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[PMID]:28632749
[Au] Autor:Weaver KJ; May CJ; Ellis BL
[Ad] Endereço:Department of Biology and Chemistry, Bethel College, Mishawaka, Indiana, United States of America.
[Ti] Título:Using a health-rating system to evaluate the usefulness of Caenorhabditis elegans as a model for anthelmintic study.
[So] Source:PLoS One;12(6):e0179376, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Soil-transmitted helminths (STHs) are intestinal parasitic nematodes that infect humans, and are transmitted through contaminated soil. These nematodes include the large roundworm (Ascaris lumbricoides), whipworm (Trichuris trichiura), and hookworm (Ancylostoma ceylanicum, Ancylostoma duodenale, and Necator americanus). Nearly 1.5 billion people (~24% of the population) worldwide are infected with at least one species of these parasites, burdening the poor, in particular, children and pregnant women. To combat these diseases, the WHO only recognizes four anthelmintic drugs, including the preferred drug, albendazole, for mass drug administration (MDA). These four drugs have a total of two different mechanisms of action, and, as expected, resistance has been observed. This problem calls for new drugs with different mechanisms of action. Although there is precedence for the use of Caenorhabditis elegans (C. elegans), a free-living nematode, as a model for drug screening and anthelmintic testing, their usefulness for such anthelmintic study is not clear as past research has shown that C. elegans did not show a strong response to albendazole, the MDA drug of choice, in comparison with various STHs under similar treatment. To further examine if C. elegans has the potential to be a good model organism for anthelmintic drug study, we employed a health rating scale in order to tease out potential effects of albendazole, and other anthelmintics, that may have been missed using a binary, dead/alive scale. Using the health-rating scale we found that although the worms may have not been dying, they were sick, showing dose responses to anthelmintic drugs, including albendazole, reinforcing C. elegans as a useful model for anthelmintic study.
[Mh] Termos MeSH primário: Anti-Helmínticos/farmacologia
Caenorhabditis elegans/efeitos dos fármacos
[Mh] Termos MeSH secundário: Albendazol/farmacologia
Albendazol/uso terapêutico
Animais
Anti-Helmínticos/uso terapêutico
Helmintíase/tratamento farmacológico
Seres Humanos
Concentração Inibidora 50
Ivermectina/farmacologia
Ivermectina/uso terapêutico
Dose Letal Mediana
Testes de Sensibilidade Parasitária
Pirantel/farmacologia
Pirantel/uso terapêutico
Tiazóis/farmacologia
Tiazóis/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anthelmintics); 0 (Thiazoles); 4QIH0N49E7 (Pyrantel); 70288-86-7 (Ivermectin); F4216019LN (Albendazole); SOA12P041N (nitazoxanide)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170919
[Lr] Data última revisão:
170919
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170621
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0179376


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[PMID]:26751958
[Au] Autor:Abongwa M; Buxton SK; Robertson AP; Martin RJ
[Ad] Endereço:Department of Biomedical Sciences, College of Veterinary Medicine, Iowa State University, Ames, Iowa, United States of America.
[Ti] Título:Curiouser and Curiouser: The Macrocyclic Lactone, Abamectin, Is also a Potent Inhibitor of Pyrantel/Tribendimidine Nicotinic Acetylcholine Receptors of Gastro-Intestinal Worms.
[So] Source:PLoS One;11(1):e0146854, 2016.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Nematode parasites may be controlled with drugs, but their regular application has given rise to concerns about the development of resistance. Drug combinations may be more effective than single drugs and delay the onset of resistance. A combination of the nicotinic antagonist, derquantel, and the macrocyclic lactone, abamectin, has been found to have synergistic anthelmintic effects against gastro-intestinal nematode parasites. We have observed in previous contraction and electrophysiological experiments that derquantel is a potent selective antagonist of nematode parasite muscle nicotinic receptors; and that abamectin is an inhibitor of the same nicotinic receptors. To explore these inhibitory effects further, we expressed muscle nicotinic receptors of the nodular worm, Oesophagostomum dentatum (Ode-UNC-29:Ode-UNC-63:Ode-UNC-38), in Xenopus oocytes under voltage-clamp and tested effects of abamectin on pyrantel and acetylcholine responses. The receptors were antagonized by 0.03 µM abamectin in a non-competitive manner (reduced Rmax, no change in EC50). This antagonism increased when abamectin was increased to 0.1 µM. However, when we increased the concentration of abamectin further to 0.3 µM, 1 µM or 10 µM, we found that the antagonism decreased and was less than with 0.1 µM abamectin. The bi-phasic effects of abamectin suggest that abamectin acts at two allosteric sites: one high affinity negative allosteric (NAM) site causing antagonism, and another lower affinity positive allosteric (PAM) site causing a reduction in antagonism. We also tested the effects of 0.1 µM derquantel alone and in combination with 0.3 µM abamectin. We found that derquantel on these receptors, like abamectin, acted as a non-competitive antagonist, and that the combination of derquantel and abamectin produced greater inhibition. These observations confirm the antagonistic effects of abamectin on nematode nicotinic receptors in addition to GluCl effects, and illustrate more complex effects of macrocyclic lactones that may be exploited in combinations with other anthelmintics.
