Travellers familiar with Timoptic from their home market may be surprised by how scattered its registration is — the brand is available in just eight countries, including Canada, Switzerland, Russia, Peru, and the United States. The active ingredient is timolol, classified within the ophthalmological and antiglaucomatous categories as a beta-adrenolytic agent delivered as an eye preparation.
Timolol-containing eye drops are prescribed in the management of glaucoma and ocular hypertension — conditions in which pressure inside the eye is elevated and benefits from long-term pharmacological control. The structured indication list on this page reflects the registered uses in the specific markets where Timoptic is sold, and a reader using this page to identify a familiar prescription abroad will want to compare against that block.
Outside its registered countries, the Timoptic brand itself is unlikely to appear on a pharmacy shelf, but timolol as a molecule is one of the most internationally established ophthalmic agents and is sold under a variety of other brand names. A patient who has been using Timoptic at home and is travelling or relocating will generally find timolol-containing products available in the destination country, though the specific brand, packaging, and bottle format will differ.
Other medications in the broader antiglaucomatous class also exist worldwide, working through different mechanisms and prescribing patterns. A local pharmacist or ophthalmologist familiar with the regional formulary is the appropriate person to identify an equivalent product. Glaucoma therapy is individualised and continuous, so any change of medication — whether a substitution of brand or a switch to a different molecule — should be made together with a healthcare provider rather than improvised at a pharmacy counter.
There have been reports of inadvertent overdosage with TIMOPTIC Ophthalmic Solution resulting in systemic effects similar to those seen with systemic beta-adrenergic blocking agents such as dizziness, headache, shortness of breath, bradycardia, bronchospasm, and cardiac arrest.
Overdosage has been reported with timolol maleate tablets. A 30-year-old female ingested 650 mg of timolol maleate tablets (maximum recommended oral daily dose is 60 mg) and experienced second and third degree heart block. She recovered without treatment but approximately two months later developed irregular heartbeat, hypertension, dizziness, tinnitus, faintness, increased pulse rate, and borderline first degree heart block.
An in vitro hemodialysis study, using 14C timolol added to human plasma or whole blood, showed that timolol was readily dialyzed from these fluids; however, a study of patients with renal failure showed that timolol did not dialyze readily.
TIMOPTIC is contraindicated in patients with (1) bronchial asthma; (2) a history of bronchial asthma; (3) severe chronic obstructive pulmonary disease ; (4) sinus bradycardia; (5) second or third degree atrioventricular block; (6) overt cardiac failure ; (7) cardiogenic shock; or (8) hypersensitivity to any component of this product.
The most frequently reported adverse experiences have been burning and stinging upon instillation (approximately one in eight patients).
The following additional adverse experiences have been reported less frequently with ocular administration of this or other timolol maleate formulations:
Body As A WholeHeadache, asthenia/fatigue, and chest pain.
CardiovascularBradycardia, arrhythmia, hypotension, hypertension, syncope, heart block, cerebral vascular accident, cerebral ischemia, cardiac failure, worsening of angina pectoris, palpitation, cardiac arrest, pulmonary edema, edema, claudication, Raynaud's phenomenon, and cold hands and feet.
DigestiveNausea, diarrhea, dyspepsia, anorexia, and dry mouth.
ImmunologicSystemic lupus erythematosus.
Nervous System/PsychiatricDizziness, increase in signs and symptoms of myasthenia gravis, paresthesia, somnolence, insomnia, nightmares, behavioral changes and psychic disturbances including depression, confusion, hallucinations, anxiety, disorientation, nervousness, and memory loss.
SkinAlopecia and psoriasiform rash or exacerbation of psoriasis.
HypersensitivitySigns and symptoms of systemic allergic reactions, including anaphylaxis, angioedema, urticaria, and localized and generalized rash.
RespiratoryBronchospasm (predominantly in patients with preexisting bronchospastic disease), respiratory failure, dyspnea, nasal congestion, cough and upper respiratory infections.
EndocrineMasked symptoms of hypoglycemia in diabetic patients.
Special SensesSigns and symptoms of ocular irritation including conjunctivitis, blepharitis, keratitis, ocular pain, discharge (e.g., crusting), foreign body sensation, itching and tearing, and dry eyes; ptosis; decreased corneal sensitivity; cystoid macular edema; visual disturbances including refractive changes and diplopia; pseudopemphigoid; choroidal detachment following filtration surgery ; and tinnitus.
