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Biomedical subjects

H Lauressergues

Publications and source records attributed to H Lauressergues.

At least 19 recordsLinked to original sources
PubMed1991

Pharmacological study in vivo of the new topical anti-inflammatory steroid 21-thiol-9 alpha-fluoro-11 beta,17 alpha-dihydroxy-16 alpha-methyl-3,20-dione-21-acetylamino cysteine.

The pharmacological evaluation, using animal models, of 21-thiol-9 alpha-fluoro-11 beta, 17 alpha-dihydroxy-16 alpha-methyl-3,20-dione- 21-acetylamino cysteine (CMJ), a new steroidal anti-inflammatory compound, is reported. The results obtained show a significant anti-inflammatory activity for CMJ. Comparison with dexamethasone indicates that CMJ is about 9 to 10 times less active in vivo. Of particular interest, however, is the dissociation of local and systemic activities of CMJ, since this compound was shown to be practically devoid of systemic activity (about 970 times less active than dexamethasone) after subcutaneous administration in rats. It is therefore expected that the topical use of CMJ in therapy may not cause the side effects provoked by many of the corticosteroids currently used.

Abscess↗
PubMed1984

Lotifazole (F 1686), a non-steroidal anti-inflammatory agent with an unusual pharmacological spectrum.

Lotifazole (F 1686) - 4-phenyl-2-(2',2',2-trichloroethoxycarboxamido) thiazole - has a range of anti-inflammatory activities in animals that differs from the activities of classic non-steroidal drugs. It reduces carrageenin-induced oedema in rats, UV-induced erythema in guinea pigs, and Arthus pleurisies in rats only at high doses. It does not affect Freund's-adjuvant polyarthritis, and it only slightly affects passive skin anaphylaxis in rats and anaphylactic shock in guinea pigs. Lotifazole does not greatly inhibit prostaglandin synthesis. However, at low doses and after various conditions of treatment, F 1686 reduces PPD- and Bordetella- pertussis-induced delayed-hypersensitivity pleurisy in guinea pigs and rats, respectively, and contact hypersensitivity reactions to picryl chloride and oxazolone in mice. Its action on the two models of delayed-hypersensitivity pleurisy is reflected in a decrease of the pleural exudate and of the number of mononuclear cells in the focus of inflammation. At active doses, Lotifazole does not cause changes in the differential leukocyte count in normal animals. It appears, furthermore, to be a T-lymphocyte stimulant.

Anaphylaxis↗
PubMed1984

Pharmacological study of cantharidin-induced ear inflammation in mice.

Cantharidin applied to the Swiss mouse ear induced a clearly observable inflammatory reaction after 6 hr, maximal after 24 hr, and persisting several days. Desonide and hydrocortisone strongly inhibited the acute (6 hr) and delayed (24 hr) phases after their local application, while, after oral treatment, a reduction in the acute edema was obtained only when using high doses. The cutaneous application of high doses of mepyramine, disodium cromoglycate, methysergide, and (at a quite lower level) cimetidine reduced the 6-hr inflammation. Phenylbutazone and acetylsalicylic acid showed little activity on the same phase after their cutaneous administration. All the nonsteroid compounds produced little or no effect on the 24-hr inflammation after their cutaneous application and were quite inactive on both phases after their systemic treatment. The cantharidin-induced inflammatory reaction in Swiss mouse seems thus to be characterized by two phases. The chronic delayed phase is an example of chronic inflammation without the involvement of immunological processes. Histamine and serotonin might be involved in the acute inflammation.

Administration, Oral↗
PubMed1984

Pharmacological comparison of the immune and non-immune inflammations induced by picryl chloride and oxazolone in mice.

Picryl chloride applied to the ears of Swiss mice induced a clearcut primary irritation inflammation (maximal after 3 to 6 hr) and after contact sensitization performed 7 days before a delayed hypersensitivity reaction. Oxazolone produced only a weak primary irritation reaction. After contact sensitization in the same conditions as above, oxazolone induced an immune response that was already substantial 3 to 6 hr after the challenge and generally reached a maximum after 24 hr. We tried to alter these four types of inflammation (the primary irritation and delayed hypersensitivity to picryl chloride, and the 6-hr and 24-hr phases of hypersensitivity to oxazolone) by various types of compounds administered cutaneously or sytemically. Mepyramine, methysergide, cimetidine, disodium cromoglycate, phenylbutazone, and acetylsalicylic acid reduced to varying degrees after cutaneous application the primary irritation and the delayed hypersensitivity inflammation induced by picryl chloride. Methysergide was the only one of these drugs that on topical application clearly reduced the immune response to oxazolone (decrease in the 6-hr phase). After systemic administration, these same drugs had no effect on the four types of reaction. Both the corticosteroids tested (hydrocortisone acetate and desonide) reduced all the inflammations to various degrees and were always more active (particularly desonide) when applied topically than when administered systemically. On the other hand indomethacin, which inhibited all types of inflammation, was more active when administered systemically. Study of the kinetics and trials of pharmacological modulation of the various reactions induced by picryl chloride and oxazolone in Swiss mice provided evidence of differences in behavior between the two agents.

