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Biomedical subjects

H Jacobi

Publications and source records attributed to H Jacobi.

At least 55 records · Page 3Linked to original sources
PubMed1980

[Metabolism and pharmacokinetics of acemetacin in man (author's transl)].

Metabolism and pharmacokinetics of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetoxy]-acetic acid (acemetacin, TV 1322, Rantudil) in comparison to equimolar doses of indometacin was investigated in human volunteers after a single oral application and in rheumatic patients after multiple application. After multiple application (t.i.d. for 10 days) of equimolar doses of acemetacin and indometacin, mean blood level curves. The bioavailability of acemetacin derived from these data, corresponds to that of indometacin, i.e., approx. 100%, whereas after a single dose bioavailability of acemetcin is found to be smaller (66% from blood level, 64% from urine). This difference between single and multiple application is explained by slow filling-up of compartments. Degradation of acemetacin occurs by esterolytic cleavage to indometacin, by O-demethylation and N-desacylation and by partial conjugation of all these compounds to glucuronic acid. Blood level ratios of acemetacin and indometacin are equal after single and after multiple application of acemetacin. Therefore, degradation of acemetacin is not induced after multiple application. After a steady-state has been reached half-life of elimination is 4.5 +/- 2.8 h, which is longer than for indometacin (2.2 +/- 0.5 h). Interindividual differences are in the same range as described for indometacin.

Anti-Inflammatory Agents↗
PubMed1980

[Toxicology of acemetacin].

Acute toxicity (DL50) of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetoxy]-acetic acid (acemetacin, TV 1322, Rantudil) was determined following different forms of application and in various animal species. Acemetacin was tolerated better than indometacin in all cases. Taking into consideration the anti-inflammatory effect (DE50 kaolin edema) a better therapeutic spectrum of acemetacin could be proved compared to a number of other anti-inflammatory agents on the market. The toxicity was typical for the symptoms of non-steroidal anti-inflammatory agents. During 6 months of chronic feeding studies in rats and monkeys better tolerance of acemetacin was observed. teratogenic effects in rats and rabbits were not traceable.

Aging↗
PubMed1978

[Problems of assessing the biological value of prostaglandin in vitro (author's transl)].

Isolated rat stomach strips were used to study the antagonism between psychotropic drugs and prostaglandin. It was found that the inhibited prostaglandin effect registered under the influence of psychotropic drugs in due not so much to the inhibition of synthetase action but rather to an inhibitory action on liberated prostaglandin. An atropine-like effect of the psychotropic drugs or an inhibition in the formation of endogenic prostaglandin in the walls are ruled out as possible explanations. The following possible explanations were discussed: a) the tested psychotropic drugs block prostaglandin receptors in the stomach; b) the test substances react with prostaglandin in the nutritive solution; c) the substances stimulate metabolic processes in the stomach wall that break down prostaglandin.

Animals↗
PubMed1977

[Pharmacology and toxicology of etofenamate. 1st Communication (author's transl)].

1. The reliable antiphlogistic action of 2-(2-hydroxyethoxy)-ethyl-N-(a,a,a-trifluoro-m-tolyl)-anthranilate (etofenamate active principle of Rheumon Gel) in various experimental inflammatory models in animals is demonstrated following oral and cutaneous administration. 2. The proven inhibition of inflammatory edema by chronic administration of Rheumon gel evidences the percutaneous absorption of the active principle through the intact skin. 3. The effect of Rheumon gel sets in independently of whether the gel is applied to normal or to pathologically inflamed tissue areas. 4. Gastrointestinal mucous tolerance is better for etofenamate than for flufenamic acid, phenylbutazone and other anti-inflammatory drugs.

Animals↗
PubMed1977

[Pharmacology and toxicology of etofenamate. 2].

1. Since the anti-inflammatory effect of 2-(2-hydroxyethoxy)-ethyl-N-(a,a,a-trifluoro-m-tolyl)anthranilate (etofenamate, TVX 485, Rheumon Gel) is occasionally stronger than that of flufenamic acid and as its toxicity is in the same range as that of the latter, a wider therapeutic margin may be expected for etofenamate in therapeutic use of Rheumon gel. 2. In subchronic oral administration, rats tolerated 22 mg/kg and dogs 100 mg/kg without any signs of toxicity. Sub-chronic cutaneous administration of Rheumon gel in pigs (2 g/kg) likewise showed no signs of toxicity. Thus, an adequate safety factor would seem to exist, bearing in mind the comparative daily dose in man of approx. 0.3 g gel/kg body weight. In histological tests oedema of kidney papillas or degeneration of papillas, respectively, could not be seen. 3. In the dose range tested, etofenamate shows no signs of teratogenic or fetotoxic effects in either rats or rabbits. 4. The evidence of the cutaneous absorption of etofenamate from Rheumon gel could be demonstrated by the biological effect in animal experiments.

Animals↗
PubMed1975

[Incidence of malignant tumors in childhood (author's transl)].

575 malignant tumors were treated in the Childrens Hospital of Freiburg University during the years 1957--1974. This means that 0.86% of all hospital admissions had a newly recognized malignant neoplasia. There was no increase in the relative frequency of tumor admissions throughout these years. The most frequent tumor groups were expectedly leukemias (41.8%), central nervous system tumors (25.6%), lymphosarcomas (6.3%), Hodgkin's disease (5%), and neuroblastomas (5%). In comparison to tumor statistics comprising whole populations instead of admissions to a single hospital the relative frequency of leukemias and CNS-tumors is higher in our series. This may due to selective admissions of patients with different tumors to different treatment centers rather than to a higher incidence of these neoplasias in this area.

Adolescent↗