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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 33 (1987), S. 211-214 
    ISSN: 1432-1041
    Keywords: temazepam ; pharmacokinetics ; oral dose ; distribution half-life
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetic disposition of temazepam was compared after a day-time and night-time dose in an open randomised crossover study. Twelve healthy male volunteers received a single oral dose of 20 mg temazepam in a soft gelatine capsule at 0900 h or 2200 h. Blood samples were taken immediately before dosing and at selected times over the 36-h period after each dose. The absorption of temazepam was slower after evening administration; the absorption half-life and time to reach maximal plasma concentration being 0.53 h and 1.67 h respectively, compared to 0.38 h and 1.02 h following morning administration. Considering distribution characteristics, evening administration produced a lower peak plasma temazepam concentration (362 ng/ml) compared with a day-time level of 510 ng/ml. Distribution half-life after night-time administration was increased compared with day-time administration (1.76 h vs 1.03 h). A significantly higher percentage of the drug, relative to Cmax, remained in the plasma at 8 and 24 h after evening dosing (39.3 and 15.4% compared to 24.7 and 11.2% following day-time administration). In spite of the half-lives of absorption, distribution and elimination all being longer after the evening dose, the overall bioavailability, as measured by the area under the curve (AUC) was comparable after the two times of administration. Similarly the difference in the mean residence time (MRT) of the two doses was within accepted limits. It is concluded that a chronopharmacokinetic effect was seen for temazepam; however it is unlikely to be of any clinical significance.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 44 (1993), S. 69-72 
    ISSN: 1432-1041
    Keywords: Allopurinol ; Gout ; oxypurinol ; benzbromarone ; interaction ; tubular reabsorption
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The objectives of this study were to establish if, and to what extent, benzbromarone affects allopurinol/oxypurinol kinetics, and to compare the uric acid lowering capabilities of Allomaron® (allopurinol 100 mg plus benzbromarone 20 mg) with the effects of allopurinol alone in patients with confirmed gout. We studied 14 adult men in an open randomized cross-over study. After a 14 day run-in period with Zyloprim® (2×100 mg allopurinol tablets in the morning), the patients were randomly allocated to morning doses of either Allomaron® (2 tablets) or Zyloprim® (2 tablets). Seven days later cross-over was effected and the alternative treatment was taken for a further 7 days. On days 7 and 14 the patients came into hospital and venous blood samples were taken over 24 h for allopurinol and oxypurinol assays by HPLC. Serum uric acid was determined on days -14, 1, 7, and 14. Benzbromarone lowered plasma oxypurinol concentrations (Allomaron®/Zyloprim® mean ratio of AUC0→24 was 59%; 95% confidence interval 54–64%), but did not affect plasma allopurinol concentrations. Despite this pharmacokinetic interaction of benzbromarone with allopurinol, resulting in lower plasma concentrations of oxypurinol, Allomaron® was superior to allopurinol alone in lowering serum uric acid, probably because of the added uricosuric effect of benzbromarone.
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 47 (1994), S. 373-375 
    ISSN: 1432-1041
    Keywords: ACE-inhibitors ; Simvastatin ; ramipril ; lipid lowering drugs ; drug interaction ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract Twenty two healthy males participated in a randomised, placebo-controlled, double blind, cross-over study to investigate the influence of simvastatin on the pharmacokinetics of ramipril and its active metabolite (ramiprilat), and on the ACE-inhibiting effect of ramiprilat. During two study periods, each of 7 days, subjects received daily either simvastatin 20 mg at 19.00 h or placebo; ramipril (5 mg) was given on Day 5 of each of the periods. Plasma concentrations of ramipril and ramiprilat and ACE-activity were measured in sequential blood specimens, and ramipril and ramiprilat concentrations were measured in urine. Blood and urine collections for pharmacokinetic and pharmacodynamic assessment were made up to 72 h after the dose of ramipril. The mean AUC of ramipril for ramipril+placebo (R+P) and ramipril+simvastatin (R+S) was 22.2 and 21.3 ng.h.ml−, respectively; for ramiprilat the corresponding figures were 61.3 and 57.6 ng.h.ml−. The urinary excretion of ramipril+metabolites for (R+P) and (R+S) was 25.2 and 24.1% of dose. The maximum percentage inhibition of ACE-activity for (R+P) was 94.6%, and for (R+S) it was 94.1%. It is concluded that concomitant administration of simvastatin and ramipril has no clinically relevant effect on the pharmacokinetics or ACE-inhibition of the latter drug and its metabolites.
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 14 (1978), S. 101-104 
    ISSN: 1432-1041
    Keywords: Digoxin ; electrocardiogram ; serum potassium ; whole body potassium ; PTQ-index
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Previous studies have shown a significant linear relationship between the PTQ-index (a combination function of the PR-interval, corrected QT-time and T-wave depression in the ECG) and serum digoxin level in chronically treated patients. The relationship was confirmed in the present study and it was shown that it could be changed by concomitant administration of potassium chloride or furosemide, and that there was marked interindividual variation in response. An inverse linear relationship between PTQ-index and whole body potassium was found during chronic administration of a constant daily dose of digoxin, but no such relationship was found for serum potassium.
