RESUMEN
Embryonated hens' eggs can be reliably infected by Pseudomonas aeruginosa in laboratory experiments. Therapy tests with the antibiotics azlocillin (CAS 37091-66-0) and gentamicin (CAS 13291-74-2) on this type of infected hens' eggs demonstrate that this test system offers a realistic alternative to septic experiments with small laboratory rodents. Chick embryos survive a lethal Pseudomonas infection when azlocillin or gentamicin in a relevant therapeutic dose are administered immediately after the infective agent. The use of Pseudomonas infected chick embryos in the screening for new antiinfectives allows, therefore, a considerable reduction of the number of laboratory rodents required.
Asunto(s)
Antibacterianos/uso terapéutico , Embrión de Pollo/microbiología , Infecciones por Pseudomonas/tratamiento farmacológico , Alternativas a las Pruebas en Animales , Animales , Azlocilina/uso terapéutico , Evaluación Preclínica de Medicamentos , Gentamicinas/uso terapéutico , Infecciones por Pseudomonas/microbiologíaRESUMEN
The Candida infected, embryonated hen's egg is a realistic complement for the model of the Candida infected mouse and can be used in the search for new systemically active antimycotics. This alternative method is rapid, sensitive convincing and inexpensive. The use of the embryonated hen's egg in an anti-Candida screening can reduce the use of small laboratory animals to a considerable amount. Thus, with the help of this new method pain and suffering of animals can be reduced in a part of the biologic-medical research in the sense of the animal protection law.
Asunto(s)
Antifúngicos/uso terapéutico , Candidiasis/tratamiento farmacológico , Anfotericina B/uso terapéutico , Alternativas a las Pruebas en Animales , Animales , Candida albicans/patogenicidad , Candidiasis/microbiología , Embrión de Pollo , Fluconazol/uso terapéutico , Propilenglicol , Glicoles de Propileno/uso terapéuticoRESUMEN
The pharmacokinetics of the broad spectrum cephem RU 29 246 and its prodrug-ester HR 916 B were investigated in mice, rats and dogs and compared to those of cefpodoxime proxetil, cefuroxime axetil and cefixime. HR 916 B is well absorbed following oral administration and efficiently converted to the antibacterially active form. In mice, mean peak blood levels of 31.1 micrograms/ml of the parent compound were recorded within 20 minutes after oral administration of a single dose equivalent to 40 mg/kg RU 29 246. The bioavailability calculated on the basis of the areas under the concentration-time curves (AUC) and the urinary recoveries was about 90%. In rats, peak blood levels of 14.5 micrograms/ml were obtained 1 hour after an oral 20 mg/kg dose. The bioavailability was calculated as 70%. In dogs, 40% of an oral 10 mg/kg dose was recovered in the urine within 24 hours. Cmax was 15.9 micrograms/ml at 4.6 hours. Mean elimination half-lives of RU 29 246 were 0.35, 0.5 and 2.1 hours in mice, rats and dogs, respectively. After an oral HR 916 B dose equivalent to 50 mg/kg of RU 29 246, tissue concentrations at 0.5 hour ranged between 0.8 micrograms/g in brain and 95.7 micrograms/g in murine kidneys. These values of HR 916 B are similar to, or distinctly higher than, those of the reference compounds. Of the oral cephalosporins tested, HR 916 B had the most balanced antibacterial spectrum. With ED50s of between 0.9 and 11.5 mg/kg against staphylococci, its activity was similar to that of the additional reference compound cefaclor and higher than that of cefuroxime. Cefixime and cefpodoxime proxetil displayed low antistaphylococcal activity or were inactive. In septicemias with Enterobacteriaceae, cefixime and cefpodoxime proxetil were more potent than HR 916 B and cefaclor. Cefuroxime axetil was inactive against most of these infections. HR 916 B was also highly effective against murine lung infections caused by Klebsiella pneumoniae DT-S or Streptococcus pneumoniae 1147.
