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1.
Crit Rev Toxicol ; 54(3): 194-213, 2024 03.
Artigo em Inglês | MEDLINE | ID: mdl-38470098

RESUMO

Neonicotinoid pesticides are utilized against an extensive range of insects. A growing body of evidence supports that these neuro-active insecticides are classified as toxicants in invertebrates. However, there is limited published data regarding their toxicity in vertebrates and mammals. the current systematic review is focused on the up-to-date knowledge available for several neonicotinoid pesticides and their non-acute toxicity on rodents and human physiology. Oral lethal dose 50 (LD50) of seven neonicotinoids (i.e. imidacloprid, acetamiprid, clothianidin, dinotefuran, thiamethoxam, thiacloprid, and nitenpyram) was initially identified. Subsequently, a screening of the literature was conducted to collect information about non-acute exposure to these insecticides. 99 studies were included and assessed for their risk of bias and level of evidence according to the Office of Health and Translation (OHAT) framework. All the 99 included papers indicate evidence of reproductive toxicity, hepatotoxicity, nephrotoxicity, neurotoxicity, immunotoxicity, and oxidative stress induction with a high level of evidence in the health effect of rodents and a moderate level of evidence for human health. The most studied type of these insecticides among 99 papers was imidacloprid (55 papers), followed by acetamiprid (22 papers), clothianidin (21 papers), and thiacloprid (11 papers). While 10 of 99 papers assessed the relationship between clothianidin, thiamethoxam, dinotefuran, and nitenpyram, showing evidence of liver injury, dysfunctions of oxidative stress markers in the reproductive system, and intestinal toxicity. This systematic review provides a comprehensive overview of the potential risks caused by neonicotinoid insecticides to humans and rodents with salient health effects. However, further research is needed to better emphasize and understand the patho-physiological mechanisms of these insecticides, taking into account various factors that can influence their toxicity.


Assuntos
Guanidinas , Inseticidas , Tiazinas , Tiazóis , Animais , Humanos , Tiametoxam , Inseticidas/toxicidade , Oxazinas/toxicidade , Neonicotinoides/toxicidade , Nitrocompostos/toxicidade , Medição de Risco , Mamíferos
2.
Mar Pollut Bull ; 199: 116013, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38183835

RESUMO

Imidacloprid and thiacloprid, two neonicotinoid insecticides that are extensively used in urban areas, are potentially toxic to non-target aquatic organisms. In this study, the concentrations of imidacloprid and thiacloprid in surface runoff after rainfall were 20.79-43.77 ng/L and 25.13-63.84 ng/L, respectively, whereas the levels for the Licun River were 10.78-41.70 ng/L and 2.66-39.68 ng/L, respectively. The acute and chronic criteria for imidacloprid and thiacloprid are 0.865, 0.006, 0.83, and 0.012 µg/L, respectively. Tiered ecological risk assessments revealed the chronic ecological risks of these micropollutants to local aquatic species. There was a moderate chronic toxicity risk associated with imidacloprid and thiacloprid in the Licun River, and the joint probability curves showed a probability of chronic ecological risk to 5 % of the aquatic organisms at 68 %-97 %. The results provide evidence of urban surface runoff transporting micropollutants from surface into rivers and estuaries, highlighting the ecological risks to aquatic ecosystems.


Assuntos
Inseticidas , Nitrocompostos , Tiazinas , Poluentes Químicos da Água , Rios , Ecossistema , Poluentes Químicos da Água/análise , Neonicotinoides/análise , Inseticidas/análise , Medição de Risco , China , Organismos Aquáticos
3.
Food Res Int ; 161: 111899, 2022 11.
Artigo em Inglês | MEDLINE | ID: mdl-36192918

RESUMO

Government regulatory actions and public policies to reduce sugar consumption were recently implemented in Brazil. To evaluate their potential impact on the supply of products containing high-intensity sweeteners (HIS) and on dietary exposure to these substances, this study aimed to create a comprehensive database on HIS declared in Brazilian commercial products and estimate their intake through consumption of these products. The occurrence of HIS was evaluated through labeling information of 1869 commercial products available in the Brazilian market, collected between January 2021 and August 2021, and the daily intake was estimated for eight HIS (acesulfame K, advantame, aspartame, cyclamate, steviol glycosides, neotame, saccharin and sucralose) using a deterministic approach by multiplying the maximum permitted levels of HIS in foods and beverages by the consumption data of these products. The consumption data were obtained from the report of Household Budget Survey (POF/IBGE), conducted from 2017 to 2018 through a 24-hour dietary recall applied to 46,164 individuals aged 10 years and over, which included only average data (i.e. average consumption for the general population or subgroups). The most frequent HIS in the investigated products were sucralose (26.8 %; n = 938) and acesulfame K (21.7 %; n = 759), and although the combination of sweeteners is a common practice in the food industry, there was a predominance of only one substance in the investigated products (46.7 %; n = 873). The estimated intake of HIS for average consumers was below the Acceptable Daily Intake (ADI) and does not suggest a toxicological concern. A similar scenario was observed for high consumers, except for cyclamate and steviol glycosides, which corresponded to 144 % and 131 % of their respective ADIs in the general population. To our knowledge, this is the most comprehensive database on HIS in Brazil and the most recent exposure assessment performed nationally.


