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  • pharmacokinetics  (6)
  • Analytical Chemistry and Spectroscopy  (5)
  • 1
    ISSN: 1432-1041
    Keywords: prednisolone ; hydrocortisone ; cushingoid syndrome ; pharmacokinetics ; renal transplant ; oral disease
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary To establish if the appearance of cushingoid side effects in patients taking exogenous glucocorticoids is related to the disposition and metabolism of these steroids and endogenous hydrocortisone, 15 stable renal transplant patients and 12 patients treated with prednisone for oral mucocutaneous vesiculo-erosive diseases were investigated. All 27 patients were given their usual prednisone dose orally on one occasion, and 24 were given the same amount of prednisolone intravenously on another occasion. Following dosing, plasma samples were obtained for determination of the areas under the plasma concentration time curves of total prednisolone, prednisone and hydrocortisone by high performance liquid chromatography, and of unbound prednisolone by equilibrium dialysis. The bioavailability of prednisone, the interconversion of prednisone into prednisolone, the clearance of total and unbound prednisolone, the prednisolone binding capacity of albumin and transcortin, and the affinity of albumin for prednisolone did not differ between the 14 patients without cushingoid side effects and the 13 cushingoid patients. Compared to those who had cushingoid features, patients who developed no side effects had a higher affinity constant for prednisolone binding to transcortin − 2.04±0.27 × 107 L/M vs. 1.34±0.16×107 (X±SE;P〈0.05), more frequently exhibited peak hydrocortisone levels within the normal range (6/14 vs 1/13), more often had measurable (〉10ng/ml) hydrocortisone in the plasma samples collected during the kinetic studies (123/291 vs 74/325;P〈0.001) and had higher areas under the plasma concentration time curve of hydrocortisone (median, range), i.e. 8081 ng/ml · min (0–21 637 ng/ml · min) vs 386 ng/ml · min (0–16 329 ng/ml · min;P〈0.005). The data suggest that endogenous hydrocortisone production is not as suppressed in patients with visible cushingoid signs as in noncushingoid patients, and that there is no significant difference in the pharmacokinetics of exogenous glucocorticoids between patients with and without cushingoid side effects.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 26 (1984), S. 505-511 
    ISSN: 1432-1041
    Keywords: prednisolone ; prednisone ; oral contraceptives ; 6β-hydroxylase ; transcortin ; protein-binding ; steroid metabolism ; pharmacokinetics ; drug interaction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The oestrogenic component of oral contraceptives affects the activity of liver enzymes and the concentrations of plasma proteins implicated in steroid metabolism and transport. The present study was designed to determine these effects on the kinetics of prednisone and prednisolone. After an oral dose of prednisone, women on oral contraceptive steroids (n=10) had higher mean (±SD) area under the plasma concentration versus time curves of total (428±67 µg/ml/min vs 188±28 µg/ml/min, p〈0.001) and unbound prednisolone (64±10 µg/ml/min vs 41±10 µg/ml/min, p〈0.001) than women not taking oral contraceptive steroids (n=10). The differences were attributable to a lower non-renal clearance of prednisolone and to a higher apparent systemic availability of the drug in contraceptive users than in the controls. The affinity of albumin and transcortin for prednisolone was lower in women on oral contraceptives than in controls (p〈0.001). Thus, altered kinetics and protein binding may account for the known increase in glucocorticoid efficacy by oestrogens.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 19 (1981), S. 209-212 
    ISSN: 1432-1041
    Keywords: prednisone ; prednisolone ; azathioprine ; 11 β-hydroxydehydrogenase ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Clinical and pharmacokinetic observations suggest that azathioprine may diminish the plasma level of prednisolone. To study the extent of this possible interaction, and to define the underlying mechanism, total and unbound prednisolone and total prednisone concentrations were assessed in 11 subjects following an oral dose of prednisone once with and once without concomitant oral administration of azathioprine. Azathioprine did not affect the area under the plasma concentration-time curve of total and unbound prednisolone; furthermore, the interconversion of prednisone into prednisolone was not influenced by azathioprine.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1432-1041
    Keywords: cefoperazone ; peritoneal dialysis ; pharmacokinetics ; terminal renal failure ; peritonitis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of cefoperazone after i.p. and/or i.v. administration were studied in 12 CAPD patients. After i.v. injection, the plasma half-life was 2.65±0.4 h, the total clearance amounting to 70.1±19.2 ml/min. Peritoneal clearance was calculated to be 6.9±1 ml/min. After peritoneal instillation, the bioavailability was 63.9±5%. After repeated i.p. administration, no accumulation of the drug in the body was observed. Thus, cefoperazone can be safely administered for the treatment of peritonitis in CAPD patients.
