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timolol (timolol, Merck / Timoptol)

✓ Approved

Teva Pharmaceutical Industries Ltd. · ADRB1 · 小分子

什么是 timolol？

timolol 是一种小分子，由Teva Pharmaceutical Industries Ltd.研发。该药已获批，用于治疗相关适应症，给药途径：Others。

药物档案

商品名timolol, Merck, Timoptol
公司Teva Pharmaceutical Industries Ltd.
药物类别小分子
分子靶点ADRB1, ADRB2
给药途径Others
状态Approved
来源： ClinicalTrials.gov, Teva Pharmaceutical Industries Ltd.

作用机制

分子靶点

timolol 作用于 2 个分子靶点：

ADRB1adrenoceptor beta 1 (B1AR, RHR)
ADRB2adrenoceptor beta 2 (B2AR, ADRBR)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

timolol 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Eye disordersGlaucoma✓ Approved

相关研究文献

PubMedAmerican journal of ophthalmology case reports2026-10-25

Recurrent delayed hyphema following latanoprost/netarsudil initiation in an eye with a XEN 63 gel stent: a case report.

Greco Antonio A, Calabresi Valerio V, Marenco Maria M, Garavelli Fabio F et al.

To describe recurrent delayed hyphema following initiation of fixed-dose latanoprost/netarsudil in an eye with a previous XEN 63 gel stent, and to discuss whether the associated IOP reduction may have unmasked a pre-existing peri-implant reflux pathway. A 72-year-old woman with advanced primary open-angle glaucoma and previous ab interno XEN 63 gel stent implantation developed recurrent spontaneous hyphema shortly after bimatoprost/timolol was replaced with latanoprost/netarsudil. Intraocular pressure decreased from 17-19 mmHg to 8-9 mmHg after treatment initiation. The first episode occurred nine days later, with blurred vision, a small anterior chamber hyphema, and fine endothelial blood deposits. Gonioscopy showed active blood reflux from tissue surrounding the proximal intracameral XEN segment, without bleeding from other angle structures. Recurrent episodes occurred despite conservative management and, subsequently, despite discontinuation of latanoprost/netarsudil. Because the peri-implant region was repeatedly identified as the reflux site, the XEN stent was eventually removed. No further bleeding episodes were observed after explantation. The clinical course is consistent with a susceptible peri-implant anatomical configuration contributing to recurrent blood reflux. The temporal association between latanoprost/netarsudil initiation, marked IOP reduction, and the first hyphema suggests a possible precipitating or unmasking role, but does not establish drug causality. Delayed or recurrent hyphema after XEN implantation should prompt review of recent medication changes and careful gonioscopic inspection of the proximal XEN segment.

PMID 42927338
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PubMedActa ophthalmologica2026-10-24

Therapeutic efficacy and systemic pharmacokinetics of a dual-drug hydrogel contact lens for sustained glaucoma therapy.

Varshitha Vangol V, Sankararajan Umadevi U

Conventional topical therapy for glaucoma is limited by poor ocular bioavailability, rapid precorneal drug loss, frequent dosing and systemic absorption through the nasolacrimal pathway, which may reduce therapeutic efficacy and increase the risk of adverse effects. Drug-eluting hydrogel contact lenses have emerged as a promising strategy to overcome these limitations by enabling sustained ocular drug delivery. This study aimed to evaluate the therapeutic efficacy, ocular biocompatibility and systemic pharmacokinetic profile of an optimized dual-drug-loaded HEMA-based hydrogel contact lens delivering timolol maleate (TM) and brimonidine tartrate (BT) for sustained glaucoma management. Optimized hydrogel contact lenses composed of 2-hydroxyethyl methacrylate (HEMA), N, N-dimethylacrylamide (DMA), N-vinylpyrrolidone (NVP) and ethylene glycol dimethacrylate (EGDMA) were fabricated by UV photopolymerization and loaded with TM and BT (4 mg/mL each). Ocular biocompatibility was assessed using the modified Draize irritation test. Therapeutic efficacy was evaluated in a steroid-induced ocular hypertension New Zealand White rabbit model by monitoring intraocular pressure (IOP) for 24 h. Systemic drug exposure was determined by validated high-performance liquid chromatography (HPLC) analysis of plasma samples, while ocular safety was further confirmed through histopathological examination. The optimized hydrogel lens exhibited excellent ocular biocompatibility, with a maximum Draize score of 0.33 ± 0.12 that resolved completely within 48 h and no histopathological evidence of ocular tissue damage. In hypertensive rabbits, the dual-drug hydrogel lens maintained normotensive IOP (16.1 ± 0.8 mmHg) for 24 h, representing a 43.5% reduction from baseline and significantly outperforming conventional eye drops beyond 4 h (p < 0.01). Plasma concentrations of both TM and BT remained below the limit of quantification (<2.0 ng/mL) throughout the study, whereas conventional eye drops produced measurable systemic exposure (TM: 18.4 ± 2.1 ng/mL; BT: 8.2 ± 1.2 ng/mL), demonstrating effective minimization of systemic drug absorption. The optimized dual-drug-loaded hydrogel contact lens provided sustained intraocular pressure reduction, excellent ocular biocompatibility and negligible systemic drug exposure compared with conventional topical therapy. These findings highlight its potential as a sustained ocular drug-delivery platform capable of improving therapeutic efficacy, reducing systemic adverse effects and enhancing long-term treatment adherence in glaucoma management. Further long-term preclinical investigations and clinical studies are warranted to support clinical translation.

