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timolol (Ophtim / timolol, Thea)

✓ Approved

Takeda · ADRB1 · 小分子

什么是 timolol？

timolol 是一种小分子，由Takeda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Ophtim, timolol, Thea
公司Takeda
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, Takeda

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

PubMedCureus2026-06-05

Postoperative Eyelid Pyogenic Granuloma: A Systematic Review of Clinical Features, Surgical Associations, and Management.

Cheung Imogen I, Cheung David D

Pyogenic granuloma (lobular capillary haemangioma) is a benign vascular lesion that may arise following trauma, inflammation, or surgery. In oculoplastic practice, it represents a recognised but likely underreported postoperative complication. We present a case of recurrent pyogenic granuloma arising from a posterior lamellar defect following eyelid reconstruction using a Hughes flap, highlighting key clinical features and management considerations. A systematic review of the literature was also performed to contextualise this case, identifying 14 studies comprising 498 cases. Lesions typically presented within weeks of surgery as rapidly growing, friable, pedunculated masses arising at sites of surgical disruption. While topical therapies such as corticosteroids and timolol may be effective in selected cases, surgical excision remains the most reliable treatment and allows histological confirmation. This case and systematic review support the theory that postoperative pyogenic granuloma represents a manifestation of dysregulated wound healing driven by aberrant angiogenesis at sites of epithelial disruption.

PMID 42245883
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PubMedDrug design, development and therapy2026-05-29

Co-Administration of MPC Polymer Enhances the Ocular Absorption and Intraocular Pressure-Lowering Effect of Timolol Maleate.

Otake Hiroko H, Ogata Fumihiko F, Kawasaki Naohito N, Sasaki Ayano A et al.

We previously developed a novel 2-methacryloyloxyethyl phosphorylcholine-based polymer (MPCP) containing a zwitterionic stearyl methacrylate moiety and an acrylic functional group, which significantly improved moisture retention on the ocular surface. In this study, we investigated whether incorporating 0.1% MPCP into 0.25% or 0.5% timolol maleate (TM) ophthalmic formulations could enhance the ocular surface retention, corneal permeability, and intraocular pressure (IOP)-lowering efficacy of TM. Male Wistar rats (7 weeks old) and male adult rabbits (body weight: 2.39 ± 0.71 kg) were used to evaluate ocular surface retention and corneal permeability of TM. IOP-lowering efficacy of TM was evaluated using a rabbit treated with 5% glucose solution (high IOP model). The TM ophthalmic formulations with MPCP (TM@MPCP-OF) were transparent, with MPCP nanoparticles (mean particle size 80.7 nm) dispersed in the formulation, and exhibited stable viscosity, regardless of the presence of MPCP (approximately 0.95-1.1 mPa∙s). The addition of MPCP reduced cytotoxicity in human corneal epithelial cells (HCE-T) and caused no damage after repeated instillation in rats. Moreover, the combination with MPCP improved TM retention on the ocular surface and increased the corneal TM concentration and aqueous humor penetration after the instillation of TM@MPCP-OF. In addition, the corneal permeability-enhancing effect of MPCP on the TM was more pronounced with TM@MPCP-OF containing 0.5% TM than with TM@MPCP-OF containing 0.25% TM. Furthermore, compared with the TM ophthalmic formulation alone, MPCP co-administration significantly prolonged the duration and magnitude of the IOP-lowering effect of TM in a rabbit model of acute ocular hypertension. These findings indicate that MPCP is a safe and biocompatible additive that enhances the pharmacological performance of ophthalmic formulations and may contribute to the development of improved and longer-acting antiglaucoma medications.

PMID 42212190
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PubMedDermatology and therapy2026-05-26

Topical Timolol Beyond Infancy: A Retrospective Study of Its Use in Persistent Infantile Hemangiomas.

Bogomolets Olga O, Bogomolets-Sheremetieva Sofiia S

Infantile hemangiomas (IH) usually undergo spontaneous involution; however, some lesions remain visible after infancy and may cause psychosocial distress in children and their families. Evidence regarding the effectiveness of topical beta-blockers when treatment is initiated after infancy remains limited. This real-world study evaluated the efficacy of topical timolol therapy in children aged 1-5 years with persistent IH. Children with IH were evaluated at a specialized vascular anomalies center in Ukraine between 2019 and 2024. Parents of children older than 1 year with persistent visible IH associated with psychosocial distress were offered vascular laser therapy or topical timolol treatment. Because topical therapy could be administered safely at home under remote medical supervision during ongoing military action, all families chose this option. A short initial treatment period of 2-4 weeks was used to assess the therapeutic response, and treatment was continued if improvement was observed. A total of 2419 children with IH were evaluated during the study period. Among them, 1287 patients used topical timolol as monotherapy. Treatment was initiated after the age of 1 year in 113 patients with persistent lesions. Positive outcomes were observed in 1151 (98.04%) patients who started therapy before the age of 1 year and in 78 (69.03%) patients who initiated treatment between 1 and 5 years of age (p < 0.001). Topical timolol 0.5% demonstrated limited effectiveness in older children, whereas switching to topical timolol 1% resulted in clinical improvement. In six patients previously treated with systemic beta-blockers, topical timolol remained effective even after systemic therapy had lost effectiveness. Natural involution of IHs may be partially responsible for the positive effect observed in some of our patients. These findings suggest that topical timolol 1% may provide clinically meaningful improvement in persistent IH beyond infancy and support telemedicine-based treatment when access to in-person care is limited.

