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  • 11
    Electronic Resource
    Electronic Resource
    A double blind trial of UK-38,485, an orally active thromboxane synthetase inhibitor, in the treatment of Raynaud’s syndrome (1984)
    Springer
    European journal of clinical pharmacology 27 (1984), S. 61-65 
    Details
    ISSN: 1432-1041
    Keywords: thromboxane synthetase inhibitors ; Raynaud’s syndrome ; systemic sclerosis ; UK-38,485 ; ischaemic attacks ; red blood cell rheology
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Ten patients with moderate to severe Raynaud’s syndrome were recruited into a four week randomised double blind crossover study to compare the efficacy of UK-38,485 50 mg, a new thromboxane synthetase inhibitor with that of placebo. With the doses used there was no significant difference between the two treatment periods in the number, severity and duration of ischaemic attacks, the mean hand temperatures, forearm and digital blood flow and red blood cell rheology.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02395208
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  • 12
    Electronic Resource
    Electronic Resource
    The relationship between theophylline clearance and age in adult life (1989)
    Springer
    European journal of clinical pharmacology 36 (1989), S. 29-34 
    Details
    ISSN: 1432-1041
    Keywords: theophylline ; asthma ; clearance ; age ; adults ; elderly ; normal subjects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Fifty three subjects (31 normal volunteers and 22 patients with asthma) between the ages of 20 and 87 years had their theophylline clearance measured. Volume of distribution (V) and terminal elimination half-life (t1/2) were also calculated in the volunteers who received i.v. theophylline. Although patients tended to have higher clearance values than volunteers, in both groups the oldest third had the lowest clearances. For the combined group (corrected for the patient effect) the oldest third (mean age 70 years) had a mean clearance of 0.53 versus 0.72 for the middle third (mean age 47 years) and 0.73 ml/min/kg CBW for the youngest third (mean age 26 years). There was no statistically significant age related change in V/kg CBW but t1/2 did rise with increasing age. Thus, although clearance does not fall with increasing age during younger adult life, there is a fall during late adult life becoming apparent in the seventh, eighth and ninth decades.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00561019
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  • 13
    Electronic Resource
    Electronic Resource
    Flupirtine maleate and antipyrine half-life (1987)
    Springer
    European journal of clinical pharmacology 33 (1987), S. 437-437 
    Details
    ISSN: 1432-1041
    Keywords: Flupirtine maleate ; antipyrine ; half-life ; pharmaco kinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00637646
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  • 14
    Electronic Resource
    Electronic Resource
    Medifoxamine: Oral tolerance and pharmacokinetic study in healthy human volunteers (1990)
    Springer
    European journal of clinical pharmacology 39 (1990), S. 169-171 
    Details
    ISSN: 1432-1041
    Keywords: antidepressant ; medifoxamine ; tolerance ; pharmacokinetics healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Medifoxamine is a monoamine reuptake inhibiting antidepressant drug. We have investigated its pharmacokinetics in normal healthy volunteers. After an overnight fast, ascending doses of 200, 500, 750 and 1000 mg of medifoxamine were taken orally. Plasma samples were analysed using a specific HPLC method. Medifoxamine was well tolerated and exhibited a first order linear pharmacokinetic profile. It underwent rapid absorption and peak plasma concentrations were achieved about 1.0 h after administration. Thereafter the elimination profile was biphasic with a mean terminal half life less than 3 hours. We found a linear relationship (r=0.80) between administered dose and AUC values for the four doses. High values were obtained for the apparent volumes of distribution and the plasma clearance.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00280053
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  • 15
    Electronic Resource
    Electronic Resource
    Antagonism by domperidone of the ocular hypotensive effect of pergolide (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 461-463 
    Details
    ISSN: 1432-1041
    Keywords: domperidone ; pergolide ; dopaminergic agonists ; intraocular pressure ; non-contact tonometer ; drug interaction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary 1 The effect of pre-dosing with 15 mg domperidone, a relatively selective dopamine 2-receptor antagonist, on the ocular hypotensive action of a single oral dose of 25 μg pergolide, a dopamine 2-receptor agonist, was studied in 9 normal human volunteers, using a non-invasive method. 2 Compared with domperidone followed after 1 h by placebo, placebo followed after 1 h by pergolide had an ocular hypotensive effect in both eyes. Domperidone followed after 1 h by pergolide had no effect on intraocular pressure in both eyes. 2 The results of this study showed that domperidone inhibited the ocular hypotensive action of pergolide, suggesting that pergolide reduces introcular pressure by the stimulation of the peripheral dopamine 2-receptors.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02336684
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  • 16
    Electronic Resource
    Electronic Resource
    Cutaneous blood flow changes and weal induced by intradermal bradykinin following pretreatment with indomethacin and captopril (1993)
    Springer
    European journal of clinical pharmacology 44 (1993), S. 41-45 
    Details
    ISSN: 1432-1041
    Keywords: Bradykinin ; Captopril ; Indomethacin ; laser Doppler ; cutaneous blood flow