UrogenitalRetroperitoneal fibrosis, decreased libido, impotence, and Peyronie's disease.
The following additional adverse effects have been reported in clinical experience with ORAL timolol maleate or other ORAL beta-blocking agents and may be considered potential effects of ophthalmic timolol maleate: Allergic: Erythematous rash, fever combined with aching and sore throat, laryngospasm with respiratory distress; Body as a Whole: Extremity pain, decreased exercise tolerance, weight loss; Cardiovascular: Worsening of arterial insufficiency, vasodilatation; Digestive: Gastrointestinal pain, hepatomegaly, vomiting, mesenteric arterial thrombosis, ischemic colitis; Hematologic: Nonthrombocytopenic purpura; thrombocytopenic purpura, agranulocytosis; Endocrine: Hyperglycemia, hypoglycemia; Skin: Pruritus, skin irritation, increased pigmentation, sweating; Musculoskeletal: Arthralgia; Nervous System/Psychiatric: Vertigo, local weakness, diminished concentration, reversible mental depression progressing to catatonia, an acute reversible syndrome characterized by disorientation for time and place, emotional lability, slightly clouded sensorium, and decreased performance on neuropsychometrics; Respiratory: Rales, bronchial obstruction; Urogenital: Urination difficulties.
TIMOPTIC Ophthalmic Solution is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.
In a study of plasma drug concentration in six subjects, the systemic exposure to timolol was determined following twice daily administration of TIMOPTIC 0.5%. The mean peak plasma concentration following morning dosing was 0.46 ng/mL and following afternoon dosing was 0.35 ng/mL.
Teratogenicity studies with timolol in mice, rats, and rabbits at oral doses up to 50 mg/kg/day (7,000 times the systemic exposure following the maximum recommended human ophthalmic dose) demonstrated no evidence of fetal malformations. Although delayed fetal ossification was observed at this dose in rats, there were no adverse effects on postnatal development of offspring. Doses of 1000 mg/kg/day (142,000 times the systemic exposure following the maximum recommended human ophthalmic dose) were maternotoxic in mice and resulted in an increased number of fetal resorptions. Increased fetal resorptions were also seen in rabbits at doses of 14,000 times the systemic exposure following the maximum recommended human ophthalmic dose, in this case without apparent maternotoxicity.
There are no adequate and well-controlled studies in pregnant women. TIMOPTIC should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
As with many topically applied ophthalmic drugs, this drug is absorbed systemically.
The same adverse reactions found with systemic administration of beta-adrenergic blocking agents may occur with topical administration. For example, severe respiratory reactions and cardiac reactions, including death due to bronchospasm in patients with asthma, and rarely death in association with cardiac failure, have been reported following systemic or ophthalmic administration of timolol maleate.
Cardiac FailureSympathetic stimulation may be essential for support of the circulation in individuals with diminished myocardial contractility, and its inhibition of beta-adrenergic receptor blockade may precipitate more severe failure.
In Patients Without a History of Cardiac Failure continued depression of the myocardium with beta-blocking agents over a period of time can, in some cases, lead to cardiac failure. At the first sign or symptom of cardiac failure, TIMOPTIC should be discontinued.
Obstructive Pulmonary DiseasePatients with chronic obstructive pulmonary disease (e.g., chronic bronchitis, emphysema) of mild or moderate severity, bronchospastic disease, or a history of bronchospastic disease (other than bronchial asthma or a history of bronchial asthma, in which TIMOPTIC is contraindicated ) should, in general, not receive beta-blockers, including TIMOPTIC.
Major SurgeryThe necessity or desirability of withdrawal of beta-adrenergic blocking agents prior to major surgery is controversial. Beta-adrenergic receptor blockade impairs the ability of the heart to respond to betaadrenergically mediated reflex stimuli. This may augment the risk of general anesthesia in surgical procedures. Some patients receiving beta-adrenergic receptor blocking agents have experienced protracted severe hypotension during anesthesia. Difficulty in restarting and maintaining the heartbeat has also been reported. For these reasons, in patients undergoing elective surgery, some authorities recommend gradual withdrawal of beta-adrenergic receptor blocking agents.
If necessary during surgery, the effects of beta-adrenergic blocking agents may be reversed by sufficient doses of adrenergic agonists.
Diabetes MellitusBeta-adrenergic blocking agents should be administered with caution in patients subject to spontaneous hypoglycemia or to diabetic patients (especially those with labile diabetes) who are receiving insulin or oral hypoglycemic agents. Beta-adrenergic receptor blocking agents may mask the signs and symptoms of acute hypoglycemia.