Asunto(s)
Cefalosporinas/farmacocinética , Profármacos/farmacocinética , Animales , Cefalosporinas/uso terapéutico , Perros , Femenino , Masculino , Ratones , Neumonía/tratamiento farmacológico , Ratas , Ratas Endogámicas , Sepsis/tratamiento farmacológico , Distribución TisularRESUMEN
The pharmacokinetic profile of cefpirome was evaluated in rats and dogs after a single intravenous or intramuscular dose. A two-compartment open model was used for the calculation of the pharmacokinetic parameters for both routes of administration. The elimination half-lives after intravenous and intramuscular administration of 20 mg/kg cefpirome did not differ significantly and ranged from 0.4 h in rats to 1.1 h in dogs. Cefpirome was mainly excreted via the kidneys. After iv or im dosing of the compound, between 80% (dogs) and 90% (rats) was recovered in urine within 24 h. The bioavailability of cefpirome in rats and dogs after both routes of administration was almost identical when calculated either by the AUC or the urinary recovery rates.
Asunto(s)
Cefalosporinas/farmacocinética , Animales , Disponibilidad Biológica , Cefalosporinas/administración & dosificación , Cefalosporinas/sangre , Perros , Relación Dosis-Respuesta a Droga , Inyecciones Intramusculares , Inyecciones Intravenosas , Masculino , Ratas , Ratas Endogámicas , CefpiromaRESUMEN
Cefpirome, cefoperazone and ceftazidime were tested for their in-vitro activity against Enterococcus faecalis and methicillin-resistant Staphylococcus aureus (MRSA) isolates. Cefpirome was the most active cephalosporin followed by cefoperazone. Ceftazidime had only very limited activity against these strains. In experiments with cefpirome/vancomycin and cefoperazone/vancomycin combinations, synergy was detected against most MRSA strains and some enterococci. Antagonism did not occur.
Asunto(s)
Cefoperazona/farmacología , Cefalosporinas/farmacología , Enterococcus/efectos de los fármacos , Staphylococcus aureus/efectos de los fármacos , Vancomicina/farmacología , Quimioterapia Combinada/farmacología , Resistencia a la Meticilina , Pruebas de Sensibilidad Microbiana , CefpiromaRESUMEN
The aminothiazolyl-cephalosporin RU 29 246 is the active metabolite of the prodrug-pivaloyl-oxyethyl-ester HR 916. RU 29 246 in vitro activity includes a wide range of clinically relevant bacterial pathogens. Against methicillin-sensitive Staphylococci RU 29 246 (MIC90 of 0.25 approximately 2 micrograms/ml) was clearly more active than cefaclor, cefuroxime, cefpodoxime, cefixime and ceftibuten, but slightly less active than cefdinir. RU 29 246 inhibited hemolytic Streptococci of the serogroups A, B, C and G as well as penicillin-sensitive Streptococcus pneumoniae at concentrations similar to cefdinir, cefpodoxime and cefuroxime (MIC90 less than or equal to 0.13 micrograms/ml), but less than the other oral cephalosporins investigated (cefixime, cefaclor and ceftibuten). MIC90s of RU 29 246 against Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Salmonella spp., Shigella spp., Proteus mirabilis and Haemophilus influenzae were less than or equal to 0.5 micrograms/ml. Only RU 29 246 and cefdinir demonstrated moderate activity against Acinetobacter baumannii (MIC90 greater than or equal to 4 micrograms/ml). Most strains of Pseudomonas spp., Serratia marcescens, Enterobacter spp., Hafnia alvei and Bacteroides spp. were resistant to RU 29 246. RU 29 246 killed Escherichia coli and Staphylococcus aureus at a rate of 99% to 99.9% at concentrations of two times MIC. The pH value of the medium (range 5.5 to 8.5) and the inoculum size (range 10(5) to 10(7) cfu/ml) had no or only low influence on the antibacterial activity of RU 29 246. RU 29 246 is a broad spectrum cephalosporin including in its activity both Gram-positive and Gram-negative pathogens and therefore--depending on the bioavailability of its prodrug--looks promising as to its therapeutic perspective.
