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1.
Molecules ; 25(17)2020 Aug 23.
Artigo em Inglês | MEDLINE | ID: mdl-32842509

RESUMO

The SARS-CoV-2 outbreak caused an unprecedented global public health threat, having a high transmission rate with currently no drugs or vaccines approved. An alternative powerful additional approach to counteract COVID-19 is in silico drug repurposing. The SARS-CoV-2 main protease is essential for viral replication and an attractive drug target. In this study, we used the virtual screening protocol with both long-range and short-range interactions to select candidate SARS-CoV-2 main protease inhibitors. First, the Informational spectrum method applied for small molecules was used for searching the Drugbank database and further followed by molecular docking. After in silico screening of drug space, we identified 57 drugs as potential SARS-CoV-2 main protease inhibitors that we propose for further experimental testing.


Assuntos
Antivirais/química , Betacoronavirus/efeitos dos fármacos , Cisteína Endopeptidases/química , Mezlocilina/química , Inibidores de Proteases/química , Raltegravir Potássico/química , Proteínas não Estruturais Virais/química , Sítio Alostérico , Antivirais/farmacologia , Betacoronavirus/enzimologia , Betacoronavirus/patogenicidade , COVID-19 , Domínio Catalítico , Proteases 3C de Coronavírus , Infecções por Coronavirus/tratamento farmacológico , Infecções por Coronavirus/enzimologia , Infecções por Coronavirus/virologia , Cisteína Endopeptidases/genética , Cisteína Endopeptidases/metabolismo , Reposicionamento de Medicamentos , Expressão Gênica , Ensaios de Triagem em Larga Escala , Humanos , Mezlocilina/farmacologia , Simulação de Acoplamento Molecular , Pandemias , Pneumonia Viral/tratamento farmacológico , Pneumonia Viral/enzimologia , Pneumonia Viral/virologia , Inibidores de Proteases/farmacologia , Ligação Proteica , Conformação Proteica em alfa-Hélice , Conformação Proteica em Folha beta , Domínios e Motivos de Interação entre Proteínas , Raltegravir Potássico/farmacologia , SARS-CoV-2 , Termodinâmica , Proteínas não Estruturais Virais/antagonistas & inibidores , Proteínas não Estruturais Virais/genética , Proteínas não Estruturais Virais/metabolismo , Replicação Viral/efeitos dos fármacos
2.
Medicine (Baltimore) ; 99(26): e20914, 2020 Jun 26.
Artigo em Inglês | MEDLINE | ID: mdl-32590802

RESUMO

RATIONALE: Methicillin-resistant Staphylococcus aureus (MRSA) has been established as an important cause of severe community-acquired pneumonia (CAP) with very high mortality. Panton-Valentine leukocidin (PVL) producing MRSA has been reported to be associated with necrotizing pneumonia and worse outcome. The incidence of community-acquired MRSA (CA-MRSA) pneumonia is very low, as only a few CA-MRSA pneumonia cases were reported in the last few years. We present a case of severe CAP caused by PVL-positive MRSA with ensuing septic shock. PATIENT CONCERNS: A 68-year-old male with no concerning medical history had developed a fever that reached 39.0°C, a productive cough that was sustained for 5 days, and hypodynamia. He was treated with azithromycin and alexipyretic in a nearby clinic for 2 days in which the symptoms were alleviated. However, 1 day later, the symptoms worsened, and he was taken to a local Chinese medicine hospital for traditional medicine treatment. However, his clinical condition deteriorated rapidly, and he then developed dyspnea and hemoptysis. DIAGNOSIS: CA-MRSA pneumonia and septic shock. The sputum culture showed MRSA. Polymerase chain reaction of MRSA isolates was positive for PVL genes. INTERVENTIONS: Mechanical ventilation, fluid resuscitation, and antibiotic therapy were performed. Antibiotic therapy included mezlocillin sodium/sulbactam sodium, linezolid, and oseltamivir. OUTCOMES: He died after 12 hours of treatment. LESSONS: This is a report of severe pneumonia due to PVL-positive CA-MRSA in a healthy adult. CA-MRSA should be considered a pathogen of severe CAP, especially when combined with septic shock in previously healthy individuals.