[Mh] Termos MeSH primário: Indóis/administração & dosagem
Ivermectina/análogos & derivados
Nematoides/efeitos dos fármacos
Oxepinas/administração & dosagem
Fenilenodiaminas/antagonistas & inibidores
Pirantel/antagonistas & inibidores
Receptores Nicotínicos/efeitos dos fármacos
[Mh] Termos MeSH secundário: Acetilcolina/química
Sítio Alostérico
Animais
Anti-Helmínticos/administração & dosagem
Clonagem Molecular
Relação Dose-Resposta a Droga
Trato Gastrointestinal/parasitologia
Regulação da Expressão Gênica
Haemonchus/metabolismo
Helmintíase/tratamento farmacológico
Enteropatias Parasitárias/tratamento farmacológico
Ivermectina/administração & dosagem
Antagonistas Nicotínicos/administração & dosagem
Oócitos/citologia
Oócitos/parasitologia
Técnicas de Patch-Clamp
Xenopus laevis
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anthelmintics); 0 (Indoles); 0 (Nicotinic Antagonists); 0 (Oxepins); 0 (Phenylenediamines); 0 (Receptors, Nicotinic); 0L0UGK6OOX (derquantel); 115103-15-6 (tribendimidine); 4QIH0N49E7 (Pyrantel); 5U8924T11H (abamectin); 70288-86-7 (Ivermectin); N9YNS0M02X (Acetylcholine)
[Em] Mês de entrada:1607
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160112
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0146854


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[PMID]:26187649
[Au] Autor:Mostafa E; Storey B; Farghaly AM; Afify HA; Taha AA; Wolstenholme AJ
[Ad] Endereço:Department of Infectious Diseases, University of Georgia, 501 D.W. Brooks Drive, Athens, GA, 30602, USA.
[Ti] Título:Transient effects of levamisole on Brugia malayi microfilariae.
[So] Source:Invert Neurosci;15(3):5, 2015 Sep.
[Is] ISSN:1439-1104
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Levamisole is an anthelmintic drug that acts by activating nicotinic acetylcholine receptors at the nematode neuromuscular junction and causing paralysis. We measured the in vitro effects of levamisole on the motility of Brugia malayi microfilariae; after 2 h incubation the apparent IC50 was 2.68 mM. Lower drug concentrations, such as 1 mM, caused an immediate total paralysis that lasted for up to 1 h, but was completely reversed by 2 h of incubation. The 'recovered' parasites were still completely susceptible to application of a second nicotinic agonist, pyrantel.
[Mh] Termos MeSH primário: Antinematódeos/farmacologia
Brugia Malayi/efeitos dos fármacos
Levamisol/farmacologia
Microfilárias/efeitos dos fármacos
Paralisia/induzido quimicamente
[Mh] Termos MeSH secundário: Animais
Relação Dose-Resposta a Droga
Pirantel/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antinematodal Agents); 2880D3468G (Levamisole); 4QIH0N49E7 (Pyrantel)
[Em] Mês de entrada:1603
[Cu] Atualização por classe:171013
[Lr] Data última revisão:
171013
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150719
[St] Status:MEDLINE
[do] DOI:10.1007/s10158-015-0181-0


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[PMID]:25983232
[Au] Autor:Sarai RS; Kopp SR; Knox MR; Coleman GT; Kotze AC
[Ad] Endereço:CSIRO Agriculture Flagship, 306 Carmody Rd, St Lucia, Brisbane, QLD 4067, Australia; School of Veterinary Science, University of Queensland, Gatton, QLD 4341, Australia.
[Ti] Título:In vitro levamisole selection pressure on larval stages of Haemonchus contortus over nine generations gives rise to drug resistance and target site gene expression changes specific to the early larval stages only.
