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  • pharmacokinetics  (19)
  • Springer  (19)
  • Oxford University Press
  • 1980-1984  (19)
  • 1981  (19)
Collection
Keywords
Publisher
  • Springer  (19)
  • Oxford University Press
Years
  • 1980-1984  (19)
Year
  • 1
    Electronic Resource
    Electronic Resource
    Clinical pharmacokinetics of chlordiazepoxide in patients with alcoholic hepatitis (1981)
    Springer
    European journal of clinical pharmacology 19 (1981), S. 279-285 
    Details
    ISSN: 1432-1041
    Keywords: chlordiazepoxide ; alcoholic liver disease ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The clearance of chlordiazepoxide from the systemic circulation was studied in 20 subjects which included 15 patients with alcoholic hepatitis and 5 normal volunteers. The half-life for the appearance of the drug in the systemic circulation was found to increase exponentially with age (r=0.73, P〈0.0005) and was independent of the presence of alcoholic hepatitis. The metabolic clearance of chlordiazepoxide was significantly lower in the patients than in the normal subjects (7.6 compared to 13.8 ml/kg-h, P〈0.005). Linear regression analysis revealed a significant correlation between clearance and albumin (r=0.77, P〈0.00005). However, the predictive value of this relationship was shown to be minimal. Multiple regression analysis produced only a slight improvement in the correlation when both albumin and lactate dehydrogenase were used as variables (r=0.83, P〈0.00005). In six of the patients, a second clearance study was conducted three weeks following their initial one. All repeat subjects showed improvement both clinically and as reflected by their laboratory tests for liver injury, but there was not a significant change in their clearance of chlordiazepoxide. Multiple regression analysis of the clearance data on the initial and repeat subjects showed a significant correlation between clearance and the variables age, albumin, and lactate dehydrogenase (r=0.91, P〈0.0025). This relationship suggests that over a short period of time (where age can be considered constant) changes in albumin and lactate dehydrogenase could be potentially useful in predicting clearance changes in a single individual.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00562805
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  • 2
    Electronic Resource
    Electronic Resource
    Clinical pharmacokinetics and pharmacodynamics of fazadinium in renal failure (1981)
    Springer
    European journal of clinical pharmacology 20 (1981), S. 293-298 
    Details
    ISSN: 1432-1041
    Keywords: neuromuscular relaxants ; fazadinium ; pharmacokinetics ; renal failure ; neuromuscular transmission
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetic behaviour and neuromuscular blockade produced by the administration of fazadinium bromide at a dose of 1 mg/kg have been studied in seven patients with end-stage renal failure. No significant differences were found in the pharmacokinetic or pharmacodynamic properties when compared with patients with normal renal function. It is suggested that fazadinium may be superior to either d-tubocurarine or pancuronium in providing muscle relaxation for patients with renal failure.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00618780
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  • 3
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of intravenous and oral tolmesoxide (1981)
    Springer
    European journal of clinical pharmacology 19 (1981), S. 119-125 
    Details
    ISSN: 1432-1041
    Keywords: tolmesoxide ; metabolite ; volunteers ; pharmacokinetics ; intravenous ; oral ; protein binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A high pressure liquid chromatographic assay was developed for simultaneous measurement of the plasma levels of tolmesoxide and its principal metabolite, RX71112. The assay was used to study the disposition of intravenous and oral tolmesoxide in ten normotensive subjects. Two exponential terms were required to describe the disposition of the drug following intravenous administration, whilst a single exponential term sufficied to account for the decay in the plasma concentration after oral administration. The bioavailability of oral tolmesoxide from capsules averaged 84.5% and was independent of dose. The mean half-life after i. v. dosing was 2.6 h (±0.3 SEM) compared to values of 1.9 h (±0.1 SEM) and 2.7 h (±0.5 SEM) following 200 and 400 mg oral doses respectively. In all subjects RX71112 appeared in plasma shortly after tolmesoxide following both routes of administration. The terminal half-life of the metabolite was significantly longer than tolmesoxide with a mean value of 4.9 h (±0.9 SEM) following the 200 mg oral dose of tolmesoxide. The binding of tolmesoxide and RX71112 at therapeutic plasma concentration was 36.8% (±0.5 SEM) and 58.5% (±0.3 SEM) and this remained unchanged at higher concentrations.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00568398
