RESUMEN
The cephalosporins have been available for clinical use for nearly 20 years and a large number is presently marketed, including drugs with a wide range of different pharmacokinetic and microbiologic properties. While some of these agents have certain specific uses in which they excel, the cephalosporins have not replaced older antibiotics but do provide the physician with a broader range of choices for the treatment of many infections, allowing greater individualization of therapy.
Asunto(s)
Cefalosporinas/uso terapéutico , Administración Oral , Bacterias/efectos de los fármacos , Infecciones Bacterianas/tratamiento farmacológico , Cefamandol/administración & dosificación , Cefamandol/metabolismo , Cefamandol/uso terapéutico , Cefazolina/administración & dosificación , Cefazolina/metabolismo , Cefazolina/uso terapéutico , Cefsulodina/administración & dosificación , Cefsulodina/metabolismo , Cefsulodina/uso terapéutico , Cefacetrilo/administración & dosificación , Cefacetrilo/metabolismo , Cefacetrilo/uso terapéutico , Cefalexina/administración & dosificación , Cefalexina/metabolismo , Cefalexina/uso terapéutico , Cefaloridina/administración & dosificación , Cefaloridina/metabolismo , Cefaloridina/uso terapéutico , Cefalosporinas/administración & dosificación , Cefalosporinas/efectos adversos , Cefalotina/administración & dosificación , Cefalotina/metabolismo , Cefalotina/uso terapéutico , Cefamicinas/administración & dosificación , Cefamicinas/metabolismo , Cefamicinas/uso terapéutico , Cefradina/administración & dosificación , Cefradina/metabolismo , Cefradina/uso terapéutico , Niño , Preescolar , Humanos , Lactante , Recién Nacido , Inyecciones IntramuscularesRESUMEN
The research of possible effects of cephacetrile (Celospor) on the reproductive function was carried out on two animal species, rats and rabbits. The animals were divided into experimental groups, each treated subcutaneously with different amounts of cephacetrile (50, 100 and 500 mg/kg/die), control group receiving physiological solution. Effects of the preparation on fertility and post-natal growth in rats were analyzed, and trials were performed to test perinatal toxicity and teratogenesis in rabbits. From the observation of the experimental data collected it can be assumed that cephacetrile, administered subcutaneously in the given doses--1, 2 and 10 times, respectively, higher than the maximum therapeutic dose advisable--does not alter fertility, gestation and post-natal development of term foetuses of rats and fertility and gestation of rabbits.
Asunto(s)
Cefacetrilo/farmacología , Cefalosporinas/farmacología , Reproducción/efectos de los fármacos , Animales , Cefacetrilo/administración & dosificación , Cefacetrilo/toxicidad , Desarrollo Embrionario y Fetal/efectos de los fármacos , Femenino , Fertilidad/efectos de los fármacos , Inyecciones Subcutáneas , Masculino , Embarazo/efectos de los fármacos , Conejos , Ratas , Ratas EndogámicasRESUMEN
The persistence of chloramphenicol, cephacetrile, and clindamycin in the udders of dry cows was studied after drying-off therapy with salts of these antibiotics suspended in conventional oil bases. Antibiotic activity was not found in dry udder secretions collected 3-5 days after treatment. After equivalent doses of encapsulated formulations of chloramphenicol were suspended in the same oil bases and infused at drying-off, most of the drug remained bound within the microcapsules; chloramphenicol concentrations higher than 10 micrograms/ml secretion were maintained for 3-4 weeks, but upon release from the microcapsule, the free drug was very quickly absorbed from the udder. Microcapsulated formulations of cephacetrile and clindamycin were infused at drying-off, suspended in the same type of oil base and at similar doses to the non-capsulated preparations. The concentrations of free drug in the secretions remained constant over a period of 2-3 weeks, although total drug (bound and free) concentrations in the udder, which were much higher than free drug levels, were progressively and markedly reduced. It appeared that after infusion of the microcapsulated preparations of cephacetrile and clindamycin, rates of drug release from the depot were equal to the rates of absorption of free drug from the udder.