[So] Source:Vet Parasitol;211(1-2):45-53, 2015 Jun 30.
[Is] ISSN:1873-2550
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:There is some evidence that resistance to levamisole and pyrantel in trichostrongylid nematodes is due to changes in the composition of nicotinic acetylcholine receptors (nAChRs) which represent the drug target site. Altered expression patterns of genes coding for nAChR subunits, as well as the presence of truncated versions of several subunits, have been implicated in observed resistances. The studies have mostly compared target sites in worm isolates of very different genetic background, and hence the ability to associate the molecular changes with drug sensitivity alone have been clouded to some extent. The present study aimed to circumvent this issue by following target site gene expression pattern changes as resistance developed in Haemonchus contortus worms under laboratory selection pressure with levamisole. We applied drug selection pressure to early stage larvae in vitro over nine generations, and monitored changes in larval and adult drug sensitivities and target site gene expression patterns. High level resistance developed in larvae, with resistance factors of 94-fold and 1350-fold at the IC50 and IC95, respectively, in larval development assays after nine generations of selection. There was some cross-resistance to bephenium (70-fold increase in IC95). The expression of all the putative subunit components of levamisole-sensitive nAChRs, as well as a number of ancillary protein genes, particularly Hco-unc-29.1 and -ric-3, were significantly decreased (up to 5.5-fold) in the resistant larvae at generation nine compared to the starting population. However, adult worms did not show any resistance to levamisole, and showed an inverse pattern of gene expression changes, with many target site genes showing increased expression compared to the starting population. A comparison of the larval/adult drug sensitivity data with the known relationships for field-derived isolates indicated that the adults of our selected population should have been highly resistant to the drug if the larval/adult sensitivity relationships were in accordance with previous field isolates. Hence, our selected worms showed a life-stage drug sensitivity pattern quite different to that seen in the field. The present study has highlighted an association between drug target site changes and resistance to levamisole in H. contortus larvae. However, it has also highlighted the artificial nature of the larval selection method with levamisole, as the resistance phenotype and the associated molecular changes were only observed in the drug-pressured life stage. The study therefore reinforces the need for caution in extrapolating larval-based laboratory selection outcomes to field resistances.
[Mh] Termos MeSH primário: Antinematódeos/farmacologia
Hemoncose/parasitologia
Haemonchus/efeitos dos fármacos
Larva/efeitos dos fármacos
Levamisol/farmacologia
Doenças dos Ovinos/parasitologia
[Mh] Termos MeSH secundário: Animais
Resistência a Medicamentos
Feminino
Regulação da Expressão Gênica/efeitos dos fármacos
Haemonchus/genética
Proteínas de Helminto/genética
Masculino
Pirantel/farmacologia
Ovinos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antinematodal Agents); 0 (Helminth Proteins); 2880D3468G (Levamisole); 4QIH0N49E7 (Pyrantel)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170413
[Lr] Data última revisão:
170413
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150519
[St] Status:MEDLINE


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[PMID]:25576440
[Au] Autor:Lawson E; Burden F; Elsheikha HM
[Ad] Endereço:School of Veterinary Medicine and Science, University of Nottingham, Sutton Bonington Campus, Leicestershire LE12 5RD, UK.
[Ti] Título:Pyrantel resistance in two herds of donkey in the UK.
[So] Source:Vet Parasitol;207(3-4):346-9, 2015 Jan 30.
[Is] ISSN:1873-2550
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Resistance to currently available anthelmintics is a serious phenomenon which is prevalent globally. Cyathostomins are one of the major parasites, and are of primary concern in donkeys. There have been reports of emerging resistance to pyrantel, but the status of pyrantel resistance in donkey populations in the UK is largely unknown. This report investigates pyrantel resistance in two geographically isolated donkey herds in the South West of England. The first herd had suspected pyrantel resistance, with already established resistance to other anthelmintics. In the second herd the efficacy of pyrantel was not suspected at the time the study took place. Faecal Egg Count Reduction Test (FECRT) was carried out, revealing large scale resistance. Eighty one percent of the first herd and 73% of the second herd had a FEC of less than 95% after treatment, and anthelmintic resistance was confirmed using the World Association for the Advancement of Veterinary Parasitology guidelines. These findings indicate that anthelmintic resistance to pyrantel exists in both tested donkey populations and illustrate the continuing development of resistance through different classes of chemotherapeutics.
