Author:
Figus Michele,Posarelli Chiara,Romano Dario,Nardi Marco,Rossetti Luca
Abstract
Abstract
Purpose
To evaluate the penetration of levofloxacin and dexamethasone sodium phosphate into the aqueous humour (AH) after administration in combination and as single molecules. Evaluation of the penetration of those agents in the site of action and their pharmacodynamic potential activity in view of the intended clinical use after cataract surgery.
Methods
Randomised, assessor-blinded, parallel-group. Patients scheduled for cataract surgery were assigned in a 1:1:1 ratio to: levofloxacin + dexamethasone sodium phosphate (L-DSP), Levofloxacin (L) or Dexamethasone sodium phosphate (DSP) eye drops. Either test or reference drugs were instilled in the cul-de-sac twice, 90 and 60 min before paracentesis.
Results
A total of 125 patients completed the study. Fraction of dose absorbed in the anterior chamber was 3.8–4.2 · 10−4 for levofloxacin and 0.3–0.4 · 10−4 for dexamethasone, respectively. No notable differences in concentration of levofloxacin were found between L-DSP arm (1.970 nmol/ml) and L arm (2.151 nmol/ml). The concentrations of levofloxacin were well above the MICs for the most frequent Gram-positive and Gram-negative eye pathogens. Dexamethasone concentrations were slightly lower in L-DSP arm (0.030 nmol/ml) than in DSP arm (0.042 nmol/ml), but still in the pharmacodynamically active range in the site of action. The difference was not clinically relevant. DSP was not detected in any HA sample, suggesting its full hydrolysis to free dexamethasone.
Conclusion
Our results confirm that no interaction is evident on the corneal penetration of levofloxacin and dexamethasone which reach pharmacologically active concentrations when instilled as fixed combination eye drops to patients undergoing cataract surgery.
Trial registration
ClinicalTrials.gov Identifier: NCT03740659
Publisher
Springer Science and Business Media LLC
Subject
Pharmacology (medical),Pharmacology,General Medicine
Reference17 articles.
1. Barry P, Cordovés L, Gardner S ESCRS Guidelines for prevention and treatment of endophthalmitis following cataract surgery: data, dilemmas and conclusions 2013. https://www.escrs.org/downloads/Endophthalmitis-Guidelines.pdf. last accessed 7 Sept 2019
2. Behndig A, Cochener B, Guell JL et al (2013) Endophthalmitis prophylaxis in cataract surgery: overview of current practice patterns in 9 European countries. J Cataract Refract Surg 39:1421–1431
3. Chang DF, Braga-Mele R, Handerson BA, Mamalis N, Vasavada A, ASCRS Cataract Clinical Commitee (2015) Antibiotic prophylaxis of postoperative endophthalmitis after cataract surgery: results of the 2014 ASCRS member survey. J Cataract Refract Surg 41(6):1300–1305
4. Cagini C, Cometa F, Torroni G, Pellegrino A, Pellegrino R, Cavallini GM (2016) Dexamethasone disodium phosphate penetration in to the human aqueous humour after topical application. Curr Eye Res 41(7):897–899
5. Bucci FA (2004) An in vivo study comparing the ocular absorption of levofloxacin and ciprofloxacin prior to phacoemulsification. Am J Ophthalmol 137:308–312
Cited by
6 articles.
订阅此论文施引文献
订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献