ABSTRACT
Ticarcillin tissue concentrations were determined in 77 patients following an infusion of 5 g over 30 min. The tissues studied in gynecology were endometrium, tube, ovary and myometrium. The relative tissue levels ranged from 17% to 30% of the corresponding serum concentrations when ticarcillin was administered once, and from 22% to 32% when the drug was infused repeatedly. In no case did these tissue levels exceed the serum concentrations. The mean relative tissue levels in early pregnancy (decidua, placenta, embryo) were 10% of the corresponding serum concentrations. Levels in late pregnancy were determined in the placenta, amniotic fluid and in serum from the umbilical cord artery and vein immediately after delivery. Maximal placenta concentrations of 30 mg/kg were determined; these declined exponentionally with half-lives of 2.8 and 1.3 h, respectively, following single and repeated dosings. Amniotic fluid levels increased from 10 mg/l immediately after the first infusion to 60 mg/l after the seventh infusion. Individual umbilical cord levels in the artery and vein were significantly different, indicating that the fetus has properties of a deep compartment. The total amount of ticarcillin excreted daily in the mother's milk was strictly correlated to its volume and ranged from 2-2.5 mg/l.
Subject(s)
Genitalia, Female/analysis , Penicillins/analysis , Ticarcillin/analysis , Adult , Embryo, Mammalian/analysis , Female , Fetal Blood/analysis , Humans , Hysterectomy , Infant, Newborn , Maternal-Fetal Exchange , Milk, Human/analysis , Postoperative Complications/prevention & control , Pregnancy , Ticarcillin/pharmacology , Tissue DistributionABSTRACT
The pharmacokinetics of alpha-amino-p-hydroxybenzylpenicillin (amoxicillin) after intravenous, intramuscular and oral application were studied and the corresponding constants are reported. Following i.v. injection of 250, 500 and 1000 mg and infusion of 2 and 5 g the data are examined by means of a two- and three-compartment model, respectively. Calculations by adopting the two-compartment model reveal no significant dose dependency of the distribution constants and the serum concentration curves decline bioexponentially. A better fit of the regression curve to the experimentally determined serum concentrations is obtained by using the three-compartment model, indicating a slow and late disposition phase whose constants are significantly dose dependent. The share of this third phase in the total distribution of amoxicillin is 33% to 43%. After an i.m. injection of 250, 500 and 1000 mg amoxicillin is absorbed without any delay to 79% to 88%; the mean absorption constant is approximately 2 h-1. No significant dose dependency could be determined. Analogous results were obtained following oral administration of 250 and 500 mg. Absorption is delayed to 16 to 18 min; the mean absorption constant is 1.4 h-1 and 72% to 86% of the administered drug is absorbed without being significantly dose dependent. On the basis of the examined parameters the bioavailability of amoxicillin following extravascular administration can be regarded as reliable and safe.
Subject(s)
Amoxicillin/metabolism , Administration, Oral , Adult , Amoxicillin/administration & dosage , Humans , Injections, Intramuscular , Injections, Intravenous , Kinetics , Male , Models, BiologicalABSTRACT
Applicability, effect and toleration of dibekacin (Orbicin) were tested in pharmacokinetic, clinical and bacteriological studies treating 29 patients with severe surgical illnesses and 10 healthy volunteers as control group. The pharmacokinetic test results and the efficacy with severe infections showed dibekacin to be equivalent to the new aminoglycoside antibiotics gentamycin, sisomicin and tobramycin. Resistance was sporadic and severe side effects did not occur. Dibekacin proved itself to be a new alternative when aminoglycoside antibiotics are indicated
Subject(s)
Dibekacin/therapeutic use , Kanamycin/analogs & derivatives , Surgical Wound Infection/drug therapy , Bacterial Infections/drug therapy , Female , Humans , Male , Microbial Sensitivity Tests , Middle AgedABSTRACT
A clinical trial on efficacy and tolerance of Cefazedone, a new semisynthetic Cephalosporine-derivate, was carried out in a gynaecological clinic on 75 patients. In 38 of these cases, besides the gynaecological affection, urinary tract infections were determined microbiologically (E. coli, P. mirabilis, klebsiella or enterococci). Inflammation of the lower abdominal area was established in the remaining 37 patients (adnexitis, pelvic peritonitis, endometritis, salpingitis). The average duration of treatment was 10 to 11 days. Cefazedone was injected intravenously twice a day, the daily dose was 2 to 4 g. The clinical assessment of the treatment was very good in 28 cases, good in 43 cases, moderate in 3 patients and poor in 1 case. All initially identified pathogens were eliminated after treatment. A slight transitory diarrhea was observed in 5 cases. There were no further side-effects. The values of gamma-GT, serum-creatinin, hemoglobin and erythrozytes were controlled before and after medication and showed no detremental effect of the drug. The local tolerance of Cefazedone was good in more than 90% of the cases treated.
Subject(s)
Cephalosporins/therapeutic use , Genital Diseases, Female/drug therapy , Adult , Clinical Trials as Topic , Drug Evaluation , Drug Tolerance , Endometritis/drug therapy , Female , Humans , Middle Aged , Pelvic Inflammatory Disease/drug therapy , Peritonitis/drug therapy , Salpingitis/drug therapy , Urinary Tract Infections/drug therapy , Urine/microbiologyABSTRACT
Applying a single i.m. dose of 80 mg (41 patients) and 120 mg (23 patients) of gentamicin, respectively, investigations in females have shown that, although the bulk of the antibiotic is excreted with the urine within the first 24 hours after injection, slow excretion is maintained at a very low level. According to the dose administered gentamicin remains detectable in the urine for many days. Thus, after injection of 120 mg in two patients gentamicin was detectable in the urine for a period of up to 20 days. Peak serum levels one hour after i.m. injection of 120 mg did not exceed 8.2 mug/ml, the mean concentration was 5.76 mug/ml. Serum half life was 2 hours. Studies of distribution in animal and human tissues have shown that gentamicin is accumulated almost exclusively in the kidneys, mainly in the cortex.
