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Biomedical subjects

G Jadot

Publications and source records attributed to G Jadot.

At least 37 records · Page 2Linked to original sources
PubMed1986

[Pharmacokinetic, biochemical and histological study of the carbamazepine-josamycin interaction in the rat following chronic administration].

The determination of possible modifications of pharmacokinetic parameters of carbamazepine by josamycin in an experimental study after chronic administration of the drugs in the rat was undertaken to assay, or not, the enzymatic inhibition hypothesis which is supported in human clinical studies. Our data do not show any alteration in the Cmax, Tmax and AUC parameters of carbamazepine (total and unbound fraction) in case of conjunction with josamycin, but an earlier increase of plasmatic concentrations. The biochemical parameters are not modified, but a significant decrease of total bilirubin compared with controls and carbamazepine alone. The histological study does not show any liver lesion.

Animals↗
PubMed1985

Valproate increases diazepam impregnation selectively in CNS of the rat after subchronic administration.

Valproate-Diazepam association is not unusual in the treatment of epilepsies. The present paper investigates in an experimental study the effect of sodium valproate (VPA) on the regional cerebral level of diazepam (DZP), and the relationship with plasma or erythrocytes amounts after subchronic administration. The VPA addition increases the DZP levels in peripheral and central compartments. The results shows a linear correlation between the drug concentration in all areas studied and the plasmatic or erythrocytic amounts during the CNS - impregnation phase. The VPA influence is greater in the CNS where the DZP impregnation is selectively increased, specially in cortex and cerebellum.

Analysis of Variance↗
PubMed1985

Circadian changes in procainamide and N-acetylprocainamide kinetics in the rat.

The aim of this study was to investigate the possible influence of the time of administration on procainamide and N-acetylprocainamide (NAPA) kinetics in the rat. A single 50 mg kg-1 i.p. dose of procainamide was given to Wistar AF SPF adult male rats maintained under controlled environmental conditions (LD: 06.00h-18.00h) at four different fixed times i.e. 10.00, 16.00, 22.00 and 04.00h. Procainamide and NAPA plasma levels were determined by an immunoenzymatic method. Our data showed significant 24 h variation of the following pharmacokinetic parameters: highest elimination half-lives at 10.00h (t1/2 beta = 0.736 +/- 0.020h) for procainamide and at 04.00h (t1/2 beta = 3.55 +/- 0.08h) for NAPA (P less than 0.001); highest apparent volume of distribution at 04.00h for procainamide (Vd = 2.35 +/- 0.17 litre) (P less than 0.05); highest ratio AUC NAPA/AUC procainamide at 04.00h (1.039 +/- 0.056) (P less than 0.001). Procainamide clearance and Cmax and AUC for procainamide and NAPA were not significantly dependent on time of day. These data indicate a 24 h variation in the metabolism of procainamide which is converted to NAPA, the N-acetylation being greatest at 04.00h.

Acecainide↗
PubMed1985

Effects of the 1,5-benzodiazepine clobazam on pituitary hormones in the male rat.

The aim of this study is to evaluate the effects of the acute and subchronic administration of the benzodiazepine clobazam (20 mg/kg orally) on the plasma levels of the pituitary hormones (prolactin, FSH and LH) in the male rat. This 1.5 benzodiazepine did not induce any variation of the hormone levels either after acute or subchronic administration. These negative data are discussed as compared to the effects of other benzodiazepines of GABA and GABA receptor agonists and antagonists on the pituitary hormone levels according to particular experimental conditions.

Animals↗
PubMed1984

Pharmacokinetic and anti-inflammatory properties in the rat of superoxide dismutases (Cu SODs and Mn SOD) from various species.

The comparison of the anti-inflammatory properties (carrageenan paw edema in the rat) of exogenous Cu SODs from various species and human Mn SOD administered at doses corresponding to clinical schedules, shows that human and bovine Cu SOD are fully active, whereas rat Cu SOD and Mn SOD are inefficient. This difference does not correspond to the similarity of pharmacokinetic properties (blood levels, subcellar location in kidney cortex) of the Cu proteins or to the increased circulating life time of Mn SOD. The pharmacological activity of exogenous SOD is limited to heterologous Cu SODs in the rat. A similar problem may occur in man. The true mechanism of action of Cu SOD remains to be elucidated.

Animals↗
PubMed1984

[Activity of clobazam on plasma prolactin and gonadotropins after administration of sulpiride in the male rat].

The acute administration of the 1,5 benzodiazepine clobazam (20 and 100 mg/kg orally) reduces the sulpiride-induced release of prolactin in the male rat. The decrease in prolactin plasma level is respectively of 66 and 75% for the two doses, whereas it has minimal effects on the gonadotropins (FSH and LH). The clobazam induced prolactin lowering effect is compared to the one observed after diazepam administration. Finally, we have shown that the two benzodiazepines have no effect either on prolactin or on gonadotropins, when administered alone.

Animals↗
PubMed1983

Antinociceptive action of sodium valproate in the mouse.

