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1.
Ann Hepatol ; 18(6): 841-848, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31611065

RESUMO

INTRODUCTION AND OBJECTIVES: Limited data describe current SBP epidemiology and specific secondary SBP prophylactic regimens, leading to variable prescribing practices. This work aims to compare 90-day and one-year SBP recurrence and mortality based on secondary SBP antibiotic prophylaxis regimens. MATERIALS AND METHODS: We performed a retrospective cohort of patients >18 years with an SBP diagnosis from 2010 to 2015 at two academic institutions. Eligible patients had ascitic PMN counts ≥250cells/mm3 or a positive ascitic culture. Patients were compared based on secondary SBP prophylaxis regimens (i.e., daily, intermittent, or no prophylaxis). RESULTS: Of 791 patients with ascitic fluid samples, 86 patients were included. Antibiotic prophylaxis included daily (n=34), intermittent (n=36), or no prophylaxis (n=16). Nearly half of SBP episodes had a positive ascitic fluid culture; 50% were gram-negative pathogens, and 50% were gram-positive pathogens. Daily and intermittent regimens had similar rates of recurrence at 90-days (19.4% vs. 14.7%, p=0.60) and one-year (33.3% vs. 26.5%, p=0.53). Similarly, mortality did not differ among daily and intermittent regimens at 90-days (32.4% vs. 30.6%, p=0.87) or one-year (67.6% vs. 63.9%, p=0.74). When comparing any prophylaxis vs. no prophylaxis, there were no differences in 90-day or one-year recurrence or mortality. CONCLUSIONS: In patients with a history of SBP, our data indicate similar outcomes with daily, intermittent, or no secondary antibiotic prophylaxis. With available data, including ours, demonstrating a changing epidemiology for SBP pathogens, further data is required to determine if traditional approaches to secondary SBP prophylaxis remain appropriate.


Assuntos
Antibacterianos/administração & dosagem , Infecções Bacterianas/prevenção & controle , Peritonite/prevenção & controle , Idoso , Ascite/etiologia , Líquido Ascítico , Infecções Bacterianas/etiologia , Infecções Bacterianas/mortalidade , Estudos de Casos e Controles , Ceftizoxima/administração & dosagem , Ceftizoxima/análogos & derivados , Quimioprevenção/métodos , Ciprofloxacina/administração & dosagem , Estudos de Coortes , Feminino , Humanos , Estimativa de Kaplan-Meier , Cirrose Hepática/complicações , Modelos Logísticos , Masculino , Pessoa de Meia-Idade , Moxifloxacina/administração & dosagem , Análise Multivariada , Peritonite/etiologia , Peritonite/mortalidade , Modelos de Riscos Proporcionais , Recidiva , Estudos Retrospectivos , Combinação Trimetoprima e Sulfametoxazol/administração & dosagem , Cefpodoxima
2.
Acta Cir Bras ; 33(1): 14-21, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29412229

RESUMO

PURPOSE: To compare the influence of two metallic implants in the diagnosis of periprosthetic infection using 99m technetium-labeled ceftizoxime. METHODS: Twenty rats were randomly divided into four groups, which received sterile and contaminated titanium and stainless steel implants. After 3 weeks, scintilographic images were obtained using a gamma chamber. Radioactivity counts were obtained for the region of interest (ROI) on the operated and non-operated paws. RESULTS: Groups A, B, and C showed homogenous distribution of the radiopharmaceutical. Hyper uptake was observed in the operated paw from group D. The ROI target count was higher in the two groups with stainless steel implants. Among the control groups, the count was higher in the stainless steel group. Furthermore, among the contaminated groups, the uptake was higher in the stainless steel group, with a significant difference. The target: non-target ratio was significantly lower in the control and contaminated groups with both titanium and stainless steel, but the comparison between control groups and contaminated groups was only significant in the former. The cpm/g observed after a decay of 48h showed statistically significant differences between groups. CONCLUSION: Different biomaterials used in implants have an influence on the results of scintigraphy with 99mTc-CFT.


