After oral ingestion of 400 mg Mefexamidehydrochloride for Mefexamide (I) and its main degradation product Desmethyl-Mefexamide (II) the following pharmakokinetic parameters have been determined: 1. Elimination of I and II follows 1st order kinetics. 2. Biological half-life t 1/2 for I is 4-6, for II 4.5-6.5 H. 3. Elimination rate constant for I and II is between 0.10 to 0.20 h-1. 4. 5-10% of the administered drug are excreted unchanged, 10-16% as Desmethyl-Mefexamide within 72 h after ingestion. 5. The described thinlayer chromatographic and gas chromatographic/mass spectrometric methods allow detection of I and II for at least 72 h after application. 6. II is excreted free and conjugated in nearly equal amounts.
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After oral ingestion of 400 mg Mefexamidehydrochloride for Mefexamide (I) and its main degradation product Desmethyl-Mefexamide (II) the following pharmakokinetic parameters have been determined: 1. Elimination of I and II follows 1st order kinetics. 2.
View Article and Find Full Text PDFAfter oral administration of a therapeutic dosage (400 mg) Mefexamide (I), six excretion products were detected in human urine and subsequently identified by GC/MS and TLC: in addition to the unchanged drug (I) in the acidic extracted urine without hydrolysis p-methoxiphenoxiaceticacid-methylester (II) and p-methoxiphenoxiaceticacid (III) were detected; the latter two and p-hydroxyanisole (IV) were also found in the acidic extract after hydrolysis (with hydrochloric acid or enzymatic). In the alkaline urine extract besides the unchanged drug (I) and the main metabolite V (partially described previously by Forist et al. [8]1), metabolite VI, which occurred only in very small amounts, could be detected.
View Article and Find Full Text PDFIn a double-blind cross-over study 15 highly motivated, healthy male subjects (Ss), aged from 23 to 29 years, were given 200 mg and 400 mg p-methoxy-phenoxyaceticacid-diethylaminoethylamide-hydrochloride (mefexamide) and a placebo. On each of the three days the Ss were tested in different tracking devices and the integrated absolute error was measured in the tests of a duration of three hours each. Influences of practice, leading to unwanted and disturbing effects were excluded by a preceding period of four training sessions on different days.
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