Raschke, Carl and Koch, Horst J. (2000) Pharmacokinetics and pharmacodynamics of oral and intravenous D,L-lysinacetylsalicylate and of oral acetylsalicylate. PERFUSION, 13 (6). 262-+. ISSN 0935-0020
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We studied the ASA pharmacokinetics of single doses of 500 mg and 1000 mg of D,L-lysine-monoacetylsalicylate (Lys-ASA) administered both orally and 500 mg parenterally as well as 500 mg acetylsalicylate (ASA) in 13 healthy volunteers. Blood samples were taken before and at defined times up to 48 hours after application of Lys-ASA and ASA. Analysis for ASA was performed by HPLC. All concentration versus time data were presented descriptively and assessed by means of ANOVA according to Friedman including post hoc Wilcoxon tests for each time point. Pharmacokinetic parameters were calculated based on a l-compartment model. The effect on platelet aggregation (closure time) as a function of time was fitted to a sigmoid model. The concentration versus time curves differed significantly (p < 0.001) between oral 500 mg Lys-ASA and ASA doses. Peak serum ASA concentrations (C-max) were 6.8 mg/l for 500 mg Lys-ASA per os and 2.7 mg/l for 500 mg ASA per os. The corresponding t(max)-values were 14.2 and 38.0 minutes. After intake of 100 mg and 1000 mg doses of Lys-ASA per os C-max was 1.5 mg/l and 15.9 mg/l, t(max) being 14.2 minutes for the 1000 mg dose. The effect versus time curves showed a faster and more marked platelet aggregation of Lys-ASS formulations compared to the ASS formulation, the effect of the 1000 mg dose of Lys-ASA being in the order of the intravenous dose. We conclude, that concerning the time dimension the application of 1000 mg oral Lys-ASA is supposed to be equivalent to i.v. Lys-ASA even in the treatment of unstable angina pectoris.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | UNSTABLE ANGINA-PECTORIS; ACUTE MYOCARDIAL-INFARCTION; ANTIPLATELET AGENTS; ASPIRIN; DISEASE; THERAPY; D,L-lysinacetylsalicylate; acetylsalicylic acid; pharmacokinetics; pharmacodynamics |
| Subjects: | 600 Technology > 610 Medical sciences Medicine |
| Divisions: | Medicine > Lehrstuhl für Psychiatrie und Psychotherapie |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 03 May 2022 07:24 |
| Last Modified: | 03 May 2022 07:24 |
| URI: | https://pred.uni-regensburg.de/id/eprint/42462 |
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