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Biomedical subjects

H Larsson

Publications and source records attributed to H Larsson.

At least 163 records · Page 9Linked to original sources
PubMed1983

Studies of blood viscosity with a newly constructed rotational viscometer which operates via a desk top computer.

Increasing interest is being shown in blood viscosity and the whole field of haemorheology. This study presents a newly constructed rotational Couette type viscometer which operates via a commercially available desk top computer and a digital plotter. The influence of haematocrit on blood viscosity is shown and the study also presents blood viscosity values of six to eight healthy men at 24 degrees C and 37 degrees C. At 37 degrees C values are shown both at natural haematocrit and at haematocrit 45%.

Blood Viscosity↗
PubMed1983

Inhibition of gastric acid secretion by omeprazole in the dog and rat.

The gastric antisecretory properties of omeprazole, a new potent substituted benzimidazole, have been evaluated in dogs and rats. Omeprazole was compared with another benzimidazole, picoprazole (H 149/94), and with the histamine H2-receptor antagonist cimetidine. The intravenous or intraduodenal administration of omeprazole in the gastric fistula dog inhibited histamine- and pentagastrin-stimulated acid secretion. The intravenous and intraduodenal, ED50 values for inhibition of histamine-stimulated secretion were 0.35 and 0.26 mumol/kg, respectively. Omeprazole was found to be approximately 5-10 times more potent than both picoprazole and cimetidine. After oral omeprazole administration in the Heidenhain pouch dog, the ED50 on histamine-stimulated acid secretion was found to be 1.2 mumol/kg, which corresponded to a potency 2 and 3.5 times greater than that of cimetidine and picoprazole, respectively. Measurement of the plasma concentration of unchanged omeprazole revealed an intraduodenal bioavailability of approximately 70% whereas the oral bioavailability was only approximately 15%. This variation is probably a result of partial degradation of omeprazole in the acid gastric juice. Single intraduodenal doses of omeprazole had a long-lasting inhibitory effect on histamine-stimulated acid secretion in the dog. After a dose of omeprazole, which produced total inhibition initially, the antisecretory effect was detectable for 3-4 days. Omeprazole inhibited basal and stimulated acid secretion in the rat. The intravenous ED50 was calculated to be 1.5 mumol/kg, whereas the oral potency was about 10 times lower. The effect in the rat was also of long duration. After a dose giving maximal inhibition, control acid secretion was restored after approximately 13 h.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed1982

Nucleation of actin polymerization from profilactin. Opposite effects of different nuclei.

The lag in polymerization of calf spleen profilactin in response to addition of MgCl2 can be overcome by small amounts of spectrin-actin-band 4.1 complex, covalently crosslinked actin oligomers or sonicated F-actin. All of these factors also nucleate polymerization of pure actin. Another nucleator of actin polymerization, villin, delays filaments formation from profilactin. A simple model of the interaction of profilin with actin can explain these apparently conflicting results in terms of the polarity with which actin filaments elongate from the different nuclei.

Actins↗
PubMed1982

Pharmacokinetics of parenteral and oral melperone in man.

The pharmacokinetics of melperone (Buronil, Ferrosan, Sweden) was studied after administration of various parenteral and oral doses to man. After parenteral administration, the data could be fitted to a two-compartment model, but after oral dosing the distribution phase could not be separated from the elimination phase, and so an one-compartment model gave the best fit. The half-lives were about 3-4 h, except after intramuscular injection, when the half-life was about 6 h. The bioavailability of oral doses was about 60% of the intravenous injection. After the highest oral dose of 100 mg, the pharmacokinetics, expressed as AUC or Cmax, showed non-linearity, possibly due to saturation of the hepatic elimination system.

Administration, Oral↗
PubMed1981

Pharmacokinetics of propranolol.

The pharmacokinetics of propranolol after the administration of 40, 80, and 120 mg p.o. and 10 mg i.v. was studied in nine healthy male volunteers. Propranolol was analyzed after extraction and derivatization by gas-liquid chromatography. A multiexponential curve-stripping program was used for the pharmacokinetic analysis. The volume of distribution was about 6 liters . kg-1, bioavailability around 25%, with a mean terminal half-life of 6 hr. There was no evidence of either dose dependent disposition kinetics or an oral threshold dose. A slight increase in urine volume was observed after propranolol administration.

Adult↗
PubMed1981

Pharmacokinetics of bendroflumethiazide after low oral doses.

The pharmacokinetics of bendroflumethiazide after oral administration of 1.25, 2.5, and 5.0 mg were studied in nine healthy male volunteers. Bendroflumethiazide was analyzed by GLC after extractive alkylation. After the lowest dose, the plasma concentration, could be followed to 14 hr, and the data were adequately fitted by a one-compartment model; the half-life was 3.1 hr. After the 2.5 and 5.0 mg doses, the plasma concentration was followed for 24 hr, and the data were fitted by a two-compartment model with half-lives of 8.9 hr. The urinary sodium concentration was doubled after bendroflumethiazide intake, but the urinary potassium concentration remained almost constant. The renal clearance of bendroflumethiazide was around 30 ml . min-1.