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effects of indomethacin and captopril on local cutaneous blood flow changes and weal induced by intradermal injections of bradykinin were assessed in two randomised, double-blind, placebo-controlled studies in healthy volunteers. Alterations in cutaneous blood flow were estimated by laser Doppler flowmetry (LDF) and erythema area. LDF output, erythema area and weal volume increased with incremental bradykinin dose. Single doses of indomethacin 25 mg and 75 mg did not affect these cutaneous responses compared with placebo. Captopril 25 mg significantly potentiated the increase in local cutaneous blood flow measured by LDF, but not erythema area, and weal volume induced by bradykinin. The effects of the combined treatment of indomethacin 75 mg and captopril 25 mg were not significantly different from those due to captopril alone. The enhanced cutaneous effects of bradykinin following administration of captopril are in keeping with effective kininase II inhibition in the tissues. Cyclo-oxygenase products release does not appear to contribute to the cutaneous actions of bradykinin nor the potentiation of these responses by captopril.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00315278
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  • 17
    Electronic Resource
    Electronic Resource
    Influence of debrisoquine hydroxylation phenotype on the pharmacokinetics of mexiletine (1993)
    Springer
    European journal of clinical pharmacology 44 (1993), S. 63-67 
    Details
    ISSN: 1432-1041
    Keywords: Mexiletine ; Debrisoquine hydroxylation phenotype ; pharmacokinetic ; variability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Marked interindividual variation has been observed in the pharmacokinetics of the antiarrhythmic agent mexiletine. The fact that its urinary excretion is dependent on urinary pH may account, in part, for such variation. The influence that genetic differences in hepatic metabolism of the debrisoquine-type may have on mexiletine pharmacokinetics was considered in this study. The pharmacokinetics and urinary excretion of mexiletine (250 mg administered intravenously) were investigated in 5 rapid extensive metabolisers (EM), 5 slow EM and 5 poor metabolisers (PM) of debrisoquine, under conditions of controlled urinary pH. Mexiletine disposition kinetics was found to be altered in PM individuals. These subjects showed higher total area under the curve (AUC), (15.7 versus 8.16 μg · h · ml−1) prolonged elimination half-lives (in serum and urine) (serum: 18.5 versus 11.6 h, urine: 19.2 versus 11.7 h) and lower total clearance values compared with EM (216 versus 450 ml · min−1). In this respect, slow EM individuals generally presented intermediate values of those pharmacokinetic parameters. A higher incidence of adverse-effects was also observed among slow EM and PM subjects. It is concluded that genetic differences in mexiletine oxidation of the debrisoquine-type have an influence on its observed pharmacokinetic variability. The clinical consequences are discussed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00315282
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  • 18
    Electronic Resource
    Electronic Resource
    Erratum (1979)
    Springer
    European journal of clinical pharmacology 15 (1979), S. 72-72 
    Details
    ISSN: 1432-1041
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00563561
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  • 19
    Electronic Resource
    Electronic Resource
    Relationship between bronchial effects and plasma practolol concentration in man (1979)
    Springer
    European journal of clinical pharmacology 15 (1979), S. 91-96 
    Details
    ISSN: 1432-1041
    Keywords: practolol ; propranolol ; cardioselectivity ; heart rate ; peak expiratory flow rate ; exercise ; plasma concentration ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A double-blind, balanced and randomised study in 8 healthy volunteers examined the effects of relatively high versus low single doses of practolol on heart rate and ventilation at rest and during standardised exercise. Practolol 1 and 4 mg/kg, a typically non-selective drug propranolol 0.2 mg/kg, and placebo were given intravenously at weekly intervals. Cardiac beta-adrenoceptor blockade was measured by the reduction in exercise heart rate 〉160 beats/min, and bronchial beta-adrenoceptor blockade by the reduction in exercise peak expiratory flow rate (PEFR) up to 4 h after each treatment. Results were assessed by analysis of co-variance. All three active treatments reduced exercise heart rate markedly, practolol 4 mg/kg causing most reduction. Exercise PEFR was significantly reduced by propranolol 0.2 mg/kg compared with both practolol 1 mg/kg and placebo at all times of measurement, and by practolol 4 mg/kg compared with practolol 1 mg/kg and placebo at most times. Mean plasma concentrations after practolol 4 mg/kg were 3.5 to 4.5 times higher than after 1 mg/kg. Practolol may lose its ‘cardioselectivity’ and cause airflow obstruction at relatively high plasma concentrations above about 2 µg/ml.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00609870
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  • 20
    Electronic Resource
    Electronic Resource
    Metabolic studies of taloximine and its effects on the respiratory response to carbon dioxide (1970)
    Springer
    European journal of clinical pharmacology 2 (1970), S. 155-160 
    Details
    ISSN: 1432-1041
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Taloximine is a phthalazine derivative with a respiratory stimulant action on the peripheral chemoreceptors. Peak plasma levels of taloximine after oral administration coincided with peak hyperventilation accompanied by a respiratory alkalosis, a, fall in venous pCO2, and a rise in plasma and urinary pH. — Taloximine was excreted in urine and bile. Metabolites included a phthalazinone, demethylated taloximine and other metabolites in ring hydroxylated form. Sulphated and glucuronated taloximine and metabolites were formed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00420343
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