Assuntos
Pneumonia Associada a Assistência à Saúde/etiologia , Staphylococcus aureus Resistente à Meticilina/patogenicidade , Infecções Estafilocócicas/complicações , Idoso , Antibacterianos/uso terapêutico , Tosse/etiologia , Pneumonia Associada a Assistência à Saúde/tratamento farmacológico , Pneumonia Associada a Assistência à Saúde/microbiologia , Humanos , Hipocinesia/etiologia , Linezolida/uso terapêutico , Masculino , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Mezlocilina/uso terapêutico , Oseltamivir/uso terapêutico , Choque Séptico/etiologia , Choque Séptico/mortalidade , Choque Séptico/fisiopatologia
3.
Medicine (Baltimore) ; 97(48): e13415, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-30508946

RESUMO

RATIONALE: Pyoderma gangrenosum (PG) is a rare postoperative complication of enterostomy, mostly developing from dermatitis, which may have serious consequence. PATIENT CONCERNS: A patient with lower rectal cancer receiving low anterior resection (LAR) and protective ileostomy was initially diagnosed with dermatitis, which very quickly developed to PG, though no medical or familial history was found. DIAGNOSIS: We diagnosed the patient with peristoaml dermatitis starting from a tiny skin ulceration, but corrected the diagnosis to PG because of the rapid development and severe consequences. INTERVENTIONS: Routine stoma care did not improve the condition, so we performed 2 terms of debridement, the closure of the stoma and autologous skin transplantation before finally solving the problem. OUTCOMES: The patient was discharged 60 days after the first surgery and 5 days after the last one. After 18 months of follow-up, the patient kept in a stable condition. LESSONS: Medical staff should not neglect peristoaml dermatitis because of its common occurrence. Once the situation develops beyond the doctors' expectation, more efforts should be made to treat it, even expand debridement if possible.


Assuntos
Desbridamento/métodos , Ileostomia/efeitos adversos , Pioderma Gangrenoso/terapia , Transplante de Pele/métodos , Antibacterianos/uso terapêutico , Humanos , Masculino , Mezlocilina/uso terapêutico , Pessoa de Meia-Idade , Transplante Autólogo , Óxido de Zinco/administração & dosagem , Óxido de Zinco/uso terapêutico
4.
Stroke ; 39(4): 1220-7, 2008 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-18309164

RESUMO

BACKGROUND AND PURPOSE: Fever after stroke is a strong predictor for a negative outcome with infections as the most common cause. The aim of this pilot study was to evaluate the effects of prophylactic antibiotic therapy on the incidence and height of fever after acute ischemic stroke. METHODS: This is a randomized, controlled study of antibiotic prophylaxis in patients with ischemic stroke enrolled within 24 hours from clinical onset who presented bedridden (modified Rankin score >3) with no significant infection. Interventions included prophylactic mezlocillin plus sulbactam (3 x 2 g/1 g for 4 days) or conventional management. Over 10 days, body temperature was continuously monitored, and the presence of infection was daily assessed. Primary end points were incidence and height of fever; secondary end points included rate of infection and clinical outcome. RESULTS: Sixty patients were included (mean, 75 years; median National Institutes of Health Stroke Scale score, 16). Over the first 3 days, patients in the intervention group showed lower mean body temperatures as well as lower daily peak temperatures (P<0.05). Throughout the observation period, 15 of 30 patients in the intervention group but 27 of 30 patients in the conventionally treated group developed an infection (P<0.05). Mean interval until the diagnosis of infection was 5.1 days in the intervention group and 3.3 days in the control group (P<0.05). Clinical outcome was more favorable in patients with prophylactic therapy (P=0.01). CONCLUSIONS: In patients with acute severe stroke, prophylactic administration of mezlocillin plus sulbactam over 4 days decreases body temperature, lowers the rate of infection, and may be associated with a better clinical outcome.


Assuntos
Antibacterianos/administração & dosagem , Isquemia Encefálica/tratamento farmacológico , Febre/prevenção & controle , Mezlocilina/administração & dosagem , Acidente Vascular Cerebral/tratamento farmacológico , Sulbactam/administração & dosagem , Doença Aguda , Idoso , Idoso de 80 Anos ou mais , Infecções Bacterianas/epidemiologia , Infecções Bacterianas/prevenção & controle , Isquemia Encefálica/epidemiologia , Quimioterapia Combinada , Feminino , Febre/epidemiologia , Humanos , Incidência , Masculino , Pessoa de Meia-Idade , Projetos Piloto , Prognóstico , Índice de Gravidade de Doença , Acidente Vascular Cerebral/epidemiologia , Resultado do Tratamento
5.
J Perinat Med ; 34(3): 203-6, 2006.
Artigo em Inglês | MEDLINE | ID: mdl-16602839