Asunto(s)
Cefacetrilo/administración & dosificación , Cefalosporinas/administración & dosificación , Cloranfenicol/administración & dosificación , Clindamicina/administración & dosificación , Mastitis Bovina/tratamiento farmacológico , Animales , Bovinos , Preparaciones de Acción Retardada , Femenino , Lactancia , EmbarazoAsunto(s)
Cefacetrilo/uso terapéutico , Cefalosporinas/uso terapéutico , Infecciones del Sistema Respiratorio/tratamiento farmacológico , Adulto , Anciano , Cefacetrilo/administración & dosificación , Cefacetrilo/efectos adversos , Evaluación de Medicamentos , Quimioterapia Combinada , Femenino , Humanos , Masculino , Persona de Mediana Edad , Infecciones del Sistema Respiratorio/fisiopatologíaRESUMEN
In open surgery, ampicillin (Solcillin) or cephacetrile (Celtol), 2 g for patients weighing 20 kg or more, and 1 g for those below 20 kg, was administered, and the antibiotic concentrations in blood and urine were estimated during extracorporeal circulation, from the time of operation to the admission in an intensive care unit (Group A). In other group, a total circulation volume of 0.3 mg/ml of the antibiotic was administered, based on body weight of patients and priming volumes (Group B). In Group A, blood concentration of antibiotics was so variable that it was difficult to decide additional dosage. In Group B, comparatively definite concentrations were estimated in each case. In extracorporeal circulation for a long time, it is preferable to maintain the blood concentration of antibiotic at 50 micrograms/ml, by additional antibiotic administration 90 approximately 120 minutes after the beginning of the extracorporeal circulation. In patients with preoperative subacute bacterial endocarditis, the blood concentration should be kept over 100 micrograms/ml during extracorporeal circulation.
Asunto(s)
Ampicilina/sangre , Cefacetrilo/sangre , Cefalosporinas/sangre , Circulación Extracorporea , Adolescente , Adulto , Ampicilina/administración & dosificación , Ampicilina/orina , Cefacetrilo/administración & dosificación , Cefacetrilo/orina , Niño , Preescolar , Femenino , Cardiopatías/sangre , Humanos , Masculino , Persona de Mediana Edad , Factores de TiempoAsunto(s)
Cefacetrilo/administración & dosificación , Cefalosporinas/administración & dosificación , Cloxacilina/análogos & derivados , Floxacilina/administración & dosificación , Infecciones del Sistema Respiratorio/tratamiento farmacológico , Niño , Preescolar , Combinación de Medicamentos , Femenino , Humanos , Lactante , MasculinoAsunto(s)
Amicacina/administración & dosificación , Infecciones Bacterianas/tratamiento farmacológico , Kanamicina/análogos & derivados , Leucemia Mieloide Aguda/complicaciones , Adulto , Anciano , Cefacetrilo/administración & dosificación , Esquema de Medicación , Quimioterapia Combinada , Femenino , Humanos , Infusiones Parenterales , Masculino , Persona de Mediana Edad , Neumonía/tratamiento farmacológico , Sulbenicilina/administración & dosificaciónAsunto(s)
Cefacetrilo/metabolismo , Cefalosporinas/metabolismo , Procedimientos Quirúrgicos Cardíacos , Cefacetrilo/administración & dosificación , Cefacetrilo/análisis , Colecistectomía , Gastrectomía , Humanos , Inyecciones Intravenosas , Cinética , Neumonectomía , Complicaciones Posoperatorias/prevención & control , Infección de la Herida Quirúrgica/prevención & controlAsunto(s)
Antibacterianos/administración & dosificación , Cefacetrilo/administración & dosificación , Esquema de Medicación , Combinación de Medicamentos , Incompatibilidad de Medicamentos , Estabilidad de Medicamentos , Gentamicinas/administración & dosificación , Hospitales , Humanos , Infusiones Parenterales , Meticilina/administración & dosificaciónRESUMEN
The potential renal tolerance of cefuroxime was investigated in 80 female albino Wistar rats and compared with that of cephacetrile. The drugs were administered i.m. in different dosages (1000, 2000, 3000 and 5000 mg/kg/day; dosage interval: 12 h) over a period of five days. The excretion of tubular cells and urinary malic dehydrogenase was assessed before, during and after administration of the antibiotics. In addition, the concentration of serum urea was analysed and the renal histology was examined. The following toxic threshold doses were estimated: cefuroxime 5000 mg/kg/day, cephacetrile 3000 mg/kg/day. In comparison with other cephalosporines cefuroxime belongs to those antibiotics with which a high degree of renal tolerance is demonstrated.
