Document Detail


Absorption and biotransformation of topically applied 8-(methylthio) cyclic AMP. Studies in dogs and humans.
MedLine Citation:
PMID:  172107     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
8-(Methylthiocyclic AMP-35S was applied topically to the intact or abraded skin of dogs at a dose of about 2-5 mg/kg. In this species, an average of 7% of the dose was absorbed through the intact and 62% through abraded skin. Half-lives for radioactivity in plasma averaged 3-6 h. After the topical application of the drug to the intact skin of dogs, the average concentration in plasma of glucose, but not of insulin, was increased by as much as 21%; after application to abraded skin, glucose and insulin were increased, on average, by as much as 84 and 221%, respectively. 8-(methylthio)adenosine and two unidentified compounds were present as metabolites in the urine of dogs; some unchanged 8-(methylthio)cyclic AMP-35S was also excreted. 8-(methylthio)cyclic AMP-35S was also applied topically (25 mg; 0-32 mg/kg) to the intact and stripped skin of normal human subjects under conditions similar to those used for dogs. Three subjects with intact skin did not absorb any of the drug, whereas three subjects with stripped skin absorbed 0-5, 8-3, and 23-3% of the dose. The half-life of radioactivity in the plasma of the subject with the greatest absorption was 0-5 h during the first 2 h, and 11 h for the next 10 h. During the first 2 h, this same subject excreted unchanged drug and 8-(methylthio)adenosine in his urine. No changes in glucose or insulin concentrations in plasma were observed in any of the subjects nor was there any apparent irritation of the skin.
Authors:
J Dreyfuss; T W Mischler; E S Neiss; J M Shaw; E C Schreiber
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Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  The British journal of dermatology     Volume:  93     ISSN:  0007-0963     ISO Abbreviation:  Br. J. Dermatol.     Publication Date:  1975 Oct 
Date Detail:
Created Date:  1976-03-01     Completed Date:  1976-03-01     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0004041     Medline TA:  Br J Dermatol     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  379-90     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Adenosine / analogs & derivatives
Administration, Topical
Animals
Biotransformation
Blood Glucose
Cyclic AMP / analogs & derivatives*,  metabolism,  urine
Dogs
Feces / analysis
Half-Life
Humans
Insulin / blood
Male
Skin / metabolism
Skin Absorption*
Time Factors
Chemical
Reg. No./Substance:
0/Blood Glucose; 11061-68-0/Insulin; 58-61-7/Adenosine; 60-92-4/Cyclic AMP

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


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