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  • Articles  (9)
  • pharmacodynamics  (9)
  • Springer  (9)
  • 2015-2019
  • 2005-2009
  • 1980-1984  (9)
  • Medicine  (9)
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  • Articles  (9)
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  • Springer  (9)
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  • 1
    Electronic Resource
    Electronic Resource
    Lack of effect of astemizole on ethanol dynamics or kinetics (1983)
    Springer
    European journal of clinical pharmacology 25 (1983), S. 567-568 
    Details
    ISSN: 1432-1041
    Keywords: astemizole ; ethanol ; antihistamine ; pharmacodynamics ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effects of astemizole (10 mg daily for 7 days) on the kinetics and CNS depressant activity of ethanol have been examined in a double-blind cross-over study agonist placebo in 7 volunteers. There was no significant change in the elimination rate or AUC of the plasma ethanol concentration-time curve after astemizole. Central nervous system effects of ethanol as monitored by visual analogues of sedation, visual discrimination, pursuit rotor and reaction time were also unaffected by astemizole pretreatment.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542130
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  • 2
    Electronic Resource
    Electronic Resource
    Pharmacokinetic and pharmacodynamic study of the combination of furosemide retard and triamterene (1984)
    Springer
    European journal of clinical pharmacology 26 (1984), S. 191-195 
    Details
    ISSN: 1432-1041
    Keywords: furosemide ; triamterene ; drug combination ; pharmacodynamics ; pharmacokinetics ; furosemide retard ; triamterene metabolite ; urine potassium
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacodynamics and pharmacokinetics of the combination of furosemide retard (30 mg)/triamterene (50 mg) were compared with furosemide (30 mg) in 18 healthy male volunteers aged 39.3±6.3 years. After the administration of furosemide the onset of its effect was very rapid, reaching a maximum between 1.5 to 3 h, and followed by rebound after 9 to 10.5 h. In contrast the combination furosemide retard/triamterene showed a protracted course with a duration of effect up to 12 h. The general effect over 12 h of the two preparations was equivalent with respect to the excretion of urine, sodium, chloride and calcium, but the combination caused significantly less excretion of potassium (p≤0.05) than furosemide. After a lag-phase of 33.9±5.4 min the maximum plasma concentration of furosemide was reached after 3.47±0.66 h, and the elimination half-life was approximately 2 h. After a lag-phase of 33.0±17.8 min the maximum plasma concentration of the main metabolite of triamterene, the OH-TA sulphuric acid ester, was reached after 1.7±0.59 h, and its elimination half-life amounted to 1.25±0.37 h. Because of the sustained release of furosemide from the retard-formulation, its principal pharmacokinetic parameters were better adapted to those of triamterene. The consequences were not only a protracted effect but also an improved electrolyte profile, especially with regard to reduced loss of potassium. In the case of renal insufficiency, however, the potassium level in serum might be increased to an undesirable extent.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00630285
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  • 3
    Electronic Resource
    Electronic Resource
    Clinical pharmacology of etintidine in patients with duodenal ulcer (1982)
    Springer
    European journal of clinical pharmacology 23 (1982), S. 495-500 
    Details
    ISSN: 1432-1041
    Keywords: cimetidine ; etintidine ; duodenal ulcer ; histamine H2 antagonist ; gastric acidity ; pharmacodynamics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The gastric antisecretory activity of etintidine, a new histamine H2-receptor antagonist, was evaluated in 5 patients with quiescent duodenal ulcer disease. Meal-stimulated acid secretion was measured after 100 and 300 mg oral doses of etintidine, 100 and 300 mg oral doses of cimetidine, and placebo. Reductions from placebo in four-hour gastric acid secretion were 49, 65, 80, and 94%, with 100 mg cimetidine, 100 mg etintidine, 300 mg cimetidine, and 300 mg etintidine, respectively. Drug concentrations in plasma were determined by HPLC. The pharmacokinetics of the 2 drugs were similar. We analyzed sigmoid-shaped concentration-response curves to both agents; the concentrations causing 50% inhibition of meal-stimulated gastric acid secretion were 0.44±0.04 and 0.15±0.04 µg/ml for cimetidine and etintidine, respectively. However, characteristics of these curves were such that the potency difference diminished at higher concentrations.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00637495
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  • 4
    Electronic Resource
    Electronic Resource
    Relationships between several pharmacokinetic parameters and psychometric indices of subjective effects of Δ9-tetrahydrocannabinol in man (1983)
    Springer
    European journal of clinical pharmacology 25 (1983), S. 633-637 
    Details
    ISSN: 1432-1041
