Maybe the FECET technique would be possibly better than the FECRT. The high anthelmintic efficacy of 200 mu g/kg moxidectin, in naturally infected cattle, against field population of nematodes that are resistant to 630 mu g/kg ivermectin, was observed in this study. (C) 2013 Elsevier Ltd. All rights reserved.

Moxidectina no soro de cordeiros : perfil farmacocinético e avaliação de seus resíduos em diferentes métodos de controle parasitário; Moxidectin in lamb serum : pharmacokinetic study and its residues in different conditions of parasiticidal control

Rafaela de Carvalho Baptista
Fonte: Biblioteca Digital da Unicamp Publicador: Biblioteca Digital da Unicamp
Tipo: Dissertação de Mestrado Formato: application/pdf
Publicado em 11/04/2013 PT
Relevância na Pesquisa
37.56%
A ovinocultura vem despertando enorme interesse em todas as regiões do Brasil e sua produção destina-se, principalmente, na criação de cordeiros. Contudo, um dos grandes impasses nos sistemas de produção, especialmente em pastagens, são as parasitoses gastrointestinais. Os problemas associados com os parasitas acarretam danos à saúde dos animais, reduzindo o seu desempenho e os lucros do produtor. Como medida profilática, faz-se uso dos anti-parasitários, medicamentos veterinários com ação contra endo e ectoparasitas. Contudo, a utilização indiscriminada dos fármacos tem favorecido o desenvolvimento de estirpes resistentes responsáveis pela rápida ineficácia do composto. Como medida de controle dos nematoides gastrointestinais nas criações comerciais de ovinos, o fármaco costuma ser administrado baseando-se no resultado de duas formas de exame diagnóstico: contagem de ovos dos parasitas nas fezes e o teste FAMACHA® (exame da coloração da mucosa ocular) ou a aplicação do composto em períodos regulares de 28 dias, independente de exame. Na tentativa de determinar a melhor posologia (dose/frequência) do anti-helmíntico a ser empregado na prática, busca-se o melhor entendimento de suas propriedades farmacocinéticas...

Effect of multidrug resistance modulators on the activity of ivermectin and moxidectin against selected strains of Haemonchus contortus infective larvae

Molento,Marcelo B.; Prichard,Roger K.
Fonte: Colégio Brasileiro de Patologia Animal - CBPA; Empresa Brasileira de Pesquisa Agropecuária (EMBRAPA) Publicador: Colégio Brasileiro de Patologia Animal - CBPA; Empresa Brasileira de Pesquisa Agropecuária (EMBRAPA)
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/09/2001 EN
Relevância na Pesquisa
38.11%
Nematode parasites have shown resistance to the anthelmintics, ivermectin and moxidectin, and there is evidence that the over-expression of parasite P-glycoprotein (P-gp) may account, at least in part, for resistance to ivermectin. The objective of this study was to evaluate whether the multidrug resistance (MDR) modulators, verapamil, CL 347.099 (an analog of verapamil) and cyclosporin A, would enhance the efficacy of ivermectin and moxidectin against selected strains of Haemonchus contortus using an in vitro larval migration assay. The modulators had no effects on the number of migrating larvae when used alone. Ivermectin and moxidectin showed a significant (P<0.05) increase in its efficacy by 52.8 and 58.5% respectively, when used in association with verapamil against a moxidectin-selected strain. CL 347,099 also increased significantly (P<0.05) the ivermectin and moxidectin efficacy by 24.2 and 40.0% respectively, against an ivermectin-selected strain and by 40.0 and 75.6% respectively, against an moxidectin-selected strain. At the concentrations tested cyclosporin A showed a variable effect on increasing the efficacy of the anthelmintics against the susceptible and resistant strains.

Evaluation of resistance in a selected field strain of Haemonchus contortus to ivermectin and moxidectin using the Larval Migration on Agar Test

Fortes,Fernanda S.; Kloster,Fernando S.; Schafer,Andressa S.; Bier,Daniele; Buzatti,Andréia; Yoshitani,Ursula Y.; Molento,Marcelo B.
Fonte: Colégio Brasileiro de Patologia Animal - CBPA; Empresa Brasileira de Pesquisa Agropecuária (EMBRAPA) Publicador: Colégio Brasileiro de Patologia Animal - CBPA; Empresa Brasileira de Pesquisa Agropecuária (EMBRAPA)
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/02/2013 EN
Relevância na Pesquisa
37.56%
Haemonchus contortus is one of the most common and economically significant causes of disease in small ruminants worldwide, and the control programs of parasitic nematodes - including H. contortus - rely mostly on the use of anthelmintic drugs. The consequence of the use of this, as the sole sanitary strategy to avoid parasite infections, was the reduction of the efficacy of all chemotherapeutic products with a heavy selection for resistance. The widespread of anthelmintic resistance and the difficulty of its early diagnosis has been a major concern for the sustainable parasite management on farms. The objective of this research was to determine and compare the ivermectin (IVM) and moxidectin (MOX) effect in a selected field strain of H. contortus with a known resistance status, using the in vitro larval migration on agar test (LMAT). Third stage larvae of the selected isolate were obtained from faecal cultures of experimentally infected sheep and incubated in eleven increasing diluted concentrations of IVM and MOX (6, 12, 24, 48, 96, 192, 384, 768, 1536, 3072 and 6144µg/mL). The dose-response sigmoidal curves were obtained using the R² value of >0.90 and the lethal concentration (LC50) dose for the tested anthelmintic drugs using a four-parameter logistic model. The LC50 value for MOX was significantly lower than IVM (1.253µg/mL and 91.06µg/mL)...

