Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 127
Filtrar
1.
J Antimicrob Chemother ; 79(4): 722-757, 2024 Apr 02.
Artigo em Inglês | MEDLINE | ID: mdl-38334389

RESUMO

BACKGROUND: Managing drug-food interactions may help to achieve the optimal action and safety profile of ß-lactam antibiotics. METHODS: We conducted a systematic review with meta-analyses in adherence to PRISMA guidelines for 32 ß-lactams. We included 166 studies assessing the impact of food, beverages, antacids or mineral supplements on the pharmacokinetic (PK) parameters or PK/pharmacodynamic (PK/PD) indices. RESULTS: Eighteen of 25 ß-lactams for which data on food impact were available had clinically important interactions. We observed the highest negative influence of food (AUC or Cmax decreased by >40%) for ampicillin, cefaclor (immediate-release formulations), cefroxadine, cefradine, cloxacillin, oxacillin, penicillin V (liquid formulations and tablets) and sultamicillin, whereas the highest positive influence (AUC or Cmax increased by >45%) for cefditoren pivoxil, cefuroxime and tebipenem pivoxil (extended-release tablets). Significantly lower bioavailability in the presence of antacids or mineral supplements occurred for 4 of 13 analysed ß-lactams, with the highest negative impact for cefdinir (with iron salts) and moderate for cefpodoxime proxetil (with antacids). Data on beverage impact were limited to 11 antibiotics. With milk, the extent of absorption was decreased by >40% for cefalexin, cefradine, penicillin G and penicillin V, whereas it was moderately increased for cefuroxime. No significant interaction occurred with cranberry juice for two tested drugs (amoxicillin and cefaclor). CONCLUSIONS: Factors such as physicochemical features of antibiotics, drug formulation, type of intervention, and patient's health state may influence interactions. Due to the poor actuality and diverse methodology of included studies and unproportionate data availability for individual drugs, we judged the quality of evidence as low.


Assuntos
Cefaclor , 60693 , Humanos , Cefaclor/farmacocinética , Cefuroxima/farmacologia , Penicilina V/farmacologia , Cefradina/farmacologia , Disponibilidade Biológica , Antiácidos , Streptococcus pneumoniae , Antibacterianos/farmacologia , beta-Lactamas/farmacologia , Monobactamas/farmacologia , Minerais/farmacologia , Testes de Sensibilidade Microbiana
2.
Pak J Pharm Sci ; 34(5(Supplementary)): 1989-1994, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34836871

RESUMO

The objective of this study was to deal with the evaluation of 7-(2-(benzylideneamino)-2-(cyclohexa-1,4-dienyl)acetamido)-3-methyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid based schiff bases as a new class of enzyme inhibitors. In this connection, a series of Schiff bases of cephradine with substituted aromatic aldehydes was synthesized and characterized using FTIR, 1HNMR and 13CNMR. The in-vitro biological activities including free radical scavenging potential using DPPH assay, acetyl cholinesterase and butyryl cholinesterase inhibition potential were evaluated. Two compounds of the series 1g and 1h were found to be active against AChE whereas no derivative was active against BChE while the whole series showed excellent 1, 1-diphenyl-2-picrylhydrazyl scavenging activity. All the synthesized compounds were found to be non-toxic and present passive gastrointestinal absorption. Furthermore, the study suggests that the synthesized cephradine derivatives exhibit inhibitory potential against different biologically relevant enzyme targets.


Assuntos
Antioxidantes/síntese química , Antioxidantes/farmacologia , Cefradina/química , Cefradina/farmacologia , Inibidores da Colinesterase/síntese química , Inibidores da Colinesterase/farmacologia , Acetilcolinesterase , Aldeídos/química , Compostos de Bifenilo , Butirilcolinesterase , Potenciais Pós-Sinápticos Excitadores/efeitos dos fármacos , Humanos , Simulação de Acoplamento Molecular , Estrutura Molecular , Picratos , Bases de Schiff , Relação Estrutura-Atividade
3.
Ecotoxicol Environ Saf ; 159: 56-62, 2018 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-29730409

RESUMO

Our research investigated the hormesis effect of cefradine on the specific growth rates (µ) of single-celled algae (Chlamydomonas reinhardtii) from aqueous solutions. We found the specific growth rate of C. reinhardtii slightly increased with cefradine concentrations within the range 0.5-10 mg/L. Effects of algae density, initial solution pH, and temperature on the adsorption batch assays were investigated. The optimum conditions for cefradine adsorption occurred at a density of 5 × 106 algae cells/mL, a solution pH of 7.0, and a temperature of 25.0 °C. A Box-Behnken design was employed to evaluate correlations between influential factors and cefradine adsorption. The results showed a significant interaction between algae density and temperature. The maximum removal rate could reach 50.13% under the optimal conditions. Additionally, the adsorption mechanisms were explored through Langmuir and Freundlich isotherm equations, adsorption kinetics, and thermodynamics. The results suggested that the adsorption process was monolayer, spontaneous, and endothermic with an increase in randomness at the algae-solution interface, which followed a pseudo-second-order model. All the data indicated that the alga performed a better removal capacity in the antibiotic-containing wastewater treatment process. This study lays the groundwork for a better understanding of the interaction mechanism between cefradine and Chlamydomonas reinhardtii in water solutions under dark condition.


