PMID: 3754215Jan 1, 1986Paper

Single dose pharmacokinetics and effects on platelet function of the thromboxane receptor blocker BM 13.177

European Journal of Clinical Pharmacology
C StaigerK Stegmeier

Abstract

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 clearance to range from 310.4 to 396.9 ml/min. The pharmacodynamic studies were performed ex vivo/in vitro in 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.

References

May 16, 1981·Lancet·J VermylenM Verstraete
Jul 1, 1981·Medical & Biological Engineering & Computing·L Vodovnik
May 6, 1982·The New England Journal of Medicine·D J GreenblattR I Shader
May 1, 1964·The American Journal of Medicine·I M WEINER, G H MUDGE

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Citations

Sep 1, 1989·British Journal of Clinical Pharmacology·C PiperK Stein
Sep 1, 1991·Medicinal Research Reviews·S E Hall

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