Timolol Hemihydrate

Generic Name: timolol hemihydrate

beta-Adrenergic Blocker [EPC]Over-the-Counter (OTC)

Brand Names:

Timolol Hemihydrate

DESCRIPTION Timolol ophthalmic solution 0.5%, is a non-selective beta-adrenergic antagonist for ophthalmic use. The chemical name of the active ingredient is (S)-1-[(1,1-dimethylethyl) amino]-3- [[4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl]oxy]-2-propanol. Timolol hemihydrate is the levo isomer. Specific rotation is [α] 25 405nm=-16° (C=10% as the hemihydrate form in 1N HCl).

Overview

DESCRIPTION Timolol ophthalmic solution 0.5%, is a non-selective beta-adrenergic antagonist for ophthalmic use. The chemical name of the active ingredient is (S)-1-[(1,1-dimethylethyl) amino]-3- [[4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl]oxy]-2-propanol. Timolol hemihydrate is the levo isomer. Specific rotation is [α] 25 405nm=-16° (C=10% as the hemihydrate form in 1N HCl).

Uses

INDICATIONS AND USAGE Timolol ophthalmic solution is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.

Dosage

DOSAGE AND ADMINISTRATION Timolol Ophthalmic Solution is available in concentration of 0.5 percent. The usual starting dose is one drop of 0.25 percent timolol ophthalmic solution 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. If the intraocular pressure is maintained at satisfactory levels, the dosage schedule may be changed to one drop once a day in the affected eye(s). Because of diurnal variations in intraocular pressure, satisfactory response to the once-a-day dose is best determined by measuring the intraocular pressure at different times during the day.

Side Effects

ADVERSE REACTIONS The most frequently reported ocular event in clinical trials was burning/stinging on instillation and was comparable between timolol ophthalmic solution and timolol maleate (approximately one in eight patients). The following adverse events were associated with use of timolol ophthalmic solution in frequencies of more than 5% in two controlled, double-masked clinical studies in which 184 patients received 0.5% timolol ophthalmic solution: OCULAR: Dry eyes, itching, foreign body sensation, discomfort in the eye, eyelid erythema, conjunctival injection, and headache. BODY AS A WHOLE: Headache.

Warnings

WARNINGS As with other topically applied ophthalmic drugs, timolol ophthalmic solution is absorbed systemically. The same adverse reactions found with systemic administration of beta-adrenergic blocking agents may occur with topical administration. For example, severe respiratory and cardiac reactions, including death due to bronchospasm in patients with asthma, and rarely, death in association with cardiac failure have been reported following systemic or topical administration of beta-adrenergic blocking agents. Cardiac Failure: Sympathetic stimulation may be essential for support of the circulation in individuals with diminished myocardial contractility, and its inhibition by beta-adrenergic receptor blockade may precipitate more severe cardiac failure. CONTRAINDICATIONS Timolol ophthalmic solution is contraindicated in patients with overt heart failure, cardiogenic shock, sinus bradycardia, second- or third-degree atrioventricular block, bronchial asthma or history of bronchial asthma, or severe chronic obstructive pulmonary disease, or hypersensitivity to any component of this product.

Storage

HOW SUPPLIED Timolol ophthalmic solution is a clear, colorless solution. Timolol ophthalmic solution 0.5% is supplied in a white, opaque, plastic, ophthalmic dispenser bottle with a controlled drop tip as follows: NDC 70069- 696 -01 5 mL fill in 5 mL bottle NDC 70069- 697 -01 10 mL fill in 10 mL bottle NDC 70069- 698 -01 15 mL fill in 15 mL bottle Rx Only STORAGE Store at 15° to 25°C (59° to 77°F)...

Frequently Asked Questions

What is Timolol Hemihydrate used for?

INDICATIONS AND USAGE Timolol ophthalmic solution is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.

What are the side effects of Timolol Hemihydrate?

ADVERSE REACTIONS The most frequently reported ocular event in clinical trials was burning/stinging on instillation and was comparable between timolol ophthalmic solution and timolol maleate (approximately one in eight patients). The following adverse events were associated with use of timolol ophthalmic solution in frequencies of more than 5% in two controlled, double-masked clinical studies in which 184 patients received 0.5% timolol ophthalmic solution: OCULAR: Dry eyes, itching, foreign body sensation, discomfort in the eye, eyelid erythema, conjunctival injection, and headache. BODY AS A WHOLE: Headache.

What are the important warnings for Timolol Hemihydrate?

WARNINGS As with other topically applied ophthalmic drugs, timolol ophthalmic solution is absorbed systemically. The same adverse reactions found with systemic administration of beta-adrenergic blocking agents may occur with topical administration. For example, severe respiratory and cardiac reactions, including death due to bronchospasm in patients with asthma, and rarely, death in association with cardiac failure have been reported following systemic or topical administration of beta-adrenergic blocking agents. Cardiac Failure: Sympathetic stimulation may be essential for support of the circulation in individuals with diminished myocardial contractility, and its inhibition by beta-adrenergic receptor blockade may precipitate more severe cardiac failure. CONTRAINDICATIONS Timolol ophthalmic solution is contraindicated in patients with overt heart failure, cardiogenic shock, sinus bradycardia, second- or third-degree atrioventricular block, bronchial asthma or history of bronchial asthma, or severe chronic obstructive pulmonary disease, or hypersensitivity to any component of this product.

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Medical Disclaimer

This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.