RESUMO

AIMS: To evaluate whether primary application of mezlozillin in preterm premature rupture of membranes (pPROM) prolongs pregnancy and lowers neonatal morbidity. METHODS: In this prospective, randomized, double blind, placebo-controlled multicenter study a total of 105 pregnant women with pPROM between 24 + 0 and 32 + 6 weeks of gestation were examined receiving i.v. injections of corticoids and tocolytics as well as mezlocillin (3 x 2 g/d) or placebo. Assessed factors were prolongation of pregnancy and neonatal morbidity such as neonatal infection, respiratory distress syndrome (RDS), intraventricular hemorrhage (IVH) and necrotizing enterocolitis (NEC). RESULTS: Prolongation of pregnancy by more than 7 days was achieved in 63.8% of the mezlocillin group versus 44.8% of the placebo group (P < 0.05). The babies of mothers treated with anibiotics had fewer neonatal infections, RDS, IVH and NEC. Total morbidity was significantly lowered in the verum group (P = 0.02). CONCLUSIONS: Antibiotic administration following preterm premature rupture of membranes is associated with a prolongation of pregnancy and a reduction of neonatal infectious morbidity.


Assuntos
Antibacterianos/uso terapêutico , Ruptura Prematura de Membranas Fetais/tratamento farmacológico , Mezlocilina/uso terapêutico , Infecções Bacterianas/epidemiologia , Infecções Bacterianas/prevenção & controle , Hemorragia Cerebral/epidemiologia , Método Duplo-Cego , Enterocolite Necrosante/epidemiologia , Feminino , Humanos , Recém-Nascido , Doenças do Recém-Nascido/epidemiologia , Doenças do Recém-Nascido/prevenção & controle , Gravidez , Resultado da Gravidez , Estudos Prospectivos , Síndrome do Desconforto Respiratório do Recém-Nascido/epidemiologia
6.
Zhonghua Fu Chan Ke Za Zhi ; 37(1): 25-6, 2002 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-11953060

RESUMO

OBJECTIVE: To study the appropriate antibiotic for prophylactic use in cesarean section. METHODS: The effects and side effects of prophylatic antibiotics in 1 266 cesarean section were studied retrospectively. Six regiems were engaged: (1) Penicillin and Ampicillin; (2) Mezlocillin sodium; (3) Sulbactam and Ampicillin; (4) Ciprofloxacin; (5) Clindamycin; (6) Cefacidal. RESULTS: The duration of postoperative body temperature return to normal of 1 - 6 group is (54.0 +/- 28.4) hours, (48.9 +/- 27.8) hours, (49.9 +/- 23.9) hours, (58.6 +/- 33.7) hours, (52.5 +/- 25.2) hours, (63.1 +/- 51.1) hours respectively. It was longer in cefazolin group than the others. There were less puerperal morbidity and side effects of Mezlocillin. CONCLUSIONS: Penicillin and Ampicillin are still the most common choices as prophylatic antibiotic in cesarean section. Mezlocillin is appropriate as well.


Assuntos
Antibacterianos/uso terapêutico , Infecção da Ferida Cirúrgica/prevenção & controle , Ampicilina/uso terapêutico , Antibioticoprofilaxia , Cesárea , Quimioterapia Combinada , Feminino , Humanos , Mezlocilina/uso terapêutico , Penicilinas/uso terapêutico , Estudos Retrospectivos , Sulbactam/uso terapêutico
7.
Clin Infect Dis ; 34(7): 902-8, 2002 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-11880954

RESUMO

We conducted a retrospective analysis of all bile specimens obtained for routine cultures from January 1995 through December 1999 at our tertiary care hospital. Results of microbiologic testing were linked to clinical parameters gathered by means of chart review. A total of 722 isolates were cultured from 345 of 454 bile specimens obtained from 288 individual patients. Prior receipt of a >7-day course of antibiotics (odds ratio [OR], 5.7), extensive leukocytosis (leukocyte count, >20,000 cells/microL) on admission (OR, 7.8), endoscopic or percutaneous biliary manipulation during the previous 14 days (OR, 2.9), and treatment in an internal medicine ward (OR, 2.5) were independent factors significantly associated (Pless-than-or-eq, slant.05) with recovery of Candida species from bile specimens. Culture of mezlocillin-resistant bacteria from bile specimens was independently associated with the specimen having been obtained >1 week after admission (OR, 3.8), lack of history of endoscopic biliary drainage (OR, 3.2), and high serum aspartate aminotransferase levels (>72 U/L) on admission (OR, 2.6). Prospective studies are warranted to evaluate accordingly adjusted empiric therapies for biliary infections.


