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timolol (Timpilo / timolol, ophthalmic)

✓ Approved

Merck & Co. · ADRB1 · 小分子

什么是 timolol？

timolol 是一种小分子，由Merck & Co.研发。该药已获批，用于治疗相关适应症。

药物档案

商品名Timpilo, timolol, ophthalmic
公司Merck & Co.
药物类别小分子
分子靶点ADRB1, ADRB2, CHRM3
状态Approved
来源： ClinicalTrials.gov, Merck & Co.

作用机制

分子靶点

timolol 作用于 3 个分子靶点：

ADRB1adrenoceptor beta 1 (BETA1AR, ADRB1R)
ADRB2adrenoceptor beta 2 (ADRBR, B2AR)
CHRM3cholinergic receptor muscarinic 3 (EGBRS, m3AChR)
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

PubMedGels (Basel, Switzerland)2026-07-27

Evaluation of Propolis and Diclofenac Sodium Eye Drops for Animals: Physicochemical Properties and In Vitro Biological Activity.

Svetikienė Dovilė D, Ambrulaitienė Vita V, Jančiukė Gintarė G, Sarapinienė Ieva I et al.

Eye diseases are common in veterinary clinical practice and are most often treated with topical ophthalmic preparations. Increasing resistance to antimicrobial agents is driving the search for safe and effective alternatives to traditional treatment methods. The aim of this study was to develop and evaluate gel-based ophthalmic formulations based on poloxamer 407 and sodium carboxymethylcellulose, containing propolis extracts and diclofenac sodium, by assessing their physical and chemical properties, antimicrobial activity, and cytotoxicity in vitro. Propolis extracts were prepared using a solvent consisting of ethanol and choline chloride, and the developed formulations were evaluated for pH, viscosity, refractive index, gelation temperature, SIRC cell viability and apoptosis, and antimicrobial activity against clinical and reference bacterial strains. The developed formulations exhibited physicochemical properties suitable for ophthalmic preparations and antimicrobial activity, particularly against Gram-positive bacteria. Most of the concentrations of the active ingredients tested were well tolerated by SIRC cells, although higher concentrations of the ethanol propolis extract caused a greater cytotoxic effect. The results obtained indicate that gelled ophthalmic formulations based on propolis extracts and diclofenac sodium are promising for the further development of topically acting ophthalmic preparations; however, their biological efficacy and safety must be confirmed. The results obtained indicate that gelled ophthalmic formulations based on propolis extracts and diclofenac sodium are promising for the further development of topical ophthalmic preparations; however, their bioavailability and safety must be confirmed by further in vivo studies.

PMID 42505333
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PubMedNeurology international2026-07-27

Route-Specific Meningo-Ophthalmic and Orbitomeningeal Communications Relevant to Middle Meningeal Artery Embolization: A Systematic Review and Meta-Analysis.

Bruna-Mejias Alejandro A, Paez-Allendes Loreto L, Perez-Lira Valentina V, Santander-Chavez Diego D et al.

