Cardiovascular responses to metipranolol and timolol eyedrops in healthy volunteers.

Abstract

1 Intraocular pressure and cardiovascular responses to metipranolol 0.1% and 0.3% and timolol 0.25% eyedrops were measured in a balanced single dose placebo-controlled crossover study in eight healthy volunteers aged 34-58 years. 2 Timolol 0.25% and metipranolol 0.3% reduced intraocular pressure throughout the 6 h period of observation to a similar extent. Metipranolol 0.1% was marginally less effective, significantly reducing pressure up to 4 h only. 3 No drug treatment significantly altered resting heart rate or blood pressure. Timolol 0.25% significantly reduced exercise tachycardia (P < 0.05), an effect which was not shown by metipranolol 0.1 or 0.3% . Exertional pain in the legs occurred more frequently after timolol 0.25% and metipranolol 0.3% than after metipranolol 0.1% or placebo eyedrops. 4 Octan-1-ol/pH 7.4 buffer distribution coefficients at 370 C were found to be: metipranolol 5.19, timolol 0.84, indicating that metipranolol has an approximately 6-fold greater lipid solubility. 5 It is concluded that, by comparison with timolol, metipranolol in eyedrop concentrations up to 0.3%, despite its greater lipid solubility, reaches concentrations in the systemic circulation which are less likely to affect the heart.

Effects of Timolol and Latanoprost on Respiratory and Cardiovascular Status in Elderly Patients With Glaucoma

“…Beta-blocker-related adverse systemic reactions following systemic or ophthalmic use have been widely reported in the literature and most commonly involve the cardiovascular and pulmonary systems. 3,14 In particular, non-cardioselective beta-blockers such as timolol, metipranolol, carteolol, and levobunolol can adversely affect cardiovascular and pulmonary functions in healthy volunteers, 15 as well as in patients with existing diseases such as heart failure, sinus bradycardia, chronic obstructive airways disease, or asthma. 16 In elderly people, other diseases may prevent breathlessness from being noticed; in addition reduced exercise tolerance and breathlessness may be accepted as part of old age.…”

Topical glaucoma medications and cardiovascular risk in the elderly

“…[3-Blockers applied topically in the eye may be absorbed into the systemic circulation. [10][11][12] Such systemic absorption would be expected to affect the cardiovascular system through [3-receptor blockade. 13 , 14 Ball,15 Linkewich and Herling, 16 and Britman'?…”

Preventive effect of lacrimal occlusion on topical timolol‐induced bronchoconstriction in asthmatics

“…Beta‐blocker‐related adverse systemic reactions following systemic or ophthalmic use have been widely reported in the literature, and most commonly involve the cardiovascular and pulmonary systems 1,2 . In particular, non‐cardioselective beta‐blockers such as timolol, metipranolol, carteolol, and levobunolol can adversely affect cardiovascular and bronchopulmonary function in healthy volunteers 3,4 , as well as in patients with existing diseases such as heart failure, sinus bradycardia, chronic obstructive airways disease, or asthma 5,6 .…”