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1.
Int J Urol ; 29(9): 977-982, 2022 09.
Artigo em Inglês | MEDLINE | ID: mdl-35384075

RESUMO

OBJECTIVES: In March 2019, cefazolin was unavailable owing to difficulty in procuring the active ingredient. Furthermore, the supply of alternative drugs, such as cefotiam and cefmetazole, was limited. In the Department of Nephro-Urology, fosfomycin-based drugs are used as substitutes for cefazolin, which is a perioperative prophylactic antibacterial drug. Herein, we investigated the effectiveness of fosfomycin sodium and cefotiam in preventing infection after endoscopic combined intrarenal surgery as a retrospective preliminary study. METHODS: A total of 200 patients who underwent endoscopic combined intrarenal surgery at our department between August 2017 and January 2021 were included. The patients were administered cefotiam (n = 95) or fosfomycin (n = 105) as perioperative antibacterial agents. There were no significant differences in the median age or surgery time between the cefotiam and fosfomycin groups. Propensity score matching was performed to match the preoperative urine bacterial counts of both groups. Sixty-eight patients were selected from each group. RESULTS: The median postoperative hospital stay duration was 4 days for the two groups. The median maximum postoperative temperatures were 37.5 and 37.4°C, respectively. There were no significant differences between the maximum postoperative temperatures in both groups. Furthermore, there were no differences between the groups regarding the white blood cell counts, C-reactive protein levels, and aspartate aminotransferase and alanine aminotransferase levels postoperatively, as well as in terms of postoperative fever requiring additional antibiotics. CONCLUSIONS: During a period of difficulty in acquiring cefazolin and cefotiam, the use of fosfomycin allowed us to continue with the procedure without increased clinical complications.


Assuntos
Fosfomicina , Antibacterianos/uso terapêutico , Cefazolina/uso terapêutico , Cefotiam , Fosfomicina/uso terapêutico , Humanos , Estudos Retrospectivos
2.
Mol Inform ; 41(2): e2100062, 2022 02.
Artigo em Inglês | MEDLINE | ID: mdl-34529322

RESUMO

In the current study, we used 7922 FDA approved small molecule drugs as well as compounds in clinical investigation from NIH's NPC database in our drug repurposing study. SARS-CoV-2 main protease as well as Spike protein/ACE2 targets were used in virtual screening and top-100 compounds from each docking simulations were considered initially in short molecular dynamics (MD) simulations and their average binding energies were calculated by MM/GBSA method. Promising hit compounds selected based on average MM/GBSA scores were then used in long MD simulations. Based on these numerical calculations following compounds were found as hit inhibitors for the SARS-CoV-2 main protease: Pinokalant, terlakiren, ritonavir, cefotiam, telinavir, rotigaptide, and cefpiramide. In addition, following 3 compounds were identified as inhibitors for Spike/ACE2: Denopamine, bometolol, and rotigaptide. In order to verify the predictions of in silico analyses, 4 compounds (ritonavir, rotigaptide, cefotiam, and cefpiramide) for the main protease and 2 compounds (rotigaptide and denopamine) for the Spike/ACE2 interactions were tested by in vitro experiments. While the concentration-dependent inhibition of the ritonavir, rotigaptide, and cefotiam was observed for the main protease; denopamine was effective at the inhibition of Spike/ACE2 binding.


Assuntos
Antivirais , Reposicionamento de Medicamentos , Drogas em Investigação/farmacologia , SARS-CoV-2/efeitos dos fármacos , Enzima de Conversão de Angiotensina 2 , Antivirais/farmacologia , COVID-19/tratamento farmacológico , Cefotiam/farmacologia , Proteases 3C de Coronavírus/antagonistas & inibidores , Avaliação Pré-Clínica de Medicamentos , Humanos , Simulação de Acoplamento Molecular , Ritonavir/farmacologia , Glicoproteína da Espícula de Coronavírus/antagonistas & inibidores
3.
J Infect Chemother ; 27(4): 625-631, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33309628

