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  • Articles  (69)
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  • Springer  (69)
  • Periodicals Archive Online (PAO)
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  • Chemistry and Pharmacology  (67)
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  • 1
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and pharmacodynamics of radio-labeled iloprost in elderly volunteers (1987)
    Springer
    European journal of clinical pharmacology 32 (1987), S. 597-605 
    Details
    ISSN: 1432-1041
    Keywords: iloprost ; prostacyclin analogue ; pharmacokinetics ; pharmacodynamics ; radiolabeled study ; volunteers ; side-effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The plasma levels and excretion of tritium-labeled iloprost in healthy elderly male and female volunteers have been measured after i.v. infusion of 2 ng·kg−1·min−1 for 4 h and oral administration of 0.1 and 0.48 μg/kg. During infusion, a steady-state of labeled compounds in the plasma was not achieved. Total radioactivity declined from a mean of 408 pg equiv/ml in three phases, with half-lives of 24 min, 1.7 h and 5.0 h, respectively. A steady-state of unchanged iloprost was reached rapidly with a peak of 81 pg/ml. Plasma levels declined biphasically with half-lives of 6 min and 31 min. Total clearance was 24 ml· min−1·kg−1. Maximum concentrations of labeled substances after oral administration were 307 and 1,051 pg equiv/ml after 29 and 39 min respectively. The peak of unchanged iloprost (116 pg/ml) was observed 7.5 min after an oral dose of 0.48 μg/kg. Bioavailability was 16%. Iloprost was totally metabolized and the metabolities were mainly excreted in urine. The main biotransformation products in plasma and urine were tentatively identified by cochromatography as dinor-and tetranoriloprost and their glucuronides. ADP-induced platelet aggregation was reduce by 60% during the i.v. infusion and 15 min after oral administration of 0.48 μg/kg. Heart rate and blood pressure were virtually unaffected. Common side-effects were facial flush, headache and nausea.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02455995
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  • 2
    Electronic Resource
    Electronic Resource
    Comparison of nicardipine and propranolol in the treatment of mild and moderate hypertension (1987)
    Springer
    European journal of clinical pharmacology 33 (1987), S. 119-126 
    Details
    ISSN: 1432-1041
    Keywords: hypertension ; nicardipine ; propranolol ; serum lipids ; electrocardiogram ; side-effects ; ECG changes
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In a double-blind controlled trial 22 patients with mild or moderate essential hypertension were treated with nicardipine 30 mg t.d.s. and 19 patients with propranolol 80 mg t.d.s. as monotherapy for 24 weeks. Blood pressure in both groups at the end of trial was equally and significantly reduced; systolic pressure 22.2 mmHg and diastolic pressure 15.5 mmHg in the supine position, and 24.4 mmHg and 18.4 mmHg, respectively, in the standing position in those on nicardipine, and by 23.7 and 16.2 mmHg and 28.0 and 19.2 mmHg, respectively, in the propranolol group. There was an initial increase in heart rate in the nicardipine group, but the rise was only moderate (3 beats/min supine p=0.3219, and 7 beats/min standing, p=0.0203) at the end of the 24 weeks. In the propranolol group heart rate was reduced markedly. Adverse effects occurred in 77% of patients on nicardipine and in 63% of those on propranolol, and there were no unexpected findings. The effects were mild in both groups and did not lead any patient to stop medication. One patient on propranolol was withdrawn from the trial because of poor blood pressure control and suspected angina pectoris after 5 weeks on active medication. There were no significant changes in blood chemistry, including lipoprotein classes. Overall, in comparison with propranolol, nicardipine was effective, well-tolerated and safe to use in the monotherapy of mild or moderate essential hypertension.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00544554
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  • 3
    Electronic Resource
    Electronic Resource
    Simvastatin and bezafibrate: Effects on serum lipoproteins and lecithin: Cholesterol acyltransferase activity in familial hypercholesterolaemia (1988)
