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  • 1
    Electronic Resource
    Electronic Resource
    Dose-proportionality of eltoprazine (1991)
    Springer
    European journal of clinical pharmacology 41 (1991), S. 485-488 
    Details
    ISSN: 1432-1041
    Keywords: Eltoprazine ; pharmacokinetic ; serenics ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Eltoprazine. HCl belongs to a new class of psychotropic drug, the serenics. The dose-proportionality and pharmacokinetics of eltoprazine HCl has been investigated after single oral doses of 5, 10, 20 mg (18 subjects) and 30 mg (12 subjects) in a partly randomized, cross-over design. Eltoprazine was well tolerated and there were no relevant changes in safety parameters. All subjects showed irregular plasma-concentration-time profiles, some subjects demonstrating secondary peaks. The mean half-life was calculated to be about 6.5 h. The renal excretion of eltoprazine was characterized by net tubular secretion. AUC, peak plasma concentrations and the amount excreted unchanged in the urine were linearly related to the dose. Renal clearance and t1/2 were independent of dose. Thus, eltoprazine HCl was well tolerated orally and exhibited a linear pharmacokinetic profile.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00626375
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Allergic contact dermatitis due to rubber chemicals in haemodialysis equipment (1987)
    Oxford, UK : Blackwell Publishing Ltd
    Contact dermatitis 17 (1987), S. 0 
    Details
    ISSN: 1600-0536
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: 6 of 80 haemodislysed patients developed a sub-acute eczematous dermatitis of the area surrounding the arteriovenous shunt in the forearm. Patch tests were positive to rubber chemicald 6 patients reacted to the thiuram group, 4 of them also to carbo compounds. Since the equipment contained only small pieces of rubber, the cause of the allergy remains obscure. It is possible that allergy was caused by short and intermittent contact of the skin with the rubber gloves used by the nursing personnel.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1600-0536.1987.tb01482.x
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  • 3
    Electronic Resource
    Electronic Resource
    Hepatic, intestinal and renal transport of 1-naphthol-β-d-glucuronide in mutant rats with hereditary-conjugated hyperbilirubinemia (1989)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 340 (1989), S. 588-592 
    Details
    ISSN: 1432-1912
    Keywords: Mutant rats ; Liver ; Intestine ; Kidney ; 1-Naphthol-β-d-glucuronide
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Recently, a mutant rat strain was described with a genetic defect for the biliary excretion of organic anions (TR− rats). To determine the possible heterogeneity of the transport systems in liver, intestine and kidney we investigated the transport of the anion 1-naphthol-β-d-glucuronide (1-NG) in isolated vascularly perfused organ preparations of the rat liver, intestine and kidney of both Wistar rats and TR− rats. 1-NG was administered as such (liver and kidney experiments) or formed intracellularly from 1-naphthol (1-N) (liver and gut experiments). Independent of the type of exposure to 1-NG, the biliary excretion was considerably impaired in TR− rats. In the intestine the total appearance and the vascular/luminal distribution pattern of 1-NG were not significantly different from the values in control rats. Furthermore, no significant disturbance was found with respect to the renal clearance of 1-NG in the TR− rat when compared with the Wistar rat. Thus, the genetic defect in the TR− rat is restricted to an impaired hepatobiliary excretion of 1-NG and does not affect the excretory systems of the intestine and kidney. These results suggest that the excretion of 1-NG by the liver, intestine and kidney involves distinct organ-specific transport systems.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00260615
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  • 4
    Electronic Resource
    Electronic Resource
    Absorption and presystemic glucuronidation of 1-naphthol in the vasculary fluorocarbon emulsion perfused rat small intestine: the influence of the luminal flow rate and intraluminal binding (1989)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 340 (1989), S. 583-587 
    Details
    ISSN: 1432-1912
