Effects of S-596 and carteolol, new beta-adrenergic blockers, and flurbiprofen on the human eye: A fluorophotometric study

Abstract

The effects of S-596 and coarteolol, new beta-adrenergic blockers, were studied by means of the oral fluorescein method. Transfer coefficients by diffusion, kd.pa, and by flow, kfa, were estimated in a total of 11 normal young volunteers, in whom the drug was instilled in one eye and the placebo in the fellow eye. With 0.5% dl-S-596, kd.pa increased to 124 +/- 9% (mean +/- SD) and kfa decreased to 67 +/- 10% of the control eye. With 1% dl-carteolol, kd.pa increased to 121 +/- 4%, and kfa decreased to 84 +/- 11% of the control eye. Both S-596 and carteolol increased iris permeability and decreased the aqueous flow rate significantly. In a group of 13 cases, intracapsular extraction of senile cataract was carried out with postoperative routine instillations, and in another group of 7 cases, it was carried out with additional topical flurbiprofen, a new nonsteroidal anti-inflammatory drug. Flurbiprofen ophthalmic solution (0.1%) was instilled 3, 2, 1, and 0.5 h before the surgery and 4 times a day postoperatively. On the 6th postoperative day, a fluorophotometric study was carried out using oral fluorescein, and a coefficient that reflects the permeability of the blood-aqueous barrier after the cataract surgery was calculated. It was found that additional topical flurbiprofen considerably suppresses the disruption of the blood-aqueous barrier.

Cardiovascular and Respiratory Considerations With Pharmacotherapy of Glaucoma and Ocular Hypertension

“…It does not have a significant effect on total outflow facility. 95,96 Carteolol eye drops lack local anesthetic activity and seem to cause less local irritation than timolol. 97 When administered as 1 or 2 drops of 1% or 2% solution twice daily, most clinical trials show carteolol to be roughly equal in efficacy to timolol, reducing mean IOP in patients with ocular hypertension or glaucoma by about 14 -26%.…”

Ocular Carteolol

“…Mean lOP was 1.7 to 1.8mm Hg (14 to 16%) lower in eyes instilled with carteolol 1 % compared with placebo or untreated eyes in 3 groups of 5, 8 and 10 healthy volunteers (Araie & Takase 1985;Negishi et al 1981;Wright et al 1989). Four hours after single topical administration of carteolol 0.1, 0.25, 0.5, 1 and 2% ophthalmic solutions to 8 volunteers, mean lOP decreased by a maximum 2.5 (19% reduction), 2.9 (22.5%), 3.7 (27.5%), 4.4 (31%) and 5.2mm Hg (38.5%), respectively, in a double-blind crossover study (Negishi et al 1981).…”

Glaucoma Treatment Outcomes in Open Angle Glaucoma Patients of African Descent

“…In addition, it has also been determined that melanin has the ability to act as a drug reservoir and can impact the pharmacokinetics of ocular drugs 33. However, only a handful of studies have specifically evaluated the effects of ocular melanin on antiglaucoma drugs, with none studying prostaglandin analogues 34–36…”

“…33 However, only a handful of studies have specifically evaluated the effects of ocular melanin on antiglaucoma drugs, with none studying prostaglandin analogues. [34][35][36] Ultimately, potential racial differences in response to topical glaucoma therapy are poorly understood and exacerbated by the fact that drug efficacy is primarily studied in ED populations. Further research specifically designed to examine drug efficacy in persons of AD, as opposed to its evaluation as a secondary outcome based on study demographics, is required.…”