    Springer
    European journal of clinical pharmacology 35 (1988), S. 579-583 
    Details
    ISSN: 1432-1041
    Keywords: simvastatin ; bezafibrate ; hypercholesterolaemia ; LCAT ; lipoproteins ; serum cholesterol ; serum triglycerides ; side-effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Sixteen subjects with familial hypercholesterolaemia were randomly assigned to treatment with simvastatin 20–40 mg/day (an inhibitor of 3-hydroxy-3-methylglutaryl CoA reductase) or with bezafibrate 600 mg/day (a clofibrate analogue) for 12 weeks. Both drugs produced significant reductions in serum and LDL cholesterol; mean percentage fall −30.5% and −38.1% (simvastatin) and −17.8% and −20.6% (bezafibrate), respectively. Both drugs also caused a decrease in VLDL cholesterol, while only bezafibrate decreased the serum and VLDL triglyceride levels and increased HDL cholesterol and serum apolipoprotein A-I and A-II levels. Serum apolipoprotein B fell by 33.3% (simvastatin) and 15.7% (bezafibrate). Simvastatin and bezafibrate produced significant increases in the mean fractional esterification rate of LCAT, by +124,1% and +20.6%, respectively. Thus simvastatin was clearly more effective than bezafibrate in lowering LDL by enhancing its turnover, but bezafibrate had specific effects on VLDL and HDL that might be favourable in combined treatment regimens.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00637592
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  • 4
    Electronic Resource
    Electronic Resource
    Effects of dilevalol, an R, R-isomer of labetalol, on blood pressure and renal function in patients with mild-to-moderate essential hypertension (1988)
    Springer
    European journal of clinical pharmacology 35 (1988), S. 9-15 
    Details
    ISSN: 1432-1041
    Keywords: dilevalol ; hypertension ; labetolol R-R-isomer ; renal function ; plasma renin activity ; plasma aldosterone ; side-effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effects of oral dilevalol (an R, R-isomer of labetalol), a new β-adrenoceptor blocker with β2-receptor stimulating and α-recepter blocking properties on blood pressure, renal function, plasma renin activity (PRA) and plasma aldosterone have been studied in 15 patients with mild-to-moderate essential hypertension treated with it for 6 weeks. Two patients with apparent treatment failure and one patient who developed muscle pain and cramps, and had an elevated creatine phosphokinase level, were excluded from the study. Dilevalol monotherapy 100 mg once daily for 6 weeks significantly lowered both the systolic and diastolic blood pressure compared to placebo. Total renal vascular resistance was significantly reduced, and RBF and GFR remained unchanged. Dilevalol significantly decreased PRA. The results suggest that prolonged daily treatment with dilevalol preserves renal function and produces a concomitant hypotensive action in patients with mild-to-moderate essential hypertension. The ancillary pharmacological properties of dilevalol rather than PRA suppression may be relevant to its renal effects.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00555500
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  • 5
    Electronic Resource
    Electronic Resource
    Field trial of the efficacy of a simplified and standard metrifonate treatments ofSchistosoma haematobium (1989)
    Springer
    European journal of clinical pharmacology 37 (1989), S. 371-374 
    Details
    ISSN: 1432-1041
    Keywords: metrifonate ; Schistosoma haematobium ; therapeutic regimen ; side-effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In a randomized double-blind study, the percentage egg reduction and cure rate after the standard schedule of metrifonate treatment ofSchistosoma haematobium (3 doses of 7.5 mg·kg−1 at two-weekly intervals; A) and an abbreviated regimen (3 doses of 5 mg·kg−1 in one day; B) were compared in five villages in Somalia. 