Adrenal Cortex Hormones↗
PubMed1983

Pharmacological study of the antitussive and respiratory-analeptic properties of N-(2'-ethylpyrrolidino)diphenylacetamide hydrochloride (F 1459).

The antitussive and respiratory stimulant properties of N-(2'-ethylpyrrolidino)diphenylacetamide hydrochloride (F 1459) in animals are reported. In the mechanical stimulation of the trachea in guinea pigs and after intraperitoneal administration of the product, F 1459 showed a better antitussive action as compared to oxeladin, zipeprol, codeine and clobutinol. Low intraduodenal doses of F 1459 also reduced in cats the cough induced by the electrical stimulation of the superior laryngeal nerve. In anesthetized dogs whose respiratory functions had been depressed by morphine, F 1459 significantly increased the volume inspired per minute, an effect not due to any uncoupling effect on oxidative phosphorylation. F 1459 has local anesthetic and broncholytic properties that may play a role in the mechanism of its antitussive action. Contrarily to codeine, the test compound did not induce a decrease in the intestinal transit.

Anesthetics, Local↗
PubMed1982

Modulation by various locally applied anti-inflammatory and anti-allergic compounds of the immune and non-immune inflammation induced by picryl chloride in mice.

The authors studied the primary irritation and contact delayed hypersensitivity inflammation induced by picryl chloride in mice. The primary irritation reaction was induced by the application of various concentrations of the phlogogenic agent on an ear. Seven days after contact sensitization of the animals on their shaved abdomen, the immune inflammation was also induced on an ear by various doses of picryl chloride. Clear 24 hour-delayed hypersensitivity reactions were induced only by picryl chloride doses that induced a primary oedematous irritation 3 to 6 hours after application. After selection of the 3%-concentration of picryl chloride for challenge on ear, attempts were made to modulate these two types of reaction pharmacologically with various anti-allergic or anti-inflammatory compounds mixed with the inflammation-inducing agent. The inhibition of the non-immune reaction by mepyramine, methysergide, and the two anti-allergic compounds F 1865 and disodium cromoglycate demonstrated the participation of histamine and serotonin in this inflammation. Vasoactive amines seemed also to be involved in the immune reaction, but to a lesser extent. Hydrocortisone reduced the two types of inflammation by the same amount, while desonide had more effect on the delayed hypersensitivity reaction. In addition, both indomethacin and acetylsalicylic acid affected the two reactions equally, whereas phenylbutazone had a greater effect on the primary irritation inflammation.

Administration, Topical↗
PubMed1982

Anti-allergic properties of ethyl-3-methoxyphenyl-4-thiazolyl-2-oxamate (F 1865).

F 1865 (ethyl-3-methoxyphenyl-4-thiazolyl-2-oxamate) has powerful oral anti-allergic properties in immediate hypersensitivity models in rats. In IgE-dependent passive cutaneous anaphylaxis (PCA) the ED50 was of 0.8 mg/kg. In IgG-dependent PCA the ED50 was of 0.6 mg/kg. This oxamate derivative inhibited the liberation of histamine during passive peritoneal anaphylaxis in rats at concentrations of 1 X 10(-6) M or higher. Doses of F 1865, active in PCA, had only weak anti-histamine and anti-serotonin effects, as measured by the increase of cutaneous capillary permeability. Likewise, its inhibitory effect on the bronchospasm due to histamine or serotonin in guinea-pigs was apparent only at doses of 1 mg/kg on i.v. administration. At doses of 100 mg/kg (X2) p.o., F 1865 was inactive against reverse passive Arthus pleurisy induced in rats by rabbit anti-bovine-albumin serum.

Amino Acids↗
PubMed1982

Modification of two models of Arthus reaction in the rat by various drugs.

The action of several steroidal and non-steroidal antiinflammatory agents, immunosuppressives, and antirheumatics (levamisole, chloroquine, sodium aurothiopropanol sulphonate, D-penicillamine) was studied in two models of Arthus-passive reaction in the rat: paw oedema induced by an anti-ovalbumin serum, and pleurisy induced by an anti-bovine-albumin serum. The steroidal antiinflammatory agents reduced both types of reaction. In pleurisy, they acted on exudate and the number of neutrophils. The non-steroidal compounds were not active on the inflammatory reaction of the paw, but they decreased the volume of exudate in pleurisy without having any clear effect on cellular phenomena. The antirheumatics and immunosuppressives showed little or no action on the two models: of these only gold salt decreased Arthus reaction in the paw.

Animals↗
PubMed1981

Differential effects of itanoxone--a new hypolipidemic and hypouricemic drug--on platelet and vascular prostaglandin generation in rats.

