Aim: It was our aim to study the penetration of sodium pyruvate into the aqueous humor of humans after its topical application as an eye drop. Methods: Two hours prior to surgery, one drop of 5% sodium pyruvate prepared in artificial tears was instilled in the eye to be operated upon for cataract extraction. The drops were given 4 times at 10-min intervals. Eye drops containing tropicamide, phenylephrine, flurbiprofen and tobramycin were also given preoperatively. At the start of surgery, an aqueous sample was withdrawn, kept refrigerated and analyzed for pyruvate within 2 h. The cataracts were then extracted either by routine extracapsular extraction or by phacoemulsification, both followed by intraocular lens implantation. The pyruvate level was determined colorimetrically by reacting it with 2,4-dinitrophenyl hydrazine. Results: The level of pyruvate in the aqueous sample of patients that did not receive pyruvate eye drops was only 0.145 ± 0.06 mM. In the group given pyruvate, it increased to approximately 0.35–0.525 mM. Conclusion: The results demonstrate that topical administration of pyruvate is effective in elevating its concentration in the aqueous humor to a level adequate to offer protection against oxidative stress to the lens and other intraocular tissues. Hence, it should be feasible to carry out clinical trials with this compound aimed at treating diseases such as cataracts and diabetic retinopathy induced by generation of reactive oxygen species and consequent oxidative stress.

Varma SD, Ets TK, Richards RD: Protection against superoxide radicals in the rat lens. Ophthalmic Res 1977;9:421–423.
Kowluru RA, Kern TS, Engerman RL, Armstrong D: Abnormalities of retinal metabolism in diabetic rat and experimental galactosemia. 3. Effect of antioxidant diets. Diabetes 1996;45:1233–1237.
Resnikoff S, Pascolino D, Etya’ale D, Kocur I, et al: Global data on visual impairment in the year 2000. Bull World Health Organ 2004;82:844–851.
Hegde KR, Varma SD: Prevention of cataract in experientially diabetic mice. Mol Cell Biochem 2005;269:115–120.
Varma SD, Hegde KR, Kovtun S: Attenuation and delay of diabetic cataracts by antioxidants: effectiveness of pyruvate after onset of cataract. Ophthalmologica 2005;219:309–315.
Ayala MN, Soderberg PG: Vitamin E can protect against ultraviolet radiation-induced cataract in albino rats. Ophthalmic Res 2004;36:264–269
Creighton MO, Ross WM, Stewart-DeHaan PJ, Sanwal M, Trevithick JR: Modelling cortical cataractogenesis. 7. Effects of vitamin E treatment on galactose-induced cataracts. Exp Eye Res 1985;40:213–222.
Monnier VM, Stevens VJ, Cerami A: Nonenzymatic glycosylation, sulfhydryl oxidation and aggregation of lens proteins in experimental sugar cataracts. J Exp Med 1979;150:1098–1107.
Case EM: The determination of pyruvic acid. Biochem J 1932;26:753–758.
Copyright / Drug Dosage / Disclaimer
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.
You do not currently have access to this content.