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  • 1
    ISSN: 1432-1440
    Keywords: Smoking ; Oral contraception ; Coagulation ; Fibrinolysis ; Fibrinopeptides
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Oral contraception as well as cigarette smoking influence haemostasis. The simulataneous effect of both on blood coagulation and fibrinolysis was studied in nine female smokers. While continuing oral contraception after a 4-week abstinence from smoking the concentration of fibrinogen, antithrombin III and alpha1-Antitrypsin decreased (P〈0.01 orP〈0.04) and of plasminogen increased (P〈0.03). The other coagulation parameters remained unchanged. Although all determinations of these parameters were in the normal range, the observed trends were statistically significant. The concentrations of the fibrinopeptide A and B 15–42 did not differ. It is concluded that the observed alteration is caused by cessation from cigarette smoking.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 39 (1990), S. 577-581 
    ISSN: 1432-1041
    Keywords: Benzbromarone ; elimination phenotypes ; pharmacokinetics ; metabolism ; genetic variation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Following oral administration of the uricosuric drug benzbromarone two major metabolites appear in the circulation, 1'-hydroxy-benzbromarone (M1), and a second product (M2) of unknown structure. The plasma concentrations of the parent drug and of M1 and M2 have now been compared in two different elimination phenotypes, 10 subjects who eliminated the drug rapidly (S1–10) and one individual (S11) whose elimination capacity was impaired, presumably due to genetic variation (S11). The AUC (0–96) of the parent drug in S11 was 145 gmg · ml−1 h, and in the other individuals it averaged 18.3 (11.4–24.5) μg · ml−1 h. The plasma elimination half life of benzbromarone was 3.34 (1.77–5.24) h in the rapid eliminators, and 13.08 h in the subject with the elimination defect. The mean plasma elimination half life of the metabolites in S1–10 amounted to 20.1 (11.9–41.2) h for M1, and 17.2 (12.9–30.7) h for M2. In S11 the plasma elimination half life of M1 was prolonged to 76.6 h, and of M2 to 75.4 h. Thus, the elimination defect in S11 was not restricted to the parent drug, but it also involved the two major metabolites M1 and M2. This might be a consequence of a hepatic enzyme deficiency, or be due to impairment of drug excretion.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1432-1041
    Keywords: sulphinpyrazone ; metabolism ; single dose ; chronic treatment ; pharmacokinetics ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of sulphinpyrazone and its major metabolites (sulfide, sulfone, p-hydroxysulfone and p-hydroxy-sulphinpyrazone) were investigated in 9 volunteers after a single oral dose as well as after chronic treatment for 23 days. Chronic administration of sulphinpyrazone, in comparison with a single oral dose, led to significant changes in plasma AUC (115.86 to 42.90 mg/l·h), in renal clearance (1.06 to 1.80l/h), in hepatic intrinsic clearance (319.0 to 598.0l/h), and in the unbound fraction in plasma 1.15 to 1.69%) and in tissue (2.73 to 1.31%). The volume of distribution changed from 20.24 to 52.041. The steady state concentrations predicted from the single dose were significantly higher than the values found after chronic treatment. The results suggest that sulphinpyrazone induces its own metabolism. The metabolism of the sulfone, p-hydroxysulfone and the p-hydroxy-sulphinpyrazone to further degradation products was also induced. Chronic treatment with sulphinpyrazone reduced the plasma AUC of the sulfide and caused a decrease in its elimination half-life (20.9 to 14.3 h). Since considerable amounts of the sulfide are formed in the G.I. tract, it is suggested that besides the induction of metabolism, bacteria which reduce sulphinpyrazone to the sulfide may also be responsible for the observed pharmacokinetic changes.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 26 (1984), S. 485-489 
    ISSN: 1432-1041
    Keywords: theophylline ; erythromycin ; interaction ; metabolism ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In 11 healthy volunteers the kinetics of theophylline and the plasma levels and the urinary excretion of its metabolites were studied before and after treatment with erythromycin for 10 days. Theophylline was administered as an intravenous bolus injection (280 mg) followed by a constant intravenous infusion (23.8±4.1 mg/h) for 6 hours. The total clearance of theophylline at steady-state (63.4±9.9 vs 63.8±14.4 ml/min, before vs after erythromycin treatment) and the elimination half-life after cessation of the infusion (6.7±2.6 vs 7.5±1.8 h, before vs after treatment) did not change during the treatment with erythromycin. No difference in the formation of metabolites before and after treatment with erythromycin was detected; the findings in urine were 40.4±5.0 vs 42.1±5.4% 1,3-dimethyluric acid, 29.6±4.6 vs 30.1±5.9% 1-methyluric acid and 13.4±3.5 vs 12.5±2.2% 3-methylxanthine before and after erythromycin treatment, respectively. It is concluded that a clinically relevant interaction between erythromycin and theophylline does not occur.