Assuntos
Aspartame , Adoçantes não Calóricos , Brasil , Ciclamatos , Açúcares da Dieta , Diterpenos do Tipo Caurano , Glucosídeos , Humanos , Sacarina , Edulcorantes/análise , Tiazinas
4.
Sci Rep ; 12(1): 3470, 2022 03 02.
Artigo em Inglês | MEDLINE | ID: mdl-35236880

RESUMO

The dissipation and residue levels of thiacloprid, spirotetramat and its four metabolites residues in cowpeas were investigated under field conditions. The QuEChERS technique with high-performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS) was used to detect thiacloprid, spirotetramat and its four metabolites residues content in cowpeas. The recoveries were 81.3-95.1% at a spike level of 0.005-0.5 mg/kg, the relative standard deviations (RSDs) were 2.1-9.5%. The dissipation kinetics data showed that thiacloprid and spirotetramat in cowpeas were degraded with the half-lives of 1.14-1.54 days and 1.25-2.79 days. The terminal residues of thiacloprid and spirotetramat were 0.0255-0.4570 mg kg-1 and 0.0314-0.3070 mg kg-1 after application 2 times with a pre-harvest interval (PHI) of 3 days under the designed dosages. The chronic and acute dietary exposure assessment risk quotient (RQ) values of thiacloprid in cowpeas for different consumers were 2.44-4.41% and 8.72-15.78%, respectively, and those of spirotetramat were 1.03-1.87% and 0.18-0.32%, respectively, all of the RQ values were lower than 100%. The dietary risk of thiacloprid through cowpeas to consumers was higher than spirotetramat. The results from this study are important reference for Chinese governments to develop criteria for the safe and rational use of thiacloprid and spirotetramat, setting maximum residue levels (MRLs), monitoring the quality safety of agricultural products and protecting consumer health.


Assuntos
Resíduos de Praguicidas , Vigna , Compostos Aza , China , Meia-Vida , Neonicotinoides , Resíduos de Praguicidas/análise , Medição de Risco , Compostos de Espiro , Espectrometria de Massas em Tandem/métodos , Tiazinas , Vigna/química
5.
Transl Vis Sci Technol ; 11(2): 1, 2022 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-35103799

RESUMO

PURPOSE: Impaired ocular blood flow has been associated with the etiopathogenesis of glaucoma. Topical brimonidine lowers intraocular pressure, a major glaucoma risk factor. However, brimonidine's influence on retinal blood flow remains to be fully elucidated. Our aim was to compare the effect of topical brimonidine and brinzolamide administration on retinal blood flow velocity in second and third order vessels in healthy adults using the retinal function imager. METHODS: In 10 healthy probands between 23 and 32 years of age, one eye was randomly selected to receive 2 treatment rounds with 3 single doses of brimonidine 2 mg/mL and brinzolamide 10 mg/mL at 12-hour intervals each. The fellow eyes served as intra-individual controls. Immediately before the first drop and 2 hours after the last drop of each treatment round, all subjects were examined, including Goldmann tonometry, Pascal tonometry, assessment of retinal blood flow velocity using the retinal function imager, as well as blood pressure and pulse measurements. RESULTS: Intraocular pressure decreased significantly in treated eyes while remaining stable in control eyes, indicating reliable application of brimonidine and brinzolamide drops. In contrast, retinal blood flow velocities did not demonstrate any significant differences between groups after both treatment rounds. CONCLUSIONS: Neither brimonidine nor brinzolamide appear to alter retinal blood flow velocity in a clinically relevant manner. The slight velocity changes detected in our study are likely physiologic fluctuations. Our findings do not support the rationale of a detrimental effect of topical brimonidine on ocular blood flow and hence brimonidine may be further administered for lowering intraocular pressure with the appropriate caution. However, our study is strongly limited by the small sample size and, thus, further research with larger cohorts of healthy volunteers and patients with glaucoma is needed to confirm the results. TRANSLATIONAL RELEVANCE: The study provides information about the effect of the topically administered antiglaucoma medications brimonidine and brinzolamide on the ocular blood flow and its regulation. The findings indicate that beside the lowering of IOP there is no evidence for an additional effect on the development of glaucoma.


