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1

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Atrial natriuretic peptides: Reproducibility of renal effects and response of liver blood flow (1986)

Biollaz, J. ; Waeber, B. ; Nussberger, J. ; [et al.]

Springer

European journal of clinical pharmacology 31 (1986), S. 1-8

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ISSN: 1432-1041

Keywords: atrial natriuretic peptides ; renal effects ; hepatic blood flow ; normotensive volunteers ; response consistency

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary To assess the variability of the response to exogenous atrial natriuretic peptide (ANP), it was infused at the rate of 1 µg/min for 2 h in 6 salt-loaded normal volunteers under controlled conditions on 2 occasions at an interval of 1 week. The effect on solute excretion and the haemodynamic and endocrine actions were highly reproducible. The constant ANP infusion caused a delayed and prolonged excretion of sodium, chloride and calcium, no change in potassium or phosphate excretion or in glomerular filtration rate but a marked decrease in renal plasma flow. Blood pressure, heart rate and the plasma levels of angiotensin II, aldosterone, arginine vasopressin and plasma renin activity were unaltered. The effect of a 2-h infusion of ANP 0.5 µg/min or its vehicle on apparent hepatic blood flow (HBF) was also studied in 14 normal volunteers by measuring the indocyanine green clearance. A 21% decrease in HBF was observed in subjects who received the ANP infusion (p〈0.01 vs vehicle). Thus, ANP infused at a dose that did not lower blood pressure decreased both renal and liver blood flow in normotensive volunteers. The renal and endocrine responses to ANP were reproducible over a 1-week interval.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00870977

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2

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Tolerability and pharmacokinetics of L-648,051. A leukotriene D4-receptor antagonist, in healthy volunteers (1988)

Biollaz, J. ; Stahl, E. ; Hsieh, J. Y. ; [et al.]

Springer

European journal of clinical pharmacology 33 (1988), S. 603-607

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ISSN: 1432-1041

Keywords: Leukotiene D4 ; L-648,051 ; LTD4-antagonist ; SRS-A ; Pharmacokinetics ; tolerability

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary Two formulations of L-648,051 (L) were studied [intravenous (i.v.) and aerosol (A)] in two separate trials. Study I (i.v.) involved 4 normal male subjects in a single blind dose ranging study where good systemic tolerability and safety was shown. However, dose dependent local irritation at the injection site was observed at all dose levels (35, 52.5 and 70 mg/5 min infusion). L has a high systemic clearance rate (1.2 l/min), a small volume of distribution (4.4 l) and a short plasma half-life (2.4 min). Study II (A) involved 16 normal male volunteers who received incremental aerosolized doses of L from 0.1 to 1.6 mg in a double-blind, placebo controlled, dose ranging study. Complaints of mild local irritation or discomfort in the upper respiratory tract were the only significant findings. No dose relationship of these complaints could be shown. In conclusion, L is a safe and well tolerated drug when administered by aerosol. It causes dose related local, but not systemic, adverse experiences when administered i.v. In view of this tolerability and of its demonstrated activity against LTD4-challenge in animals, clinical efficacy studies with the aerosol formulation are warranted.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00542495

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3

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Lactitol: Gastrointestinal absorption and effect on blood lactate in healthy volunteers and patients with cirrhosis (1988)

Metzger, J. ; Chollet, C. ; Wermeille, M. ; [et al.]

Springer

European journal of clinical pharmacology 35 (1988), S. 97-99

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ISSN: 1432-1041

Keywords: lactitol ; gastrointestinal absorption ; blood lactate ; cirrhosis ; metabolic effects

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The gastrointestinal absorption of lactitol has been studied in 6 healthy volunteers and 8 patients with cirrhosis. Following administration of lactitol 0.5 g/kg, no lactitol was found in serum. The urinary excretion of lactitol over 24 h ranged from 0.1 to 1.4% of the administered dose (0.46% in cirrhotics and 0.35% in healthy volunteers). Blood D- and L-lactate and plasma glucose did not increase following lactitol. The data indicate that lactitol was poorly absorbed from the gastrointestinal tract in healthy volunteers and patients with cirrhosis, and that the disaccharide did not disturb glucose or lactate homeostasis.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00555516

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4

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The effect of a low dose of quinidine on the disposition of flecainide in healthy volunteers (1992)

Munafo, A. ; Buclin, T. ; Tuto, D. ; [et al.]

