+ Resolve Article
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter

+ Translate
+ Subscribe to Site Feed
GeoScience Most Shared ContentMost Shared Content

The pharmacodynamics and pharmacokinetics of a novel thromboxane receptor blocking drug vapiprost (GR32191) after single intravenous doses in healthy subjects

, : The pharmacodynamics and pharmacokinetics of a novel thromboxane receptor blocking drug vapiprost (GR32191) after single intravenous doses in healthy subjects. British Journal of Clinical Pharmacology 32(2): 181-186

1 The effect of single, serially increasing, intravenous doses of a specific thromboxane receptor blocking drug, vapiprost, upon platelet aggregation induced ex vivo by the thromboxane A2 mimetic, U-46619, was examined in 12 healthy males. 2 Subjects received either 1 (n = 1 subject), 2 (n = 6), 3 (n = 2), or 4 (n = 3) administrations of vapiprost within the dose range 0.125 to 16 mg and, in random order, placebo on separate study days at intervals of at least 48 h. 3 All doses of vapiprost produced an immediate antagonism of U-46619-induced platelet aggregation in whole blood. Both the magnitude and duration of the rightward displacement of the concentration-effect curves increased with dose. Although lower doses produced parallel displacements of these curves, with the higher doses the maximum response to U-46619 was reduced such that 50% platelet aggregation was not achieved. After the 16 mg dose of vapiprost, virtually complete suppression of platelet aggregation (up to a concentration of 30 microM) was seen. This degree of inhibition was maintained for 2 h after dosing, following which there was a gradual return to pre-dose U-46619 sensitivity over the next 12 to 24 h. U-46619-induced platelet aggregation was unaffected by placebo. 4 Across the dose range, vapiprost was rapidly cleared from plasma, with an elimination half-life of 69-84 min and a plasma clearance of 514-721 ml min-1.


PMID: 1834144

Other references

Malyshaw F.A.; Lato L.P., 1991: The organic component of peat in soddy podzolic loamy soil. Vyestsi Akademii Navuk BSSR Syeryya Syel'skahaspadarchykh Navuk (1): 22-27

Peringuey, L., 1904: Some new Coleoptera collected by Rev. Henri A. Junod at Shilouvane, near Leydsdorp, in the Transvaal. : 448-450

Jaleta, K.T.; Hill, S.R.; Seyoum, E.; Balkew, M.; Gebre-Michael, T.; Ignell, R.; Tekie, H., 2014: Agro-ecosystems impact malaria prevalence: large-scale irrigation drives vector population in western Ethiopia. Development strategies in Ethiopia have largely focused on the expansion of irrigated agriculture in the last decade to reduce poverty and promote economic growth. However, such irrigation schemes can worsen the socio-economic state by aggravating...

Ashley-Koch, A.; Murphy, C.C.; Khoury, M.J.; Boyle, C.A., 2001: Contribution of sickle cell disease to the occurrence of developmental disabilities: a population-based study. Purpose: Population-based surveillance of children aged 3-10 years from metropolitan Atlanta was used to determine if stroke-related neurological damage in children with sickle cell disease (SCD) is associated with developmental disabilities (DD)....

Muraoka Makoto; Tanemura M., 1953: The Myojo limestone, Niigata prefecture. The upper part of the Myojo limestone, a member of the Paleozoic limestone-slate complex thrust over Mesozoic sedimentary formations of Niigata, Japan, is suitable for use in the manufacture of cement.

Polatdemir, N.; Sahin, Y., 1997: Still-waters systems in and around Eskisehir Chironomidae Diptera larvae Eskisehir ve cevresi durgun su sistemleri Chironomidae Diptera larvalari. During this study 25 species were found. Among these species, the ones showing highly widespread distribution were; "Chironomus thummi K.", Chironomus viridicollis K., Chironomus anthracinus (Zett.). Polypedilum scalaenum Schr. 7 species...

Sedlacek J., 1974: Fetal development of cortical sensory systems in the guinea pig. Physiologia Bohemoslovaca 23(2): 174-175

Alataş, F.; Ozdemir, N.; Işiksoy, S.; Metintaş, M.; Erginel, S.; Harmanci, E.; Mutlu, S., 1999: An unusual case of esophageal tuberculosis in an adult. Tuberculous infection of the esophagus is a rare disease and usually occurs secondary to tuberculous mediastinal lymphadenopathy. We report a 74-year-old woman presenting with dysphagia and weight loss. The chest radiograph showed punctuated calci...

Cohen, M.E., 1996: Effect of model fitting artifacts on the stepwise approach to identifying patterns of attachment loss. The stepwise approach to the determination of periodontal attachment loss involves fitting linear, logarithmic, and exponential models to individual site data and concluding that the form of loss is consistent with the model that has the greatest...

Sackett, D.L.; Parkes, J., 1998: Teaching critical appraisal: no quick fixes. Cmaj 158(2): 203-204