RESUMO

INTRODUCTION: In March 2019, cefazolin availability was limited owing to the contamination of the drug substance. In addition, there was a difficulty in supplying drugs alternative to cefazolin, such as cefotiam and cefmetazole. In our Department of Nephro-urology, we used fosfomycin-based drugs to substitute cefazolin as perioperative preventive antibacterial drugs. In this study, we aimed to evaluate the usage status of perioperative prophylactic antibacterial drugs before and after the period of limited cefazolin supply and to investigate the efficacy and safety of fosfomycin sodium in preventing infections following transurethral resection of bladder tumor. METHODS: We enrolled 346 patients who underwent transurethral resection of bladder tumor in our department from April 2018 to August 2020. The patients received the following perioperative antibacterial agents: cefotiam (n = 146), fosfomycin (n = 166), and other antibacterial agents (n = 34). There was no significant difference in the median age or surgery time. RESULTS: The median length of hospital stay was 6, 5, and 5 days in the cefotiam, fosfomycin, and other antibacterial groups, respectively, with significant difference. The median maximum postoperative temperature was 37.1 °C in all groups, with no significant difference. There were no differences in C-reactive protein, aspartate aminotransferase, and alanine aminotransferase levels determined by postoperative blood tests; preoperative and postoperative urinary white blood cell counts; preoperative urine bacterial counts; and surgery-related infection requiring additional antibiotic treatments among the groups. CONCLUSIONS: The use of fosfomycin-based agents helped overcome the limited supply of cefazolin without worsening clinical outcomes.


Assuntos
Fosfomicina , Neoplasias da Bexiga Urinária , Antibacterianos/uso terapêutico , Cefazolina/uso terapêutico , Cefmetazol/uso terapêutico , Cefotiam , Fosfomicina/uso terapêutico , Humanos , Neoplasias da Bexiga Urinária/cirurgia
4.
J Infect Chemother ; 26(11): 1158-1163, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32828676

RESUMO

Bacteremia is often caused by gram-negative bacteria (represented by EKP; Escherichia coli, Klebsiella species, and Proteus mirabilis), and the excessive use of cefazolin, as the first-line antimicrobial in its treatment, has been a source of concern in the emergence of resistant strains. As an antimicrobial, cefotiam may be an alternative to cefazolin; however, little evidence is available for its use in the treatment of bacteremia. The purpose of this non-inferiority study was to retrospectively compare the therapeutic efficacy of cefotiam with some antimicrobials of narrow spectrum (cefazolin, cefmetazole, and flomoxef) in the treatment of EKP-induced bacteremia. The number of patients recruited was 32 in the cefotiam group and 29 in the control group. In the primary endpoint, the survival rate on day 28 for the cefotiam group and the control group was 93.5% and 89.3%, respectively (relative risk at day 28, 1.048; 95% confidence interval, 0.894-1.227). In the secondary end point, treatment success rate in the two groups was 71.9% and 69.0%, respectively (relative risk, 1.042; 95% confidence interval, 0.752-1.445). Intensive care unit admission, low body weight, hypoalbuminemia, and infections unassociated with the urinary tract were identified to be the risk factors responsible for treatment failure. We demonstrated cefotiam may be non-inferior to other antimicrobials of similar spectrum, in terms of survival rate, in EKP-induced bacteremia.


Assuntos
Bacteriemia , Proteus mirabilis , Antibacterianos/uso terapêutico , Bacteriemia/tratamento farmacológico , Cefotiam , Escherichia coli , Humanos , Klebsiella , Estudos Retrospectivos
5.
Ther Drug Monit ; 42(5): 733-736, 2020 10.
Artigo em Inglês | MEDLINE | ID: mdl-32251152

