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Biomedical subjects

E Bechgaard

Publications and source records attributed to E Bechgaard.

24 records · Page 2Linked to original sources
PubMed1978

Potent depletion of 5HT from monkey whole blood by a new 5HT uptake inhibitor, paroxetine (FG 7051).

The potent 5-hydroxytryptamine (5HT) uptake inhibitor FG 7051 (paroxetine, INN) was administered to rhesus monkeys in doses of 1.0, 2.5 or 7.5 mg/kg by oral gavage once daily for 13 weeks. Blood samples for analysis of 5HT in whole blood and paroxetine in plasma were taken prior to and after 1, 4 and 13 weeks of treatment. The lowest dose 1 mg/kg caused 30% depletion of 5HT in whole blood with a level of paroxetine in plasma below 2 ng/ml. Doses of 2.5 mg/kg produced an 85% depletion of 5HT and a steady state plasma concentration of about 5 ng paroxetine/ml, while 7.5 mg/kg caused a 93% depletion of 5HT and a steady state plasma concentration of 100--450 ng paroxetine/ml. There was no concentration-dependent 5HT reduction with the highest dose level suggesting that maximal depletion was produced by concentrations below 100 ng/ml. The results showed that paroxetine is a strong depletor of 5HT from whole blood of monkeys conceivably because it inhibits 5HT uptake inhibition. The effect of the drug reached its maximum within 1 week and no tolerance developed during 13 weeks.

Animals↗
PubMed1977

Determination of (+)-(3R), (4S)-3-[(4methoxyphenoxy)methyl]-1-methyl-4-phenylpiperidine hydrochloride (FG 4963) in biological fluids using competition for adsorption to glass.

A procedure has been developed for the gas chromatographic determination of a structurally new 5HT-uptake inhibitor with antidepressant properties (FG 4963) in plasma and urine. The method involves an extraction from alkaline solution with n-pentane, and a quantitative determination by gas chromatography using an internal standard and a nitrogen-sensitive detector. The binding of FG 4963 to glass during storage and evaporation necessitates the addition of a structurally similar compound to the vials used for collection of the blood and urine, in order to compete for the binding sites of the glass. The method is suitable for pharmacokinetic and clinical studies, the sensitivity being ca. 5 ng/ml in plasma and 1 ng/ml in urine and the precision being 10-15% for concentrations greater than 10 ng/ml.

Adsorption↗
PubMedDate not supplied

Bioavailability of bromhexine tablets and preliminary pharmacokinetics in humans.

The absorption of bromhexine from Bromhexin tablets 8 mg, DAK has been compared with that from Bisolvon tablets 8 mg, Boehringer Ingelheim, in a two-way complete crossover study. Four tablets of each of the two bromhexine products, corresponding to a single dose of 32 mg of bromhexine hydrochloride (77.6 mumol), was administered to each of the 10 volunteers. The plasma concentration was followed over the 4-hour period following each administration. By means of Pratt's test for paired data no statistically significant difference (p greater than 0.10) between the two products was found with respect to maximum plasma concentration (89 and 84 nmol.1(-1), respectively), the times for their occurrence (1.3 and 1.0 h, respectively), and the area under the plasma concentration-time curves (140 and 132 nmol.1(-1).h, respectively). It is concluded that Bromhexin, DAK and Bisolvon are bioequivalent. Provisional pharmacokinetic data for bromhexine, after oral administration, in man were obtained. The first-pass effect and the biological half-life were estimated by combining plasma and 30 h urine data from four of the volunteers. The first-pass effect was estimated to be c. 75 per cent, the biological half-life to be c. 6 h, and c. 0.1 per cent of the dose was found as unmetabolized bromhexine in the urine. The data indicate that the pharmacokinetics of bromhexine may be described as a two-compartment open model.

Adult↗