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  • metabolism  (6)
  • Springer  (6)
  • Annual Reviews
  • Wiley
  • 1980-1984  (6)
  • 1983  (6)
  • 1
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of triamterene after i.v. administration to man: Determination of bioavailability (1983)
    Springer
    European journal of clinical pharmacology 25 (1983), S. 237-241 
    Details
    ISSN: 1432-1041
    Keywords: triamterene ; bioavailability ; pharmacokinetics ; metabolism ; hydroxy triamterene sulphate ; urinary excretion ; i.v. administration ; first-pass-effect
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary With a new formulation, which made intravenous infusion of triamterene (TA) possible, plasma levels and urinary excretion rates of TA and its main metabolite (OH-TA-ester) were measured in a randomized, cross-over trial in 6 healthy volunteers given triamterene 10 mg i.v. and 50 mg p.o. TA and OH-TA-ester were determined by densitometric measurement of native fluorescence after thin layer chromatography. Distribution volumes of the central compartment of TA and OH-TA-ester were 1.49 l/kg and 0.11 l/kg, respectively. Terminal half-lives were 255 min for TA and 188 min for OH-TA-ester after i.v. administration. For TA total plasma clearance was 4.5 l/min and renal plasma clearance 0.22 l/kg. The formation of OH-TA-ester was very rapid and the concentration of the metabolite exceeded that of TA at all times. After i.v. administration the urinary recovery of TA and OH-TA-ester was 4.4% and 50.9%, respectively. The bioavailability of TA was 52%, corresponding to absorption of 83%. TA is partly eliminated by a first-pass-effect. The main metabolite of TA is OH-TA-ester, which is pharmacologically active.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00543797
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  • 2
    Electronic Resource
    Electronic Resource
    Formation of a metabolite of dibromosulfophthalein (DBSP) in man (1983)
    Springer
    European journal of clinical pharmacology 24 (1983), S. 703-709 
    Details
    ISSN: 1432-1041
    Keywords: dibromosulfophthalein ; glutathione conjugate ; metabolism ; biliary excretion ; hepatic transport test ; chemical stability ; thin layer chromatography
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In bile specimens from postoperative patients with biliary drainage following cholecystectomy, in addition to unchanged dibromosulfophthalein (DBSP), a single polar metabolite of DBSP was found after i.v. injection of 5 mg/kg of the diagnostic dye. This metabolite, which has not previously been detected, was resistant to β-glucuronidase and arylsulfatase and was remarkably stable in strongly acid and alkaline solutions. It exhibited the same spectrum and colour change interval as unchanged DBSP. Further studies of its identity revealed that it gave a ninhydrin-positive reaction and that its Rf-value on TLC could be restored by Raney-nickel reduction. Amino-acid analysis after reduction and acid hydrolysis showed an increase in glutamic acid and alanine that can be considered as splitting products of conjugated glutathione following these procedures. Estimation of the quantity of this possible glutathione conjugate indicates that it is formed less rapidly than the glutathione derivative of the tetrabromoanalogue BSP, and that it represents up to 25% of the total dye excreted in bile. The observed metabolism of DBSP in man may complicate its use in the study of hepatic transport function, and negates the previous assumption that, as in certain other animal species, the dye is excreted unchanged.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542226
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  • 3
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of diltiazem in severe renal failure (1983)
    Springer
    European journal of clinical pharmacology 24 (1983), S. 635-638 
    Details
    ISSN: 1432-1041
    Keywords: calcium antagonist ; diltiazem ; renal failure ; pharmacokinetics ; desacetyldiltiazem ; metabolism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The acute effects of a single dose of diltiazem (Tildiem®), a calcium antagonist, were studied in 9 patients with severely impaired renal function (GFR between 0.03 and 0.87 ml/s/1.73 m2). Control measurements were made of inulin and PAH clearance, creatinine, blood pressure, heart rate and ECG. Following administration of diltiazem 120 mg, 7 blood samples were collected in the first 12 h and after 24 h, 32 h, 48 h; urine was collected for the first 12 h, 12–24 h and 24–48 h, and blood pressure, heart rate and ECG were recorded after 6 h. Diltiazem and its main metabolite, desacetyldiltiazem, had a pharmacokinetic profile similar to that in patients with normal renal function (peak plasma concentration, half-life and urinary excretion). Diltiazem is normally eliminated in the urine to a small extent, because it is metabolized, and this also applies to desacetyldiltiazem, which is probably further metabolized.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542213