PMID 42920388
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PubMedIndian journal of ophthalmology2026-10-16

Gonioscopy-assisted transluminal trabeculotomy versus trabeculectomy with phacoemulsification in primary open angle glaucoma - One-year outcomes.

Maheshwari Devendra D, Shivakumar Shreedhar S, Pillai Madhavi R MR, Nagdev Nimrita Gyanchand NG et al.

To assess the safety and efficacy of gonioscopy-assisted transluminal trabeculotomy (GATT) with phacoemulsification in primary open-angle glaucoma (POAG). In this prospective, nonrandomized, comparative study, patients with POAG underwent either phaco-GATT (Group A, n = 75) or phacotrabeculectomy (Group B, n = 77) and were followed up for one year. Changes in intraocular pressure (IOP), antiglaucoma medications (AGMs), complications, and success rates over one year were compared. Success rate was described under two criteria: 1: IOP between 6 and 21 mmHg and a decrease of >20% from the baseline; 2: IOP between 6 and 18 mmHg and a decrease of >25% from the baseline. Mean IOP decreased by 25.1%, from 17.93 ± 4.29 mmHg to 13.00 ± 3.18 mmHg (P < 0.001) in Group A (n = 70) and by 28% from 17.81 ± 4.52 mmHg to 12.16 ± 3.28 mmHg (P < 0.001) in Group B (n = 74) at one year. AGM reduced from 1.03 ± 0.43 to 0.09 ± 0.29 in Group A (P < 0.001) and from 1.04 ± 0.41 to 0.16 ± 0.37 in Group B (P < 0.001), with no significant difference between the groups (P = 0.24). 91.4% of patients in Group A and 85.1% in Group B were free of medications. The cumulative one-year success was 68% and 63.6% by Criteria 1 (P = 0.52) and 60% and 50.7% by Criteria 2 (P = 0.23) in Groups A and B, respectively, with no significant difference between the groups. Sixteen patients in Group A had microhyphema, seven had macrohyphema, and two patients underwent anterior chamber (AC) wash. Four patients in Group B had hypotony, one required conjunctival resuturing, and one required AC reformation. Phaco-GATT demonstrated comparable intraocular pressure reduction, medication independence, and surgical success rates to phacotrabeculectomy at one year, with minimal complications.

PMID 42885835
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PubMedArquivos brasileiros de oftalmologia2026-10-15

Bovine pericardium as a patch graft in glaucoma drainage implant surgery: a case series.

Endo Camila Matsuura CM, Sousa Luciene Barbosa de LB, Fernandes Rodrigo Antônio Brant RAB, Andrade Mirella Millena Carmo de MMC et al.

To evaluate the short-term safety and efficacy of bovine pericardium as a patch graft in glaucoma drainage implant surgery. We included 10 eyes from 10 patients with glaucoma. All patients underwent glaucoma drainage implant surgery using a bovine pericardial patch graft. The pericardial membrane was trimmed to 5 × 7 mm and used to cover the tube's scleral track. Intraocular pressure, best-corrected visual acuity, and the number of antiglaucoma medications were assessed preoperatively and postoperatively on Days 1, 7, 14, 28, 45, 60, 75, and 90. Conjunctival hyperemia and intraocular inflammation were clinically graded postoperatively. Symptoms, including foreign body sensation, itching, and tearing, as well as postoperative complications, were recorded. Surgical failure was defined as tube exposure resulting from erosion of the overlying patch graft and conjunctiva. The mean patient age was 63.4±15.6 years (range, 45-87 years). The most common postoperative symptom was foreign body sensation. During follow-up, three eyes developed asymptomatic thinning of the pericardial graft overlying the tube; in one of these eyes, the thinning progressed to tube exposure (10.0%; 95% CI, 0.3-44.5). No cases of endophthalmitis were observed. In this short-term follow-up study, bovine pericardium may be a viable alternative for coverage of glaucoma drainage implants. Larger studies with longer follow-up periods are warranted to confirm these findings.

