Timoptol

TIMOPTOL (timolol maleate) is a sterile eyedrop.
Each mL of solution contains either 2.5 mg or 5 mg of timolol as the active ingredient.
Benzalkonium chloride is added as preservative.
TIMOPTOL 0.25% or TIMOPTOL 0.5% is available in vials containing 5 mL of solution.
TIMOPTOL is an ophthalmic beta-blocking drug which lowers pressure in the eye.

TIMOPTOL (timolol maleate) 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 field loss. The higher the level of intraocular pressure, the greater the likelihood of glaucomatous visual field loss and optic nerve damage.
Onset of action of TIMOPTOL is usually rapid, occurring approximately 20 minutes after topical application to the eye. Maximum reduction of intraocular pressure occurs in one to two hours. Significant lowering of intraocular pressure has been maintained for as long as 24 hours with 0.25 percent or 0.5 percent Ophthalmic Solution TIMOPTOL. This extended duration of action permits control of intraocular pressure over the usual sleeping hours. Repeated observations over a period of three years indicate that the intraocular pressure-lowering effect of TIMOPTOL is well maintained.
Timolol maleate is a nonselective β-adrenergic receptor blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity.
The precise mechanism of action of TIMOPTOL in lowering intraocular pressure is not clearly established at this time, although a fluorescein study and tonography studies indicate that the predominant action may be related to reduced aqueous formation. However, in some studies a slight increase in outflow facility was also observed.
Unlike miotics, TIMOPTOL reduces intraocular pressure with little or no effect on accommodation or pupil size. Thus, changes in visual acuity due to increased accommodation are uncommon, and dim or blurred vision and night blindness produced by miotics are not evident. In addition, in patients with cataracts the inability to see around lenticular opacities when the pupil is constricted by miotics is avoided. When changing patients from miotics to TIMOPTOL a refraction might be necessary when these effects of the miotic have passed.
In clinical studies TIMOPTOL was generally effective in more patients and produced fewer and less severe side effects than either pilocarpine or epinephrine.
As with the use of other antiglaucoma drugs, diminished responsiveness to TIMOPTOL after prolonged therapy has been reported in some patients. However, in clinical studies in which 164 patients have been followed for at least three years, no significant difference in mean intraocular pressure has been observed after initial stabilization.
TIMOPTOL has also been used in patients with glaucoma wearing conventional hard contact lenses, and has generally been well tolerated. TIMOPTOL has not been studied in patients wearing lenses made with materials other than polymethylmethacrylate.

TIMOPTOL is indicated for the reduction of elevated intraocular pressure. In clinical trials it has been shown to reduce intraocular pressure in: Patients with ocular hypertension.
Patients with chronic open-angle glaucoma.
Aphakic patients with glaucoma.
Some patients with secondary glaucoma.
Patients with 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 Precautions).
TIMOPTOL is also indicated as concomitant therapy in patients with pediatric glaucoma, who are inadequately controlled with other antiglaucoma therapy.

The usual starting dose is one drop of 0.25 percent TIMOPTOL 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 percent solution in the affected eye(s) twice a day.
For a small proportion of patients, one drop of 0.1 percent TIMOPTOL in the affected eye(s) twice a day may be satisfactory. If the clinical response is not adequate with 0.1 percent solution, the dosage should be increased to one drop of 0.25 percent in the affected eye(s) twice a day.
If needed, concomitant therapy with other agent(s) for lowering intraocular pressure may be given with TIMOPTOL. The use of two topical beta-adrenergic blocking agents is not recommended (see Precautions).
Since in some patients the pressure-lowering response to TIMOPTOL may require a few weeks to stabilize, evaluation should include a determination of intraocular pressure after approximately 4 weeks of treatment with TIMOPTOL.
If the intraocular pressure is maintained at satisfactory levels, many patients can be placed on once-a-day therapy.
When using nasolacrimal occlusion or closing the eyelids for 2 minute, the systemic absorption is reduced. This may result in an increase in local activity.
When using nasolacrimal occlusion or closing eyelids for 2 minutes, the systemic absorption is reduced. This may result in an increase local activity.
Transferring Patients from Other Therapy: When a patient is transferred from another topical ophthalmic β-adrenergic blocking agent, that agent should be discontinued after proper dosing on one day and treatment with TIMOPTOL started on the following day with one drop of 0.25% TIMOPTOL in the affected eye twice a day. The dose may be increased to one drop of  0.5 percent TIMOPTOL twice a day if the clinical response is not adequate.
When a patient is transferred from a single antiglaucoma agent, other than a topical ophthalmic beta-adrenergic-blocking agent, continue the agent already being used and add one drop of 0.25 percent TIMOPTOL in each affected eye twice a day. On the following day, discontinue the previously used antiglaucoma agent completely and continue with TIMOPTOL. If a higher dosage of TIMOPTOL is required, substitute one drop of 0.5% solution in each affected eye twice a day.
Use in Children: The usual starting dose is one drop of 0.25 percent TIMOPTOL in the affected eye(s) every 12 hours, in addition to other anti-glaucoma medication. The dosage may be increased to one drop of 0.5 percent solution in the affected eye(s) every 12 hours, if necessary. The use of TIMOPTOL is not recommended in premature infants or neonates.