RESUMO

BACKGROUND: Cefotiam, a second-generation cephalosporin, is a broad-spectrum antibiotic with good antibacterial action against both gram-negative and gram-positive bacteria. It is used widely in clinical practice, although bacterial drug resistance makes its clinical use problematic. The authors hypothesized that subtherapeutic concentrations of cefotiam leads to bacterial resistance. The present study was conducted to evaluate whether the standard cefotiam dosing regimen resulted in a subtherapeutic concentrations in children. METHOD: Data were prospectively collected from pediatric patients with suspected or confirmed community-acquired pneumonia who were receiving cefotiam at the standard dosing regimen (40-80 mg/kg, 2 or 3 times daily). A blood sample was collected after 70%-100% of the dosing interval, and plasma concentrations were determined by high-performance liquid chromatography using an ultraviolet detector. RESULTS: The data from 88 patients (age, 3.0 ± 2.8 years; weight, 15.4 ± 8.3 kg) were used for analysis. The average of cefotiam concentrations was 0.06 mcg/mL (range: <0.05-0.79 mcg/mL). Most patients (n = 72, 81.8%) had concentrations below 0.1 mcg/mL; only 2 patients had concentrations higher than 0.4 mcg/mL. CONCLUSIONS: The standard dosing regimen for cefotiam resulted in extremely low plasma concentrations in children; such low concentrations may lead to antimicrobial drug resistance. Thus, an increase in cefotiam dosage in children to 80 mg/kg 4 times daily is recommended (maximum dose on the label).


Assuntos
Antibacterianos/uso terapêutico , Cefotiam/uso terapêutico , Adolescente , Infecções Bacterianas/tratamento farmacológico , Criança , Pré-Escolar , Resistência Microbiana a Medicamentos/efeitos dos fármacos , Feminino , Humanos , Lactente , Recém-Nascido , Masculino , Estudos Prospectivos
6.
J Gastroenterol Hepatol ; 34(9): 1486-1491, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31245885

RESUMO

BACKGROUND: Tissue adhesive injection is the first-line treatment for gastric varices rebleeding. Available studies are focused on antibiotic usage in emergency endoscopy, while the use of antibiotics in selective endoscopic tissue adhesive treatment remains controversial. METHODS: This is a randomized controlled study conducted in a tertiary referral hospital. Consecutive patients were enrolled from February 16, 2016, to November 19, 2016, and blindly randomized into two treatment groups. Patients in the prophylactic group received 2 g of cefotiam during endoscopic injection of tissue adhesive. All the subjects were observed for rebleeding, fever, and changes in laboratory indicators in hospital and post-discharge. RESULT: One hundred and seven patients who received endoscopic therapy for gastroesophageal varices were included. Fifty-three patients were allocated to the antibiotic prophylactic group and 54 patients to the on-demand group. The two groups had similar baseline characteristics. The incidence of fever in hospital was 2/53 (3.8%) vs 9/54 (16.7%) (P = 0.028). Perioperative and postoperative clinical events were significantly lower in the antibiotic prophylactic group (5.7% vs 24.1%, P = 0.018; 7.5% vs 20.4%, P = 0.050). Inflammation indices were elevated on the first day after endoscopic therapy; however, no significant difference was observed between the two groups. The cumulative rebleeding free rate within 2 months was lower in the antibiotic prophylactic group (1.9% vs 9.3%, P = 0.100). CONCLUSION: Our study illustrated that prophylactic use of antibiotics in selective endoscopic injection of tissue adhesive reduced the incidence of the total clinical events in perioperative period and had a trend towards lower rebleeding in 2 months.


Assuntos
Antibacterianos/administração & dosagem , Antibioticoprofilaxia , Cefotiam/administração & dosagem , Endoscopia Gastrointestinal , Varizes Esofágicas e Gástricas/terapia , Hemorragia Gastrointestinal/terapia , Hemostase Endoscópica , Adesivos Teciduais/administração & dosagem , Adulto , Idoso , Antibacterianos/efeitos adversos , Antibioticoprofilaxia/efeitos adversos , Cefotiam/efeitos adversos , China , Endoscopia Gastrointestinal/efeitos adversos , Feminino , Febre/etiologia , Hemostase Endoscópica/efeitos adversos , Humanos , Injeções , Masculino , Pessoa de Meia-Idade , Projetos Piloto , Recidiva , Fatores de Tempo , Adesivos Teciduais/efeitos adversos , Resultado do Tratamento
7.
J Pharm Biomed Anal ; 158: 425-430, 2018 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-29945059

RESUMO

Two structural isomers of cefotiam in cefotiam hydrochloride for injection were observed, and the structures of the isomers were determined by mass spectrometry and various 1D and 2D NMR techniques. The thermo-isomerization mechanism of cefotiam was also discussed. Thermo-isomerization occurred not only in cefotiam but also in cephalosporins containing a 1-alkyl-1H-tetrazole-5-thiol side chain at C-3. Furthermore, the toxic effects of the two impurities of cefotiam hydrochloride were predicted and it is thought that they could be more toxic than cefotiam. The results reported in this article may be important for quality control and stability studies of this class of drugs.