[Mh] Termos MeSH primário: Anti-Helmínticos/farmacologia
Resistência a Medicamentos
Equidae/parasitologia
Pirantel/farmacologia
Infecções por Strongylida/veterinária
Strongyloidea/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Anti-Helmínticos/uso terapêutico
Inglaterra
Contagem de Ovos de Parasitas
Pirantel/uso terapêutico
Infecções por Strongylida/tratamento farmacológico
Infecções por Strongylida/parasitologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anthelmintics); 4QIH0N49E7 (Pyrantel)
[Em] Mês de entrada:1506
[Cu] Atualização por classe:150119
[Lr] Data última revisão:
150119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150111
[St] Status:MEDLINE


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[PMID]:25007041
[Au] Autor:Lassen B; Peltola SM
[Ad] Endereço:Estonian University of Life Sciences, Institute of Veterinary Medicine and Animal Sciences,Kreutzwaldi 62,51014Tartu,Estonia.
[Ti] Título:Anthelmintic resistance of intestinal nematodes to ivermectin and pyrantel in Estonian horses.
[So] Source:J Helminthol;89(6):760-3, 2015 Nov.
[Is] ISSN:1475-2697
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:There is evidence of resistance in horses to anthelmintic treatment using ivermectin and pyrantel. However, little information is available about the parasites, treatment practices or anthelmintic resistance in the horse population in Estonia. In the present study, we examined 41 trotting and riding horses aged < 3 years from four stables in Estonia. Faecal samples were collected, and horses were selected for treatment if the nematode egg count per gram faeces exceeded 200. Horses (n= 32) that shed strongyle-type eggs were treated with pyrantel, whereas Parascaris equorum-positive animals received ivermectin. Up to 78% of horses required anthelmintic treatment and the efficiency of the anthelmintics was evaluated using a faecal egg count reduction test. Resistance of P. equorum was observed in 50% of horses treated with ivermectin and of strongyles in 27% of horses treated with pyrantel. Ivermectin treatment resulted in a mean reduction of 100% for strongyle eggs and an 89% reduction in P. equorum, and pyrantel-treated horses exhibited an 88% reduction in strongyle eggs. These results are considered to be the first indication of resistance to pyrantel, but further studies of ivermectin resistance are required. According to questionnaires completed by the owners of horses, resistance might be explained by a lack of evidence-based strategies, a strong preference for using ivermectin and possibly a subjective evaluation of the body weight of horses.
[Mh] Termos MeSH primário: Anti-Helmínticos/farmacologia
Infecções por Ascaridida/veterinária
Ascaridoidea/efeitos dos fármacos
Resistência a Medicamentos
Doenças dos Cavalos/parasitologia
Intestinos/parasitologia
Ivermectina/farmacologia
Pirantel/farmacologia
[Mh] Termos MeSH secundário: Animais
Infecções por Ascaridida/tratamento farmacológico
Infecções por Ascaridida/parasitologia
Ascaridoidea/fisiologia
Estônia
Feminino
Doenças dos Cavalos/tratamento farmacológico
Cavalos
Masculino
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anthelmintics); 4QIH0N49E7 (Pyrantel); 70288-86-7 (Ivermectin)
[Em] Mês de entrada:1604
[Cu] Atualização por classe:151007
[Lr] Data última revisão:
151007
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140710
[St] Status:MEDLINE
[do] DOI:10.1017/S0022149X14000510


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[PMID]:25387542
[Au] Autor:Schneider S; Pfister K; Becher AM; Scheuerle MC
[Ad] Endereço:Comparative Tropical Medicine and Parasitology, Faculty of Veterinary Medicine, Ludwig-Maximilians-Universität, Leopoldstr. 5, D-80802, Munich, Germany. Stephanie_Schneider82@yahoo.de.
[Ti] Título:Strongyle infections and parasitic control strategies in German horses - a risk assessment.
[So] Source:BMC Vet Res;10:262, 2014 Nov 12.
