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Biomedical subjects

C Harvengt

Publications and source records attributed to C Harvengt.

At least 145 records · Page 8Linked to original sources

In vitro binding of various biological substances by two hypocholesterolaemic resins. Cholestyramine and colestipol.

The ability of cholestyramine and colestipol, two hypocholesterolaemic resins, to bind in vitro several compounds such as vitamin B12, vitamin B12-intrinsic factor complex, folic acid, iron citrate and calcium chloride was investigated. Both resins bound to a high extent vitamin B12-intrinsic factor complex, folic acid and iron citrate; in addition, cholestyramine also caused appreciable binding of calcium. Throughout a large range of pH, there was no change in the binding capacity; however, at pH 2, cholestyramine exhibited a marked drop in the binding of tested substances (with exception of folic acid). By increasing the molarity of the solutions, the binding to the resins of vitamin B12-intrinsic factor complex and of calcium chloride was completely inhibited. In human gastric and duodenal juices, the uptake by the resins of the studied compounds depends on the molarity of the physiological medium tested and partly confirms the results obtained with aqueous solutions. These data obtained in vitro emphasize the necessity of regular monitoring these biochemical parameters during chronic treatment of hypercholesterolaemia conducted with these two resins.

Body Fluids↗

Clinical pharmacokinetic study of procetofene, a new hypolipidemic drug, in volunteers.

The clinical pharmacokinetics of a new hypolipidemic drug, procetofene (Lipanthyl), have been determined in 10 normolipemic volunteers after a single 300 mg dose and repeated 300 mg fractioned doses (b.i.d.) during 10 days, followed by an additional single dose (300 mg) on day 11. The peak plasma level of procetofenic acid, the circulating active metabolite, was observed after 4 or 6 hr. A steady-state plasma level above 10 microgram/ml was reached on day 5 and maintained to day 10 on continued fractioned administration. This mean plasma level was not reached during the single-dose study. A double-exponential plasma decay curve was observed in volunteers after repeated doses: alpha phase, 5.27 +/- 1.05 hr; beta phase, 21.73 +/- 1.07 hr. As shown by the urinary excretion data, the drug is poorly absorbed by the digestive tract, i.e., only about 30% is absorbed.

Adult↗

Dose-dependent effect of TRH on plasma oleic acid in man.

Administered to normal subjects of either sex, the TRH enhances the plasma oleic acid after 60 minutes without any significantly marked modification in the blood concentration of total FFA. The oleic acid increase is significantly dependent on the amount of administered TRH (200 microgram and greater than or equal to 400 microgram). It is accompanied by 1) a more or less pronounced but acute release of TSH, and 2) a rise in circulating T3 but a submaximal value within the time-course of the experiment (1 h). This elevation is presumably due to a preferential liberation of oleic acid by the adipose tissue, through a direct action of TSH and/or under the permissive influence of the thyroid hormone, among other factors that may intervene in the process.

Adult↗

Plasma clofibric acid (CPIB) levels induced by three marketed compounds releasing clofibric acid, in volunteers.

The very low plasma clofibric acid levels achieved in normolipemic volunteers during 96 h by a single dose of alufibrate (basic aluminum salt of clofibric acid) as 4 x 360 mg tablets, have been confirmed. With a crossover study in healthy volunteers receiving therapeutic doses of clofibrate as 2x500 mg capsules, clofibride as 2x450 mg capsules, twice daily for ten days, the plasma clofibric acid concentrations were already found in the therapeutic range after two days and remained above 80 mug/ml at the tenth day. On the other hand, the plasma clofibric acid concentrations measured during a ten-day administration of alufibrate as 2x360 mg tablets twice daily, were regularly found to be much lower at each time; they did not reach levels exceeding 60 mug/ml.

Adult↗

Colestipol in familial type II hyperlipoproteinemia: a three-year trial.