Asunto(s)
Cefalosporinas/toxicidad , Riñón/efectos de los fármacos , Animales , Cefacetrilo/administración & dosificación , Cefacetrilo/toxicidad , Cefalosporinas/administración & dosificación , Femenino , Furanos/administración & dosificación , Furanos/toxicidad , Riñón/citología , Malato Deshidrogenasa/orina , Ratas , Urea/sangreAsunto(s)
Cefazolina/metabolismo , Cefacetrilo/metabolismo , Cefalosporinas/metabolismo , Cefalotina/metabolismo , Adulto , Cefazolina/administración & dosificación , Cefazolina/sangre , Cefacetrilo/administración & dosificación , Cefacetrilo/sangre , Cefalotina/administración & dosificación , Cefalotina/sangre , Evaluación de Medicamentos , Semivida , Humanos , Inyecciones Intravenosas , MasculinoRESUMEN
1. When gentamicin (GM) and sulbenicillin (SBPC) or cephacetrile (CEC), in combination with pre- or post-treatment, were injected intravenously to the rat, their pharmacokinetics were investigated. 2. The antibiotics in the samples were separated by paper electrophoretic technique and their concentrations were determined by cup thin layer plate method using Bacillus subtilis as the test organism. 3. The biological half-life of SBPC in the serum was shortened in pretreatment with GM and prolonged in posttreatment with GM, while that of GM did not vary in pre- or post-treatment with SBPC. 4. The half-life of CEC was prolonged in treatment with GM, while that of GM did not vary. 5. These phenomena may be considered to be produced as the results of a concentration ratio of SBPC and GM or of CEC and GM, and protein binding of these antibiotics, as far as plasma initial levels, tissue distribution, urinary excretion and protein binding of these antibiotics are concerned.
Asunto(s)
Cefacetrilo/metabolismo , Cefalosporinas/metabolismo , Gentamicinas/metabolismo , Penicilina G/análogos & derivados , Sulbenicilina/metabolismo , Animales , Cefacetrilo/administración & dosificación , Cefacetrilo/farmacología , Quimioterapia Combinada , Gentamicinas/administración & dosificación , Gentamicinas/farmacología , Semivida , Técnicas In Vitro , Cinética , Resistencia a las Penicilinas , Unión Proteica , Ratas , Albúmina Sérica Bovina/metabolismo , Sulbenicilina/administración & dosificación , Sulbenicilina/farmacologíaRESUMEN
In order to elucidate the usefulness of cephacetrile (CEC), comparative trials with cefazolin (CEZ) were carried out in the patients with complicated infections of the urinary tract, and the following results were obtained: 1. There were no statistically significant differences or tendencies observed between the groups given CEC and CEZ in either of the global effects, bacteriological effects, rate of superinfection, relapse, relapse with bacterial alternation, drug usefulness, rate of improvements in symptoms and findings in all the cases. 2. According to a result of stratified analyses, there were statistically significant differences observed, showing more inferior results of CEC than CEZ in either stratum of "below 50" in the age, "acute" in the disease phase, "infections of the upper urinary tract" in the disease pattern, and "E. coli including mixed infections with gram-positive organisms" in the pathogenic strains. However, it should be taken into consideration that certain background factors influence greatly in the effects and there were some problems on deviated backgrounds in these strata. On the other hand, CEC displayed better bacteriological effects than those of CEZ in higher stratum of "chronic" in the disease phase and "Klebsiella, Proteus, Citrobacter, Enterobacter including mixed infections" in the pathogenic strains, and statistically significant differences were not observed. 3. In consequence of bacteriological studies, CEC showed stronger resistance than CEZ against beta-lactamase produced in all the strains of gram-negative bacilli. Particularly there were significant differences or tendencies observed in those of Proteus, Cirtobacter, and Enterobacter, and at the same time there were great differences in the activity of beta-lactamase between CEC and CEZ as the substrate. 4. In correlation of the MIC and effects, CEC showed weaker actions than CEZ against susceptible organisms, but slightly stronger actions against moderately or highly resistant strains. A study of the relationship between the MIC of pathogenic strains, beta-lactamase, and bacteriological effects, showed possibilities that even the high activity of beta-lactamase results in remarkable effects in susceptible strains and the drugs with stronger resistance against beta-lactamase given better results in moderately or highly resistant organisms. 5. The incidence rate of adverse reactions was 2 out of 51 cases in the CEC group (3.9%) and 3 out of 50 cases in the CEZ group (6.0%), showing no significant difference, and those symptoms were similar. In conclusion, when the usefulness of CEC in complicated infections of the urinary tract is compared with that of CEZ, the former is said to be equal to the latter without significant difference as a whole...