[Is] ISSN:1746-6148
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: As a consequence of the increasing levels of anthelmintic resistance in cyathostomes, new strategies for equine parasite control are being implemented. To assess the potential risks of these, the occurrence of strongyles was evaluated in a group of 1887 horses. The distribution of fecal egg counts (FECs), the frequency of anthelmintic drug use, and the deworming intervals were also analyzed. Between June 2012 and May 2013, 1887 fecal samples from either selectively or strategically dewormed horses were collected at 195 horse farms all over Germany and analyzed quantitatively with a modified McMaster technique. All samples with FEC ≥20 eggs per gram (EPG) were subjected to coproculture to generate third-stage larvae (LIII) for species differentiation. RESULTS: Egg counts were below the limit of detection (20 EPG) in 1046 (55.4%) samples and above it in 841 (44.6%) samples. Strongylus vulgaris larvae were identified in two of the 841 positive samples. Infections with cyathostomes were found on every farm. The most frequently applied anthelmintic was ivermectin (788/50.8%), followed by pyrantel (336/21.6%). The mean time since last treatment was 6.3 months. High-egg-shedding (>500 EPG) strategically dewormed horses (183/1357) were treated, on average, three times/year. The planned treatment date was already exceeded by 72.5% of the high egg-shedders and by 58.1% of the moderate (200-500 EPG) and low egg-shedders (20-199 EPG). CONCLUSIONS: S. vulgaris seems to be rare in Germany and no difference in its frequency has yet been found between selectively treated horses and horses receiving treatment in strategic intervals. However, inconsistent parasite control has been observed. Therefore, to minimize the risks for disease, consistent and efficient parasite control should be implemented.
[Mh] Termos MeSH primário: Infecções Equinas por Strongyloidea/prevenção & controle
[Mh] Termos MeSH secundário: Animais
Anti-Helmínticos/administração & dosagem
Anti-Helmínticos/uso terapêutico
Esquema de Medicação/veterinária
Fezes/parasitologia
Alemanha/epidemiologia
Cavalos/parasitologia
Ivermectina/administração & dosagem
Ivermectina/uso terapêutico
Contagem de Ovos de Parasitas/veterinária
Pirantel/administração & dosagem
Pirantel/uso terapêutico
Medição de Risco
Infecções Equinas por Strongyloidea/epidemiologia
Strongylus/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anthelmintics); 4QIH0N49E7 (Pyrantel); 70288-86-7 (Ivermectin)
[Em] Mês de entrada:1604
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141113
[St] Status:MEDLINE
[do] DOI:10.1186/s12917-014-0262-z


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[PMID]:25224788
[Au] Autor:Armstrong SK; Woodgate RG; Gough S; Heller J; Sangster NC; Hughes KJ
[Ad] Endereço:School of Animal & Veterinary Sciences, Charles Sturt University, Locked Bag 588, Wagga Wagga, New South Wales 2678, Australia.
[Ti] Título:The efficacy of ivermectin, pyrantel and fenbendazole against Parascaris equorum infection in foals on farms in Australia.
[So] Source:Vet Parasitol;205(3-4):575-80, 2014 Oct 15.
[Is] ISSN:1873-2550
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:This study was performed to estimate the prevalence of patent Parascaris equorum infections and determine the efficacy of ivermectin, pyrantel and fenbendazole against P. equorum infection in foals on farms in southern Australia. Foals aged >3 months on five farms in the south-western slopes region of New South Wales were used. Faeces were collected from each foal and foals with a P. equorum faecal egg count (FEC) of >100 eggs per gram (EPG) were used to measure anthelmintic efficacy using the FEC reduction (FECR) test, after random allocation to a control group or an ivermectin, pyrantel embonate or fenbendazole treatment group. Treatment was administered on day 0 and faeces were collected on day 14 and a FEC was performed. For determination of anthelmintic efficacy, FECRs and lower 95% confidence intervals (LCL) were calculated using previously described methods, based on individual or group FECRs. P. equorum populations were considered susceptible when FECR was >90% and LCL >90%, suspected resistant when FECR was FECR was 80-90% and LCL <90% and resistant when FECR was <80% and LCL <90%. A Poisson distribution quality control method was applied to the data to remove suspected erroneous FECR results. Prevalence of patent P. equorum infection was 58.3% (147/252 foals) and 89 foals on 5 farms were included in the FECR study. Resistance of P. equorum to ≥ 1 anthelmintic was present on all five farms prior to and on four farms after application of the quality control method. Two farms had evidence of multiple drug resistance. Ivermectin was effective and ineffective on two and three farms, respectively. Fenbendazole was effective on two farms, equivocal on one farm and ineffective on one farm. Pyrantel embonate was effective on three farms and ineffective on one farm. These data indicate that anthelmintic-resistant P. equorum populations are present on farms in Australia and multiple drug resistance may occur on individual farms.