PMID 42189400
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PubMedCureus2026-05-11

Importance of History in the Management of New-Onset Hyperkalemia.

Kagan Igor I, Sarmosyan Kristine K, Lei Sean S, Hwang Michelle M

Hyperkalemia is a life-threatening disorder with a multitude of causes. We present a case of a 64-year-old woman with new-onset hyperkalemia. A patient with a documented history of normokalemia developed consistent hyperkalemia on repeat blood testing. The patient was initially managed by her primary care physician, then referred to nephrology for persistent hyperkalemia, at which point sodium polystyrene sulfonate was initiated. The patient presented for a second opinion on the hyperkalemia, and after a thorough history and chart review, it was determined that the patient's dorzolamide-timolol eye drops were the cause of the hyperkalemia. Discontinuation of the eye drops resolved the hyperkalemia.

PMID 42110035
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PubMedAmerican journal of physiology. Regulatory, integrative and comparative physiology2026-05-11

Intracardiac neuromodulation of pacemaker rate in the adult zebrafish heart in vitro.

O'Shea Keegan P D KPD, Long Zachary D ZD, Smith Frank M FM

Heart rate (HR) in vertebrates is determined by the discharge frequency of cardiac pacemaker cells, which are innervated by the autonomic nervous system. The portion of this system located within the heart, the intracardiac nervous system (ICNS), transmits impulses to cardiac effectors for control of cardiac output. Central autonomic neurons modulate the heart through sympathetic (acceleratory) and parasympathetic (inhibitory) axons in the vagosympathetic trunks. In the classical model of cardiac control, the balance between sympathetic and parasympathetic efferent signals determines HR. Recent evidence of spontaneous neural activity within the ICNS in isolated hearts suggests a local regulatory element in cardiac control. We examined the potential for ICNS modulation of HR in the isolated zebrafish heart, using atropine to block parasympathetic drive to the pacemaker and timolol to block sympathetic drive. Atropine (3, 10, and 30 µM) evoked tachycardia of similar magnitude at 22 and 28°C. Timolol (3, 10, and 30 µM) caused bradycardia at both temperatures, with greater proportional HR responses to all doses at the higher temperature. Our results suggest that both sympathetic and parasympathetic outputs from the ICNS influence the pacemaker, with the degree of sympathetic drive being temperature-sensitive. Intrinsic HR, obtained after dual antagonist application, was not significantly different from HR before drug application so the effects of sympathetic and parasympathetic drive on pacemaker rate appeared to be evenly balanced. We propose that the ICNS in the isolated zebrafish heart is capable of modulating HR in the absence of extracardiac autonomic inputs.NEW & NOTEWORTHY In this study, we show that the intracardiac nervous system, a key integrative pathway for autonomic control of the heart, can modulate pacemaker rate in the absence of extracardiac innervation in the isolated adult zebrafish heart. Pharmacological blockade of muscarinic and β-adrenergic receptors reveals opposing inhibitory and excitatory influences on heart rate, and these effects are eliminated when intracardiac nicotinic synaptic transmission is disrupted with hexamethonium.

PMID 42113566
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PubMedDermatology and therapy2026-05-10

Therapies for Infantile Haemangiomas: Current Practice and Evolving Perspectives.

Nolan B B, O'Connor C C

Infantile haemangiomas (IH) are the most common vascular tumours of infancy, characterised by a predictable trajectory of rapid proliferation, plateau, and slow spontaneous involution. Although most regress uneventfully, a significant minority risk ulceration, functional compromise, or disfigurement, and therefore require timely intervention. The therapeutic landscape was once dominated by corticosteroids, interferon, and cytotoxic chemotherapeutics of modest efficacy and considerable toxicity. Management was revolutionized in 2008 by the discovery that the beta-blocker propranolol induced prompt and sustained regression. Propranolol has since become the established first-line therapy for IH, with efficacy and safety confirmed by randomized controlled trials and corroborated by observational cohorts. Mechanistically there are multiple temporally stratified actions: immediate vasoconstriction, suppression of angiogenic signalling pathways, induction of endothelial apoptosis, and ultimately the promotion of adipogenic differentiation in keeping with natural involution. Safety is favourable under expert supervision, though hypoglycemia remains the principal preventable hazard, necessitating caregiver education on feeding regimens and "sick day" rules. Rebound growth, encountered in roughly one-fifth of cases, usually responds to re-treatment. Alternative beta-blockers such as atenolol and nadolol provide comparable efficacy with potential advantages in tolerability or dosing convenience. Topical timolol has limited effectiveness for small superficial lesions, while sirolimus, becaplermin gel, laser devices, and surgery may have circumscribed adjunctive roles. Corticosteroids and cytotoxic agents are now confined to salvage use. Contemporary perspectives extend beyond pharmacology to encompass caregiver experience and health-system burden. Recent work highlights the low burden of treatment with propranolol, while digital innovations such as photo-triage during the COVID-19 pandemic illustrate opportunities to reduce healthcare exposure and improve equity of access. This review describes the evolution of drug therapy for IH and integrates mechanistic insights, clinical pragmatism, and patient-centred innovations to chart the current trajectory of care.

PMID 42105055
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