Asunto(s)
Cefazolina/uso terapéutico , Cefacetrilo/uso terapéutico , Cefalosporinas/uso terapéutico , Infecciones Urinarias/tratamiento farmacológico , Adulto , Anciano , Bacterias/efectos de los fármacos , Cefazolina/administración & dosificación , Cefazolina/efectos adversos , Cefacetrilo/administración & dosificación , Cefacetrilo/efectos adversos , Ensayos Clínicos como Asunto , Farmacorresistencia Microbiana , Femenino , Humanos , Masculino , Persona de Mediana Edad , Infecciones Urinarias/microbiologíaRESUMEN
The therapeutic efficacy of cephacetrile (CEC) in bacterial pneumonia was evaluated in contrast with that of cefazolin (CEZ) by a double blind method. Both drugs were administered via intravenous route at a dose of 1 g twice daily for 14 days. 1) Of 81 patients, each 2 from both groups were eliminated from the study because of unknown results. In CEC group, 36 out of 38 obtained a slightly effective or better results (94.7% of effectiveness). In CEZ group, 31 out of 39 showed a similar result and there was no significant difference between the two groups. 2) In more detail, CEC achieved significantly better results in AaDo2 and cardiac insufficiency than CEZ, and this trend was also seen in dyspnea. 3) Regarding background factors, pretreatment severity was slightly in favor of CEC. However, so long as supplementary analysis is concerned, we could not find any relation between the pretreatment severity of symptom and drug efficacy or improvement of symptom. 4) Since there was a slight bias in the background factors, it is difficult to conclude that CEC is better than CEZ in terms of effectiveness. However, we consider CEC is superior to CEZ if compared in details. 5) Both drugs had the same incidence of side effect (6.25%, 3/48 in both groups). When clinical efficacy of CEC in bacterial pneumonia is evaluated together with the incidence of side effect, we may consider that CEC is an effective antibiotic agent equal to or better than CEZ.
Asunto(s)
Infecciones Bacterianas/tratamiento farmacológico , Cefazolina/uso terapéutico , Cefacetrilo/uso terapéutico , Cefalosporinas/uso terapéutico , Neumonía/tratamiento farmacológico , Factores de Edad , Anciano , Cefazolina/administración & dosificación , Cefazolina/efectos adversos , Cefacetrilo/administración & dosificación , Cefacetrilo/efectos adversos , Ensayos Clínicos como Asunto , Evaluación de Medicamentos , Femenino , Humanos , Masculino , Persona de Mediana Edad , Neumonía Estafilocócica/tratamiento farmacológicoRESUMEN
This pharmacokinetic investigation was based on the determination of serum and urinary levles of cephacetrile in 50 subjects given single intramuscular or intravenous doses of 0.5 or 1 gm of the antibiotic; 30 normal subjects, 10 patients with renal insufficiency, and 10 patients with chronic nephritis undergoing maintenance haemodialysis were included in this study. In normal subjects, mean serum half-life was 1.09 hours (Ke = 0.6337) after intramuscular injection of 0.5 gm cephacetrile, 1.31 hours (Ke = 0.5276) after intramuscular injection of 1 gm, and 0.89 hours (Ke = 0.7806) after intravenous injection of 1 gm. Absorption half-life was 0.45 hours after intramuscular injection of 1 gm cephacetrile. The urinary elimination of cephacetrile over the first 6 hours after injection was on the average 72.7% of the administered dose. After intravenous injection of 1 gm of the antibiotic, the plasma clearance of cephacetrile was 407 ml/min., and its renal clearance 313 ml/min. A linear correlation was found between the values of overall elimination rate constant (Ke) and creatinine clearance in the subjects under investigation (Ke = 0.0080 + 0.0061 ClCr). The established pharmacokinetic characteristics were used to calculate the maintenance and loading doses as well as the intervals between injections adjusted to creatinine clearance. These data constitute true dosage schemes adapted to the particular case of each patient according to his kidney function.