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  • 4
    Electronic Resource
    Electronic Resource
    Metabolism of propranolol in the human maternal-placental-foetal unit (1983)
    Springer
    European journal of clinical pharmacology 24 (1983), S. 727-732 
    Details
    ISSN: 1432-1041
    Keywords: propranolol ; foetus ; placenta ; metabolism ; pregnancy ; plasma levels ; plasma protein binding ; delivery
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Propranolol (P) and all of its major known metabolites were found in maternal plasma, cord plasma and neonatal plasma in 10 women at term, irrespective of the P doses administered and the time elapsed (up to 15 h) between administration of the last P dose and delivery. The ratios of cord plasma to simultaneous maternal plasma levels for propranolol and its major metabolites (mean±SD) were: propranolol 0.32±0.17, propranolol glucuronide 0.86±0.36, 4-hydroxypropranolol 1.4±1.0, 4-hydroxypropranolol glucuronide 0.71±0.45 and naphthoxylactic acid 3.0±1.6. P binding in cord plasma at delivery was 67.2±3.9% (mean±SD) which was significantly less (‘t’=13.4,df=13,p〈0.001) than the P binding in maternal plasma at delivery (87.5±1.6%, mean±SD). The plasma protein binding (mean±SD) of naphthoxylactic acid in cord plasma (98.6±0.2%) was significantly greater (‘t’=3.808,df=4,p〈0.02) than the naphthoxylactic acid binding in maternal plasma at delivery (97.6±0.4%). When the simultaneous concentrations of P and naphthoxylactic acid in maternal and cord plasma are compared in conjunction with protein binding and ionic effects, it would seem that metabolism of P does occur in the placental/foetal unit.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00607078
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  • 5
    Electronic Resource
    Electronic Resource
    Biotransformation of furosemide in kidney transplant patients (1983)
    Springer
    European journal of clinical pharmacology 24 (1983), S. 787-790 
    Details
    ISSN: 1432-1041
    Keywords: furosemide ; kidney transplant patients ; metabolism ; renal function ; furosemide glucuronide ; biliary excretion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The metabolic fate of furosemide was studied in kidney transplant patients after oral and intravenous administration of the diuretic at therapeutic doses. Serial urine samples were collected over a 24 h period and furosemide was analyzed by a specific high performance liquid chromatographic method using fluorescence detection. We found no evidence of the putative furosemide metabolite, 2-amino-4-chloro-5-sulfamoylanthranilic acid (CSA), in any of the samples analyzed. The amount of furosemide excreted as the glucuronide metabolite accounted for 8% of the available dose, whether administered orally or by intravenous infusion. In addition, the significant positive correlation observed between the percent of the available dose excreted as furosemide glucuronide and the renal clearance of furosemide (r=0.581,p〈0.02) suggests that the glucuronidation process for furosemide may be occurring in the kidney. Furosemide and its glucuronide metabolite accounted for only 45% of the intravenous dose recovered in the urine. Biliary excretion of unchanged furosemide and/or furosemide glucuronide into the feces probably accounts for the remainder of the dose not recovered.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00607088
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  • 6
    Electronic Resource
    Electronic Resource
    Formation of a metabolite of dibromosulfophthalein (DBSP) in man (1983)
    Springer
    European journal of clinical pharmacology 25 (1983), S. 427-428 
    Details
    ISSN: 1432-1041
    Keywords: dibromosulfophthalein ; glutathione conjugate ; metabolism ; biliary excretion ; hepatic transport test ; chemical stability ; thin layer chromatography
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01037960
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