Meningo-ophthalmic and orbitomeningeal arterial communications comprise route-specific relationships between the middle meningeal artery (MMA) and the ophthalmic or orbital arterial system. Their recognition is relevant to middle meningeal artery embolization because orbital or ophthalmic collateral pathways may create routes for non-target embolization. This systematic review aimed to synthesize the prevalence and anatomical patterns of these communications, using quantitative pooling only where the anatomical definition and denominator were sufficiently coherent. This systematic review and meta-analysis were conducted according to PRISMA 2020 principles and registered in PROSPERO (CRD420261361050). Eligible studies were original human cadaveric anatomical, angiographic, or radiological investigations reporting MMA-ophthalmic or MMA-orbital arterial relationships. After the closure of the full-text retrieval audit, studies and extracted rows were audited by anatomical family, unit of analysis, numerator, denominator, and independence. No global pooled prevalence was calculated across anatomical families. When family-specific pooling was methodologically defensible, proportions were synthesized using logit transformation, restricted maximum likelihood random-effects models, and Hartung-Knapp confidence intervals. Database searches identified 558 records. After removal of 228 duplicates, 330 records were screened, and 285 were excluded by title and abstract. Forty-five reports were sought for retrieval; 10 were not retrieved or were not available as assessable full-text reports after retrieval auditing. Thirty-five full-text reports were assessed; thirteen were excluded for reasons, and three were duplicate reports at the full-text stage. Nineteen studies were included in the qualitative synthesis, and 12 contributed independent data to the final R-ready matrix. MMA arising from the ophthalmic artery was uncommon, with a pooled prevalence of 0.03 (95% CI 0.01 to 0.13; I2 = 75.9%). After excluding the clinically selected chronic subdural hematoma subgroup, the estimate was 0.02 (95% CI 0.01 to 0.06; I2 = 7.7%). The meningolacrimal/lacrimal-MMA route yielded an exploratory pooled proportion of 0.45 (95% CI 0.09 to 0.86; I2 = 95.9%), with substantial anatomical and methodological heterogeneity. The available evidence supports route-specific synthesis rather than a single global prevalence estimate. MMA arising from the ophthalmic artery appears uncommon but procedurally important; however, this estimate should be interpreted as a route-specific estimate across eligible angiographic/anatomical series rather than as a universal anatomical prevalence. Meningolacrimal and lacrimal-MMA routes are frequently described, but their prevalence remains difficult to generalize because detection methods, populations, and denominators differ across studies. Future anatomical and angiographic reports should standardize route definitions, laterality, unit of analysis, and denominator reporting to improve prevalence estimation and procedural safety interpretation.

PMID 42506050
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PubMedPharmacy (Basel, Switzerland)2026-07-27

Sublingual Tropicamide Eye Drops for the Management of Clozapine-Induced Hypersalivation: A Case Series of Seven Patients.

Chatterjee Seshadri Sekhar SS, Das Soumitra S, Agrawal Adesh A

Clozapine-induced hypersalivation (CIH) affects 30-80% of patients on clozapine and is a major contributor of non-adherence. Current managements, largely based on systemic anticholinergics, can worsen other clozapine-related side effects. Here sublingual tropicamide 1% eye drops can be a low-cost alternative worth evaluating. We report a case series of seven patients with schizophrenia treated with sublingual tropicamide 1% ophthalmic solution (4-8 drops/day) for CIH. Treatment response was assessed by patient-reported percentage reduction in salivation. All seven patients reported improvement (25-80%). One patient reported a transient bitter taste; no systemic anticholinergic effects occurred. Sublingual tropicamide was associated with patient-reported improvement in CIH and was well tolerated in this small, uncontrolled series. Its short duration of action and local administration may offer practical advantages over systemic anticholinergics, though the mechanism remains unproven. Randomised trials with validated outcome measures are needed to establish its efficacy and safety.

PMID 42506791
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PubMedAntibiotics (Basel, Switzerland)2026-07-27

Current Recommendations, Antibiotic Resistance, and Emerging Treatments for Gram-Positive Ocular Infections in the United States.

Fenniri Inès I, André Camille C

Severe bacterial keratitis and endophthalmitis are leading causes of corneal scarring, enucleation, and permanent vision loss, and are increasingly complicated by multidrug-resistant Gram-positive ocular pathogens. In the United States, according to the ARMOR surveillance program (2009-2020), methicillin resistance reached 45.9% of intraocular Staphylococcus aureus and 47.9% of coagulase-negative staphylococci (CoNS), with multidrug resistance exceeding 70% among methicillin-resistant intraocular isolates. While new antibiotics have been approved for systemic infections, vancomycin remains the standard of care for severe Gram-positive ocular infections. However, its ophthalmic use is constrained by limited ocular surface tolerability, physical incompatibility with intravitreal ceftazidime, and an association with hemorrhagic occlusive retinal vasculitis. To address this gap and further stimulate the development of next-generation targeted therapies in ophthalmology, this review focuses on current recommendations and new vancomycin alternative treatments for Gram-positive ocular infections in the antibiotic resistance era. This review details the current antimicrobial recommendations for the most frequent ocular infections, followed by the epidemiology and molecular mechanisms of resistance in S. aureus, CoNS, and S. pneumoniae. Finally, this review discusses new drugs that represent promising alternatives to vancomycin in ophthalmology.

