Comparison of carteolol plasmatic levels after repeated instillations of long-acting and regular formulations of carteolol 2% in glaucoma patients

  • P. Renard
  • J. L. Kovalski
  • I. Cochereau
  • S. Jaulerry
  • W. Williamson
  • P. P. Elena
  • M. Lablache Combier
  • C. AllaireEmail author
  • R. Siou-Mermet
Clinical Investigation



A new long-acting (LA) formulation of carteolol 2% instilled once daily has been shown to provide a therapeutic effect similar to that of the regular formulation of carteolol 2% instilled twice daily. This study was designed to test whether the new formulation reduces the systemic delivery of carteolol.


In this double-masked, randomised, intra-subject comparative study, 23 patients with bilateral primary open-angle glaucoma or bilateral ocular hypertension received sequentially, according to the randomised order of administration, each of the 2 following treatments: carteolol 2% LA once daily for 2 months and carteolol 2% regular twice daily for 2 months. Treatments were instilled in both eyes throughout the study period. At the end of each period of treatment, blood samples were taken immediately before the last morning instillation (residual time), then 30 min, 1 h, 2 h and 4 h after this instillation in order to measure the carteolol plasma concentrations.


The mean values of maximal plasma concentration (Cmax), residual level and area under the curve obtained following carteolol 2% LA treatment were significantly lower than the values obtained after carteolol 2% regular treatment (mean±SD): Cmax (ng/ml): 1.72±0.85 versus 3.64±3.65; residual level (ng/ml): 0.70±0.58 versus 1.80±0.84; area under the curve (ng/ml×h): 5.50±2.66 versus 10.27±5.46. Regarding safety, two drug-related, non-serious adverse events were reported in the LA group: one case of moderate, superficial, punctate keratitis and one case of “bitter taste in the throat.” Both treatments appeared to be well tolerated.


The data from this study showed that the systemic delivery of carteolol is lower for the once-daily LA formulation than for the regular twice-daily formulation. Consequently, long-acting carteolol eye-drops should reduce the risk of β-blocking systemic side effects.


Carteolol Beta-blocker Alginic acid Systemic delivery Kinetics 



The authors would like to thank R. Garraffo, pharmacist, France, for his advice on pharmacokinetics; C. Whately-Smith, statistician, UK, for reviewing the article; and all the study participants.


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Copyright information

© Springer-Verlag 2005

Authors and Affiliations

  • P. Renard
    • 1
  • J. L. Kovalski
    • 2
  • I. Cochereau
    • 3
  • S. Jaulerry
    • 4
  • W. Williamson
    • 5
  • P. P. Elena
    • 6
  • M. Lablache Combier
    • 7
  • C. Allaire
    • 7
    Email author
  • R. Siou-Mermet
    • 7
  1. 1.Institut VernesParisFrance
  2. 2.HIA Clermont TonnerreBrestFrance
  3. 3.CHRUAngersFrance
  4. 4.CH Tarbes Vic BigorreTarbesFrance
  5. 5.CH François MitterrandPauFrance
  6. 6.Iris Pharma-ClirophthaLa GaudeFrance
  7. 7.Bausch & LombParisFrance

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