Document Detail


Cathodal iontophoresis of treprostinil and iloprost induces a sustained increase in cutaneous flux in rats.
MedLine Citation:
PMID:  20860718     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
BACKGROUND AND PURPOSE: The treatment of scleroderma-related digital ulcers is still a therapeutic challenge. The most effective drugs are prostacyclin analogues. However, their usage is limited to an intravenous route of administration and by their frequent side effects. The objective of this study was to test whether treprostinil, iloprost and epoprostenol can induce sustained vasodilatation in rats when delivered locally using cutaneous iontophoresis.
EXPERIMENTAL APPROACH: Treprostinil, iloprost and epoprostenol were delivered by cathodal and anodal iontophoresis onto the hindquarters of anaesthesized rats (n= 8 for each group). Skin blood flow was quantified using laser Doppler imaging and cutaneous tolerance was assessed from day 0 to day 3.
KEY RESULTS: Cathodal but not anodal iontophoresis of treprostinil (6.4 mM), iloprost (0.2 mM) and epoprostenol (1.4 mM) induced a significant and sustained increase in cutaneous blood flow. The effects of treprostinil and iloprost were significantly different from those of treprostinil vehicle. Only weak effects were observed when both drugs were applied locally without current. Skin resistance was unchanged in areas treated with prostacyclin analogues. Finally, skin tolerance was good, with no evidence of epidermal damage.
CONCLUSIONS AND IMPLICATIONS: Cathodal iontophoresis of treprostinil and iloprost increases cutaneous blood flow with a good local tolerance. The effects of cathodal iontophoresis of these drugs should be investigated in humans, as they could have potential as new local therapies for digital ulcers in patients with scleroderma.
Authors:
S Blaise; M Roustit; C Millet; C Ribuot; J Boutonnat; J L Cracowski
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  British journal of pharmacology     Volume:  162     ISSN:  1476-5381     ISO Abbreviation:  Br. J. Pharmacol.     Publication Date:  2011 Feb 
Date Detail:
Created Date:  2011-01-13     Completed Date:  2011-07-26     Revised Date:  2012-02-01    
Medline Journal Info:
Nlm Unique ID:  7502536     Medline TA:  Br J Pharmacol     Country:  England    
Other Details:
Languages:  eng     Pagination:  557-65     Citation Subset:  IM    
Copyright Information:
© 2011 The Authors. British Journal of Pharmacology © 2011 The British Pharmacological Society.
Affiliation:
Inserm ERI17, Grenoble Medical School, University Grenoble 1, Grenoble, France.
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MeSH Terms
Descriptor/Qualifier:
Administration, Cutaneous
Animals
Antihypertensive Agents / administration & dosage*,  adverse effects,  therapeutic use
Electrodes
Epoprostenol / administration & dosage*,  adverse effects,  analogs & derivatives*,  therapeutic use
Hemodynamics
Humans
Iloprost / administration & dosage*,  adverse effects,  therapeutic use
Iontophoresis*
Male
Nitroprusside / administration & dosage
Rats
Rats, Wistar
Skin / drug effects*
Chemical
Reg. No./Substance:
0/Antihypertensive Agents; 0/treprostinil; 15078-28-1/Nitroprusside; 35121-78-9/Epoprostenol; 78919-13-8/Iloprost

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


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