Asunto(s)
Antibacterianos/farmacología , Cefalosporinas/farmacología , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Profármacos/farmacología , Concentración de Iones de Hidrógeno , Pruebas de Sensibilidad MicrobianaRESUMEN
The aminothiazolyl-cephalosporin RU 29 246, the active metabolite of the prodrug-ester HR 916, is active against strains producing the widespread plasmid-encoded TEM-1, TEM-2 and SHV-1 beta-lactamases. Except for TEM-7 the activity of RU 29 246 against strains producing extended broad spectrum beta-lactamases (TEM-3, TEM-5, TEM-6, SHV-2, SHV-4, SHV-5, CMY-1, CTX-M), however, is low. Relative hydrolysis rates of RU 29 246 are comparable with those of cefpodoxime, the active metabolite of CS-807, and are extremely low for the TEM-1 and SHV-1 beta-lactamases. The compound demonstrates remarkable inhibitory activity against the chromosomal beta-lactamase of Enterobacter cloacae P99. In the presence of 1.7 microM this enzyme loses 50% of its activity. At concentrations of 0.43, 0.003 and 0.01 micrograms/ml the compound binds preferentially to the penicillin-binding protein (PBP) 3 of Escherichia coli K12, to the PBPs 2x and 3 of Streptococcus pneumoniae R6 and to PBP 1 of Staphylococcus aureus SG 511, respectively.
Asunto(s)
Antibacterianos/farmacología , Proteínas Bacterianas , Proteínas Portadoras/metabolismo , Cefalosporinas/farmacología , Hexosiltransferasas , Muramoilpentapéptido Carboxipeptidasa/metabolismo , Penicilinas/metabolismo , Peptidil Transferasas , Profármacos/farmacología , beta-Lactamasas/metabolismo , Unión Competitiva , Cefalosporinas/metabolismo , Estabilidad de Medicamentos , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Gramnegativas/enzimología , Pruebas de Sensibilidad Microbiana , Proteínas de Unión a las Penicilinas , PlásmidosRESUMEN
The in-vitro activity of cefpirome was compared with other antibiotics against organisms causing sexually transmitted diseases (STD). The excellent activity of cefpirome against Neisseria gonorrhoeae (MIC90 1.0 mg/L), Haemophilus ducreyi (MIC90 0.5 mg/L), and Gardnerella vaginalis (MIC90 1.0 mg/L) suggests that this agent might be useful in the empirical treatment of a variety of venereal diseases.
Asunto(s)
Cefalosporinas/farmacología , Enfermedades Bacterianas de Transmisión Sexual/microbiología , Chancroide/microbiología , Chlamydia/efectos de los fármacos , Infecciones por Chlamydia/microbiología , Gardnerella vaginalis/efectos de los fármacos , Gonorrea/microbiología , Haemophilus ducreyi/efectos de los fármacos , Humanos , Pruebas de Sensibilidad Microbiana , Neisseria gonorrhoeae/efectos de los fármacos , Penicilinas/farmacología , Quinolonas/farmacología , CefpiromaRESUMEN
The in vivo potency of cefodizime (HR 221), tiprotimod (a new synthetic thiazole derivative of HR 221, HBW 538) and cefotaxime to modulate the initiation of immune response in the draining lymph node (LN) after subcutaneous injection of SRBC was evaluated. The timing and sequence of events in the regional LN was investigated by immunophenotypization of node cells with monoclonal antibodies, and the systemic reaction was estimated as primary antibody response to SRBC. From the results it is possible to conclude that: (1) subcutaneous administration of a small dose (2.5-3.0 mg/kg) of cephalosporins, together with antigen, enhanced primary antibody production and persistence; (2) the increase in serum antibodies was preceded by a change in percentage of L3T4+ cells within the regional (popliteal) lymph node. In comparison to antigen alone, cephalosporins (during early immune response) increased the percentage of L3T4+ cells; (3) LN cellularity was strongly enhanced by cephalosporins; (4) cefotaxime influenced the kinetics of the cellularity and the L3T4/Lyt-2 index differently than cefodizime and HBW 538. HBW 538 had either a similar or stronger effect than cefodizime, as judged by the adjuvant effect on antibody production and the appearance of L3T4+ cells during the immunizing period.