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  • 5
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 35 (1988), S. 319-321 
    ISSN: 1432-1041
    Keywords: H1 antagonists ; cetirizine ; dexchlorpheniramine ; skin wheal ; CNS depression
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A double-blind cross-over study was performed in 12 healthy female volunteers comparing cetirizine di-HCl (10 mg) and sustained release dexchlorpheniramine maleate (6 mg) with respect to attentuation of histamine-induced skin wheals and subjective central nervous system (CNS) effects. Cetirizine was significantly more effective than dexchlorpheniramine in suppressing the size of wheals from 2 to 24 h after drug administration. In fact, at 24 h cetirizine was still as affective as 2 h after ingestion. Ten subjects receiving dexchlorpheniramine reported subjective symptoms relating to CNS depression, in contrast to only one subject given cetirizine.
    Type of Medium: Electronic Resource
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  • 6
    ISSN: 1432-1041
    Keywords: clobazam ; cimetidine ; N-desmethylclobazam ; kinetic interaction ; man
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetic interaction between clobazam and cimetidine was studied in 9 healthy male volunteers in an open-labelled study. After a single oral dose of clobazam 30 mg, a wash-out period of 14 days was followed by daily doses of cimetidine 1 g for one week. Thereafter a single oral dose of clobazam 30 mg was again given. The plasma concentrations of clobazam and its main metabolite N-desmethyl-clobazam were measured by gas-chromatography. The area under the curve (AUC0−∞) of plasma clobazam level was significantly larger after pretreatment with cimetidine and the elimination half life of clobazam was significantly longer. There were no statistically significant differences in Cmax and tmax for plasma clobazam. The plasma levels of N-desmethyl-clobazam did not show any significant change after the intake of cimetidine.
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  • 7
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 25 (1983), S. 783-785 
    ISSN: 1432-1041
    Keywords: piretanide ; urine K+ and Na+ clearance ; pharmacodynamic effects ; pharmacokinetic effects ; diuretic effects ; dose-response relationship ; trial design
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Three doses (3 mg, 6 mg and 12 mg) of piretanide, a new high ceiling diuretic, and placebo were given to 8 volunteers to investigate the relationship between the pharmacodynamic parameters, the dose and its urinary excretion. Intake of food and fluid were standardized from 48 h before until 24 h after drug administration. Urinary output, excretion of unchanged drug, and the excretion and clearance of Na+ and K+ were measured hourly for 7 h after treatment. A clear dose-response relationship was found for cumulative urinary output, cumulative excretion of Na+ and K+, clearance of Na+ and K+ and the urinary sodium/potassium ratio. A significant correlation was found between the net urine volume and the excretion of piretanide per time interval. The clearances of Na+ and K+ were significantly correlated with the excretion of piretanide. Clearance values correlated well with corresponding urine volumes.
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  • 8
    ISSN: 1432-1041
    Keywords: Meloxicam ; Furosemide ; drug interactions ; electrolytes ; NSAIDs
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract Fifteen healthy male volunteers participated in an open, multiple-dose study to investigate a possible interaction between furosemide and meloxicam, a new non-steroidal anti-inflammatory agent (NSAID). The study comprised three treatment periods. First, furosemide (40 mg) was administered as a single oral daily dose for 3 days. A wash-out day was followed by the administration of meloxicam (15 mg) as a single oral daily dose for 10 days. Thereafter, meloxicam and furosemide were administered concomitantly at the same doses as described above, for 3 days. The effect of concomitant ingestion of meloxicam and furosemide on furosemide-induced diuresis, urine and serum electrolytes, and furosemide pharmacokinetics was determined, after both single and repeated administration of furosemide. Estimates of the “(furosemide + meloxicam)/(furosemide alone)” mean ratio of the variable AUC(0-∞) for plasma furosemide and the cumulative sodium excretion (0–8 h) were 97.4% (90% confidence interval 89.7–106%) and 88% (90% confidence interval 82–94%), respectively. The study results indicate that meloxicam does not affect the pharmacokinetics of furosemide in healthy volunteers, nor does it affect furosemide-induced diuresis or serum electrolytes. The cumulative urinary electrolyte excretion after concomitant administration of meloxicam and furosemide is somewhat lower than after administration of furosemide alone, in particular for the period 0–8 h after administration of furosemide. This effect of meloxicam on furosemide dynamics is small, and is probably not clinically relevant in healthy volunteers under the dosing regime studied.
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  • 9
    Electronic Resource
    Electronic Resource
    Springer
    Cellular and molecular life sciences 26 (1970), S. 169-170 
    ISSN: 1420-9071
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Zusammenfassung Ratten (20 Tiere, 45 Tage alt) erhielten 150 mg/kg paraglynes Hydrochlorid s.c. injiziert. Akustischer Schock (2 h später) ergab bei 16 von 20 Tieren eine reversible subkapsuläre Linsentrübung.
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  • 10
    Publication Date: 1970-02-01
    Print ISSN: 0014-4754
    Topics: Biology , Medicine
    Published by Springer
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