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At least 1,027 records · Page 57Linked to original sources
PubMed2003

Efficacy and safety of timolol maleate/latanoprost fixed combination versus timolol maleate and brimonidine given twice daily.

PURPOSE: To evaluate the efficacy and safety of the timolol maleate/latanoprost fixed combination (TLFC) given once each evening versus brimonidine and timolol solution given twice daily as concomitant therapy in primary open-angle glaucoma or ocular hypertension patients. METHODS: Qualified subjects were begun on timolol alone twice daily for 1 month and then randomized to either TLFC or brimonidine and timolol concomitant therapy for 6 weeks. Patients were then switched to the other treatment regimen. Intraocular pressures (IOPs) were measured every 2 hours between 08 : 00 and 20 : 00 hours at baseline and at the end of periods 1 and 2. RESULTS: This study found that in 32 subjects the IOP diurnal curve on timolol alone (20.9 +/- 2.8 mmHg) decreased to 17.9 +/- 3.2 mmHg when patients were treated with TLFC and to 19.0 +/- 2.4 mmHg when patients were treated with brimonidine and timolol (p = 0.02). Intraocular pressures at individual time-points were statistically similar between the groups at the 08 : 00 trough and 2 and 4 hours after dosing. However, beyond 4 hours after dosing, TLFC-treated subjects demonstrated a trend towards lower IOPs at each 2-hour time-point that was not statistically significant after a Bonferroni correction (p <or= 0.05). The incidence of both solicited and unsolicited side-effects was similar between groups. CONCLUSION: This study suggests that TLFC given in the evening reduces the mean daytime diurnal IOP more than brimonidine and timolol given concomitantly twice daily.

Antihypertensive Agents↗
PubMed1988

A comparative evaluation of timolol maleate and pilocarpine in the treatment of chronic open angle glaucoma.

Ninety-two eyes with newly-diagnosed chronic open angle glaucoma (COAG) were treated in a randomised prospective trial with either timolol or pilocarpine. Their visual field survival was monitored on a 3-monthly basis over 2 years using both Goldmann and Friedmann perimetry. Concomitant tonometric data was derived by applanation. Fields were assessed and quantified using algorithms designed to give the greatest sensitivity for glaucomatous field loss. Microcomputer programmes specifically designed for this purpose were used in the data collection and subsequent analysis.

Aged↗
PubMed2006

Sunitinib maleate.

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Antineoplastic Agents↗
PubMed1999

Inhibition of HERG channels stably expressed in a mammalian cell line by the antianginal agent perhexiline maleate.

Perhexiline has been used as an anti-anginal agent for over 25 years, and is known to cause QT prolongation and torsades de pointes. We hypothesized that the cellular basis for these effects was blockade of I(Kr). A stable transfection of HERG into a CHO-K1 cell line produced a delayed rectifier, potassium channel with similar properties to those reported for transient expression in Xenopus oocytes. Perhexiline caused voltage- and frequency-dependent block of HERG (IC50 7.8 microM). The rate of inactivation was increased and there was a 10 mV hyperpolarizing shift in the voltage-dependence of steady-state inactivation, suggestive of binding to the inactivated state. In conclusion, perhexiline potently inhibits transfected HERG channels and this is the probable mechanism for QT prolongation and torsades de pointes. Channel blockade shows greatest affinity for the inactivated state.

Algorithms↗
PubMed2004

Diurnal intraocular pressure reduction with latanoprost 0.005% compared to timolol maleate 0.5% as monotherapy in subjects with exfoliation glaucoma.

AIMS: To compare the diurnal intraocular pressure (IOP) efficacy and safety of timolol vs latanoprost in subjects with exfoliation glaucoma (XFG). METHODS: A 3-month prospective, single-masked, active-controlled, parallel comparison performed in six centres in Greece that randomized subjects in a 1 : 1 ratio to either latanoprost in the evening (2000 hours) and placebo in the morning (0800 hours), or timolol twice daily (0800 and 2000 hours). RESULTS: In all, 103 subjects completed the study. After 3 months of chronic dosing, the latanoprost group exhibited a trend to a greater diurnal IOP reduction from an untreated baseline (24.9+/-3.2-17.4+/-2.9) compared with timolol (24.7+/-2.8-18.3+/-1.9 mmHg) (P=0.07). Latanoprost showed a significantly greater IOP reduction at 0800 hours (-8.5 vs -6.0 mm Hg for timolol, P<0.0001) whereas no difference was observed between the two medications at 1000, 1400, and 2000 hours after a Bonferroni Correction. In addition, latanoprost demonstrated a narrower range of diurnal IOP (2.4) than timolol (3.2 mmHg)(P=0.0017). Safety was similar between groups, except there was more conjunctival hyperaemia with latanoprost (n=8) than timolol (n=1)(P=0.01). CONCLUSIONS: This study suggests that latanoprost provides a statistically lower 08:00-hour IOP and better range of IOP than timolol in the treatment of XFG glaucoma.

