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C Larousse

Publications and source records attributed to C Larousse.

At least 37 records · Page 2Linked to original sources

Viloxazine as a betamimetic antidepressant drug.

A comparison was made between the effects of maprotiline, the sole action of which is to inhibit the reuptake of noradrenaline, of salbutamol and of viloxazine on hypothermia induced by reserpine, oxotremorine or apomorphine. The dose/effect curves in the three tests showed a similarity in profile between viloxazine and salbutamol, whereas no resemblance was evident between these two drugs and maprotiline. These facts suggest that viloxazine which has a weak effect on noradrenaline reuptake acts probably as antidepressant by betamimetic activity.

Albuterol↗

Effects of kainic acid on hypothermia induced by reserpine, oxotremorine and apomorphine in mice.

Antagonists of the norepinephrine reuptake and beta-adrenoreceptor agonists are potent, at once, on the three following tests: antagonism of hypothermia induced by reserpine, oxotremorine and apomorphine. 2-Carboxy-4-isopropenyl-3-pyrrolidine-acetic acid (kainic acid), which is a powerful stimulant of the neurons and a destroyer of the dopaminergic neurons, has been used in these tests to show if it is possible to antagonize hypothermia induced by different substances. The results obtained show that kainic acid is potent on these three tests, thus providing evidence that it is a stimulant of norepinephrine neurons as well as serotoninergic neurons, even if it is peripherically injected.

Animals↗

A barbital derivative as an atypical antidepressant drug in mice.

An isopropyl derivative of barbital (5,5-diethyl-2-(isopropyloxy)pyrimidine-4,6-dione, O2IB) was administered intraperitoneally 30 min before tests in mice. Former experimental investigations have shown that O2IB has an antidepressant psychopharmacological spectrum. It increases toxicity of yohimbine in mice at 175 mg/kg, antagonises from 50 mg/kg on hypothermia induced by a high dose of apomorphine and is active on the behavioural despair test at 125 mg/kg. These effects are those observed with classical antidepressants. Since phenytoin has an antidepressant profile in mice, carbamazepine is active on manic-depressive illness and beta-mimetic drugs are antidepressants, the question presents itself whether isopropylation or anticonvulsive activity is more important for the antidepressant psychopharmacological spectrum, or whether both are of equal importance.

Animals↗

Pharmacokinetics of isoniazid: influence of age.

The distribution of the acetylator phenotype of isoniazid was studied in 458 patients of different ages, and the influence of age on its apparent distribution volume, clearance and half-life was investigated in slow and rapid acetylators. The doses of isoniazid for the patients were determined according to the inactivation index method, as described by Vivien. Apparent distribution volume showed no difference between slow and rapid acetylators but it did decrease significantly with age. Clearance and half-life varied significantly in slow acetylators, and these variations led to a decrease in the necessary dose of isoniazid.

Acetylation↗

Piracetam interactions with neuroleptics in psychopharmacological tests.

Two psychopharmacological tests which usually predict neuroleptic activity were conducted after joint administration of piracetam and three neuroleptics (haloperidol, fluphenazine and sulpiride) chosen for their different chemical classes and dopaminergic affinities. In these tests, specific doses of the neuroleptics were used to determine whether piracetam induced potentiation or antagonism of their action. Overall, piracetam increased neuroleptic action regardless of the administration timetable used, but the interaction of fluphenazine differed from that of the other two substances, because piracetam did not modify its action in a specific test of the presynaptic DA-2 dopaminergic receptors. This variation for fluphenazine may be explained by the fact that its pKa value is closer to that of piracetam, thus preventing better bioavailability of the neuroleptic, or its better affinity for DA-1 dopaminergic receptors. Nevertheless, the variation may have been due to a differing affinity for dopaminergic receptors, although this hypothesis is not completely satisfactory because it does not account for differences due to the administration timetable. It is thus suggested that action occurs on nonspecific sites and has the effect of increasing overall neuroleptic bioavailability.

Amphetamines↗

A monitoring study of cardiotonic treatment by immunoenzymologic measurement of digoxinemia (emit).

We performed a study on 96 patients to compare monitoring by immunoenzymologic measurement (EMIT) of digoxinemia. In doing so, we uniquely relied on clinical and electrocardiographic results. Compliance was good because only 9 patients had a digoxinemia equal or below 0.8 ng/ml, but we emphasize that our patients were hospitalized. Correlation between intoxications and plasmatic levels shows that 5 patients presented clinical or electrocardiographic signs indicative of digitalis intoxication with a digoxinemia less than 2.5 ng/ml and 14 patients without intoxication with a digoxinemia higher than 2.5 ng/ml. We point out in this study that for EMIT immunoassay it is better to take 2.5 ng/ml as the concentration limit to be sure to avoid intoxication.

Adult↗

Pharmacokinetics of intravenous and intramuscular methohexitone in dogs.

