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  • Articles  (578)
  • Articles: DFG German National Licenses  (578)
  • Chemistry  (530)
  • Physics  (23)
  • pharmacokinetics  (16)
  • Noctuidae  (9)
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  • Articles  (578)
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  • 11
    Electronic Resource
    Electronic Resource
    The disposition kinetics of diazepam in pregnant women at parturition (1978)
    Springer
    European journal of clinical pharmacology 13 (1978), S. 275-284 
    Details
    ISSN: 1432-1041
    Keywords: Diazepam ; pharmacokinetics ; pregnant women ; plasma clearance ; blood/plasma concentration ratio ; placental transfer
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The disposition of diazepam has been studied in pregnant women at parturition. The plasma concentration of diazepam was monitored for at least 3 days in 18 women who received a single intravenous injection of 10 mg during the 10 h-period prior to delivery. Fourteen mothers had uneventful puerperia (Group I) and in 13 of these cases there was a pronounced postnatal increase in the plasma concentration of diazepam. The terminal phase half-life (t1/2) was significantly greater for Group I (mean = 65 h; range = 24–114 h) than for age-matched non-pregnant patients (mean = 29 h; range = 18–44 h from literature). The prolonged t1/2 appeared to be related to changes in the distribution of diazepam and not to a reduction in hepatic elimination since the total plasma clearance (Cltp) in these 14 pregnant patients (mean = 28 ml/min; range = 18–43 ml/min) was not reduced compared to that reported for non-pregnant controls (mean = 30 ml/min; range = 22–45 ml/min). Four mothers underwent postnatal surgery for tubal ligation (Group II) and the plasma concentration-time profiles for this group did not show the same postnatal phenomenon as did the profiles obtained for Group I. The t1/2 for Group II was shorter (mean = 31 h; range = 24–37 h) than for Group I and similar to that for the non-pregnant controls. The Cltp for Group II was greater (mean = 56 ml/min; range = 48–63 ml/min) than for both Group I and non-pregnant controls. These results suggest that delivery alters the disposition of diazepam and is generally associated with a postnatal re-distribution of diazepam into the systemic circulation. The blood/plasma concentration ratio was determined in 9 patients (mean = 0.62; range = 0.54–0.77). There was no difference in the total blood clearance between the pregnant patients of Group I and the non-pregnant controls. In most cases the umbilical venous plasma concentration (Cpuv) of diazepam was greater than the peripheral maternal venous plasma concentration (Cpmv) at delivery. The foetus appears to constitute a slowly equilibrating tissue-group in which diazepam does not reach equilibrium with the maternal systemic circulation for at least 5–10 h at which time the diazepam concentration in maternal and foetal plasma is similar.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00716363
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  • 12
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of betamethasone in healthy adults after intravenous administration (1983)
    Springer
    European journal of clinical pharmacology 25 (1983), S. 643-650 
    Details
    ISSN: 1432-1041
    Keywords: betamethasone ; pharmacokinetics ; cortisol ; high-performance liquid chromatography
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of betamethasone and its phosphate ester are described in 8 healthy adults after i. v. bolus injection of 10.6 mg betamethasone phosphate. Both compounds were measured by high-performance liquid chromatography with ultraviolet detection using sample handling methods which prevented hydrolysis of the ester in vitro. Betamethasone phosphate disappeared rapidly from plasma (mean half-life=4.7 min) as betamethasone levels rose. Betamethasone plasma levels reached a peak 10–36 min after administration of the phosphate before declining in a biexponential manner. The terminal slow disposition phase had a mean half-life of 6.5 h. Only about 5% of the dose was recovered from urine as betamethasone, indicating extensive extrarenal clearance of betamethasone. Protein binding and blood/plasma concentration ratio were also determined. In comparison with its stereoisomer, dexamethasone, betamethasone is also cleared mainly by metabolism but has a lower plasma clearance, is less plasma bound, has a higher blood/plasma concentration ratio, and a higher volume of distribution. Endogenous cortisol levels were measured in the subjects who received betamethasone phosphate and in a matched control group of 4 subjects who did not. Betamethasone abolished the normal episodic secretion of cortisol and rapidly reduced its plasma concentration to a basal level. Cortisol plasma levels were not restored at 24 h but had returned to normal by 48 h after dosing.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542353
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  • 13
    Electronic Resource