Asunto(s)
Formación de Anticuerpos/efectos de los fármacos , Cefotaxima/análogos & derivados , Cefalosporinas/farmacología , Animales , Anticuerpos Monoclonales , Formación de Anticuerpos/inmunología , Antígenos/inmunología , Cefotaxima/farmacología , Eritrocitos/inmunología , Femenino , Hipertrofia/inmunología , Inmunofenotipificación , Isoanticuerpos/inmunología , Ganglios Linfáticos/efectos de los fármacos , Ganglios Linfáticos/inmunología , Ganglios Linfáticos/patología , Ratones , Ratones Endogámicos CBA , Factores de TiempoRESUMEN
Cefquinome is a new injectable aminothiazolyl cephalosporin derivative. It is stable against chromosomally and plasmid-encoded beta-lactamases and has a broad antibacterial spectrum. Staphylococcus aureus, streptococci, Pseudomonas aeruginosa, and members of the family Enterobacteriaceae (Escherichia coli, Salmonella spp., Klebsiella spp., Enterobacter spp., Citrobacter spp., and Serratia marcescens) are inhibited at low concentrations. Cefquinome is also active against many strains of methicillin-resistant staphylococci and enterococci. Its in vitro activity against gram-negative anaerobes is very limited. The high in vitro activity of cefquinome is reflected by its high in vivo efficacy against experimental septicemia due to different gram-positive and gram-negative bacteria. We studied the pharmacokinetic properties of cefquinome in mice, dogs, pigs, and calves. After single parenteral administrations, cefquinome displayed high peak levels, declining with half-lives of about 0.5, 0.9, 1.2, and 1.3 h, respectively. The areas under the concentration-time curve determined for dogs and mice showed linear correlations to the given doses. In dogs the urinary recovery was more than 70% within 24 h of dosing.
Asunto(s)
Antibacterianos/farmacología , Proteínas Bacterianas , Cefalosporinas/farmacología , Hexosiltransferasas , Peptidil Transferasas , Animales , Antibacterianos/metabolismo , Antibacterianos/farmacocinética , Bacterias Anaerobias/efectos de los fármacos , Proteínas Sanguíneas/metabolismo , Proteínas Portadoras/metabolismo , Bovinos , Cefalosporinas/metabolismo , Cefalosporinas/farmacocinética , Medios de Cultivo , Perros , Estabilidad de Enzimas , Femenino , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Caballos , Concentración de Iones de Hidrógeno , Masculino , Ratones , Pruebas de Sensibilidad Microbiana , Muramoilpentapéptido Carboxipeptidasa/metabolismo , Proteínas de Unión a las Penicilinas , Sepsis/tratamiento farmacológico , Porcinos , beta-Lactamasas/metabolismoRESUMEN
Due to the important role of monocytes/macrophages in the pathogenesis of AIDS, potential drugs with anti-HIV activity in lymphocytes must also be effective in monocytes/macrophages. For testing the efficacy of antiviral substances, monocytes/macrophages from peripheral blood were infected, respectively, with highly replicating HIV1 and HIV2 strains, thereby providing an extremely sensitive system of testing. Azidothymidine was found to inhibit both HIV types at 0.04 microgram/ml. The polysulphated polyxylan, Hoe/Bay-946 (MW 6,000 Daltons), which acts through a different mechanism and is being tested in clinical pilot studies in Germany, was also found to be effective against HIV1 and HIV2 in macrophages at concentrations of 10-50 micrograms/ml.
Asunto(s)
Síndrome de Inmunodeficiencia Adquirida/tratamiento farmacológico , Antivirales/farmacología , VIH-1/efectos de los fármacos , VIH-2/efectos de los fármacos , Macrófagos/microbiología , Monocitos/microbiología , Polisacáridos/farmacología , Replicación Viral/efectos de los fármacos , Células Cultivadas , Humanos , Macrófagos/efectos de los fármacos , Monocitos/efectos de los fármacos , Poliéster Pentosan SulfúricoRESUMEN
In systemic and local infections, the therapeutic efficacy of cefpirome was compared to that of imipenem and cefotaxime. Murine septicemia induced with methicillin-sensitive and methicillin-resistant Staphylococcus aureus strains responded well to cefpirome and imipenem therapy, the ED50 values ranged from 0.8 to 28.40 mg/kg and 0.5 to 15.58 mg/kg, respectively. The carbapenem also displayed high efficacy against Enterococci and was more potent than cefpirome. Cefotaxime, however, exhibited lower activity or proved to be inactive against these strains. With ED50 values of 0.03 to 31.33 mg/kg, cefpirome was the most active of the three antibiotics in protecting mice challenged with Enterobacteriaceae. The corresponding ED50 values of imipenem and cefotaxime ranged from 0.72 to 70.95 mg/kg and 0.06 to 66.30 mg/kg, respectively. Despite distinctly lower in vitro activity against the infecting organism, cefpirome showed efficacy similar to imipenem in the treatment of subcutaneous S. aureus abscesses in mice. It was more effective than imipenem and cefotaxime against experimental Klebsiella pneumonia in mice and the Escherichia coli infected granuloma pouch in rats.