Moxidectin interference on motor activity of rats

Rodrigues-Alves,Patrícia de Sá e Benevides; Flório,Jorge Camilo; Lebrun,Ivo; Bernardi,Maria Martha; Spinosa,Helenice de Souza
Fonte: Instituto de Tecnologia do Paraná - Tecpar Publicador: Instituto de Tecnologia do Paraná - Tecpar
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/08/2009 EN
Relevância na Pesquisa
37.56%
The present study investigated the effects of t moxidectin (MXD) in some parameters of rat motor function and neurochemical. The general activity in the open field and the motor coordination in the wooden beam were employed to evaluate the MXD effects. The results showed that, in the open field, even at high doses (2.0 and 20.0 mg/kg), the MXD did not alter the locomotion and the rearing frequencies. However, MXD was able to impair the motor coordination of the animals at wooden beam. Neurochemical studies of striatal GABA and dopamine neurotransmitters showed a reduced levels of dopamine and its metabolite, homovanillic acid, without interference on striatal GABA levels. Since GABAergic receptor stimulation had an inhibitory effect on dopaminergic striatal system, the decreased motor coordination could be attributed to an action of MXD on dopamine system via GABA activation.

Evaluation of a strategic deworming program in dairy heifers in Quebec based on the use of moxidectin, an endectocide with a long persistency.

Elsener, J; Villeneuve, A; DesCôteaux, L
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
Publicado em /01/2001 EN
Relevância na Pesquisa
27.89%
Two different deworming strategies based on the use of moxidectin, a broad spectrum endectocide with persistency against Ostertagia ostertagi, were evaluated in grazing dairy heifers. Eighty-four heifers unexposed to parasitic infection were randomly allocated to 3 different groups: untreated (Group 1), treated at 3 and 10 weeks after turnout with 0.5 mg/kg/body weight (BW) of topical moxidectin (Group 2), or treated at turnout and 10 weeks later with 0.5 mg/kg/BW of topical moxidectin (Group 3). The heifers were turned out on June 6 (Day 0) to a naturally contaminated pasture divided into 3 sections by an electrical fence. Each group of heifers was put on a different section of pasture. The trial ended when they were housed on October 29 (Day 143). The results of this experiment confirmed the beneficial effect of 2 strategic treatments with moxidectin pour-on under field conditions in Quebec. The parasitological parameters showed a statistical difference in terms of mean fecal egg counts between treated and control groups (ANOVA, P < or = 0.006). After turnout, pasture larval counts were consistently higher for Group 1 compared with counts for Group 2 or 3. All heifer groups gained weight during the trial period, but the weight gain profile of both treated groups was significantly higher than that of the untreated controls (ANOVA...

The persistence of benzimidazole-resistant cyathostomes on horse farms in Ontario over 10 years and the effectiveness of ivermectin and moxidectin against these resistant strains

Slocombe, J. Owen D.; Coté, John F.; de Gannes, Rolph V.G.
Fonte: Canadian Veterinary Medical Association Publicador: Canadian Veterinary Medical Association
Tipo: Artigo de Revista Científica
Publicado em /01/2008 EN
Relevância na Pesquisa
27.75%
Three clinical trials with fecal egg count reduction tests and coproculture were conducted on 2 standardbred farms in Ontario. On Farm A, the treatment groups were mebendazole and ivermectin in trial 1, and fenbendazole and moxidectin in another. On Farm B, treatment groups were mebendazole and ivermectin. All horses treated with mebendazole or fenbendazole were subsequently treated with ivermectin or moxidectin. Strongyle eggs/g feces were estimated pre- and post-treatment using the Cornell-McMaster dilution and Cornell-Wisconsin centrifugal flotation techniques. After treatment, there was no change in the arithmetic mean eggs/g feces for horses given mebendazole, and a reduction of only 49.1% for those given fenbendazole. All horses receiving ivermectin or moxidectin had their egg counts reduced to 0. Only cyathostomes were found on culture. On both farms the benzimidazole resistant strains appeared to have persisted for at least 10 years. Development of and monitoring for anthelmintic resistance are briefly discussed.

