0000000000206489
AUTHOR
Gilfrich Hj
showing 12 related works from this author
Beta-adrenergic blocking activity and haemodynamic effects in man of K� 1313, a new beta-adrenergic antagonist
1971
The beta-adrenergic blocking activity and haemodynamic effects of o-[2-hydroxy-3-(isopropylamino)-propoxy]-benzonitril (Ko 1313) have been studied in 22 patients. Antagonism of isoproterenol-induced tachycardia was used as a measure of the beta-adrenergic blocking activity. Ko 1313 1.0 mg had its maximum beta-adrenoceptor blocking effect 5–30 min after intravenous injection. Ko 1313 10.0 mg produced maximum betablockade 1–4 h after oral administration. 1.0 mg Ko 1313 injected intravenously had approximately the same beta-adrenergic blocking effect as 1.0 mg propranolol also given intravenously. After intravenous administration Ko 1313 was 3–4 times as potent as the same dose given orally. A…
Influence of digoxin on sinus node function after pharmacologic autonomic blockade.
1983
The effect of iv digoxin on normal sinus node function was studied after pharmacologic autonomic blockade (AB) in ten patients. Sinus cycle length (SCL), sinus node recovery time (SNRT) and sinoatrial conduction time (SACT) were determined before and after AB with propranolol (0.2 mg/kg body weight) and atropine sulfate (0.04 mg/kg body weight) iv, and 15 min, 30 min, and 45 min after 1 mg iv digoxin. AB resulted in a significant decrease (P less than 0.01) in SCL (916 +/- 158 to 716 +/- 120 ms), in SNRT (1,229 +/- 221 to 871 +/- 190 ms), and in SACT (79 +/- 34 to 44 +/- 10 ms). Fifteen minutes after iv digoxin there was no significant change observed in SCL (716 +/- 120 to 708 +/- 92 ms), …
Pharmacokinetics of triamterene after i.v. administration to man: determination of bioavailability.
1983
With a new formulation, which made intravenous infusion of triamterene (TA) possible, plasma levels and urinary excretion rates of TA and its main metabolite (OH-TA-ester) were measured in a randomized, cross-over trial in 6 healthy volunteers given triamterene 10 mg i.v. and 50 mg p.o. TA and OH-TA-ester were determined by densitometric measurement of native fluorescence after thin layer chromatography. Distribution volumes of the central compartment of TA and OH-TA-ester were 1.49 l/kg and 0.11 l/kg, respectively. Terminal half-lives were 255 min for TA and 188 min for OH-TA-ester after i.v. administration. For TA total plasma clearance was 4.5 l/min and renal plasma clearance 0.22 l/kg. …
Interruption of the enterohepatic circulation of phenprocoumon by cholestyramine
1977
The effect of cholestyramine (12 gm/day divided into 3 doses) on the pharmacokinetics and pharmacodynamics of a single intravenouse dose (30 mg) of phenprocoumon was studied in 6 normal subjects. Cholestyramine treatment led to an increase in the rate of elimination of phenprocoumon in all. Total clearance increased 1.5- to 2-fold. The total anticoagulant effect per dose was considerably reduced during treatment with cholestyramine. Binding studies in vitro showed that phenprocoumon is strongly bound to cholestyramine and that at a given cholestyramine concentration the percentage of phenprocoumon bound remained constant over a large concentration range of phenprocoumon. The results suggest…
Pharmacokinetic analysis of the interaction between dicoumarol and tolbutamide in man
1976
The effect of repeated administration of tolbutamide on the elimination and anticoagulant action of a single oral dose of dicoumarol 600 mg was studied in four healthy male subjects using a crossover design. In all subjects the plasma concentration of dicoumarol in the postabsorptive phase was lower during concomitant tolbutamide treatment. However, the subjects differed with respect to the elimination kinetics of dicoumarol and the effect of tolbutamide on some of the measured pharmacokinetic paramaters. In two subjects dicoumarol was eliminated by apparent first-order kinetics. Tolbutamide led to a pronounced increase in the elimination rate and a shift in the plasma concentration-respons…
Dose-response relationships and plasma concentrations of digitalis glycosides in man.