Assuntos
Antibacterianos/análise , Cefotiam/análise , Cefalosporinas/análise , Contaminação de Medicamentos/prevenção & controle , Controle de Qualidade , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antibacterianos/toxicidade , Cefotiam/química , Cefotiam/isolamento & purificação , Cefotiam/toxicidade , Cefalosporinas/química , Cefalosporinas/isolamento & purificação , Cefalosporinas/toxicidade , Química Farmacêutica , Simulação por Computador , Estabilidade de Medicamentos , Isomerismo , Espectroscopia de Ressonância Magnética/instrumentação , Espectroscopia de Ressonância Magnética/métodos , Espectrometria de Massas/instrumentação , Espectrometria de Massas/métodos , Simulação de Acoplamento Molecular , Temperatura
8.
Clin Exp Dermatol ; 42(5): 527-531, 2017 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-28543395

RESUMO

A 26-year-old woman presented with recurrent attacks of widespread urticaria and systemic symptoms. The patient was a nurse, and the attacks occurred only in her workplace, without an apparent trigger. A patch test to cefotiam (CTM) induced an immediate skin reaction. ELISA detected the patient's serum IgE antibody binding to CTM conjugated with human serum albumin (CTM-HSA), and her basophils released histamine in response to CTM-HSA in a histamine release assay (HRA). Both reactions in ELISA and HRA were inhibited by pretreatment of the patient's serum or basophils with cefotiam. No crossreactivity in skin tests or in vitro assays was observed against other antibiotics, even those containing a beta-lactam ring and/or side chains similar to CTM. Certain antibiotics including CTM may cause extremely sensitive and specific contact urticaria syndrome, which is mediated by IgE and evoked even without apparent skin contact with the culprit drug and in the absence of any history of an allergic reaction against other antibiotics with similar structures.


Assuntos
Cefotiam/imunologia , Imunoglobulina E/imunologia , Doenças Profissionais/induzido quimicamente , Urticária/induzido quimicamente , Adulto , Cefotiam/efeitos adversos , Feminino , Humanos , Recursos Humanos de Enfermagem no Hospital , Doenças Profissionais/imunologia , Urticária/imunologia
9.
Artif Organs ; 38(1): 48-55, 2014 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-23865445

RESUMO

Routine perioperative intravenous antimicrobial agents are administered as surgical prophylaxis. However, whether balanced ultrafiltration during extracorporeal circulation has substantial effect on the concentration of antimicrobial agents remains unclear. The concentrations of antimicrobial agents in plasma and ultrafiltrate samples were measured in this pseudo-extracorporeal circulation model. Extracorporeal circulation consisted of cardiotomy reservoir, membrane oxygenator, and pediatric arterial line filter. A hemoconcentrator was placed between the arterial purge line and oxygenator venous reservoir. Fresh donor human whole blood was added into the circuit and mixed with Ringer's solution to obtain a final hematocrit of 24-28%. Two kinds of antimicrobial agents, cefotiam (320 mg) and cefmetazole (160 mg), were bolus added into the circuit. After 30 min of extracorporeal circulation, zero-balanced ultrafiltration was initiated and arterial line pressure was maintained at approximately 100 mm Hg with a Hoffman clamp. The rate of ultrafiltration (12 mL/min) was controlled by ultrafiltrate outlet pressure. An identical volume of Plasmalyte A was dripped into the circuit to maintain stable hematocrit during 45 min of experiment. Plasma and ultrafiltrate samples were drawn every 5 min, and concentrations of antimicrobial agents (including cefotiam and cefmetazole) were measured with high performance liquid chromatography. Both antimicrobial agents were detected in ultrafiltrate, demonstrating hemoconcentration may remove antimicrobial agents. The concentrations of plasma antimicrobial agents decreased linearly with the increase of ultrafiltrate volume. At end of balanced ultrafiltration, the concentration of plasma cefotiam was 104.96 ± 44.36 mg/L, which is about 44.38% ± 7.42% of the initial concentration (238.95 ± 101.12 mg/L) (P < 0.001); the concentration of plasma cefmetazole decreased linearly to 25.76 ± 14.78 mg/L, which is about 49.69% ± 10.49% of the initial concentration (51.49 ± 28.03 mg/L) (P < 0.001). The total amount of cefotiam in ultrafiltrate is 27.16% ± 12.17% of the total dose administered, whereas cefmetazole in ultrafiltrate is 7.74% ± 4.17%. Balanced ultrafiltration may remove antimicrobial agents from plasma and has a prominent influence on plasma concentration of antimicrobial agent. The strategy of surgical prophylaxis should consider this unique technique during extracorporeal circulation.


