pharmacocinetic

No abstract text is available yet for this article.

No abstract text is available yet for this article.

No abstract text is available yet for this article.

No abstract text is available yet for this article.

In the capacity of an initial study both, the pharmacocinetics as well as the metabolism of etorphine were investigated. In a self-trial a bolus of 8 micrograms tritium-marked etorphine as administered intravenously and subsequently the half-lives in serum and urine were determined. To achieve this, etorphine and etorphineclucuronide were separated via HPLC and then quantified by measuring the radioactivity. The development of the concentrations was devided into 3 phases. Within the first phase half-lives of etorphine and etorphineglucuronide were found in the range of 0...

1. In mice isolated for one week and observed in pairs with non-isolated mice under a reversed beaker, the serotonergic agonist: 1-3-(trifluoromethyl)phenylpiperazine (TFMPP) increased the number of escape attempts. 2. A partial tolerance to this effect has been observed in mice which were tested a first time after administration of TFMPP one week sooner. 3. An analysis of this form of tolerance was carried out by changing successively and separately each of the events concomitant of this tolerance. 4. The results show that this tolerance is not a pharmacocinetic or a pharmacodynamic one...

Drug treatment of high blood pressure had important improvements is the last few decades, that allowed an efficiente control of hypertension, avoiding or stabilysing cardiovascular consequences. Non pharmacological management is always important; however most hypertensive patients need also drug treatment that is unavoiable in severe and in most cases of moderate hypertension. Borderline hypertension involves difficult decisions. Quantitative diagnosis of high blood pressure has been based on casual measurement...

No abstract text is available yet for this article.

Comparative review of widely used classic and modern antimycotic agents - Polyene-group, Griseofulvin, Tolnaphthate, 5-Fluorcytosin and the new Imidazolyl-group - in view of antimycotic, pharmacocinetic and therapeutic properties.

The present studies were carried out to obtain pharmacokinetic data about the elemination of intravenously administered alpha-Larabinofuranosidase from the blood stream and about the distribution and retention of the enzyme in different organs and in a transplantable sarcoma of mouse. The results were used for the planning of therapeutical experiments, in which detoxified transport forms of cancerostatic agents were to be toxified by exogenous enzymes specifically in the tumour tissue. The alpha-Larabinofuranosidase is eliminated from the blood circulation quite rapidly (half-life about 20 min); a large portion is apparently excreted through the kidneys...

Alternative current polarography has been applied to specific determination of INH and acetyl-isoniazide in serum and urine. Determinations can be achieved directly on diluted urines. The method allows measure of pharmacocinetic parameters and determination of acetylation phenotype following I.V. administration of the drug.

With different oral oestrogens it was studied, if relations are existing between pharmacokinetic and vaginal effect. By means of Karyopycnotic Index and Dynamic Oestrogenicity Index the cytological effect was quantified from a single dose of oestradiol valerianate, mestranol, ethinyloestradiol and 3 depot oestrogens proved on postmenopause women and compared with adequate pharmacocinetical investigations. The courses of oestrogen levels did not correlate with indices. Both methods of investigation do not compensate, but complete one another...

The methylmethacrylate-monomer deported into circulation from bone cement implantation during endoprothetic operation is subject to unaltered exhalation. Qualitative evidence of monomer excretion in the exhaled air is established in animal experiment. The quantitative determination of monomer in the exhaled air in man undergoing hip-joint replacement are stated and the method is demonstrated. Pharmacocinetically exhalation has priority over metabolisation.

Two series of work are reported. The first concerns the pharmacocinetic study of the product after it was administered through different ways and the corresponding evolution of PaCO2. The second study concerns the effect on pulmonary arterial pressure, blood gases and some parameters of ventilatory mechanics, of a perfusion of 200 mg of this product over a two hours period.

Severe acute gastrointestinal side-effects following high oral doses of metronidazole (6 g/m2) could be avoided by a combined oral and rectal application. With tablets and an enema (1 g metronidazole/2 ml) in a ratio 1:4 and an increased dosage of 10 g/m2, maximal serum concentrations of about 200 micrograms/ml are obtained like after an oral dosage of 6 g/m2. The maximal radiosensitizing effect on hypoxic tumor cells is seen five hours after oral application and seven hours after the combined oro-rectal application...

Azlocillin concentrations in the rabbit eye were studied after intravenous and subconjunctival injections. The following results were found: therapeutic levels of Azlocillin were achieved in the aqueous humor, using either way of administration. Concentrations of the antibiotic were much higher after s. c. injection than after i. v. administration. The pharmacocinetics of Azlocillin proved to be comparable to those of other penicillins. No antibiotic could be detected in the vitreous body, irrespectively of the administration...

After introductory notes on the history of heparin research the chemistry of this mucopolysaccharide is described. It is shown that the chemistry of heparin cannot be exactly described by one chemical formula because heparin represents a family of compounds with different chain-length. Molecular features responsible for the high structural specificity of anticoagulant activity are described. The present status of knowledge on the mechanism of the anticoagulant action of heparin is described in detail. It is shown that basic mechanism is the acceleration of the interaction of antithrombin III with the clotting factors IXa, Xa, XIa, XIIa, and thrombin which are known to be serine proteases...

Ten new cases of perhexiline induced peripheral neuropathies are reported. The authors emphasize the possible association of other neurological disorders: cerebellar symptoms in one case, complex tremor in two other cases, marked decrease of photomotor reflexes in one case and disgeusia in another one. The pharmacocinetic study of 4 cases revealed the presence of a low metabolism of the drug in one of them. Polymorphous inclusions have been seen in Schwann cell and endothelial cell cytoplasm in the three patients with electron microscopic study of the nerves...

N-Methyl-N-beta-chloroethyl-hydrazine and its benzaldehydhydrazone are two new cytostatic methylhydrazines. Administered intraperitoneally, they are more effective in inhibiting the ascites tumor growth (Ehrlich's carcinoma in mice and Yoshida sarcoma in rats) than procarbazine in vitro as well as in vivo. The intraperitoneal administration of hydrazone shows a minor effect on the solid tumor. This may be explained by a different pharmacocinetical behaviour. Hydrazone is less toxic than procarbazine.

A field-trial on Etofibrat was performed on 4405 patients suffering from primary and secondary hyperlipoproteinemia. The results were proved statistically. After a 3 to 4 weeks treatment the concentration of cholesterol as well as tryglicerides in the serum decreased significantly. After 6 to 8 weeks treatment the lipid-lowering effect was even stronger. Nearly 90% of the patients investigated gave a positive response to the treatment. Part of the population had undergone a treatment with other lipid-lowering agents before-most likely without sufficient success-in these cases a further lipid-lowering effect due to Etofibrat could be shown...