Assuntos
Antibacterianos/química , Cefradina/química , Chlamydomonas reinhardtii/química , Eliminação de Resíduos Líquidos/métodos , Poluentes Químicos da Água/química , Adsorção , Antibacterianos/análise , Antibacterianos/farmacologia , Cefradina/análise , Cefradina/farmacologia , Chlamydomonas reinhardtii/efeitos dos fármacos , Chlamydomonas reinhardtii/genética , Concentração de Íons de Hidrogênio , Cinética , Soluções , Temperatura , Termodinâmica , Poluentes Químicos da Água/análise , Poluentes Químicos da Água/farmacologia , Purificação da Água/métodos
4.
J Vet Med Sci ; 79(10): 1633-1636, 2017 Oct 07.
Artigo em Inglês | MEDLINE | ID: mdl-28819087

RESUMO

This study was undertaken to investigate drug resistance in Escherichia coli (E. coli) strains isolated from bamboo rats in Zhejiang province of China. One hundred and fifty-four E. coli strains were isolated from dead bamboo rats. Polymerase chain reaction (PCR) was used to detect the representative genes encoding resistance to commonly used ß-lactam antibiotics. Highest resistance was observed for cefradine (24.03%), followed by penicillin (20.78%) and ceftazidime (20.13%). The isolation rates of ß-lactam resistance genes were 53.25, 48.70, 15.58 and 14.29% for bla TEM, bla CTX-M, bla OXA and bla SHV, respectively, while 62 (40.26%) E. coli isolates harbored multiple ß-lactam resistance genes. These results also suggested that long term use of these antibiotics leads to antibimicrobial resistance. We believe that this study will provide a guideline for veterinarians and a research basis for examining resistance-encoding genes in other food animals like bamboo rats.


Assuntos
Escherichia coli/efeitos dos fármacos , Resistência beta-Lactâmica/genética , Animais , Ceftazidima/farmacologia , Cefradina/farmacologia , China/epidemiologia , Escherichia coli/genética , Feminino , Genes Bacterianos/genética , Masculino , Testes de Sensibilidade Microbiana , Penicilinas/farmacologia , Reação em Cadeia da Polimerase/veterinária , Ratos/microbiologia
5.
Lab Chip ; 16(16): 3130-8, 2016 08 02.
Artigo em Inglês | MEDLINE | ID: mdl-27452345

RESUMO

Antimicrobial resistance (AMR) is a rapidly increasing threat to the effective treatment of infectious diseases worldwide. The two major remedies include: (1) using narrow-spectrum antibiotics based on rapid diagnosis; and (2) developing new antibiotics. A key part of both remedies is the antimicrobial susceptibility test (AST). However, the current standard ASTs that monitor colony formation are costly and time-consuming and the new strategies proposed are not yet practical to be implemented. Herein, we report a strategy to fabricate whole-hydrogel microfluidic chips using alginate-doped agar. This agar-based microfabrication makes it possible to prepare inexpensive hydrogel devices, and allows a seamless link between microfluidics and conventional agar-based cell culture. Different from common microfluidic systems, in our system the cells are cultured on top of the device, similar to normal agar plate culture; on the other hand, the microfluidic channels inside the hydrogel allow precise generation of linear gradient of drugs, thus giving a better performance than the conventional disk diffusion method. Cells in this system are not exposed to any shear flow, which allows the reliable tracking of individual cells and AST results to be obtained within 2-3 hours. Furthermore, our system could test the synergistic effect of drugs through two-dimensional gradient generation. Finally, the platform could be directly implemented to new drug discovery and other applications wherein a fast, cost-efficient method for studying the response of microorganisms upon drug administration is desirable.


Assuntos
Antibacterianos/farmacologia , Escherichia coli/efeitos dos fármacos , Hidrogéis/química , Dispositivos Lab-On-A-Chip , Testes de Sensibilidade Microbiana/instrumentação , Ágar/química , Alginatos/química , Ampicilina/farmacologia , Cefradina/farmacologia , Difusão , Desenho de Equipamento , Escherichia coli/crescimento & desenvolvimento , Escherichia coli/metabolismo , Gentamicinas/farmacologia , Ácido Glucurônico/química , Proteínas de Fluorescência Verde/genética , Proteínas de Fluorescência Verde/metabolismo , Ácidos Hexurônicos/química , Temperatura Alta , Microscopia de Fluorescência , Organismos Geneticamente Modificados
6.
Oncotarget ; 7(17): 24633-45, 2016 Apr 26.
Artigo em Inglês | MEDLINE | ID: mdl-27016423

