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Biomedical subjects

O Lafont

Publications and source records attributed to O Lafont.

At least 37 records · Page 2Linked to original sources

[A short letter revealing the concerns of XVIIIth century apothecaries].

A letter from Demoret, Paris apothecary, to Le Chandelier, Rouen apothecary, evoked the defense of the interests of the profession, the practice of the profession and the family life of apothecaries of the XVIIIth Century. The important question of the examinations of hospital apothecaries, called "gagnants-maîtrises", and the question of soft drinks makers sailing syrups were treated. The trouble caused by the public display of theriaca, the illness of an assistant or the inspection by guards and physicians were described. Drug supply by colleagues from another town was pointed out. Finally the family life showed the hardness of the period and the way the sons of an apothecary were educated. The interest of this text is that it gives the opinion of an individual concerning general matters.

Antidotes↗

[The Gallot affair, or the long history of drugs from the Flanders army].

After the war, for the Austrian succession, the drugs which had been prepared for the french army, operating in Flanders, were sold to a grocer from Rouen, Pierre Gallot. He tried during twenty years to sail these drugs, which were getting older and older. The apothecaries' community members made their best to avoid the dispensation of these faulty drugs by an unqualified person. These periods 1750, 1756-1758 and 1770-1771 were especially rich in incidents. Many documents allow to follow the evolution of the conflict. Finally the grocer was condamned.

Drug and Narcotic Control↗

Phenobarbital metabolism by hepatocytes isolated from rat.

In order to test the validity of the use of hepatocytes as an alternative to studies of metabolism in live animals, phenobarbital (PB) was applied at 37 degrees C to isolated rat hepatocytes, which had been previously induced by PB. The metabolites were extracted by ethyl acetate, at various pH, and identified and evaluated by GC-MS. PB was not metabolized to p-hydroxyphenobarbital as is usually the case in living animals, but it was transformed into sulphoconjugated 2-phenyl-gamma-butyrolactone. This pathway, beta-hydroxylation of the ethyl side chain followed by lactonization, previously described as a secondary metabolic pathway occurring during intoxications, was here the only observed biodegradation. These results show that it is not possible to use hepatocytes as an alternative to live animals.

Animal Testing Alternatives↗

[Clarification on publications concerning the synthesis of acetylsalicylic acid].

Charles Frédéric Gerhardt (1816-1856) mentioned in his Traité de chimie Organique (1854) a publication, in French (realized in 1852 but published in 1853) entitled "Researches on anhydrous organic acids" in which, was reported the reaction of sodium salicylate with acetyl chloride. He thought that the reaction product was an acid anhydride, but obtained really crude acetylsalicylic acid. Later on, but also in 1853, a publication in german, by the same author related the same experiments. Surprisingly only the second publication has been mentioned in most of the historical studies on the subject. Acetyl salicylic acid was identified and synthesised in 1859 by von Gilm by another method and the product obtained by Gerhardt was identified to it in 1869.

Acids↗

[Iminodimethylation, a method for pharmacomodulation in pyrimido-[3,4-a]-s-triazine series].

Primary amines react with two formaldehydes and compounds presenting two mobile hydrogen atoms, this reaction can be called iminodimethylation. This reaction can be used in order to perform a pharmacomodulation in the pyrimido [3,4-a]-s-triazine series. Against Epidermophyton floccosum, the activity is better when nitrogen 7 is not substituted, when the heroatom in position 2 is 0 instead of S and when an aromatic nucleus is directly linked to the nitrogen atom in position 3.

Antifungal Agents↗

GC-MS determination of phenobarbitone entrapped in poly-epsilon-caprolactone nanocapsules.

In order to evaluate the concentration of a hydrophilic drug, phenobarbitone, in a suspension of poly-epsilon-caprolactone nanocapsules, a gas chromatographic-mass spectrometric procedure, performed after methylation of the drug, was developed and validated. Free phenobarbitone (in solution in the liquid phase), released phenobarbitone (after opening the nanocapsules with ethyl acetate) and total entrapped phenobarbitone (after extraction with methylene chloride), were measured. Experimental results for four lots with various concentrations showed that the highest preparation of entrapped drug (80%) was obtained for a total concentration of 3.64 mg ml-1 in the nanocapsule suspension.

Drug Compounding↗

[Appreciation of the evolution of the price of drugs in Rouen from 1640 to 1788].