There have been reports of inadvertent overdosage with TIMOPTOL 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.

TIMOPTOL is contraindicated in patients with: Reactive airway disease, bronchial asthma or with a history of bronchial asthma, or severe chronic obstructive pulmonary disease.
Sinus bradycardia; sino-atrial block; second and third degree atrioventricular block; overt cardiac failure; cardiogenic shock.
Hypersensitivity to any component of TIMOPTOL.

As with other topically applied ophthalmic drugs, TIMOPTOL may be absorbed systemically.
The same adverse reactions found with systemic administration of β-adrenergic blocking agents may occur with topical administration.
CARDIO-RESPIRATORY REACTIONS: Cardiac failure should be adequately controlled before beginning therapy with TIMOPTOL. Patients with a history of cardiovascular disease, including cardiac failure, should be watched for signs of deterioration of these diseases and pulse rates should be checked.
Due to its negative effect on conduction time, beta-blockers should be given with caution to patients with first-degree heart block.
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 administration of TIMOPTOL.
In patients with mild/moderate chronic obstructive pulmonary disease (COPD), TIMOPTOL should be used with caution and only if the potential benefit outweighs the potential risk.
VASCULAR DISORDERS: Patients with severe peripheral circulatory disturbance/disorders (e.g., severe forms of Raynaud's disease or Raynaud's syndrome) should be treated with caution.
MASKING OF HYPOGLYCEMIC SYMPTOMS IN PATIENTS WITH DIABETES MELLITUS: Beta-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 blocking agents may mask the signs and symptoms of acute hypoglycemia.
MASKING OF THYROTOXICOSIS: Beta-adrenergic blocking agents may mask certain clinical signs of hyperthyroidism (e,g., tachycardia). Patients suspected of developing thyrotoxicosis should be managed carefully to avoid abrupt withdrawal of beta-adrenergic blocking agents which might precipitate a thyroid storm.
SURGICAL ANESTHESIA: The necessity or desirability of withdrawal of beta-adrenergic blocking agents prior to major surgery is controversial. If necessary during surgery, the effects of beta-adrenergic blocking agents may be reversed by sufficient doses of adrenergic agonists.
OTHER: Patients who are already receiving a β-adrenergic blocking agent systemically and who are given TIMOPTOL should be observed for a potential additive effect either on the intraocular pressure or on the known systemic effects of β-blockade. The use of two topical β-adrenergic blocking agents is not recommended.
In patients with angle-closure glaucoma, the immediate objective of treatment is to reopen the angle. This requires constricting the pupil with a miotic. TIMOPTOL has little or no effect on the pupil. When TIMOPTOL is used to reduce elevated intraocular pressure in angle-closure glaucoma, it should be used with a miotic and not alone.
Choroidal detachment has been reported with administration of aqueous suppressant therapy (e.g., timolol, acetazolamide) after filtration procedures.
TIMOPTOL contains the preservative benzalkonium chloride, which may be absorbed by soft contact lenses. Therefore, TIMOPTOL should not be administered while wearing soft contact lenses. The contact lenses should be removed before application of the drops and not be re-inserted earlier than 15 minutes after use.
RISK FROM ANAPHYLACTIC REACTION: While taking β-blockers, patients with a history of 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.
Use in Pregnancy: TIMOPTOL has not been studied in human pregnancy. The use of TIMOPTOL requires that the anticipated benefit be weighed against possible hazards.
Use in Lactation: TIMOPTOL is detectable in human milk. Because of the potential for serious adverse reactions from TIMOPTOL in infants, a decision should be made whether to discontinue nursing or to discontinue TIMOPTOL, taking into account the importance of the drug to the mother.