RESUMO

Skin inflammation, and skin cancer induced by excessive solar ultraviolet (SUV) is a great threat to human health. SUV induced skin inflammation through activating p38 mitogen-activated protein kinase (p38) and c-Jun N-termeinal kinases (JNKs). T-LAK cell-originated protein kinase (TOPK) plays an important role in this process. Herein, the clinical data showed TOPK, phospho-p38, phospho-JNKs were highly expressed in human solar dermatitis. Ex vivo studies showed that SUV induced the phosphorylation of p38 and JNKs in HaCat and JB6 cells in a dose and time dependent manner. Molecule docking model indicated cefradine, an FDA-approved cephalosporin antibiotic, directly binds with TOPK. The result of in vitro binding assay verified cefradine can directly bind with TOPK. In vitro kinase results showed cefradine can inhibit TOPK activity. Ex vivo studies further showed cefradine inhibited SUV-induced the phosphorylation level of p38, JNKs and H2AX through inhibiting TOPK activity in a dose and time dependent manner, and cefradine inhibited the secretion of IL6 and TNF-α in HaCat and JB6 cells. In vivo studies showed that cefradine down-regulated SUV-induced the phosphorylation of p38, JNKs and H2AX and inhibited the secretion of IL6 and TNF-α in Babl/c mice. These results indicated that cefradine can inhibit SUV-induced skin inflammation by blocking TOPK signaling pathway, and TOPK is an effective target for suppressing inflammation induced by SUV irradiation.


Assuntos
Cefradina/farmacologia , Dermatite/prevenção & controle , Quinases de Proteína Quinase Ativadas por Mitógeno/antagonistas & inibidores , Raios Ultravioleta/efeitos adversos , Animais , Linhagem Celular , Dermatite/enzimologia , Dermatite/etiologia , Humanos , Queratinócitos/efeitos dos fármacos , Queratinócitos/enzimologia , MAP Quinase Quinase 4/metabolismo , Camundongos , Camundongos Endogâmicos BALB C , Quinases de Proteína Quinase Ativadas por Mitógeno/metabolismo , Simulação de Acoplamento Molecular , Transdução de Sinais , Pele/efeitos dos fármacos , Pele/patologia , Pele/efeitos da radiação , Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo
7.
Ecotoxicology ; 24(7-8): 1788-97, 2015 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-26141733

RESUMO

Binary pollution of both heavy metals and antibiotics has received increasing attentions for their joint effects of eco-toxicity and health hazards. To reveal the effects of mixtures of different pollutants on bacterial antioxidant response system, Pseudomonas fluorescens ZY2, a new strain isolated from swine wastewater, was chosen to determinate growth (bacterial density OD600), reactive oxygen species (ROS) concentration, protein concentration and superoxide dismutase (SOD) activity under exposure treatments of Zn, Cefradine or Zn + Cefradine. Bacterial densities of all the treatment groups increased significantly over the incubation time, but those containing pollutant addition were slightly lower than the control at different times of incubation. Both ROS concentration and SOD activity increased first and then decreased (p < 0.01) over time, which was opposite to the protein concentrations (p < 0.01), showing a much significant increase by Cefradine alone. With Zn concentration increasing from 40 to 160 mg/L, the intracellular SOD activity increased as a response to the improvement of ROS (p < 0.05), while the balance between ROS and SOD was broken down due to the disproportionate change of total SOD activity and ROS concentration, the bacterial densities therefore decreased for the weak resistance. With the combined treatment of Zn (200 mg/L) and Cefradine (1 mg/L), though the toxicity of Zn caused a much significant increase of ROS, the bacterial resistance was further improved showing a more significant increase of total SOD activity and the bacterial densities therefore increased bacterial growth. Zn concentration also affected the protein synthesis. Either single or binary stress induced the bacterial resistance by regulating SOD activity to eliminate ROS. All results of the bacterial oxidant stress, SOD response and protein synthesis in the combined treatment groups were more complicated than those in single treatment groups, which depended on the properties of the single treatment as well as the interaction between the two treatments upon bacterial activity. For P. fluorescens ZY2, the mediation of SOD activity to eliminate ROS in response to the combined exposure to Zn and Cefradine was first revealed as one of the co-resistance mechanisms, which is informative to further understanding the risk of antibiotics resistant bacteria to human and environmental health more accurately.