Assuntos
Doenças dos Ductos Biliares/diagnóstico , Candidíase/diagnóstico , Bactérias/efeitos dos fármacos , Doenças dos Ductos Biliares/tratamento farmacológico , Doenças dos Ductos Biliares/microbiologia , Candida/efeitos dos fármacos , Candidíase/tratamento farmacológico , Resistência Microbiana a Medicamentos , Humanos , Mezlocilina/farmacologia , Testes de Sensibilidade Microbiana , Penicilinas/farmacologia , Penicilinas/uso terapêutico , Prognóstico , Estudos Retrospectivos
8.
Langenbecks Arch Surg ; 386(6): 397-401, 2001 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-11735011

RESUMO

BACKGROUND: Perioperative antibiotic prophylaxis surely reduces surgical infection rate. Pharmacokinetic data of oral ofloxacin in combination with its antibacterial spectrum suggest effective protection against perioperative infection. In addition, costs, adverse effects, and induction of microbial resistance are low. Therefore we performed a controlled randomized study comparing oral and intravenous single dose prophylaxis. METHODS: A total of 61 patients undergoing colonic or pancreatic resection randomly received either a single dose standard intravenous prophylaxis or ofloxacin 400 mg and metronidazole 500 mg orally 2 h before surgery. Postoperative infections were recorded for 3 weeks. RESULTS: Groups were very well comparable regarding age, overweight, concomitant disease, type and duration of surgery, blood loss, and volume support. Infectious complications occurred in 14.8% after parenteral and 3.3% after enteral antibiotic prophylaxis. There was no difference in post-operative hospital stay. CONCLUSION: The data demonstrate that single-dose oral ofloxacin is at least as effective as a standard intravenous prophylaxis in patients with colonic or pancreatic resection. It offers significant advantages regarding costs and ease of administration.


Assuntos
Antibioticoprofilaxia , Ofloxacino/uso terapêutico , Infecção da Ferida Cirúrgica/prevenção & controle , Administração Oral , Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/uso terapêutico , Colo/cirurgia , Feminino , Humanos , Injeções Intravenosas , Masculino , Metronidazol/administração & dosagem , Metronidazol/uso terapêutico , Mezlocilina/administração & dosagem , Mezlocilina/uso terapêutico , Pessoa de Meia-Idade , Ofloxacino/administração & dosagem , Pâncreas/cirurgia , Infecção da Ferida Cirúrgica/epidemiologia
9.
Infection ; 29(4): 222-7, 2001 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-11545485

RESUMO

BACKGROUND: Perioperative prophylaxis is recommended to be administered intravenously which, compared to oral prophylaxis, is more expensive. However, pharmacokinetic data on oral perioperative prophylaxis in patients with preoperative surgical and anesthesiological preparation are not available. PATIENTS AND METHODS: 40 patients with open hernial repair or cholecystectomy (low-risk group), colonic or pancreatic resection (high-risk group) received a standard single-dose perioperative prophylaxis with 4.5 g mezlocillin and 0.5 g metronidazole intravenously in addition to 400 mg ofloxacin orally 2 h prior to surgery. Antibiotic concentrations were measured perioperatively and pharmacokinetic data calculated. RESULTS: Serum and tissue concentrations of ofloxacin were above the MIC90 of the potential bacterial spectrum for surgical infection throughout the entire operation. Pharmacokinetic data were not influenced by preoperative surgical or anesthesiological preparation. CONCLUSION: Tissue and serum concentrations and the antibacterial spectrum of orally administered ofloxacin suggest effective protection against perioperative infection. Pharmacokinetic data confirm that oral ofloxacin may be used effectively as single-dose perioperative antibiotic prophylaxis. Since there are no clinical data comparing oral and intravenous singLe-dose prophylaxis, a prospective randomized clinical trial should be performed.


