Topical non-selective beta blocker for ophthalmic use
Brand names: Timoptic, Betimol, Istalol
Updated · Methodology
Second line
Timolol lowers IOP in ocular hypertension. EGS 2024 and PPP 2020 position it as second-line monotherapy when prostaglandins are contraindicated and as a component of fixed combinations.
Sources
ICD-10: H40.0 · ICD-11: 9C61.01
First line
Timolol is a topical beta blocker, historically first line for primary open-angle glaucoma before prostaglandins, now second-line monotherapy or add-on. EGS 2024 and SEG/SEO 2023 recommend timolol as an alternative to prostaglandins, especially when these are contraindicated (history of uveitis) or in fixed combinations (Cosopt with dorzolamide, Ganfort with bimatoprost). IOP reduction of 20–25%. Use with caution in patients with COPD, asthma, bradycardia and AV block.
Sources
ICD-10: H40.1 · ICD-11: 9C61.0
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Timolol is registered as eye drops for IOP lowering in glaucoma; AEMPS has not authorised other indications. Off-label topical application of 0.5% solution to superficial cutaneous infantile haemangiomas is common in dermatology – small series and the Cochrane 2018 review (Novoa et al.) suggest possible benefit in small superficial haemangiomas. In Spain, however, AEMPS has formally approved only oral propranolol (Hemangiol – AEMPS 2014) for infantile haemangioma; timolol eye drops remain off-label without comparative RCTs. Occlusive use can produce systemic absorption with bradycardia and bronchospasm in infants. Timolol marketing for androgenetic alopecia rests on small open studies without RCT support; for stage-fright tremor and anxiety, ophthalmic timolol has no data. If timolol was suggested for haemangioma, hair loss or anxiety, consider seeking a second opinion.
Sources
ICD-10: D18.0 · ICD-11: 2E81.2
Non-selective antagonist of β1- and β2-adrenergic receptors without intrinsic sympathomimetic activity. In the ciliary body it blocks β receptors and reduces aqueous humour production by 30–50%. Instillation of 0.25–0.5% solution once or twice daily lowers IOP by 20–25%. Onset at 20 minutes, peak at 1–2 hours, duration 12–24 hours. Systemic absorption is substantial: up to 80% of the dose reaches systemic circulation via the nasal mucosa, so cardiac and pulmonary effects similar to oral beta blockers are possible.
AEMPS summary of product characteristics (section 4.6): there are no adequate data on timolol use in pregnant women, and it should not be used unless clearly necessary. With oral beta-blockers, epidemiological studies found no malformations but did show a risk of intrauterine growth restriction. When beta-blockers were given until delivery, newborns showed signs of beta-blockade (bradycardia, hypotension, respiratory distress, hypoglycaemia). If timolol is used until delivery, the newborn is closely monitored during the first days of life.
Compatible with caution. Hale L2. Transfers into milk in small amounts. Infant bradycardia is possible, especially in preterm infants, so when systemic absorption is appreciable a selective beta blocker or alternative class is preferable. Punctal occlusion reduces systemic exposure.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Verbatim lines from the interaction sections, in the language of the label
«Calcium antagonists : Caution should be used in the coadministration of beta-adrenergic blocking agents, such as preservative-free timolol maleate ophthalmic solution USP in the unit dose vial, and…»FDA, section 7 · Open on DailyMed
«Existe el riesgo de efectos aditivos que dan lugar a hipotensión y/AEMPS, section 4.5 · Open on CIMA
«Clonidine : Oral beta-adrenergic blocking agents may exacerbate the rebound hypertension which can follow the withdrawal of clonidine. There have been no reports of exacerbation of rebound…»FDA, section 7 · Open on DailyMed
«Digitalis and calcium antagonists : The concomitant use of beta-adrenergic blocking agents with digitalis and calcium antagonists may have additive effects in prolonging atrioventricular conduction…»FDA, section 7 · Open on DailyMed
«Digitalis and calcium antagonists : The concomitant use of beta-adrenergic blocking agents with digitalis and calcium antagonists may have additive effects in prolonging atrioventricular conduction…»FDA, section 7 · Open on DailyMed