    Keywords: delta-9-tetrahydrocannabinol ; mood ratings ; pharmacodynamics ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary This study explored the relationships in man between various pharmacological effect of Δ9-tetrahydrocannabinol (THC), plasma THC concentration, and pharmacokinetic parameters of THC. Three male and three female experienced marihuana users smoked two standard marihuana cigarettes. The relationships between heart rate, subjective “high” rating, Linear Mood Scale factors, and plasma THC concentration were assessed. Significant correlations were observed between various Linear Mood Scale factors and pharmacokinetic parameters reflecting the magnitude of drug intake and the degree of temporal dissociation between the time courses of plasma THC concentration and pharmacological effects (tachycardiac effect, “high”). In particular, the disturbed/weird and sensitive/aware mood factors correlated positively with pharmacokinetic measures of drug intake and time lag to effect. A more reliable index of intoxication with THC may be provided by the global subjective “high” rating, rather than other ratings more specific for particular moods.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542351
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  • 5
    Electronic Resource
    Electronic Resource
    Disposition of intravenous diazepam in young men and women (1981)
    Springer
    European journal of clinical pharmacology 20 (1981), S. 207-213 
    Details
    ISSN: 1432-1041
    Keywords: diazepam ; benzodiazepines ; N-desmethyldiazepam ; plasma ; saliva ; pharmacokinetics ; pharmacodynamics ; psychomotor ; impairment ; oral contraceptives
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The disposition of a single intravenous dose of diazepam (10 mg) was studied in 11 young, healthy subjects (6 males and 5 females on oral contraceptives). Plasma samples were obtained over 28 days and diazepam and N-desmethyldiazepam plasma concentrations and diazepam free fractions were determined. The salivary excretion of diazepam and N-desmethyldiazepam was studied over 72 h. A series of psychomotor performance tests were administered over the first 8 h. Interindividual variation in mean diazepam disposition over time is not principally related to variation in plasma protein binding; 93% of the variation in clearance is accounted for by variation in intrinsic clearance. Interindividual variation in diazepam disposition is modest but the plasma clearance of diazepam in women on oral contraceptives (median 14.0 ml/min) is significantly (p=0.004) less than in men (median 23.4 ml/min) and the area under the curve (AUC) of diazepam is highly correlated with the AUC of the principal active metabolite (r=0.90, p〈0.001). The AUC of N-desmethyldiazepam (median 9.2 µg·h/ml) in women is greater (p=0.06) than in men (median 7.5 µg·h/ml). On chronic administration of diazepam, therefore, women taking oral contraceptives will have greater plasma concentrations per unit dose of both diazepam and N-desmethyldiazepam than men. The clearance of diazepam in control groups of 11 young men (median 23.8 ml/min) and 10 young women not taking oral contraceptives (median 26.8 ml/min) is not significantly different. Plasma and salivary concentratrions of diazepam are correlated (p〈0.001) but the predictive value of this correlation is limited (r=0.70) since the ratio of salivary to plasma concentrations varies significantly over the day. The use of calculated free diazepam plasma concentrations does not improve the correlation (r=0.68) but the slope of this regression (1.00) is that predicted by theory.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00544599
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  • 6
    Electronic Resource
    Electronic Resource
    Analytical model of some pharmacokinetic and pharmacodynamic properties of fazadinium in man (1983)
    Springer
    European journal of clinical pharmacology 24 (1983), S. 407-413 
    Details
    ISSN: 1432-1041
    Keywords: neuromuscular blockade ; fazadinium ; pharmacokinetics ; pharmacodynamics ; predictive model ; receptor occupation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The neuromuscular blocking characteristics and plasma concentration decay of fazadinium bromide, a short acting, non-depolarizing muscular relaxant, were simultaneously observed under standardised conditions in 6 healthy, anaesthetized, adult patients. The results were analyzed by a new pharmacodynamic model, which takes into account certain relationships describing the binding of non-depolarizing neuromuscular blocking agents and the postsynaptic receptor occupation ratio. According to the simulations performed, the pharmacodynamic parameters determined: KB-apparent value of equilibrium constant of fazadinium — receptors exchange (mean ± SEM) 0.404+0.045 µmol/l, and the value of postsynaptic occupation ratio for 50% paralysis of 0.89±0.004 were in agreement with values reported in the literature for mammalian neuromuscular junctions in vitro. The apparent validity of the pharmacodynamic model and its value in simulating dose/effect relationships of non-depolarizing neuromuscular blocking agents are discussed and illustrated.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00610063
