Document Detail

Nanosuspension formulation of itraconazole eliminates the negative inotropic effect of SPORANOX in dogs.
MedLine Citation:
PMID:  20238196     Owner:  NLM     Status:  MEDLINE    
Previously, it was observed that a nanosuspension formulation of itraconazole was more efficacious and yet less acutely toxic in rats as compared with the conventional solution formulation, SPORANOX (itraconazole) Injection. The present study compares the two formulations with respect to specifically myocardial contractility in conscious dogs. Motivation for doing so is highlighted by the black-box warning in the package insert for SPORANOX (itraconazole) Injection, which warns of negative inotropic effects. Conscious dogs, instrumented with a high-fidelity pressure transducer in the left ventricle, were placed in a sling for dosing and cardiac monitoring. Test and control articles were administered intravenously via a peripheral vein, and left ventricular parameters were measured continuously through 60 min from the start of dosing. As expected, SPORANOX (itraconazole) Injection caused a significant reduction in myocardial contractility as determined by the contractility index. In contrast, the itraconazole nanosuspension administered at twice the dose and at twice the rate of infusion did not result in significant changes in myocardial contractility. A novel formulation technology applied to itraconazole completely prevented the negative inotropic effect observed in conscious dogs as compared with SPORANOX (itraconazole) Injection.
Jeff McKee; Barrett Rabinow; Chyung Cook; Jerry Gass
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of medical toxicology : official journal of the American College of Medical Toxicology     Volume:  6     ISSN:  1556-9039     ISO Abbreviation:  J Med Toxicol     Publication Date:  2010 Sep 
Date Detail:
Created Date:  2010-08-30     Completed Date:  2010-11-09     Revised Date:  2013-07-31    
Medline Journal Info:
Nlm Unique ID:  101284598     Medline TA:  J Med Toxicol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  331-6     Citation Subset:  IM    
Baxter Healthcare, 25212 W. Illinois Rt. 120, WG2-1S, Round Lake, IL 60073, USA.
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MeSH Terms
Antifungal Agents / administration & dosage,  toxicity*
Depression, Chemical
Drug Stability
Itraconazole / administration & dosage,  blood,  chemistry,  toxicity*
Myocardial Contraction / drug effects*
Reg. No./Substance:
0/Antifungal Agents; 0/Suspensions; 84625-61-6/Itraconazole

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

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