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PACIFIC/GREENST
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60758080210

timolol 0.25% eye drops

Generic
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Uses

Ocular Hypertension and Glaucoma

In ophthalmology, topical timolol is used to reduce elevated IOP in patients with open-angle glaucoma or ocular hypertension. Dorzolamide hydrochloride and timolol maleate in a fixed-combination ophthalmic solution is used topically to reduce elevated IOP in patients with open-angle glaucoma or ocular hypertension who have not responded adequately (i.e., failed to achieve target IOP as determined after multiple measurements over time) to a topical β-adrenergic blocking agent. Topical timolol also has been used to reduce elevated IOP in patients with aphakic glaucoma and some secondary glaucomas. Elevated IOP presents a major risk factor in glaucomatous visual field loss; the higher the level of IOP, the greater the likelihood of optic nerve damage and glaucomatous visual field loss. Current data from a limited number of controlled studies suggest similar clinical efficacy for ophthalmic timolol maleate and ophthalmic timolol as the hemihydrate.

Timolol may be used alone or in conjunction with a topical miotic (e.g., pilocarpine), latanoprost and/or a topical or systemic carbonic anhydrase inhibitor. When used in conjunction with these agents, timolol may have an additive IOP-lowering effect. 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 mm Hg) than the twice-daily regimen of timolol in fixed combination with dorzolamide. If timolol is used to reduce IOP in patients with angle-closure glaucoma, the drug should not be used alone but rather in combination with a topical miotic since timolol has little or no effect on pupil size.

Like levobunolol, timolol reduces elevated IOP in patients with chronic open-angle glaucoma without producing the miosis and/or ciliary spasm that are associated with miotic agents. In double-blind studies in patients with open-angle glaucoma, usual doses of timolol have been found to be at least as effective as therapeutic doses of pilocarpine in reducing elevated IOP without the miosis, ocular irritation, and blurred vision associated with pilocarpine therapy. Timolol maleate also has been found in multiclinic studies to be at least as effective as epinephrine in reducing IOP in patients with open-angle glaucoma. Like other ophthalmic nonselective β-blocking agents (e.g., levobunolol), ophthalmic timolol has been associated with adverse systemic pulmonary and cardiovascular effects. The drug should be used with caution in patients with diminished pulmonary function, and is contraindicated in patients with asthma or a history of asthma and in patients with severe chronic obstructive pulmonary disease. Following prolonged therapy with topical timolol, the effect in reducing IOP is generally well maintained, but tolerance has been reported in some patients. In one long-term study in patients receiving timolol for at least 3 years, the reduction in mean IOP was maintained following initial stabilization with the drug.

For systemic uses of timolol maleate, see 24:24.

Dosage and Administration

Administration

Timolol is applied topically to the eye as an ophthalmic solution. Care should be taken to avoid contamination of the solution container. (See Cautions: Precautions and Contraindications.)

The fixed-combination ophthalmic solution of dorzolamide hydrochloride and timolol maleate should not be administered while wearing soft contact lenses. Contact lenses may be reinserted 15 minutes after a dose of the fixed-combination ophthalmic solution.

If the patient is receiving more than one ophthalmic drug, the drugs should be administered at least 10 minutes apart. Containers of timolol maleate ophthalmic gel-forming solution should be inverted and shaken once just prior to administration of each dose. Patients receiving ophthalmic gel-forming solutions of the drug who also are receiving other ophthalmic preparations should be instructed that other topical preparations be administered at least 10 minutes before a dose of the gel-forming solution.

Dosage

Ocular Hypertension and Glaucoma

Dosage of timolol maleate or timolol (as the hemihydrate) is expressed in terms of timolol.

When used alone or when added to existing glaucoma therapy, the usual initial dosage of timolol is 1 drop of a 0.25% solution in the affected eye(s) twice daily. If necessary for adequate reduction of IOP, dosage may be increased to 1 drop of a 0.5% solution in the affected eye(s) twice daily. The dose may then be reduced to 1 drop of the effective strength in the affected eye(s) once daily if satisfactory IOP is maintained. When timolol maleate ophthalmic gel-forming solution is used, the usual dosage of timolol is 1 drop of a 0.25 or 0.5% solution in the affected eye(s) once daily. Because of diurnal variations in IOP, IOP should be measured at different times during the day to determine if an adequate effect is maintained in patients receiving single daily dose therapy. Since IOP may not stabilize for a few weeks after initiating timolol therapy in some patients, IOP should also be determined after about 4 weeks of therapy with the drug. Dosages exceeding 1 drop of a 0.5% solution twice daily generally have not produced a further reduction in IOP. Dosages exceeding 1 drop of a 0.5% gel-forming solution once daily or 1 drop of a 0.5% solution containing timolol as the hemihydrate administered twice daily have not been studied.