Twenty-four dogs received methohexitone, either intravenously injected (2 mg kg-1 of a 1% solution) or intramuscularly (10 mg kg-1 of a 2% solution). Plasma methohexitone concentrations were measured by gas/liquid chromatography and pharmacokinetics were obtained from the general equations of a multicompartment model. Peak blood concentrations were equivalent following i.v. (18.2 +/- 9.9 mg 1(-1); at 30 s) and i.m. (19.1 +/- 5.6 mg 1(-1); at 3 min) injections. After i.v. injection a rapid distribution phase (half-life t 1/2 lambda 1; 1.3 +/- 0.5 min) was followed by an elimination phase (elimination half-life t 1/2 lambda z; 26.4 +/- 7.8 min). After i.m. injection the distribution phase was followed by two further phases (half-lives: 10.1 +/- 3.6 min and 75.6 +/- 22.6 min). The authors conclude that an i.m. dose five times as great as the i.v. dose produces equivalent peak blood concentration 30 s after i.v. injection and 3 min after i.m. injection. In addition, after i.m. injection of 10 mg kg-1 an additional compartment was apparent, indication substantial drug uptake by poorly perfused tissues.

Animals↗

[Association of Recklinghausen's disease with carcinoid of Vater's ampulla. A new nosologic entity: apudoma. A case].

The coexistence of neurofibromatous skin lesions and carcinoid of Vater's ampulla is not fortuitous. The melanocytes in the brownish pigmented skin lesions bind DOPA, while the chromaffin cells in the digestive tumour contain cytoplasmic granules where precursors of amines with digestive activity are synthetized and stored. DOPA is one of these precursors. Both diseases, therefore, are interrelated by a common embryological origin: the neural crest.

Adult↗

[Simultaneous study of the induction effect of rifampicin and the phenotype for acetylation of isoniazid in 21 patients with tuberculosis undergoing a combination treatment].

Enzyme induction during an antituberculous treatment with Rifampin, Isoniazid and Ethambutol was studied in 21 patients with tuberculosis. Two tests were used: increase in urinary excretion of D-saccharic acid and decrease of the half-life of antipyrineee. Induction is constant with D-saccharic acid. On the other hand there is a significant decrease in the half-life of antipyrin in only 10 patients. There is an increase in the 11 other patients: all of them are slow acetylators for isoniazid. We suggest that INH has an inhibitor effect on the hydroxylation of antipyrin. This study allows us to discuss the interactions of drugs with INH and Rifampin, as well the predominance of rapid acetylators among subjects suffering of isoniazid hepatitis, recently questioned.

Acetylation↗

Tuberculosis therapy and enzyme induction in man.

The enzymatic inducing effect of an antituberculous treatment (Rifampicin, Isoniazid and Ethambutol) is tested by recording variations in the urinary D-glucaric acid elimination and in the antipyrine half-life test, measured before starting treatment and after two weeks of treatment. This study concerns 21 patients: 14 are slow acetylators and 7 are rapid acetylators of isoniazid. After two weeks of treatment an increase of the urinary glucaric acid elimination is observed but variations in the antipyrine half-life test are not univocal and allow us to separate two categories of patients: 10 have a significant decrease of antipyrine half-life, 11 have not. A link seems to exist between the rapid acetylator phenotype and this enzyme induction which is revealed by the antipyrine test. An interpretation of these two enzyme induction tests, the nature of the rifampicin inducing action and its relation to the acetylator phenotype are discussed.

Acetylation↗

Research on the eventual enzymatic induction activity of cetiedil in rat and man.

Therapeutic consequences of the enzyme induction phenomenon are briefly reminded. This action was investigated: 1.--In the rat: by measuring the P450 Cytochrome content of hepatic microsomes in rats treated with Cetiedil. The results were compared with those obtained with controlled rats in similar conditions who had received either phenobarbital or no drugs at all. 2.--In man: by measuring the urinary elimination of D-glucaric acid and by measuring the plasma half-life of antipyrine before and after Cetiedil. These results in man were compared with similar results obtained before and after treatment with Rifampicin. Cetiedil does not seem to produce any increase in hepatic enzyme activity.

Adult↗

Rifampicin.

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Animals↗

Methodology and results of a survey of adverse reactons to a drug in private practice.

A survey of tolerance of a drug, determined in private practice under "naturalistic" conditions by 591 physicians, and involving 22277 patients is presented. The procedure used in private practice to gather systematic information about reactions to the drug involved a system of data sheets with detachable cards for optical reading and computer analysis. The survey was conducted under the responsiblity at regional level of a team of scientific coordinators-hospital pharmacologists and poison control centres. Possible side effects were noticed in 13,82% of patients, a figure similar to known nocebo reactions. Tolerance was significantly related to sex, age, weight, geographical area, duration of treatment, association with other durgs and therapeutic result. When related to individual physicians, the overall number of side effects and the frequency of three of them in particular did not follow a binomial distribution; the rate of adverse reactions was significantly related to the number of years of practice of the physicians.

Adult↗