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  • 1
    Electronic Resource
    Electronic Resource
    Pharmacological characterisation of cardiovascular histamine receptors in man in vivo (1982)
    Springer
    Journal of molecular medicine 60 (1982), S. 978-982 
    Details
    ISSN: 1432-1440
    Keywords: Histamine receptors ; H1-,H2-receptor antagonist ; Histamine injection ; Infusion ; Cardiovascular response ; Histaminrezeptoren ; H1,H2-Rezeptorantagonisten ; Histamininjektion ; -infusion ; karidovaskuläre Reaktionen
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung Es wird über pharmakologische Studien an Probanden berichtet, wobei systemisch Histamin, Impromidin und ihre Antagonisten getestet wurden. Exogenes Histamin, welches durch schnelle Injektion appliziert wurde, scheint nur H1-Rezeptoren zu stimulieren, weil die Wirkungen des Histamins allein durch Chlorpheniramin antagonisiert werden können. Die Effekte der kardiovaskulären H2-Rezeptorstimulation können am besten durch dauernde und hohe Dosen infundierten Histamins gezeigt werden. Sollen alle kardiovaskulären Reaktionen auf endogenes Histamin geblockt werden, so ergeben sich aufgrund der vorhandenen pharmakologischen Daten beim Menschen, daß diese am besten durch eine Kombination von H1- und H2-Rezeptorantagonisten erreicht werden können.
    Notes: Summary Data from pharmacological studies carried out in healthy subjects using systemic histamine or impromidine and their antagonists are reviewed. Exogenous histamine by rapid injection appears to stimulate only H1-receptors. Chlorpheniramine alone antagonised the responses to histamine. The effects of cardiovascular H2-receptor stimulation are demonstrated best by a sustained and large dose of histamine given by infusion. If it be considered desirable to antagonise all the cardiovascular responses to endogenous histamine, the available pharmacological data in man suggest this would be achieved best by a combination of an H1- and H2-receptor antagonist.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01716958
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of xamoterol after intravenous and oral administration to volunteers (1988)
    Springer
    European journal of clinical pharmacology 34 (1988), S. 469-473 
    Details
    ISSN: 1432-1041
    Keywords: xamoterol ; cardiac failure ; beta1-adrenoceptor partial agonist ; pharmacokinetics ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of xamoterol, a β-adrenoceptor partial agonist under clinical evaluation for the treatment of mild to moderate heart failure, have been studied in 12 healthy male subjects. They received 14 mg i.v. and oral doses of 50 and 200 mg as a tablet and 200 mg as a solution in a 4 way cross-over design. After i.v. dosing the elimination half-life was 7.7 h, the total body clearance was 224 ml·min−1 and the volume of distribution at steady-state (Vss) was 48 l. Sixty-two percent of the dose was recovered unchanged in urine. After oral doses, the absolute bioavailability of xamoterol was shown to be 5% irrespective of whether the dose was administered as a tablet or solution. Peak plasma concentrations occurred at about 2 h for the tablet dose and slightly earlier (1.4 h) for the solution. Peak plasma concentration, AUC and urinary recovery of unchanged drug increased in proportion to dose. The apparent elimination half-life after oral doses (16 h) was significantly longer than that observed after an intravenous dose. Despite the low bioavailability, the degree of inter-subject variability of oral bioavailability was small probably indicating that the controlling factor is the hydrophilic nature of the molecule rather than extensive first pass metabolism or poor dissolution of xamoterol from the tablet formulation.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01046704
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  • 3
    Electronic Resource
    Electronic Resource
    Single dose topical corticosteroid inhibits IL-5 and IL-13 in nasal lavage following grass pollen challenge (2005)
    Oxford, UK : Munksgaard International Publishers
    Allergy 60 (2005), S. 0 
    Details
    ISSN: 1398-9995
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Background:  Nasal lavage is a noninvasive method of obtaining inflammatory exudates following nasal allergen challenge (NAC), and permits cells and released mediators to be evaluated.Objective:  To determine the effects of a single dose of topical steroid on eosinophils and levels of chemokines and cytokines in nasal lavage fluid following NAC in patients with allergic rhinitis.Methods:  Patients with grass pollen seasonal allergic rhinitis (n = 32) out of the allergy season received either nasal budesonide (100 μg per nostril) or matched placebo before allergen challenge in a double blind two-way crossover design. A semi-automated mixed bead array system was employed to measure multiple chemokines and cytokines in small volumes (50 μl) of nasal lavage supernatants.Results:  Following NAC there was a rapid onset of nasal symptoms together with nasal eosinophilia, and the appearance of IL-5 and IL-13 in lavages between 4 and 8 h. Elevated levels of eotaxin, RANTES, IL-8 and MCP-1 were also detected following allergen challenge. A single dose of nasal budesonide caused a decrease in symptoms (P 〈 0.05) and nasal eosinophils (P 〈 0.05) with selective abrogation of IL-5 and IL-13 responses (P 〈 0.05), but a lack of effect on levels of eotaxin, RANTES, IL-8 and MCP-1.Conclusion:  This study suggests that a single dose of nasal steroid has the capacity to selectively abolish IL-5 and IL-13 responses following NAC. This model should be convenient for testing novel anti-inflammatory and immunoregulatory agents intended for the treatment of allergic rhinitis.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1398-9995.2005.00928.x
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    Paper (German National Licenses)
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