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ABSTRACT: Twenty-seven human volunteer asthmatic patients were each given one tablet of mofebutazone (300 mg) twice daily for 15 days. Pulmonary ventilatory function test (forced expiratory volume test) as well as bronchoalveolar lavage (BAL) were performed one day before initiation of treatment and one day after completion of the course; in the BAL, prostaglandin E2 (PGE2), prostaglandin F2alpha (PGF2alpha) and leukotrienes (LTs) were also estimated. It was found that there was no increase in the incidence or severity of the asthmatic attacks during the course of mofebutazone treatment. The drug tended to improve the tested pulmonary ventilatory functions or at least to leave them unchanged. All the mofebutazone-treated individuals showed a dramatic reduction in the concentrations of PGE2, PGF2alpha and LTs in their BAL, but there was no consistent correlation between the extent of reduction and the degree of benefit or worsening sustained by any individual patient. It is evident from the present study that mofebutazone has shown good tolerability which was associated with an improvement in the pulmonary ventilatory functions, a fact that would seem to advocate the use of this non-steroidal antiinflammatory drug (NSAID) in asthmatic patients whenever a need for such therapy becomes necessary.
International journal of clinical pharmacology research 02/1995; 15(4):145-51.
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ABSTRACT: The isolated perfused lung preparation from actively sensitized guinea-pigs was used; after it was challenged with antigen, mediators such as histamine, prostaglandins and leukotrienes were released into the lung effluent. It was found that treatment of the perfused lungs before and during challenge with mofebutazone (10 micrograms/ml) inhibited the immunological release of prostaglandins as well as leukotrienes. Phenylbutazone, on the other hand, at the same dose level inhibited the release of prostaglandins, whereas the release of leukotrienes was much less affected by the drug. Histamine release was not altered by either drug. When clinically mofebutazone tablets (300 mg) were given as an analgesic twice daily for 15 days to a number of asthmatic volunteers including 3 aspirin-sensitive individuals, there was no increase in the incidence or intensity of the asthmatic attacks, even in the aspirin-sensitive patients. Pulmonary ventilatory functions which showed a certain obstructive pattern were not worsened by the treatment and even tended to be somewhat improved.
International journal of clinical pharmacology research 02/1993; 13(5):255-61.
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ABSTRACT: Aqueous/alcoholic extracts of Populus tremula, Solidago virgaurea and Fraxinus excelsior (components of Phytodolor N) were tested individually and in 3 different combinations for anti-inflammatory activity using carrageenan induced edema and/or adjuvant induced arthritis of the rat paw. The tested combinations as well as the individual extracts significantly reduced the paw edema to varying degrees and also dose dependently inhibited the arthritic paw volume. The anti-inflammatory activity of the combinations was respectively comparable to the tested doses of diclofenac.
Arzneimittel-Forschung 04/1992; 42(3):333-6. · 0.72 Impact Factor
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ABSTRACT: The effects of radiation exposure and drug treatment on the immediate type of hypersensitivity reaction were studied. Guinea-pigs were sensitized by s.c. injections of antigen. The animals were killed 3 weeks later and the lungs were perfused through the pulmonary artery. The perfusate was allowed to superfuse a guinea-pig ileum to estimate its total content of mediators. Results revealed that the mere injection of antigen to the perfused lung resulted in the release of spasmogens which caused contraction of the guinea-pig ileum. Analysis of the effluent showed an increase in the amount of PGs (measured biologically) and histamine (measured fluorimetrically) released during challenge. The response of the ileum to the antigen challenge was inhibited by the infusion of diclofenac (20 micrograms.ml-1) or piroxicam (25 micrograms.ml-1). The drugs also inhibited the release of PGs and histamine from the perfused lungs. Exposure of animals to gamma-radiation, before sensitization, caused a reduction in the amount of mediators released during challenge. On the other hand, in nonsensitized animals, a single radiation dose level of 2 Gy caused fluctuation in the amount of PGs and histamine released during challenge throughout the 3 weeks period of the experiment. Diclofenac and piroxicam effectively reduced the amount of mediators released from sensitized perfused lung isolated from both nonirradiated and irradiated animals. This may, at least partly, explain their protective effect against the exaggerated inflammatory response following gamma-irradiation exposure.
Archives internationales de pharmacodynamie et de thérapie. 03/1989; 298:247-63.
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ABSTRACT: The anti-inflammatory activity of piroxicam was assessed after whole body irradiation in rats. Two models of inflammation, the carrageenan-induced oedema and the adjuvant-induced arthritis in rats have been utilised. Piroxicam at doses of 1, 5 & 10 mg kg-1 i.p. was effective in inhibiting the paw oedema produced in both models of inflammation. The inflammatory response in irradiated was significantly higher than that produced in normal animals and was dependent on the radiation dose level used (0.5-2 Gy). The effect of piroxicam on the late inflammatory response produced by exposure to 2 Gy was studied by measuring the carrageenan-induced oedema 4 h after irradiation and on the third and seventh day thereafter. The increase in paw volume was significantly suppressed in animals receiving the drug. Administration of piroxicam (5 mg kg-1) one hour before irradiation of animals at 0.5 Gy, produced inhibition to the exaggerated inflammatory response in irradiated animals. This suggests that piroxicam possibly owes its protective value to prevention of the increase in cellular permeability induced by radiation. Alternatively, the drug may exert this effect by inhibiting PG synthesis, thereby reducing their potentiating influence on the other mediators of inflammation. Furthermore, the inhibition of lysosomal enzyme release possibly induced by the drug may contribute to the probable reduction in the release of inflammatory mediators.
Pharmacological Research Communications 07/1986; 18(6):563-80.
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ABSTRACT: The effect of radiation exposure on the inflammatory process was studied in rats using the carrageenan-induced paw oedema and adjuvant-induced arthritis tests. Irradiation (0.5,1 and 2 Grays) resulted in a significant augmentation of the tissue response to carrageenan and the early phase of adjuvant-induced arthritis, but suppressed the late phase. Diclofenac (1-5 mg kg-1) effectively reduced the exaggerated inflammatory response in irradiated animals in both the carrageenan paw oedema and adjuvant-induced arthritis tests. The drug also had a prophylactic value in guarding against the induction of radiation damage. The inflammatory responses produced by irradiation and the benefits obtained by drug treatment may be related to changes in tissue prostaglandin levels and/or changes in the immune system.
British Journal of Pharmacology 06/1985; 85(1):45-50. · 4.41 Impact Factor