Assuntos
Anti-Infecciosos/farmacocinética , Anti-Infecciosos/uso terapêutico , Antibioticoprofilaxia , Ofloxacino/farmacocinética , Ofloxacino/uso terapêutico , Cuidados Pré-Operatórios/métodos , Administração Oral , Anti-Infecciosos/administração & dosagem , Humanos , Injeções Intravenosas , Metronidazol/farmacocinética , Metronidazol/uso terapêutico , Mezlocilina/farmacocinética , Mezlocilina/uso terapêutico , Ofloxacino/administração & dosagem , Penicilinas/farmacocinética , Penicilinas/uso terapêutico , Fatores de Risco , Resultado do Tratamento
10.
Int J Antimicrob Agents ; 17(3): 203-8, 2001 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-11282265

RESUMO

The in vitro susceptibility profile of Borrelia burgdorferi is not yet well defined for several antibiotics. Our study explored the in vitro susceptibility of B. burgdorferi to mezlocillin, meropenem, aztreonam, vancomycin, teicoplanin, ribostamycin and fusidic acid. Minimal inhibitory concentrations (MICs) and minimal borreliacidal concentrations (MBCs) were measured using a standardised colorimetric microdilution method and conventional subculture experiments. MIC values were lowest for mezlocillin (MIC(90), < or =0.06 mg/l) and meropenem (MIC(90), 0.33 mg/l). Vancomycin (MIC(90), 0.83 mg/l) was less effective in vitro. Borreliae proved to be resistant to aztreonam (MIC(90), >32 mg/l), teicoplanin (MIC(90), 6.6 mg/l), ribostamycin (MIC(90), 32 mg/l), and fusidic acid (MIC(90), >4 mg/l). The mean MBCs resulting in 100% killing of the final inoculum after 72 h of incubation were lowest for mezlocillin (MBC, 0.83 mg/l). This study gathered further data on the in vitro susceptibility patterns of the B. burgdorferi complex. The excellent in vitro effectiveness of acylamino-penicillin derivatives and their suitability for the therapy of Lyme disease is emphasised.


Assuntos
Antibacterianos/farmacologia , Grupo Borrelia Burgdorferi/efeitos dos fármacos , Aztreonam/farmacologia , Resistência Microbiana a Medicamentos , Ácido Fusídico/farmacologia , Humanos , Meropeném , Mezlocilina/farmacologia , Testes de Sensibilidade Microbiana , Monobactamas/farmacologia , Penicilinas/farmacologia , Ribostamicina/farmacologia , Teicoplanina/farmacologia , Tienamicinas/farmacologia , Vancomicina/farmacologia
11.
Antimicrob Agents Chemother ; 44(12): 3368-73, 2000 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-11083642

RESUMO

An amoxicillin-resistant (Amox(r)) strain of Helicobacter pylori was selected for by culturing an amoxicillin-sensitive (Amox(s)) strain in increasingly higher concentrations of amoxicillin, resulting in a 133-fold increase in MIC, from 0.03 to 0.06 microg/ml to 4 to 8 microg/ml. This resistance was stable upon freezing for at least 6 months and conferred cross-resistance to seven other beta-lactam antibiotics. beta-Lactamase activity was not detected in this Amox(r) strain; however, analysis of the penicillin-binding protein (PBP) profiles generated from isolated bacterial membranes of the Amox(s) parental strain and the Amox(r) strain revealed a significant decrease in labeling of PBP 1 by biotinylated amoxicillin (bio-Amox) in the Amox(r) strain. Comparative binding studies of PBP 1 for several beta-lactams demonstrated that PBP 1 in the Amox(r) strain had decreased affinity for mezlocillin but not significantly decreased affinity for penicillin G. In addition, PBP profiles prepared from whole bacterial cells showed decreased labeling of PBP 1 and PBP 2 in the Amox(r) strain at all bio-Amox concentrations tested, suggesting a diffusional barrier to bio-Amox or a possible antibiotic efflux mechanism. Uptake analysis of (14)C-labeled penicillin G showed a significant decrease in uptake of the labeled antibiotic by the Amox(r) strain compared to the Amox(s) strain, which was not affected by pretreatment with carbonyl cyanide m-chlorophenylhydrazone, eliminating the possibility of an efflux mechanism in the resistant strain. These results demonstrate that alterations in PBP 1 and in the uptake of beta-lactam antibiotics in H. pylori can be selected for by prolonged exposure to amoxicillin, resulting in increased resistance to this antibiotic.