Use of Selamectin and Moxidectin in the Treatment of Mouse Fur Mites

Mook, Deborah M; Benjamin, Kimberly A
Fonte: American Association for Laboratory Animal Science Publicador: American Association for Laboratory Animal Science
Tipo: Artigo de Revista Científica
EN
Relevância na Pesquisa
27.75%
A breeding colony consisting of 250 different strains of mice was treated with the topical acaricide selamectin for the mouse fur mite Myocoptes musculinus, with no apparent ill effect, suggesting that this drug is safe for use in mice. To further evaluate their efficacy in treating Myocoptes spp., we compared selamectin with another acaricide, moxidectin, in a controlled manner. Infested mice were treated with selamectin or moxidectin at the time of cage change, and a subset of mice was retreated 10 d later. Mice underwent routine cellophane tape examination of the pelage for 1 y. Although no adult mites were found in any group at 1 mo after treatment, egg casings were found in the selamectin treatment group as late as 6 mo after treatment, prompting concern about its effectiveness. Moxidectin used in combination with cage changing was effective in eradicating mites, with mice negative for traces of mites on cellophane tape examination of the pelage from months 2 through 12 after treatment.

Moxidectin Toxicity in Senescence-Accelerated Prone and Resistant Mice

Lee, Vanessa K; Tiwary, Asheesh K; Sharma-Reddy, Prachi; Lieber, Karen A; Taylor, Douglas K; Mook, Deborah M
Fonte: American Association for Laboratory Animal Science Publicador: American Association for Laboratory Animal Science
Tipo: Artigo de Revista Científica
EN
Relevância na Pesquisa
28.11%
Moxidectin has been used safely as an antiparasitic in many animal species, including for the eradication of the mouse fur mite, Mycoptes musculinus. Although no side effects of moxidectin have previously been reported to occur in mice, 2 strains of the senescence-accelerated mouse (SAMP8 and SAMR1) sustained considerable mortality after routine prophylactic treatment. To investigate the mechanism underlying this effect, moxidectin toxicosis in these mice was evaluated in a controlled study. Moxidectin was applied topically (0.015 mg), and drug concentrations in both brain and serum were analyzed by using HPLC coupled with mass spectrometry. The moxidectin concentration in brain of SAMP8 mice was 18 times that in controls, and that in brain of SAMR1 mice was 14 times higher than in controls, whereas serum moxidectin concentrations did not differ significantly among the 3 strains. Because deficiency of the blood–brain barrier protein P-glycoprotein leads to sensitivity to this class of drugs in other SAM mice, Pgp immunohistochemistry of brain sections from a subset of mice was performed to determine whether this commercially available analysis could predict sensitivity to this class of drug. The staining analysis showed no difference among the strains of mice...

Comparative tissue pharmacokinetics and efficacy of moxidectin, abamectin and ivermectin in lambs infected with resistant nematodes: Impact of drug treatments on parasite P-glycoprotein expression☆

Lloberas, Mercedes; Alvarez, Luis; Entrocasso, Carlos; Virkel, Guillermo; Ballent, Mariana; Mate, Laura; Lanusse, Carlos; Lifschitz, Adrian
Fonte: Elsevier Publicador: Elsevier
Tipo: Artigo de Revista Científica
Publicado em 03/12/2012 EN
Relevância na Pesquisa
27.89%
The high level of resistance to the macrocyclic lactones has encouraged the search for strategies to optimize their potential as antiparasitic agents. There is a need for pharmaco-parasitological studies addressing the kinetic-dynamic differences between various macrocyclic lactones under standardized in vivo conditions. The current work evaluated the relationship among systemic drug exposure, target tissue availabilities and the pattern of drug accumulation within resistant Haemonchus contortus for moxidectin, abamectin and ivermectin. Drug concentrations in plasma, target tissues and parasites were measured by high performance liquid chromatography. Additionally, the efficacy of the three molecules was evaluated in lambs infected with resistant nematodes by classical parasitological methods. Furthermore, the comparative determination of the level of expression of P-glycoprotein (P-gp2) in H. contortus recovered from lambs treated with each drug was performed by real time PCR. A longer persistence of moxidectin (P < 0.05) concentrations in plasma was observed. The concentrations of the three compounds in the mucosal tissue and digestive contents were significant higher than those measured in plasma. Drug concentrations were in a range between 452 ng/g (0.5 day post-treatment) and 32 ng/g (2 days post-treatment) in the gastrointestinal (GI) contents (abomasal and intestinal). Concentrations of the three compounds in H. contortus were in a similar range to those observed in the abomasal contents (positive correlation P = 0.0002). Lower moxidectin concentrations were recovered within adult H. contortus compared to abamectin and ivermectin at day 2 post-treatment. However...