PMID 42505673
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PubMedEuropean journal of neurology2026-07-27

Video-Oculographic Saccadic Fatigability Distinguishes Myasthenia Gravis From Unilateral Ocular Motor Cranial Nerve Palsy in Diplopia: A Prospective Diagnostic Study.

Chae Juhee J, Lee Min-Woo MW, Oh Sun-Young SY

To determine whether repetition-based saccadic fatigability measured with three-dimensional video-oculography (VOG) distinguishes myasthenia gravis (MG) from unilateral ocular motor cranial nerve palsy (CNP) in patients with diplopia. In this prospective cross-sectional diagnostic study conducted from August 2022 to July 2024, consecutive patients with MG or unilateral third, fourth, or sixth CNP, and healthy controls underwent repetitive horizontal and vertical saccade testing (±°15 targets; 75 cycles at 0.25 Hz). Prespecified index metrics were percentage change in saccadic range and time to target acquisition from the second saccade to the mean of the last five saccades. Diagnostic discrimination was assessed using receiver operating characteristic (ROC) curves. The cohort comprised 231 participants: 93 with MG, 54 with CNP and 84 healthy controls. MG showed greater repetition-related range decrement and longer time to target acquisition than healthy controls and axis-matched CNP. In the horizontal comparison (MG vs. sixth CNP), AUCs were 0.800 for percentage range change and 0.787 for percentage time-to-target change. In the vertical comparison (MG vs. third/fourth CNP), percentage range change showed the best discrimination (AUC 0.868, 95% CI 0.783 to 0.934); a threshold of -5.95% yielded 79.6% sensitivity and 87.5% specificity. CNP showed early baseline slowing, whereas MG showed progressive hypometria with relatively preserved peak velocity. Repetition-based VOG captures a dynamic fatigability signature in MG that differs from the more static deficit of unilateral ocular motor CNP. Quantitative saccadic fatigability may provide a useful objective adjunct to the neuro-ophthalmic evaluation of diplopia.

PMID 42504749
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PubMedGraefe's archive for clinical and experimental ophthalmology = Albrecht von Graefes Archiv fur klinische und experimentelle Ophthalmologie2026-07-27

Structural and microvascular retinal changes in tamoxifen users assessed by optical coherence tomography and OCT angiography.

Kilic Songul S, Ozturk Mine M, Ağın Abdullah A, Onder Feyza F

To investigate subclinical retinal structural, microvascular, and outer retinal reflectivity changes in women receiving tamoxifen therapy for at least 12 months without clinically apparent retinopathy. A total of 48 eyes from 48 women who had been receiving tamoxifen therapy for at least 12 months and 52 eyes from 52 age-matched healthy female controls were included in the study. Only the right eye of each participant was analyzed to avoid inter-eye correlation. All participants underwent comprehensive ophthalmic examination, swept-source optical coherence tomography (OCT), OCT angiography (OCTA), and quantitative outer retinal reflectivity analysis using ImageJ. Retinal thickness, choroidal thickness, and OCTA-derived vessel density parameters were compared between groups. Absolute and RPE-normalized reflectivity values of the retinal pigment epithelium (RPE), ellipsoid zone (EZ), and external limiting membrane (ELM) were quantified using standardized vertical line-profile analysis. The mean age was 45.9 ± 5.4 years in the tamoxifen group and 46.6 ± 4.7 years in the control group. Retinal thickness parameters, choroidal thickness, and OCTA-derived vessel density metrics of the superficial and deep capillary plexuses and choriocapillaris were comparable between tamoxifen users and controls (all p > 0.05). Mean and central RPE reflectivity were significantly higher in the tamoxifen group than in controls (RPEav, p = 0.037; RPEc, p = 0.003), whereas EZ and ELM reflectivity values and all RPE-normalized relative reflectivity indices did not differ significantly between groups. A localized increase in outer retinal vessel density was observed in the superior sector in tamoxifen users, without corresponding widespread microvascular alterations. No significant correlations were found between duration of tamoxifen exposure and OCT, OCTA, or reflectivity parameters. Tamoxifen therapy for at least 12 months is associated with selective increases in RPE reflectivity despite preserved retinal structure and microvasculature. Quantitative reflectivity analysis may serve as a sensitive, noninvasive marker for early, subclinical retinal stress preceding clinically apparent tamoxifen retinopathy.

PMID 42507182
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