Assuntos
Amoxicilina/farmacologia , Proteínas de Bactérias , Resistência a Múltiplos Medicamentos/fisiologia , Helicobacter pylori/metabolismo , Hexosiltransferases , Resistência às Penicilinas/fisiologia , Peptidil Transferases , Radioisótopos de Carbono , Proteínas de Transporte/metabolismo , Reações Cruzadas , Helicobacter pylori/efeitos dos fármacos , Helicobacter pylori/enzimologia , Humanos , Mezlocilina/farmacologia , Muramilpentapeptídeo Carboxipeptidase/metabolismo , Penicilina G/farmacologia , Proteínas de Ligação às Penicilinas , Resistência beta-Lactâmica/fisiologia , beta-Lactamases/metabolismo
14.
J Antimicrob Chemother ; 43(1): 133-6, 1999 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-10381111

RESUMO

The in-vitro activities of imipenem and four beta-lactam-beta-lactamase inhibitor combinations were tested against 816 strains of the Bacteroides fragilis group, and compared with other anti-anaerobic agents. None of the strains was resistant to metronidazole, and only one was resistant to chloramphenicol. Mezlocillin and piperacillin were moderately active, while clindamycin was the least active. Rates of resistance varied between various species. The new beta-lactam agents tested showed excellent activity; piperacillin-tazobactam and imipenem were the most active. The emergence of strains that are resistant to these agents, observed in this study, suggests there is a need to perform periodic antimicrobial susceptibility tests.


Assuntos
Antibacterianos/farmacologia , Bacteroides fragilis/efeitos dos fármacos , Amoxicilina/farmacologia , Ampicilina/farmacologia , Cefoxitina/farmacologia , Ceftizoxima/farmacologia , Cloranfenicol/farmacologia , Ácido Clavulânico/farmacologia , Clindamicina/farmacologia , Quimioterapia Combinada , Inibidores Enzimáticos/farmacologia , Imipenem/farmacologia , Metronidazol/farmacologia , Mezlocilina/farmacologia , Testes de Sensibilidade Microbiana , Ácido Penicilânico/análogos & derivados , Ácido Penicilânico/farmacologia , Penicilinas/farmacologia , Piperacilina/farmacologia , Especificidade da Espécie , Sulbactam/farmacologia , Tazobactam , Tienamicinas/farmacologia , Ticarcilina/farmacologia , Inibidores de beta-Lactamases
15.
Eur J Obstet Gynecol Reprod Biol ; 82(1): 5-9, 1999 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-10192476

RESUMO

OBJECTIVE: To evaluate the safety and efficacy of ultrasound-guided fine needle aspiration in the treatment of ovarian cysts during pregnancy. STUDY DESIGN: Nine out of twenty-nine patients between the 6th and the 16th week of gestation with unilateral ovarian cysts ranging between 65 and 540 cm3 in volume were selected for sonographically-guided fine needle aspiration. RESULTS: No complications were observed at either short or long-term follow-up; all patients delivered healthy infants at term. Clinical and sonographic post-partum follow-up was uneventful in all cases. In three cases it was necessary to repeat the procedure once and in one case twice during pregnancy. In one case a recurrent serous cyst was excised at operative laparoscopy performed 3 months after delivery. CONCLUSIONS: Ultrasound-guided fine needle aspiration was safely performed in nine patients as an alternative treatment to surgery when persistent monolateral and unilocular ovarian cysts with regular borders and completely anechoic structure are detected during pregnancy.


Assuntos
Cistos Ovarianos/cirurgia , Ovário/patologia , Complicações na Gravidez/cirurgia , Adulto , Biópsia por Agulha/métodos , Feminino , Humanos , Mezlocilina/uso terapêutico , Cistos Ovarianos/diagnóstico por imagem , Ovário/diagnóstico por imagem , Penicilinas/uso terapêutico , Gravidez , Complicações na Gravidez/diagnóstico por imagem , Resultado da Gravidez , Primeiro Trimestre da Gravidez , Segundo Trimestre da Gravidez , Progesterona/uso terapêutico , Recidiva , Sucção , Ultrassonografia Pré-Natal
16.
J Antimicrob Chemother ; 42(2): 147-52, 1998 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-9738831

RESUMO

In continuous-flow culture, long generation times and high bacterial counts favour survival of bacteria. A chemotherapeutic agent that achieves a bactericidal effect under these circumstances can therefore be seen as highly effective. In our continuous-flow culture we obtained bactericidal effects with ciprofloxacin 1-2 mg/L, cefotaxime 4 mg/L and mezlocillin 32 mg/L. These effects were seen irrespective of whether conditions were aerobic or anaerobic. There were no significant differences between monocultures and mixed cultures simulating faecal flora with the various Escherichia coli strains tested. Cefotaxime had an initial effect but an increase in counts was then observed as a result of regrowth of E. coli survivor strains in aerobic monoculture and mixed cultures. Mezlocillin was completely bactericidal in monocultures, but regrowth occurred in mixed cultures under anaerobic conditions. Neither the bacterial composition of this culture nor the resistance pattern explained this regrowth. These results were observed in long-term experiments followed for up to 7 days. We conclude that the antibiotics tested are highly effective against E. coli under unfavourable conditions simulating in-vivo situations.


