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  • 1
    Electronic Resource
    Electronic Resource
    The anti-inflammatory activity of Ebselen but not thiols in experimental alveolitis and bronchiolitis (1988)
    Springer
    Inflammation research 24 (1988), S. 313-319 
    Details
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract This paper describes the effects of the thiol compounds glutathione and N-acetylcysteine and the seleno-organic agent Ebselen on the development of Sephadex-induced lung edema and cell infiltration in the rat. Neither thiol had any effect upon the development of the edema when administered in large, repeated doses. In contrast, when Ebselen was co-administered with the thiols, there was a dose-dependent inhibition of the development of the edema, but lung weights could not be returned to normal values. However, when the thiols were omitted and Ebselen was administered alone, the development of the edema was totally blocked. In addition, in Ebselen-only treated animals there was a selective inhibition of the infiltration of lymphocytes, basophils and eosinophils into the lung lumen without affecting the populations of macrophages and neutrophils. Again, the Ebselen-induced effect was reduced by coadministration of either thiol. These findings are discussed in terms of the potential mechanism of action of Ebselenin vivo and of the possibility of Ebselen being of therapeutic potential in cases of diffuse pulmonary inflammation in humans.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02028288
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  • 2
    Electronic Resource
    Electronic Resource
    Topical and systemic glucocorticoid potencies of budesonide and beclomethasone dipropionate in man (1982)
    Springer
    European journal of clinical pharmacology 22 (1982), S. 523-529 
    Details
    ISSN: 1432-1041
    Keywords: beclomethasone diproprionate ; budesonide ; glucocorticoids ; aerosol ; plasma cortisol ; differential WBC ; topical effect ; topical administration
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Topical anti-inflammatory (cutaneous “vasoconstriction”) and systemic glucocorticoid (depression of plasma cortisol and changes in differential WBC count) potencies of the two glucocorticoids budesonide and beclomethasone dipropionate (BDP) were compared in human volunteers. After topical application, budesonide was 2–3 times more potent than BDP in inducing “vasoconstriction”. After oral administration, on the other hand, budesonide was 2–4 times less potent than BDP in depressing plasma cortisol and changing the total or differential WBC. After inhalation, too, significant differences in favour of budesonide were noted, but the divergence between the drugs was less pronounced. The improved relationship between the topical and systemic glucocorticoid effects of budesonide makes it a promising alternative for aerosol treatment in asthma.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00609625
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  • 3
    Electronic Resource
    Electronic Resource
    Glutathione peroxidase-like activity of diaryl tellurides.
    Amsterdam : Elsevier
    Bioorganic & Medicinal Chemistry Letters 3 (1993), S. 2553-2558 
    Details
    ISSN: 0960-894X
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Chemistry and Pharmacology , Medicine
    Type of Medium: Electronic Resource
    URL: http://linkinghub.elsevier.com/retrieve/pii/S0960-894X(01)80715-0
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  • 4
    Electronic Resource
    Electronic Resource
    Antioxidant activity of some diarylselenides in biological systems
    Amsterdam : Elsevier
    Free Radical Biology and Medicine 16 (1994), S. 17-28 
    Details
    ISSN: 0891-5849
    Keywords: Antiinflammatory ; Antioxidant ; Diarylselenide ; Free radicals ; LTB"4 ; Lipid peroxidation ; PGE"2
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Biology , Chemistry and Pharmacology , Medicine
    Type of Medium: Electronic Resource
    URL: http://linkinghub.elsevier.com/retrieve/pii/0891-5849(94)90238-0
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  • 5
    Electronic Resource
    Electronic Resource
    Topical anticolitic efficacy and selectivity of the glucocorticoid budesonide in a new model of acetic acid-induced acute colitis in the rat (1994)
    Oxford, UK : Blackwell Publishing Ltd
    Alimentary pharmacology & therapeutics 8 (1994), S. 0 
    Details
    ISSN: 1365-2036