Assuntos
Velocidade do Fluxo Sanguíneo , Tartarato de Brimonidina , Hipertensão Ocular , Sulfonamidas , Tiazinas , Adulto , Velocidade do Fluxo Sanguíneo/efeitos dos fármacos , Tartarato de Brimonidina/administração & dosagem , Glaucoma , Humanos , Hipertensão Ocular/diagnóstico por imagem , Hipertensão Ocular/tratamento farmacológico , Sulfonamidas/administração & dosagem , Tiazinas/administração & dosagem , Adulto Jovem
6.
J Vet Intern Med ; 35(5): 2196-2204, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34464464

RESUMO

BACKGROUND: Diagnosis of gastric ulcers by methods other than gastroscopy in dogs has been problematic for many years and biomarkers such as serum gastrin (SG) concentrations have been introduced as a noninvasive way to evaluate gastric diseases. OBJECTIVES: To determine the time course changes in hematology, SG concentrations, and gastroscopic images of meloxicam-induced gastric ulceration in dogs and identify a relationship between SG and gastroscopic image analysis in a clinical setting. ANIMALS: Fifteen crossbreed dogs. METHODS: Two groups: control (n = 5) and meloxicam-treated (n = 10). The meloxicam-treated group received meloxicam 0.2 mg/kg PO for 15 days. Clinical signs, hematology, SG, and image analysis (PI, pixel intensity; ID, integrated density; RA, relative area; and UI, ulcer index) of the gastroscopic examination were evaluated across time (T5, time 5 day; T10, time 10 day; and T15, time 15 day). RESULTS: Significant changes were observed among 3 time points and between the 2 groups in terms of SG, hematology, and gastroscopic image analysis. In the meloxicam-treated group, decreases in hemoglobin concentration, red blood cell count and packed cell volume at T10 and T15 (P = .0001) were observed, whereas SG, ID, and UI increased over time (P < .0001). The PI decreased significantly (P = .0001) in the meloxicam-treated group compared to controls. Significant correlations were found between SG and PI, and ID and ulcer area (r = -0.89, 0.81, 0.64), respectively. CONCLUSION AND CLINICAL IMPORTANCE: Gastroscopy is the gold standard for early descriptive diagnosis of gastric ulcerations in dogs, and SG is a good indicator for meloxicam-induced gastric ulcers in dogs and can predict the gastroscopic score of the lesion.


Assuntos
Doenças do Cão , Hematologia , Úlcera Gástrica , Tiazinas , Animais , Doenças do Cão/induzido quimicamente , Doenças do Cão/diagnóstico , Cães , Gastrinas , Gastroscopia/veterinária , Meloxicam , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/veterinária , Tiazinas/efeitos adversos , Tiazóis/efeitos adversos
7.
Environ Monit Assess ; 193(3): 129, 2021 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-33587214

RESUMO

Samples of leaves, flowers, soil, pollen, bee workers, bee brood, honey, and beeswax were collected to assess the possibility of a transfer of captan, thiacloprid, penthiopyrad, and λ-cyhalothrin from apple trees of Idared variety to honey bee (Apis mellifera) hives. Chemical analyses were performed using the Agilent 7890 Gas Chromatograph equipped with the Micro-cell Electron Capture Detector. It was found that significant amounts of penthiopyrad, the active ingredient of Fontelis 200 SC, were present in leaves, flowers, pollen, bee workers, and beeswax. Simultaneously, captan was present in the brood, worker bees, and honey samples. Significant levels of the captan residues were also detected on the soil surface. In honey samples, captan residue levels exceeded the acceptable standard, reaching 160% of its maximum residue level. However, in no case the amounts of captan, thiacloprid, penthiopyrad, and λ-cyhalothrin ingested with honey by an adult consumer exceeded the level of 0.02% of the acceptable daily intake. Despite the trace amounts of pesticide residues in honey samples collected during the field trial, bee honey consumption can be considered safe. An adult consumer can safely consume about 16 kg of honey.


Assuntos
Inseticidas , Malus , Animais , Abelhas , Captana/análise , Monitoramento Ambiental , Insetos , Inseticidas/análise , Inseticidas/toxicidade , Neonicotinoides , Nitrilas , Pirazóis , Piretrinas , Tiazinas , Tiofenos
8.
J Hazard Mater ; 403: 123935, 2021 02 05.
Artigo em Inglês | MEDLINE | ID: mdl-33264984

RESUMO

UV/monochloramine (UV/NH2Cl) is an emerging advanced oxidation process that can generate various reactive species like reactive chlorine species (RCS) and hydroxyl radicals for micropollutant removal. This study investigated the potential toxicity of transformation products resulting from UV/NH2Cl treatment of acesulfame (ACE), as an example of micropollutant, found in worldwide aquatic environment. Compared with UV photolysis and chloramination, the UV/NH2Cl process more effectively degraded ACE. The transformation products of ACE treated with the UV/NH2Cl process were identified and characterized with high resolution mass spectrometry. The formation of chlorinated-TPs indicated the role of RCS in UV/NH2Cl transformation even though UV photolysis was predominantly responsible for the ACE degradation. The Vibrio fischeri bioluminescence inhibition assay revealed a higher toxicity of TPs derived from UV/NH2Cl than from UV photolysis. The increased toxicity could be attributed to most of the generated chlorinated-TPs (Cl-TPs), in particular those halo-alcohols. The ECOSAR program predicts that halo-alcohol TPs are more toxic than their non-chlorinated analogues and other Cl-TPs. This study provides insight into the important role of reactive species in the micropollutants' transformation of UV/NH2Cl process. It further provides information relevant to the potential risk when applying the process for micropollutant removal in water treatment.