Springer

European journal of clinical pharmacology 43 (1992), S. 441-443

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ISSN: 1432-1041

Keywords: Flecainide ; quinidine ; pharmacokinetics ; metabolism inhibition ; drug interaction ; renal transport

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary We have studied the effects of quinidine on ECG intervals and on the pharmacokinetics of flecainide and its two metabolites in 6 healthy men in an open randomized crossover study. Flecainide acetate (150 mg) was given as a constant rate i. v. infusion over 30 min. Quinidine (50 mg orally), given the previous evening, did not change the volume of distribution of flecainide (7.9 vs 7.41·kg−1), but significantly increased its half-life (8.8 vs 10.7 h). This was attributable to a reduction in total clearance (10.6 vs 8.1 ml·min−1·kg−1), most of it being accounted for by a reduction in non-renal clearance (7.2 vs 5.2 ml·min−1·kg−1). The excretion of the metabolites of flecainide over 48 h was significantly reduced. These findings suggest that quinidine inhibits the first step of flecainide metabolism, although it may also reduce its renal clearance, but to a lesser extent (3.5 vs 2.9 ml·min−1·kg−1). The effects of flecainide on ECG intervals were not altered by quinidine. Thus, quinidine tends to shift extensive metabolizer status for flecainide towards poor metabolizer status and may also alter its renal excretion.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF02220625

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5

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Whole-blood pharmacokinetics and metabolic effects of the topical carbonic anhydrase inhibitor dorzolamide (1995)

Biollaz, J. ; Munafo, A. ; Buclin, T. ; [et al.]

Springer

European journal of clinical pharmacology 47 (1995), S. 453-460

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ISSN: 1432-1041

Keywords: Dorzolamide ; Glaucoma ; carbonic anhydrase ; pharmacokinetics ; renal effects

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Abstract Following a single-dose, open-label, pilot pharmacokinetic study in six subjects, the systemic pharmacokinetics and metabolic effects of dorzolamide after topical ocular administration were investigated in a double-blind, randomised, placebo-controlled study in 12 healthy volunteers. The subjects received a controlled diet on the 5 days before treatment initiation and throughout the study. For 14 days, a bilateral q.i.d. regimen of 3% dorzolamide, consisting of approximately 7.7 μg per day (21.3 μmol) dorzolamide hydrochloride, or placebo was given. Blood and urine electrolytes and acid-base profiles were measured 1 day prior to treatment and on days 1, 7 and 14 of treatment, and 24-h urine samples were collected daily. Topically applied dorzolamide was slowly taken up in erythrocytes and eliminated with a half life of approximately 120 days. Compared to the pre-study values, no significant treatment effect was observed in either the daily profiles or the 14-day cumulative sodium, potassium and citrate excretions. Two other volunteers given acetazolamide (125 mg q.i.d.) and assessed with the identical set of observations demonstrated marked metabolic changes. In spite of the prolonged and marked inhibition of carbonic anhydrase in red blood cells by dorzolamide, clinically significant metabolic and renal effects were not observed. The ocular tolerability profile was acceptable to all subjects.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00196861

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6

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Altered flecainide disposition in healthy volunteers taking quinine (1990)

Munafo, A. ; Reymond-Michel, G. ; Biollaz, J.

Springer

European journal of clinical pharmacology 38 (1990), S. 269-273

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ISSN: 1432-1041

Keywords: flecainide ; quinine ; pharmacokinetics ; metabolism inhibition ; drug interaction ; renal transport

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The pharmacokinetics of flecainide and its two sequential metabolites, both free and conjugated, its pharmacodynamics, and the influence of simultaneously administered quinine, have been studied in 10 healthy subjects. The study comprised two, 48-h open phases at an interval of 1 week. Flecainide acetate 150 mg was given as a 30-min i.v. infusion and quinine sulphate orally 500 mg×3 over 24 h. Quinine administration did not change the apparent volume of distribution or the renal clearance of flecainide, but it significantly reduced its systemic clearance (9.2 vs 7.6 ml · kg−1 · min−1), thus increasing the elimination half-life (9.6 vs 11.5 h). The amount of flecainide transformed to its first, meta-O-dealkylated metabolite (MODF) fell with no change in the renal excretion of the latter, either in its free or conjugated forms. This finding, in association with a fall in amount of the second, meta-O-dealkylated lactam metabolite (MODLF) recovered in its conjugated forms in the urine, suggests that quinine inhibits both the first and the second steps of the sequential metabolism of flecainide. When the subjects received quinine in addition to flecainide, the PR interval in the ECG was slightly more prolonged than with flecainide alone. Due to the study design, an effect of quinine per se and the consequence of increased serum flecainide levels could not be distinguished.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00315029

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7

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Hypertensive crisis treated with orally administered captopril (1983)

Biollaz, J. ; Waeber, B. ; Brunner, H. R.

