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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 36 (1989), S. 395-400 
    ISSN: 1432-1041
    Keywords: pyrazinamide ; antituberculous chemotherapy ; pharmacokinetics ; xanthine oxidase ; microsomal deaminase
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The plasma and urine pharmacokinetic parameters of pyrazinamide and of its metabolites (pyrazinoic acid, 5-hydroxy-pyrazinamide, 5-hydroxy-pyrazinoic acid and pyrazinuric acid) have been studied after a single oral dose of pyrazinamide 27 mg · kg−1 in 9 healthy subjects. Pyrazinamide was rapidly absorbed (tmax ≤1 h) and showed a short distribution phase followed by an elimination phase of t1/2β=9.6 h. The close similarity of the apparent elimination rates of the metabolites led to a second trial of a single oral dose of pyrazinoic acid to evaluate the formation and elimination stages. The limiting factor was found to be the activity of a microsomal deamidase (pyrazinoic acid formation from pyrazinamide and 5-hydroxy-pyrazinoic acid formation from 5-hydroxy-pyrazinamide). In contrast, oxidation by xanthine oxidase occurred very rapidly (5-hydroxy-pyrazinamide formation and pyrazinoic acid catabolism to 5-hydroxy-pyrazinoic acid).
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 37 (1989), S. 309-311 
    ISSN: 1432-1041
    Keywords: pyrazinamide ; haemodialysis ; pharmacokinetics ; uraemic patients ; drug metabolites ; anti-tuberculous chemotherapy
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of PZA during haemodialysis were determined in 6 patients with chronic renal impairment after a single oral dose of 25.7 (1.9) mg·kg−1. The dialysis clearance of PZA and of its metabolites were: pyrazinamide 132 ml·min−1; pyrazinoic acid 121 ml·min−1; 5-hydroxy-pyrazinamide 107 ml·min−1; 5-hydroxy-pyrazinoic acid 118 ml·min−1. The average amount extracted during a dialysis session of 4.1 h was 926 mg after an oral dose of 1700 mg. The high dialysability shows that PZA can property be administered at the end of each dialysis session in the usual dose of 25 to 30 mg·kg−1.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Amsterdam : Elsevier
    Journal of Chromatography B: Biomedical Sciences and Applications 307 (1984), S. 137-144 
    ISSN: 0378-4347
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Amsterdam : Elsevier
    Journal of Chromatography B: Biomedical Sciences and Applications 415 (1987), S. 85-94 
    ISSN: 0378-4347
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    Amsterdam : Elsevier
    Journal of Chromatography B: Biomedical Sciences and Applications 525 (1990), S. 240-245 
    ISSN: 0378-4347
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 6
    ISSN: 1439-0973
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung In 16 Fällen schwerer bronchopulmonaler Infektionen wurde als einziger bakterizider Wirkstoff Sisomicin — ein Aminoglykosid — in einer Tagesdosis von durchschnittlich 3.5 mg/kg während 7–14 Tagen (Durchschnitt 11.5) dreimal täglich intramuskulär injiziert. Fünfzehn der hospitalisierten Patienten hatten eine chronische obstruktive Ventilationsstörung mit verminderter O2-Sättigung (SaO2 86.1%, Bereich 74–93%); bei 12 Patienten wurde eine Hyperkapnie (PaCO2=55.7 torr, Bereich 33–73) festgestellt; zwei von ihnen wurden kontinuierlich künstlich beatmet. Je ein Patient hatte eine Verschattung des Unterlappens und einen Lungenabszess. In den Bronchialsekretionen wurden mit der Mulder-Methode folgende vorherrschende Stämme isoliert: 3 Proteus, 9 Pseudomonas, 2 K.pneumoniae und je ein E.coli, Enterobacter, S.aureus und D.pneumoniae; in 3 Fällen wurde P.aeruginosa je einmal zusammen mit K.pneumoniae, P.rettgeri oder E.coli isoliert. In 13 Fällen erfolgte eine klinische Heilung oder eine wesentliche Besserung (Sputumvolumen und purulente Beimengungen, Auskultationsbefund, Temperatur); bei 3 dieser Patienten wurde jedoch eine Superinfektion/Kolonisation und bei 2 Patienten persistierende Pseudomonas festgestellt. Außerdem wurde in 2 der 3 nicht geheilten Fälle eine Kolonisation beobachtet. Dank der intensiven Antibiotikabehandlung mit gleichzeitiger unterstützender Therapie konnte ein sehr gutes Resultat erzielt werden. Lokale oder allgemeine Unverträglichkeit des Medikamentes konnte nicht beobachtet werden.
    Notes: Summary Sisomicin, an aminoglycoside antibiotic, was used as sole bactericidal therapy in sixteen cases of severe bronchopulmonary infection for an average of 11.5 days (range 7 to 14) with a dose of 3.5 mg/kg per day in three intramuscular injections. Fifteen of these hospitalized patients presented with chronic airway obstruction which resulted in lowered O2 saturation (SaO2-86.1%, range 74 to 93) and, in twelve patients, hypercapnia (PaCO2=55.7 torr, range 33–73). Two of these patients were under continuous assisted ventilation. Two patients had a lower lobe infiltrate and a lung abcess respectively. Proteus (n=3), Pseudomonas (n=9), K. pneumoniae (n=2), E.coli (n=1), Enterobacter (n=1), S. aureus (n=1) and D. pneumoniae (n=1) were the dominant organisms in the bronchial secretions isolated by Mulder's method; P. aeruginosa was associated with K. pneumoniae, P. rettgeri and E.coli respectively in three cases. In thirteen cases, either a clinical cure (n=2) or a definite improvement was observed (sputum volume and purulence, auscultatory signs, temperature). However, among these patients were three cases of superinfection/colonization and two cases of persistent organisms. In addition, in two of the three cases showing no improvement colonization occurred. The favorable results of this study appear to be due to vigorous antibiotic therapy combined with intensive adjunct therapy. No adverse local or systemic reactions clearly attributable to the drug were observed.
    Type of Medium: Electronic Resource
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