Assuntos
Anti-Infecciosos/sangue , Cefmetazol/sangue , Cefotiam/sangue , Circulação Extracorpórea/instrumentação , Ultrafiltração/instrumentação , Desenho de Equipamento , Hemodinâmica , Humanos
11.
Sichuan Da Xue Xue Bao Yi Xue Ban ; 44(3): 481-4, 493, 2013 May.
Artigo em Chinês | MEDLINE | ID: mdl-23898540

RESUMO

OBJECTIVE: To detect unknown impurities in raw drug material of cefotiam hexetil. METHODS: High performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) was employed for the determination of impurities in cefotiam hexetil. Agilent SB-C18 column (150 mm x 2.1 mm i. d. , 3.5 microm particles) was used for chromatographic separations of cofotiam hexetil dissolved in deionized water, with mobile phase consisting of (A) 0.1% formic acid and (B) acetonitrile and timed gradient program T (min)/B (%): 0/3, 5/3, 15/20, 20/40, 30/60, 40/80. The flow rate was set at 0. 3 mL/min with DAD detector wavelength fixed at 254 nm. Electrospray ionization source was applied and operated in positive ion MRM mode. The source voltage was kept at 4 kV and cone voltage was 100 V with the mass range m/z 50-1000. Nitrogen was used as nebulizing gas and the nebulizer pressure was 40 psi. The drying gas temperature was 350 degrees C and the drying gas flow was 10 L/min. Results Unknown impurities of cefotiam hexetil were identified. Substance 1 was delta3-isomer of cefotiam hexetil. The structures of 3 other substances were also determined. CONCLUSION: The method is sensitive, rapid and credible for the analysis of cefotiam hexetil and its related impurities, which can be applied in quality control of cefotiam hexetil.


Assuntos
Cefotiam/análogos & derivados , Cromatografia Líquida de Alta Pressão , Contaminação de Medicamentos , Espectrometria de Massas em Tandem , Cefotiam/química , Contaminação de Medicamentos/prevenção & controle , Controle de Qualidade
12.
Kansenshogaku Zasshi ; 87(2): 207-10, 2013 Mar.
Artigo em Japonês | MEDLINE | ID: mdl-23713331

RESUMO

Kingella species including K. kingae are non-motile coccobacilli or short straight rods, and their normal habitats appear to be the upper respiratory and oropharyngeal tracts of humans. In recent years, K. kingae strains have been increasingly recognized as common causes of invasive infections in children at the age of less than 4 years. In Japan, however, invasive K. kingae infections including osteomyelitis have rarely been described. We incidentally encountered isolation of a K. kingae strain from intraoperatively obtained specimens from a previously healthy 44-month-old boy. He first consulted a nearby medical facility and a suspected diagnosis of osteomyelitis was made, after which the patient was then transferred to our Nagano Children's hospital. There was evidence of inflammation in his right calcaneus and toe walking was noted. He was treated with surgical drainage. An isolate grown on sheep blood agar with positive oxidase and negative catalase was biochemically characterized with the ID-Test HN20 (Nissui Pharmaceutical Co., Ltd., Tokyo, Japan) kit system together with genetic examinations involving sequencing the 16S rRNA gene, and the infection was finally identified as K. kingae. The patient was successfully treated with cefotiam (CTM) for the first 7 days followed by the administration of trimethoprim-sulfamethoxazole (ST) for an additional 2 months. The K. kingae isolate was confirmed as a sure causative pathogen by observing that the serum showed high agglutinin titers against the isolate. Accumulation of the case reports in Japan with the isolation of this species is essential for clarifying invasive infections due to K. kingae. Our case report is a noteworthy and useful piece of information.