Asunto(s)
Cefacetrilo/administración & dosificación , Cefalosporinas/administración & dosificación , Cefacetrilo/sangre , Cefacetrilo/orina , Humanos , Inyecciones Intramusculares , Inyecciones Intravenosas , Enfermedades Renales/metabolismo , CinéticaRESUMEN
1. The metabolic fate of 14C-cephacetrile was studied in rats and rabbits. The plasma level of intravenously injected cephacetrile decreased with half-lives of 17 and 22 minutes in rats and rabbits respectively, this decline being associated with a rapid appearance of the active metabolite, desacetylcephacetrile. Intramuscularly injected cephacetrile was rapidly absorbed by rats with a maximum plasma level at 20 minutes and a half-life of 16 minutes. Cephacetrile and desacetylcephacetrile did not enter erythrocytes. Cephacetrile was weakly bound to the plasma protein in the rat, rabbit and man. 2. Both in rats and rabbits, almost all of the injected radioactivity was excreted in the urine within 72 hours as the intact antibiotic and desacetylcephacetrile, only small amounts appearing in feces via bile. Neither the gamma-lactone of desacetyl-7-cyanacetamidocephalosporanic acid nor the violet-reddish pigment (CGP-695) produced from cephacetrile were detectable in the plasma or urine of the animals. 3. In rats given the labeled antibiotic intravenously, the radioactivity was widely distributed with concentrations being high in the kidney, plasma and liver, and lowest in the brain. The radioactivity crossed the rat placenta and appeared in the fetus. Radioactivity in these tissues disappeared as the plasma level declined. 4. During daily intramuscular injection of 14C-cephacetrile to rat, no significant changes were observed in the peak level of the plasma radioactivity or in the half-lives. In addition, dosing of the labeled antibiotic for 7 days caused no increase in tissue levels of radioactivity.
Asunto(s)
Cefacetrilo/metabolismo , Cefalosporinas/metabolismo , Animales , Bacterias/efectos de los fármacos , Líquidos Corporales/metabolismo , Cefacetrilo/administración & dosificación , Cefacetrilo/farmacología , Cromatografía en Capa Delgada , Eritrocitos/metabolismo , Heces/análisis , Infusiones Parenterales , Cinética , Masculino , Unión Proteica , Conejos , RatasRESUMEN
It is necessary to start with antibiotic treatment in infections of the lower respiratory system, especially pneumonias. The finding of the infectious agent is difficult and without security. With simple investigations, as sedimentation rate, white blood cell count and cell differentiation there is a possibility of 80% to get a diagnosis of bacterial infection. In 25 patients aged 1 1/2 to 9 years with x-ray diagnosis of pneumonia the results of treatment with cephacetril (100 mg/kg/d) are given. Clinical symptoms disappeared after 5 days, the average time of illness was 12 days. One patient got a severe pleural effusion.
Asunto(s)
Cefacetrilo/uso terapéutico , Cefalosporinas/uso terapéutico , Neumonía/tratamiento farmacológico , Cefacetrilo/administración & dosificación , Niño , Preescolar , Evaluación de Medicamentos , Hematopoyesis/efectos de los fármacos , Hemólisis/efectos de los fármacos , Humanos , Lactante , Inyecciones Intramusculares , Riñón/efectos de los fármacos , Hígado/efectos de los fármacosRESUMEN
A patient on chronic intermittent hemodialysis at home showed signs of acute encephalopathy after an 8-day's treatment with a total dose of 78 g cephacetril (Celospor). Features included papilledema, loss of visual fields, severe generalized EEG changes and bilateral occipital abnormalities on a brain scintigram. Psychopathological findings consisted of a severe psychosis. The visual fields defects were the last sign of the encephalopathy to disappear.