Springer

European journal of clinical pharmacology 25 (1983), S. 145-149

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ISSN: 1432-1041

Keywords: captopril ; emergency treatment ; hypertensive crisis ; furosemide ; combined treatment

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Summary The value of the orally active converting enzyme inhibitor captopril in managing hypertensive crisis was tested in 9 untreated patients admitted to the emergency room, who were in need of rapid blood pressure reduction because of signs and symptoms of neurological and/or cardiac complications. During the 30 min following administration of captopril 25 mg the blood pressure decreased from 239/134±12/4 mmHg (mean±SEM) to 204/118±8/4 mmHg (p〈0.05). From that time on, captopril 200 to 300 mg/day was continued for 2 to 5 days. In 5 patients furosemide in a total dose of 40 to 160 mg i.v. or p.o. had also to be given in order to control the blood pressure. 12 and 24 h after admission blood pressure averaged 140/93 and 139/86 mmHg respectively, in the patients treated with captopril alone, and 166/107 and 153/91 mmHg in those treated both with captopril and furosemide. The pronounced fall in blood pressure produced by blockade of the renin system was well tolerated and did not cause tachycardia. It appears, therefore, that captopril given alone or in association with a diuretic makes it possible to treat the hypertensive crisis without the need for monitoring in an intensive care unit.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00543783

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8

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High-performance liquid chromatographic assay with fluorometric detection for flecainide and its major metabolites in urine and serum

Munafo, A. ; Biollaz, J.

Amsterdam : Elsevier

Journal of Chromatography B: Biomedical Sciences and Applications 490 (1989), S. 450-457

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ISSN: 0378-4347

Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002

Topics: Chemistry and Pharmacology

Type of Medium: Electronic Resource

URL: http://linkinghub.elsevier.com/retrieve/pii/S0378-4347(00)82805-4

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9

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Bioavailability of repeated oral administration of MDL 100,240, a dual inhibitor of angiotensin-converting enzyme and neutral endopeptidase in healthy volunteers (2000)

Rousso, P. ; Buclin, T. ; Nussberger, J. ; [et al.]

Springer

European journal of clinical pharmacology 55 (2000), S. 749-754

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ISSN: 1432-1041

Keywords: Key words NEP ; ACE inhibitor ; ANP

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: Abstract Background: MDL 100,240 (pyrido[2,1-a] [2]benzazepine-4-carboxylic acid,7-[[2-(acetylthio)-1-oxo-3-phenylpropyl]amino]-1,2,3,4,6,7,8,12b-octahydro-6-oxo, [4S-[4α,7α(R*),12bβ]]-) is a molecule possessing an inhibiting ability on both angiotensin converting enzyme (ACE) and neutral endopeptidase, the enzyme responsible for atrial natriuretic peptide (ANP) degradation. Such a dual mechanism of action presents a potential clinical interest for the treatment of hypertension and congestive heart failure. Objectives: To evaluate the bioavailability of MDL 100,240 and its accumulation over repeated oral administration, using ACE inhibition as a surrogate for plasma drug level and determining its profile after oral and i.v. administration. Methods: First, in an open, one-period, single-dose study, the ACE inhibition profile was characterised following a 12.5 mg MDL 100,240 i.v. infusion. Second, in a three-group, parallel, randomised, double-blind study, each group of four subjects received q.d., over 8 days, 2.5, 10 or 20 mg of MDL 100,240 orally. The ACE inhibition profile was determined on day 1 and day 8. Trough plasma ACE was measured on days 2, 3 and 4. The recovery of ACE activity was monitored up to 72 h after the last dose of MDL 100,240. Results: ACE inhibition profile was similar on day 1 and day 8, and trough inhibition remained unchanged after the 8 days of treatment with 10 mg or 20 mg. Following repeated 2.5-mg ingestion, trough inhibition increased from 33% to 44% after the eighth dose. The oral bioavailability of MDL 100,240 was estimated at 85%, not statistically different from 100%. The accumulation ratio at steady state was estimated at 112%. Expressing the accumulation ratio in terms of half-life, a t1/2 of 0.31 days or 7.5 h was estimated. Conclusion: MDL 100,240 (oral solution) has a good bioavailability, as estimated by ACE inhibition, and no drug accumulation seems to occur over 8 days with the 10-mg and 20-mg doses, but a slight rise in the trough level is observed with the 2.5-mg dose.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/s002280050009

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