Asunto(s)
Infecciones Bacterianas/tratamiento farmacológico , Cefalosporinas/uso terapéutico , Imipenem/uso terapéutico , Absceso/tratamiento farmacológico , Animales , Cefotaxima/farmacología , Cefotaxima/uso terapéutico , Cefalosporinas/farmacología , Infecciones por Enterobacteriaceae/tratamiento farmacológico , Infecciones por Escherichia coli/tratamiento farmacológico , Femenino , Granuloma/tratamiento farmacológico , Imipenem/farmacología , Masculino , Ratones , Ratones Pelados , Ratones Endogámicos C3H , Neumonía/tratamiento farmacológico , Ratas , Ratas Endogámicas , Sepsis/tratamiento farmacológico , Infecciones Cutáneas Estafilocócicas/tratamiento farmacológico , Staphylococcus aureus/efectos de los fármacos , Infecciones Estreptocócicas/tratamiento farmacológico , CefpiromaAsunto(s)
Cefotaxima/farmacología , Cefotaxima/farmacocinética , Lactamas/farmacología , Lactamas/farmacocinética , Antibacterianos/sangre , Antibacterianos/farmacocinética , Antibacterianos/farmacología , Cefotaxima/sangre , Sinergismo Farmacológico , Fermentación , Cinética , Lactamas/sangre , Modelos Biológicos , Distribución TisularRESUMEN
Xylanpoly-(hydrogen sulphate) disodium salt with a molecular weight of about 6000 daltons (HOE/BAY 946) completely inhibited syncytium formation induced by the infection of T lymphocytes with HIV as well as viral replication at concentrations above 25 micrograms/ml. This dose was found to be inhibitory for several strains of HIV-1 and HIV-2. Low molecular weight fractions of the compound were less active against HIV, and high molecular derivatives were as active as HOE/BAY 946. A direct influence of the drug on the infectivity of the virus could not be demonstrated. The drug inhibited the reverse transcriptase of HIV. Treatment of permanently HIV-infected U937 cells resulted in a drastic reduction of virus particles released into the supernatant and points to an additional mode of action. A therapeutic effect of HOE/BAY 946 against retroviruses in vivo could be demonstrated in Friend leukaemia virus-infected mice. A clinical pilot study with the compound was started recently in Germany with AIDS patients who did not tolerate or refused to take zidovudine and with asymptomatic virus carriers.
Asunto(s)
VIH/efectos de los fármacos , Polisacáridos/farmacología , Replicación Viral/efectos de los fármacos , Animales , Antivirales/farmacología , Médula Ósea/efectos de los fármacos , Células de la Médula Ósea , Supervivencia Celular/efectos de los fármacos , Femenino , VIH/enzimología , VIH/fisiología , VIH-1/efectos de los fármacos , VIH-1/fisiología , VIH-2/efectos de los fármacos , VIH-2/fisiología , Humanos , Técnicas In Vitro , Interleucina-1/biosíntesis , Linfocitos/citología , Linfocitos/efectos de los fármacos , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Ratones , Oxígeno/metabolismo , Poliéster Pentosan Sulfúrico , Inhibidores de la Transcriptasa InversaRESUMEN
7-[2-(2-Aminothiazol-4-yl)-2-(Z)-oxyiminoacetamido]-3-[(s ubs tituted-1-pyridinio)methyl]ceph-3-em-4-carboxylates II are a group of beta-lactam antibiotics with extraordinary high antibacterial activity. The promising member of this group, cefpirome (HR 810, II-1) is a candidate for clinical use. Synthetic pathways to II starting from cefotaxime derivatives I or 7-aminocephalosporanic acid (7-ACA) are described. A preferred method for the conversion of I to II or 7-ACA to precursors III respectively employs iodotrimethylsilane and an excess of the pyridine base. Structure-activity studies reveal an optimum overall activity in the series of pyridines with fused saturated and unsaturated rings or cyclopropyl- and alkoxy substituents. Favorable oxyimino substituents are methyl, ethyl, difluoromethyl and carbamoylmethyl groups. Acidic substituents lead to decreased activity against Staphylococcus aureus SG 511. Introduction of halogen in the thiazole nucleus causes improvement of activity against the K1 beta-lactamase producing Klebsiella aerogenes 1082 E strain.
