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  • healthy volunteers  (31)
  • Springer  (31)
  • Copernicus
  • 1985-1989  (31)
  • 1970-1974
  • 1986  (31)
Collection
Keywords
Publisher
  • Springer  (31)
  • Copernicus
Years
  • 1985-1989  (31)
  • 1970-1974
Year
  • 1
    Electronic Resource
    Electronic Resource
    The effect of ranitidine and cimetidine on imipramine disposition (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 285-290 
    Details
    ISSN: 1432-1041
    Keywords: imipramine ; ranitidine ; cimetidine ; pharmacokinetics ; metabolism ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetic characteristics of imipramine were studied after a single, oral, 100 mg dose was taken by 12 healthy male subjects following 3 days of pretreatment with placebo, cimetidine (300 mg every 6 h), and ranitidine (150 mg every 12 h) in a randomized, double blind, crossover trial. After each imipramine dose plasma samples were collected for 72 h and assayed for imipramine, desipramine, 2-hydroxyimipramine and 2-hydroxydesipramine by HPLC. Cimetidine preadministration statistically prolonged imipramine t1/2 compared to ranitidine (22.7 vs. 13.0 h) or placebo (10.8 h). Mean imipramine area under the curve (AUC) following cimetidine pretreatment was more than double that following placebo (2.633 vs. 0.966 µg·h·ml−1) or ranitidine (1.14 µg·h·ml−1) pretreatment. Imipramine apparent oral clearance was reduced in all 12 subjects after cimetidine. Compared to ranitidine or placebo, cimetidine pretreatment was associated with an increased imipramine/desipramine AUC ratio, suggesting cimetidine-induced impairment of demethylation of imipramine. Ranitidine was not observed to alter imipramine pharmacokinetics.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00981125
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  • 2
    Electronic Resource
    Electronic Resource
    Femoxetine and cimetidine: Interaction in healthy volunteers (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 299-302 
    Details
    ISSN: 1432-1041
    Keywords: femoxetine ; cimetidine ; pharmacokinetics ; drug interaction ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The possibility of a pharmacokinetic interaction between femoxetine and cimetidine has been evaluated in 8 healthy volunteers. Two volunteers received single doses of femoxetine, and 6 were given multiple doses of femoxetine for 7 days with and without concurrent cimetidine. No influence of cimetidine was observed on the kinetics of single doses of femoxetine, but after multiple doses the plasma concentration of femoxetine was significantly increased. Similarly, the AUC at steady state tended to be increased, but not to a significant extent. Concurrent cimetidine did not cause a reduction in the AUC of the active desmethyl metabolite. It is recommended that femoxetine is given in reduced doses (e.g. 400 mg) when administered with cimetidine.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00981127
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  • 3
    Electronic Resource
    Electronic Resource
    Influence of slow calcium-channel blockade on the cardiovascular effects of coffee (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 171-175 
    Details
    ISSN: 1432-1041
    Keywords: caffeine ; verapamil ; coffee ; blood pressure ; slow calcium-channel blockade ; drug interaction ; healthy volunteers ; plasma catecholamines ; plasma renin activity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary An increase in blood pressure after coffee and caffeine has recently been reported. A possible pharmacological mechanism for this pressor response is a rise in the intracellular calcium concentration, caused by an increase in calcium influx due to a direct effect of caffeine. Accordingly, the cardiovascular effects of drinking coffee after placebo and verapamil 3 × 80 mg in 1 day in 10 normotensive volunteers have been examined in a single-blind study. After placebo, coffee led to an increase in blood pressure (7/14 mm Hg), and a fall in heart rate (−7 beats/min); forearm blood flow did not change. Plasma epinephrine rose (257%), plasma norepinephrine did not change and the plasma renin activity fell significantly. The haemodynamic and humoral changes after coffee were not altered by pretreatment with verapamil. It is concluded that increased transmembrane calcium influx after caffeine does not appear to be an important pharmacological mechanism for the circulatory effects of coffee.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00614297
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  • 4
    Electronic Resource
    Electronic Resource
    Correlations between in vitro dissolution, in vivo bioavailability and hypoglycaemic effect of oral glibenclamide (1986)
    Springer
    European journal of clinical pharmacology 31 (1986), S. 177-182 
    Details
    ISSN: 1432-1041
