[Dialysability of sulfonylurea compounds].
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Biomedical subjects
Publications and source records attributed to M Herrmann.
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The effect of the indirect sympathomimetic agent tyramine on the isoprenaline-induced increase in plasma renin concentration was investigated in conscious rats. Tyramine caused a dose-dependent decrease in the isoprenaline-induced elevation of plasma renin concentration. Pretreatment of the rats with reserpine abolished this effect of tyramine, indicating that tyramine released catecholamines which acted on the inhibitory adrenoceptors. Pretreatment with phenoxybenzamine, an alpha-adrenoceptor antagonist, also abolished the inhibitory effect of tyramine on renin release, indicating that alpha-adrenoceptors mediated the observed inhibition of renin release. In rats with chronically denervated kidneys tyramine did not inhibit renin release. It is concluded that catecholamines which are released from renal sympathetic nerve endings can suppress renin release by activating alpha-adrenoceptors.
The tissue adhesive Fimomed (made in GDR), which is supplied in a non-sterilised form, was tested for its bacteriostatic behaviour. No such behaviour was found for Gram-negative bacteria, so that in view of the typical microorganisme occurring in hospitals sterilisation of the adhesive by means of gamma rays or an aseptic filling by the manufacturers is suggested.
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Technology, evidence as well as indications and contraindications of the suprapubic bladder puncture are shown from a gynecological and obstetrical point of view. The bacteriological result of urine obtained by puncture from 476 women has been compared with that obtained subsequently by midstream voiding. It was proved statistically that bladder puncture yielded less positive results than midstream voiding. In 8.4 per cent of the cases there was a positive voided midstream urine culture with pathogenic bacteria while the samples of bladder puncture were sterile, thus 29.2 per cent of the positive voided midstream urine cultures proving to be "false-positive" concerning an infection of the bladder and of the upper urinary tract. The frequency of pathogenic bacteria, "apathogenic" bacteria and mixed cultures is given, divided into conforming and nonconforming culture results of puncture and midstream urines.
Ethyl (Z)-(3-ethyl-4-oxo-5-piperidino-thiazolidin-2-ylidene)- acetate (piprozoline, Gö 919, Problin) is a new potent choleretic which can be classified as a true cholepoietic agent. Accordingly the substance increases bile fluid and solid content as well. A dose-dependent choleretic effect could be shown in all species investigated. The choleretic effect of piprozoline is long-lasting and superior to that of the other choleretics compared with. There was a significant inhibition of experimentally induced liver damage in animals by piprozoline given prophylactically. Our experiments did not reveal any pharmacological properties interfering with the use of piprozoline as a choleretic.
A method has been described that enables to check secretory processes in animals directly. This has been demonstrated in dog exocrine pancreas stimulated by secretin and on bile secretion induced by sodium dehydrocholate. The design of this method permits to run experiments on pancreas and choleresis separately as well as simultaneously. The directly recorded absorption curves are in good agreement with the data obtained from the collected fractions. Based on the optical density curves, it is possible to determine the contents of the fractions more directly and more specifically. It is also possible to study kinetic problems and time dependent reactions by using this method and this design.
Ethyl (Z)-(3-ethyl-4-oxo-5-piperidino-thiazolidin-2-ylidene)-acetate (piprozoline, Gö 919, Probilin) and its main metabolite Gö 3284 induce a strong choleretic effect in dogs after i.v. and i.d. administration as well. Intestinal absorption is fast, and already 3.5 min after administration of the substances a rise of the bile volume and of the optical density of the secreted bile can be observed. The secretion rates of bile solids and bile acids per time (min) increase almost at the same time, too. Moreover, piprozoline presumably stimulates the synthesis of bile acids and of the other matter in addition to the raised secretory rate. In the group of choleretics, piprozoline is to be placed among the cholepoietics. Under the influence of piprozoline and Gö 3284, the content of solids sometimes decreases for a short period immediately after administration of substances. A strong linear correlation occurs between the secretion rate of bilirubin and bile acids. The increase of bile volume under the influence of piprozoline and Gö 3284 may be seen as osmotic effects caused by the stimulation of the bile acid dependent and the bile acid independent (Na+-ion dependent) canalicular mechanisms of choleresis.
The compatibility of ethyl (Z)-(3-ethyl-4-oxo-5-piperidino-thiazolidin-2-ylidene)acetate (piprozoline, Gö 919, Probilin) was tested orally in rats and intragastrically in dogs for 6 months. Moreover, the effect of the substance was studied on pregnant rats and rabbits and their foetuses after intragastric administration and on the fertility and breeding capacity of rats after oral application. In the course of the chronic experiments, in the highest dosage group of rats a slight sedation and a decrease of body weight gain and food intake could be observed. The female animals showed an enlargement of the adrenal glands. A small hyperemesis was noted in the highest dosage group of dogs. Subtoxic doses applied to rats and rabbits during gestation did not induce malformations in the newborns. Even treatment with large doses did not influence fertility and breeding capacity.
Ethyl (Z)-(3-methyl-4-oxo-5-piperidino-thiazolidin-2-ylidene)acetate (etozolin, Gö 687, Elkapin) is a diuretic with a new chemical structure. Animal experiments with etozolin showed low toxicity, potent diuretic and saluretic properties with a mild onset of action. A marked antihypertensive effect was found in long-term experiments in hypertensive rats. In investigations concerning general pharmacology etozolin showed no effects which stand against its use as a diuretic.
The tolerance of ethyl (Z)-(3-methyl-4-oxo-5-piperidino-thiazolidin-2-ylidene)acetate (etozolin, Gö 687, Elkapin) has been investigated over 18 months after oral administration in rats and over 1i months after intragastric application in dogs. Further the influence of the compound on pregnant animals and their fetuses after intragastric application has been investigated in rats and rabbits. The investigation of the influence on fertility and breeding capacity as well as on the peri- and postnatal development was carried out in rats after peroral administration. In the course of the chronic experiments a dose related increase of the excretion of fluid and electrolytes was observed. Side-effects, which mainly occurred during the last weeks of the experiment in the highest dosage group, were most probably due to the exhaustion of the fluid and especially of the electrolyte reserves of the animals. The experiments in rats and rabbits did not yield any findings indicating teratogenic properties. Fertility and breeding capacity were likewise not influenced by etozolin. An influence on the peri- and postnatal development could be demonstrated only in the toxic dose range.
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A crude human hypophyseal extract (HE), as well as human growth hormone (GH), ovine prolactin (PRL) and commercial preparations of ACTH, TSH, pregnant mare's serum gonadotrophins (PMS) and chorionic gonadotrophin (CG) were tested for their ability to induce the activities of cytoplasmic 17 beta-hydroxysteroid dehydrogenase and microsomal delta 4-5alpha-hydrogenase and to repress the activities of microsomal 3alpha- and 3beta-hydroxysteroid dehydrogenases in the liver of hypophysectomized rats. The activity of 17beta-hydroxysteroid dehydrogenase was not affected by any of the administered hormones. For the other enzymes, only PRL was effective in causing changes in the activities; the repressive effect on 3alpha-hydroxysteroid dehydrogenase activity was highly significant (P less than 0.001). These results indicate that PRL is involved in the regulation of at least some of the enzyme activities of hepatic steroid hormone metabolism.
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