Assuntos
Tornozelo/patologia , Artrite Infecciosa/tratamento farmacológico , Cefotiam/uso terapêutico , Kingella kingae/isolamento & purificação , Osteomielite/tratamento farmacológico , Combinação Trimetoprima e Sulfametoxazol/uso terapêutico , Artrite Infecciosa/diagnóstico , Pré-Escolar , Humanos , Japão , Masculino , Osteomielite/diagnóstico , Resultado do Tratamento
13.
ANZ J Surg ; 83(9): 641-5, 2013 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-22946966

RESUMO

BACKGROUND: The aim of this study was to investigate the hypothesis that prevention of surgical site infection (SSI) is equally effective when patients receive single-dose (SD) or three-dose antibiotic prophylaxis with second-generation cephalosporin and metronidazole in elective colorectal surgery. METHODS: Ninety-three patients were enrolled from May 2009 to November 2010. The SD group received only one preoperative prophylactic intravenous dose and the three-dose or multiple-dose (MD) group received one preoperative prophylactic and two additional post-operative doses of second-generation cephalosporin and metronidazole. The incidence of infectious complications (SSI of the incision site and organ/space) was compared in the two groups. RESULTS: The overall post-operative infection rate did not differ between the two groups (16.7% in the SD versus 13.3% in the MD, P = 0.653). The incidence of SSI of the incision site and organ/space also did not differ between the groups (6.3% (3/48) versus 4.4% (2/45), P = 0.700; 4.2% versus 6.7%, P = 0.593, respectively). The number of antibiotics administered was not an independent risk factor for SSIs in multivariable analysis. CONCLUSIONS: SD antibiotic prophylaxis with second-generation cephalosporin and metronidazole is equivalent to a three-dose prophylaxis for preventing SSI in elective colorectal surgery. But further study would be needed to clarify this because of the small number of participants.


Assuntos
Antibacterianos/administração & dosagem , Antibioticoprofilaxia/métodos , Cefotiam/administração & dosagem , Colectomia , Metronidazol/administração & dosagem , Reto/cirurgia , Infecção da Ferida Cirúrgica/prevenção & controle , Administração Intravenosa , Adulto , Idoso , Idoso de 80 Anos ou mais , Antibacterianos/uso terapêutico , Cefotiam/uso terapêutico , Esquema de Medicação , Quimioterapia Combinada , Procedimentos Cirúrgicos Eletivos , Feminino , Humanos , Incidência , Masculino , Metronidazol/uso terapêutico , Pessoa de Meia-Idade , Cuidados Pós-Operatórios/métodos , Cuidados Pré-Operatórios/métodos , Modelos de Riscos Proporcionais , Fatores de Risco , Infecção da Ferida Cirúrgica/epidemiologia , Infecção da Ferida Cirúrgica/etiologia , Resultado do Tratamento
14.
Mod Rheumatol ; 22(4): 610-5, 2012 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-22068684

RESUMO

Pneumatosis intestinalis (PI) is a comparatively rare disease characterized by the presence of intramural gas in the gastrointestinal tract. PI is known to be associated with several clinical conditions, such as pulmonary diseases, gastrointestinal diseases, and traumatic injury, as well as autoimmune disorders. In particular, PI is commonly seen in systemic sclerosis (SSc) but rarely in systemic lupus erythematosus and dermatomyositis (DM). In this report, we present three cases of PI presenting in autoimmune diseases, including DM, Sjögren's syndrome, and limited SSc, and further discuss its background characteristics.


