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

BACKGROUND: 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. METHODS: 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. RESULTS: 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. CONCLUSIONS: 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.

[Comparison of three antiallergic eyedrops in a specific conjunctival provocation test: mequitazine, levocabastine and dexamethasone]. / Comparaison de trois collyres anti-allergiques lors d'un test de provocation conjonctivale spécifique: méquitazine, lévocabastine et dexaméthasone.

PURPOSE: In order to assess the efficacy of an antihistaminic eye drop containing 0.05% mequitazine in the prevention of allergy induced by a conjunctival provocation test, a double-masked, randomized, intraindividual study compared this eye drop to 0.05% levocabastine and 0.1% dexamethasone eye drops in 24 subjects allergic to grass pollen. METHOD: During the first phase of treatment, randomized subjects received one drop of dexamethasone in one eye and one drop of either mequitazine or levocabastine in the fellow eye. During the second phase of treatment, they were given one drop of dexamethasone in the same eye as previously, and one drop of the treatment that had not been given during the first phase (levocabastine or mequitazine) in the fellow eye. Fifteen minutes after each instillation phase, a conjunctival provocation test was performed. Hyperemia, itching, tearing, chemosis and palpebral edema were the five signs or symptoms taken into account to assess the treatment efficacy. Their intensity was evaluated 3, 5 and 10 min after the conjunctival provocation test. The primary efficacy criterion was the global score obtained by measuring hyperemia and itching intensity. RESULTS: The score was reduced significantly more (p < 0.0001) for the eyes treated with mequitazine or levocabastine than for those treated with dexamethasone at all evaluation times. The difference was also significant for hyperemia (p < 0.001), itching (p < 0.001), and tearing (p < 0.05). The tolerability of the three eyedrops was satisfactory. CONCLUSION: Mequitazine and levocabastine were safe and significantly more effective than dexamethasone in preventing the allergic response induced by a conjunctival provocation test when they were instilled 15 min before contact with the allergen.

Comparison of two fixed beta-blocker-pilocarpine combinations. The Carteolol-Pilocarpine Study Group.

PURPOSE: To compare the efficacy and safety of a newly developed ophthalmic solution containing carteolol 2% and pilocarpine (2% (CBS341A) with a timolol 0.5% and pilocarpine 2% fixed combination. PATIENTS AND METHODS: A randomized, double-masked, multicenter study was conducted in 209 patients with primary open-angle glaucoma or ocular hypertension, whose intraocular pressure (IOP) was higher than 21 mm Hg on bet-blocker twice a day alone. The test medications were administered twice daily for 4 months. IOP was measured at 9 and 11 a.m. at the beginning of the study (with beta-blocker alone) and after one and four months of treatment. Adverse effects were recorded. RESULTS: Both combinations caused a similar, statistically significant decrease in IOP. At four months, in the CBS341A group a 2.4 mm Hg (9%) reduction in IOP was achieved at 9 a.m. and 4.1 mm Hg (17.3%) at 11 a.m. compared with respectively 3 mm Hg (11%) and 4.5 mm Hg (19.5%) in the timolol-pilocarpine group. No statistical difference was observed between the two groups in safety and efficacy. CONCLUSIONS: The carteolol-pilocarpine combination appears as safe and as effective as the timolol-pilocarpine combination in the medical treatment of primary open-angle glaucoma or ocular hypertension.

[Comparative prospective study of effects of Biovisc and Healonid on endothelial cell loss and intraocular pressure in cataract surgery]. / Etude prospective comparative des effets du Biovisc et du Healonid sur la perte endothéliale cellulaire et de la pression intraoculaire dans la chirurgie de la cataracte.

PURPOSE: The goal of this trial was to evaluate the efficacy (protective action on corneal endothelium and ability to facilitate the procedure) as well as safety (effect on intraocular pressure and inflammation) of Biovisc (new viscoelastic agent made of 1% sodium hyaluronate produced by bacterial fermentation) versus Healonid) postcataract surgery (manual or phacoemulsification). METHODS: 106 patients, 45 males and 61 females (31-94 years) were included in this prospective randomized multicentre trial and followed up for three months. Specular microscopy and intraocular pressure (IOP) measurement were the main evaluation criteria. RESULTS: At D 90, no significant difference was observed between the two viscoelastic agents on the mean endothelial cell loss (group Viovis: -8.6%; group Healonid: -6%) as well as on IOP (early peaks were transitory and resolutive). CONCLUSION: Biovisc and Healonid were similar in terms of efficacy and tolerance.

[Comparative efficacy of 0.1% indomethacin eyedrops, 0.03% flurbiprofen eyedrops and placebo for maintaining peroperative mydriasis]. / Efficacité comparée de l'indométacine collyre à 0.1%, du flurbiprofène collyre à 0.03% et d'un placebo sur le maintien de la mydriase peropératoire.

A randomized, double-blind study was conducted to compare the effect of 0.1% indomethacin solution versus 0.03% flurbiprofen versus placebo on the maintenance of mydriasis during cataract surgery. Ninety-five patients undergoing extracapsular cataract extraction with posterior chamber lens implantation were enrolled. Pupillary diameters were measured horizontally under operating-microscope visualization before 5 surgical steps: 1. corneo-scleral incision; 2. lens nucleus expression; 3. lens cortex material aspiration; 4. intra-ocular lens implantation; 5. end of surgery. The mydriasis loss during surgery was statistically less in the 2 groups treated by non steroidal anti-inflammatory drugs than in the placebo group. This effectiveness appeared at the time of lens nucleus expression (p = 0.0001) and persisted until the end of surgery. Then, the mydriasis was maintained during 2 crucial surgical steps requiring optimal pupillary dilation: lens cortex material aspiration and intra-ocular lens implantation. No significant difference was found between 0.1% indomethacin and 0.03% flurbiprofen concerning effectiveness and tolerance.