Assuntos
Poluentes Químicos da Água , Purificação da Água , Cloraminas , Cinética , Oxirredução , Fotólise , Tiazinas , Raios Ultravioleta , Poluentes Químicos da Água/análise , Poluentes Químicos da Água/toxicidade
9.
Xenobiotica ; 51(5): 536-548, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-33086928

RESUMO

Thiacloprid (THI) is a widely used neonicotinoid insecticide where concerns have been raised regarding low absorption by crops, substantial distribution in surrounding areas, and potential adverse effects to terrestrial and aquatic organisms.Prior to this study, there was very limited information addressing the ex vivo (precision-cut liver slices) metabolism of THI by fish species and the metabolic pathways regulating its potential for adverse effects.The in vitro and ex vivo biotransformation pathway of THI is defined by the formation of three primary metabolites (TM1, TM2 and TM3) via separate paths differentiated by reductive decyanation, reductive dechlorination with hydration and dealkylation processes, respectively.Kinetic rates were calculated for the rat microsomal decyanation of THI into TM1 (Km = 299.2 µM and Vmax = 5.3 pmol/min/mg), and for the dealkylation of THI into TM3 (Km = 368.9 µM and Vmax = 3.95 pmol/min/mg).Formation confirmation and identity inference of THI metabolites in absence of standards were achieved by LC-UV and High Resolution-MS strategies.The in vitro and ex vivo metabolic products of THI are conserved both across species (rat and Rainbow trout) and levels of biological organization (microsomes and liver slices), as previously reported for the neonicotinoid insecticides Imidacloprid and Acetamiprid.


Assuntos
Inseticidas , Oncorhynchus mykiss , Tiazinas , Animais , Espectrometria de Massas , Neonicotinoides , Ratos
10.
J Sports Sci ; 37(18): 2159-2167, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31156048

RESUMO

Average acceleration (AvAcc) and intensity gradient (IG) have been proposed as standardised metrics describing physical activity (PA) volume and intensity, respectively. We examined hypothesised between-group PA differences in AvAcc and IG, and their associations with health and well-being indicators in children. ActiGraph GT9X wrist accelerometers were worn for 24-h·d-1 over 7days by 145 children aged 9-10. Raw accelerations were averaged per 5-s epoch to represent AvAcc over 24-h. IG represented the relationship between log values for intensity and time. Moderate-to-vigorous PA (MVPA) was estimated using youth cutpoints. BMI z-scores, waist-to-height ratio (WHtR), peak oxygen uptake (VO2peak), Metabolic Syndrome risk (MetS score), and well-being were assessed cross-sectionally, and 8-weeks later. Hypothesised between-group differences were consistently observed for IG only (p < .001). AvAcc was strongly correlated with MVPA (r = 0.96), while moderate correlations were observed between IG and MVPA (r = 0.50) and AvAcc (r = 0.54). IG was significantly associated with health indicators, independent of AvAcc (p < .001). AvAcc was associated with well-being, independent of IG (p < .05). IG was significantly associated with WHtR (p < .01) and MetS score (p < .05) at 8-weeks follow-up. IG is sensitive as a gauge of PA intensity that is independent of total PA volume, and which relates to important health indicators in children.


Assuntos
Aceleração , Exercício Físico , Acelerometria/instrumentação , Índice de Massa Corporal , Aptidão Cardiorrespiratória , Criança , Estudos Transversais , Feminino , Monitores de Aptidão Física , Humanos , Masculino , Síndrome Metabólica , Consumo de Oxigênio , Obesidade Infantil , Projetos Piloto , Qualidade de Vida , Classe Social , Tiazinas , Razão Cintura-Estatura , Punho
11.
Water Res ; 153: 357-368, 2019 04 15.
Artigo em Inglês | MEDLINE | ID: mdl-30763901

