Document Detail


Tear concentration and safety of levofloxacin ophthalmic solution 1.5% compared with ofloxacin ophthalmic solution 0.3% after topical administration in healthy adult volunteers.
MedLine Citation:
PMID:  20098307     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
PURPOSE: This study evaluated the tear concentration and safety of levofloxacin ophthalmic solution 1.5%. METHODS: Healthy adult volunteers (N = 125) received a single initial two-drop bilateral dose of either levofloxacin 1.5% (n = 100) or ofloxacin 0.3% (n = 25). Tear-fluid drug concentrations were measured at 15 minutes and at 2, 6, 12, and 24 hours after dosing. Subjects were dosed every 2 hours while awake and 4 and 6 hours after retiring (Days 1-3) and four times daily while awake (Days 4-14). Final measurements and evaluations were done on Day 15. Tear concentrations were determined by high-performance liquid chromatography. Safety and tolerability parameters included visual acuity, ophthalmoscopy, biomicroscopy, rose bengal staining, and adverse effects. RESULTS: Tear concentrations after a single two-drop dose of levofloxacin 1.5% and ofloxacin 0.3% were above 2 microg/mL, a concentration that exceeds the minimum inhibitory concentration90 for levofloxacin in typical ocular bacterial pathogens at all time points through 24 hours. The area under the curve for the first 12 hours for levofloxacin 1.5% was 2703.5 +/- 574.22 microg.h/mL and 414.1 +/- 1179.00 microg.h/mL with ofloxacin 0.3%. Maximal concentrations were 806.9 +/- 8.57 and 73.3 +/- 165.46 microg/mL, respectively. Levofloxacin 1.5% and ofloxacin 0.3% did not differ in adverse event incidence, except for transient mild/moderate dysgeusia (14% of levofloxacin-treated subjects versus 4% of ofloxacin-treated subjects). No corneal epithelial damage or inflammatory changes were associated with levofloxacin. CONCLUSION: A single dose of levofloxacin 1.5% produced tear fluid concentrations that were well above the minimum inhibitory concentration90 for typical ocular pathogens and was safe and well tolerated.
Authors:
Thomas Walters; Mike Rinehart; William Krebs; Mark Holdbrook
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Publication Detail:
Type:  Journal Article; Randomized Controlled Trial    
Journal Detail:
Title:  Cornea     Volume:  29     ISSN:  1536-4798     ISO Abbreviation:  Cornea     Publication Date:  2010 Mar 
Date Detail:
Created Date:  2010-02-24     Completed Date:  2010-05-07     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8216186     Medline TA:  Cornea     Country:  United States    
Other Details:
Languages:  eng     Pagination:  263-8     Citation Subset:  IM    
Affiliation:
Keystone Research, Ltd., Austin, TX, USA. twalters@austin.rr.com
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MeSH Terms
Descriptor/Qualifier:
Administration, Topical
Adult
Aged
Anti-Bacterial Agents / adverse effects,  pharmacokinetics*
Area Under Curve
Biological Availability
Chromatography, High Pressure Liquid
Double-Blind Method
Female
Half-Life
Humans
Male
Microbial Sensitivity Tests
Microscopy, Acoustic
Middle Aged
Ofloxacin / adverse effects,  pharmacokinetics*
Ophthalmic Solutions / adverse effects,  pharmacokinetics*
Ophthalmoscopy
Tears / metabolism*
Visual Acuity / drug effects
Young Adult
Chemical
Reg. No./Substance:
0/Anti-Bacterial Agents; 0/Ophthalmic Solutions; 82419-36-1/Ofloxacin

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


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