ThyrotoxicosisBeta-adrenergic blocking agents may mask certain clinical signs (e.g., tachycardia) of hyperthyroidism. Patients suspected of developing thyrotoxicosis should be managed carefully to avoid abrupt withdrawal of beta-adrenergic blocking agents that might precipitate a thyroid storm.
PRECAUTIONS GeneralBecause of potential effects of beta-adrenergic blocking agents on blood pressure and pulse, these agents should be used with caution in patients with cerebrovascular insufficiency. If signs or symptoms suggesting reduced cerebral blood flow develop following initiation of therapy with TIMOPTIC, alternative therapy should be considered.
There have been reports of bacterial keratitis associated with the use of multiple-dose containers of topical ophthalmic products. These containers had been inadvertently contaminated by patients who, in most cases, had a concurrent corneal disease or a disruption of the ocular epithelial surface.
Choroidal detachment after filtration procedures has been reported with the administration of aqueous suppressant therapy (e.g., timolol).
Angle-closure GlaucomaIn patients with angle-closure glaucoma, the immediate objective of treatment is to reopen the angle. This requires constricting the pupil. Timolol maleate has little or no effect on the pupil. TIMOPTIC should not be used alone in the treatment of angle-closure glaucoma.
AnaphylaxisWhile taking beta-blockers, patients with a history of atopy or a history of severe anaphylactic reactions to a variety of allergens may be more reactive to repeated accidental, diagnostic, or therapeutic challenge with such allergens. Such patients may be unresponsive to the usual doses of epinephrine used to treat anaphylactic reactions.
Muscle WeaknessBeta-adrenergic blockade has been reported to potentiate muscle weakness consistent with certain myasthenic symptoms (e.g., diplopia, ptosis, and generalized weakness). Timolol has been reported rarely to increase muscle weakness in some patients with myasthenia gravis or myasthenic symptoms.
Carcinogenesis, Mutagenesis, Impairment Of FertilityIn a two-year study of timolol maleate administered orally to rats, there was a statistically significant increase in the incidence of adrenal pheochromocytomas in male rats administered 300 mg/kg/day (approximately 42,000 times the systemic exposure following the maximum recommended human ophthalmic dose). Similar differences were not observed in rats administered oral doses equivalent to approximately 14,000 times the maximum recommended human ophthalmic dose.
In a lifetime oral study in mice, there were statistically significant increases in the incidence of benign and malignant pulmonary tumors, benign uterine polyps and mammary adenocarcinomas in female mice at 500 mg/kg/day, (approximately 71,000 times the systemic exposure following the maximum recommended human ophthalmic dose), but not at 5 or 50 mg/kg/day (approximately 700 or 7,000, respectively, times the systemic exposure following the maximum recommended human ophthalmic dose). In a subsequent study in female mice, in which post-mortem examinations were limited to the uterus and the lungs, a statistically significant increase in the incidence of pulmonary tumors was again observed at 500 mg/kg/day.
The increased occurrence of mammary adenocarcinomas was associated with elevations in serum prolactin which occurred in female mice administered oral timolol at 500 mg/kg/day, but not at doses of 5 or 50 mg/kg/day. An increased incidence of mammary adenocarcinomas in rodents has been associated with administration of several other therapeutic agents that elevate serum prolactin, but no correlation between serum prolactin levels and mammary tumors has been established in humans. Furthermore, in adult human female subjects who received oral dosages of up to 60 mg of timolol maleate (the maximum recommended human oral dosage), there were no clinically meaningful changes in serum prolactin.
Timolol maleate was devoid of mutagenic potential when tested in vivo (mouse) in the micronucleus test and cytogenetic assay (doses up to 800 mg/kg) and in vitro in a neoplastic cell transformation assay (up to 100 mcg/mL). In Ames tests the highest concentrations of timolol employed, 5,000 or 10,000 mcg/plate, were associated with statistically significant elevations of revertants observed with tester strain TA100 (in seven replicate assays), but not in the remaining three strains. In the assays with tester strain TA100, no consistent dose response relationship was observed, and the ratio of test to control revertants did not reach 2. A ratio of 2 is usually considered the criterion for a positive Ames test.
Reproduction and fertility studies in rats demonstrated no adverse effect on male or female fertility at doses up to 21,000 times the systemic exposure following the maximum recommended human ophthalmic dose.