Assuntos
Antioxidantes/metabolismo , Cefradina/farmacologia , Farmacorresistência Bacteriana , Pseudomonas fluorescens/efeitos dos fármacos , Pseudomonas fluorescens/fisiologia , Zinco/farmacologia , Criação de Animais Domésticos , Animais , Antibacterianos/farmacologia , Proteínas de Bactérias/genética , Proteínas de Bactérias/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Superóxido Dismutase/metabolismo , Sus scrofa , Águas Residuárias
8.
Ecotoxicology ; 24(4): 835-43, 2015 May.
Artigo em Inglês | MEDLINE | ID: mdl-25678231

RESUMO

A better understanding on the mechanism involved in bacterial resistance to combined exposure to antibiotics and heavy metals is helpful in implementing practices to mitigate their ecological risk and spread of resistance genes in microbial population. Pseudomonas fluorescens ZY2, a strain isolated from swine wastewater, was chosen to study its growth (bacterial density OD600), the formation of reactive oxygen species (ROS), nitric oxide (NO) and NO synthases (NOS) under Zn, cefradine or Zn + cefradine treatments. Using Zn and cefradine as representative heavy metal and antibiotic in this investigation, respectively, the resistance of P. fluorescens ZY2 to toxic chemical exposure was investigated. Bacterial densities of treatment groups significantly increased over the time of incubation, but less than the control. ROS, NO and NOS initially increased, but then decreased after the initial 8 h of culturing, and were positively related to Zn concentrations. Moreover, the formation of ROS, NOS, and NO was activated by cefradine at Zn of up to 160 mg/L, but inhibited at Zn of 200 mg/L whether cefradine was added or not. Zn concentration affected ROS and NO concentrations between treatments and also was closely related to the variation of the relative bacterial density. For P. fluorescens ZY2, the mediation of endogenous NO to overcome ROS in response to the combined exposure of Zn and cefradine was suggested as a co-resistance mechanism, which would be beneficial to evaluate the ecological risk of heavy metals and antibiotics.


Assuntos
Antibacterianos/farmacologia , Cefradina/farmacologia , Pseudomonas fluorescens/efeitos dos fármacos , Poluentes Químicos da Água/farmacologia , Zinco/farmacologia , Animais , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase/metabolismo , Pseudomonas fluorescens/enzimologia , Pseudomonas fluorescens/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Sus scrofa , Águas Residuárias/análise
9.
Food Chem Toxicol ; 78: 116-21, 2015 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-25684417

RESUMO

The present work evaluated the combined effects of cefradine and ceftazidime on the green alga Chlorella pyrenoidosa using response surface methodologies (RSM). After a 48 h-exposure, the population growth rate (PGR), the chlorophyll-a content and the SOD content of the alga increased with increased concentrations of two antibiotics. However, the three responses did not continue to demonstrate significant increases once antibiotic concentrations exceed a moderate level. Three two order polynomial regression equations were obtained to describe well the relationship between the responses of the alga and the two antibiotics' concentration (R(2) = 0.9997, 0.9292 and 0.9039, respectively). Three 3 D-surface graphs and their contour plots showed directly the changing trends of the alga under the combined effects of two antibiotics. This study for the first time employed the RSM in ecotoxicology, which indicated that the RSM should be placed under a feasible and a potential application prospect in toxicity assessment.


Assuntos
Ceftazidima/farmacologia , Cefradina/farmacologia , Chlorella/efeitos dos fármacos , Antibacterianos/farmacologia , Chlorella/metabolismo , Clorofila/metabolismo , Clorofila A , Superóxido Dismutase/metabolismo
10.
Int J Mol Sci ; 16(2): 2839-50, 2015 Jan 27.
Artigo em Inglês | MEDLINE | ID: mdl-25633105

RESUMO

A Pseudomonas fluorescens strain ZY2, isolated from swine wastewater, was used to investigate the synergistic effects of five heavy metals (Pb, Cu, Zn, Cr(VI) and Hg) on bacterial resistance to antibiotics. Results indicate that the combined effects of antibiotic type, heavy metal type and concentration were significant (p < 0.01). Cross-resistance to Hg and antibiotics was the most noticeable. Moreover, the resistance to Hg and cefradine or amoxicillin, and Cr and amoxicillin were synergistic for low heavy metal concentrations, and turned antagonistic with increasing concentrations, while the resistances to Cr or Cu and cefradine, Pb or Cu and amoxicillin, Cu and norfloxacin showed reverse effects. In addition, resistance to Zn and amoxicillin were always synergetic, while resistance to Pb and cefradine or norfloxacin, Cr or Hg and norfloxacin as well as all the heavy metals and tetracycline were antagonistic. These results indicate that bacterial resistance to antibiotics can be affected by the type and concentration of co-exposed heavy metals and may further threaten people's health and ecological security severely via horizontal gene transfer.


Assuntos
Antibacterianos/farmacologia , Metais Pesados/toxicidade , Pseudomonas fluorescens/efeitos dos fármacos , Águas Residuárias/microbiologia , Amoxicilina/farmacologia , Animais , Cefradina/farmacologia , Farmacorresistência Bacteriana , Testes de Sensibilidade Microbiana , Norfloxacino/farmacologia , Pseudomonas fluorescens/isolamento & purificação , Suínos
11.
J Periodontol ; 85(2): 327-34, 2014 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-23659425