RESUMO

The monitoring and control of drinking water quality is generally important as it significantly contributes to the health of the population. In this context, particular attention has to be paid to the use of treatment techniques during drinking water treatment. It is known that the formation of reaction products (transformation products) has to be taken into account when oxidizing agents such as ozone are used. Different transformation products are classified as critical to health and require analytical examination. The risk assessment for previously unknown transformation products can be difficult as far as not all transformation products are present as single substances or the individual substances are not present in a sufficient high concentration or cannot be isolated from the original solution. The aim of this work is to show exemplarily the identification and quantification of ozonation products (OPs) after ozonation and their toxicological characterization, using the artificial sweetener acesulfame. It was shown that OPs can be fully characterized using ion chromatography in combination with different detection systems. A major OP could be recovered as a pure substance by crystallization and direct genotoxicological testing was possible without previous enrichment processes. Acesulfame samples of different concentrations in ultrapure and in drinking water after ozonation were tested in several genotoxicity tests. These tests revealed genotoxic effects of acesulfame after ozonation in ultrapure water in several genotoxicological test systems (micronucleus test, umu test, Ames-fluctuation-test and comet assay). In contrast, the crystallized ozonation product OP168 did not show any positive effects. Therefore, it seems likely that the observed effect was caused by the second major product OP170. However, a sufficiently large amount of analytically pure substance OP170 could not be obtained. It was also shown that the rate of the OP170 formation in drinking water is significantly lower than in ultrapure water and that ozonation in drinking water did not induce genotoxic effects.


Assuntos
Água Potável , Ozônio , Tiazinas , Poluentes Químicos da Água , Purificação da Água , Edulcorantes
12.
J Contam Hydrol ; 215: 11-20, 2018 08.
Artigo em Inglês | MEDLINE | ID: mdl-29983209

RESUMO

The assessment of vulnerability in karst systems reveals to be extremely challenging since it varies significantly with time and highly depends on the identification of diffuse and concentrated infiltration from surface karst features. The origin, consumed loads, and transport mode of selected micropollutants (MPs) including two artificial sweeteners (ASWs) Sucralose (SUC) and Acesulfame-K (ACE-K), in addition to other less investigated pharmaceuticals such as the lipid regulator Gemfibrozil (GEM), and the contrast media Iohexol (IOX) were investigated in a karst system under dynamic conditions. A detailed analysis of selected spring responses' chemograph and hydrograph following a multi precipitation event shows that three of the tracked MPs, especially ACE-K, and to the exception of IOX, can be used as specific indicators for point source domestic wastewater in karst systems. They have revealed to be persistent, source specific, conservative, and highly correlated with in-situ parameters easily measurable at the spring (chloride and turbidity). Even if the selected MPs are found in the system during low flow periods, they are mostly transported to the spring through fast flow pathways from flushed wastewater with surface water or flood rainwater. The highest mass inflow of ACE-K, IOX and GEM originated from a sinking stream, while SUC infiltrated exclusively through fast infiltration points (dolines). Their breakthrough curves coincide with the arrival of new waters and turbidity peaks. Unlike IOX, the mass fluxes of ASWs, and GEM to a lesser extent, can be linearly correlated with chloride mass fluxes and turbidity flux. Moreover, the variance of the normalized breakthrough curves of the MPs with respect to a mean transit time, increases in that order IOX

Assuntos
Genfibrozila , Água Subterrânea , Iohexol , Sacarose/análogos & derivados , Tiazinas , Águas Residuárias , Monitoramento Ambiental , Rios , Edulcorantes , Águas Residuárias/análise
13.
J Dairy Sci ; 101(4): 3387-3397, 2018 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-29398019

RESUMO

Recently, it has been shown that the addition of meloxicam to standard antimicrobial therapy for clinical mastitis (CM) improves the conception rate of dairy cows contracting CM in the first 120 d in milk. The objective of our study was to assess whether this improved reproduction through additional treatment with meloxicam would result in a positive net economic benefit for the farmer. We developed a stochastic bio-economic simulation model, in which a dairy cow with CM in the first 120 d in milk was simulated. Two scenarios were simulated in which CM cases were treated with meloxicam in conjunction with antimicrobial therapy or with antimicrobial therapy alone. The scenarios differed for conception rates (31% with meloxicam or 21% without meloxicam) and for the cost of CM treatment. Sensitivity analyses were undertaken for the biological and economic components of the model to assess the effects of a wide range of inputs on inferences about the cost effectiveness of meloxicam treatment. Model results showed an average net economic benefit of €42 per CM case per year in favor of the meloxicam scenario. Cows in the no-meloxicam treatment scenario had higher returns on milk production, lower costs upon calving, and reduced costs of treatment. However, these did not outweigh the savings associated with lower feed intake, reduced number of inseminations, and the reduced culling rate. The net economic benefit favoring meloxicam therapy was a consequence of the better reproductive performance in the meloxicam scenario in which cows had a shorter calving to conception interval (132 vs. 143 d), a shorter intercalving interval (405 vs. 416 d), and fewer inseminations per conception (2.9 vs. 3.7) compared with cows in the no-meloxicam treatment scenario. This resulted in a shorter lactation, hence a lower lactational milk production (8,441 vs. 8,517 kg per lactation) with lower feeding costs in the meloxicam group. A lower culling rate (12 vs. 25%) resulted in lower replacement costs in the meloxicam treatment scenario. All of the scenarios evaluated in the sensitivity analyses favored meloxicam treatment over no meloxicam. This study demonstrated that improvements in conception rate achieved by the use of meloxicam, as additional therapy for mild to moderate CM in the first 120 d in milk, have positive economic benefits. This inference remained true over a wide range of technical and economic inputs, demonstrating that use of meloxicam is likely to be cost effective across many production systems.