Pregnancy Teratogenic EffectsTeratogenicity studies with timolol in mice, rats, and rabbits at oral doses up to 50 mg/kg/day (7,000 times the systemic exposure following the maximum recommended human ophthalmic dose) demonstrated no evidence of fetal malformations. Although delayed fetal ossification was observed at this dose in rats, there were no adverse effects on postnatal development of offspring. Doses of 1000 mg/kg/day (142,000 times the systemic exposure following the maximum recommended human ophthalmic dose) were maternotoxic in mice and resulted in an increased number of fetal resorptions. Increased fetal resorptions were also seen in rabbits at doses of 14,000 times the systemic exposure following the maximum recommended human ophthalmic dose, in this case without apparent maternotoxicity.
There are no adequate and well-controlled studies in pregnant women. TIMOPTIC should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Nursing MothersTimolol maleate has been detected in human milk following oral and ophthalmic drug administration. Because of the potential for serious adverse reactions from TIMOPTIC in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric UseSafety and effectiveness of timolol maleate ophthalmic solution have been established when administered in pediatric patients aged 2 years and older. Use of timolol maleate ophthalmic solution in these children is supported by evidence from adequate and well controlled studies in children and adults. Safety and efficacy in pediatric patients below the age of 2 years have not been established.
Geriatric UseNo overall differences in safety or effectiveness have been observed between elderly and younger patients.
TIMOPTIC Ophthalmic Solution is available in concentrations of 0.25 and 0.5%. The usual starting dose is one drop of 0.25% TIMOPTIC in the affected eye(s) twice a day. If the clinical response is not adequate, the dosage may be changed to one drop of 0.5% solution in the affected eye(s) twice a day.
Since in some patients the pressure-lowering response to TIMOPTIC may require a few weeks tostabilize, evaluation should include a determination of intraocular pressure after approximately 4 weeks oftreatment with TIMOPTIC.
If the intraocular pressure is maintained at satisfactory levels, the dosage schedule may be changed to one drop once a day in the affected eye(s). Because of diurnal variations in intraocular pressure, satisfactory response to the once-a-day dose is best determined by measuring the intraocular pressure at different times during the day.
Dosages above one drop of 0.5% TIMOPTIC twice a day generally have not been shown to produce further reduction in intraocular pressure. If the patient's intraocular pressure is still not at a satisfactory level on this regimen, concomitant therapy with other agent(s) for lowering intraocular pressure can be instituted. The concomitant use of two topical beta-adrenergic blocking agents is not recommended.
The most frequently reported adverse experiences have been burning and stinging upon instillation (approximately one in eight patients).
The following additional adverse experiences have been reported less frequently with ocular administration of this or other timolol maleate formulations:
Body As A WholeHeadache, asthenia/fatigue, and chest pain.
CardiovascularBradycardia, arrhythmia, hypotension, hypertension, syncope, heart block, cerebral vascular accident, cerebral ischemia, cardiac failure, worsening of angina pectoris, palpitation, cardiac arrest, pulmonary edema, edema, claudication, Raynaud's phenomenon, and cold hands and feet.
DigestiveNausea, diarrhea, dyspepsia, anorexia, and dry mouth.
ImmunologicSystemic lupus erythematosus.
Nervous System/PsychiatricDizziness, increase in signs and symptoms of myasthenia gravis, paresthesia, somnolence, insomnia, nightmares, behavioral changes and psychic disturbances including depression, confusion, hallucinations, anxiety, disorientation, nervousness, and memory loss.
SkinAlopecia and psoriasiform rash or exacerbation of psoriasis.
HypersensitivitySigns and symptoms of systemic allergic reactions, including anaphylaxis, angioedema, urticaria, and localized and generalized rash.
RespiratoryBronchospasm (predominantly in patients with preexisting bronchospastic disease), respiratory failure, dyspnea, nasal congestion, cough and upper respiratory infections.
EndocrineMasked symptoms of hypoglycemia in diabetic patients.
Special SensesSigns and symptoms of ocular irritation including conjunctivitis, blepharitis, keratitis, ocular pain, discharge (e.g., crusting), foreign body sensation, itching and tearing, and dry eyes; ptosis; decreased corneal sensitivity; cystoid macular edema; visual disturbances including refractive changes and diplopia; pseudopemphigoid; choroidal detachment following filtration surgery ; and tinnitus.
UrogenitalRetroperitoneal fibrosis, decreased libido, impotence, and Peyronie's disease.
