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Comparison of carteolol plasmatic levels after repeated instillations of long-acting and regular formulations of carteolol 2% in glaucoma patients
- Source :
- Graefe's Archive for Clinical and Experimental Ophthalmology. 243:1221-1227
- Publication Year :
- 2005
- Publisher :
- Springer Science and Business Media LLC, 2005.
-
Abstract
- 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 (C(max)), 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): C(max) (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/mlxh): 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 beta-blocking systemic side effects.
- Subjects :
- Male
medicine.drug_class
Adrenergic beta-Antagonists
Cmax
Ocular hypertension
Cellular and Molecular Neuroscience
Double-Blind Method
medicine
Humans
Carteolol
Adverse effect
Beta blocker
Intraocular Pressure
Aged
Aged, 80 and over
Cross-Over Studies
business.industry
Therapeutic effect
Area under the curve
Middle Aged
medicine.disease
Crossover study
Sensory Systems
Ophthalmology
Instillation, Drug
Treatment Outcome
Delayed-Action Preparations
Anesthesia
Female
Ocular Hypertension
business
Glaucoma, Open-Angle
medicine.drug
Subjects
Details
- ISSN :
- 1435702X and 0721832X
- Volume :
- 243
- Database :
- OpenAIRE
- Journal :
- Graefe's Archive for Clinical and Experimental Ophthalmology
- Accession number :
- edsair.doi.dedup.....c880a1b06f95c2b9fb6acb0dbc2ccca8
- Full Text :
- https://doi.org/10.1007/s00417-005-0024-5