    Keywords: glibenclamide ; bioavailability ; pharmacokinetics ; dissolution ; hypoglycaemia ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A study has been carried out investigating four different marketed oral preparations of glibenclamide, correlating the effectiveness of the drug in these preparations in lowering plasma glucose concentrations with (i) the in vitro dissolution of the drug, measured by the British Pharmacopoeal and Desaga methods, and (ii) the in vivo bioavailability, assessed in 12 healthy human volunteers. The two dissolution methods yielded different rank orders of ease of dissolution of the drug from the various preparations; the findings of neither dissolution method correlated adequately with the results of the in vivo bioavailability studies, which correctly predicted the abilities of the preparations to reduce plasma glucose concentrations. Relative to an oral glibenclamide solution the bioavailabilities of the drug from three tablet preparations were 0.69, 0.49 and 0.24. The mean elimination half-life of the drug was 1.5 h and assuming complete bioavailability of the drug from oral solution the mean systemic clearance was 0.095 l kg−1h−1, and the mean apparent volume of distribution was 0.20 l kg−1. It is concluded that it may be unsafe to use in vitro dissolution data as a basis for assessing the bioequivalences of different glibenclamide preparations intended for oral use.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00606655
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  • 5
    Electronic Resource
    Electronic Resource
    Effects of angiotensin converting enzyme inhibitor, perindopril, on autonomic reflexes (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 177-182 
    Details
    ISSN: 1432-1041
    Keywords: perindopril ; blood pressure ; heart rate ; parasympathetic ; sympathetic ; converting enzyme inhibitor ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of the angiotensin converting enzyme inhibitor, perindopril, on autonomic function was assessed in a double blind, placebo controlled, crossover study in 10 normotensive males. Eight milligram of perindopril given orally lowered blood pressure without a change in heart rate. Perindopril enhanced the vagally mediated heart rate variation with deep breathing. There was no impairment of the responses to either bicycle exercise at 175 W for 5 min or isometric handgrip. The pressor response to cold was not changed and the response to the Valsalva manoeuvre was unaltered. These results suggest that the absence of tachycardia after perindopril may be in part related, as has been reported with other converting enzyme inhibitors, to enhanced cardiac parasympathetic tone. Vagomimetic action may be a property of converting enzyme inhibitors in general.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00614298
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  • 6
    Electronic Resource
    Electronic Resource
    Increased effect of multiple doses of 40 749 RP a new long acting gastric antisecretory agent (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 269-271 
    Details
    ISSN: 1432-1041
    Keywords: gastric antisecretory agent ; 40 749 RP ; long acting drug ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary 40 749 RP, a pyridyl-2-tetrahydrothiophene derivative is known to be a potent gastric antisecretory agent in animals and man. In 27 healthy volunteers in four double-blind cross-over studies, this activity has been examined against basal and pentagastrin stimulated gastric acid secretion. The effect of a single oral dose of 2 mg/kg was still present after 12, 24 and 48 h. The effect of 1 mg/kg was definitely increased after treatment for 7 days as compared to a single dose of 1 mg/kg.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541526
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  • 7
    Electronic Resource
    Electronic Resource
    Methylprednisolone versus prednisolone pharmacokinetics in relation to dose in adults (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 323-329 
    Details
    ISSN: 1432-1041
    Keywords: methylprednisolone ; prednisolone ; pharmacokinetics ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The disposition and plasma binding of methylprednisolone were examined in seven normal volunteers following the administration of 5, 20 and 40 mg of intravenous methylprednisolone sodium succinate. Methylprednisolone exhibits linear plasma protein binding averaging 77%. The mean plasma methylprednisolone clearance of 337 ml·h−1. kg−1 was independent of dose. The steroid appears to moderately distribute into tissue spaces with a mean volume of distribution of 1.41·kg−1. Methylprednisolone disposition parameters were compared with the non-transcortin bound parameters for prednisolone. The prednisolone plasma clearance based on the transcortin free-drug is similar to methylprednisolone total plasma clearance. However, the corrected volume of distribution of prednisolone is only one-half that of methylprednisolone. The disposition rate of these two steroids is thus similar, in spite of their metabolic control by different enzymatic pathways and major influence of saturable transcortin binding on prednisolone elimination.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541537