PMID 42879646
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PubMedJournal of the Chinese Medical Association : JCMA2026-10-14

Nonselective beta-blockers and hepatic encephalopathy in liver cirrhosis:A meta-analysis of randomized controlled trials.

Kuo Tai-Hui TH, Chen Yu-Jen YJ, Lee Pei-Chang PC, Yang Tsung-Chieh TC et al.

Liver cirrhosis leads to portal hypertension and related complications, including ascites, esophageal varices, and hepatic encephalopathy (HE). Non-selective beta blockers (NSBBs) decrease portal pressure, but it is not yet clear whether they contribute to HE development. Therefore, we examined the association between NSBB therapy and HE in randomized controlled trials (RCTs) involving patients with cirrhosis. We systematically searched PubMed, Web of Science, ScienceDirect, and the Cochrane Library (from inception to December 31, 2024) for RCTs comparing NSBBs with a placebo, endoscopic band ligation, or injection sclerotherapy for variceal bleeding prevention in relation to HE. The risk ratios (RRs) and 95% confidence intervals (CIs) were pooled using a random-effects model. Subgroups were defined according to the comparator, NSBB type, and hepatic function status (weighted mean Child-Pugh score ≤6 vs. >6). The risk of bias was assessed using the revised Cochrane risk-of-bias tool for randomized trials (RoB 2). There were 12 relevant studies, which included 775 NSBB-treated and 771 comparator patients (54 and 57 HE events). NSBB therapy was not associated with a statistically significant change in HE risk (RR 1.04, 95% CI 0.73-1.47; p = 0.84; I² = 0%). Estimates were consistent across all subgroups of hepatic function statuses (compensation, RR 1.18, 0.44-3.14; decompensation, RR 1.02, 0.70-1.48; p = 0.79), comparators (placebo, RR 1.19, 0.79-1.80; endoscopic therapy, RR 0.72, 0.38-1.39; p = 0.20), and NSBB types (propranolol/timolol, RR 1.06, 0.72-1.55; carvedilol, RR 0.95, 0.42-2.15; p = 0.82). Current evidence does not indicate a statistically significant association between NSBB therapy and HE development in patients with cirrhosis, regardless of disease severity.

PMID 42870342
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PubMedActa paediatrica (Oslo, Norway : 1992)2026-10-10

Oral Propranolol Versus Topical Timolol for the Treatment of Infantile Haemangiomas: A Systematic Review and Meta-Analysis of Randomized Controlled Trials.

Weng Liwen L, Zuo Hongli H, Zhao Min M, Dong Jialin J

This systematic review and meta-analysis aimed to compare the efficacy and safety of oral propranolol versus topical timolol for the treatment of superficial infantile haemangiomas. We systematically searched PubMed, Cochrane Library, Embase, Web of Science and China National Knowledge Infrastructure from inception to April 23, 2026. Only randomized controlled trials comparing oral propranolol with topical timolol for superficial infantile haemangiomas were included. Two reviewers independently screened studies, extracted data and assessed risk of bias using the Cochrane risk of bias 2.0 tool. The primary outcomes were overall response rate and incidence of systemic adverse events. Pooled risk ratios (RRs) with 95% confidence intervals (CIs) were calculated using fixed-effect models. Seven randomized controlled trials comprising 428 infants were included. Topical timolol was comparable to oral propranolol in overall response rate (RR = 1.09, 95% CI 0.97-1.23, p = 0.17; I2 = 0%). Topical timolol significantly reduced the risk of systemic adverse events compared with oral propranolol (RR = 0.35, 95% CI 0.20-0.59, p < 0.0001; I2 = 9%). Topical timolol demonstrates comparable efficacy to oral propranolol for superficial infantile haemangiomas and has a significantly superior safety profile with a 65% reduction in systemic adverse events.

PMID 42855991
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