Timolol: Difference between revisions

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Latest revision as of 07:13, 23 May 2026

Beta blocker (non-selective), Antiglaucoma medicine, Antihypertensive, Migraine prophylactic

Timolol (maleate)

Timoptic (ophthalmic), Timoptic-XE (gel-forming once-daily), Istalol (once-daily 0.5%), Betimol; Blocadren (oral, discontinued in many markets); combination eye drops Combigan (with brimonidine), Cosopt (with dorzolamide)

Experience

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Problems

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Titration strategies

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Effects

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Summary

Classes

Beta blocker (non-selective), Antiglaucoma medicine, Antihypertensive, Migraine prophylactic

Common uses

Open-angle glaucoma and ocular hypertension (FDA, ophthalmic; the dominant current use)0, Hypertension (FDA, oral)0, Post-myocardial-infarction secondary prevention (FDA, oral)0, Migraine prophylaxis (FDA, oral)0

Pharmacy

Starting dose

Ophthalmic: 1 drop 0.5% in affected eye(s) BID (or once daily for XE / Istalol). Oral hypertension: 10 mg PO BID, titrate to 60 mg/day. Migraine prophylaxis: 10 mg BID, titrate to 30 mg/day

Preparations

Tablets 5, 10, 20 mg; ophthalmic solution 0.25%, 0.5%; ophthalmic gel-forming solution 0.25%, 0.5% (Timoptic-XE)

US FDA Max

60 mg/day (oral, hypertension); 0.5% BID (ophthalmic)

Pharmacology

Routes

Oral, ophthalmic

Onset

BP effect within hours (oral); IOP reduction within 30 minutes, full effect 1-2 weeks (ophthalmic)

Duration

12 hours (oral BID); 24 hours (Timoptic-XE)

Half-life

~4 hours (oral)^[1]

Bioavailability

~50% (oral); systemic absorption from ophthalmic application is clinically meaningful via nasolacrimal drainage^[1]

Pregnancy

Limited human data; β-blocker class effects include fetal growth restriction and neonatal bradycardia/hypoglycemia.^{[citation needed]}

Legal status

Rx-only in US

Purported mechanism

Non-selective β1 and β2 adrenergic receptor antagonist. Ophthalmic application reduces aqueous humor production at ciliary-body β2 receptors, lowering intraocular pressure 20-30%, the basis of the glaucoma indication. Systemic oral use achieves the standard β-blocker effects on heart rate, contractility, and renin secretion.0 Systemic absorption from eye drops is clinically meaningful via nasolacrimal drainage, producing bradycardia, bronchospasm (worth considering in asthma and COPD), and hypoglycemia masking in diabetic patients. Nasolacrimal occlusion (pressing on the inner canthus for 1-2 minutes after instillation) reduces systemic exposure by approximately 70% and is the standard counseling pearl^[1].

References

↑ ^1.0 ^1.1 ^1.2 FDA Prescribing Information, Timoptic (timolol maleate ophthalmic solution), Bausch & Lomb/Merck, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/018086s068lbl.pdf

[timoptic-label-1] 1.0 ^1.1 ^1.2 FDA Prescribing Information, Timoptic (timolol maleate ophthalmic solution), Bausch & Lomb/Merck, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/018086s068lbl.pdf

[1]

@@ Line 1: / Line 1: @@
-{{Stub}}
 {{MedTemplate
-| generic = Timolol
+| generic           = Timolol (maleate)
-| brand   = Blocadren
+| brand             = Timoptic (ophthalmic), Timoptic-XE (gel-forming once-daily), Istalol (once-daily 0.5%), Betimol; Blocadren (oral, discontinued in many markets); combination eye drops Combigan (with brimonidine), Cosopt (with dorzolamide)
-| classes = Beta blocker
+| structure         =
-| intro   = Timolol is a non-selective beta blocker. In addition to cardiovascular uses, it is widely used as an eye drop in the treatment of glaucoma.
+| classes           = [[:Category:Beta blockers|Beta blocker (non-selective)]], [[:Category:Antiglaucoma medicines|Antiglaucoma medicine]], [[:Category:Antihypertensives|Antihypertensive]], [[:Category:Migraine prophylactics|Migraine prophylactic]]
+| uses              = <vote slug="open-angle-glaucoma-use">Open-angle glaucoma and ocular hypertension (FDA, ophthalmic; the dominant current use)</vote>, <vote slug="hypertension-use">Hypertension (FDA, oral)</vote>, <vote slug="post-mi-use">Post-myocardial-infarction secondary prevention (FDA, oral)</vote>, <vote slug="migraine-prophylaxis-use">Migraine prophylaxis (FDA, oral)</vote>
+| starting_dose     = Ophthalmic: 1 drop 0.5% in affected eye(s) BID (or once daily for XE / Istalol). Oral hypertension: 10 mg PO BID, titrate to 60 mg/day. Migraine prophylaxis: 10 mg BID, titrate to 30 mg/day
+| preparations      = Tablets 5, 10, 20 mg; ophthalmic solution 0.25%, 0.5%; ophthalmic gel-forming solution 0.25%, 0.5% (Timoptic-XE)
+| fda_max           = 60 mg/day (oral, hypertension); 0.5% BID (ophthalmic)
+| pill_id           =
+| routes            = Oral, ophthalmic
+| onset             = BP effect within hours (oral); IOP reduction within 30 minutes, full effect 1-2 weeks (ophthalmic)
+| duration          = 12 hours (oral BID); 24 hours (Timoptic-XE)
+| halflife          = ~4 hours (oral)<ref name="timoptic-label">FDA Prescribing Information, Timoptic (timolol maleate ophthalmic solution), Bausch & Lomb/Merck, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/018086s068lbl.pdf</ref>
+| bioavailability   = ~50% (oral); systemic absorption from ophthalmic application is clinically meaningful via nasolacrimal drainage<ref name="timoptic-label" />
+| pregnancy         = Limited human data; β-blocker class effects include fetal growth restriction and neonatal bradycardia/hypoglycemia.{{citation needed}}
+| legal             = [[USLegal:Prescription only|Rx-only]] in US
+| mechanism         = <vote slug="timolol-mech-claim">Non-selective β1 and β2 adrenergic receptor antagonist. Ophthalmic application reduces aqueous humor production at ciliary-body β2 receptors, lowering intraocular pressure 20-30%, the basis of the glaucoma indication. Systemic oral use achieves the standard β-blocker effects on heart rate, contractility, and renin secretion.</vote> '''Systemic absorption from eye drops is clinically meaningful''' via nasolacrimal drainage, producing bradycardia, bronchospasm (worth considering in asthma and COPD), and hypoglycemia masking in diabetic patients. '''Nasolacrimal occlusion''' (pressing on the inner canthus for 1-2 minutes after instillation) reduces systemic exposure by approximately 70% and is the standard counseling pearl<ref name="timoptic-label" />.
 }}
+== References ==
+<references />
+[[Category:Beta blockers]]
+[[Category:Antiglaucoma medicines]]
+[[Category:Antihypertensives]]
+[[Category:Migraine prophylactics]]

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