Colestipol, a new bile acid sequestrant polymer, has been shown to lower the serum cholesterol level more than 30% in 13 patients with familial type II hyperlipoproteinemia. Placebo for 6 wk was followed by colestipol for periods up to 36 mo. A slight but not significant increase of serum triglyceride concentrations was observed during the first 18 no, but they returned to values under the baseline level thereafter. No signs of impaired intestinal fat resorption were noted. Side effects were primarily gastrointestinal (mild and transient constipation). Colestipol seems to be an effective and safe drug in the treatment of the famiial type II hyperlipoproteinemia, without escape phenonmenon.

Adolescent↗

Naproxen plasma levels in volunteers after single-dose administration by oral and rectal routes.

The bioavailability (plasma concentrations, AUC) of a rectal formulation (suppository) of naproxen was investigated in six healthy volunteers by comparison with an oral preparation (tablets). Plasma half-lives after both formulations were identical 10 hr 15 min+/-25 min (S.D.). Determined by the AUC the bioavailability of naproxen in the suppositories was 94.8%+/-6.3% of the bioavailability of naproxen in the tablets. This paper describes also a new gas-liquid chromatographic method for determining unchanged naproxen in human plasma which is quick, sensitive, and specific.

Administration, Oral↗

Pharmacokinetic study and bioavailability of three marketed compounds releasing p-chlorophenoxyisobutyric acid (CPIB) in volunteers.

The bioavailability and the pharmacokinetics of three hypolipidemic marketed drugs: clofibride, clofibrate and basic aluminium salt of p-chlorophenoxyisobutyric acid (CPIB), releasing in vivo p-chlorophenoxyisobutyric acid (CPIB), the active metabolite, have been investigated in seven healthy male volunteers. The plasma and urinary concentrations of CPIB were determined by a gaschromatographic method, after oral ingestion of a single dose of each compound, releasing 1,3 g of CPIB, as a therapeutic dose, according to a crossover repetition design. The CPIB peak plasma level achieved by clofibride occurs earlier and is higher than this observed after clofibrate, but the CPIB bioavailability, measured by the areas under the plasma concentration-time curve released by clofibride and clofibrate, has be found similar. On the other hand, the CPIB released by the basic aluminium salt of CPIB is slowly absorbed as shown by the very low plasma levels and CPIB urinary excretion during this 24h study.

Adult↗

Pharmacokinetics of practolol in the rabbit with experimental glomerulonephritis.

The pharmacokinetics of practolol were studied after intravenous injection (5 mg/kg) in conscious normal rabbits and rabbits with experimental glomerulonephritis induced by daily intravenous injection of bovine gamma-globulin. The results obtained demonstrated that the practolol elimination was impaired in animals with experimental glomerulonephritis: significant lengthening of the half-life of the beta-phase, with marked decrease of the body clearance and diminution of the drug concentration decrease in plasma. Neither conjugates nor deacetylpractolol could be detected in the urine of the controls or immunized rabbits.

Animals↗

Predictive value of various parameters for the antihypertensive effect of the beta blocker ICI 66,082 (1).

The antihypertensive effect of the new beta-blocker, ICI 66,082 was studied in 37 patients with renal or essential hypertension. A daily dose of 75 mg produced a significant antihypertensive effect and a further blood pressure decrease was obtained by increasing the daily dose up to 300 mg; at this treatment level, the antihypertensive effect averaged 29.4/24.0 mm Hg. Increasing the dose from 300 to 600 mg daily did not produce a significant additional blood pressure decrease. Six of the 37 patients retained fluid, producing a loss in the antihypertensive effect. No significant correlation was found between the percentage systolic blood pressure fall and the following parameters determined before therapy: systolic blood pressure and its variability, heart rate (at rest and after stimulation by exercise or isoproterenol), cardiac output and total peripheral resistance, renin concentration (at rest and after stimulation) and urinary excretion of catecholamines and derivates.

Adrenergic beta-Antagonists↗