Timolol Maleate Dosage & Rx Info

Timolol Maleate Generic Name & Formulations

Legal Class

General Description

Timolol (as maleate) 0.25%, 0.5%; oph soln; contains benzalkonium chloride.

Pharmacological Class

Noncardioselective beta-blocker.

How Supplied

Soln, gel—contact supplier; Ocudose—60

Manufacturer

Various generic manufacturers

Mechanism of Action

Timolol maleate is a beta₁ and beta₂ (non-selective) adrenergic receptor blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity. When applied topically on the eye, it has the action of reducing elevated, as well as normal intraocular pressure, whether or not accompanied by glaucoma. The precise mechanism of the ocular hypotensive action is not clearly established at this time. Tonography and fluorophotometry studies in man suggest that its predominant action may be related to reduced aqueous formation.

Timolol Maleate Indications

Indications

Elevated intraocular pressure in ocular hypertension or open-angle glaucoma.

Timolol Maleate Dosage and Administration

Adults and Children

<2yrs: not established. ≥2yrs: Initially 1 drop of 0.25% twice daily; max 1 drop of 0.5% twice daily. Transfer from other drugs, see full labeling.

Timolol Maleate Contraindications

Contraindications

Greater than 1^st-degree AV block. Uncompensated cardiac failure. Cardiogenic shock. Sinus bradycardia. History of bronchospasm. Bronchial asthma. Severe COPD.

Timolol Maleate Boxed Warnings

Not Applicable

Timolol Maleate Warnings/Precautions

Warnings/Precautions

Not for use as sole agent in angle-closure glaucoma. Poor cardiac reserve should be controlled with digitalis and diuretics. Diabetes. Presbyopia. May mask hypoglycemia or thyrotoxicosis. Myasthenia gravis. Cerebrovascular insufficiency. Measure intraocular pressure after 4 weeks of treatment. Avoid abrupt cessation. Discontinue at 1^st sign of cardiac failure and before surgery. Pregnancy. Nursing mothers: not recommended.

Timolol Maleate Pharmacokinetics

Metabolism

Hepatic.

Elimination

Renal. Half-life: ~2.9 hours.

Timolol Maleate Interactions

Interactions

May potentiate systemic β-blockers, reserpine, hypoglycemics and mydriatic effect of topical epinephrine. Additive cardiac and pulmonary effects with anticholinesterase miotics. May antagonize bronchodilation from β-adrenergic agonists. May cause conduction defects with calcium channel blockers, digoxin. May be potentiated by CYP2D6 inhibitors (eg, quinidine, SSRIs).

Timolol Maleate Adverse Reactions

Adverse Reactions

Ocular irritation, sensitization, rash, dizziness, blurred vision, corneal anesthesia, headache, GI upset, paresthesias. Systemic β-blocker effects (bradycardia, arrhythmias, hypotension, bronchospasm, heart failure). Aphakic maculopathy (rare).

Timolol Maleate Clinical Trials

See Literature

Timolol Maleate Note

Notes

Formerly known under the brand name Timoptic.

Timolol Maleate Patient Counseling