摘要:

Investigations on deoxythymidine Kinase show that: (a) 5-ethyl-2′-deoxyuridine-β (EDU-β) binds to about 100-fold weaker (Km 2.7 × 10-4) than deoxythymidine (Km 2.5 × 10-6) and the rate of its phosphoration (0.7 nmol/mg protein/15 min) is about the half of the deoxythymidine (1.52 nmol/mg protein/15 min); (b) 5-ethyl-2′-deoxyuridine-α (EDU-α), 5-propyl-2′-deoxyuridine (α and β) as well as α and β-5-isopropyl-2′- deoxyuridines do not serve as substrate

ISSN:0009-3157    

DOI:10.1159/000221271

出版商:S. Karger AG    

年代:1973

数据来源: Karger

摘要:

Trimethoprim is absorbed well in man. Plasma peak levels between 0.9 and 1.9 μg/ml are reached within 2–4 h after ingestion of 160 mg TMP alone or in combination with 800 mg SMZ. Plasma disappearance of TMP is characterized by first order processes. Elimination half-lives range between 6 and 17 h. Assuming total absorption the apparent volume of distribution for TMP is approximately 1001. Urine recovery of TMP after single oral administration is 75% of the administered dose. Pharmacokinetics of TMP after single oral application are not altered by simultaneous administration of SMZ. Steady-state plasma levels of almost always 1.2–1.7 μg/ ml are achieved after 2–3 days and maintained on a chronic oral dosing schedule of 160 mg TMP every 12 h. The recovery of intact TMP in the urine during chronic administration is approximately 50% for all subjects studied. Simultaneous application of SMZ in the repetitive dosing study does not change the pharmacokinetics of TMP. Peak plasma levels after single oral administration correspond to plateau concentrations during chronic oral application

ISSN:0009-3157    

DOI:10.1159/000221272

出版商:S. Karger AG    

年代:1973

数据来源: Karger

摘要:

The effect of the combination preparation TMP/SMZ on the alimentary flora of human subjects was investigated at different doses. Following the short-term administration of the preparation, E. coli was particularly markedly reduced at doses as low as one tablet a day. The other alimentary organisms, however, showed no pronounced changes. Enterobacteriaceae, particularly E. coli, were markedly reduced in the course of long-term treatment, with four tablets daily for 3 months. No resistant populations were found. The response of enterococci, anaerobic lactobacteria and Gram-negative bacteria of the Bacteroidaceae family showed no uniformity. No overgrowth of the alimentary flora by Pseudomonas, staphylococci or Candida was observed.

ISSN:0009-3157    

DOI:10.1159/000221273

出版商:S. Karger AG    

年代:1973

数据来源: Karger

摘要:

The bactericidal activity of aminosidine has been studied in vitro using an experimental device able to reproduce in vitro the serum concentration-time curve observed in man after administration of 1 or 0.5 g of drug by intramuscular route. The data reported show that aminosidine is strongly bactericidal on some strains of Staphylococcus aureus, Escherichia coli and Salmonella typhi in these experimental conditions and that the inhibitory effect is maintained for at least 24 h when the dose of 1 g is considered. The test method proposed may be useful for assessing in dynamic conditions the antibacterial activity of drugs, particularly in body fluids.

ISSN:0009-3157    

DOI:10.1159/000221274

出版商:S. Karger AG    

年代:1973

数据来源: Karger

摘要:

During the first 4 days after the intravenous administration of a lethal dose (100 μg) of mustine hydrochloride to mice, there is a marked decrease in the weights of the lymph nodes, thymus and spleen and in the cellularity of the femoral bone marrow. In the subsequent 4 days, the cellularity of the bone marrow increases to values within the normal range while the weights of the lymph nodes, thymus and spleen remain exceedingly small. In this bone marrow regenerating after the injection of mustine hydrochloride, 94% of the recognisable haematopoietic cells are granulocytes at various stages of maturation

ISSN:0009-3157    

DOI:10.1159/000221275

出版商:S. Karger AG    

年代:1973

数据来源: Karger

摘要:

Doxycycline was used in a single dose for the treatment of 37 cases of classic epidemic typhus caused by Rickettsia prowazekii. The results were excellent and, as expected, no side effects were reported.

ISSN:0009-3157    

DOI:10.1159/000221276

出版商:S. Karger AG    

年代:1973

数据来源: Karger

ISSN:0009-3157    

DOI:10.1159/000221277

出版商:S. Karger AG    

年代:1973

数据来源: Karger