34 accounts of medicines found in the rolls of "Maîtrise Notre-Dame" of Rouen were studied. Data concerning clysters, ptysans, violet sirup, theriac, marsh-mallow paste and physic were particularly collected. Their interpretation showed a relative stability of the market prices of drugs and medicines, expressed in pounds, during a century and a half, in Rouen.

Antidotes↗

Gas chromatographic-mass spectrometric method for analysis of a pyrimido-s-triazine and some of its metabolites in dog urine.

3-Phenylpyrimido-[3,4-a]-s-triazines exhibit antiparasitic, antibacterial and antifungal activity. In order to study the metabolism of these heterocycles, 9,9-diethyl-3-phenyl-6,8-dioxo-2,3,4,5,6,7,8,9-octahydropyrimido[3 ,4-a]-s- triazine (TZ) was administered to dogs. Three potential metabolites were synthesized, and these models were identified and quantified with gas chromatography-mass spectrometry. The heterobicyclic compounds, TZ and its hydroxy derivative, underwent thermal degradation under chromatographic conditions. Dog urine spiked with the model metabolites was extracted, and the substances were quantified. The urine of dogs treated with TZ was studied, and two of the potential metabolites were recovered, identified and quantified.

Animals↗

[Not Available].

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France↗

[Preparation of monodesethylamodiaquine from human urine].

60 mg of monodesethylamodiaquine, the active metabolite of amodiaquine were prepared by extraction from human urine, at pH 11-12, using ethyl acetate. The purification was carried out by medium pressure liquid chromatography. The identity and the purity of the compound were checked by thin layer chromatography, 1H nuclear magnetic resonance and mass spectrometry.

Amodiaquine↗

Pharmacokinetics of pyrazinamide and its metabolites in patients with hepatic cirrhotic insufficiency.

The pharmacokinetics of pyrazinamide (Pirilène) and its metabolites are evaluated in ten subjects with hepatic insufficiency, after an oral dose of 19.3 +/- 0.6 mg.kg-1 and the results are compared to those of a group of nine healthy subjects (control group). The results exhibit a marked reduction of the pyrazinamide total clearance (0.48 vs 0.84 ml.min-1.kg-1) and an increase in half-life from 9.19 h to 15.07 h in the patients group. The area under the curve of pyrazinoic acid (the main metabolite) is increased from 97 to 280 mg.h.l-1 with a half-life twice as much as that of the control group. The hepatic insufficiency entails a marked reduction of the common posology as well as a closer survey of the biologic hepatic parameters and of uric acid the renal elimination of which is inhibited by pyrazinoic acid.

Adult↗

Pharmacokinetics of pyrazinamide and its metabolites in healthy subjects.

The plasma and urine pharmacokinetic parameters of pyrazinamide and of its metabolites (pyrazinoic acid, 5-hydroxy-pyrazinamide, 5-hydroxy-pyrazinoic acid and pyrazinuric acid) have been studied after a single oral dose of pyrazinamide 27 mg.kg-1 in 9 healthy subjects. Pyrazinamide was rapidly absorbed (tmax less than or equal to 1 h) and showed a short distribution phase followed by an elimination phase of t1/2 beta = 9.6 h. The close similarity of the apparent elimination rates of the metabolites led to a second trial of a single oral dose of pyrazinoic acid to evaluate the formation and elimination stages. The limiting factor was found to be the activity of a microsomal deamidase (pyrazinoic acid formation from pyrazinamide and 5-hydroxy-pyrazinoic acid formation from 5-hydroxy-pyrazinamide). In contrast, oxidation by xanthine oxidase occurred very rapidly (5-hydroxy-pyrazinamide formation and pyrazinoic acid catabolism to 5-hydroxy-pyrazinoic acid).

Chromatography, High Pressure Liquid↗

Haemodialysis of pyrazinamide in uraemic patients.

The pharmacokinetics of PZA during haemodialysis were determined in 6 patients with chronic renal impairment after a single oral dose of 25.7 (1.9) mg.kg-1. The dialysis clearance of PZA and of its metabolites were: pyrazinamide 132 ml.min-1; pyrazinoic acid 121 ml.min-1; 5-hydroxy-pyrazinamide 107 ml.min-1; 5-hydroxy-pyrazinoic acid 118 ml.min-1. The average amount extracted during a dialysis session of 4.1 h was 926 mg after an oral dose of 1700 mg. The high dialysability shows that PZA can properly be administered at the end of each dialysis session in the usual dose of 25 to 30 mg.kg-1.

Adult↗

[Not Available].

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Economics, Medical↗