| Autor: |
Staiger, Ch., Patscheke, H., Neugebauer, G., Kaufmann, B., Strein, K., Endele, R., Stegmeier, K. |
| Zdroj: |
European Journal of Clinical Pharmacology; September 1986, Vol. 29 Issue: 5 p573-579, 7p |
| Abstrakt: |
The pharmacokinetics and pharmacodynamic effect on platelet activation of a single 800 mg oral dose of BM 13.177 have been investigated in 8 male volunteers. BM 13.177 disappeared from plasma with a terminal elimination half-life of 0.85 h. 52% of the dose was excreted unchanged in urine. Assuming complete absorption, total clearance was calculated to be 741.3 ml/min and renal celearance to range from 310.4 to 396.9 ml/min. The pharmacodynamic studies were performed ex vivo/in vitro in platelets stimulated either with methyl mercury chloride or with U 46619. Methyl mercury chloride is a platelet activator that requires TXA2 formation from endogenous arachidonic acid, whereas U 46619 is a stable PGH2 analogue and thromboxane mimetic at the platelet TXA2/PGH2 receptor. A close correlation between the plasma concentration-time profile of BM 13.177 and inhibition of platelet shape change or aggregation was demonstrated. |
| Databáze: |
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| Externí odkaz: |
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