The antinociceptive action of sodium valproate (VPA) was examined using male NMRI mice. Using the hot-plate assay at 60 degrees C, orally-administered VPA (50-400 mg/kg) produced antinociceptive effects; the ED50 was about 160 mg/kg. Oral doses of VPA (6.3-400 mg/kg) decreased the writhing response elicited by intraperitoneally-injected acetic acid. The antinociceptive effect of VPA, as determined with the writhing test, exhibited complex characteristics, the most pronounced effect occurring at doses of 12.5-50 mg/kg. The antinociceptive effect of VPA in the writhing test was not antagonized by bicuculline or by naloxone. VPA, like other agents which enhance central GABA-ergic mechanisms, might possess analgesic activity.

Acetates↗
PubMed1983

[Alpha 1-acid glycoprotein and carbamazepine].

Levels of alpha 1-acid glycoprotein (alpha 1-AGP) were determined in 40 epileptic patients who had been also treated with carbamazepine (CBZ) and, in some patients, phenobarbital (PB) for at least 3 months. alpha 1-AGP levels were also determined in 28 controls. CBZ dit not alter blood levels of alpha 1-AGP while CBZ-PB decreased them. Such results are at variance with recent studies which suggested an increase of alpha 1-AGP in epileptic patients treated either with phenytoin or phenytoin + PB, or + CBZ, or + primidone.

Adult↗
PubMed1982

Sodium valproate: kinetic profile and effects on GABA levels in various brain areas of the rat.

1. The kinetic profile of sodium valproate (VPA) and the GABA levels were studied in discrete brain areas of the rat after an i.p. injection of 200 mg/kg. The results were discussed comparatively with GABA-T and GAD activities reported in the literature. 2. VPA was rapidly distributed in brain areas; its concentrations, its kinetic parameters and the GABA levels after the drug administration were not uniform in the different brain areas studied. 3. The results showed a particular relation of the VPA to the olfactory bulbs; in this specific area the VPA effect on GABA level was stronger; the VPA apparent half life of elimination was longest; the VPA apparent disappearance rate constant was smallest; the initial GABA level was higher; the activities of GABA-T and GAD were higher than in other brain areas studied except the hypothalamus. 4. These data were correlated with the role of the olfactory bulbs in the behaviour of the rodents.

Animals↗
PubMed1982

[Neuro-endocrine effects of chronic clonidine administration in rats].

Neuroendocrine effects of chronic clonidine administration - which has been proposed as antimanic drug - have been evaluated in the female rat for a twenty one days period at the following doses : 0,5 ; 5 ; 25 and 50 micrograms.kg-1.day-1. No modification of the evolution of the oestrus cycle was observed, whereas pituitary hormones (PRL, FSH and LH) plasma levels were not statistically modified. The results of this study are opposed to those frequently observed with classical neuroleptic drugs.

Animals↗
PubMed1982

[Absence of effects of sodium valproate on the estrous cycle of the rat].

Regarding interrelationships between epilepsy, antiepileptic drugs and neuroendocrinological events, sodium valproate effects on estrous cycle of the rat have been performed by daily vaginal smears for twenty one days with 200, 100, 20 and 10 mg per kg bodyweight. Our data showed that sodium valproate did not significantly modify the evolution of estrous cycle even if intracerebral GABA content increase has been reported to influence hormonal secretions.

Animals↗
PubMed1981

Circadian effect on carbamazepine kinetics in rat.

The purpose of the present study was to investigate whether the time of day (24 h) at which carbamazepine is administered influences its pharmacokinetics in the rat. The pharmacokinetics of a single, 100 mg . kg-1 bodyweight per os, dose of carbamazepine were studied at four different fixed time points of a 24-hour period (i.e. 10.00, 16.00, 22.00 or 04.00 h) in Wistar AF-SPF adult male rats maintained under controlled environmental conditions (LD: 18.00 - 06.00h) during October 1978. The total plasma levels and the unbound fraction were measured according to an immunoenzymatic method (EMIT). The effects of fasting were also investigated. The data shows circadian variations of pharmacokinetic parameters: the maximum peak concentration and the maximum time to reach this peak was observed when the drug was given respectively at 16.00h and at 10.00h. The elimination half-life varied from 15.15 hours at 16.00h to 10.48 hours at 22.00h. The observed variations may be related to: daily fluctuations of absorption or binding of the drug; diurnal variations of the hepatic drug metabolizing enzymes responsible for the inactivation; and/or diurnal variations in excretion rate of the drug.

Administration, Oral↗
PubMed1981

[Possible effects of propranolol on the estrous cycle of the rat].

Propranolol effects on oestrous cycle of the rat have been studied by daily vaginal smears for twenty one days with doses nearby similar to those used in psychiatric disorders (e.g. 3, 10 and 30 mg.kg(-1). Our data showed that propranolol did not modify the evolution of of oestrous cycles even if plasma prolactin levels have been increased by the highest dose used (30 mg.kg(-1).

Animals↗
PubMed1980

[An experimental study of veralipride (author's transl)].

The administration of doses of 0,001, 0, 01, 0,1, and 1 mg/kg/day of veralipride to female rats produces a dose-related blocking effect on dioestrus. No histological changes are noted in the genital tract and mammary gland tissues after 0,001 and 0,01 mg/kg/day. Doses of 0,1 and 1 mg/kg/day block ovulation and the resulting estrogen impregnation modifies the appearance of the uterine glands and vaginal epithelium. Mammotropic effects, seen as a moderate hyperplasia but without galactogenic secretion, occur after 1 mg/kg/day only.

Animals↗