RESUMO

BACKGROUND: This study attempts to determine the antimicrobial resistance profiles of obligate anaerobic bacteria that were isolated from a periodontal abscess and to evaluate the prevalence of resistance genes in these bacteria. METHODS: Forty-one periodontal abscess samples were cultivated on selective and non-selective culture media to isolate the oral anaerobes. Their antibiotic susceptibilities to clindamycin, doxycycline, amoxicillin, imipenem, cefradine, cefixime, roxithromycin, and metronidazole were determined using the agar dilution method, and polymerase chain reaction assays were performed to detect the presence of the ermF, tetQ, nim, and cfxA drug resistance genes. RESULTS: A total of 60 different bacterial colonies was isolated and identified. All of the isolates were sensitive to imipenem. Of the strains, 6.7%, 13.3%, 16.7%, and 25% were resistant to doxycycline, metronidazole, cefixime, and amoxicillin, respectively. The resistance rate for both clindamycin and roxithromycin was 31.7%. Approximately 60.7% of the strains had the ermF gene, and 53.3% of the amoxicillin-resistant strains were found to have the cfxA gene. Two nim genes that were found in eight metronidazole-resistant strains were identified as nimB. CONCLUSIONS: In the present study, the Prevotella species are the most frequently isolated obligate anaerobes from periodontal abscesses. The current results show their alarmingly high resistance rate against clindamycin and roxithromycin; thus, the use of these antibiotics is unacceptable for the empirical therapy of periodontal abscesses. A brief prevalence of four resistance genes in the anaerobic bacteria that were isolated was also demonstrated.


Assuntos
Bactérias Anaeróbias/genética , Farmacorresistência Bacteriana/genética , Genes Bacterianos/genética , Abscesso Periodontal/microbiologia , Amoxicilina/farmacologia , Antibacterianos/farmacologia , Bactérias Anaeróbias/classificação , Proteínas de Bactérias/genética , Técnicas Bacteriológicas , Infecções por Bacteroidaceae/microbiologia , Cefixima/farmacologia , Cefradina/farmacologia , Clindamicina/farmacologia , Doxiciclina/farmacologia , Feminino , Humanos , Imipenem/farmacologia , Masculino , Metiltransferases/genética , Metronidazol/farmacologia , Pessoa de Meia-Idade , Prevotella/classificação , Prevotella/genética , Roxitromicina/farmacologia , Resistência a Tetraciclina/genética , Resistência beta-Lactâmica/genética , beta-Lactamases/genética
12.
Pak J Pharm Sci ; 26(5): 953-9, 2013 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-24035952

RESUMO

The astounding and exceptional growth of generic pharmaceutical Industry in Pakistan has raised certain questions for drug regulatory authorities contemplating their efficacy and quality. The current study focuses on assessing the in-vitro antimicrobial activity of 24 brands of Cephradine 500mg capsules against 4 different strains by employing standardized methods. Disk diffusion method was performed on all brands to look into the susceptibility and resistance patterns. Standard disk of 5µg Cephradine powder were used during evaluation. The zones of inhibitions were ranged from 24-40mm against S. aureus, 24-40mm against E. coli, 20-25mm against K. pneumonia and 19-23mm P. mirabilis. On the basis of mean value, the multinational brands were found to have better zone of inhibitions and were better than local Pharmaceutical companies but ANOVA cooperative study showed that all brands of Cephradine showed similar comparable results. Further investigations by employing MIC method, quality of raw material with special emphasis on the shelf-life, excepients and method of manufacturing will be needed to obtain more authenticated results. The price of National and Multinational brands ranges from Rs.156.00-212.00 for 10 capsules. It is concluded that Public health is at risk because of noticeable growing widespread curse of the manufacture and trade of sub-standard or below par pharmaceuticals. The pecuniary accountability of management of pharmaceutical agents is additionally apparent. The results of the study need to be made public to boost the confidence of medical profession about the quality of locally manufactured pharmaceuticals. It will succour the foreign exchange being incurred on the trade in of medicines.


Assuntos
Antibacterianos/farmacologia , Bactérias/efeitos dos fármacos , Cefradina/farmacologia , Medicamentos Genéricos/farmacologia , Análise de Variância , Antibacterianos/normas , Bactérias/crescimento & desenvolvimento , Cápsulas , Cefradina/normas , Química Farmacêutica , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Medicamentos Genéricos/normas , Controle de Qualidade
13.
J Clin Pharmacol ; 49(3): 360-7, 2009 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-19246733

RESUMO

Intestinal peptide transporters, including hPEPT1, facilitate the absorption of cephalosporins and angiotensin-converting enzyme inhibitors, and have been investigated as a means to improve oral drug absorption. Renal peptide transporters including hPEPT2, may also facilitate renal reabsorption of such compounds. In vitro and animal studies suggest that co-administration of peptidomimetic compounds may alter oral pharmacokinetics, although this has not been well studied in humans. The purpose of this study was to determine whether co-administration of the hPEPT substrates captopril and cephradine alters the oral pharmacokinetics of either agent. Nine healthy male volunteers received a single oral 25-mg dose of captopril, a single oral 500-mg dose of cephradine, or concurrent ingestion of captopril and cephradine in a cross-over manner. Venous blood samples were taken and captopril and cephradine pharmacokinetics were determined using noncompartmental analyses. No significant differences were observed in captopril or cephradine pharmacokinetics when administered together as compared to each agent alone (a marginal decrease in C(max) was observed for both captopril and cephradine during co-administration [5-15%]; however, differences were not statistically significant). The results of our study suggest that hPEPT1 and hPEPT2 are unlikely to contribute to clinically important drug interactions in humans.