    Keywords: Intestinal absorption ; 1-Naphthol ; Glucuronidation ; Rat ; Albumin binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Using an isolated vasculary perfused rat small intestine we studied the role of luminal flow rate and intraluminal binding on the absorption of 1-naphthol (1-N) and the intestinal metabolism of 1-N to 1-naphthol-β-d-glucuronide (1-NG). Raising the luminal perfusion rate resulted in a decrease in the luminal 1-N extraction ratio and an increase in the luminal 1-N clearance Cl lum. The dependency of Cl lum on flow rate appeared to conform to a convective diffusion model. A differential susceptibility of 1-N absorption and the total 1-NG appearance to the luminal flow rate resulted in a flow-dependent first-pass effect of 1-N. Next, the effect of intraluminal binding on 1-N disposition was studied in experiments in which albumin was added to the luminal perfusion fluid. The unbound concentration, as the driving force for the uptake of 1-N, seems not to be rate-limiting for the appearance of 1-NG. The total appearance of 1-NG in the presence of albumin was greater than would be anticipated from the free concentration of 1-N. As a result the extent of presystemic extraction increased with increasing albumin concentration. The precise mechanisms responsible for the phenomenona are not entirely clear. Consideration of the heterogeneity in the glucuronidation capacity along the rat small intestine and along the crypt-villus axis can help to explain the obtained results.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00260614
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  • 5
    Electronic Resource
    Electronic Resource
    Absorption and presystemic glucuronidation of 1-naphthol in the vascularly fluorocarbon emulsion perfused rat small intestine (1989)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 340 (1989), S. 239-245 
    Details
    ISSN: 1432-1912
    Keywords: Intestinal absorption ; Vascular perfusion ; Glucuronidation ; 1-Naphthol ; Rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Using the isolated vascularly fluorocarbon emulsion perfused rat small intestine some factors which determine the extent of the intestinal glucuronidation of 1-naphthol to 1-naphthol-β-d-glucuronide were studied. Increasing the luminal 1-naphthol concentration resulted in a concomitant increase in the 1-naphthol appearance in the vascular perfusate. In contrast, the total appearance of 1-naphthol-β-d-glucuronide increased less than proportional to the increase in the luminal 1-naphthol concentration. About 88% of the total amount of 1-naphthol-β-d-glucuronide excreted was released into the vascular perfusate. The capacity-limited intestinal glucuronide efflux is most likely due to saturation of the excretory mechanism for 1-naphthol-β-d-glucuronide. Decreasing the vascular flow rate influenced both the appearance of 1-naphthol and 1-naphtol-β-d-glucuronide in the vascular perfusate, whereas the appearance of 1-naphthol-β-d-glucuronide in the luminal perfusate was essentially flow-independent. A noradrenaline-induced change in the haemodynamic state of the vascular bed (with the total flow kept constant) resulted in a marked decrease in the 1-naphthol vascular concentration. The vascular 1-naphthol-β-d-glucuronide concentration was only slightly affected. These results indicate that changes in blood flow and blood flow distribution within the intestinal wall can affect the extent of presystemic intestinal metabolism by interfering with the absorption of the parent compound and the efflux of formed conjugates. These parameters can be of paramount importance for causing variable intestinal first-pass effects of drugs in vivo.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00168975
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  • 6
    Electronic Resource
    Electronic Resource
    A ready-to-use activated charcoal mixture (1989)
    Springer
    Pharmacy world & science 11 (1989), S. 56-60 
    Details
    ISSN: 1573-739X
    Keywords: Adsorption capacity ; Charcoal, activated ; Clearance enhancement ; Paracetamol ; Poisoning ; Theophylline
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A practical, ready-to-use preparation of activated charcoal (AZU mixture) for application in toxicology has been formulated. Tb establish its efficacy, the formulation was testedin vitro and in dogs. Thein vitro adsorption capacity was compared to that of freshly prepared charcoal suspension in water (CW) and to Carbomix®. Langmuir adsorption coefficients demonstrated small but clinically insignificant differences in adsorption capacity between the preparations. The laxative sodium sulfate did not reduce the adsorption capacity of charcoalin vitro. Dogs were given 60 mg of paracetamol per kg as an oral solution followed by 5 g of activated charcoal preparation. The area under the plasma concentration versus time curve (control 2955±353 mg·min−1·1−1) was significantly reduced following CW (921±453) and AZU (786±270). The premixed AZU charcoal formulation is efficacious, inexpensive and overcomes the problems of bed-side preparation. An isolated vascularly perfused rat small intestine can be used to describe the effect of activated charcoal on the intestinal secretion of theophylline.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01962976
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