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  • 4
    Electronic Resource
    Electronic Resource
    Plasma mexiletine concentrations following combined oral and intramuscular administration (1981)
    Springer
    European journal of clinical pharmacology 19 (1981), S. 301-304 
    Details
    ISSN: 1432-1041
    Keywords: mexiletine ; intramuscular injection ; oral administration ; intravenous injection ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Mexiletine in doses of 50, 100 and 400 mg was administered by intramuscular injection to a healthy subject and the resulting plasma concentrations were compared with those after 100 mg given intravenously. The bioavailability of mexiletine given by this route is complete and the kinetics are linear with dose. Plasma mexiletine concentrations resulting from 200 mg given orally with either two 4-ml intramuscular injections each containing 100 mg (Mexitil® — for intravenous use) or one 2-ml intramuscular injection of an experimental preparation containing 200 mg were compared in 3 and 6 normal subjects respectively. Plasma levels within the therapeutic range of 0.75–2 µg/ml were attained at mean times of 28.7 and 42.5 min respectively. Apart from raised plasma creatine phosphokinase levels (as would be expected following an intramuscular injection) the tolerability of intramuscular mexiletine injections was satisfactory. Further studies in patients will be required to determine whether the combined oral and intramuscular administration of mexiletine is of value in acute myocardial infarction.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00562808
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  • 5
    Electronic Resource
    Electronic Resource
    The influence of food on the absorption of diclofenac after single and multiple oral doses (1981)
    Springer
    European journal of clinical pharmacology 19 (1981), S. 33-37 
    Details
    ISSN: 1432-1041
    Keywords: diclofenac sodium ; enteric-coating ; food ; absorption ; plasma levels ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A single dose of enteric-coated diclofenac sodium was taken fasting and immediately after a standard breakfast by twelve healthy volunteers. A considerable delay in the onset of absorption was observed, non-fasting, varying from 2.5 to 12 h compared with 1.5 to 2.75 h when fasting. Peak plasma concentrations were reduced after food but areas under plasma concentration-time curves were comparable. Six subjects then took part in a study involving single and repeated dosing under fasting and non-fasting conditions. As before, prolonged and variable delays were observed when the enteric-coated tablets were taken after food. On repeated dosing, maximum plasma concentrations were reached after 6 h non-fasting compared with 2.5 h fasting. Peak plasma levels were, however, similar.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00558380
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  • 6
    Electronic Resource
    Electronic Resource
    A comparison of the pharmacokinetics of theophylline in asthmatic children in the acute episode and in remission (1981)
    Springer
    European journal of clinical pharmacology 20 (1981), S. 443-447 
    Details
    ISSN: 1432-1041
    Keywords: theophylline ; asthma ; children ; acute episode ; remission ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of theophylline following a single intravenous dose of aminophylline were determined in 8 asthmatic patients in each of the acute, the recovery and the remission phases. The overall results for mean plasma theophylline clearance (78.6±33.3 ml/kg/h), plasma theophylline half-life (4.14±1.36 h) and apparent volume of distribution (0.41±0.066 l/kg) are in accordance with previously published values. There was no general statistically significant difference in any of the pharmacokinetic parameters when results from the acute and remission phases were compared. However, certain patients showed reductions in plasma theophylline clearance in the acute phase of the illness such that a dosage regimen standardised during remission may cause toxicity if continued in the acute episode. It is suggested that monitoring the plasma theophylline levels is desirable in all patients in the acute episode.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542097
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  • 7
    Electronic Resource
    Electronic Resource
    Single-dose pharmacokinetics of metoclopramide (1981)
    Springer
    European journal of clinical pharmacology 20 (1981), S. 465-471 
    Details
    ISSN: 1432-1041
    Keywords: metoclopramide ; pharmacokinetics ; bioavailability ; first-pass effect