Assuntos
Inibidores da Enzima Conversora de Angiotensina/farmacologia , Antibacterianos/farmacologia , Captopril/farmacologia , Cefradina/farmacologia , Absorção Intestinal/efeitos dos fármacos , Simportadores/fisiologia , Adulto , Inibidores da Enzima Conversora de Angiotensina/metabolismo , Antibacterianos/metabolismo , Transporte Biológico , Captopril/metabolismo , Cefradina/metabolismo , Estudos Cross-Over , Interações Medicamentosas , Humanos , Rim/metabolismo , Masculino , Transportador 1 de Peptídeos
14.
Yao Xue Xue Bao ; 44(10): 1127-30, 2009 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-20055136

RESUMO

The effects of cephradinum and ceftazidime on the metabolism of Escherichia coli (E. coli) DH5alpha was determined by microcalorimetry. The microbial activity was recorded as power-time curves through an ampoule method with a TAM Air Isothermal Microcalorimeter at 37 degrees C. The parameters such as the growth rate constant (k), inhibitory ratio (I), the maximum power output (Pm) and the time (tm) corresponding to the maximum power output were calculated. The results show that the ceftazidime has a better inhibitory effect on E. coli DH5alpha than cephradinum.


Assuntos
Antibacterianos/farmacologia , Calorimetria/métodos , Ceftazidima/farmacologia , Cefradina/farmacologia , Escherichia coli/efeitos dos fármacos , Antibacterianos/administração & dosagem , Ceftazidima/administração & dosagem , Cefradina/administração & dosagem , Escherichia coli/crescimento & desenvolvimento , Escherichia coli/metabolismo , Testes de Sensibilidade Microbiana
15.
Acta Paediatr ; 97(12): 1681-5, 2008 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-18691162

RESUMO

AIM: To analyse the characteristics of Streptococcus pyogenes isolates from Chinese children with scarlet fever. METHODS: Minimal inhibitory concentration with nine antibiotics was performed on 145 Streptococcus pyogenes isolates acquired from Beijing and Shanghai in 2007. Their macrolide-resistant genes (mefA, ermB and ermA- a subclass of ermTR), superantigens (speA and speC), and en-coding mature M protein gene (emm gene) were amplified by PCR. RESULTS: A total of 97.9% of the isolates exhibited resistance to the macrolides, while 96.6% manifested resistance to tetracycline. All isolates were sensitive to chloramphenicol, penicillin, cefradine, and ofloxacin. Moreover, 94.5% exhibited a cMLSB phenotype, while 90.3% had the ermB gene. Five emm types (emm1.0, emm4.0, emm12.0, emm22.0 and st5240) were discovered, of which 9.7% carried the superantigen speA, 35.9% carried the speC, 42.8% carried both speA and speC and 11.7% carried neither speA nor speC. Finally, 85.5% of emm1.0 and 15.5% of emm12.0 isolates carried speA, while 79.0% of emm1.0 and 75.9% of emm12.0 isolates carried speC. CONCLUSION: The Streptococcus pyogenes isolates had high resistance rates against macrolides and tetracycline. They mainly expressed the ermB gene type and cMLSB phenotype. Their common emm types are emm1.0 and emm12.0, which have different frequencies of speA and speC.


Assuntos
Farmacorresistência Bacteriana/efeitos dos fármacos , Escarlatina/microbiologia , Streptococcus pyogenes/isolamento & purificação , Antibacterianos/farmacologia , Proteínas da Membrana Bacteriana Externa/genética , Cefradina/farmacologia , Criança , Pré-Escolar , China , Cloranfenicol/farmacologia , Clindamicina/farmacologia , Farmacorresistência Bacteriana/genética , Farmacorresistência Bacteriana/imunologia , Humanos , Macrolídeos/farmacologia , Testes de Sensibilidade Microbiana/métodos , Ofloxacino/farmacologia , Penicilinas/farmacologia , Fenótipo , Reação em Cadeia da Polimerase , Streptococcus pyogenes/genética , Streptococcus pyogenes/imunologia , Superantígenos/genética , Tetraciclinas/farmacologia
16.
Pak J Pharm Sci ; 18(1): 36-42, 2005 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-16431381

