| Development of D-timolol for the treatment of glaucoma and ocular hypertension. | |
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MedLine Citation:
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PMID: 2193994 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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It has been found that D-timolol is equipotent or slightly less potent than L-timolol to lower the intraocular pressure (IOP) in normotensive rabbits, water loaded ocular hypertensive rabbits, alpha-chymotrypsin induced glaucoma rabbits, hypertonic saline infused IOP recovery model of rabbits, normotensive human volunteers, glaucoma patients and ocular hypertensive human individuals. Although L-timolol has been used widely for the treatment of glaucoma and ocular hypertension, it produces numerous side effects including cardiovascular disturbances, asthmatic attack, psychological depression, etc. Since D-timolol has much weaker affinity toward beta-adrenergic receptors, it was found to have 1/80-1/300 the beta-adrenergic blocking potency of L-timolol to block beta-adrenergic receptors in guinea pig tracheal preparations and 1/90 of L-timolol to block beta-adrenergic receptors in guinea pig atrial preparations. As a result, D-timolol showed no subjective nor objective side effects on pupil size, conjunctiva, cornea, blood pressure and pulse rate. Further, D-timolol was reported to increase retinal and choroid blood flow in rabbits without affecting overall ocular blood flow. On the contrary, L-timolol was found to significantly reduce the overall ocular blood flow and retinal and choroid blood flows in rabbits, although it might slightly increase the retinal blood flow in normotensive individuals. D-Timolol was well absorbed across the cornea as L-timolol and produced the duration of action as long as L-timolol. These results indicate that D-timolol could be a better agent than L-timolol for the treatment of glaucoma and ocular hypertension. |
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Authors:
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G C Chiou |
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Publication Detail:
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Type: Journal Article; Review |
Journal Detail:
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Title: Journal of ocular pharmacology Volume: 6 ISSN: 8756-3320 ISO Abbreviation: J Ocul Pharmacol Publication Date: 1990 |
Date Detail:
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Created Date: 1990-08-08 Completed Date: 1990-08-08 Revised Date: 2005-11-16 |
Medline Journal Info:
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Nlm Unique ID: 8511297 Medline TA: J Ocul Pharmacol Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 67-74 Citation Subset: IM |
Affiliation:
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Department of Medical Pharmacology and Toxicology, Texas A&M University College of Medicine, College Station. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Drug Evaluation Glaucoma / drug therapy* Humans Ocular Hypertension / drug therapy* Timolol / therapeutic use* |
| Chemical | |
Reg. No./Substance:
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26839-75-8/Timolol |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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