A Randomized, Single-Ascending-Dose, Ivermectin-Controlled, Double-Blind Study of Moxidectin in Onchocerca volvulus Infection

Awadzi, Kwablah; Opoku, Nicholas O.; Attah, Simon K.; Lazdins-Helds, Janis; Kuesel, Annette C.
Fonte: Public Library of Science Publicador: Public Library of Science
Tipo: Artigo de Revista Científica
Publicado em 26/06/2014 EN
Relevância na Pesquisa
27.89%
Around 100 million Africans live in onchocerciasis endemic areas. Control of onchocerciasis as a public health problem and possibly even elimination of onchocerciasis infection relies on annual community-directed mass treatment with ivermectin. Given concerns about possible emergence of ivermectin resistance of the parasite Onchocerca volvulus and elimination of infection in areas where very high numbers of vectors can result in continued parasite transmission even when only few parasites are present in only a few people, research for drugs with higher effect on the parasite remains important. A series of non-clinical and clinical studies was planned to find out whether moxidectin, a veterinary anthelminthic, is sufficiently safe for mass treatment and has a better effect on the parasite than ivermectin. We report here results from the first study in infected people conducted to assess in small numbers of individuals the adverse reactions to the killing of parasites by moxidectin. A single dose of 8 mg moxidectin reduced skin parasite numbers better and for a longer time than ivermectin. The frequency and severity of adverse reactions was so low that a larger study to better characterize the adverse reactions to moxidectin and compare its efficacy with that of ivermectin was initiated.

Pharmacokinetics of moxidectin in the Southern hairy-nosed wombat (Lasiorhinus latifrons)

Death, C.; Taggart, D.; Williams, D.; Milne, R.; Schultz, D.; Holyoake, C.; Warren, K.
Fonte: Wildlife Disease Assn Inc Publicador: Wildlife Disease Assn Inc
Tipo: Artigo de Revista Científica
Publicado em //2011 EN
Relevância na Pesquisa
37.98%
Sarcoptic mange, caused by Sarcoptes scabiei var. wombati, could be a significant threat to populations of southern hairy-nosed wombats (Lasiorhinus latifrons; SHNW) in Australia. Treatment is currently based on the off-label use of various parasiticidal drugs, with limited clinical efficacy trials. Our primary aim was to determine the pharmacokinetic parameters of a macrocyclic lactone, moxidectin, to assist in the development of effective treatment protocols. Pharmacokinetic parameters were determined in four female SHNW following a single subcutaneous injection of 0.2 mg/kg moxidectin. Blood samples were collected for 38 days following injection (August–September 2008), for analysis using liquid chromatography and tandem mass spectrometry. The mean peak plasma concentration occurred at 13.6 hr, with a mean peak plasma level of 98.6 ng/ml. The mean elimination half-life was 5.03 days, resulting in a mean area under the curve of 377 ng.day/ml. The peak plasma moxidectin concentration was higher than that seen in livestock species but the plasma elimination half-life was shorter. This study suggests that a single injection of 0.2 mg/kg moxidectin may not be sufficient to clear a mange infection in this species.; Clare E. Death, David A. Taggart...

Efeitos da moxidectina no comportamento sexual de ratos machos; Effects of moxidectin on male rats' sexual behavior

Rodrigues Alves, Patricia de Sá e Benevides
Fonte: Biblioteca Digitais de Teses e Dissertações da USP Publicador: Biblioteca Digitais de Teses e Dissertações da USP
Tipo: Dissertação de Mestrado Formato: application/pdf
Publicado em 17/03/2003 PT
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A moxidectina é uma droga antiparasitária, do grupo das milbemicinas, utilizada em animais domésticos. Em mamíferos seu mecanismo de ação envolve o GABA, neurotansmissor que tem um papel relevante na regulação do comportamento sexual. Assim, o presente trabalho estudou os efeitos da moxidectina no comportamento sexual de ratos machos. Uma vez que alterações na função motora podem interferir na manifestação deste comportamento, avaliou-se, inicialmente, a atividade geral no campo aberto e a coordenação motora na trave elevada, e posteriormente, o comportamento sexual de ratos inexperientes e experientes. A avaliação da atividade geral dos ratos observados no campo aberto mostrou que, mesmo em altas doses (2,0 e 20,0mg/kg), a moxidectina não altera o comportamento de ratos no campo aberto. Esta droga, porém, prejudicou a coordenação motora dos animais avaliados na trave elevada, sendo este efeito atribuído, ao menos em parte, à ação da moxidectina em receptores GABAérgicos. Os resultados obtidos na avaliação do comportamento sexual de ratos inexperientes mostraram redução da motivação sexual dos animais que receberam 0,2mg/kg de moxidectina e foram observados 24 ou 72horas depois. Nenhuma alteração significante foi observada nos diferentes parâmetros do comportamento sexual dos ratos experientes...