The following additional adverse effects have been reported in clinical experience with ORAL timolol maleate or other ORAL beta-blocking agents and may be considered potential effects of ophthalmic timolol maleate: Allergic: Erythematous rash, fever combined with aching and sore throat, laryngospasm with respiratory distress; Body as a Whole: Extremity pain, decreased exercise tolerance, weight loss; Cardiovascular: Worsening of arterial insufficiency, vasodilatation; Digestive: Gastrointestinal pain, hepatomegaly, vomiting, mesenteric arterial thrombosis, ischemic colitis; Hematologic: Nonthrombocytopenic purpura; thrombocytopenic purpura, agranulocytosis; Endocrine: Hyperglycemia, hypoglycemia; Skin: Pruritus, skin irritation, increased pigmentation, sweating; Musculoskeletal: Arthralgia; Nervous System/Psychiatric: Vertigo, local weakness, diminished concentration, reversible mental depression progressing to catatonia, an acute reversible syndrome characterized by disorientation for time and place, emotional lability, slightly clouded sensorium, and decreased performance on neuropsychometrics; Respiratory: Rales, bronchial obstruction; Urogenital: Urination difficulties.
DRUG INTERACTIONSAlthough TIMOPTIC used alone has little or no effect on pupil size, mydriasis resulting from concomitant therapy with TIMOPTIC and epinephrine has been reported occasionally.
Beta-Adrenergic Blocking AgentsPatients who are receiving a beta-adrenergic blocking agent orally and TIMOPTIC should be observed for potential additive effects of beta-blockade, both systemic and on intraocular pressure. The concomitant use of two topical beta-adrenergic blocking agents is not recommended.
Calcium AntagonistsCaution should be used in the coadministration of beta-adrenergic blocking agents, such as TIMOPTIC, and oral or intravenous calcium antagonists because of possible atrioventricular conduction disturbances, left ventricular failure, and hypotension. In patients with impaired cardiac function, coadministration should be avoided.
Catecholamine-Depleting DrugsClose observation of the patient is recommended when a beta blocker is administered to patients receiving catecholamine-depleting drugs such as reserpine, because of possible additive effects and the production of hypotension and/or marked bradycardia, which may result in vertigo, syncope, or postural hypotension.
Digitalis And Calcium AntagonistsThe concomitant use of beta-adrenergic blocking agents with digitalis and calcium antagonists may have additive effects in prolonging atrioventricular conduction time.
CYP2D6 InhibitorsPotentiated systemic beta-blockade (e.g., decreased heart rate, depression) has been reported during combined treatment with CYP2D6 inhibitors (e.g., quinidine, SSRIs) and timolol.
ClonidineOral 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 hypertension with ophthalmic timolol maleate.
Injectable Epinephrine.
Timoptic is prescribed in the management of glaucoma and ocular hypertension — conditions related to elevated pressure inside the eye that, left unmanaged, can affect the optic nerve over time. As an ophthalmological beta-adrenolytic preparation, it falls within a category of eye medications used for long-term pressure control. The structured indication block further down this page details the registered uses recognised in the markets where Timoptic is sold.
The active ingredient in Timoptic is timolol, classified as a beta-adrenolytic agent used in ophthalmology and within the antiglaucomatous category. Timolol is one of the most established molecules in this therapeutic area and circulates internationally under a number of brand names — the same active ingredient is found in many ophthalmic preparations sold worldwide, even where the Timoptic brand itself is not registered.
Timoptic carries marketing authorisation in eight countries, with a geographically scattered footprint that includes Canada, Switzerland, Russia, Peru, the United States, Romania, Bulgaria, and Lithuania. The brand is not consistently available across every continent, but timolol-containing eye preparations exist far more widely. If your country is not on this list, a local pharmacist can confirm which timolol product is registered in that market.
Timolol is available under several brand names internationally, particularly in markets where generic ophthalmic preparations are well established. Other medications within the broader antiglaucomatous category also exist, working through different mechanisms, although they are not interchangeable without medical guidance. To identify a regional equivalent, search the active ingredient timolol on Pill2Trip or ask an ophthalmologist or pharmacist in your country.
Yes. Timoptic is a prescription ophthalmic medication, and glaucoma therapy in particular is calibrated to a patient's intraocular pressure readings, optic-nerve status, and broader medical picture. This matters especially for travellers and people relocating between countries, since prescription rules, available brands, and even the specific timolol formulations on the local market can differ. Any decision to start, stop, or substitute should sit with a healthcare provider.
