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  • 1
    ISSN: 1432-1041
    Keywords: pirprofen ; pharmacokinetics ; old age
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma concentrations of pirprofen and of its pyrrol metabolite were assessed in 9 elderly patients (3 males, 6 females; mean age 76 years) suffering from chronic degenerative disease. Pirprofen 400 mg in 4 ml was administered i.m. and the pharmacokinetic profile of the drug and the metabolite was calculated. The AUC, Cmax and t1/2 of pirprofen were similar to those found in previous studies, and, as expected, those parameters for the pyrrol metabolite were lower (Cmax=2.8 µg/ml−1; tmax=6.4 h; AUC(0–32)=56.5 µg · h · ml−1). One patient (n=8) showed different pharmacokinetic behaviour, which is discussed. The data suggest that age has little influence on the pharmacokinetic of pirprofen, although unpredictable responses should always be considered in clinical practice.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 35 (1988), S. 81-83 
    ISSN: 1432-1041
    Keywords: pirprofen ; pharmacokinetics ; cerebrospinal fluid
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary We have measured the concentrations of pirprofen at various times in plasma and cerebrospinal fluid (CSF) samples, drawn during diagnostic myelography from 28 patients affected by sciatica. After intramuscular injection of 400 mg plasma concentrations of pirprofen reached a peak in 60 min then fell slowly. In contrast, the CSF concentration rose until 12 h and then fell. Pirprofen rapidly crossed the blood-brain barrier and was detectable in CSF at 15–30 min after injection. These results support the suggested hypothesis of a central analgesic action of pirprofen along with the known peripheral one. A new sensitive HPLC method was developed for measuring the concentration of pirprofen in the CSF.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1432-1041
    Keywords: Diclofenac sodium ; gut ; manometry ; motility
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In experimental animal models nonsteroidal anti-inflammatory drugs may influence gastrointestinal motility, but as evidence is lacking in man. The effect of diclofenac sodum 75 mg i.m. on the motor response of the upper gastrointestinal tract to food has been studied by manometry in 9 healthy volunteers. Diclofenac had no effect on the motor activity of the stomach, duodenum, or jejunum after a 605 kcal meal.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1600-0625
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Abstract: We have previously shown an imbalance of the antioxidant system in some cultures of normal melanocytes from patients with melanoma. In order to evaluate if the alteration of the antioxidants could be the basis of an increased sensitivity to exposure to peroxidative agents, in cultured melanocytes from normal individuals (n=11) and from patients with melanoma (n=11), superoxide dismutase and catalase activities were evaluated by spectrophotometer, and the levels of vitamin E and of the polyunsaturated fatty acid of cell membranes were determined by gas chromatography mass spectrometry. In 5 out of the 11 cultures of melanocytes from melanoma patients, with respect to those from normal individuals, a significant decrease of catalase activity (Cat) associated with an increase of vitamin E (Vit E) concentration was found, whereas no significant modification of superoxide dismutase activity (SOD) was observed. A wide range of variablity was detected in the percentage of the polyunsaturated fatty acids of the cell membranes and a correlation was found between the ratio SOD/Cat and the percentage of linoleic acid, indicating that the imbalance of the enzymatic antioxidants leads to a lipoperoxidative process. The electron microscopic examination of these cultures revealed many microvilli in the plasma membranes and nuclear infoldings and in the cytoplasm light vacuoles. Moreover some cells contained several dense bodies with a round shape and numerous spherical lamellae possibly representing immature melanosomes. Treatment with cumene hydroperoxide between 0.66 and 20 μM did not produce a significant modification of cell viability in melanocytes from normal individuals. On the contrary in melanocytes from melanoma patients correlated with the ratio Vit E/Cat, considered as a parameter of the antioxidant imbalance, a stimulatory effect was observed at 0.66 μM CUH and a cytotoxic effect at 20 μM. In conclusion our results suggest that a constutional alteration of the scavenger system could be present in normal melanocytes from melanoma patients and that this could be the basis for an increased sensitivity to pro-oxidant agents.
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    Springer
    Inflammation research 21 (1987), S. 121-129 
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Oxygen derived free radical release from activated neutrophils may be in part responsible of tissue damage in the acute phase of inflammation. We have shown that the methane sulfonanilide antiinflammatory agent nimesulide inhibits the respiratory burst of phagocytosing neutrophils without affecting their phagocytic or chemotactic responsiveness. In fact, chemiluminescence and superoxide anion generation by polymorphonuclear leukocytes (PMN) stimulated with zymosan particles or with the synthetic peptide FMLP are inhibited by nimesulide and its 4-OH metabolite in a dose dependent fashion without affecting cell viability. The control of the extracellular flux of radical species by phamacological compounds may affect the course of inflammation reducing tissue damage. Our data suggest that the inhibition of superoxide anion production by neutrophils is an additional mechanism of action of the antiinflammatory agent nimesulide.
    Type of Medium: Electronic Resource
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