Use in Pregnancy: TIMOPTOL has not been studied in human pregnancy. The use of TIMOPTOL requires that the anticipated benefit be weighed against possible hazards.
Use in Lactation: TIMOPTOL is detectable in human milk. Because of the potential for serious adverse reactions from TIMOPTOL in infants, a decision should be made whether to discontinue nursing or to discontinue TIMOPTOL, taking into account the importance of the drug to the mother.

TIMOPTOL is usually well tolerated. The following adverse reactions have been reported with ocular administration of this or other timolol maleate formulations, either in clinical trials or since the drug has been marketed.
Special Senses: Signs and symptoms of ocular irritation, including burning and stinging, 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 Precautions), tinnitus.
Cardiovascular: Bradycardia, arrhythmia, hypotension, syncope, heart block, cerebrovascular 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 anaphylaxis, angioedema, urticaria, localized and generalized rash.
Nervous System/Psychiatric: Dizziness, depression, insomnia, nightmares, memory loss, increase in signs and symptoms of myasthenia gravis, paresthesia.
Digestive: Nausea, diarrhea, dyspepsia, dry mouth, abdominal pain.
Urogenital: Decreased libido, Peyronie’s disease, sexual dysfunction.
Immunologic: Systemic lupus erythematosus.
Musculoskeletal: Myalgia.
Potential Side Effects: Side effects reported in clinical experience with systemic timolol maleate may be considered potential side effects of ophthalmic timolol maleate.

Although Timoptol used alone has little or no effect on pupil size, mydriasis resulting from concomitant therapy with Timoptol and epinephrine has been reported occasionally.
Potentiated systemic β-blockade (e.g., decreased heart rate) has been reported during combined treatment with CYP2D6 inhibitors (e.g., quinidine and SSRIs) and timolol.
The potential exists for additive effects and production of hypotension and/or marked bradycardia when TIMOPTOL is administered together with an oral calcium-entry blocker, catecholamine-depleting drugs, antiarrhythmics, parasympathomimetics or β-adrenergic-blocking agents.
Oral β-adrenergic blocking agents may exacerbate the rebound hypertension which can follow the withdrawal of clonidine.

Do not allow the tip of the container to touch the eye or areas around the eye. It may become contaminated with bacteria that can cause eye infections leading to serious damage of the eye, even loss of vision. To avoid possible contamination of the container, keep the tip of the container away from contact with any surface.
Instructions for Use: 1. Before using the medication for the first time, be sure the perforated seal is unbroken. A gap between the bottle and the cap is normal for an unopened bottle.
2. To open the bottle, unscrew the cap by turning as indicated by the arrows on the top of the cap. Do not pull the cap directly up and away from the bottle. Pulling the cap directly up will prevent the container from operating properly.
3. Tilt head back and pull the lower eyelid down slightly to form a pocket between the eyelid and the eye.
4. Invert the bottle and press lightly with the thumb or index finger over the "Finger Push Area" until a single drop is dispensed into the eye as directed by the physician.
Do not touch the eye or eyelid with the dropper tip.
Ophthalmic medications, if handled improperly, can become contaminated by common bacteria known to cause eye infections. Serious damage to the eye and subsequent loss of vision may result from using contaminated ophthalmic medications. If the medication may be contaminated or if the patient develop an eye infection, contact the physician immediately concerning continued use of this bottle.
5. After using Timoptol, press a finger into the corner of the eye by the nose for 2 minutes. This helps keep TIMOPTOL in the eye.
6. If drop dispensing is difficult after opening for the first time, replace the cap on the bottle and tighten (DO NOT OVERTIGHTEN) and then remove by turning the cap in the opposite direction as indicated by the arrows on top of the cap.
7. Repeat steps 3 & 4 with the other eye if instructed to do so by the physician.
8. Replace the cap by turning until it is firmly touching the bottle. The arrow on the left side of the cap must be aligned with the arrow on the left side of the bottle label for proper closure. Do not overtighten or may damage the bottle and cap.
9. The dispenser tip is designed to provide a single drop; therefore, do NOT enlarge the hole of the dispenser tip.
10. After all doses have been used, there will be some TIMOPTOL left in the bottle. The patient should not be concerned since an extra amount of TIMOPTOL has been added and the patient will get the full amount of TIMOPTOL that the physician prescribed. Do not attempt to remove excess medicine from the bottle.

Store at 25°C. Protect from light.

Antiglaucoma Preparations

S01ED01 - timolol ; Belongs to the class of beta blocking agents. Used in the treatment of glaucoma.

POM