Assuntos
Anti-Infecciosos/farmacologia , Ciprofloxacina/farmacologia , Escherichia coli/efeitos dos fármacos , Aerobiose , Anaerobiose , Cefotaxima/farmacologia , Cefalosporinas/farmacologia , Contagem de Colônia Microbiana , Meios de Cultura , Fezes/microbiologia , Gentamicinas/farmacologia , Mezlocilina/farmacologia , Penicilinas/farmacologia
17.
J Chromatogr A ; 812(1-2): 213-20, 1998 Jul 03.
Artigo em Inglês | MEDLINE | ID: mdl-9691320

RESUMO

High-performance liquid chromatographic methods have been developed for the determination of piperacillin and mezlocillin in human serum and urine samples. The methods involve ultrafiltration of samples followed by reaction with 1.5 M 1, 2, 4-triazole and 0.5 x 10(-3) M mercury (II) chloride in solution (pH 8.50) at 50 degrees C for 15 min. The resulting products were separated on a C18 column following stabilisation in an eluent containing sodium thiosulphate. They were detected at 323 nm for both penicillins. The methods have been applied to assays applied to assays of these penicillins in human serum and urine samples. The procedures, which permit the determination of penicillin concentration down to 0.1 microgram m1-1 in serum and 1 microgram m1-1 in urine samples, are specific to intact penicillins without interference from corresponding penicilloates [see J. Haginaka et al., Anal. Sci. 1 (1985) 73]. At concentrations of 1-500 micrograms ml-1 for each compound, the within- and between-day precisions were 1.8-4.8 and 3.7-6.9, respectively. The accuracy was ca. 100% for all samples assayed.


Assuntos
Mezlocilina/análise , Penicilinas/análise , Piperacilina/análise , Calibragem , Inibidores da Anidrase Carbônica/farmacologia , Cromatografia Líquida de Alta Pressão , Concentração de Íons de Hidrogênio , Indicadores e Reagentes , Mezlocilina/sangue , Mezlocilina/urina , Penicilinas/sangue , Penicilinas/urina , Piperacilina/sangue , Piperacilina/urina , Reprodutibilidade dos Testes , Soluções , Espectrofotometria Ultravioleta , Temperatura , Triazóis , Ultrafiltração
18.
J Neurol Neurosurg Psychiatry ; 64(3): 379-81, 1998 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-9527154

RESUMO

An accidental high dose of intraventricular mezlocillin was given during antibiotic treatment for pneumonia in a patient admitted because of severe traumatic brain injury and occlusive hydrocephalus. Because of serial epileptic seizures not responsive to antiepileptic drug treatment, CSF exchange was performed. The CSF was drained through a ventricular catheter, while mock CSF was infused into the lumbar subarachnoid space. The patient soon recovered to her clinical status previous to intraventricular mezlocillin application. Side effects of CSF exchange were not seen. Under continued antiepileptic medication no more seizures occurred. It is concluded that high doses of intraventricular mezlocillin have proconvulsive effects. In this patient CSF exchange was a suitable means of preventing putatively permanent impairment of brain function caused by serial epileptic seizures due to intraventricular mezlocillin application.