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The time courses of plasma metoclopramide concentrations were followed in six subjects after oral and intravenous single dose administration. Plasma concentration-time data following i.v. administration in each subject were found to fit a two compartment model with a mean terminal half-life of 4.55 h±0.80 h and a mean distribution half-time of 0.35 h±0.09 h. Volumes of distribution were high (3.43±1.181 · kg−1), and clearances (0.53±0.191 · kg−1h−1) approached liver plasma flow. This suggests that metoclopramide occurs at higher concentrations in tissues than in plasma, and that its clearance is probably limited by liver blood flow rather than liver metabolic capacity. The post-absorption decline in metoclopramide plasma levels after oral administration was also biexponential in each subject. The terminal half-life was 5.17 h±0.98 h. Mean volume of distribution and mean clearance were similar to intravenous values (after adjustment for bioavailability). Oral absorption was rapid with peak plasma concentrations being reached at a mean time of 0.93 h. A mean bioavailability of 0.77 was calculated for the six subjects, and it was postulated that this incomplete availability is due to a first-pass effect. The inter-individual variation in the degree of ‘first-pass’ was considerable (0.47–1.14).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542101
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  • 8
    Electronic Resource
    Electronic Resource
    Pharmacokinetic study of chloramphenicol in patients with liver disease (1981)
    Springer
    European journal of clinical pharmacology 20 (1981), S. 479-483 
    Details
    ISSN: 1432-1041
    Keywords: chloramphenicol ; liver disease ; pharmacokinetics ; intravenous administration ; serum albumin ; prothrombin time index
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of intravenous chloramphenicol has been studied in 42 patients with liver disease and in 8 controls. The half-life of chloramphenicol (t1/2) was increased in the various liver disorders, the metabolic clearance rate (MCR) and apparent volume of distribution (Vd) were decreased and the area under the time — concentration curve (AUC) showed an increase. The t1/2 of chloramphenicol showed a significant correlation with serum albumin and prothrombin time index.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542103
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  • 9
    Electronic Resource
    Electronic Resource
    Proof of the linearity of the pharmacokinetics of alinidine in man (1981)
    Springer
    European journal of clinical pharmacology 21 (1981), S. 201-207 
    Details
    ISSN: 1432-1041
    Keywords: alinidine ; pharmacokinetics ; radioimmunoassay ; computer model
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of alinidine was investigated in two groups of volunteers: Group I (N=5) received on two different occasions single doses of14C-labelled drug given orally (40 mg) or intravenously (10 mg); Group II (N=6) received single oral doses 10, 30 or 90 mg dissolved in 20 ml water. The samples from Group I were analysed by two different and independent methods (RIA and counting total radioactivity). The results obtained by the two methods were identical, since the compound was not metabolized. The plasma concentrations and renal excretion data obtained from both groups were individually fitted to an open three compartment model. Independent of the route of administration and of the doses given, similar pharmacokinetic parameters were calculated for each group and each trial. The half lives of the distribution and elimination phases were t1/2α: 36–41 s, t1/2β : 9.9–11.1 min and t1/2γ: 2.7–3.8 h. There was a linear relationship between the dose administered and the resulting areas under the plasma concentration curves (AUC). Following a lag period (τ=0.19–0.22 h), the peak plasma concentration was reached 0.6–1.2 h after oral administration. Oral alinidine was 100% bioavailable.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00627921
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  • 10
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of N-desmethyldiazepam after a single oral dose of clorazepate: The effect of smoking (1981)
    Springer
    European journal of clinical pharmacology 21 (1981), S. 229-233 
    Details
    ISSN: 1432-1041
    Keywords: benzodiazepines ; clorazepate ; dipotassium clorazepate ; N-desmethyldiazepam ; pharmacokinetics ; smoking
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of N-desmethyl-diazepam was evaluated after oral administration of clorazepate 20 mg to 12 healthy male volunteers (6 smokers; 6 non-smokers), aged 23–29 years. Plasma levels of desmethyldiazepam were measured by gas liquid chromatography. The half life of elimination (t1/2β) was significantly longer in the non-smoking volunteers than in the smokers: 54.7±17.7 versus 29.8±9.9 h (p〈0.05). Peak plasma concentrations (Cmax) were higher in non-smokers than in smokers, 413±106 µg/l and 245±50 µg/l, respectively (p〈0.05). The sedative effect of clorazepate was less severe in smokers than in non-smokers.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00627925
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