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Aims: To study the effect of local or parenteral administration of the glucocorticoid budesonide in the acetic acid-induced colitis model in the rat.Methods: Colitis was induced in an exteriorized colonic segment by administration of 4% acetic acid for 15 s. Four days later, this colonic segment with colitis was examined using a morphological scoring system, and measurements of myeloperoxidase activity and of plasma exudation into the colonic segment. The experimental colitis showed morphological similarities to human ulcerative colitis, with 3-fold increase in myeloperoxidase activity and 6-fold increase in the plasma exudation. Budesonide in different doses administered for 3 days, starting one day after acetic acid instillation, prevented the development of colitis in a dose-dependent manner. The best effect of budesonide on the morphological score was achieved after local treatment at a dose of 10″5 M twice daily (76% reduction compared with a control colitis group) and parenteral treatment with 0.75 mg/kg (80% reduction). These doses also normalized myeloperoxidase activity and significantly reduced the plasma exudation. The systemic effects of the drug were most pronounced in the group treated with parenteral budesonide. This group showed the greatest reduction in body weight and a significant reduction of the weight of adrenal glands and spleen (as compared to controls). Thymus weight in animals treated systemically was significantly lower than in locally treated animals. In the group treated with local budesonide the weight of adrenals was reduced. However, the weights of spleen and thymus were not reduced and the reduction of the body weight was even less than in the control group.Conclusion: Local treatment with budesonide at a dose of 10−5 M (0.17 mg/kg if completely absorbed, but only 0.03 mg/kg with 15% bioavailability on colonic application) was as effective as parenteral treatment at a dose of 0.75 mg/kg in the attenuation of acetic acid-induced colitis in the rat, but resulted in minor systemic side-effects.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1365-2036.1994.tb00311.x
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  • 6
    Electronic Resource
    Electronic Resource
    Gut mucosal uptake and retention characteristics contribute to the high intestinal selectivity of budesonide compared with prednisolone in the rat (2001)
    Oxford UK : Blackwell Science Ltd
    Alimentary pharmacology & therapeutics 15 (2001), S. 0 
    Details
    ISSN: 1365-2036
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Budesonide and prednisolone are both effective for the treatment of inflammatory bowel disease, but budesonide produces fewer adverse systemic effects. High first-pass hepatic inactivation of budesonide partially explains its favourable ratio between topical and systemic activity, but it is probable that its uptake and retention in intestinal target tissues are also contributory.〈section xml:id="abs1-2"〉〈title type="main"〉Aim:To compare the uptake and retention of radio-labelled budesonide and prednisolone in rat ileal mucosa in vivo.〈section xml:id="abs1-3"〉〈title type="main"〉Methods: 3H-Budesonide and 3H-prednisolone were applied for 10 min directly to a perfused segment of rat ileum in vivo, followed by saline lavage every 10 min. Steroid uptake into the mucosa and submucosa was assessed at 20 min and 4 h. The uptake of budesonide was also measured in allergen-challenged animals vs. saline-challenged controls to assess whether inflammation of the mucosa with ongoing plasma exudation would impair its uptake.〈section xml:id="abs1-4"〉〈title type="main"〉Results:Budesonide was better absorbed into ileal tissue (15-fold at 20 min) than prednisolone and better retained (50-fold at 4 h) after topical administration. The uptake of budesonide was not impaired by exudation processes following allergen challenge.〈section xml:id="abs1-5"〉〈title type="main"〉Conclusions:The higher uptake and retention characteristics of budesonide in gut mucosa should contribute to its greater intestinal selectivity compared with that of prednisolone.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1046/j.1365-2036.2001.01129.x
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  • 7
    Electronic Resource
    Electronic Resource
    Biotransformation rate (in vitro) and systemic potency (in vivo) of the topical glucocorticoid budesonide in male and female rats
    Amsterdam : Elsevier
    Journal of Steroid Biochemistry 17 (1982), S. 703-706 
    Details
    ISSN: 0022-4731
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Biology , Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://linkinghub.elsevier.com/retrieve/pii/0022-4731(82)90574-X
