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Biomedical subjects

K H Beyer

Publications and source records attributed to K H Beyer.

At least 55 records · Page 3Linked to original sources

[Pentazocine--an addiction problem? (author's transl)].

Pentazocine dependencies are rare. In a period of 5 years, 60 were notified. The majority of these were not dependent. Of 46 utilizable notifications, 38 were false, 5 had taken pentazocine only temporarily or not at all. 19 received it for chronic or recurrent pains, 13 were polytoxicomaniacs, and 1 patient could not be classified. Only 8 cases could be referred to as pentazocine-dependent. The dose for addicts and polytoxicomaniacs was 11 ampoules daily on the average, almost three times as high as that for patients with painful diseases. Pentazocine dependencies are considerably less of a problem than those of opiates used up to now: withdrawal symptoms are slight, neglect and social dangers need scarely be considered. "Users" generally only turn to pentazocine when a painful disease supervenes. Dependency practically never occurs with oral administration.

Adolescent↗

A career or two.

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Animals↗

Saluretic and uricosuric effects of (6, 7-dichloro-2-methyl=1-oxo-2-phenyl-5-indanyloxy) acetic acid (MK-196) in the chimpanzee.

The saluretic and uricosuric responses elicited by a novel agent, MK-196, have been studied in a great ape, the chimpanzee. This agent is orally active at very low doses and has a prolonged duration of action. Probenecid does not appear to influence the saluretic and uricosuric properties of MK-196. Net tubular secretion of urate was reduced by MK-196. Urinary pH changes did not compromise the efficacy of this new agent. On a dose basis, MK-196 was more saluretic (and uricosuric) than ethacrynic acid or furosemide and possessed a longer duration of action. Because of the marked natriuresis caused by MK-196, some increase in potassium excretion occurred.

Animals↗

Effects of enzyme induction and inhibition on microsomal oxidation of 1,4-benzodiazepines.

Metabolic oxidative profiles of diazepam (I) were obtained by aromatic C-4'-hydroxylation, N-1-demethylation, and 3-hydroxylation using a supernatant of rat liver. Incubation of 3-methyldiazepam (VI), which suppressed 3-hydroxylation, and N-1-nor-3-methyldiazepam (VII), were used to separately investigate these three oxidative pathways. Treatment of animals with phenobarbital enhanced N-1-demethylation and 3-hydroxylation, and to a variable extent C-4'-hydroxylation. Application of metyrapone reduced metabolite formation by 3-hydroxylation and N-1-demethylation, but had no effect on C-4'-hydroxylation. Metyrapone inhibition was more pronounced following than prior to phenobarbital treatment. C-2-hydroxylation was studied using medazepam (XX) incubations. This pathway was increased by phenobarbital pretreatment and reduced by metyrapone inhibition which was again more pronounced following than prior to phenobarbital pretreatment. These results support earlier conclusions on the heterogeneity of liver microsomes and suggests the presence of different species of hepatic microsomal terminal oxidases. Phenobarbital treatment and metyrapone change the metabolic profile via induction and inhibition, respectively, and, thus, in the case of 1,4-benzodiazepines, the formation of metabolites with varying pharmacological activity. This could become important in clinical situations as a diagnostic mean to determine induction under various treatment or, possibly, during cumulation of metabolites with a long half-life.

Animals↗

[Effect of naftidrofuryl on creatinine serum concentration and on PAH/inulin clearance in peripheral arterial occlusive diseases].

The effect of 200 mg 3-(1-naphthyl)-2-tetrahydrofurfurylpropionic acid beta-diethylaminoethylester (naftidrofuryl, Dusodril) administered as a single i.v. infusion, on serum creatinine was investigated in 10 patients with occlusive disease of the peripheral arteries (average age 58.6 years). In a second group of similar patients (average age 60.5 years) determinations of PAH/inulin clearance and serum creatinine were performed prior to and immediately after treatment with 400 mg naftidrofuryl per day over a period of two weeks. Creatinine concentration did not change following acute or chronic administration of naftidrofuryl; glomerular filtration rate and renal plasma flow were not affected by prolonged treatment (2 alpha less than 0.05). An obligatorily nephrotoxic effect of naftidrofuryl can therefore be ruled out.

Aminohippuric Acids↗

Functional characteristics of the renal tubular secretion of amprolium, a quaternary organic base.

Amprolium [1-(4-amino-2-propyl-5-pyrimidinemethyl)-2-methyl-pyridinium chloride hydrochloridel is a basic (quaternary) organic compound. At very low plasma concentration, it is cleared by the kidney at a rate approximating renal plasma flow in the dog. Its renal clearance is not depressed by organic acids (p-aminohippurate or probenecid) but is reduced by the quaternary base, mepiperphenidol. Acetate and pantothenate may influence the clearance of amprolium but, if this is the case, the effect is less than for p-aminohippurate. Its clearance is depressed as urinary pH is increased. The clearance of amprolium was not altered over a substantial range in urine flow at either high or low urinary pH.

Acetates↗