Ocular hypotensive efficacy and safety of once daily carteolol alginate

Abstract

Background/aim-Carteolol is a adrenoceptor antagonist used topically to reduce intraocular pressure, typically twice daily. In an eVort to provide a once daily dosing regimen, carteolol was formulated with 1% alginic acid. The objective of this study was to evaluate the eYcacy and safety of carteolol alginate solution in comparison with standard carteolol solution.Methods-This was a double masked, parallel group, multicentre study. Patients with ocular hypertension or open angle glaucoma (n=235) were randomly assigned to receive either carteolol alginate four times daily or standard carteolol solution, twice daily. The masking was maintained through the use of a vehicle in the evening for the alginate group. Patients were evaluated at baseline, 15, 60, and 120 days. Results-At 0900 (presumed trough) on day 60, mean reductions in intraocular pressure (IOP) from baseline were 6.09 (SD 2.97) and 6.09 (3.18) mm Hg for the standard carteolol and alginate, respectively. At 1100 (presumed peak), mean reductions were 6.51 (2.53) and 6.47 (2.76) mm Hg, respectively. Results were similar at other times (day 15 and day 120). The most common side eVect was transient stinging on instillation of drops, which did not diVer significantly between groups. There were no diVerences of note in other ocular or systemic signs or symptoms. Conclusion-The new alginate formulation of carteolol 2% given once daily was as eVective as standard carteolol 2% given twice daily with no meaningful diVerences regarding safety. (Br J Ophthalmol 2001;85:921-924)

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

“…13 These results suggest that ocular wavefront analysis is a useful method to objectively and quantitatively evaluate the influence of ocular treatment, such as long-acting eye drops, on optical quality of the eye.…”

“…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. 13 However, there have been no studies that investigated the influence of carteolol long-acting solution on optical quality of the eye. As for timolol gel-forming solution, there is a need to examine changes in optical quality in more detail in the early phase after instillation.…”

“…Recently, a new carteolol ophthalmic solution containing alginic acid (carteolol long-acting solution) was developed to allow once-daily administration, 12 while offering similar efficacy and tolerability as the standard formulation. 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.…”

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

“…SPK has been reported with numerous eye-drops, including betablockers [5,14,16]. In a larger series comparing carteolol 2% LA to regular carteolol 2%, no significant difference was shown with regard to local and systemic drug-related adverse effects [1]. In comparison with other beta-blocking eye-drops, carteolol has demonstrated a very good tolerability profile [14,19].…”

“…is as effective at reducing intraocular pressure (IOP) as the regular formulation instilled twice daily (b.i.d.) [1,18].…”