Systemic and Local Tolerability of Ophthalmic Drug Formulations

Abstract

All eye drops raise problems of local tolerance, but with variable frequencies. They can induce pain on instillation, allergic reactions, delayed healing, punctate keratitis, disturbances of lacrimal secretion, disturbances of accommodation (especially the parasympathomimetics) and local pigmentation after prolonged use. Corticosteroids are associated with 2 major risks: chronic glaucoma and cataract, initially reversible if treatment is stopped. There is still a major risk of corneal herpes with corticosteroids. It is important to be aware of these local problems as they are responsible for poor patient compliance. The systemic effects essentially concern the agonists and antagonists of the autonomic nervous system. beta-Blocker eye drops can cause bronchospasm, heart failure, syncope and psychiatric disorders, especially at high doses and with nonselective beta-blockers. These consequences are usually related to failure to comply with the prescribing precautions. alpha-Adrenergic agonists, which exert dose-dependent effects, can induce hypertensive crises or angina attacks. Apart from patients at risk (children under the age of 30 months and the elderly), parasympathomimetics cause few systemic adverse effects; anticholinesterases, which have curare-like properties, are contraindicated for 6 weeks before general anesthesia. In the very young and the very old, atropinic eye drops carry a risk of cardiovascular collapse and neuropsychiatric disturbances. Problems may also occur with other classes of drugs such as anti-infectives, antispectics, anti-inflammatories and contact lens products. Nevertheless, it is clear that this form of treatment is generally very well tolerated in relation to the volume of eye drops prescribed by ophthalmologists each day.

Comparison of Ocular Surface Side Effects of Topical Travoprost and Bimatoprost

“…All eyedrops can cause some local adverse events, but with variable frequencies on the basis of individual susceptibility. They may induce pain on instillation, allergic reactions, delayed healing response, punctate keratitis, altered lacrimal secretion, disturbed accommodation and local pigmentation, especially after prolonged use [9, 10]. Local side effects of antiglaucomatous drugs may have a negative effect both on the compliance of the patient and the success of subsequent filtrating surgery [11,12,13,14] and may cause some other pathologies such as dry eye.…”

Ocular surface changes induced by topical application of latanoprost and timolol: a short-term study in glaucomatous patients with and without allergic conjunctivitis

“…They can induce pain on instillation, allergic reactions, delayed healing, punctate keratitis, altered lacrimal secretion, and disturbed accommodation and local pigmentation, especially after prolonged use [19]. Many of these conditions are caused by the pharmacological peculiarities of the compounds themselves, but the ophthalmological formulations may also be responsible for the occurrence of the side effects.…”

A review of evidence guiding the use of corticosteroids in the treatment of intraocular inflammation

“…The pharmacology and side effects of corticosteroids have been previously addressed elsewhere; no attempt is made to duplicate those efforts in this review. [1][2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18] available corticosteroid formulations The most commonly used corticosteroids in ophthalmic practice are listed in Tables 1 and 2. The pharmacology of the currently available agents employed in the treatment of intraocular inflammatory disease has been exhaustively reviewed in other publications.…”