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  • 1
    Electronic Resource
    Electronic Resource
    Effects of the new angiotensin-converting enzyme inhibitor, ramipril, in patients with essential hypertension (1986)
    Springer
    Journal of molecular medicine 64 (1986), S. 558-562 
    Details
    ISSN: 1432-1440
    Keywords: Angiotensin-converting enzyme inhibition ; Ramipril ; Essential hypertension
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The antihypertensive and hormonal effects of the new angiotensin-converting enzyme (ACE) inhibitor, ramipril, were assessed by means of a single-blind trial in ten unselected patients with mild-to-moderate essential hypertension. After a 2-week period on placebo, 5 mg ramipril was administered once daily for 2 weeks. Blood pressure returned to normal in five patients and decreased in the remaining patients, without significant changes in heart rate or orthostatic hypotension. A fall in blood pressure was apparent within 1–2 h of the first dose; the maximum decrease was reached at 4–6 h and a fall in pressure was still detectable after 24 h. At 24 h post dose angiotensin-converting enzyme activity was suppressed to 40% of the baseline. Blood pressures for the 10 h interval post dosing showed smooth through-the-day control with minimal peak/trough difference in lowering effect. The magnitude of the blood pressure decrement achieved with the inhibitor did not correlate with baseline renin levels or the rise in renin following treatment. No side-effects were noted during the 2-week observation period. The study demonstrates that ramipril, given in a once-daily regimen over a period of 2 weeks, is well tolerated and provides smooth and effective blood pressure control throughout the 24-h interval between doses.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01735319
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Pharmacokinetic aspects of the interaction between clobazam and cimetidine (1983)
    Springer
    European journal of clinical pharmacology 25 (1983), S. 139-142 
    Details
    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.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00544031
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and pharmacodynamics of a novel orally active angiotensin converting enzyme inhibitor (HOE 498) in healthy subjects (1984)
    Springer
    European journal of clinical pharmacology 27 (1984), S. 577-581 
    Details
    ISSN: 1432-1041
    Keywords: HOE 498 ; ACE inhibitor ; pharmacokinetics ; pharmacodynamics ; urinary excretion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics and pharmacodynamics of the angiotensin converting enzyme inhibitor HOE 498 were investigated in 10 healthy normotensive male subjects. Serum levels of the active metabolite M 1 (dicarboxylic acid) of HOE 498 were measured by HPLC up to 14 days after a single oral dose of 10 m g HOE 498. Peak serum concentration of M 1 between 5–50 ng/ml was observed 1.5–3.0 h after administration. The serum concentration-time curve of M 1 was polyphasic and exhibited a prolonged terminal phase with a half-life of approximately 110 h. Despite the long terminal half-life M 1 could not be detected in urine later than 72 h after administration. The activity of the angiotensin converting enzyme in plasma was completely suppressed for up to 12 h, and 72 h after dosing 50% inhibition of the enzyme was still observed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00556895
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    Paper (German National Licenses)
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  • 4
    Electronic Resource
    Electronic Resource
    Single-dose pharmacokinetics of temocapril and temocapril diacid in subjects with varying degrees of renal impairment (1997)
    Springer
    European journal of clinical pharmacology 53 (1997), S. 215-220 
    Details
    ISSN: 1432-1041
    Keywords: Key words Temocapril ; Renal failure
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract Objective: The aim of this study was to determine the influence of renal impairment on the single-dose pharmacokinetics of temocapril and its pharmacologically active metabolite, temocapril diacid. Methods: A single oral dose of 20 mg temocapril hydrochloride was given after an overnight fast to eight healthy (control) subjects (group A, n=8) with a mean baseline creatinine clearance (CLCR) of 115.2 ml · min−1 and to three groups of patients with decreased renal function (mean CLCR 56.9 ml in group B, n=8, 30.0 ml · min−1 in group C, n=8 and 15.4 ml · min−1 in group D, n=5). Results: The mean peak concentration and median time to peak concentration for both temocapril and its diacid metabolite as well as the mean area under the curve (AUC0∞) for temocapril did not differ significantly between groups. The mean AUC0∞ for temocapril diacid increased only two- to threefold from group A to D. The mean terminal elimination half-life (t½) for temocapril diacid was prolonged in subjects with impaired renal function. However, prolongation of mean t½ and increase in AUC0−∞ did not parallel the decrease of mean renal clearance for temocapril diacid. Conclusion: The results suggest the existence of an alternative pathway in addition to the renal excretion of temocapril, e.g. via the bile. This pathway substantially contributes to the elimination of the active metabolite, temocapril diacid, in patients with decreased renal function. Nonetheless, to avoid any risks, the dose of temocapril hydrochloride in patients with moderate to severe renal impairment should be reduced.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/s002280050365
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    Paper (German National Licenses)
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