300 patients who were excreting 20 or more eggs ofS. haematobium in 10 ml urine were recruited. The patients were classified according to their home villages and were then, randomly allocated to treatment A or B. They had similar ages, weights and egg output. Each patient received 3 doses of metrifonate and 2 doses of identical appearing placebo. Group A received metrifonate on the 1st, 4th and 5th dosing occasions and placebo on the 2nd and 3rd times. Group B received metrifonate on the 1st, 2nd and 3rd dosing times and placebo on the 4th and 5th times. Two hundred and one patients were followed up from 1 to 6 months. The remaining 99 (33%) patients either did not complete treatment or were lost during follow up. Egg reduction in the groups 1, 2, 3 and 6 months after treatment were 97, 97, 95 and 93% in Group A and 96, 96, 94 and 92% in Group B (NS). Corresponding cure rates for Group A were 52, 50, 48 and 44%, and in Group B they were 47, 48, 43 and 40% (NS). Seven patients from Group A and 9 from Group B complained of minor side-effects. Thus, under field conditions abbreviated regimen of metrifonate 5 mg·kg−1 3-times in one day could have as much efficacy and safety as the standard schedule of 3 doses of 7.5 mg·kg−1 at two-weekly intervals.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00558502
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  • 6
    Electronic Resource
    Electronic Resource
    Comparison of the pharmacokinetic profile of metaclazepam in old and young volunteers (1985)
    Springer
    European journal of clinical pharmacology 29 (1985), S. 247-249 
    Details
    ISSN: 1432-1041
    Keywords: metaclazepam ; benzodiazepines ; (KC-2547) ; N-desmethyl-methaclazepam KC-3755) ; pharmacokinetics ; old and young volunteers ; side-effects ; age effect
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A single-centre, open, Phase I-study comparison of the pharmacokinetics of a single dose of metaclazepam 10 mg, a new 1,4-benzodiazepine has been done in 10 older and 20 younger volunteers. No important age-related effect was found on the kinetics of metaclazepam or its N-desmethyl derivative, the principal metabolite in man.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00547431
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  • 7
    Electronic Resource
    Electronic Resource
    Pharmacokinetic study of a paediatric formulation of amoxycillin and clavulanic acid in children (1985)
    Springer
    European journal of clinical pharmacology 29 (1985), S. 235-239 
    Details
    ISSN: 1432-1041
    Keywords: amoxycillin ; clavulanic acid ; pharmacokinetics ; side-effects ; paediatric formulation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A combination of amoxycillin and clavulanic acid 4:1 was administered to 35 children (aged 2 to 10 years) with infections. The combination was administered orally as a suspension, every 8 h for 5 to 7 days. Sixteen children (aged 2 to 5 years), received 125 mg amoxycillin and 31.25 mg clavulanic acid, and 19 (6 to 10 years) received 250 mg amoxycillin and 62.5 mg clavulanic acid per dose. Following the first dose serum concentrations of amoxycillin and clavulanic acid were determined by microbiological assay. In the younger group receiving the lower dosage (mean: amoxycillin 9.11 mg/kg and clavulanic acid 2.34 mg/kg), the mean peak concentration of amoxycillin was 3.5 mg/l and of clavulanic acid 1.2 mg/l, occurring 1.32 h and 1.39 h, respectively, after administration. In the older group receiving the higher dosage (mean: amoxycillin 12.35 mg/kg and clavulanic acid 3.14 mg/kg) the mean peak serum level of amoxycillin was 4.0 mg/l and of clavulanic acid 1.3 mg/l, occurring 1.43 h and 1.23 h, respectively, after administration. The higher dose per kilogram body weight resulted in a higher peak serum concentration both of amoxycillin and clavulanic acid. The formulation was well tolerated by all the children and no serious side-effects were recorded. Treatment was considered clinically effective in all cases.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00547429
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  • 8
    Electronic Resource
    Electronic Resource
    Follow-up study of enzymuria and β 2 microglobulinuria during cis-platinum treatment (1985)
    Springer
    European journal of clinical pharmacology 29 (1985), S. 313-318 
    Details
    ISSN: 1432-1041