Assuntos
Doenças Autoimunes/diagnóstico , Dermatomiosite/diagnóstico , Lúpus Eritematoso Sistêmico/diagnóstico , Pneumatose Cistoide Intestinal/diagnóstico , Escleroderma Sistêmico/diagnóstico , Adulto , Antibacterianos/uso terapêutico , Doenças Autoimunes/complicações , Cefotiam/uso terapêutico , Colostomia , Terapia Combinada , Dermatomiosite/complicações , Diagnóstico Diferencial , Evolução Fatal , Feminino , Humanos , Lúpus Eritematoso Sistêmico/complicações , Pessoa de Meia-Idade , Terapia Nutricional , Pneumatose Cistoide Intestinal/complicações , Pneumatose Cistoide Intestinal/terapia , Indução de Remissão , Escleroderma Sistêmico/complicações , Tomografia Computadorizada por Raios X
15.
Drug Metab Pharmacokinet ; 26(6): 602-11, 2011.
Artigo em Inglês | MEDLINE | ID: mdl-21897051

RESUMO

ß-Lactam antibiotics have cerebral and peripheral adverse effects. Multidrug resistance-associated protein 4 (MRP4) has been reported to transport several ß-lactam antibiotics, and its expression at the blood-brain barrier also serves to limit their distribution to the brain. Therefore, the purpose of this study was to clarify the structure-activity relationship of MRP4-mediated transport of ß-lactam antibiotics using MRP4-expressing Sf9 membrane vesicles. The transport activity was evaluated as MRP4-mediated transport per MRP4 protein [nL/(min·fmol MRP4 protein)] based on measurement of MRP4 protein expression by means of liquid chromatography-tandem mass spectrometry. Cefotiam showed the greatest MRP4-mediated transport activity [8.90 nL/(min·fmol MRP4 protein)] among the ß-lactam antibiotics examined in this study. Measurements of differential transport activity of MRP4 for various ß-lactam antibiotics indicated that (i) cephalosporins were transported via MRP4 at a greater rate than were penams, ß-lactamase inhibitors, penems, or monobactams; (ii) MRP4-mediated transport activity of anionic cephalosporins was greater than that of zwitterionic cephalosporins; and (iii) higher-molecular-weight anionic ß-lactam antibiotics showed greater MRP4-mediated transport activity than lower-molecular-weight ones, whereas zwitterionic ß-lactam antibiotics did not show molecular weight dependency of MRP4-mediated transport. These quantitative data should prove useful for understanding MRP-related adverse effects of ß-lactam antibiotics and their derivatives.


Assuntos
Antibacterianos/química , Antibacterianos/farmacocinética , Proteínas Associadas à Resistência a Múltiplos Medicamentos/metabolismo , beta-Lactamas/química , beta-Lactamas/metabolismo , Transporte Biológico , Barreira Hematoencefálica/metabolismo , Cefotiam/metabolismo , Humanos , Peso Molecular , Proteínas Associadas à Resistência a Múltiplos Medicamentos/biossíntese , Proteínas Associadas à Resistência a Múltiplos Medicamentos/genética , Relação Estrutura-Atividade
16.
Hinyokika Kiyo ; 56(10): 559-63, 2010 Oct.
Artigo em Japonês | MEDLINE | ID: mdl-21063159

RESUMO

An adequate protocol for antimicrobial prophylaxis (AMP) in radical prostatectomy (RP) has not been established. We retrospectively compared the occurrence of perioperative infection following RP between two different AMP protocols. This study included 340 cases with prostate cancer who underwent RP at our institution between January 2005 and December 2008. The 1-day group consisting of 93 cases received a second generation cephem, cefotiam, intravenously during and after the operation on the operative day. The single dose group consisting of 247 cases received cefotiam during the operation only. The incidence of surgical site infection (SSI) and remote infection (RI) was retrospectively investigated. There was no significant difference in the rate of SSI and RI occurrence between the 1-day group (2.2, 0%) and single dose group (3.6, 0.4%) (p = 0.52). The single dose protocol of AMP seems sufficient for prevention of perioperative infection in RP.