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  • 7
    Electronic Resource
    Electronic Resource
    Comparison of the effects of muzolimine and furosemide in patients with end-stage renal failure on chronic dialysis (1981)
    Springer
    European journal of clinical pharmacology 20 (1981), S. 23-26 
    Details
    ISSN: 1432-1041
    Keywords: muzolimine ; furosemide ; renal failure ; pharmacodynamics ; haemodialysis ; diuretics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacodynamic effects of muzolimine and furosemide were compared in a single dose cross-over study in 8 patients on regular dialysis treatment, who had a residual diuresis of more than 300 ml/day. The study periods comprised two dialysis-free intervals of 3 days. On the second dialysis-free day either muzolimine 240 mg or furosemide 240 mg was administered orally. Urine was collected in 12-h periods on the pre-treatment, treatment and post-treatment days, and the excretion of sodium, potassium, urea and creatinine were measured. After administration of muzolimine 240 mg urine volume rose to twice that of the previous day, and sodium excretion increased approximately threefold. In contrast, the effect of furosemide 240 mg was not as pronounced; the diuresis was only 1.6 times that on the previous day and natriuresis was only 2.2 times as large. Excretion of potassium and creatinine was only slightly increased by either substance. The elimination of urea was increased by both substances to the same degree as the corresponding increase in diuresis.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00554662
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  • 8
    Electronic Resource
    Electronic Resource
    Pharmacodynamic studies on mianserin and its interaction with clonidine (1981)
    Springer
    European journal of clinical pharmacology 21 (1981), S. 97-102 
    Details
    ISSN: 1432-1041
    Keywords: mianserin ; clonidine ; pharmacodynamics ; interaction ; alpha2-receptors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary There is evidence that clonidine's hypotensive effect is reduced by the concurrent administration of tricyclic antidepressants. It has been proposed that this results from an interaction at α2-receptors in the brain stem where clonidine acts as a relatively selective agonist and the tricyclic antidepressants as antagonists. Mianserin is an antidepressant with a tetracyclic structure and, although it has been reported to cause less cardiovascular disturbance, there is evidence that it also has α-adrenoceptor blocking effects. This study in 6 normotensive healthy male volunteers was designed to investigate a possible interaction between clonidine and the antidepressant mianserin. Administration of the first dose of 20 mg mianserin was associated with acute cardiovascular effects, notably transient postural hypotension, but no significant disturbance of heart rate or blood pressure was detected after 3 days continuous treatment with mianserin 20 mg tid. Following pre-treatment with mianserin or placebo the responses to a single oral dose of 300 µg clonidine were then assessed. The combination of mianserin and clonidine was not associated with any attenuation of clonidine's hypotensive effect, erect or supine, but there was significant attenuation of clonidine's supine bradycardic effect. There was no evidence that mianserin interfered with the ability of clonidine to diminish salivary flow, cause sedation, and reduce catecholamine output, but it was noted that mianserin itself had a very pronounced sedative effect. Mianserin alone had no significant effect on salivary flow. This short term study demonstrates that mianserin does not significantly interfere with the responses to a single oral dose of clonidine.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00637508
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  • 9
    Electronic Resource
    Electronic Resource
    Intravenous and oral administration of molsidomine, a pharmacodynamic and pharmacokinetic study (1984)
    Springer
    European journal of clinical pharmacology 27 (1984), S. 203-208 
    Details
    ISSN: 1432-1041
    Keywords: molsidomine ; vasodilators ; pharmacokinetics ; pharmacodynamics ; dose-response relationship ; haemodynamics ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In 12 healthy male volunteers, molsidomine 1, 2 and 4 mg i.v. increased resting heart rate and decreased systolic blood pressure, the latter still being affected after 8 hours. After single oral doses of 1 and 2 mg, systolic pressure tended to be reduced for 90 minutes and exercise heart rate tended to be increased. After oral treatment with 2 mg molsidomine three times daily for 1 week, the pharmacokinetic parameters and the effects on heart rate and blood pressure after the final dose were not different from those after the first dose. The terminal half-life was independent of dose and route of administration. Clearance and distribution volume were not dose-dependent. The bioavailability of a 2 mg oral dose of molsidomine was 44%. Inter-individual variation in heart rate, blood pressure and pharmacokinetics was observed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00544046
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