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Biomedical subjects

M G Bogaert

Publications and source records attributed to M G Bogaert.

At least 127 records · Page 7Linked to original sources

Plasma levels of the cis- and trans-isomers of doxepin and desmethyldoxepin after administration of doxepin to patients.

In depressed patients treated with doxepin (Sinequan), a 15:85% mixture of cis- and trans-isomers, plasma levels of the cis- and trans-forms of doxepin and desmethyldoxepin were measured using a GLC-method with a capillary column and a nitrogen detector. A gradual increase of the concentration of the products in the plasma is seen in the first days of administration. There is a remarkable variation from patient to patient in the steady-state concentrations of trans-doxepin and of cis- and trans-desmethyldoxepin. cis-Doxepin levels are always very low. It is suggested that for studies of correlation between plasma levels and therapeutic and toxic effects of doxepin, the isomers of the parent compound and its metabolite should be measured separately.

Doxepin↗

Plasma levels of isosorbide dinitrate and the isosorbide mononitrates after increasing doses of a retard preparation of isosorbide dinitrate.

Different doses of a retard preparation of isosorbide dinitrate (40, 80 and 120 mg) were given in a cross-over design with one week intervals to 6 patients with angina pectoris. Plasma concentrations of isosorbide dinitrate and of the isosorbide 2- and 5-mononitrates were measured by a gas-liquid chromatographic method. The concentrations of isosorbide dinitrate rose with the dose given, and with the highest dose, levels above 5 ng/ml were obtained for 12 hours. Concentrations of the mononitrates were much higher than those of the parent compound.

Angina Pectoris↗

Radioimmunoassay of bromperidol and haloperidol in human and canine plasma.

In order to check the specificity of a radioimmunological assay for haloperidol and bromperidol reported by Michiels et al. (1) and commercialized by IRE (Fleurus, Belgium), the assay was performed on canine and human plasma samples with and without extraction. After a single dose of bromperidol in dogs, plasma levels obtained with and without extraction were similar. In man the plasma levels for bromperidol after a single administration were markedly lower after extraction. The same was true for haloperidol plasma levels after chronic dosing in man. The findings suggest that the direct radioimmunoassay of haloperidol or bromperidol with the commercialized kit, lacks specificity of humans, possibly because of the presence of one or more polar metabolites.

Animals↗

Simultaneous determination of isosorbide dinitrate and its mononitrates in human plasma by capillary column GLC.

A previously described electron-capture GLC method for determination of isosorbide dinitrate in human plasma was adapted for the simultaneous determination of isosorbide dinitrate, isosorbide 2-mononitrate, and isosorbide 5-mononitrate using a capillary column. Quantitation was done with two internal standards. The lower limits of detection were approximately 0.5 ng/ml of plasma for isosorbide dinitrate, 2 ng/ml for isosorbide 2-mononitrate, and 20 ng/ml for isosorbide 5-mononitrate.

Biotransformation↗

Quantitative GLC determination of cis- and trans-isomers of doxepin and desmethyldoxepin.

A GLC method for the simultaneous quantitative determination of the cis- and trans-isomers of doxepin and desmethyldoxepin in human plasma was developed. The method involves the use of a capillary column for efficient separation of the four compounds and the internal standards, amitriptyline and nortriptyline. A high sensitivity is obtained with a nitrogen detector, enabling quantitation of the compounds in plasma of humans treated chronically with doxepin. Confirmation of the identity of the cis- and trans-isomers of doxepin and desmethyldoxepin in biological samples was carried out by selected ion monitoring.

Adult↗

Hypotension produced by intravenous apomorphine in the anaesthetized dog is not centrally mediated.

1 Intravenous administration of apomorphine (1.25 to 20 microgram/kg) in the anaesthetized dog produced a dose-dependent decrease in blood pressure which was antagonized by haloperidol but not influenced by propranolol or atropine. 2 Intracarotid administration of apomorphine produced a systemic hypotension which was significantly smaller than that seen with intravenous injection. 3 Doses of apomorphine that caused a decrease in blood pressure on intravenous injection, had no effect on blood pressure or caused retching accompanied by an increase in blood pressure on intravertebral or intracisternal administration. The animals showed a marked hypotension on intravertebral or intracisternal injection of clonidine. 4 From these results it is concluded that the hypotension seen with intravenous apomorphine cannot be explained by a central site of action.

Animals↗

Metabolism of papaverine IV. Urinary elimination of papaverine metabolites in man.

1. A gas chromatographic method is described for the quantitative determination of the metabolites of papaverine in urine. 2. The urinary excretion of papaverine metabolites was studied in man. About 50% of the metabolites of papaverine are excreted in the urine within 48 h. 6-Desmethylpapaverine is the major metabolite in the urine. The metabolites are excreted almost completely in conjugated form.

Biotransformation↗