Assuntos
Antibacterianos/uso terapêutico , Anti-Inflamatórios não Esteroides/uso terapêutico , Indústria de Laticínios/economia , Mastite Bovina/tratamento farmacológico , Tiazinas/uso terapêutico , Tiazóis/uso terapêutico , Animais , Bovinos , Indústria de Laticínios/métodos , Feminino , Lactação/efeitos dos fármacos , Mastite Bovina/economia , Meloxicam , Leite/economia , Modelos Econômicos , Reprodução , Processos Estocásticos
14.
Eur J Pharm Sci ; 112: 146-151, 2018 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-29174987

RESUMO

Meloxicam (MLX) is a non-steroidal anti-inflammatory cyclooxygenase (COX) inhibitor that is used to relieve inflammation and pain. MLX has a preferential affinity for COX-2, which is associated with a lower incidence of gastrointestinal side effects. The drug belongs to Class II of the Biopharmaceutical Classification System (BCS) in which dissolution is the limiting step of its bioavailability. In view of this classification, carrying out further studies regarding the compatibility of MLX with excipients and the mechanisms and kinetics of its degradation reactions is fundamental because any changes would directly influence the quality of the product. The aim of the present work is to evaluate solid pharmaceutical formulations containing MLX found on the market to define the more suitable excipients to improve the stability of the pharmaceutical formulations. Thermal analysis techniques were used to characterize and evaluate the compatibility between the drug and the excipients present in the market formulations. In the evaluation of its solid-state kinetics, MLX raw material under inert conditions had a shelf life of approximately 6years. In the study of compatibility between the drug and excipients, MLX was found to be incompatible with magnesium stearate after DSC analysis under binary mixtures, which was confirmed by stress studies and chromatographic analyzes.


Assuntos
Anti-Inflamatórios não Esteroides/química , Excipientes/química , Tiazinas/química , Tiazóis/química , Varredura Diferencial de Calorimetria , Composição de Medicamentos , Estabilidade de Medicamentos , Meloxicam
15.
Vet Anaesth Analg ; 44(5): 1166-1174, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29037798

RESUMO

OBJECTIVE: To evaluate the efficacy of oral meloxicam, topical anaesthetic cream and cautery iron in mitigating acute nociceptive responses of pigs to tail docking. STUDY DESIGN: A prospective, randomized, controlled experimental study. ANIMALS: A total of 40 healthy Large WhitexLandrace pigs aged 21±1 days, weighing 6.1±0.9 kg. METHODS: Pigs were randomly assigned to one of four treatments (n=10 per treatment): CONTROL: docked using clippers without analgesia; MEL: docked using clippers after administration of oral meloxicam; EMLA: docked using clippers after application of topical anaesthetic cream; and CAUT: docked using a cautery iron without analgesia. Anaesthesia was induced and maintained with halothane in oxygen. Following induction, end-tidal halothane was stabilized at 0.95-1.05% and electroencephalograph (EEG) recording commenced. After 5 minutes of baseline data collection, tail docking was performed and recording continued for a further 10 minutes. The EEG summary variables median frequency (F50), 95% spectral edge frequency (F95) and total power (PTOT) were calculated for the baseline period and for consecutive 30-second intervals following docking. RESULTS: Following docking, F50 increased and PTOT decreased significantly in CONTROL and MEL pigs. EMLA pigs exhibited no change in any variable, whilst CAUT pigs exhibited a reduction in PTOT but no change in F50. F50 was higher in control pigs than in EMLA pigs 30-60 seconds after docking (p≤0.01). PTOT was lower in CONTROL than in EMLA pigs 30-90 seconds after docking (p<0.03) and in CAUT pigs 60 seconds after docking (p=0.01). CONCLUSIONS AND CLINICAL RELEVANCE: Prior application of EMLA cream abolished EEG indicators of nociception in pigs docked using clippers. Docking using a cautery iron without analgesia ameliorated EEG indicators of nociception, relative to using clippers without analgesia. Prior administration of EMLA cream or the use of cautery instead of clippers may reduce the acute pain experienced by pigs undergoing tail docking.