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 36 (1989), S. 389-393 
    ISSN: 1432-1041
    Keywords: ornidazole ; haemodialysis ; pharmacokinetics ; renal function ; metabolism ; urine concentration
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of ornidazole was studied in 6 patients treated by haemodialysis and in 8 subjects with a creatinine clearance between 4 and 99 ml/min × 1.73 m2. Blood and urine collections were performed for 72 h after i.v. and oral administration of 1.0 g ornidazole. Total body clearance, half-life, volume of distribution and systemic availability were independent of renal function and did not differ from previously reported values in normal volunteers. The haemodialysis clearance of ornidazole was 〉100% higher than the total body clearance. The renal clearance of ornidazole accounted for less than 7% of the total body clearance. The percentage of the dose of ornidazole recovered in urine as parent compound or as the biologically active metabolites [α-(chloromethyl)-2 hydroxymethyl-5 nitroimidazole-1 ethanol and 3-(2 methyl-5 nitroimidazole-1-yl)1,2 propanediol] decreased linearly with decreasing renal function. Although the sum of those three compounds recovered in urine accounted for less than 10% of the total dose of ornidazole administered, they yielded therapeutic concentrations (〉4 µg/ml) in urine over 24 h after dosing. Due to the peculiar pharmacokinetic behaviour of ornidazole, i.e. high haemodialysis clearance in the absence of significant renal clearance, no dosage adjustment is necessary while renal function declines, but an increased dose is mandatory while patients are on dialysis.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 29 (1986), S. 697-701 
    ISSN: 1432-1041
    Keywords: tenoxicam ; renal insufficiency ; non-steroidal antiinflammatory agents ; protein binding ; metabolism ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of tenoxicam after a single oral dose of 20 mg has been studied in 12 patients with various degrees of decreased renal function. Unchanged tenoxicam and its 5′OH-metabolite in plasma and urine were determined by HPLC. The mean areas under the plasma concentration-time curve (138±53 µg/ml·h) and terminal half-lives in patients with impaired renal function did not differ from values previously reported in normal volunteers, nor did the peak concentration of tenoxicam. The half-life of 5′OH-tenoxicam and unchanged tenoxicam where the same. The urinary excretion of 5′OH-tenoxicam fell with decreasing renal function. Thus no dosage adjustment should be necessary and the usual daily dose of tenoxicam may be administered once daily also to patients with renal failure.
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Journal of High Resolution Chromatography 1 (1978), S. 213-214 
    ISSN: 0935-6304
    Keywords: Liquid chromatography ; Specific detections ; Post-column derivatization ; Fluorometric ion-pair technique ; Fluorometric determination of pharmaceutical amines ; Chemistry ; Analytical Chemistry and Spectroscopy
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Additional Material: 2 Ill.
