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  • pharmacokinetics  (19)
  • Autoradiography  (4)
  • Springer  (23)
  • Oxford University Press
  • 1980-1984  (23)
  • 1981  (23)
Collection
Keywords
Publisher
  • Springer  (23)
  • Oxford University Press
Years
  • 1980-1984  (23)
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
    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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  • 3
    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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  • 4
    Electronic Resource
    Electronic Resource
    Histochemical, cytochemical and autoradiographic studies on the rostellum ofHymenolepis diminuta (1981)
    Springer
    Parasitology research 64 (1981), S. 335-345 
    Details
    ISSN: 1432-1955
    Keywords: Hymenolepis diminuta ; Autoradiography ; Ultracytochemistry ; Histochemistry
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract Histochemical studies on the rostellum ofHymenolepis diminuta revealed diastase-stable, protein/neutral carbohydrate-rich material localized in the rostellum tegument. The remainder of the rostellum, primarily composed of the glycogen-rich myocytons of the rostellum musculature, is protein-poor, but rich in diastase-labile, neutral and acidic carbohydrates. Ultrastructural cytochemical studies, using the periodic acid-thiocarbohydrazideosmium (PATCO) technique, indicated that the granules of the rostellar tegumental cytons and distal cytoplasm are carbohydrate-rich. Lipids are present in the rostellar myocytons but not in the tegumental cytons. Autoradiography using a pulse-labeling with [3H]leucine revealed an apical translocation of tegumental granules, but at a slower rate than had been reported for the strobilar tegument of the same organism. Neither [3H]galactose nor [3H]glucose were incorporated into the rostellar tegumental granules. The function of the secretory glycoprotein(s) produced in the rostellar tegument and its (their) possible role in the regulation of maturation and/or strobilization remain enigmatic.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00927380
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  • 5
    Electronic Resource
    Electronic Resource
    Synthesis of the intranuclear crystals in Scolopendrium vulgare (L.) SM (1981)
    Springer
    Planta 152 (1981), S. 137-144 
    Details
    ISSN: 1432-2048
    Keywords: Autoradiography ; Intranuclear crystals ; Nucleus, crystolo-Protein transfer-Pteridophytes ; Scolopendrium
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract Proteinaceous intranuclear crystals are found in the fern Scolopendrium vulgare. During mitosis these crystals are eliminated from the nucleus into the cytoplasm, where they are dissolved. New crystals appear in the nucleus. The site of synthesis of intranuclear crystal proteins was investigated using quantitative ultrastructural autoradiography after incubation with tritiated lysine. The results suggest a migration of cytoplasmic proteins to the nucleus, part of which would then be incorporated into the intranuclear crystals.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00391185
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  • 6
    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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  • 7
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of parenteral paracetamol and its analgesic effects in post-operative dental pain (1981)
    Springer
    European journal of clinical pharmacology 20 (1981), S. 215-218 
    Details
    ISSN: 1432-1041
    Keywords: paracetamol ; acetaminophen ; dental pain ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A double-blind, randomised, crossover trial was undertaken to compare the analgesic effects of a single dose of paracetamol (1000 mg i. v.) with placebo in the immediate post-operative period following removal of impacted lower third molars. There was no significant difference in the pain relief between paracetamol and placebo in the first hour following injection. Thereafter, there was significantly less pain (P〈0.05) after treatment with paracetamol than after placebo. Plasma concentrations of paracetamol were measured and pharmacokinetic variables were determined. Over the four hour period of investigation there was no clear relationship between analgesia and paracetamol concentration in either central or peripheral compartments.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00544600
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  • 8
    Electronic Resource
    Electronic Resource
    Plasma and salivary pharmacokinetics of caffeine in man (1981)
    Springer
    European journal of clinical pharmacology 21 (1981), S. 45-52 
    Details
    ISSN: 1432-1041
    Keywords: caffeine ; pharmacokinetics ; plasma ; saliva ; urinary elimination
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma and salivary caffeine concentrations were measured by gas-liquid chromatography in 6 healthy caffeine-free volunteers following oral administration of 50, 300, 500 and 750 mg caffeine. Caffeine was also given to a single subject intravenously in doses of 300, 500 and 750 mg. Caffeine was rapidly absorbed and was completely available at all doses. The apparent first-order elimination rate constant decreased linearly with dose and was 0.163±0.081 h−1 for 50 mg and 0.098±0.027 h−1 for 750 mg. The total body clearance was unaffected by dose and was 0.98±0.38 ml/min/kg. There was a trend towards increasing apparent volume of distribution with increasing dose. A linear relationship existed between the area under the plasma concentration, time curve and dose and dose-normalised plasma concentration, time plots were superimposable. These findings suggest that caffeine obeys linear pharmacokinetics over the dose range investigated. Despite significant inter-individual differences in pharmacokinetic parameters there was good reproducibility within 5 subjects given 300 mg caffeine orally on 3 occasions. Salivary caffeine levels probably reflect the unbound plasma caffeine concentration and can be used to estimate the pharmacokinetic parameters of the drug. Overall the saliva/plasma concentration ratio was 0.74±0.08 but within subjects some time-dependence of the ratio was found with higher ratios initially (even after intravenous administration) and lower ratios at longer time intervals after the dose. Urinary elimination of caffeine was low and independent of dose: 1.83% of the dose was eliminated unchanged.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00609587
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  • 9
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of bupropion, a novel antidepressant agent, following oral administration to healthy subjects (1981)
    Springer
    European journal of clinical pharmacology 21 (1981), S. 127-135 
    Details
    ISSN: 1432-1041
    Keywords: antidepressant ; bupropion ; pharmacokinetics ; oral administration ; radioimmunoassay ; urinary excretion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of bupropion hydrochloride, a structurally novel antidepressant agent, have been studied in healthy male and female subjects following administration of single oral doses of 50, 100 and 200 mg. Plasma drug concentrations were determined directly by a specific radioimmunoassay (r. i. a.), while urinary measurements required a prior solvent extraction to remove substances interfering in the assay. Bupropion appeared rapidly in the plasma, suggesting good absorption. Drug plasma concentration-time data were fitted well to a two-compartment open model of drug disposition by use of the computer program NONLIN. By comparison of AUC, Cmax and tmax values, the pharmacokinetics of bupropion were found to be linear across the 50–200 mg dose range in both sexes. When the data were normalized for subjects' body weights, no differences between pharmacokinetic parameters for male and female subjects were found. Mean disposition half-lives across treatments were 1.2–1.4 h for t1 2α and 10.7–13.8 h for the t1 2β. Bupropion was extensively bound (85%) to human plasma proteins over a wide drug concentration range. Less than 1% of a 200 mg oral dose of bupropion hydrochloride appeared in the urine of 16 subjects as unchanged drug, indicating extensive metabolism of the parent compound.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00637513
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  • 10
    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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