Assuntos
Dor Aguda/veterinária , Amputação Cirúrgica/veterinária , Analgésicos , Anestesia Local/veterinária , Anestésicos Locais , Eletroencefalografia/veterinária , Sus scrofa/cirurgia , Cauda/cirurgia , Tiazinas , Tiazóis , Dor Aguda/fisiopatologia , Dor Aguda/prevenção & controle , Administração Oral , Amputação Cirúrgica/instrumentação , Amputação Cirúrgica/métodos , Analgésicos/administração & dosagem , Anestesia Local/métodos , Anestésicos Locais/administração & dosagem , Animais , Anti-Infecciosos Locais , Feminino , Masculino , Meloxicam , Tiazinas/administração & dosagem , Tiazóis/administração & dosagem
16.
Vet Anaesth Analg ; 44(3): 646-655, 2017 May.
Artigo em Inglês | MEDLINE | ID: mdl-28237682

RESUMO

OBJECTIVE: To evaluate the effects of demeanor on validated pain assessment scales. STUDY DESIGN: Prospective, blind, clinical trial. ANIMAL POPULATION: Thirty three adult domestic cats scheduled for orchiectomy. METHODS: Cats were assessed for pain pre (baseline) and 1, 2, 4 hours postoperatively using two validated pain scales [Composite Measures Pain Scale-Feline (rCMPS-F) and UNESP-Botucatu multidimensional composite pain scale (psychomotor and pain expression subscales; U-B MCPS-psych and -painex)], and a demeanor scale. Return of sternal recumbency and postoperative feeding were recorded. Anesthesia consisted of a single intramuscular injection of dexmedetomidine-ketamine-hydromorphone with intratesticular lidocaine and atipamezole and meloxicam postoperatively. Following data collection, cats were assigned to two groups based on baseline demeanor scores (LO ≤ 5/21, 18 cats; HI ≥ 6/21, 15 cats) and data from each group compared. RESULTS: Baseline demeanor predicted pain scores with the U-B MCPS-psych scale: baseline [LO 0 (0-0), HI 2 (0-6), p = 0.0005], 1 hour [LO 1 (0-5), HI 3 (1-5), p = 0.02], and 4 hours [LO 0 (0-2), HI 1 (0-6), p = 0.01]. A similar pattern was observed with the rCMPS-F. This resulted in more crossings of the analgesic intervention threshold in the HI group: U-B UNESP-psych (9 versus 1, p = 0.005) and rCMPS-F (23 versus 3, p < 0.0001). In contrast, U-B MCPS-painex scores did not differ between LO/HI groups: baseline (p > 0.99), 1 hour (p = 0.34), 2 hours (p > 0.99) and 4 hours (p = 0.31). LO cats ate sooner (61% versus 33% by 1 hour, p < 0.0001) despite similar times to sternal recumbency (p = 0.48). CONCLUSIONS AND CLINICAL RELEVANCE: Demeanor affected pain assessment with U-B UNESP-psych and rCMPS-F scales, but not U-B UNESP-painex scale. Demeanor had a significant effect on postoperative feeding. These data highlight the potential for demeanor to confound pain assessment.


Assuntos
Orquiectomia/veterinária , Medição da Dor/veterinária , Dor Pós-Operatória/veterinária , Anestesia/veterinária , Animais , Gatos , Dexmedetomidina , Hidromorfona , Imidazóis , Ketamina , Lidocaína , Masculino , Meloxicam , Orquiectomia/efeitos adversos , Medição da Dor/métodos , Dor Pós-Operatória/diagnóstico , Dor Pós-Operatória/psicologia , Período Perioperatório , Estudos Prospectivos , Tiazinas , Tiazóis
17.
Chemosphere ; 171: 185-191, 2017 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-28013080

RESUMO

Biochars can significantly sorb pesticides, and reduce their bioavailability in agricultural soils. In this study, the effects of a type of biochar (BC500) on the sorption, degradation, bioaccumulation and bioavailability of thiacloprid, which is a commonly used insecticide, were investigated. The thiacloprid sorption constant (Kf values) increased by 14 times after 2% BC500 application, and the degradation of the insecticide decreased with increasing amounts of the biochars in the soil. Coupled with the exhaustive extraction and single-point Tenax method, the bioavailability of thiacloprid was predicted in the presence of the biochar. In soils amended with BC500, the thiacloprid concentrations accumulated in Tenax correlated well with those observed in earthworms (R2 = 0.887), whereas the concentrations extracted by exhaustive method followed a less significant relationship with those in earthworms (R2 = 0.624). The results of Tenax extractions and earthworm bioassays indicate that biochar reduces the bioavailability of thiacloprid in soil, but the delayed degradation and increased earthworm accumulation in aged biochar-amended soil imply that the environmental risks of biochar application to earthworms remain.