    Type of Medium: Electronic Resource
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  • 8
    Electronic Resource
    Electronic Resource
    Chichester : Wiley-Blackwell
    Organic Magnetic Resonance 7 (1975), S. 199-205 
    ISSN: 0030-4921
    Keywords: Chemistry ; Analytical Chemistry and Spectroscopy
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Using the pulse Fourier transform technique, the undecoupled carbon-13 NMR spectra of the products obtained in the reaction of methyltriazines with 1-(dimethylamino)-1-ethoxyethylene have been recorded and completely assigned. A comparison of the observed 13C chemical shifts and 13C—H coupling constants with those in the starting triazines and in 2-dimethylamino-2-penten-4-one confirms the (2-dimethylamino-1-propenyl) triazine structure. The data are discussed in terms of steric effects and of the configuration and conformation of the sidechain.
    Notes: Die unentkoppelten 13C-NMR-Spektren der bei der Reaktion von Methyltriazinen mit 1-Äthoxy-1-(dimethylamino)-äthylen entstandenen Produkte wurden mit Hilfe der Puls-Fourier-Transform-Technik aufgenommen und analysiert. Der Vergleich der beobachteten 13C-chemischen Verschiebungen und 13C—H-Kopplungskonstanten mit denen der Ausgangstriazine und des 2-Dimethylamino-2-penten-4-ons bestätigt die (2-Dimethylamino-1-propenyl)triazin-Struktur. Die Daten werden im Hinblick auf sterische Effekte sowie die Konfiguration und Konformation der Seitenkette diskutiert.
    Additional Material: 4 Ill.
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    Chichester : Wiley-Blackwell
    Organic Magnetic Resonance 7 (1975), S. 194-198 
    ISSN: 0030-4921
    Keywords: Chemistry ; Analytical Chemistry and Spectroscopy
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Using the pulse Fourier transform technique, the high resolution carbon-13 NMR spectra of 1,2,4- and 1,3,5-triazine and their methyl derivatives as well as the 1H noise decoupled spectra of phenyl- and methylphenyl substituted triazines, have been recorded and analysed. The chemical shifts of the polysubstituted 1,2,4-triazines normally show additivity; deviations observed with phenyl derivatives are ascribed to steric effects. The 13C—H coupling constants are compared to those of benzene, pyridine, the diazines and disubstituted ethylenes. The strong influence on the coupling constants exerted by number and position of the nitrogen atoms is revealed by the observation that geminal couplings in 1,2,4-triazine are larger than vicinal ones, in contrast to the usual sequence.
    Notes: Mit Hilfe der Puls-Fourier-Transform-Technik wurden die Hochauflösungs-13C-NMR-Spektren des 1,2,4- und 1,3,5-Triazins sowie ihrer Methylderivate aufgenommen, ferner auch die 1H-breitbandentkoppelten 13C-Spektren von phenyl- und methyl-phenyl-substituierten Triazinen. Die chemischen Verschiebungen der mehrfach substituierten 1,2,4-Triazine verhalten sich weitgehend additiv; Abweichungen bei Phenylderivaten werden sterischen Ursachen zugeschrieben. Die 13C—H-Kopplungskonstanten werden mit denen im Benzol, im Pyridin, in den Diazinen sowie in disubstituierten Äthylenen verglichen. Der starke Einfluß von Anzahl und Position der Stickstoffatome auf die Kopplungskonstanten läßt sich daran erkennen, daß im 1,2,4-Triazin, entgegen der üblichen Reihenfolge, geminale Kopplungen größer als vicinale sind.
    Additional Material: 1 Ill.
    Type of Medium: Electronic Resource
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  • 10
    Electronic Resource
    Electronic Resource
    Chichester : Wiley-Blackwell
    Organic Magnetic Resonance 33 (1995), S. 874-878 
    ISSN: 0749-1581
    Keywords: NMR ; 17O NMR ; diaryl α-diketones ; Hammett correlation ; conformations ; Chemistry ; Analytical Chemistry and Spectroscopy
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Natural abundance 17O NMR spectra of eleven diaryl α-diketones are reported. An excellent correlation was found between 17O shifts and σp+. Conformations and π character of the intercarbonyl C—C bond are discussed.
    Additional Material: 2 Tab.
    Type of Medium: Electronic Resource
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