    Electronic Resource
    Papaverine disposition in cardiac surgery patients and the effect of cardiopulmonary bypass (1984)
    Springer
    European journal of clinical pharmacology 27 (1984), S. 127-130 
    Details
    ISSN: 1432-1041
    Keywords: papaverine ; cardiopulmonary bypass ; pharmacokinetics ; cardiac surgery patients
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Cardiac surgery involving cardiopulmonary bypass (CPB) causes substantial physiologic changes which may potentially alter the pharmacokinetic properties of drugs used during and after the procedure. Studies with fentanyl have implied a relationship between prolonged elimination half-lives following CPB and decreased liver perfusion during and after the procedure. To further test this hypothesis, the effects of CPB on the pharmacokinetics of papaverine, a coronary vasodilator currently being added to the cardioplegic solution to prevent vasospasm, were studied. The drug was given to two groups of patients, one (n=6) undergoing surgery with and one (n=5) without CPB, the latter serving as controls. Plasma papaverine concentrations declined biexponentially in the control patients with a mean elimination half-life of 1.30±0.25 h, total plasma clearance of 13.8±3.75 ml/min/kg, volume of distribution of 1.52±0.45 l/kg and volume of distribution, steady-state, of 0.992±0.530 l/kg. For the CPB group, only half-life was estimated, and averaged 2.77±0.28 h, significantly greater (p〈0.01) than that in the controls. These results further confirm the increased half-lives seen with other hepatically cleared drugs following CPB and have implications in the clinical management of patients given drugs eliminated in this manner.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00544033
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  • 14
    Electronic Resource
    Electronic Resource
    Application of a radioreceptor assay in a pharmacokinetic study of oxitropium bromide in healthy volunteers after single i.v., oral and inhalation doses (1989)
    Springer
    European journal of clinical pharmacology 37 (1989), S. 507-512 
    Details
    ISSN: 1432-1041
    Keywords: oxitropium bromide ; pharmacokinetics ; radioreceptor assay ; side-effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Oxitropium bromide (OXBR) is a new anticholinergic drug, which is expected to be useful in the treatment of nocturnal asthma. The only pharmacokinetic data were obtained with the14C-labelled compound. A sensitive radioreceptor assay for the determination of unlabelled OXBR in plasma was developed, based on competition between OXBR and3H-N-methylscopolamine for binding to muscarinic receptors. OXBR was isolated from plasma by ion-pair extraction and re-extraction. Active metabolites present in significant amounts might interfere in the assay, but this was not the case for OXBR metabolites. Detection limits were 300 pg·ml−1 and 3 ng·ml−1 for plasma and urine, respectively. For the latter no extraction step was required. The single dose pharmacokinetics of OXBR was studied following inhalation (3 mg), oral (2 mg) and i.v. (1 mg) administration to 12 men, following an open, cross-over design. After i.v. administration the kinetic parameters were: Vc 38.4 l; t1/2α 5.3 min; t1/2β 142 min; AUC 8.9 h·ng·ml−1; renal excretion 50.2%, k10 3.5 l·h−1 and total clearance 1874 ml/min. The apparent bioavailabilities were 0.48% and 12.4% by the oral and inhalation routes, respectively, based on the cumulative renal excretion. There were moderate adverse reactions due to the anticholinergic properties of the drug.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00558132
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  • 15
    Electronic Resource
    Electronic Resource
    The excretion of enalapril and enalaprilat in human breast milk (1990)
    Springer
    European journal of clinical pharmacology 38 (1990), S. 99-99 
    Details
    ISSN: 1432-1041
    Keywords: enalapril ; milk ; enalaprilat ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00314815
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  • 16
    Electronic Resource
    Electronic Resource
    Haemodynamic and pharmacokinetic evaluation of alfuzosin in man. A dose ranging study and comparison with prazosin (1989)
    Springer
    European journal of clinical pharmacology 37 (1989), S. 53-58 
    Details
    ISSN: 1432-1041