Bendroflumethiazide↗
PubMed1981

Metabolism of femoxetine.

The metabolism of femoxetine, a serotonin uptake inhibitor, has been investigated in rats, dogs, monkeys, and human subjects using two 14C-femoxetine compounds with labelling in different positions. The metabolic pathways were oxidation (and glucuronidation) and demethylation, both reactions most probably taking place in the liver. Nearly all femoxetine was metabolised, and the same metabolites were found in urine from all four species. Only a small percentage of the radioactivity excreted in the urine was not identified. Rat and dog excreted more N-oxide than monkey and man, while most of the radioactivity (60-100%) in these two species was excreted as two hydroxy metabolites. The metabolic pattern in monkey and man was very similar. About 50% was excreted in these two species as one metabolite, formed by demethylation of a methoxy group. A demethylation of a N-CH3 group formed an active metabolite, norfemoxetine. The excretion of this metabolite in urine from man varied from 0 to 18% of the dose between individuals. Most of the radioactivity was excreted with the faeces in rat and dog, while monkey and man excreted most of the radioactivity in urine. This difference in excretion route might be explained by the difference in the metabolite pattern. No dose dependency was observed in any of the three animal species investigated.

Animals↗
PubMed1980

The effect of melperon on ocular readaptation time, as assessed by a new recording technique.

A new simplified technique recording readaptation time after photo stress, RAT, is described. The psychometric properties in terms of internal consistency and retest reliability were tested, and the effect on RAT after intake of melperon at two different dose levels was investigated and correlated to blood plasma levels. The results show that there was a satisfactory consistency of RAT at each occasion but stability over a 1 month period could not be demonstrated. Significantly dose-dependent changes were recorded after intake of melperon but the prolongation of RAT was not significantly correlated to blood plasma levels.

Adaptation, Ocular↗
PubMed1979

Differences in microtubule stability to colchicine in extracts of guinea pig, rat and rabbit brain.

1. Microtubules (MT) from a guinea pig brain 25,000 g supernatant are not depolymerized by colchicine in contrast to MT from similar preparations of rat and rabbit. 2. The colchicine-stability was lost if the guinea pig brain homogenate was centrifuged at a higher g-level, further purified or if only the grey matter was used. 3. The association constant of colchicine to tubulin did not differ between a stable and a labile guinea pig brain preparation. 4. The GTP-hydrolysis was higher in the guinea pig preparation containing stable MT, than in the preparation containing labile MT. Additional GTP added to the polymerized MT before colchicine exposure, labilized the MT. Preincubation with NaF decreased the GTP-hydrolysis and caused a colchicine depolymerization. 5. The results indicate species differences in colchicine sensitivity of in vitro polymerized MT, probably depending on differences in GTP-hydrolysis.

Animals↗
PubMed1979

Pharmacokinetics of femoxetine in man.

The pharmacokinetics of a structurally new 5HT-uptake inhibitor, femoxetine (FG 4963), with antidepressant properties have been investigated in man using a radioactive as well as a non-labelled substance. A two compartment open model gives a good description of the data, both after oral and intravenous administration. The substance was almost completely absorbed after an oral dose, but only 5-10% reached the systemic circulation due to extensive first pass metabolism. The metabolites had distribution and excretion rates similar to the parent compound. Only a small part (less than 2%) was excreted as femoxetine in the urine. The urinary excretion of the parent compound varied more than a 100-fold depending on the pH of the urine. The urine pH, however, did not influence the plasma concentration of femoxetine. Most of the substance (up to 80%) was eliminated by urinary excretion of metabolites, and only a small part of the radioactive dose was excreted in the faeces (up to 11%). The pharmacokinetic parameters were not found to be dose dependent in the range investigated, but it was not possible to decide whether the bioavailability was dependent on the dose. The variation between subjects was rather large, giving only a limited possibility for prediction of the plasma concentration from one subject to another.

Administration, Oral↗
PubMed1979

The effect of oxazepam on ocular readaptation time.

The readaptation time (RAT) is the interval during which a person exposed to a bright intense light flash cannot perceive a given target. In this study the target used was an optokinetic pattern and the elicited nystagmus (OKN) was registered with electrooculography (EOG), thus giving an objective registration of RAT. Oxazepam in therapeutic doses was given to five healthy subjects and the RAT and serum concentrations of the drug were registered simultaneously at different time intervals. An almost parallel increase of RAT and serum concentration of oxazepam was recorded. This suggests that RAT reflects the depressant effect on the CNS of this drug and it may be used as an objective method of following the clinical effect of a depressant drug as a function of time after intake.

Adaptation, Ocular↗
PubMed1978

Tocopherol and local X-ray irradiation of two transplantable rat tumours.

The influence of tocopherol in an intramuscular dose of 5 mg/100 g body wt. on the effect of local X-ray irradiation of 2 intramuscularly transplanted tumours in the rat was studied. A significantly enhanced effect of irradiation by tocopherol was found, in contrast to the tumour radioprotecting effect with large doses of tocopherol earlier described in literature.

Animals↗