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. For the treatment of glaucoma or ocular hypertension, the usual dosage of timolol maleate in fixed combination with dorzolamide hydrochloride is 1 drop in the affected eye(s) twice daily. If further reduction in IOP is needed in patients receiving 1 drop of a timolol 0.5% gel-forming solution once daily, concomitant therapy should be considered. When once-daily dosing of timolol gel-forming ophthalmic solution has been substituted for twice-daily dosing of timolol maleate conventional ophthalmic solution, the IOP-lowering effect has remained consistent.

Cautions

Timolol ophthalmic solutions generally are well tolerated following topical application to the eye; however, adverse effects may occasionally be severe enough to require discontinuance of the drug.

Ocular Effects

In clinical studies, blurred vision (lasting 0.5-5 minutes) upon instillation has been reported in about 33% of patients receiving timolol maleate gel-forming ophthalmic solution. Blurred vision requiring discontinuance of the gel-forming solution reportedly occurred in less than 1% of patients. The most common adverse effects of ophthalmic timolol solutions, occurring in about 13% of patients, are burning or stinging upon instillation.

Signs and symptoms of ocular irritation, including conjunctivitis, blepharitis, keratitis, ocular pain, discharge (e.g., crusting), itching and tearing, foreign body sensation, dry eyes, eyelid erythema, and blepharoptosis have been reported occasionally in patients receiving topical timolol therapy. Visual disturbances including refractive changes (resulting from withdrawal of miotic therapy in some patients) have been infrequently associated with timolol therapy. Decreased corneal sensitivity, diplopia, cystoid macular edema, pseudopemphigoid, choroidal detachment following filtration surgery, epiphora, photophobia, blurred vision, conjunctival injection, corneal fluorescein staining, cataract, retinal vascular disorder, and ptosis also have occurred.

Systemic Effects

Cardiovascular Effects

Aggravation or precipitation of certain cardiovascular disorders, presumably related to effects of systemic β-adrenergic blockade, may occur during therapy with topical timolol and may include bradycardia, arrhythmia, congestive heart failure, hypotension, hypertension, syncope, heart block, cerebrovascular accident, cerebral ischemia, cardiac failure, worsening of angina pectoris, cardiac arrest, pulmonary edema, palpitation, chest pain, peripheral edema, edema, claudication, Raynaud's phenomenon, and cold hands and feet. Slight reduction of resting heart rate also may occur, and slightly decreased blood pressure has been reported in some patients receiving high doses of the drug (i.e., 1 drop of a 1% solution to each eye). Rarely, death associated with cardiac failure has been reported in patients receiving systemic or topical (ocular) timolol.

Nervous System Effects

Headache and dizziness occurred in 1-5% of patients receiving timolol maleate gel-forming ophthalmic solution in clinical studies. Other adverse nervous system effects reported with ocular administration of topical timolol therapy include exacerbation of myasthenia gravis (e.g., increased muscle weakness), paresthesia, asthenia and/or fatigue, somnolence, insomnia, nightmares, behavioral changes and psychic disturbances (e.g., depression, confusion, hallucinations, anxiety, disorientation, nervousness, memory loss).

Respiratory Effects

Aggravation or precipitation of certain respiratory disorders, presumably related to effects of systemic β-adrenergic blockade, may occur during therapy with topical timolol and may include dyspnea, nasal congestion, cough, upper respiratory infections, sinusitis, and respiratory failure. Severe respiratory reactions, including death resulting from bronchospasm (mainly in patients with preexisting bronchospastic disease [e.g., asthma]) have been reported in patients receiving topical timolol therapy.

Dermatologic and Sensitivity Reactions

Hypersensitivity reactions, including anaphylaxis, angioedema, urticaria, and localized or generalized rash have occurred rarely during topical timolol therapy. Alopecia, psoriasiform rash, exacerbation of psoriasis, and systemic lupus erythematosus also have been reported.

GI Effects

Diarrhea, nausea, dyspepsia, anorexia, and dry mouth have been reported in patients receiving topical timolol therapy.

Genitourinary Effects

Retroperitoneal fibrosis, impotence, decreased libido, and Peyronie's disease have been reported in some patients receiving topical timolol therapy.

Endocrine Effects

Because β-adrenergic blocking agents may mask the signs and symptoms of acute hypoglycemia, these agents should be administered with caution in patients subject to spontaneous hypoglycemia and in diabetic patients (especially those with labile diabetes) who are receiving insulin or oral hypoglycemic agents. However, masked symptoms of hypoglycemia in insulin-dependent diabetics, have been reported rarely with topical timolol.

