Linked Life Data

6184151

Source:http://linkedlifedata.com/resource/pubmed/id/6184151

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1983-2-25
pubmed:abstractText
5-Aza-2'-deoxycytidine (5-aza-dCyd) is an effective antileukemic agent. In view of the importance for an antileukemic agent to cross effectively the blood-brain-barrier, we studied the plasma and cerebrospinal fluid (CSF) pharmacokinetics of this drug in rabbits and dogs. The 5-aza-dCyd concentrations in biological fluids were determined by bioassay and high-performance liquid chromatography. 5-Aza-dCyd was administered either as an i.v. bolus or as a continuous i.v. infusion following a loading dose. Blood and CSF samples were collected at various time intervals. After an i.v. bolus, the plasma disappearance of 5-aza-dCyd was biphasic with half-lives of 5 and 43 min in rabbits and of 5 and 75 min in dogs. The apparent volume of distribution at steady state was in the order of 800 ml/kg for both species. The total plasma clearance of the drug was 15 ml/min/kg in rabbits and 9 ml/min/kg in dogs. After a 180 min i.v. infusion, 5-aza-dCyd slow disappearance half-lives were of 39 min in rabbits and of 144 min in dogs. The 5-aza-dCyd concentrations attained in the CSF were 27 and 58% of the plateau plasma concentration in rabbits and dogs, respectively. The drug disparition from the CSF followed closely the plasma profile after an i.v. infusion with a somewhat longer half-life. These results showed that 5-aza-dCyd can cross the blood-CSF barrier effectively, producing cytotoxic concentrations in the CSF when given by i.v. infusion.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Feb
pubmed:issn
0008-5472
pubmed:author
pubmed:issnType
Print
pubmed:volume
43
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
592-7
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1983
pubmed:articleTitle
Plasma and cerebrospinal fluid pharmacokinetics of 5-Aza-2'-deoxycytidine in rabbits and dogs.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't