Asunto(s)
Cefalosporinas/síntesis química , Animales , Cefalosporinas/farmacocinética , Cefalosporinas/farmacología , Fenómenos Químicos , Química , Perros , Haplorrinos , Humanos , Klebsiella/efectos de los fármacos , Klebsiella/enzimología , Espectroscopía de Resonancia Magnética , Ratones , Pseudomonas aeruginosa/efectos de los fármacos , Staphylococcus/efectos de los fármacos , Relación Estructura-Actividad , beta-Lactamasas/biosíntesis , CefpiromaRESUMEN
Cefotaxime (CTX) and HRE 664 (a novel penem antibiotic) possess complementary in vitro properties. Differences can be observed in their antibacterial spectra, their beta-lactamase stability and -inhibition, and their affinity to penicillin-binding proteins. These differences suggested that combinations of the cephalosporin and the penem antibiotic would be advantageous and should be studied. The fractional inhibitory concentration values of checkerboard studies confirmed that CTX and HRE 664 act synergistically against various Gram-positive and Gram-negative bacteria. Fixed combinations containing 80% CTX and 20% HRE 664 possess broader antibacterial spectra and in certain cases higher antibacterial activities than each of the components alone. The combinations had improved activity against Staphylococci including methicillin-resistant strains, beta-lactamase producing strains of Enterobacter sp. and Bacteroides fragilis. The combination as well as the single antibiotics had only limited activity against Pseudomonas aeruginosa.
Asunto(s)
Antibacterianos/administración & dosificación , Cefotaxima/administración & dosificación , Lactamas , Bacterias Anaerobias/efectos de los fármacos , Sinergismo Farmacológico , Bacterias Aerobias Gramnegativas/efectos de los fármacos , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Pruebas de Sensibilidad MicrobianaRESUMEN
The pharmacokinetic and chemotherapeutic properties of the new penem antibiotic HRE 664 (Fig. 1) were evaluated in experimental animals. High and sustained blood and serum levels were achieved following parenteral injection in mice, rats, dogs and monkeys. Half-lives ranged from 27 to 40 minutes in the various species tested. The antibiotic was well distributed in the rodents and penetrated well into tissues and body fluids. At 30 minutes after subcutaneous administration to mice (50 mg/kg), concentrations of between 12.4 and 35.9 micrograms/g were measured in the lungs, liver, heart and kidneys, that is 33 approximately 95% of the corresponding level in murine blood (37.7 micrograms/ml). In experimentally induced infections in mice, HRE 664 displayed good chemotherapeutic activity particularly against septicemias caused by methicillin-sensitive and methicillin-resistant Staphylococcus aureus strains and on abscess formation induced by Bacteroides fragilis. Most of the cephalosporins and other beta-lactam antibiotics exhibited low efficacy against these strains of bacteria.
Asunto(s)
Antibacterianos/farmacocinética , Infecciones Bacterianas/tratamiento farmacológico , Lactamas , Absceso/tratamiento farmacológico , Animales , Antibacterianos/uso terapéutico , Bioensayo , Cefotaxima/uso terapéutico , Perros , Macaca , Ratones , RatasRESUMEN
The new penem antibiotic HRE 664 displays potent antibacterial activity in vitro against a broad spectrum of clinically relevant bacterial strains including Gram-negative and Gram-positive aerobes and anaerobes. With an MIC 90% of 0.43 micrograms/ml, it is also active against methicillin-resistant staphylococci. HRE 664 is extremely stable against beta-lactamases, it binds preferentially to the penicillin-binding proteins 2, 3, 5 and 6 of Escherichia coli.
Asunto(s)
Antibacterianos , Lactamas , beta-Lactamas , Bacterias Aerobias/efectos de los fármacos , Bacterias Anaerobias/efectos de los fármacos , Enterobacteriaceae/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , beta-Lactamasas/metabolismoRESUMEN
The synthesis as well as in vitro antibacterial activity and pharmacokinetic behavior of cefodizime (HR 221, 1a), its analogs and derivatives is described. In this comparison, cefodizime stands out for its balance between its high antibacterial activity, prolonged elimination half-life and high AUC in mice and dogs.