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  • 8
    Electronic Resource
    Electronic Resource
    Influence of 16α,17α-acetal substitution and steroid nucleus fluorination on the topical to systemic activity ratio of glucocorticoids
    Amsterdam : Elsevier
    Journal of Steroid Biochemistry 16 (1982), S. 779-786 
    Details
    ISSN: 0022-4731
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Biology , Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://linkinghub.elsevier.com/retrieve/pii/0022-4731(82)90035-8
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  • 9
    Electronic Resource
    Electronic Resource
    Antigen-Induced Bronchial Anaphylaxis in Actively Sensitized SD Rats (1986)
    Oxford, UK : Blackwell Publishing Ltd
    Allergy 41 (1986), S. 0 
    Details
    ISSN: 1398-9995
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: We examined the effects of glucocorticosteroids (GCS) on antigen-induced bronchial anaphylactic reactions (BAR) in SD rats immunized with ovalbumin (OA) and alum. The animals were treated with vehicle, budesonide (BUD), dexamethasone (DEX), or hydrocortisone (HC) at various times before intravenous (i.v.) antigen challenge. The drugs were administered either intraperitoneally (i.p.) or intratracheally (i.t.); the BAR was elicited by a low or by a high challenge dose of antigen. A BAR elicited by a low challenge dose of antigen was reduced in a dose-dependent way by all GCS after i.p. administration; al 1 mg/kg, BUD and DEX significantly reduced BAR and at 50 mg/kg all three of the examined compounds inhibited the BAR by 50 % or more. For BUD, maximum effect was recorded when it was given 12 h before test. There was only a slight variation in the inhibitory effects of the GCS with immunization conditions of test animals. I.t. instillation of the drugs did not markedly increase their inhibitory capacity as compared to i.p. administration. BAR elicited by a high antigen dose was at best marginally affected by the GCS when given either i.p. or i.t. Thus, antigen-induced airway reactivity in rats can be reduced by GCS treatment provided that this is performed sufficiently long before the test and that the challenge dose of antigen is not too high.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1398-9995.1986.tb00302.x
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  • 10
    Electronic Resource
    Electronic Resource
    Antigen-Induced Bronchial Anaphylaxis in Actively Sensitized SD Rats (1986)
    Oxford, UK : Blackwell Publishing Ltd
    Allergy 41 (1986), S. 0 
    Details
    ISSN: 1398-9995
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: We studied the effects of anti-asthmatic and anti-inflammatory drugs on antigen-induced bronchial anaphylactic reactions (BAR) in Sprague Dawley (SD) rats immunized with ovalbumin (OA) and alum. The animals were treated locally (intratracheal instillation (i.t.) or by aerosol) with terbutaline (TERB), disodium cromoglycate (DSCG), theophylline (THEO), the xanthine derivative 3,7-dihydro-1,8-dimethyl-3-phenyl-1H-purine-2,6-dione (D4026), budesonide (BUD) or dexamethasone (DEX) at various times before intravenous (i.v.) challenge with OA. The BAR was elicited by giving a low dose of OA. When the response to that challenge had levelled an additional high dose of antigen was given. Previous work had shown that TERB, DSCG, and D4026 given systemically (i.v.) at a suboptimal dose, had a better inhibitory efficacy when the animals were challenged with a low antigen dose late (6 weeks) than when challenged early (2–3 weeks) after immunization. We show here that such a difference in efficacy is not recorded after local treatment. Moreover, each of the drugs inhibited BAR to the same extent after i.t. as after i.v. treatment. Potent drugs like TERB and D4026 seemed to show similar efficacy when given cither i.t. or by aerosol, whereas less potent drugs like DSCG and THEO were less effective when given by aerosol. In a previous study, we showed that the inhibitory capacity of glucocorticoids (GCS) on the BAR did not vary with sensitization conditions of the rats, BUD and DEX showed the same inhibitory capacity after intraperitoneal (i.p.) treatment as after i.t. treatment. In the present study, DEX showed increased whereas BUD showed decreased inhibitory capacity when given by aerosol 18–24 h before challenge. The duration of the anti-anaphylactic activity after inhalation was longer for DEX than for BUD.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1398-9995.1986.tb00352.x
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