Document Detail

Perfusion and molecular modification of idoxuridine to alter its cerebrospinal fluid metabolism.
MedLine Citation:
PMID:  903879     Owner:  NLM     Status:  MEDLINE    
Two methods to deter the rapid intrathecal degradation of idoxuridine were investigated: (a) rapid drug perfusion through the ventricular system, and (b) modification of the molecule to its uronic acid derivative, 2'-deoxy-5-iodo-5'-uridinecarboxylic acid, to make it less susceptible to enzymatic digestion. Perfusion of idoxuridine through the ventricular system (ventriculocisternal) of dogs at 0.97 ml/min saturated the metabolic pathway so that the outflow solution yielded a single spot (Rf 0.76) on TLC indicative of the intact molecule. The 125I-labeled uronic acid was synthesized from the 125I-labeled parent compound, and the labeled compounds were compared after their individual intracisternal injection in dogs. Since there was no difference in the disappearance rates, the stability of the uronic acid was, in fact, no greater than that of the parent compound in vivo. Ventricular perfusion of idoxuridine, however, seems a suitable means for increasing the amount of active drug delivered to central nervous system tumors and viral infections.
P H Gutin; L D Prockop; K F Yip; J D Weinstein; K C Tsou
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Publication Detail:
Type:  Journal Article; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  66     ISSN:  0022-3549     ISO Abbreviation:  J Pharm Sci     Publication Date:  1977 Sep 
Date Detail:
Created Date:  1977-11-25     Completed Date:  1977-11-25     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1338-40     Citation Subset:  IM    
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MeSH Terms
Cerebral Ventricles
Chemistry, Pharmaceutical
Chromatography, Thin Layer
Cisterna Magna
Idoxuridine / administration & dosage,  analogs & derivatives*,  cerebrospinal fluid*,  chemical synthesis
Iodine Radioisotopes / diagnostic use
Time Factors
Reg. No./Substance:
0/Iodine Radioisotopes; 54-42-2/Idoxuridine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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