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    Springer
    Journal of molecular medicine 56 (1978), S. 445-448 
    ISSN: 1432-1440
    Keywords: Fibrinolysis ; Circadian rhythms ; Clinical trial ; Euglobulinlysis-time ; Fibrinolyse ; circadiane Rhythmik ; klinische Prüfung ; Euglobulinlyse-Zeit
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung Bei 5 Probanden wurde über einen Zeitraum von 6 Wochen fünfmal die Anstiegsphase im Tagesrhythmus der fibrinolytischen Aktivität untersucht. Als Parameter wurden die Euglobulinlyse-Zeit und die Papierfibrinolyse, die Plasmaproteine, Fibrinogen, Plasminogen, α1-Antitrypsin und α2-Makroglobulin sowie die Thrombinocoagulase-Zeit und die Fibrinspaltprodukte erfaßt. Es zeigte sich bei allen Probanden der Anstieg der Fibrinolyse am Vormittag. Die Schwankungsbreite der fibrinolytischen Aktivität ist intraindividuell kleiner als bei einem interindividuellen Vergleich. Weiterhin zeigt sie mittags eine geringere Streuung als vormittags. Bei Untersuchungen zur klinischen Prüfung eines Soforteffektes von Arzneimitteln auf die Fibrinolyse sollte der Zeitraum der Plateauphase der fibrinolytischen Aktivität gewählt werden, um die Streuung der Ausgangswerte möglichst gering zu halten. Weiterhin ist die intraindividuelle Streuung der fibrinolytischen Aktivität in diesem Zeitraum geringer als während der Anstiegsphase im Rahmen des circadianen Rhythmus der Fibrinolyse. Eine intraindividuelle Kontrolle muß gewährleistet werden.
    Notes: Summary In five volunteers fibrinolytic activity has been measured five times over a period of six weeks during increasing values of circadian rhythm. Euglobulinlysis-time, paper fibrinolysis, fibrinogen, plasminogen, α1-antitrypsin, α2-makroglobulin, thrombinocoagulase-time and fibrin-split-products were used in one study. An increase of fibrinolytic activity in the mooning was observed in all volunteers. Intraindividual variation of values is considerable but less than variation of values compared interindividually. Moreover variation was smaller at noon than in the time before noon. In clinical trial of the short-time effect of drugs the period of the plateau of the fibrinolytic activity should be used because of its smaller variation of values. Furthermore, in this period the intraindividual variation of the fibrinolytic activity is smaller than during increasing slope of the circadian rhythm of fibrinolysis. Intraindividual control should be granted.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Chemie in unserer Zeit 23 (1989), S. 210-214 
    ISSN: 0009-2851
    Keywords: Chemistry ; Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Additional Material: 1 Ill.
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    New York, NY : Wiley-Blackwell
    Helvetica Chimica Acta 24 (1941), S. 278-288 
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Additional Material: 7 Ill.
    Type of Medium: Electronic Resource
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  • 8
    Electronic Resource
    Electronic Resource
    New York, NY : Wiley-Blackwell
    Journal für Praktische Chemie/Chemiker-Zeitung 327 (1985), S. 479-486 
    ISSN: 0021-8383
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Cleavage of Z-Group and Formation of Hydantoine during Saponification of Z-Peptide EstersIn the course of alkaline decomposition of the tetrapeptide ester Z-Arg(NO2)-Gly-Phe-Phe-OMe one gets a high output of a by-product. the latter was isolated and identified by 13C-n.m.r. spectroscopy to be the hydantoine derivative arising from a loss of Z-group and from a cyclisation. A possibility to suppress the undesired side-reaction by addition of benzylalcohol is proposed resulting from the discussion of a probable mechanism of reaction.
    Additional Material: 2 Ill.
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    New York, NY : Wiley-Blackwell
    Journal für Praktische Chemie/Chemiker-Zeitung 335 (1993), S. 235-243 
    ISSN: 0941-1216
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: New Macrocyclic Hosts for the Inclusion of Organic Guest Molecules - Crystal Structure of a Complex with Dimethylformamide (1 : 1)New pyridino crowns with amide and sulfonamide groups 1b and 1c are synthesized. They form numerous stoichiometric crystalline inclusion complexes with alcohols, various dipolar-aprotic solvents, as well as cyclic ethers. Host-guest stoichiometries are discussed and inclusion selectivities (relating to DMF) are shown. The structure of the crystalline DMF inclusion compound of the sulfonamide host 1c (1 : 1) is determined by X-ray diffraction, showing a lattice void inclusion mode.
    Additional Material: 2 Ill.
    Type of Medium: Electronic Resource
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  • 10
    Electronic Resource
    Electronic Resource
    New York, NY : Wiley-Blackwell
    Journal für Praktische Chemie/Chemiker-Zeitung 337 (1995), S. 451-455 
    ISSN: 0941-1216
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: New crown compounds 3-5 comprising beside ophenylene groups 1,8-naphthyridine or 4-pyridone groups as characteristic building units are synthesized. They form numerous stoichiometric crystalline complexes with uncharged organic molecules including alcohols, nitro compounds and other dipolar-aprotic solvents, as well as cyclic ethers and aromatic hydrocarbons. Properties of complex formation and host-guest stoichiometries are discussed making a comparison with parent host analogues.
    Additional Material: 1 Tab.
    Type of Medium: Electronic Resource
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