Celsus Timolol Maleate

Celsus Timolol Maleate



Ashford Pharma


Full Prescribing Info
Timolol maleate.
Timolol maleate is a formulation that reduces elevated and normal intraocular pressure whether or not associated with glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual loss. With higher intraocular pressure, there is greater likelihood of glaucoma visual field loss and optic nerve damage.
Each mL of solution contains: Timolol (as Maleate) 5 mg.
Excipients/Inactive Ingredients: Preservatives: Benzalkonium Chloride.
Timolol maleate is a nonselective beta-adrenergic receptor blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity.
Timolol maleate's onset of action is usually rapid, occurring approximately within 20 minutes after topical application to the eye. The precise mechanism of action of timolol maleate in lowering intraocular pressure is not clearly established. A fluorescein study and tonography studies indicate that the predominant action may be related to reduce aqueous formation. However, in some studies a slight increase in outflow facility was also observed.
Clinical studies show timolol maleate was generally effective in more patients and produced fewer and less severe side effects than either pilocarpine or epinephrine.
Timolol maleate reduces intraocular pressure with practically no miotic effect. There is little or no effect on accommodation or pupil size. Visual acuity changes due to increased accommodation are uncommon, and the dim or blurred vision and night blindness produced by miotics are not evident. The inability to see around lenticular opacities in patients with cataracts when pupils is constricted by miotics is avoided. Refraction may be necessary when changing patients from miotics to timolol maleate, after the effects of the miotic have passed.
Diminished responsiveness to timolol maleate after the prolonged therapy has been reported in some patients, as with other anti-glaucoma drugs. However, in clinical studies of timolol maleate in which 164 patients were followed for at least 3 years, no significant difference in mean intraocular pressure was observed after the initial stabilization. This indicates that the intraocular pressure-lowering effect of timolol maleate is well maintained.
For the reduction of elevated intraocular pressure Timolol maleate is indicated in patients with: Ocular hypertension; chronic open-angle glaucoma; aphakia and glaucoma; secondary glaucoma (some cases); narrow angles and a history of spontaneous or iatrogenically induced narrow-angle closure in the opposite eye in whom reduction of intraocular pressure is necessary (see Warnings).
Dosage/Direction for Use
Initially 1 drop of 0.25% solution in the affected eye(s) twice a day; maximum 1 drop of 0.5% solution twice a day. If intraocular pressure is maintained at satisfactory levels, patient can be placed on once a day therapy. To transfer to another beta-blocking ophthalmic solution discontinue at the end of a full-day treatment & begin treatment next day. To transfer from single anti-glaucoma agent to other ophthalmic beta-blocker, continue agent already being used and add therapy at an initial of timolol maleate. On the next day discontinue the previously used anti-glaucoma agent.
In patients with: Bronchial asthma or with history of bronchial asthma or 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 with Timolol maleate is contraindicated.
As with other topically applied ophthalmic drugs, this drug may be absorbed systemically.
The same adverse reactions found with systemic administration of beta-adrenergic blocking agents may occur with topical administration.
Cardiac disease should be adequately controlled before beginning therapy with timolol maleate. In patients with history of severe cardiac problems, signs of cardiac failure should be sought and pulse rates should be monitored.
Potential complications of therapy with timolol maleate include: Respiratory complications, including death due to bronchospasm in patients with asthma, and cardiac complications, including cardiac failure, have been reported following administration of beta-adrenergic blocking agents. However, reports of deaths have been rare.
Patients already receiving a beta-adrenergic blocking agent systemically and who are given timolol maleate should be observed for a potential additive effect either on the intraocular pressure or on the known systemic effects of beta blockade. Concomitant use of two topical beta-adrenergic blocking agents is not recommended.
For angle-closure glaucoma patients, the immediate objective of treatment is to reopen the angle. Constricting the pupil with a miotic is necessary. Timolol maleate has little or no effect on the pupil. In angle-closure glaucoma, Timolol maleate should be used with a miotic.
There have been reports of Choroidal detachment with administration of aqueous suppressant therapy (e.g. timolol, acetazolamide) after filtration procedures.
Timolol maleate has not been studied in patients wearing contact lenses.
Special Precautions
Reports of accidental overdosage with timolol maleate show systemic effects similar to those seen with systemic beta-adrenergic blocking agents such as dizziness, headache, shortness of breath, bradycardia, bronchospasm, and cardiac arrest.
Danger from Anaphylactic Reaction: Patients with a history atopy or a history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated challenge with such allergens, either accidental, diagnostic, or therapeutic. Such patients may be unresponsive to the usual doses of epinephrine used to treat anaphylactic reactions.
Adverse Reactions
Usually Timolol maleate is well tolerated. Transient blurred vision (6.0%), lasting from 30 seconds to 5 minutes, following instillation was the most frequent drug-related complaint in clinical studies.
Other probable or possible drug related adverse reactions occurred with frequency of at least 1% in parallel active treatment controlled clinical trials include: Ocular: Burning and stinging, discharge, foreign body sensation, itching of the eye.
Other reported adverse reactions with ocular administration of this or other timolol maleate formulations, either in clinical trials or since the drug has been marketed include: Special Senses: Ocular irritation, including conjunctivitis, blepharitis, keratitis, decreased corneal sensitivity, and dry eyes. Visual disturbances, including refractive changes (due to withdrawal of miotic therapy in some cases), diplopia, ptosis, choroidal detachment following filtration surgery (see Warnings), tinnitus.
Cardiovascular: Bradycardia, arrhythmia, hypotension, syncope, heart block, cardiovascular accident, cerebral ischemia, congestive heart failure, palpitation, cardiac arrest, edema, claudication, Raynaud's phenomenon, cold hands and feet.
Respiratory: Bronchospasm (predominantly in patients with pre-existing bronchospastic disease), respiratory failure, dyspnea, cough.
Body as a Whole: Headache, asthenia, fatigue, chest pain.
Integumentary: Alopecia, psoriasiform rash or exacerbation of psoriasis.
Hypersensitivity: Signs and symptoms of allergic reactions including angioedema, urticaria, localized and generalized rash.
Nervous System/Psychiatric: Dizziness, depression, insomnia, nightmares, memory loss, paresthesia.
Neuromuscular: Increase in signs and symptoms of myasthenia gravis.
Digestive: Nausea, diarrhea, dyspepsia, dry mouth.
Urogenital: Decreased libido, Peyronie's disease.
Immunologic: Systemic lupus erythematosus.
Keep tightly closed after use. Store below 25°C.
ATC Classification
S01ED01 - timolol ; Belongs to the class of beta blocking agents. Used in the treatment of glaucoma.
Eye drops (sterile) 0.5% x 5 mL.
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