Assuntos
Carvão Vegetal/química , Oligoquetos/metabolismo , Piridinas/metabolismo , Poluentes do Solo/metabolismo , Solo/química , Tiazinas/metabolismo , Agricultura , Animais , Disponibilidade Biológica , Meio Ambiente , Neonicotinoides , Piridinas/química , Poluentes do Solo/química , Tiazinas/química
18.
J Hazard Mater ; 323(Pt A): 471-477, 2017 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-27061679

RESUMO

In the present study, we investigated the possibility to abate Acesulfame K, a persistent emerging contaminant, in aqueous media using zinc oxide based materials. For this purpose, bare and Ce-doped zinc oxide was prepared via an easy and cheap hydrothermal process using different cerium salts as precursors. Their photocatalytic performance was evaluated in different media, namely ultrapure and river water under both UV-vis and visible light. Commercial TiO2 P25 was also employed and used as a reference photocatalyst for comparison purposes. The obtained results pointed out that cerium doped zinc oxide composites exhibit higher performance than TiO2 P25, especially under visible light and in the presence of organic matter, when the activity of the latter is greatly depressed. In particular, ZnO doped with cerium (1%) was the most effective material, and could be a promising alternative to TiO2 P25, especially in the treatment of natural waters.


Assuntos
Cério/química , Edulcorantes/análise , Tiazinas/análise , Poluentes Químicos da Água/química , Óxido de Zinco/química , Algoritmos , Catálise , Luz , Processos Fotoquímicos , Rios , Raios Ultravioleta
19.
Biomed Chromatogr ; 31(5)2017 May.
Artigo em Inglês | MEDLINE | ID: mdl-27696449

RESUMO

This study was undertaken to quantify the residue levels and propose the dissipation kinetics of thiacloprid formulated as suspension concentrate in field-incurred Asian pears grown under two different open-field conditions. Samples were extracted with 20% distilled water in acetonitrile; partitioned with brine water and dichloromethane; and purified with a Florisil solid phase extraction cartridge. The analyte was identified with an LC ultraviolet detector, and field-incurred samples were confirmed using LC-MS/MS. The calibration curve was linear over the range 0.05-5.0 mg/L with a satisfactory coefficient of determination (R2 = 0.9994). The limits of detection and limits of quantification (LOQ) were 0.003 and 0.01 mg/kg, respectively. The recovery rate fortified to blank samples at LOQ, 10× LOQ, and the maximum residue limit (MRL) were between 73.7 and 86.2% with relative standard deviation ≤9.0%. The residual concentrations at both sites were considerably lower than the MRL (0.7 mg/kg) set by the Korean Ministry of Food Drug Safety, with biological half-lives of 5.0 and 7.4 days, for sites 1 and 2, respectively. From the pre-harvest residue limit curve, it was predicted that if the residues were <1.13 or 1.40 mg/kg 10 days before harvest, the residue level would be lower than the MRL during harvest. Risk assessment on day 0 showed an acceptable daily intake (%) of 13.0% and 11.0% for sites 1 and site 2, respectively, which indicates that the residual amounts are not hazardous to the Korean population.


Assuntos
Cromatografia Líquida/métodos , Resíduos de Praguicidas/análise , Piridinas/análise , Pyrus/química , Espectrometria de Massas em Tandem/métodos , Tiazinas/análise , Calibragem , Análise de Alimentos/métodos , Contaminação de Alimentos/análise , Cinética , Limite de Detecção , Neonicotinoides , Medição de Risco , Sensibilidade e Especificidade
20.
J Econ Entomol ; 109(5): 2182-9, 2016 10.
Artigo em Inglês | MEDLINE | ID: mdl-27498842

RESUMO

Myzus persicae (Sulzer, 1776), a major crop pest worldwide, displays insecticide resistance to most molecules. The R81T substitution on the ß1 subunit of nicotinic receptors of acetylcholine (nAChR) confers target site resistance to neonicotinoids and is widespread in aphid populations colonizing peach tree orchards in Southern Europe. But the impact of this resistance in the field, as well as ways to optimize its management, depends largely on the dominance level of the R81T mutation. In this study, we measured by in vitro assays the response of R81T mutation to two neonicotinoids (imidacloprid and thiacloprid) in 23 M. persicae clones with different resistance genotypes in order to assess the dominance status of this allele. In this study, all homozygous clones for the R81T mutation (genotype 81(TT)) showed a much higher level of resistance to both active substances than other clones. The heterozygous clones 81(RT) displayed a slightly higher level of resistance than wild homozygous, though resistance phenotypes against both neonicotinoids in these two genotypes were overlapping. A great variation of resistance level was found within these two latter clones' categories. The dominance level of insecticide resistance (DLC) strongly suggested that the mutant allele 81T is semirecessive (the wild 81R allele being rather dominant) for both insecticide molecules under test. Mean DLC values were 0.316 for imidacloprid and 0.351 for thiacloprid. Cross-resistance was shown between imidacloprid and thiacloprid. This partial recessivity is valuable information to broaden the knowledge on neonicotinoid resistance, a prerequisite for devising adapted management strategies against insecticide-resistant populations of M. persicae.


Assuntos
Afídeos/efeitos dos fármacos , Afídeos/genética , Genótipo , Resistência a Inseticidas , Inseticidas/farmacologia , Animais , França , Imidazóis/farmacologia , Mutação , Neonicotinoides , Nitrocompostos/farmacologia , Piridinas/farmacologia , Tiazinas/farmacologia
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