Assuntos
Ceftizoxima/análogos & derivados , Compostos de Organotecnécio , Infecções Relacionadas à Prótese/diagnóstico por imagem , Compostos Radiofarmacêuticos , Aço Inoxidável/efeitos da radiação , Titânio/efeitos da radiação , Animais , Materiais Biocompatíveis/química , Infecções Relacionadas à Prótese/microbiologia , Radioatividade , Cintilografia , Distribuição Aleatória , Ratos Wistar , Valores de Referência , Reprodutibilidade dos Testes , Aço Inoxidável/química , Fatores de Tempo , Titânio/química
3.
Acta cir. bras ; Acta cir. bras;33(1): 14-21, Jan. 2018. tab, graf
Artigo em Inglês | LILACS | ID: biblio-886252

RESUMO

Abstract Purpose: To compare the influence of two metallic implants in the diagnosis of periprosthetic infection using 99m technetium-labeled ceftizoxime. Methods: Twenty rats were randomly divided into four groups, which received sterile and contaminated titanium and stainless steel implants. After 3 weeks, scintilographic images were obtained using a gamma chamber. Radioactivity counts were obtained for the region of interest (ROI) on the operated and non-operated paws. Results: Groups A, B, and C showed homogenous distribution of the radiopharmaceutical. Hyper uptake was observed in the operated paw from group D. The ROI target count was higher in the two groups with stainless steel implants. Among the control groups, the count was higher in the stainless steel group. Furthermore, among the contaminated groups, the uptake was higher in the stainless steel group, with a significant difference. The target: non-target ratio was significantly lower in the control and contaminated groups with both titanium and stainless steel, but the comparison between control groups and contaminated groups was only significant in the former. The cpm/g observed after a decay of 48h showed statistically significant differences between groups. Conclusion: Different biomaterials used in implants have an influence on the results of scintigraphy with 99mTc-CFT.


Assuntos
Animais , Aço Inoxidável/efeitos da radiação , Titânio/efeitos da radiação , Ceftizoxima/análogos & derivados , Compostos de Organotecnécio , Infecções Relacionadas à Prótese/diagnóstico por imagem , Compostos Radiofarmacêuticos , Radioatividade , Valores de Referência , Aço Inoxidável/química , Fatores de Tempo , Titânio/química , Materiais Biocompatíveis/química , Distribuição Aleatória , Cintilografia , Reprodutibilidade dos Testes , Infecções Relacionadas à Prótese/microbiologia , Ratos Wistar
5.
Acta Cir Bras ; 30(9): 632-8, 2015 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-26465108

RESUMO

PURPOSE: To evaluate whether scintigraphy with technetium-99m-labeled ceftizoxime ((99m)Tc-CFT) can differentiate mediastinitis from aseptic inflammation associated with sternotomy. METHODS: Twenty female Wistar rats were randomly distributed into four groups: S (control) -partial upper median sternotomy with no treatment; SW (control) - sternotomy and treatment of sternal wounds with bone wax; SB - sternotomy and infection with Staphylococcus aureus; SWB - sternotomy with bone wax treatment and bacterial infection. Scintigraphy with (99m)Tc-CFT was performed eight days after surgery and images were collected 210 and 360 min after infusion of the radiopharmaceutical. RESULTS: No animals exhibited clinical signs of wound infection at the end of the experiment, although histological data verified acute inflammatory response in those experimentally infected with bacteria. Scintigraphic images revealed that tropism of (99m)Tc-CFT to infected sternums was greater than to their non-infected counterparts. Mean counts of radioactivity in bacteria-infected sternal regions (SB and SWB) were significantly higher (p = 0.0007) than those of the respective controls (S and SW). CONCLUSION: Scintigraphy with technetium-99m-labeled ceftizoxime is a method that can potentially detect infection post sternotomy and differentiate from aseptic inflammation in animals experimentally inoculated with S. aureus.


Assuntos
Ceftizoxima/análogos & derivados , Mediastinite/diagnóstico por imagem , Compostos de Organotecnécio , Esternotomia/efeitos adversos , Esterno/diagnóstico por imagem , Infecção da Ferida Cirúrgica/diagnóstico por imagem , Animais , Modelos Animais de Doenças , Feminino , Cintilografia , Distribuição Aleatória , Ratos Wistar , Reprodutibilidade dos Testes , Infecções Estafilocócicas/diagnóstico por imagem , Staphylococcus aureus , Esterno/microbiologia , Infecção da Ferida Cirúrgica/microbiologia
6.
Acta cir. bras ; Acta cir. bras;30(9): 632-638, Sep. 2015. tab, ilus
Artigo em Inglês | LILACS | ID: lil-761493

