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Timoptic Overdose, Contraindications and Information - Timolol Maleate

Timoptic Overdose, Contraindications and Information - Timolol Maleate

OVERDOSE

Tablets, Ophthalmic Solutions, and Ophthalmic Gel Forming Solution

There have been reports of inadvertent overdosage with timolol maleate 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 (see ADVERSE REACTIONS).

Overdosage has been reported with timolol maleate tablets. A 30-year-old female ingested 650 mg of timolol maleate (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.

Significant lethality was observed in female rats and female mice after a single dose of 900 and 1190 mg/kg (5310 and 3570 mg/m2) of timolol maleate, respectively.

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.

Additional Information for Ophthalmic Gel Forming Solution: No data are available in regard to human overdosage with or accidental oral ingestion of timolol maleate ophthalmic gel forming solution.

Tablets

The most common signs and symptoms to be expected with overdosage with a beta-adrenergic receptor blocking agent are symptomatic bradycardia, hypotension, bronchospasm, and acute cardiac failure. Therapy with timolol maleate should be discontinued and the patient observed closely. The following additional therapeutic measures should be considered:

1. Gastric Lavage.

2. Symptomatic Bradycardia: Use atropine sulfate intravenously in a dosage of 0.25 mg to 2 mg to induce vagal blockade. If bradycardia persists, intravenous isoproterenol HCl should be administered cautiously. In refractory cases the use of a transvenous cardiac pacemaker may be considered.

3. Hypotension: Use sympathomimetic pressor drug therapy, such as dopamine, dobutamine or levarterenol. In refractory cases the use of glucagon HCl has been reported to be useful.

4. Bronchospasm: Use isoproterenol HCl. Additional therapy with aminophylline may be considered.

5. 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 HCl which has been reported to be useful.

6. Heart Block (Second or Third Degree): Use isoproterenol HCl or a transvenous cardiac pacemaker.

CONTRAINDICATIONS

Timolol maleate is contraindicated in patients with bronchial asthma or with a history of bronchial asthma, or severe chronic obstructive pulmonary disease (see WARNINGS); sinus bradycardia; second or third degree atrioventricular block; overt cardiac failure (see WARNINGS); cardiogenic shock; or hypersensitivity to any component of this product.

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