Itanoxone ((chloro-2'-diphenyl)-4-oxo-4 methylene 2-butyric acid), a newly developed, hypolipidemic and hypouricemic compound with moderate anti-inflammatory activity, showed a short-lived, dose-dependent (20--200 mg/kg, orally), apparently competitive inhibition of platelet malondialdehyde (MDA), stimulated by either thrombin or arachidonic acid. Repeated doses did not result in any cumulative effect. At doses which completely blocked MDA production, itanoxone also inhibited thrombin-stimulated thromboxane B2 production in platelets but had no measurable effect on vascular prostacyclin generation. Pretreatment with itanoxone partially prevented the inhibitory effect of aspirin on both platelet and vascular prostaglandin synthesis. This suggests that itanoxone--like aspirin--acts at the level of cyclo-oxygenase but with greater selectivity on the platelet enzyme. This pharmacological activity is of great theoretical interest for the potential use of this compound as an antithrombic drug.

Animals↗
PubMed1981

Plasma viscosity and biochemical parameters in the "fatty" rat.

The essential part played by rheological factors in the genesis of thrombosis and atherosclerosis has often been mentioned. Thus, we undertook an investigation on plasmatic rheological factors in an animal model with modifications in plasma lipids (homozygotic and heterozygotic "fatty" rats) compared to normal animals (Sprague-Dawley rats). Test parameters were: cholesterol, triglycerides, lipidograms, glucose, total proteins, fibrinogen, plasmatic viscosity. Experiments gave the following results in homozygotic animals as compared to heterozygotic rats and controls: hyperlipidemia with massive increase in triglycerides, hyperfibrinogenemia, increase in total proteins and glucose, modifications in lipidogram in the form of more lipoproteins migrating in the beta-position and fewer proteins migrating in the alpha-position. Such changes were accompanied by an increase in whole blood and plasma viscosity. After considering the various correlations between these parameters, the authors suggest the application of such an animal model to atherogenesis.

Animals↗
PubMed1980

Comparison of the effect of phenylbutazone, desonide and cyclophosphamide on four types of experimental pleurisy.

The action of phenylbutazone, a non-steroid anti-inflammatory drug, desonide, a corticosteroid, and cyclophosphamide, an immunosuppressant agent, was studied on four types of experimental pleurisy: carrageenan-pleurisy in rats; passive reversed Arthus pleurisy in rats; Bordetella pertussis-delayed hypersensitivity pleurisy in rats and PPD (purified protein derivative)--delayed hypersensitivity pleurisy in guinea-pigs. For each compound, the action on the exudate and on the number of the different categories of leucocytes in the inflammation focus was evaluated. In carrageenan-inflammation, phenylbutazone reduced the oedema and the number of neutrophils and macrophages. Its favourable effect on exudative events in Arthus--and B. pertussis--reactions was not accompanied by high modifications at the cellular level. With the exception of PPD-pleurisy, desonide reduced the three other reactions. Its action related to the exudate and the various leucocyte types, except in the Arthus reaction in which only the number of neutrophils was decreased. The effect of cyclophosphamide was mainly in B. pertussis pleurisy in which it resulted in a decrease of oedema and a reduction in the number of mononuclears. For each compound, correlations between the effect on exudative and cellular phenomena are discussed.

Animals↗
PubMed1979

Action of mannitol in various immunological experimental models.

The authors describe the inhibiting action of mannitol after repeated administration of low subcutaneous doses in a number of experimental immunological models. For example, in the rat it produces a reduction of the secondary arthritis of Freund's adjuvant polyarthritis and also of the pleurisy due to Bordetella pertussis hypersensitivity. In the mouse it reduces the reaction of delayed hypersensitivity to sheep red cells. Its action is also marked against ovalbumin-induced active skin anaphylaxis in the albino guinea-pig and on IgE synthesis in the rat. Moreover, after several injections it produces a reduction of carbon phagocytosis in the mouse. At the doses at which the effect appeared, no action could be found on various models of acute non-immune inflammation, diuresis, blood pressure, hematocrit and protein and plasma sodium levels.

Acute Disease↗
PubMed1979

Action of various drugs with anti-inflammatory or anti-rheumatic properties on pleurisy due to Bordetella pertussis hypersensitivity in the rat.

The authors studied various drugs with anti-inflammatory or antirheumatic properties on pleurisy due to Bordetella pertussis hypersensitivity in the rat. The following compounds were studies according to various methods of treatment: indomethacin, phenylbutazone, cyclophosphamide, desonide, chloroquine, levamisole, D-penicillamine and sodium aurothiopropanol sulphonate. The action on the volume of pleural exudate and on cell events depended on the compounds and the conditions of treatment. Only gold salt produced no reduction in the pleural volume under all methods of treatment. All the compounds studied produced various degrees of significant modifications at the level of the cell events.

Animals↗