RESUMO

PURPOSE:To evaluate whether scintigraphy with technetium-99m-labeled ceftizoxime (99mTc-CFT) can differentiate mediastinitis from aseptic inflammation associated with sternotomy.METHODS:Twenty female Wistar rats were randomly distributed into four groups: S (control) -partial upper median sternotomy with no treatment; SW (control) - sternotomy and treatment of sternal wounds with bone wax; SB - sternotomy and infection with Staphylococcus aureus; SWB - sternotomy with bone wax treatment and bacterial infection. Scintigraphy with 99mTc-CFT was performed eight days after surgery and images were collected 210 and 360 min after infusion of the radiopharmaceutical.RESULTS: No animals exhibited clinical signs of wound infection at the end of the experiment, although histological data verified acute inflammatory response in those experimentally infected with bacteria. Scintigraphic images revealed that tropism of 99mTc-CFT to infected sternums was greater than to their non-infected counterparts. Mean counts of radioactivity in bacteria-infected sternal regions (SB and SWB) were significantly higher (p = 0.0007) than those of the respective controls (S and SW).CONCLUSION:Scintigraphy with technetium-99m-labeled ceftizoxime is a method that can potentially detect infection post sternotomy and differentiate from aseptic inflammation in animals experimentally inoculated with S. aureus.


Assuntos
Animais , Feminino , Ceftizoxima/análogos & derivados , Mediastinite , Compostos de Organotecnécio , Esternotomia/efeitos adversos , Esterno , Infecção da Ferida Cirúrgica , Modelos Animais de Doenças , Distribuição Aleatória , Ratos Wistar , Reprodutibilidade dos Testes , Staphylococcus aureus , Infecções Estafilocócicas , Esterno/microbiologia , Infecção da Ferida Cirúrgica/microbiologia
7.
Acta cir. bras. ; 30(9): 632-638, Sep. 2015. tab, ilus
Artigo em Inglês | VETINDEX | ID: vti-334069

RESUMO

To evaluate whether scintigraphy with technetium-99m-labeled ceftizoxime (99mTc-CFT) can differentiate mediastinitis from aseptic inflammation associated with sternotomy. Twenty female Wistar rats were randomly distributed into four groups: S (control) -partial upper median sternotomy with no treatment; SW (control) - sternotomy and treatment of sternal wounds with bone wax; SB - sternotomy and infection with Staphylococcus aureus; SWB - sternotomy with bone wax treatment and bacterial infection. Scintigraphy with 99mTc-CFT was performed eight days after surgery and images were collected 210 and 360 min after infusion of the radiopharmaceutical. No animals exhibited clinical signs of wound infection at the end of the experiment, although histological data verified acute inflammatory response in those experimentally infected with bacteria. Scintigraphic images revealed that tropism of 99mTc-CFT to infected sternums was greater than to their non-infected counterparts. Mean counts of radioactivity in bacteria-infected sternal regions (SB and SWB) were significantly higher (p = 0.0007) than those of the respective controls (S and SW). Scintigraphy with technetium-99m-labeled ceftizoxime is a method that can potentially detect infection post sternotomy and differentiate from aseptic inflammation in animals experimentally inoculated with S. aureus.(AU)


Assuntos
Animais , Feminino , Ceftizoxima/análogos & derivados , Mediastinite , Compostos de Organotecnécio , Esternotomia/efeitos adversos , Esterno , Infecção da Ferida Cirúrgica , Modelos Animais de Doenças , Distribuição Aleatória , Ratos Wistar , Reprodutibilidade dos Testes , Infecções Estafilocócicas , Staphylococcus aureus , Esterno/microbiologia , Infecção da Ferida Cirúrgica/microbiologia
8.
Int J Nanomedicine ; 10: 2441-50, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25848262

RESUMO

Osteomyelitis is a progressive destruction of bones caused by microorganisms. Inadequate or absent treatment increases the risk of bone growth inhibition, fractures, and sepsis. Among the diagnostic techniques, functional images are the most sensitive in detecting osteomyelitis in its early stages. However, these techniques do not have adequate specificity. By contrast, radiolabeled antibiotics could improve selectivity, since they are specifically recognized by the bacteria. The incorporation of these radiopharmaceuticals in drug-delivery systems with high affinity for bones could improve the overall uptake. In this work, long-circulating and alendronate-coated liposomes containing (99m)technetium-radiolabeled ceftizoxime were prepared and their ability to identify infectious foci (osteomyelitis) in animal models was evaluated. The effect of the presence of PEGylated lipids and surface-attached alendronate was evaluated. The bone-targeted long-circulating liposomal (99m)technetium-ceftizoxime showed higher uptake in regions of septic inflammation than did the non-long-circulating and/or alendronate-non-coated liposomes, showing that both the presence of PEGylated lipids and alendronate coating are important to optimize the bone targeting. Scintigraphic images of septic or aseptic inflammation-bearing Wistar rats, as well as healthy rats, were acquired at different time intervals after the intravenous administration of these liposomes. The target-to-non-target ratio proved to be significantly higher in the osteomyelitis-bearing animals for all investigated time intervals. Biodistribution studies were also performed after the intravenous administration of the formulation in osteomyelitis-bearing animals. A significant amount of liposomes were taken up by the organs of the mononuclear phagocyte system (liver and spleen). Intense renal excretion was also observed during the entire experiment period. Moreover, the liposome uptake by the infectious focus was significantly high. These results show that long-circulating and alendronate-coated liposomes containing (99m)technetium-radiolabeled ceftizoxime have a tropism for infectious foci.