Beta-adrenergic blocking agents also may mask certain clinical signs (e.g., tachycardia) of hyperthyroidism. Patients suspected of developing thyrotoxicosis should be managed carefully to avoid abrupt withdrawal of β-adrenergic blocking agents that might precipitate a thyroid storm.

Other Systemic Effects

Common cold and pain in the extremities have been reported in some patients receiving topical timolol therapy. The possibility that other adverse systemic effects associated with systemic timolol or other β-adrenergic blocking agents may occur during topical timolol therapy should be considered.

Precautions and Contraindications

Timolol ophthalmic solution shares the toxic potentials of systemically administered timolol, and the usual precautions of systemic timolol therapy should be observed with the topical preparation. () Severe respiratory and cardiac reactions, including death resulting from bronchospasm in patients with asthma and, rarely, death associated with cardiac failure, have been reported in patients receiving systemic or topical (ocular) timolol. Patients receiving topical timolol and a systemic β-adrenergic blocking agent concomitantly should be observed carefully for potential additive effects on IOP and/or systemic effects of β-adrenergic blockade.

Patients who have a history of atopy or of a severe anaphylactic reaction to a variety of allergens reportedly may be more reactive to repeated accidental, diagnostic, or therapeutic challenges with such allergens while taking β-adrenergic blocking agents and may be unresponsive to usual doses of epinephrine used to treat anaphylactic reactions.

Bacterial keratitis has been reported with the use of multidose containers of topical ophthalmic preparations. These containers had been contaminated inadvertently by patients who, in most cases, had a concurrent corneal disease or disruption of the ocular epithelial surface. Patients should be informed that improper handling of ocular solutions can result in contamination of the solution by common bacteria known to cause ocular infections and should be instructed to avoid allowing the tip of the dispensing container to contact the eye or surrounding structures. Serious damage to the eye and subsequent loss of vision may result from using contaminated ophthalmic solutions. Patients also should be advised to seek their physician's advice immediately regarding the continued use of the present multidose container if an intercurrent ocular condition (e.g., trauma, ocular surgery or infection) occurs. Because benzalkonium chloride may be absorbed by soft contact lenses, patients receiving timolol ophthalmic solutions that contain this preservative should be advised to wait at least 15 minutes after instillation of the ophthalmic solution before they insert their soft contact lenses.

Because timolol has little or no effect on pupil size, the drug should not be used alone in patients with angle-closure glaucoma, but only in combination with a miotic. Timolol ophthalmic solutions usually should not be used concomitantly with another ophthalmic β-adrenergic blocking agent concomitantly; in patients being transferred from another β-blocker to timolol, the other β-blocker should be discontinued before initiating timolol.

Patients with mild or moderately severe chronic obstructive pulmonary disease (e.g., chronic bronchitis, emphysema), bronchospastic disease, or a history of bronchospastic disease (other than bronchial asthma or a history of bronchial asthma in which condition timolol ophthalmic solution is contraindicated) generally should not receive β-adrenergic blocking agents. 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.

Pediatric Precautions

Safety and efficacy of timolol ophthalmic solutions in children have not been established.

Geriatric Precautions

Safety and efficacy of timolol ophthalmic solutions were similar in patients 65 years of age or older compared with younger patients; however, the possibility that some older patients may exhibit increased sensitivity to the preparation cannot be ruled out.

Pregnancy, Fertility, and Lactation

Pregnancy

Reproduction studies in mice, rats, and rabbits using oral timolol dosages up to 50 mg/kg daily (7000 times the systemic exposure following the maximum recommended human ophthalmic dosage) have not revealed evidence of harm to the fetus. Although delayed fetal ossification was observed at this dosage in rats, no adverse effects on postnatal development occurred in this species. Oral timolol dosages of 1 g/kg daily (142,000 times the systemic exposure following the maximum recommended human ophthalmic dosage) were maternotoxic and resulted in an increased number of fetal resorptions in mice. Increased fetal resorptions were also observed in rabbits receiving oral timolol dosages 14,000 times the systemic exposure following the maximum recommended human ophthalmic dosage. 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.

Fertility

Reproduction studies in male and female rats using oral timolol dosages up to 125 times the maximum human oral dosage (based on patient weight of 50 kg) have not revealed evidence of impaired fertility.

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.

Drug Interactions

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 mm Hg) 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.

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. In individuals receiving topical timolol 0.5% as the gel-forming ophthalmic solution once daily in the morning, mean peak plasma concentrations following the dose were 0.28 ng/mL. Following topical application to the eye of a 0.25 or 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.

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