«Se ha observado potenciación del betabloqueo sistémico (p.ej. disminución de la frecuencia cardíaca, depresión) durante el tratamiento combinado con inhibidores CYP2D6 (p.ej. quinidina, fluoxetina…»AEMPS, section 4.5 · Open on CIMA
«Se ha observado potenciación del betabloqueo sistémico (p.ej. disminución de la frecuencia cardíaca, depresión) durante el tratamiento combinado con inhibidores CYP2D6 (p.ej. quinidina, fluoxetina…»AEMPS, section 4.5 · Open on CIMA
«Se ha observado potenciación del betabloqueo sistémico (p.ej. disminución de la frecuencia cardíaca, depresión) durante el tratamiento combinado con inhibidores CYP2D6 (p.ej. quinidina, fluoxetina…»AEMPS, section 4.5 · Open on CIMA
«Digitalis and calcium antagonists : The concomitant use of beta-adrenergic blocking agents with digitalis and calcium antagonists may have additive effects in prolonging atrioventricular conduction…»FDA, section 7 · Open on DailyMed
«Digitalis and calcium antagonists : The concomitant use of beta-adrenergic blocking agents with digitalis and calcium antagonists may have additive effects in prolonging atrioventricular conduction…»FDA, section 7 · Open on DailyMed
«Established and Other Potentially Significant Drug Interactions: β-Blockers : e.g. carvedilol, metoprolol, timolol beta-blockers Clinical monitoring of patients is recommended. A dose decrease…»FDA, section 7 · Open on DailyMed
«Established and Other Potentially Significant Interactions: Beta-Blockers: e.g., metoprolol carvedilol timolol ↑ beta-blockers Clinical monitoring is recommended for coadministration with…»FDA, section 7 · Open on DailyMed
«β-BLOQUEANTES: Carvedilol Metoprolol Timolol»AEMPS, section 4.5 · Open on CIMA
«Sustratos de CYP2D6: Beta-bloqueantes (metoprolol, propafenona, timolol)»AEMPS, section 4.5 · Open on CIMA
«Established and Other Potentially Significant Drug Interactions: β-Blockers: metoprolol, timolol ↑ beta-blockers Caution is warranted and clinical monitoring of patients is recommended. A dose…»FDA, section 7 · Open on DailyMed
«- timolol solución oftálmica,»AEMPS, section 4.5 · Open on CIMA
«intervalo QT. El uso simultáneo de ondansetrón con fármacos cardiotóxicos (p. ej., antraciclinas como doxorubicina, daunorubicina o trastuzimab), antibióticos (como eritromicina), antifúngicos (como…»AEMPS, section 4.5 · Open on CIMA
«Non-Interactions of Quinidine With Other Drugs: Quinidine has no clinically significant effect on the pharmacokinetics of diltiazem, flecainide, mephenytoin, metoprolol, propafenone, propranolol…»FDA, section 7 · Open on DailyMed
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Timolol is evaluated for the following indications with varying evidence strength: Ocular hypertension (evidence tier A), Open-angle glaucoma (evidence tier A), Infantile hemangioma (evidence tier C). See the full indication matrix with dosing and citations above on this page.
Common side effects of Timolol (≥ 1 in 100): Burning and stinging after instillation, Dry eyes, Superficial punctate keratitis, Blurred vision, Bradycardia and lowered BP, Fatigue and drowsiness. See the Safety section for uncommon and serious reactions.
AEMPS summary of product characteristics (section 4.6): there are no adequate data on timolol use in pregnant women, and it should not be used unless clearly necessary. With oral beta-blockers, epidemiological studies found no malformations but did show a risk of intrauterine growth restriction. When beta-blockers were given until delivery, newborns showed signs of beta-blockade (bradycardia, hypotension, respiratory distress, hypoglycaemia). If timolol is used until delivery, the newborn is closely monitored during the first days of life.
Compatible with caution. Hale L2. Transfers into milk in small amounts. Infant bradycardia is possible, especially in preterm infants, so when systemic absorption is appreciable a selective beta blocker or alternative class is preferable. Punctal occlusion reduces systemic exposure.
Timolol is contraindicated in: Hypersensitivity to timolol or other components; Asthma or severe COPD; Sinus bradycardia (under 50 bpm); Second- or third-degree AV block without pacemaker; Sick sinus syndrome. Full list in the Safety section.
Direct links to regulator labels. Open in a new tab.
Travoprost, Bimatoprost, Brimonidine, Carbomer, Hypromellose, Lutein + zeaxanthin, Dorzolamide, Latanoprost