Assuntos
Alendronato , Ceftizoxima/análogos & derivados , Lipossomos , Compostos de Organotecnécio , Osteomielite , Alendronato/química , Alendronato/farmacocinética , Animais , Ceftizoxima/química , Ceftizoxima/farmacocinética , Lipossomos/química , Lipossomos/farmacocinética , Compostos de Organotecnécio/química , Compostos de Organotecnécio/farmacocinética , Osteomielite/diagnóstico , Osteomielite/metabolismo , Osteomielite/patologia , Ratos , Ratos Wistar
9.
Bioorg Med Chem Lett ; 22(14): 4605-8, 2012 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-22726927

RESUMO

Osteomyelitis is an infectious disease located in the bone or bone marrow. Long-circulating and pH-sensitive liposomes containing a technetium-99m-labeled antibiotic, ceftizoxime, (SpHL-(99m)Tc-CF) were developed to identify osteomyelitis foci. Biodistribution studies and scintigraphic images of bone infection or non infection-bearing rats that had been treated with these liposomes were performed. A high accumulation in infectious foci and high values in the target-non target ratio could be observed. These results indicate the potential of SpHL-(99m)Tc-CF as a potential agent for the diagnosis of bone infections.


Assuntos
Ceftizoxima/análogos & derivados , Compostos de Organotecnécio/farmacocinética , Compostos de Organotecnécio/uso terapêutico , Osteomielite/tratamento farmacológico , Animais , Ceftizoxima/administração & dosagem , Ceftizoxima/química , Ceftizoxima/farmacocinética , Ceftizoxima/uso terapêutico , Modelos Animais de Doenças , Concentração de Íons de Hidrogênio , Lipossomos , Masculino , Estrutura Molecular , Especificidade de Órgãos , Compostos de Organotecnécio/administração & dosagem , Compostos de Organotecnécio/química , Ratos , Ratos Wistar , Staphylococcus aureus/efeitos dos fármacos
10.
Nucl Med Commun ; 29(9): 830-6, 2008 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-18677212

RESUMO

PURPOSE: To investigate inflammatory (zymosan) and infectious (Staphylococcus aureus) processes in experimental models in rats using technetium-99m-labeled ceftizoxime (CFT). METHODS: Male Wistar rats were used for the development of the inflammatory (zymosan) and infectious (S. aureus) processes in the medullary cavity of the left tibia. Sterile saline was used for the control group. At 48 h after induction of the processes, the animals were anesthetized and scintigraphic images were acquired at 1, 2, 4, and 6 h after intravenous injection of 0.1 ml of 99mTc-CFT (55 MBq). Quantitative analysis of the scintigraphic images was performed by counting the radioactivity in the regions of interest. Samples of tibia were taken for histopathological examination. RESULTS: The images showed that 99mTc-CFT presented higher tropism to infectious foci than with the inflammatory site. The average value of the target/nontarget ratio of the 99mTc-CFT was significantly higher in the infected (2.40+/-0.22) than in the inflamed tibia (1.50+/-0.05) and the control group (1.05+/-0.04) for all of the investigated times. The histological data showed a similar inflammatory response for both the S. aureus and zymosan groups. CONCLUSION: The 99mTc-CFT presented a high tropism and retention for an infected region in this model of osteomyelitis, thereby constituting an interesting strategy to distinguish aseptic from septic sites.


