Timolol 10mg / Bendroflumethiazide 2.5mg tablets

PURPOSE: To evaluate the efficacy and ocular and systemic safety of netarsudil 0.02% ophthalmic solution, a rho-kinase inhibitor and norepinephrine transporter inhibitor, in patients with open-angle glaucoma and ocular hypertension. DESIGN: Double-masked, randomized noninferiority clinical trials: Rho Kinase Elevated IOP Treatment Trial 1 and 2 (ROCKET-1 and ROCKET-2). METHODS: After a washout of all pre-study ocular hypotensive medications, eligible patients were randomized to receive netarsudil 0.02% once daily (q.d.), timolol 0.5% twice a day (b.i.d.), and (ROCKET-2 only) netarsudil 0.02% b.i.d. Data through 3 months from both studies are provided in this report. RESULTS: Enrolled into the 2 studies were 1167 patients. Treatment with netarsudil q.d. produced clinically and statistically significant reductions from baseline intraocular pressure (P < .001), and was noninferior to timolol in the per-protocol population with maximum baseline IOP < 25 mm Hg in both studies (ROCKET-2, primary outcome measure and population, ROCKET-1, post hoc outcome measure). Netarsudil b.i.d. was also noninferior to timolol (ROCKET-2). The most frequent adverse event was conjunctival hyperemia, the incidence of which ranged from 50% (126/251, ROCKET-2) to 53% (108/203, ROCKET-1) for netarsudil q.d., 59% (149/253, ROCKET-2) for netarsudil b.i.d., and 8% (17/208, ROCKET-1) to 11% (27/251, ROCKET-2) for timolol (P < .0001 for netarsudil vs timolol). CONCLUSIONS: In 2 large, randomized, double-masked trials reported here, once-daily dosing of netarsudil 0.02% was found to be effective and well tolerated for the treatment of patients with ocular hypertension and open-angle glaucoma. The novel pharmacology and aqueous humor dynamic effects of this molecule suggest it may be a useful addition to the armamentarium of ocular hypotensive medications.

Abstract licence: CC BY-NC-ND

PURPOSE: To compare the diurnal intraocular pressure (IOP)-lowering effect of latanoprostene bunod (LBN) ophthalmic solution 0.024% every evening (qpm) with timolol maleate 0.5% twice daily (BID) in subjects with open-angle glaucoma (OAG) or ocular hypertension (OHT). DESIGN: Phase 3, randomized, controlled, multicenter, double-masked, parallel-group clinical study. PARTICIPANTS: Subjects aged ≥18 years with a diagnosis of OAG or OHT in 1 or both eyes. METHODS: Subjects were randomized (2:1) to a 3-month regimen of LBN 0.024% qpm or timolol 0.5% 1 drop BID. Intraocular pressure was measured at 8 am, 12 pm, and 4 pm of each postrandomization visit (week 2, week 6, and month 3). Adverse events were recorded throughout the study. MAIN OUTCOME MEASURES: The primary efficacy end point was IOP in the study eye measured at each of the 9 assessment time points. Secondary efficacy end points included the proportion of subjects with IOP ≤18 mmHg consistently at all 9 time points and the proportion of subjects with IOP reduction ≥25% consistently at all 9 time points. RESULTS: Of 420 subjects randomized, 387 completed the study (LBN 0.024%, n = 264; timolol 0.5%, n = 123). At all 9 time points, the mean IOP in the study eye was significantly lower in the LBN 0.024% group than in the timolol 0.5% group (P ≤ 0.002). At all 9 time points, the percentage of subjects with mean IOP ≤18 mmHg and the percentage with IOP reduction ≥25% were significantly higher in the LBN 0.024% group versus the timolol 0.5% group (mean IOP ≤18 mmHg: 22.9% vs. 11.3%, P = 0.005; IOP reduction ≥25%: 34.9% vs. 19.5%, P = 0.001). Adverse events were similar in both treatment groups. CONCLUSIONS: In this phase 3 study, LBN 0.024% qpm demonstrated significantly greater IOP lowering than timolol 0.5% BID throughout the day over 3 months of treatment. Latanoprostene bunod 0.024% was effective and safe in these adults with OAG or OHT.

Abstract licence: CC BY-NC-ND

Glaucoma is a progressive, chronic optic neuropathy characterized by a typical visual field defects. Four main classes of topical medication are actually available on the market: beta-blockers, prostaglandins, alpha2-agonists, and topical carbonic anhydrase inhibitor to treat intraocular pressure (IOP). The aim of this review is to outline the efficacy of timolol and to evaluate the impact of this treatment on patients' quality of life. Among beta-blockers, timolol is most used at three different concentrations: 0.1%, 0.25%, and 0.5%. While the first one is a gel, the other two products are solution. Timolol has few topical side effects, while it has some important systemic side effects on the cardiac and respiratory systems. The balance between efficacy and safety is always the main aspect to care patients. Because of the less efficacy of timolol 0.1% solution, the possibility to use carbomers as vehicle in the gel drops helped timolol 0.1 to be used in clinics, extending the time contact between the active ingredient and the surface of the cornea. Using preservative-free timolol 0.1 for treatment, IOP was at the same level of the other beta-blockers at higher concentration, but it was better tolerated. Preservative-free treatment improved the quality of life reducing dry-eye like symptoms; furthermore, the presence of an artificial tear in the medication bottle could help adherence. The once daily dosing improves compliance.

Abstract licence: CC BY