    Keywords: alfuzosin ; prazosin ; alpha1-adrenoceptor antagonist ; noradrenaline ; pharmacokinetics ; pharmacodynamics ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In an open dose ranging study with random inclusion of placebo, alfuzosin (α1-adrenoceptor antagonist) 1, 2.5 and 5 mg was administered to 6 healthy volunteers, 3 of the volunteers received 10 mg alfuzosin. Supine systolic blood (SBP) pressure was not reduced by alfuzosin although significant increases occurred in supine heart rate (HR) after 2.5 and 5 mg. In the standing position, SBP was reduced at 2 and 4 h with 5 mg alfuzosin; significant increases in HR occurred following 1, 2.5 and 5 mg at 2, 4, 6 and 8 h after administration. Exercise SBP was not reduced; diastolic blood pressure was significantly reduced at 4 and 6 h with 5 mg alfuzosin. More marked effects were seen in the 3 subjects who received 10 mg alfuzosin. After 1 and 5 mg, tmax ranged from 1–2 h; Cmax (4.1 to 20.8 ng · ml−1; AUC (0–24) 20 to 132 ng · ml−1 · h (1 and 5 mg respectively) increased progressively with dose indicating dose dependent kinetics; no significant changes occurred in the visual analogue scale for sedation. A comparison of alfuzosin 5 mg, prazosin 1 mg and placebo each administered for 4 days, indicated that alfuzosin did not significantly reduce standing SBP on either Day 1 or Day 4; prazosin reduced SBP at 2 and 4 h on Day 1 and 6 h on Day 4 compared to placebo. Standing HR was increased by alfuzosin at 2 h on Day 1 and Day 4; increases occurred with prazosin at 2, 4, 6 and 8 h on Day 1 and 6 h on Day 4. Supine plasma noradrenaline increased with alfuzosin and prazosin at 2 and 4 h on Days 1 and 4; the increases were not significantly different. The plasma elimination half-life (t1/2) for alfuzosin was 3.4 h and 3.1 h after acute and chronic administration; (t1/2) for prazosin was 2.6 and 2.9 h. In conclusion alfuzosin causes small reductions in systolic blood pressure, accompanied by a dose dependent increase in heart rate in the supine and standing position and following exercise.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00609425
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  • 17
    Electronic Resource
    Electronic Resource
    Impact of UV radiation on activity of linear furanocoumarins andBacillus thuringiensis var.Kurstaki againstSpodoptera exigua: Implications for tritrophic interactions (1991)
    Springer
    Journal of chemical ecology 17 (1991), S. 973-987 
    Details
    ISSN: 1573-1561
    Keywords: Linear furanocoumarins ; Spodoptera exigua ; Lepidoptera ; Noctuidae ; UV light ; tritrophic interactions ; Bacillus thuringiensis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Abstract Acidic fogs with a pH of 2.0 and duration of 2 hr did not reduce the efficacy ofBacillus thuringiensis var.Kurstaki (Berliner). Therefore, the impact of UV radiation was investigated on the interactions between (1) levels of the antibacterial linear furanocoumarins psoralen, bergapten, and xanthotoxin inApium graveolens (L.) occurring following a 2.0 pH acidic fog episode, (2) the noctuidSpodoptera exigua (Hübner), and (3) a sublethal dosage of the microbial pathogenB. thuringiensis var.Kurstaki. Mean time to pupation in the absence of UV radiation (survival was too low to conduct this analysis for insects exposed to UV) was significantly extended by the addition of either psoralens orB. thuringiensis. Larvae developing on diets containingB. thuringiensis plus psoralens required nearly 40% longer to pupate than controls, but their effects were additive as the interaction was not significant. Although the mean times to adult emergence were significantly different, time spent in the pupal stage did not vary significantly between treatments, indicating that increases in larval developmental time were responsible for the observed decrease in developmental rate. Mean time to mortality, a weighted average time of death, was not significantly affected by any of the treatments. In a 2 × 2 × 2 factorial analysis, all main effects (linear furanocoumarins.B. thuringiensis, UV radiation) reduced survival significantly, as did the three-way interaction. Thus, antagonistic interactions with psoralens that would reduce the effectiveness ofB. thuringiensis in the field were not observed. When pairs of main effects were nested within the two levels (presence and absence) of the third factor, several two-way interactions were found. Interestingly, the activity ofB. thuringiensis and the psoralens, individually or in combination, was enhanced by exposure to UV radiation. Implications of this research are discussed for both natural and agricultural ecosystems.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01395603
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  • 18
    Electronic Resource
    Electronic Resource
    The dynamics of the helix-coil transition in poly-α, L-glutamic acidAn account of this work formed part of a paper delivered at the Fifth International Congress of Biochemistry, Moscow, 1961. (1964)
    New York : Wiley-Blackwell
    Biopolymers 2 (1964), S. 489-500 
    Details
    ISSN: 0006-3525
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Temperature jump measurements employing optical rotation to follow transients show an upper limit of 10μsec. on the half time of the helix-random coil relaxation in poly-α, L-glutamic acid. No relaxations are observed under conditions where the polymer exists in completely helical or completely random coil form. Assuming that the helix-coil transition can be described kinetically as a pure growth process, expressions for the relaxation time are derived for three special cases. A comparison is made between the rate of the helix-coil transition and the rate of imide proton exchange.