Assuntos
Drenagem/métodos , Epilepsia/induzido quimicamente , Epilepsia/terapia , Hidrocefalia/complicações , Erros de Medicação , Mezlocilina/envenenamento , Penicilinas/envenenamento , Pneumonia/tratamento farmacológico , Ventriculostomia , Adulto , Traumatismos Craniocerebrais/complicações , Drenagem/instrumentação , Monitoramento de Medicamentos , Overdose de Drogas , Epilepsia/líquido cefalorraquidiano , Feminino , Humanos , Hidrocefalia/diagnóstico por imagem , Hidrocefalia/terapia , Injeções Intraventriculares , Pneumonia/complicações , Tomografia Computadorizada por Raios X
19.
Hepatology ; 25(4): 833-6, 1997 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-9096584

RESUMO

Aminoglycosides are frequently used to treat sepsis in patients with liver disease. However, it has been suggested that cirrhotic patients are particularly sensitive to aminoglycoside-induced renal dysfunction. We investigated the efficacy and incidence of renal impairment with netilmicin plus mezlocillin compared with ceftazidime in 128 cirrhotic patients who required empirical treatment for sepsis. Renal impairment developed in 8 of 63 (13%) patients receiving netilmicin compared with 2 of 65 (3%) patients receiving ceftazidime (P < .05); it occurred despite regular monitoring of trough netilmicin levels. Renal impairment was present at the time of death in 1 of 13 (8%) patients treated with ceftazidime compared with 5 of 9 (56%) of the netilmicin patients (P < .05). Mortality rates were similar in the two groups (ceftazidime 20%, aminoglycoside 14%; P = NS). Renal dysfunction is significantly more frequent in cirrhotic patients treated with netilmicin but with careful attention to dosage and fluid management the clinical effect is likely to be relatively modest.


Assuntos
Ceftazidima/uso terapêutico , Cefalosporinas/uso terapêutico , Quimioterapia Combinada/administração & dosagem , Cirrose Hepática/complicações , Mezlocilina/administração & dosagem , Netilmicina/administração & dosagem , Sepse/complicações , Sepse/tratamento farmacológico , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Quimioterapia Combinada/efeitos adversos , Feminino , Gentamicinas/administração & dosagem , Gentamicinas/efeitos adversos , Humanos , Rim/efeitos dos fármacos , Rim/fisiopatologia , Masculino , Pessoa de Meia-Idade , Netilmicina/efeitos adversos , Penicilinas/administração & dosagem , Estudos Prospectivos
20.
Eur J Clin Pharmacol ; 53(2): 111-5, 1997.
Artigo em Inglês | MEDLINE | ID: mdl-9403281

RESUMO

OBJECTIVE: In intensive care medicine, continuous detoxication methods, such as continuous veno-venous hemodialysis (CVVHD), are used for treating acute renal failure. However, in contrast to conventional hemodialysis, little is known about the pharmacokinetics of many drugs administered in this setting and guidelines for dosages of drugs often do not exist. This holds particularly true for broad-spectrum antibiotics, which are often required during intensive care. METHODS: In this study, we investigated the pharmacokinetics of the acylureidopenicillin mezlocillin and the beta-lactamase inhibitor sulbactam during CVVHD and deduced dosage recommendations from the kinetic parameters with the goal of maintaining trough levels of above 10 mg.l-1 for mezlocillin and 5 mg.l-1 for sulbactam. Six intensive care patients with acute renal failure, receiving mezlocillin (n = 5) and/or sulbactam (n = 4), were examined during CVVHD and during intervals between CVVHD. The serum concentrations and the amounts of the drugs excreted into the dialyzate and into the urine within one dosage interval were measured using high performance liquid chromatography (HPLC). Three of the patients were jaundiced, indicating functional impairment of the liver. RESULTS: The clearances by CVVHD (CLCVVHD) for mezlocillin ranged between 11.0 and 44.9 ml.min-1 and the half lives ranged between 1.12 and 8.84 h. Low CL and long half lives were observed in the patients with jaundice. For sulbactam, CLCVVHD ranged between 10.1 and 22.8 ml.min-1 and serum half lives were 4.25-6.11 h, independent of liver function. CONCLUSION: Due to high hepatobiliary clearance of mezlocillin, dosage adjustments in patients with acute renal failure, treated by CVVHD, are needed only with concurrent impaired liver function. For sulbactam, the optimal dose was found to be 0.5 g, administered every 12 h, regardless of liver function.


Assuntos
Injúria Renal Aguda/terapia , Antibacterianos/farmacocinética , Mezlocilina/farmacocinética , Penicilinas/farmacocinética , Diálise Renal/métodos , Sulbactam/farmacocinética , Adulto , Idoso , Antibacterianos/sangue , Área Sob a Curva , Feminino , Meia-Vida , Humanos , Unidades de Terapia Intensiva , Masculino , Taxa de Depuração Metabólica , Mezlocilina/sangue , Pessoa de Meia-Idade , Penicilinas/sangue , Sulbactam/sangue
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