Assuntos
Ceftizoxima/análogos & derivados , Compostos de Organotecnécio/farmacologia , Osteomielite/diagnóstico por imagem , Osteomielite/diagnóstico , Cintilografia/métodos , Animais , Proteínas Sanguíneas/química , Ceftizoxima/farmacologia , Modelos Animais de Doenças , Inflamação , Masculino , Compostos Radiofarmacêuticos/farmacologia , Ratos , Ratos Wistar , Sepse/diagnóstico , Sepse/diagnóstico por imagem , Infecções Estafilocócicas/diagnóstico , Infecções Estafilocócicas/diagnóstico por imagem , Fatores de Tempo , Zimosan/metabolismo
11.
Rev Esp Med Nucl ; 24(5): 312-8, 2005.
Artigo em Espanhol | MEDLINE | ID: mdl-16194463

RESUMO

UNLABELLED: This study aimed to investigate the biodistribution of the 99mTc-ceftizoxime in normal rats and in rats bearing septic and sterile induced abscess. MATERIAL AND METHODS: Three groups of rats were studied. a) Six normal rats b) 15 rats with E. coli induced abscess and c) 15 rats with sterile zymosan induced abscess. Septic abscess was induced with 2 x 10(8) colony forming units of E. coli and sterile one with 0.1 mL of 5% sterile Zymosan. 24 h after the abscess induction, 12 MBq of 99mTc-CFT were injected iv. and whole body images were collected at 30 min, 1, 2, 4 and 6 h p.i. Areas of interest were drawn and lesion/background index was calculated. The 6 normal rats were scanned at the same times, killed at 6 h p.i and kidney, liver, spleen, lung, heart and muscle activity were measured. Each organ was weighed, cut and its activity measured. Parallelly, the biological activity of the labeled antibiotic and its binding to the E. coli and S. aureus bacteria were analyzed. RESULTS: High biliary excretion was seen in all rats. Organ measurement showed the maximal uptake in kidney and very low uptake in muscles. Mean +/- s.d abscess/background ratio at 30 min, 1, 2, 4 and 6 h were 2.60 +/- 0.36, 2.67 +/- 0.66, 2.6 0 +/- 0.58, 2.78 +/- 0.84, 3.24 +/- 1.00 for septic abscess and 2.37 +/- 0.39, 2.10 +/- 0.38, 1.97 +/- 0.34, 1.82 +/- 0.25, 1.65 +/- 0.23 for aseptic abscess. The 99mTc-CFT uptake was significantly higher in the septic abscess than in sterile one (p < 0.05). The 99mTc-CFT uptake in the septic abscess remains stable or increases until along the 6 h. The 99mTc-CFT uptake in the aseptic abscess decreases along the time. CONCLUSIONS: The scintigraphy with 99mTc-CFT seems able to differentiate sterile inflammation from infection. High biliary excretion limits its application in abdomen. Main application could be diagnosis of osteoarticular infection.


Assuntos
Abscesso/diagnóstico por imagem , Ceftizoxima/análogos & derivados , Compostos de Organotecnécio , Compostos Radiofarmacêuticos , Abscesso/microbiologia , Animais , Ceftizoxima/farmacocinética , Diagnóstico Diferencial , Compostos de Organotecnécio/farmacocinética , Cintilografia , Compostos Radiofarmacêuticos/farmacocinética , Ratos , Ratos Sprague-Dawley
12.
Rev Med Chil ; 133(8): 903-10, 2005 Aug.
Artigo em Espanhol | MEDLINE | ID: mdl-16163428

RESUMO

BACKGROUND: Cefpodoxime is a new antimicrobial in the Chilean market, recommended for treatment of respiratory and urinary tract infections. AIM: To study the susceptibility of common pathogens isolated from Chilean patients to cefpodoxime and other antimicrobials. MATERIAL AND METHODS: The in vitro activity of cefpodoxime, expressed as Minimal Inhibitory Concentration, was studied in 331 S pneumoniae, H influenzae, M catarrhalis, E coli, S aureus and S pyogenes strains, isolated between 2000 and 2004 from respiratory, urinary and soft tissue infections, respectively. RESULTS: Eleven percent of S pneumoniae isolates were resistant to penicillin, 11% were resistant to cefuroxime and 10% to cefpodoxime. All H influenzae isolates were susceptible to cefpodoxime. No H influenzae isolates were resistant to second or third generation cephalosporines. Four percent of H influenzae isolates were resistant to ampicillin by ss-lactamase production. In contrast 81% of M catarrhalis strains were resistant to ampicillin. Six percent of E coli isolates were resistant to cefpodoxime, 9% to cefuroxime, 11% to cefadroxile and 50% to ampicillin or trimethoprim/sulphamethoxazole. Cefpodoxime was the most active antimicrobial against S pyogenes. CONCLUSIONS: Cefpodoxime, recently introduced in Chile, is a good alternative for the treatment of common respiratory and urinary tract infections.