Adult↗
PubMed2005

A 6-month assessment of bimatoprost 0.03% vs timolol maleate 0.5%: hypotensive efficacy, macular thickness and flare in ocular-hypertensive and glaucoma patients.

AIM: To compare 6 months of treatment with bimatoprost and timolol in terms of their hypotensive efficacy and secondary effects, including changes in macular thickness and the inflammatory reaction induced in the anterior chamber. METHODS: A prospective, randomized, parallel-group trial performed on 30 eyes of 30 patients per group. The main outcome measure was the difference between the IOP value taken between the baseline visit and the 6-month-visit. Macular thickness determined through optical coherence tomography and anterior chamber inflammation estimated using the laser flare meter was also evaluated. Adverse events were recorded during the study period. RESULTS: Bimatoprost treatment gave rise to a significantly lower mean IOP than timolol in all follow-up visits as from the first month (P<0.05). Bimatoprost achieved high percentage IOP reductions from baseline in a significantly higher proportion of patients (P<0.05). Macular thickness and anterior chamber flare failed to vary significantly both between the two groups and within each group during the 6-month evaluation (P>0.05). CONCLUSIONS: Bimatoprost 0.03% once daily showed a greater efficacy then timolol 0.05% twice daily in patients with elevated IOP. No significant differences were detected in macular thickness or anterior uveitis using optical coherence tomography and laser flare photometry.

Adult↗
PubMed2000

Drug release from film-coated chlorpheniramine maleate nonpareil beads: effect of water-soluble polymer, coating level, and soluble core material.

The purpose of this research was to use a new drug release model to study the effects of formulation parameters on drug release from a film-coated chlorpheniramine (CPM) nonpareil system. The film-coated CPM nonpareils were prepared by using a fluid bed apparatus. A hydroxylpropylmethylcellulose (HPMC) solution was blended with an aqueous ethylcellulose dispersion (Surelease) to adjust the permeability of the film. The apparent permeability of samples was obtained from dissolution data using a previously reported drug release equation. The apparent permeability was plotted versus the film coating level or the HPMC concentration in the film. When the natural logarithm of the apparent permeability versus coating level was graphed, a biphasic plot was observed in the group without HPMC in the film, showing the occurrence of a critical coating level. It was suggested that a mechanically formed porous film (due to an incomplete coating) could change to a nonporous film after the bead was completely coated. However, in the group that contained 12% HPMC in the film, the critical coating level was not observed. A porous film, formed by the leaching out of the water-soluble polymer, would not change to a nonporous film even after the bead is completely coated. Through a mathematical derivation, the decrease of apparent permeability versus coating level was related to the reduction of the total hole area. The apparent permeability was found to increase with the HPMC concentration. After a critical concentration was reached, the further addition of HPMC into the film caused a rapid increase in apparent permeability. The critical HPMC concentration was related to a minimum domain formation concentration (MDFC). A rapid increase of the drug release was observed when the dissolution profile of a sample made from a regular sugar nonpareil core (soluble) was compared with the sample made from a precoated nonpareil core (insoluble), which suggests that the drug release can be enhanced by the dissolution of the core. A minimum concentration of the HPMC was required to effectively modify permeability of the film. The critical coating level and critical concentration of HPMC can be determined from the apparent permeability plot using a previously published equation. The dissolution of a soluble core can greatly enhance the release of the drug from the nonpareil system.

Anti-Allergic Agents↗
PubMed2004

Intraocular pressure and safety in glaucoma patients switching to latanoprost/timolol maleate fixed combination from mono- and adjunctive therapies.

PURPOSE: The aim of this study was to evaluate the efficacy and safety in ocular hypertensive or open-angle glaucoma patients changed to a latanoprost/timolol fixed combination (LTFC) from previous therapy. METHODS: We employed a retrospective, multicenter, active-controlled study evaluating patients who had a previous therapy substituted with LTFC and had a 3-month follow-up. RESULTS: In the 168 patients included in the trial, LTFC reduced the intraocular pressure (IOP) after switching from previous therapies: timolol (22.8+/-3.5 to 19.0+/-3.9 mmHg, N=49, p<0.001), latanoprost (21.2+/-3.8 to 18.3+/-2.5 mmHg, N=54, p<0.001), and a dorzolamide/timolol fixed combination (20.9+/-2.4 to 20.0+/-2.7 mmHg, N=32, p=0.03). In switching from a latanoprost and timolol unfixed combination, the pressure changed from 18.3+/-3.8 to 18.9+/-3.0 mmHg (N=33, p=0.38). LTFC was persistent in 131 (78%) patients within the 3-month treatment period. The most common adverse event with LTFC was conjunctival hyperemia, which occurred in patients not previously treated with latanoprost therapy (N=16, 10%). CONCLUSIONS: LTFC generally provides reduced IOP and limited side effects when substituted for other common glaucoma therapies, while providing similar pressure when switched from its own individual components.

Aged↗