Assuntos
Infecções Bacterianas/prevenção & controle , Cefotiam/administração & dosagem , Prostatectomia , Idoso , Humanos , Masculino , Complicações Pós-Operatórias/prevenção & controle , Neoplasias da Próstata/cirurgia , Estudos Retrospectivos , Infecção da Ferida Cirúrgica/prevenção & controle
19.
Euro Surveill ; 14(37)2009 Sep 17.
Artigo em Inglês | MEDLINE | ID: mdl-19761737

RESUMO

Antimicrobial resistance is an increasing problem in Neisseria gonorrhoeae (NG) treatment. Presently, third-generation parenteral cephalosporins, like ceftriaxone and cefotaxime, are the first option. Resistance to oral, but not to parenteral, third-generation cephalosporins has been reported previously. We analysed the microbial susceptibility (as minimum inhibitory concentration - MIC) of NG cultures obtained from high-risk visitors of the largest Dutch outpatient clinic for sexually transmitted infections (STI) in Amsterdam, the Netherlands. Among 1,596 visitors, we identified 102 patients with at least one NG isolate with reduced susceptibility to cefotaxime (0.125 microg/ml < MIC < or = 0.5 microg/ml). The percentage of NG isolates with reduced susceptibility to cefotaxime rose from 4.8% in 2006 to 12.1% in 2008 (chi2 17.5, p<0.001). With multivariate logistic regression, being a man who has sex with men (MSM) was significantly associated with reduced susceptibility to cefotaxime (p<0.001). Compared to susceptible NG isolates, those with decreased susceptiblity to cefotaxime were more often resistant also to penicillin (16.5% vs. 43.3%), tetracycline (21.5% vs. 68.9%) and ciprofloxacin (44.4% vs. 90.0%, all p<0.001). The increased prevalence of NG strains with reduced susceptibility to cefotaxime among MSM may herald resistance to third-generation parenteral cephalosporins. A considerable proportion of these strains show resistance to multiple antibiotics which could limit future NG treatment options.


Assuntos
Cefotiam/uso terapêutico , Síndrome de Creutzfeldt-Jakob/epidemiologia , Surtos de Doenças/estatística & dados numéricos , Gonorreia/tratamento farmacológico , Gonorreia/epidemiologia , Homossexualidade Masculina/estatística & dados numéricos , Neisseria gonorrhoeae , Adolescente , Adulto , Idoso , Antibacterianos/uso terapêutico , Surtos de Doenças/prevenção & controle , Farmacorresistência Bacteriana Múltipla , Humanos , Incidência , Masculino , Pessoa de Meia-Idade , Países Baixos/epidemiologia , Vigilância da População , Medição de Risco/métodos , Fatores de Risco , Adulto Jovem
20.
Hinyokika Kiyo ; 55(5): 259-61, 2009 May.
Artigo em Japonês | MEDLINE | ID: mdl-19507543

RESUMO

Cases 1 and 2 were a 84-year-old, 64-year-old female relatively. Case 2 had a history of uncontrolled diabetes mellitus. Both cases were referred to our hospital with a chief complaint of high fever. Initial diagnosis was acute pyelonephritis based on the findings of pyuria and right costovertebral angle knock pain. Abdominal computed tomography (CT) scan revealed a gas shadow in the right renal pelvis and calyx with right ureteral stone. The definitive diagnosis was emphysematous pyelonephritis (EPN). We selected transureteral catheterization into the right ureter immediately. Escherichia coli was identified from urine culture. Conservative therapy with antibiotics was also effective and general condition improved. Herein we discussed the etiology, symptomatology, choice of treatment and prognosis of emphysematous pyelonephritis. Recently CT is an effective imaging method for diagnosis at an early stage. Antibiotics therapy combined with transureteral drainage of gas-forming urolithiasis is effective as the initial conservative therapy.


Assuntos
Enfisema/terapia , Pielonefrite/terapia , Stents , Cateterismo Urinário , Idoso de 80 Anos ou mais , Cefotiam/administração & dosagem , Enfisema/diagnóstico , Enfisema/diagnóstico por imagem , Infecções por Escherichia coli , Feminino , Humanos , Pessoa de Meia-Idade , Pielonefrite/diagnóstico por imagem , Tomografia Computadorizada por Raios X , Resultado do Tratamento
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