Assuntos
Antibacterianos/farmacologia , Ceftizoxima/análogos & derivados , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Ceftizoxima/farmacologia , Bactérias Gram-Negativas/isolamento & purificação , Bactérias Gram-Positivas/isolamento & purificação , Humanos , Testes de Sensibilidade Microbiana , Cefpodoxima
13.
Rev. méd. Chile ; 133(8): 903-910, ago. 2005. tab
Artigo em Espanhol | LILACS | ID: lil-429224

RESUMO

Background: Cefpodoxime is a new antimicrobial in the Chilean market, recommended for treatment of respiratory and urinary tract infections. Aim: To study the susceptibility of common pathogens isolated from Chilean patients to cefpodoxime and other antimicrobials. Material and methods: The in vitro activity of cefpodoxime, expressed as Minimal Inhibitory Concentration, was studied in 331 S pneumoniae, H influenzae, M catarrhalis, E coli, S aureus and S pyogenes strains, isolated between 2000 and 2004 from respiratory, urinary and soft tissue infections, respectively. Results: Eleven percent of S pneumoniae isolates were resistant to penicillin, 11% were resistant to cefuroxime and 10% to cefpodoxime. All H influenzae isolates were susceptible to cefpodoxime. No H influenzae isolates were resistant to second or third generation cephalosporines. Four percent of H influenzae isolates were resistant to ampicillin by ß-lactamase production. In contrast 81% of M catarrhalis strains were resistant to ampicillin. Six percent of E coli isolates were resistant to cefpodoxime, 9% to cefuroxime, 11% to cefadroxile and 50% to ampicillin or trimethoprim/sulphamethoxazole. Cefpodoxime was the most active antimicrobial against S pyogenes. Conclusions: Cefpodoxime, recently introduced in Chile, is a good alternative for the treatment of common respiratory and urinary tract infections.


Assuntos
Humanos , Antibacterianos/farmacologia , Ceftizoxima/análogos & derivados , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Ceftizoxima/farmacologia , Bactérias Gram-Negativas/isolamento & purificação , Bactérias Gram-Positivas/isolamento & purificação , Testes de Sensibilidade Microbiana
14.
Farmaco ; 58(5): 363-9, 2003 May.
Artigo em Inglês | MEDLINE | ID: mdl-12729830

RESUMO

Cefpodoxime proxetil, a third-generation cephalosporin for oral administration, was synthesized by a method based on the following sequence of reactions: acylation of 7-aminocephalosporanic acid (7-ACA) with S-benzothiazol-2-yl(2-amino-4-thiazolyl)(methoxyimino)thioacetate (MAEM), chloroacetylation of the cefotaxime formed with chloroacetyl chloride, esterification of the acid function with 1-iodoethyl isopropyl carbonate and final cleavage of chloroacetamide protective group by treatment with thiourea in N,N-dimethylacetamide. The developed procedure allows us to obtain better yields of cefpodoxime proxetil and to eliminate the final purification step by column chromatography, necessary during the synthesis of this antibiotic by the previously reported methods.


Assuntos
Acetatos/síntese química , Antibacterianos/síntese química , Ceftizoxima/análogos & derivados , Ceftizoxima/síntese química , Tiazóis/síntese química , Acilação , Administração Oral , Benzotiazóis , Cefalosporinas/química , Química Farmacêutica , Composição de Medicamentos , Cefpodoxima Proxetil
15.
J Pharm Biomed Anal ; 30(3): 643-49, 2002 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-12367689

RESUMO

A high-performance liquid chromatography isocratic procedure was developed for the assay of cefetamet pivoxil hydrochloride in drug substance and powder for oral suspension. The method validation yielded good results and included the range, linearity, precision intra- inter-day, accuracy, specificity, LOD and LOQ values. The chromatographic system consisted of a C(18) absorbosphere column (150 x 4.6 mm i.d., 5 microm particle size), a mobile phase composed of water-acetonitrile-methanol-phosphate buffer, pH 3.5 (50:35:10:5, v/v), flow rate of 1.5 ml min(-1) and UV detection at 254 nm. The relative standard deviation varied between 0.03 and 1.76%, and accuracy of 100.09% was found. Calibration curve was linear from 30.0-80.0 microg ml(-1); its correlation coefficient was 0.99989.