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  • 8
    Electronic Resource
    Electronic Resource
    Substance P and human nasal mucociliary activity (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 355-357 
    Details
    ISSN: 1432-1041
    Keywords: substance P ; mucociliary activity ; inflamatory reactions ; nose ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Substance P (SP), a potent inflammatory agent, has been found in sensory nerve fibres in the nasal mucosa in several experimental animals as well as in man. It may participate in the inflammatory response as part of the mucosal defence against foreign materials. In experimental animals SP has been found to increase mucociliary in airway mucosa. The present study was performed in order to find out the relationship between topically applied SP and nasal mucociliary function in humans. Thirteen healthy volunteers were challenged with 65 µg SP or placebo in a randomized cross over fashion and mucociliary transport time was determined each time using the saccharine dye test. The dose of SP was chosen after an open dose-response study. No statistically significant change in the mucociliary transport time was found after challenge with SP as compared to placebo. The possible reasons for this are discussed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541544
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  • 9
    Electronic Resource
    Electronic Resource
    Venoconstrictor effects of dihydroergotamine after intranasal and intramuscular administration (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 581-584 
    Details
    ISSN: 1432-1041
    Keywords: dihydroergotamine ; venoconstriction ; nasal spray ; healthy volunteers ; i.m. administration
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A parenteral formulation of dihydroergotamine (DHE) is the only galenical form now available for the treatment of acute attacks of migraine in which a rapid onset of action is required. A recently developed nasal spray of DHE has been compared with intramuscular DHE for its venoconstrictor activity. In a randomised double-blind, cross-over trial, 9 healthy male volunteers received a single dose of DHE 1 mg intranasally, DHE 0.5 mg i.m. or placebo (intranasally and i.m.) on three different occasions, with an interval of at least 1 week between doses. Both active treatments, but not placebo, produced marked venoconstriction as shown by reduced compliance of superficial hand veins. The effect persisted for more than 8 h. The maximum venoconstrictor effect of 1 mg DHE intransally was 40±12% (mean ± SEM) and after 0.5 mg i.m. it was 52±15%. The time course of the venoconstrictor effect was similar after both routes of administration. Blood pressure and heart rate changes in these normotensive subjects were almost identical after dihydroergotamine and placebo. The results suggest that the nasal spray could be used as an alternative to parenteral DHE, permitting self-administration of the drug for the treatment of acute attacks of migraine.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542418
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  • 10
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of cimetidine after subchronic administration (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 741-744 
    Details
    ISSN: 1432-1041
    Keywords: cimetidine ; subchronic administration ; pharmacokinetics ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The influence of cimetidine on its own pharmacokinetics after subchronic administration was assessed in 8 healthy volunteers, aged 26–29 years. On control Day 1, each subject received cimetidine 300 mg i.v., and serum and urine samples were obtained. Each subject was initiated on cimetidine 600 mg b.i.d. orally for 2 weeks. There were 3 further study days repeated after 1 and 2 weeks of cimetidine dosing and 1 week after stopping cimetidine. There was no significant difference in the mean total body clearance of cimetidine among the 4 study days. Mean elimination t1/2β and Vβ were similarly unchanged. However mean renal clearance (CLR) and fe were significantly increased following 2 weeks of drug dosing (CLR 5.41 ml·min−1 kg−1; fe 0.61) compared to control (CLR 4.00 ml·min−1·kg−1; fe 0.48). Although the non renal clearance was reduced from control values of 4.29 to 3.51 ml·min−1·kg−1 following 2 weeks of dosing the difference was not significant. Dosage adjustment of cimetidine appears unnecessary after short-term dosing in the presence of normal renal function.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00608228
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