ABSTRACT
The clinical importance of the method of obtaining a urine sample (spontaneous vs. catheter and midstream specimens) was investigated in 507 in-patients. Whereas leucocyturia was demonstrated with the Cytur-Test on spontaneous urine from 105 patients, only 30 out of 89 of these patients showed leucocyturia in catheter or midstream specimens one to three days later. All 30 positive cases were found to have a disease state which causes leucocyturia. A direct comparison between spontaneous urine and midstream or catheter urine taken at the same time in 68 patients showed a leucocyturia in 20 cases in spontaneous urine which could not be confirmed in the midstream or catheter urine. This drastic difference shows the importance of the method of obtaining specimens in estimating leucocyturia.
Subject(s)
Leukocytes , Urine/cytology , Diagnostic Errors , Female , Humans , Male , Methods , Urinary CatheterizationABSTRACT
AR-L 57 CL is an imidazole derivative which has been shown in animal studies to have a pronounced positive inotropic effect. This effect and the pharmacokinetics of AR-L 57 CL have been investigated by non-invasive methods in 8 healthy volunteers. After a single intravenous dose of 200 mg, administered as part of Phase 1 of the clinical studies, AR-L 57 CL plasma concentrations were measured by fluorimetry at intervals for up to one hour. Its inotropic action on the heart was demonstrated by changes in the systolic time intervals: QS2 = duration of electro-mechanical systole; PEP = pre-ejection period; LVET = left ventricular ejection time. The decrease in plasma concentration could be expressed in terms of an open two-compartment pharmacokinetic model. The shorter elimination phase had a t1/2 of 4 min and the longer a t1/2 of 30 min. Immediately after injection, QS2 and PEP (corrected for heart rate) as well as PEP/LVET (independent of heart rate) decreased considerably. They had returned to normal by 22 min after injection. The plasma concentrations of AR-L 57 CL of 2 - 5 mug-equivalents/ml showed a highly significant correlation with the decrease in systolic time intervals. Both systolic and diastolic blood pressure rose briefly after injection. The AV conduction time fell initially and the heart-rate increased briefly. Thus AR-L 57 CL was shown to be a short acting drug with a high degree of positive inotropic action. It did not cause bradycardia or increase atrioventricular transmission time and appeared to be easily controllable.
Subject(s)
Heart/drug effects , Imidazoles/pharmacology , Myocardial Contraction/drug effects , Adult , Half-Life , Hemodynamics/drug effects , Humans , Imidazoles/metabolism , Injections, Intravenous , Male , Stimulation, ChemicalABSTRACT
The aim of this study was to establish data on the plasma levels of the glycoside derivative methyl-proscillaridin (MP) following repeated intravenous and oral doses. The study was carried out on healthy male volunteers. Each received 0.5 mg of MP daily at 8 a.m. for 7 days. 6 volunteers received the drug i.v., 6 p.o. as tablets and 5 p.o. as elixir. Plasma glycoside concentrations were measured utilizing a 86Rb-erythrocyte assay. The mean plasma concentrations on the 6th and 7th days of application were: 752.9 (Sx = 303.5) pg/ml for the i.v. route, 432.9 (Sx = 115.5) pg/ml for the tablets and 473.1 (Sx = 321.5) pg/ml for the elixir. The mean ratio between plasma concentrations with tablets and i.v. injection averaged 63%. It is concluded that the therapeutic activity of oral MP is about 60 to 70% that of the i.v. application.
Subject(s)
Bufanolides/blood , Proscillaridin/blood , Administration, Oral , Adult , Humans , Injections, Intravenous , Kinetics , Male , Proscillaridin/administration & dosage , Proscillaridin/analogs & derivativesABSTRACT
The aim of this study was to determine the half-life of beta-acetyl digoxin in plasma after cessation of its continous oral application. 18 healthy male volunteers received 0.4 mg p.o. of beta-acetyl digoxin daily for a period of 14 days. Plasma glycoside concentrations were measured up to 108 hours after the last application utilizing a 86Rb-erythrocyte assay. Mean plasma digoxin concentration 12 hours after the alst dose was -x=1.05 ng/ml, sx=0.301. Mean half-life in plasma was 55.8 hours (sx=21.7). This corresponds to a mean daily elimination rate of abour 25.8%. These results are in good agreement with the 20% loss of effect on the heart as reported in the literature.
