Timolol Maleate 0.25% or 0.5% · ophthalmic gel-forming solution
Antiglaucoma
Approved uses
Elevated IOP in ocular hypertension or open-angle glaucoma
1 drop (0.25% or 0.5%) in the affected eye(s) QD
OFF-LABELNot in the FDA label for this product
Superficial infantile hemangioma, including periocular lesions
Timolol maleate 0.5% gel applied to the lesion, maximum 0.5 mg daily, for 24 weeks (trial regimen)
RCT · n=41 · gel unspecified
Double-blind RCT in 41 infants aged 5 to 24 weeks with non-ulcerated superficial lesions away from mucosal surfaces (32 completed): blinded photographic color improvement at week 24 (P=.003), a higher proportion of treated lesions reduced in size by more than 5% at weeks 20 and 24 (P<.02), and no significant difference in heart rate or blood pressure. Single small trial, and it does not identify the gel used as this product.
Bronchial asthma or a history of bronchial asthma.
Severe chronic obstructive pulmonary disease.
Sinus bradycardia.
Second or third degree atrioventricular block.
Overt cardiac failure.
Cardiogenic shock.
Hypersensitivity to any component of this product.
Available Forms
0.25% and 0.5% gel forming solution, 5 mL in a 7.5 mL dispenser bottle
Mechanism of Action
Non-selective beta-1 and beta-2 adrenergic blocker that lowers elevated and normal IOP, predominantly by reducing aqueous formation, with a slight increase in outflow facility in some studies. The gellan gum vehicle gels on contact with the precorneal tear film and is then removed by tear flow.
Warnings & Precautions
Systemic absorption: Topical dosing can produce the same reactions as systemic beta-blockade, including death from bronchospasm in patients with asthma and, rarely, death in association with cardiac failure.
Cardiac failure: In patients without a history of cardiac failure, continued myocardial depression can lead to failure; discontinue at the first sign or symptom.
Obstructive pulmonary disease: Patients with mild or moderate COPD or bronchospastic disease should generally not receive beta-blockers.
Perioperative beta-blockade: Impairs the ability of the heart to respond to beta-adrenergically mediated reflex stimuli and may augment the risk of general anesthesia; protracted severe hypotension during anesthesia and difficulty restarting and maintaining the heartbeat have been reported, and some authorities recommend gradual withdrawal before elective surgery.
Diabetes mellitus: Masks the signs and symptoms of acute hypoglycemia; caution with labile diabetes or spontaneous hypoglycemia.
Thyrotoxicosis: Masks tachycardia and other signs of hyperthyroidism; abrupt withdrawal may precipitate thyroid storm.
Anaphylaxis: Patients with atopy or prior severe anaphylaxis may be more reactive on re-challenge and unresponsive to usual epinephrine doses.
Myasthenic symptoms: Beta-blockade can potentiate diplopia, ptosis, and generalized weakness.
Angle-closure glaucoma: Little or no effect on the pupil, so not for use alone in angle closure.
Choroidal detachment: Reported with aqueous suppressant therapy after filtration procedures.
Cerebrovascular insufficiency: Consider alternative therapy if signs of reduced cerebral blood flow develop after starting treatment.
Common Side Effects
Ocular, blurred vision: Transient in about 1 in 3 patients, lasting 30 seconds to 5 minutes, and able to impair driving or operating machinery; fewer than 1% of trial patients discontinued for it.
Ocular, instillation discomfort: Burning and stinging in about 1 in 8 patients, comparable to timolol ophthalmic solution.
Ocular, 1% to 5%: Pain, conjunctivitis, discharge, foreign body sensation, itching, tearing.
Ocular, less common: Blepharitis, keratitis, dry eye, ptosis, decreased corneal sensitivity, cystoid macular edema, pseudopemphigoid, choroidal detachment after filtration surgery.
Systemic, 1% to 5%: Headache, dizziness, upper respiratory infection.
Systemic, less common: Bradycardia, arrhythmia, hypotension, heart block, cardiac failure, bronchospasm (predominantly in patients with pre-existing bronchospastic disease), depression, increased signs and symptoms of myasthenia gravis.
Heart rate: Mean resting reduction of 3.8 beats/min at 2 hours and 0.8 beats/min at 24 hours after the 0.5% dose.
Pregnancy & Lactation
Pregnancy: No adequate and well-controlled studies in pregnant women; use only if the potential benefit justifies the potential fetal risk (animal studies showed no malformations, with increased fetal resorptions in rabbits at 14,000 times the ophthalmic exposure without maternotoxicity).
Lactation: Timolol is detected in human milk after oral and ophthalmic dosing; decide whether to stop nursing or the drug, weighing its importance to the mother.
Bacterial keratitis: Reported with inadvertently contaminated multi-dose containers, mostly in eyes with concurrent corneal disease or a disrupted epithelial surface.
Contact lens wear: Not studied in patients wearing contact lenses.
Additive beta-blockade: Oral beta-blockers, calcium antagonists, digitalis, and CYP2D6 inhibitors can potentiate systemic effects; two topical beta-blockers together are not recommended.
Pediatric Use
Established at 2 years and older; not established below 2 years.
Timoptic XE (Timolol Maleate 0.25% or 0.5%) | EyeKnow O.D.
Available Forms
Mechanism of Action
Pregnancy & Lactation
Pediatric Use