Each 1 mL contains Timolol maleate 6.830 mg Equivalent to Timolol 5 mg.
Excipients/Inactive Ingredients: Preservative: Benzalkonium chloride 0.01%.
Pharmacology: Pharmacodynamics: Timolol maleate is a non-selective beta(1) and beta(2) adrenergic receptor blocking agent. Its effectivity in ocular hypertension is related to an increased outflow and decreased formation of the aqueous humor which results in a decreased intraocular pressure. It also exhibits an insignificant direct myocardial depressant activity, intrinsic sympathomimetic action and local anesthetic activity.
Pharmacokinetics: The degree of systemic absorption of timolol after topical application to the eye has not been fully elucidated; however, some absorption can apparently occur, since adverse systemic effects have occurred following ophthalmic instillation of the drug. Following topical administration of timolol 0.5% solution twice daily to the eye in a limited number of individuals, mean peak plasma concentrations were 0.46 or 0.35 ng/mL following the morning or afternoon dose, respectively. Following topical application to the eye of a 0.5% solution of the drug, reduction in IOP usually occurs within 15-30 minutes, reaches a maximum within 1-5 hours, and persists about 24 hours.
Treatment of elevated intraocular pressure (IOP) in patients with ocular hypertension or open-angle glaucoma.
Recommended Dose: 1 drop of a 0.5% solution in the affected eye(s) twice daily. The dose may then be reduced to 1 drop in the affected eye(s) once daily if satisfactory IOP is maintained.
If further reduction of IOP is required in patients receiving 1 drop of a timolol 0.5% solution twice daily, pilocarpine or other miotics, latanoprost, and/or topical or systemically administered carbonic anhydrase inhibitors (e.g., acetazolamide) may be added to the timolol regimen.
Mode of Administration: Ophthalmic route.
No specific data are available. Overdosage is unlikely to occur as one 5 ml bottle of Timolol Eye Drops 0.5% contains 25 mg of Timolol maleate compared with the usual adult oral dose of 20-60 mg per day. However, in the rare event that overdosage occurs the most common signs and symptoms to be expected following overdosage with a beta-adrenergic receptor blocking agent are symptomatic bradycardia, hypotension, bronchospasm, and acute cardiac failure. If overdosage occurs, the following measures should be considered: Gastric lavage, if ingested. Studies have shown that timolol cannot be easily removed by hemodialysis.
Symptomatic bradycardia: Atropine sulphate, 0.25 to 2mg intravenously, should be used to induce vagal blockade. If bradycardia persists, intravenous isoprenaline hydrochloride should be administered cautiously. In refractory cases, the use of a cardiac pacemaker may be considered.
Hypotension: A sympathomimetic pressor agent such as dopamine, dobutamine or noradrenaline should be used. In refractory cases, the use of glucagon has been reported to be useful.
Bronchopasm: Isoprenaline hydrochloride should be used. Additional therapy with aminophylline may be considered.
Acute cardiac failure: conventional therapy with digitalis, diuretics and oxygen should be instituted immediately. In refractory cases, the use of intravenous aminophylline is suggested. This may be followed, if necessary, by glucagon which has been reported to be useful.
Heart block (second or third degree): Isoprenaline hydrochloride or a pacemaker should be used.
Timolol ophthalmic solution is contraindicated in patients with bronchial asthma or a history of bronchial asthma and in patients with severe chronic obstructive pulmonary disease, sinus bradycardia, atrioventricular block greater than first degree, overt cardiac failure, or cardiogenic shock. Timolol ophthalmic solution also is contraindicated in patients with known hypersensitivity to the drug or any ingredient in the formulation.
Atopy history or a history of severe anaphylaxis (may be unresponsive to the usual doses of epinephrine).
Anesthesia during major surgery; protracted severe hypotension and difficulty maintaining heart rate has been reported; consider dose reduction prior to surgery.
Cardiac failure; increased risk of exacerbation or precipitation; discontinue at the first sign or symptom.
Cerebrovascular insufficiency; increased risk of reduced cerebral blood flow; consider discontinuation.
Choroidal detachment after filtration procedures has been reported with the administration of aqueous suppressant therapy.
COPD, mild or moderate.
Concomitant use with a second topical beta-blocker is not recommended.
Concomitant use with calcium antagonists in patients with impaired cardiac function; avoid use.