1978
An inter-individual, randomized, double-blind study of digitoxin (Dt) and β-acetyl digoxin (D) was performed in 120 healthy male volunteers. Groups of 10 persons each received orally D 0, 0.1, 0.2, 0.3, 0.4, 0.5 or 0.6 mg and Dt 0.04, 0.08, 0.12, or 0.16 mg daily for 7 days; Loading doses were given for the first three days. Plasma levels were measured with an86Rb-erythrocyte assay 24 h after the last dose. ECG, carotid artery pulse and phonocardiogram were recorded prior to (b) and 24 h after (a) the last dose. QTc, amplitude of T-waves in V2 to V6, electromechanical systole (QS2c) and left ventricular ejection time (LVETc) were measured. The differences between a and b (Δ-values) reflect …
Magnesium concentration in saliva — an indicator of digitalis toxicity
1981
In a prospective study salivary magnesium was measured by atomic absorption spectrophotometry in 168 patients on chronic digoxin therapy. Magnesium concentration in saliva was correlated with clinical data and plasma digoxin levels. A significant elevation in salivary magnesium concentration was caused by digoxin therapy (0.58 +/- 0.39 mmol/l, n = 93) in comparison to patients with no digitalis treatment (0.17 +/- 0.07 mmol/l, n = 35). Magnesium concentrations in saliva were significantly higher in toxic patients (1.1 +/- 0.68 mmol/l, n = 32) than in nontoxic patients. Possibly toxic patients showed a magnesium level of saliva of 0.63 +/- 0.39 mmol/l (n = 40). In 89% of the intoxicated pati…
The enantiomers of phenprocoumon: pharmacodynamic and pharmacokinetic studies.
1976
The pharmacodynamics and pharmacokinetics of the optical enantiomers of phenprocoumon were studied in 5 normal subjects and compared to the racemic mixture. Each subject received a single oral dose of 0.6 mg/kg of racemic, S(-), and R(+) phenprocoumon. S(-) phenprocoumon was 1.6 to 2.6 times as a potent as R(+) phenprocoumon when the area under the effect/time curve was used to quantify the total anticoagulant effect per dose. Comparing the plasma concentrations that elicited the same anticoagulant effect, S(-) phenprocoumon was 1.5 to 2.5 times as potent as R(+) phenprocoumon. The anticoagulant activity of the racemic mixture was between that of the enantiomers. There was no distinct diffe…
Massive digoxin intoxication in childhood.
1978
In a 10 year old boy 8 hours after taking about 16 mg beta-acetyl-digoxin a maximum serum digoxin level of 31.8 ng/ml was measured radioimmunologically. This is the highest digitalis level in childhood described to date. The serum potassium level rose to 7.4 mmol/l. Complete atrio-ventricular block, and salves of ventricular premature beats were the most serious rhythm disturbances. The absence of life threatening rhythm disturbances is attributed to the early use of diphenylhydantoin in small frequent doses.
Disposition of azapropazone in chronic renal and hepatic failure.
1981
The disposition of azapropazone 600 mg i.v. was investigated in 6 healthy subjects, 13 patients with cirrhosis and 8 patients with renal failure. In healthy subjects the elimination half-life was 12.2±2.1 h (mean ± SD), the volume of distribution 10.6±3.31 and the total clearance was 597±135 ml·h−1. Renal clearance accounted for about 62% of the total clearance. The free fraction of azapropazone in the plasma was 0.0045±0.0006. The patients with cirrhosis were divided into Group I with modest and Group II with severe impairment of liver function. In Group I the total clearance of azapropazone was not significantly different from that in healthy subjects. There was a 2.5-fold increase in its…
Digoxin and digitoxin elimination in man by charcoal hemoperfusion
1978
Since there is no widely used causal means of reducing the severity of massive digitalis intoxication the capability of hemoperfusion with coated activated charcoal to remove toxicologically relevant amounts of digoxin and digitoxin was evaluated in vitro and in man. At a blood flow rate of 100 ml/min the digoxin clearance by hemoperfusion in vitro was 51±8 ml/min in comparison to 24.3±11.3 ml/min by hemodialysis. The average hemoperfusion clearance of digitoxin was 31.7±13.4 ml/min, whereas almost no digitoxin was removed by hemodialysis. These clearance values point to the ability of hemoperfusion of eliminating digitalis glycosides from the blood. They do not clarify the essential questi…
Transthoracic electrical impedance during extracorporeal hemodialysis in acute respiratory failure ("Shocked Lung syndrome").
1980
The alteration (delta Z0) of transthoracic electrical impedance (TEI) during extracorporeal hemodialysis (EHD) was investigated in two Groups of patients with acute renal and acute respiratory failure, that differed with respect to the severity of respiratory insufficiency. Group I had moderate respiratory failure (FiO2 0.31 +/- 0.10, PaO2 84 +/- 14 mmHg), and Group II had severe respiratory failure (FiO2 0.75 +/- 0.17, PaO2 77 +/- 14 mmHg). There was a significant correlation between increase in TEI (delta Z0) and decrease in body weight (delta BW) in each individual patient, but the slope of regression lines was remarkably flattened in Group II. In Group I, delta TEI was 1.9 +/- 0.9 omega…