RESUMO

Cephradine, the first generation cephalosporin, is active against a wide range of Gram-positive and Gram-negative bacteria including penicillinase-producing Staphylococci. Since the presence of complexing ligand may affect the bioavailability of a metal in the blood or tissues, therefore, in order to study the probable interaction of cephradine with essential and trace elements present in human body, cephradine has been reacted with cobalt, copper, zinc and cadmium metal halides in L:M ratio of 2:1 in methanol and the products recrystallized from suitable solvents to pure crystals of consistent melting points. Infrared and ultraviolet studies of these complexes were carried out and compared with ligand. Magnetic susceptibility studies of these complexes were also carried out showing their paramagnetic behavior. From the infra red studies and elemental analysis of the complexes, it has been shown that the drug molecule serves as a bidentate ligand coordinating through both its carboxylate at C-3 and beta-lactam nitrogen and the metal having a square planar or octahedral geometry. To evaluate the changes in microbiological activity of cephradine after complexation, antibacterial studies were carried out by observing the changes in MIC (minimum inhibitory concentration) of the complexes and compared with the parent drug by measuring the zone of inhibition of complexes and compared with the parent cephalosporin against both Gram-positive and Gram-negative organisms. For MIC observation, serial dilution method was employed and zone series were determined by disk diffusion method. Our investigations reveal that formation of complexes results in decrease in antibacterial activity of cephradine and MIC values are increased.


Assuntos
Antibacterianos/síntese química , Cefradina/análogos & derivados , Metais Pesados/química , Antibacterianos/química , Antibacterianos/farmacologia , Cádmio/química , Cefradina/farmacologia , Cobalto/química , Cobre/química , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Negativas/crescimento & desenvolvimento , Bactérias Gram-Positivas/efeitos dos fármacos , Bactérias Gram-Positivas/crescimento & desenvolvimento , Zinco/química
17.
J Antimicrob Chemother ; 47(3): 305-13, 2001 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-11222563

RESUMO

Routine susceptibility data for urinary coliform isolates from community practice were analysed in comparison with dispensed antibiotic prescriptions for all conditions and social deprivation data for Bro Taf and North Wales Health Authorities for financial years 1996--1998. Prescribing rates and resistance rates varied widely between practices. Among isolates from practices with high usage of an antibiotic, rates of resistance to that antibiotic tended to be high, and usage correlated significantly with resistance between practice population units. Cross-correlations were found between usage of one antibiotic and resistance to another, particularly for trimethoprim and ampicillin. Usage, particularly of trimethoprim, was associated with multi-resistance to up to four antibiotics. Resistance was more frequent in isolates from males, children and the elderly. Ampicillin resistance correlated with social deprivation. Analyses including or excluding potential repeat isolates yielded closely similar results. Indices reflecting sampling behaviour (laboratory coliform positivity rates, positivity per 1000 registered patients, specimens submitted per 1000 registered patients) varied widely between surgeries, suggesting lack of consensus on urine sampling policies. These indices showed only weak correlations with usage or resistance. Associations between resistance and usage were compared for isolates from two patient subsets that were likely to differ in their proportions of non-Escherichia coli isolates: female patients aged 16--55 years; and males, children and patients aged >55 years. The latter showed higher base levels of resistance, but the associations of resistance with usage were statistically indistinguishable for the two populations. The results suggest that usage of antibiotics in a practice population may affect the rate of urinary infection caused by resistant coliform organisms in that population.


Assuntos
Antibacterianos/farmacologia , Infecções Comunitárias Adquiridas/microbiologia , Resistência Microbiana a Medicamentos , Enterobacteriaceae/efeitos dos fármacos , Infecções Urinárias/microbiologia , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Combinação Amoxicilina e Clavulanato de Potássio/farmacologia , Ampicilina/farmacologia , Cefalexina/farmacologia , Cefradina/farmacologia , Criança , Pré-Escolar , Ciprofloxacina/farmacologia , Infecções Comunitárias Adquiridas/urina , Enterobacteriaceae/crescimento & desenvolvimento , Enterobacteriaceae/isolamento & purificação , Infecções por Enterobacteriaceae/microbiologia , Feminino , Humanos , Recém-Nascido , Masculino , Testes de Sensibilidade Microbiana , Pessoa de Meia-Idade , Trimetoprima/farmacologia
18.
J Microencapsul ; 17(5): 615-24, 2000.
Artigo em Inglês | MEDLINE | ID: mdl-11038120

RESUMO

The physical entrapment of a hydrophilic drug within degradable microspheres is generally difficult because of poor entrapment yield and/or fast release, depending on the microsphere fabrication method. In order to counter the effects of drug hydrophilicity, it is proposed to covalently attach the drug to lactic acid oligomers, with the aim of achieving temporary hydrophobization and slower release controlled by the separation of the drug from the degradable link within the polymer matrix. This strategy was tested on microspheres of the antibiotic cephradin. As the prodrug form, the entrapment of the drug was almost quantitative. The prodrug did degrade in an aqueous medium, modelling body fluids, but cleavage did not occur at the drug-oligomer junction and drug molecules bearing two lactyl residual units were released. When the prodrug is entrapped within a PLAGA matrix, no release was observed within the experimental time period. However, data suggest that conjugation via a bond more sensitive to hydrolysis than the main chain PLA ester bonds should make the system work as desired.


