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      A Comparison of the Short-Term Hypotensive Effects and Side Effects of Unilateral Brimonidine and Apraclonidine in Patients with Elevated Intraocular Pressure

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          Abstract

          Purpose: To compare the short-term ocular hypotensive efficacy and side effects of 0.2% brimonidine and 0.5% apraclonidine in patients with elevated intraocular pressure (IOP). Methods: We performed a double-masked, placebo-controlled study to compare the efficacy of the application of 0.2% brimonidine and 0.5% apraclonidine for the effect of IOP, systemic blood pressure and heart rate in 20 newly diagnosed ocular hypertensive patients. Effects on the untreated fellow eye and ocular side effects were also determined. All measurements were performed 1, 2, 4, 6 and 8 h after the instillation of one drop. Results: Brimonidine and apraclonidine significantly reduced IOP from baseline at all observation times. No significant difference was observed between the treatment groups. IOP decreased significantly in the untreated fellow eye in the brimonidine group at 4-, 6- and 8-hour checks and at 6-hour checks in the apraclonidine group when compared with placebo. Blood pressure and heart rate decreased significantly in the brimonidine group compared with placebo. Apraclonidine did not affect blood pressure or heart rate any differently than placebo. The pupil diameter and the interpalpebral fissure width significantly increased in the apraclonidine group, but not in the brimonidine group. There were no significant differences in the overall incidence of foreign body sensation, burning and stinging and dry mouth in the treatment groups. Conclusions: In the short-term, brimonidine was effective in reducing IOP in patients with elevated IOP and was equivalent in efficacy to apraclonidine. On the other hand, a significant change in blood pressure and heart rate was observed with brimonidine; there was no change at all in the apraclonidine group.

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          Sub types of α2-adrenoceptors: Pharmacological and molecular biological evidence converg

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            Apraclonidine and brimonidine effects on anterior ocular and cardiovascular physiology in normal and sympathectomized monkeys.

            Apraclonidine and brimonidine administered topically to one eye of ketamine-anesthetized normal cynomolgus monkeys each produced a dose-related bilateral reduction in intraocular pressure which was not dependent on intact sympathetic innervation. Brimonidine was more potent and efficacious (10-12 mmHg maximum intraocular pressure reduction 2 hr after 200 micrograms) but produced a shorter-lasting effect than apraclonidine (4 mmHg maximum intraocular pressure reduction 1-6 hr after 600-1000 micrograms). Apraclonidine had little effect on pupil diameter, but brimonidine produced a dose-related bilateral miosis which was dependent on intact sympathetic innervation. Neither drug significantly affected refractive error. Topical brimonidine, but not apraclonidine, produced a dose-dependent reduction in mean arterial blood pressure, while both drugs lowered heart rate. A dose-dependent bilateral reduction in aqueous humor flow rate calculated over a 6-hr period following drug administration was produced by both topical apraclonidine (maximum 30-35% reduction with 600 micrograms) and brimonidine (maximum 30-45% reduction with 50-250 micrograms), which was not dependent on intact sympathetic innervation. Maintenance of blood pressure by intravenous infusion of angiotensin II had no effect on the aqueous humor flow suppression produced by 100 micrograms of topical brimonidine, but pentobarbital anesthesia abolished it. Intracameral injection of 10 micrograms brimonidine in rhesus monkeys produced an ipsilateral approximately 15% reduction in aqueous humor flow calculated for the 1-3 hr post-injection period. The cardiovascular and contralateral ocular effects observed with both drugs are presumably related to the monkeys' small body weight, and the magnitude of IOP reduction for a given degree of flow suppression would be greater in hypertensive than in normotensive eyes. Caution must therefore be exercised in extrapolating from our data in ocular normotensive monkeys to the glaucomatous human.
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              Author and article information

              Journal
              OPH
              Ophthalmologica
              10.1159/issn.0030-3755
              Ophthalmologica
              S. Karger AG
              0030-3755
              1423-0267
              2002
              February 2002
              14 March 2002
              : 216
              : 1
              : 45-49
              Affiliations
              Department of Ophthalmology, Kocaeli University, School of Medicine, Kocaeli, Turkey
              Article
              48296 Ophthalmologica 2002;216:45–49
              10.1159/000048296
              11901288
              841ed682-3607-441d-ac6c-a4fe7e16438b
              © 2002 S. Karger AG, Basel

              Copyright: All rights reserved. No part of this publication may be translated into other languages, reproduced or utilized in any form or by any means, electronic or mechanical, including photocopying, recording, microcopying, or by any information storage and retrieval system, without permission in writing from the publisher. Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in government regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug. Disclaimer: The statements, opinions and data contained in this publication are solely those of the individual authors and contributors and not of the publishers and the editor(s). The appearance of advertisements or/and product references in the publication is not a warranty, endorsement, or approval of the products or services advertised or of their effectiveness, quality or safety. The publisher and the editor(s) disclaim responsibility for any injury to persons or property resulting from any ideas, methods, instructions or products referred to in the content or advertisements.

              History
              Page count
              Figures: 2, Tables: 2, References: 27, Pages: 5
              Categories
              Original Paper · Travail original · Originalarbeit

              Vision sciences,Ophthalmology & Optometry,Pathology
              Apraclonidine,Intraocular pressure,Glaucoma, primary open angle,Brimonidine

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