    Keywords: Cis-platinum ; nephrotoxicity ; longitudinal study ; plasma and urinary beta2 microglobulin ; urinary sodium excretion ; N-acetyl-glucosamidase ; side-effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Twenty patients with epithelian ovarian cancer treated with DDP (cis-diammine-dichloroplatinum II) 50 mg/m2 were followed for 24 weeks in order to assess the nephrotoxicity of the drug. Ten patients received the total dose in one day with heavy osmotic hydration (Group A), and for the other 10 the dose was subdivided over 3 consecutive days (Group B). The renal tubular toxicity of DDP treatment was evaluated over a total of 120 courses. After the first DDP administration, there was a prompt, reversable and dose-dependent increase in the urinary excretion of β 2 microglobulin with no difference between the two groups: Group A from 405 to 990 and Group B from 109 to 585 ng/mg creatinine. An increase always occurred during subsequent courses, but it was significantly lower in Group B after the sixth course, from 125 to 331 ng/mg creatinine. A similar pattern was found for the urinary excretion of N-acetyl-glucosaminidase (NAG), a lysosomal enzyme of tubular origin. The percentage fraction of urinary sodium excretion (FeNa%) increased after each dose of DDP; Group A from 0.82 to 2.30 and Group B from 0.68 to 2.53. This effect was reversible and it occurred to the same extent during the subsequent courses. There was no impairment of the glomerular filtration rate. Thus, enzymuria and β 2 microglobulin excretion are a sensitive tool to reveal minor tubular damage. Their use to predict serious renal dysfunction in longitudinal studies, however, seems questionable.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00544087
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  • 9
    Electronic Resource
    Electronic Resource
    Felodipine in hypertension (1985)
    Springer
    European journal of clinical pharmacology 29 (1985), S. 383-389 
    Details
    ISSN: 1432-1041
    Keywords: felodipine ; hypertension ; calcium antagonist ; vasodilator ; side-effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Felodipine, a selective arteriolar dilator, was given to 13 hypertensive patients to assess its hypotensive effects and duration of action. Nine patients were treated with 5 mg three times a day and 4 with 10 mg three times a day. Mean blood pressures fell with both treatment regimens: 5 mg placebo 170/103 mmHg; 5 mg felodipine 148/91 mmHg; 10 mg placebo 154/93 mmHg; 10 mg felodipine 137/82 mmHg. Heart rates increased as blood pressures fell with both treatments. However, in the patients given 5 mg three times a day this effect was less noticeable after successive doses. Plasma concentrations of noradrenaline, both resting and tilted, increased after felodipine. There was a negative correlation between the fall in blood pressure and the increase in noradrenaline, suggesting that those patients with good baroreceptor reflexes were better able to counteract the effects of vasodilatation. Four of the nine patients treated with 5 mg felodipine three times a day experienced mild and transient adverse effects. Of the four patients treated with 10 mg three times a day, three experienced moderate to severe headache, and for this reason recruitment into this group was stopped. Felodipine at a divided daily dose of 15 mg effectively lowered blood pressure.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00613449
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  • 10
    Electronic Resource
    Electronic Resource
    Baclofen in the elderly stroke patient its side-effects and pharmacokinetics (1985)
    Springer
    European journal of clinical pharmacology 29 (1985), S. 467-469 
    Details
    ISSN: 1432-1041
    Keywords: baclofen ; stroke ; elderly patients ; pharmacokinetics ; side-effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A double blind crossover trial of baclofen against placebo in elderly stroke patients was discontinued because the drug produced an unacceptably high level of drowsiness. In a subsequent study baclofen 10 mg was given orally to 12 elderly stroke patients, and drug concentrations measured from a series of plasma samples. A group of healthy subjects given the same dose in a previous study were used as controls. Elderly patients took longer to achieve peak plasma baclofen concentrations, but healthy controls had higher peak values and eliminated the drug more rapidly; areas under the curve were similar in the two groups. Simulations based on mean data suggest that increased drowsiness in the elderly was probably not due to changes in the drug's pharmacokinetic behaviour.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00613463
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