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

Renard, P; Kovalski, J.L.; Cochereau, Isabelle; Jaulerry, S.; Williamson, W. Paul; Elena, Pierre-Paul; Combier, M. Lablache; Allaire, Catherine; Siou-Mermet, Raphaële

doi:10.1007/s00417-005-0024-5

Cited by 10 publications

(4 citation statements)

References 14 publications

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“…13 The addition of alginic acid in this formulation prolongs the action of eye-drops by increasing viscosity of the preparation, resulting in increased precorneal retention time of carteolol. 12,14 In addition, alginic acid has good mucoadhesive properties, [15][16][17] which increases the corneal contact time of carteolol and allows increased penetration of carteolol into the aqueous humor. 12 This formulation does not produce a gel on the corneal surface and has a relatively low viscosity that is not significantly affected by contact with tears, 14 but still blurred vision is caused by carteolol long-acting solution in some patients.…”

Section: Introductionmentioning

confidence: 99%

Time Course of Changes in Ocular Aberrations After Instillation of Carteolol Long-Acting Solution and Timolol Gel-Forming Solution

Hiraoka

Daito

Okamoto

et al. 2011

Journal of Ocular Pharmacology and Therapeutics

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Section: Introductionmentioning

confidence: 99%

Time Course of Changes in Ocular Aberrations After Instillation of Carteolol Long-Acting Solution and Timolol Gel-Forming Solution

Hiraoka

Daito

Okamoto

et al. 2011

Journal of Ocular Pharmacology and Therapeutics

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“…Carteolol has a weaker ability to slow the heart rate than timolol and thus carries a lower risk of cardiovascular events (5). The plasma concentration after ocular administration of carteolol is significantly lower than that after oral administration of carteolol (6). Previous reports of cardiovascular events using ophthalmic beta-blockers described only three cases of bradycardia (7)(8)(9).…”

Section: Discussionmentioning

confidence: 99%

Life-threatening Vasospastic Angina Induced by Carteolol Eye Drops

et al. 2023

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Vasospastic angina (VSA) can be worsened by oral nonselective beta-blockers. Ophthalmic carteolol eye drops are non-selective beta blockers and effective against glaucoma and ocular hypertension. Systemic effects of ophthalmic beta blockers on VSA have not yet been reported. We herein report a case of VSA that developed after a patient started carteolol eye drops for ocular hypertension. Even though benidipine, a calcium channel blocker. was started, a VSA attack with incessant non-sustained ventricular tachycardia occurred. Once the carteolol eyedrops were discontinued, the VSA resolved. This case demonstrates that carteolol eye drops can induce life-threatening VSA.

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“…20 Currently available treatments for glaucoma based on β-blockers reach the bloodstream at concentrations that can induce adverse effects. Both timolol and carteolol have been detected in plasma after ocular instillation; 21,22 and side effects have been recorded following administration of β-blockers in eye drops.…”

Section: Discussionmentioning

confidence: 99%

Phase I Clinical Trial of SYL040012, a Small Interfering RNA Targeting β-Adrenergic Receptor 2, for Lowering Intraocular Pressure

Moreno-Montañés

Sádaba

Ruz³

et al. 2014

Molecular Therapy

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The objective of this study was to evaluate ocular tolerance, safety, and effect on intraocular pressure (IOP) of a topically administered small interfering RNA; SYL040012, on healthy volunteers. The study was an open-label, controlled, single-center study comprised of two intervals that enrolled 30 healthy subjects having IOP below 21 mmHg. SYL040012 was administered to one eye as a single dose to six subjects during interval 1. During interval 2 two different doses of SYL040012 were administered to one eye on a daily basis to two separate groups of 12 subjects each, over a period of 7 days. The contralateral eye was evaluated but not administered and served as control for the tolerance study. SYL040012 was well tolerated locally. No local or systemic adverse events related to the product developed in response to any of the doses studied. SYL040012 was not detected in plasma at any time point. Administration of SYL040012 over a period of 7 days reduced IOP values in 15 out of 24 healthy subjects regardless of the dose used. IOP decrease was statistically significant in response to one of the doses tested and responsiveness to SYL040012 seemed to be greater in individuals with higher baseline IOP.

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

Abstract: 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.

Cited by 10 publications

References 14 publications

Time Course of Changes in Ocular Aberrations After Instillation of Carteolol Long-Acting Solution and Timolol Gel-Forming Solution

Time Course of Changes in Ocular Aberrations After Instillation of Carteolol Long-Acting Solution and Timolol Gel-Forming Solution

Life-threatening Vasospastic Angina Induced by Carteolol Eye Drops

Phase I Clinical Trial of SYL040012, a Small Interfering RNA Targeting β-Adrenergic Receptor 2, for Lowering Intraocular Pressure

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