    Additional Material: 1 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/bip.1964.360020507
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  • 19
    Electronic Resource
    Electronic Resource
    Low-sulfur proteins from α-keratins. Interrelationships between their amino acid compositions, α-helix contents, and the supercontraction of the parent keratin (1966)
    New York : Wiley-Blackwell
    Biopolymers 4 (1966), S. 905-916 
    Details
    ISSN: 0006-3525
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: S-Carboxymethyl (SCM) kerateine preparations from a range of keratins were fractionated by acid precipitation into low-sulfur (SCMKA) and high-sulfur (SCMKB) fractions. Amiono acid analyses and optical rotatory dispersion measurements on the SCMKA fractions from different keratins indicated that the proportion of α-helical material (30-64%) increased with increasing leucine and glutamic acid contents and decreased with increasing SCM-cysteine and proline contents. It is shown that these variations in α-helix contents are due mainly to differences in the conformations of the principal components of the SCMKA fractions, although there is also a smaller contribution arising from contamination with varying amounts of non helical components. The thiol + disulfide contents for the parent keratins were measured and compared with the SCM -cysteine contents of the solubilized fractions. In general the SCM-cysteine contents of the SCMKA fractions increased with increasing thiol + disulfide content of the parent keratin, but these values were not directly proportional. The extent of total supercontraction in 8M LiBr solution was measured for the parent keratins and shown to bear no significant relationship to their disulfide contents. From the extents of first-stage and total supercontractions the disulfide contents of the contractile structures in the fibers were calculated according to a model described previously and compared with the analytical values for the SCM -cysteine contents of the SCMKA and SCMKB fraction. Data for both fractions were consistent with the model in that they were in each case related to the calculated values by a constant factor. However, because of simplifying assumptions in the model, it was not possible to identity positively one or other of these protein fractions with the contractile elements in the fiber.
    Additional Material: 3 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/bip.1966.360040807
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  • 20
    Electronic Resource
    Electronic Resource
    Absorption and Fluorescence Studies on Neutral and Cationic Isoalloxazines (1979)
    New York, NY : Wiley-Blackwell
    Helvetica Chimica Acta 62 (1979), S. 593-608 
    Details
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The electronic properties of a variety of methylated isoalloxazine derivatives have been investigated with absorption and fluorescece techniques (Table 1). The spectral effects of methyl substitution at different positions in the isoalloxazine ring are interpreted in terms of different bond orders between the C-atoms of the methyl groups and of the aromatic ring. Methyl groups at C(6) or C(9) induce quenching of the fluorescence and shortening of the lifetime whereas a methyl group at C(7) has an opposite effect. The quenching effect might be due to strain in the molecular framework caused by the methyl groups.The lowest energy levels of the isoalloxazine cations are shifted to higher energy as compared to the neutral isoalloxazines. Apart from these shifts the trends in spectral behaviour upon methylation are similar to those observed for the neutral isoalloxazine (cf. Table 2). The fluorescence of the isoalloxazine cations is strongly quenched in auqeous solution and their lifetime much shortened. These observations indicated that there is substantial interaction between the charged fluorophore and the water dipoles and that this interaction produces efficient radiationless deactivation of the first excited singlet state.
    Additional Material: 4 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/hlca.19790620227
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