Linked Life Data

2502563

Source:http://linkedlifedata.com/resource/pubmed/id/2502563

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
6
pubmed:dateCreated
1989-8-29
pubmed:abstractText
The safety, pharmacological action and pharmacokinetics of Y-20811, a thromboxane (TX) synthetase inhibitor, were investigated by single intravenous administration of 5, 10, and 25 mg each to six healthy adult male volunteers. Throughout the entire test period, no abnormality attributable to the test drug was found in subjective and objective symptoms, routine laboratory tests, physical tests, or bleeding time; and the drug was well tolerated by subjects. Inhibition of serum TXB2 production and an increase in 6-keto-prostaglandin (PG) F1 alpha production during whole-blood coagulation exhibited a dose-dependent change from 0.5 hours after administration. In addition, arachidonic acid (AA)-induced platelet aggregation was inhibited, and adenosine diphosphate (ADP)-induced secondary aggregation was also inhibited. The duration of these actions was long; inhibition of serum TXB2 production and the increase in 6-keto-PGF1 alpha production lasted for 168 hours after administration , and inhibition of platelet aggregation lasted for more than 48 h after administration. The initial phase half-life (t1/2 alpha) and final phase half-life (t1/2 beta) of Y-20811, calculated from the change in plasma concentration, were 0.1-0.3 hours and 1.9-3.1 hours, respectively. The area under the plasma concentration-time curve (AUC) increased in a dose-dependent manner, but the values of volume of distribution (Vss) and total clearance (CLt) were almost constant in any dose group. At each of the three doses, 60-64% of the dose was excreted in unchanged form, and 8-10% in conjugated form in the urine, within 48 hours after administration.(ABSTRACT TRUNCATED AT 250 WORDS)
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0091-2700
pubmed:author
pubmed:issnType
Print
pubmed:volume
29
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
563-7
pubmed:dateRevised
2004-11-17
pubmed:meshHeading
pubmed:year
1989
pubmed:articleTitle
Phase I study of Y-20811, a new long-acting thromboxane synthetase inhibitor by intravenous administration.
pubmed:affiliation
Department of Pharmacology, Hamamatsu University School of Medicine, Japan.
pubmed:publicationType
Journal Article