Assuntos
Ceftizoxima/análogos & derivados , Ceftizoxima/análise , Administração Oral , Ceftizoxima/química , Química Farmacêutica , Cromatografia Líquida/métodos , Pós
16.
Rev Assoc Med Bras (1992) ; 43(1): 47-52, 1997.
Artigo em Português | MEDLINE | ID: mdl-9224992

RESUMO

UNLABELLED: Cefetamet pivoxil is a new beta lactamase orally stable administered cephalosporin. Antimicrobial resistance among respiratory pathogens has become an important problem for both the physician and the microbiologist and the patterns of resistance vary greatly depending on geographic location, often requiring in vitro susceptibility testing of isolates. PURPOSE: The in vitro activity of cefetamet, the microbiologically active metabolite of the prodrug cefetamet pivoxil, was compared with other 11 drugs against 376 bacterial strains recently isolated from patients with respiratory tract infections. METHODS: The comparative activity in vitro of cefetamet and other 11 antimicrobial agents was measured against 376 bacterial strains isolated from patients with respiratory tract infections, during a six month period. Through the determination of minimum inhibitory concentration by the microdilution technique, patterns of antimicrobial resistance were reported. RESULTS: Cefetamet showed high in vitro activity against all the bacterial tested, possessing a spectrum of activity similar to that other recently developed oral cephalosporins. The good activity of cefetamet against beta-lactamase producing isolates, like Moraxella catarrhalis, can be due to its beta-lactamase stability. At a concentration of 1.0 microgram/mL, cefetamet inhibited 97% of all the tested bacteria. CONCLUSION: The MIC90 of the cumulative susceptibility results of the 12 antimicrobics tested in the 376 strains studied, confirm the excellent activity of cefetamet against the common respiratory tract pathogens.


Assuntos
Bactérias/efeitos dos fármacos , Ceftizoxima/análogos & derivados , Infecções Respiratórias/microbiologia , Antibacterianos/farmacologia , Bactérias/isolamento & purificação , Ceftizoxima/farmacologia , Resistência Microbiana a Medicamentos , Humanos
17.
J Antimicrob Chemother ; 37(3): 565-73, 1996 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-9182113

RESUMO

A multicentre open-label, randomised trial was performed to compare the efficacy and safety of cefpodoxime proxetil bd and cefaclor tds in the treatment of acute otitis media in children. A total of 167 children aged from 1 month to 11 years were enrolled in five centres: 78 treated with cefpodoxime and 83 treated with cefaclor, were evaluated in the ITT analysis. After tympanocentesis and culture of middle ear fluid, a pathogen was isolated from 85 (53%) of the 161 evaluable patients for the ITT analysis. The organisms isolated were as follows: Streptococcus pneumoniae: (n = 33, 37.5%); Haemophilus influenzae: (n = 22, 25%); Staphylococcus aureus: (n = 15, 17.1%); Streptococcus pyogenes: (n = 8, 9.1%); Moraxella catarrhalis: (n = 2, 2.3%); others (n = 6, 6.8%). Success (defined as a satisfactory clinical outcome, either cure or improvement) was achieved at the end of treatment, in 93.6% of ther patients in the cefpodoxime group and 91.6% of the patients in the cefaclor group (P> 0.05). Clinical recurrence was identified at the follow-up visit (30 days after inclusion), in 6.4% of the cefpodoxime-treated patients and 7.2% of the cefaclor-treated patients (P> 0.05). The drugs were well tolerated by 78/79 (99%) of patients in the cefpodoxime-treated group and 80/85 (94%) in the cefaclor-treated group. The incidence of adverse effects was higher in the cefaclor group than in the cefpodoxime group, but this was not statistically significant (P > 0.05). IN conclusion, cefpodaxime proxetil administered bd is as effective as cefaclor administered tds in the treatment of acute otitis media in children. The less frequent dosing schedule of cefpodoxime (bd) compared with cefaclor (tds) appears to be more convenient for the treatment of the infections in children.