[Mh] Termos MeSH primário: Anti-Helmínticos/uso terapêutico
Infecções por Ascaridida/veterinária
Ascaridoidea/efeitos dos fármacos
Doenças dos Cavalos/tratamento farmacológico
[Mh] Termos MeSH secundário: Criação de Animais Domésticos
Animais
Infecções por Ascaridida/tratamento farmacológico
Infecções por Ascaridida/epidemiologia
Ascaridoidea/isolamento & purificação
Resistência a Múltiplos Medicamentos
Fezes/parasitologia
Feminino
Fenbendazol/uso terapêutico
Doenças dos Cavalos/epidemiologia
Doenças dos Cavalos/parasitologia
Cavalos
Ivermectina/uso terapêutico
New South Wales/epidemiologia
Contagem de Ovos de Parasitas/veterinária
Prevalência
Pirantel/uso terapêutico
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anthelmintics); 4QIH0N49E7 (Pyrantel); 621BVT9M36 (Fenbendazole); 70288-86-7 (Ivermectin)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170302
[Lr] Data última revisão:
170302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140917
[St] Status:MEDLINE


  9 / 326 MEDLINE  
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[PMID]:25080682
[Ti] Título:Drug may guard against periodontitis.
[So] Source:J Calif Dent Assoc;42(1):14, 2014 Jan.
[Is] ISSN:1043-2256
[Cp] País de publicação:United States
[La] Idioma:eng
[Mh] Termos MeSH primário: Biofilmes/efeitos dos fármacos
Periodontite/prevenção & controle
Pirantel/análogos & derivados
[Mh] Termos MeSH secundário: Animais
Antinematódeos/uso terapêutico
Periodontite/microbiologia
Pirantel/uso terapêutico
Succinato Desidrogenase/antagonistas & inibidores
[Pt] Tipo de publicação:NEWS
[Nm] Nome de substância:
0 (Antinematodal Agents); 4QIH0N49E7 (Pyrantel); 94AJJ30D9E (oxantel); EC 1.3.99.1 (Succinate Dehydrogenase)
[Em] Mês de entrada:1408
[Cu] Atualização por classe:140801
[Lr] Data última revisão:
140801
[Sb] Subgrupo de revista:D
[Da] Data de entrada para processamento:140802
[St] Status:MEDLINE


  10 / 326 MEDLINE  
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[PMID]:24412397
[Au] Autor:Somvanshi VS; Ellis BL; Hu Y; Aroian RV
[Ad] Endereço:Section of Cell and Developmental Biology, Division of Biological Sciences, University of California San Diego, La Jolla, CA, USA.
[Ti] Título:Nitazoxanide: nematicidal mode of action and drug combination studies.
[So] Source:Mol Biochem Parasitol;193(1):1-8, 2014 Jan.
[Is] ISSN:1872-9428
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Intestinal nematodes or roundworms (aka soil-transmitted helminths or STHs) cause great disease. They infect upwards of two billion people, leading to high morbidity and a range of health problems, especially in infected children and pregnant women. Development of resistance to the two main classes of drugs used to treat intestinal nematode infections of humans has been reported. To fight STH infections, we need new and more effective drugs and ways to improve the efficacy of the old drugs. One promising alternative drug is nitazoxanide (NTZ). NTZ, approved for treating human protozoan infections, was serendipitously shown to have therapeutic activity against STHs. However, its mechanism of action against nematodes is not known. Using the laboratory nematode Caenorhabditis elegans, we show that NTZ acts on the nematodes through avr-14, an alpha-type subunit of a glutamate-gated chloride ion channel known for its role in ivermectin susceptibility. In addition, a forward genetic screen to select C. elegans mutants resistant to NTZ resulted in isolation of two NTZ resistant mutants that are not in avr-14, suggesting that additional mechanisms are involved in resistance to NTZ. We found that NTZ combines synergistically with other classes of anthelmintic drugs, i.e. albendazole and pyrantel, making it a good candidate for further studies on its use in drug combination therapy of STH infections. Given NTZ acts against a wide range of nematode parasites, our findings also validate avr-14 as an excellent target for pan-STH therapy.
[Mh] Termos MeSH primário: Anti-Helmínticos/farmacologia
Caenorhabditis elegans/efeitos dos fármacos
Canais de Cloreto/antagonistas & inibidores
Tiazóis/farmacologia
[Mh] Termos MeSH secundário: Albendazol/farmacologia
Animais
Caenorhabditis elegans/enzimologia
Sinergismo Farmacológico
Pirantel/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anthelmintics); 0 (Chloride Channels); 0 (Thiazoles); 0 (glutamate-gated chloride channels); 4QIH0N49E7 (Pyrantel); F4216019LN (Albendazole); SOA12P041N (nitazoxanide)
[Em] Mês de entrada:1411
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140114
[St] Status:MEDLINE



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