ISTALOL (timolol maleate)

In a study of plasma drug concentration in 12 healthy subjects, the systemic exposure to timolol was determined following twice daily administration of ISTALOL (exaggerated regimen) for eight days. With ISTALOL, mean plasma concentrations of timolol were 0.68 ng/mL and 0.88 ng/mL two hours after the first dose and the dose on the eighth day, respectively.

In a controlled, double-masked, parallel study in 332 patients with untreated intraocular pressures of 22 mm Hg or greater, ISTALOL 0.5% administered once daily (AM) was equivalent to timolol maleate ophthalmic solution 0.5% administered twice daily. In both groups, mean intraocular pressure decreased from 25 mm Hg at baseline to 18 mm Hg at peak and 19 mm Hg at trough. ISTALOL was generally well tolerated, and 3% of patients had treatment discontinued for adverse events judged related to treatment. There was a slight decrease in cardiovascular function consistent with known systemic absorptio...

The most frequently reported adverse reactions have been burning and stinging upon instillation in 38% of patients treated with ISTALOL. Additional reactions reported with ISTALOL at a frequency of 4% to 10% include: blurred vision, cataract, conjunctival injection, headache, hypertension, infection, itching and decreased visual acuity. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Bausch & Lomb Incorporated at 1-800-553-5340 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical ...

Bronchial asthma, a history of bronchial asthma, severe chronic obstructive pulmonary disease ( 4.1 , 5.1 , 5.3 ) Sinus bradycardia, second or third degree atrioventricular block, overt cardiac failure, cardiogenic shock ( 4.2 , 5.2 ) Hypersensitivity to any component of this product ( 4.3 ) 4.1 Asthma, COPD ISTALOL is contraindicated in patients with bronchial asthma; a history of bronchial asthm...

Potentiation of Respiratory Reactions Including Asthma ( 5.1 ) Cardiac Failure ( 5.2 ) Obstructive Pulmonary Disease ( 5.3 ) Increased Reactivity to Allergens ( 5.4 ) Potentiation of Muscle Weakness ( 5.5 ) Masking of Hypoglycemic Symptoms in Patients with Diabetes Mellitus ( 5.6 ) Masking of Thyrotoxicosis ( 5.7 ) 5.1 Potentiation of Respiratory Reactions Including Asthma ISTALOL contains timolol maleate; and although administered topically, it can be absorbed systemically. Therefore, the same ...

7 DRUG INTERACTIONS Concomitant use with systemic beta-blockers may potentiate systemic beta-blockade. ( 7.1 ) Oral or intravenous calcium antagonists may cause atrioventricular conduction disturbances, left ventricular failure, and hypotension. ( 7.2 ) Catecholamine-depleting drugs may have additive effects and produce hypotension and/or marked bradycardia. ( 7.3 ) Digitalis and calcium antagonis...