Diabetes mellitus or patients subject to spontaneous hypoglycemia; may mask symptoms of acute hypoglycemia.
Glaucoma, angle-closure; do not use as monotherapy.
Hyperthyroidism; may mask clinical signs, such as tachycardia.
Thyrotoxicosis, suspected; discontinuation may precipitate thyroid storm; avoid abrupt withdrawal.
Myasthenic conditions; risk of increasing muscle weakness.
Systemic absorption may occur.
Pregnancy: There are no adequate and controlled studies to date using timolol ophthalmic solution in pregnant women, and the drug should be used during pregnancy only when the potential benefits justify the possible risks to the fetus.
Lactation: Timolol is distributed into milk following oral or ophthalmic administration. Because of the potential for serious adverse reactions from timolol in nursing infants, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.
Common: Cardiovascular: Angina pectoris, Hypotension.
Dermatologic: Pruritus, Rash, Urticaria.
Gastrointestinal: Abdominal pain, Diarrhea, Indigestion, Nausea, Vomiting.
Musculoskeletal: Cramp.
Neurologic: Confusion (13%), Headache (1% to 5%).
Ophthalmic: Blurred vision (15% to 33%), Burning sensation in eye (12.5% to 20%), Dry eyes.
Psychiatric: Depression (9.2%, ophthalmic), Hallucinations (11%), Psychotic disorder (3%).
Respiratory: Cough.
Other: Infectious disease.
Serious: Cardiovascular: Cardiac dysrhythmia (1%), Myocardial infarction (rare).
Ocular Hypotensive Agents: When used in conjunction with topical miotics, latanoprost, and/or topical or systemically administered carbonic anhydrase inhibitors, the effect of timolol in lowering IOP may be additive. This effect may be used to therapeutic advantage in the treatment of glaucoma. While therapy with timolol in fixed combination with dorzolamide twice daily is associated with greater decreases in IOP than monotherapy with timolol 0.5% twice daily or dorzolamide 2% three times daily, therapy with timolol 0.5% twice daily in combination with dorzolamide 2% three times daily is associated with a slightly greater decrease in IOP (1 mmHg) than the twice-daily regimen of timolol in fixed combination with dorzolamide.
Systemic β-Adrenergic Blocking Agents: The possibility of an additive effect on IOP and/or systemic β-adrenergic blockade should be considered in patients who are receiving a systemic β-adrenergic blocking agent and topical timolol concomitantly.
Catecholamine-depleting Drugs: When topical timolol is administered concomitantly with a catecholamine-depleting drug (e.g., reserpine), the patient should be observed closely for possible additive effects and the production of hypotension and/or marked bradycardia, which may result in vertigo, syncope, and/or postural hypotension.
Other Cardiovascular Drugs: Concomitant administration of β-adrenergic blocking agent and a calcium-channel blocking agent and a cardiac glycoside may have additive effects on prolonging AV conduction. Because AV conduction disturbances, left ventricular failure, and/or hypotension may occur, caution should be exercised if timolol and a calcium-channel blocking agent are used concomitantly, and such concomitant use should be avoided in patients with impaired cardiac function. Severe bradycardia (e.g., 36 bpm), which was associated with a wandering pacemaker in one patient, and transient asystole have been reported when ophthalmic timolol and oral verapamil were used concomitantly. A single IV dose of atropine was effective in managing serious bradycardia in at least one patient. Verapamil should be used with extreme caution in patients receiving ophthalmic timolol; when therapy with a calcium-channel blocking agent is indicated (e.g., for angina) in such patients, an agent with minimal effects on SA node and cardiac conduction (e.g., nifedipine) should be used if possible.
Sinus bradycardia, which recurred upon rechallenge, has been reported when ophthalmic timolol and oral quinidine were used concomitantly. This interaction has been attributed to inhibition of timolol metabolism (via the cytochrome P-450 [CYP] 2D6 isoenzyme) by quinidine. Although oral β-adrenergic blocking agents may exacerbate rebound hypertension that may occur following discontinuance of clonidine, such an effect has not been reported in patients receiving ophthalmic timolol.
Store below 30°C, protect from light. Discard 30 days after first opening.
S01ED01 - timolol ; Belongs to the class of beta blocking agents. Used in the treatment of glaucoma.
T-Oph ophth soln 5 mg/mL
((5 mL, eye drops)) 1's
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