Assuntos
Cefradina/administração & dosagem , Composição de Medicamentos/métodos , Sistemas de Liberação de Medicamentos , Ácido Láctico , Ácido Poliglicólico , Polímeros , Biodegradação Ambiental , Cápsulas , Cefradina/farmacologia , Preparações de Ação Retardada , Escherichia coli/efeitos dos fármacos , Técnicas In Vitro , Copolímero de Ácido Poliláctico e Ácido Poliglicólico , Staphylococcus aureus/efeitos dos fármacos
19.
Rev. méd. Chile ; 128(7): 749-57, jul. 2000. tab
Artigo em Espanhol | LILACS | ID: lil-270885

RESUMO

Background: Second generation cephalosporins (CFPs) are more active in the treatment of acute pyelonephritis during pregnancy but their cost is considerably higher than their predecessors. Cefuroxime, a second generation CFP with oral and parenteral presentations, might offer significant advantages and become a first choice antimicrobial in this setting. Aim: To compare the efficacy, safety and cost of cefuroxime and cephradine in the treatment of acute pyelonephritis in pregnancy. Patients and methods: Hospitalized women with 12 to 34 weeks of pregnancy, with clinical and bacteriological diagnosis of acute pyelonephritis, were randomly assigned to receive cefuroxime (Curocef (r), GlaxoWellcome) 750 mg t.i.d, i.v or cephradine 1 g q.i.d., i.v. If the isolated organism was resistant to the assigned drug the patient was excluded. Once patients were afebrile, they were switched to an oral form of the same antimicrobial. They were discharged according to the clinical status and treated for a total of 14 days. Laboratory tests, including urine culture were requested during controls and at the end of follow-up at 28 days. Results: One hundred and one patients were randomized: 49 to receive cephradine and 52 to receive cefuroxime. Patients in the cefuroxime group had fewer febrile days (mean 1.7 vs 2.2, p<0.05), faster clinical recovery (mean 2.7 vs 3.1 days, p<0.05), a higher rate of bacteriological cure at 28 days (78.8 percent and 59.2 percent, p<0.05) and lower rate of failure (21.2 percent vs 40.8 percent p<0.05). The rate of resistance of isolated uropathogens was l4 percent to cephradine and 1 percent to cefuroxime. Conclusions: Cefuroxime can be considered as a first choice option in the treatment of acute pyelonephritis during pregnancy due to its tolerance, microbiological activity and efficacy


Assuntos
Humanos , Feminino , Adulto , Complicações Infecciosas na Gravidez/etiologia , Complicações Infecciosas na Gravidez/tratamento farmacológico , Pielonefrite/tratamento farmacológico , Cefuroxima/farmacologia , Cefradina/farmacologia , Paridade , Pielonefrite/economia , Pielonefrite/etiologia , Urina/microbiologia , Estudos Prospectivos , Resultado do Tratamento , Escherichia coli/isolamento & purificação , Escherichia coli/efeitos dos fármacos , Escherichia coli/patogenicidade , Custos de Cuidados de Saúde/estatística & dados numéricos , Tempo de Internação/estatística & dados numéricos
20.
Med Dosw Mikrobiol ; 51(3-4): 413-9, 1999.
Artigo em Polonês | MEDLINE | ID: mdl-10803271

RESUMO

The aim of the study was to determine the influence of certain antibiotics on the production of IFN-gamma by mouse lymphocytes T after four days incubation with Listeria monocytogenes. The level of mouse IFN-gamma was determined by ELISA method (Inter Test-gamma Mouse IFN-gamma Kit, Genzyme). The strongest immunosuppression effect was demonstrated using rifampicin (39 ng/ml IFN-gamma) (Control: 123 +/- 29 ng/ml IFN-gamma, p < 0.05). Lower immunosuppression effects were observed also with cephradine (54 ng/ml IFN-gamma), amikacin (56 ng/ml IFN-gamma) and ticarcillin (83 ng/ml). The obtained results show that all tested cephalosporins (cephamandole, cefotaxime, cephradine) and aminogllycosides (gentamicin, streptomycin, amicacin) inhibit production of IFN-gamma by mouse lymphocytes T. The influence of penicillin G and ampicillin, as well as, erythromycin and lincomycin on the production IFN-gamma was not observed. Our results suggest that rifampicin, ticarcillin, cephalosporins and aminoglycosides act as inhibitors of production IFN-gamma.


Assuntos
Antibacterianos/farmacologia , Interferon gama/biossíntese , Linfócitos T/efeitos dos fármacos , Amicacina/farmacologia , Animais , Células Cultivadas , Cefalosporinas/farmacologia , Cefradina/farmacologia , Ensaio de Imunoadsorção Enzimática , Listeria monocytogenes/imunologia , Camundongos , Penicilinas/farmacologia , Rifampina/farmacologia , Linfócitos T/imunologia , Linfócitos T/metabolismo , Ticarcilina/farmacologia
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA
...