Assuntos
Cefaclor/uso terapêutico , Ceftizoxima/análogos & derivados , Cefalosporinas/uso terapêutico , Otite Média/tratamento farmacológico , Pró-Fármacos/uso terapêutico , Doença Aguda , Cefaclor/efeitos adversos , Ceftizoxima/efeitos adversos , Ceftizoxima/uso terapêutico , Cefalosporinas/efeitos adversos , Criança , Pré-Escolar , Feminino , Infecções por Haemophilus/tratamento farmacológico , Haemophilus influenzae , Humanos , Lactente , Masculino , Moraxella catarrhalis , Infecções por Neisseriaceae/tratamento farmacológico , Otite Média/microbiologia , Pró-Fármacos/efeitos adversos , Infecções Estafilocócicas/tratamento farmacológico , Staphylococcus aureus , Infecções Estreptocócicas/tratamento farmacológico , Streptococcus pneumoniae , Streptococcus pyogenes , Suspensões , Cefpodoxima Proxetil
18.
Diagn Microbiol Infect Dis ; 19(2): 121-7, 1994 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-7805356

RESUMO

We studied the efficacy and safety of cefetamet pivoxil (CAT), an oral aminothiazolyl cephalosporin, in a series of open, comparative multicenter studies in 207 women (four study centers) with uncomplicated gonorrhea, and summarized and pooled the results with those of earlier open dose-finding trials (360 men; six study centers). We compared single-dose treatment regimen of CAT--over the range of 400-1500 mg--with spectinomycin, thiamphenicol, ampicillin, or amoxicillin plus probenecid. The overall cure rates were 100% in 88 women treated with 1500 mg CAT and in 137 men treated with 1200 or 1500 mg CAT, 98% (114 of 116 men) in those treated with 800 or 1000 mg CAT, and 93% (42 of 45 men) in those treated with 400 or 500 mg CAT; the composite cure rate of the comparators was 97%. The tolerability of CAT (n = 428) compared favorably (1.8% adverse events) with that of the standard drugs (n = 139) (4.3% adverse events). Single-dose treatment with 1500 mg CAT is effective and safe in adults with uncomplicated gonorrhea.


Assuntos
Ceftizoxima/análogos & derivados , Gonorreia/tratamento farmacológico , Adolescente , Adulto , Idoso , Ceftizoxima/efeitos adversos , Ceftizoxima/uso terapêutico , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Estudos Prospectivos
20.
Pathol Biol (Paris) ; 41(4): 385-91, 1993 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-8233640

RESUMO

Since resistance to several oral antimicrobials useful for the treatment of pediatric urinary tract infections (UTI) is overwhelming in Argentina, an in vitro investigation was performed testing 400 isolates obtained from urines of children suffering UTI's, 200 collected in 1990 and 200 in 1991. Their susceptibility against oral antimicrobials marketed in Argentina and appropriate for the treatment of UTI was determined by the agar dilution methods. An increase of the resistance to aminopenicillin combined with beta-lactamase inhibitors and to fluoroquinolones was observed comparing the two periods. Cefpodoxime (CPD), cefixime and fluoroquinolones except norfloxacin were the sole oral antimicrobials showing in vitro activity at the 90 per cent level. Unfortunately fluoroquinolones are not yet approved for pediatric use. Consequently we realized an in vitro and in vivo pharmacokinetic study in order to determine CPD activity against E. coli isolated in UTI cases. Five children (6-10 y) showing E. coli UTI infections received 10 mg/kg/d CPD in a single oral daily dose and were treated up to 10 days, 3 had lower UTI and 2 upper UTI. All patients were clinical and bacteriologically cured. Cultures obtained up to 4 weeks after treatment were negative. CPD serum levels at 2 hours after the first dose of treatment showed a median of 2.7 mg/l (2.3-3.4 range). Bactericidal serum titers at the same time against the patients own strain and an E. coli TEM-1 hyperproducer strain (MIC 4,096 mg/l for ampicillin and 0.5 mg/l for CPD) showed a median value of 1/8 against patients strains and 1/2 against the THP strain.(ABSTRACT TRUNCATED AT 250 WORDS)


Assuntos
Ceftizoxima/análogos & derivados , Infecções por Escherichia coli/tratamento farmacológico , Escherichia coli/efeitos dos fármacos , Infecções Urinárias/tratamento farmacológico , Antibacterianos/farmacologia , Anti-Infecciosos Urinários/uso terapêutico , Ceftizoxima/sangue , Ceftizoxima/farmacologia , Ceftizoxima/uso terapêutico , Ceftizoxima/urina , Criança , Relação Dose-Resposta a Droga , Escherichia coli/isolamento & purificação , Infecções por Escherichia coli/microbiologia , Feminino , Humanos , Técnicas In Vitro , Klebsiella/efeitos dos fármacos , Klebsiella/isolamento & purificação , Masculino , Proteus mirabilis/efeitos dos fármacos , Proteus mirabilis/isolamento & purificação , Infecções Urinárias/microbiologia , Cefpodoxima
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