Timolol hemihydrate: a new formulation of timolol for the treatment of glaucoma. 1996

W C Stewart
Department of Ophthalmology, Medical University of South Carolina, Charleston, USA.

Timolol maleate, a non-selective beta-adrenergic blocker, has been used to treat glaucoma and ocular hypertension for almost two decades. Recently a new preparation, timolol hemihydrate, has been described which eliminates the maleate buffer and simplifies the purification step for the R-enantiomer. The ocular pharmacology of the two medicines is expected to be similar. Ocular bioavailability as well as toxicity for timolol hemihydrate is similar to that which has been shown previously for timolol maleate. In a multicenter trial in the United States, timolol hemihydrate was shown to reduce the intraocular pressure to a similar extent as timolol maleate. At the week 12 visit intraocular pressure was 19.5 and 19.5 mm Hg for the hemihydrate and maleate groups respectively for the 0.25% concentration and 18.3 and 18.6 mm Hg respectively for the 0.5% concentration. Following a nine month open-label portion where patients were treated with timolol hemihydrate only intraocular pressure was 19.9 and 19.1 mm Hg for the 0.25% and 0.5% concentrations respectively. Ocular and systemic adverse events, as well as vital signs, were similar between timolol hemihydrate and maleate. In conclusion, timolol hemihydrate appears to be a safe and effective medicine in the treatment of ocular hypertension and chronic open-angle glaucoma.

UI MeSH Term Description Entries
D009798 Ocular Hypertension A condition in which the intraocular pressure is elevated above normal and which may lead to glaucoma. Glaucoma, Suspect,Hypertension, Ocular,Glaucomas, Suspect,Hypertensions, Ocular,Ocular Hypertensions,Suspect Glaucoma,Suspect Glaucomas
D002626 Chemistry, Pharmaceutical Chemistry dealing with the composition and preparation of agents having PHARMACOLOGIC ACTIONS or diagnostic use. Medicinal Chemistry,Chemistry, Pharmaceutic,Pharmaceutic Chemistry,Pharmaceutical Chemistry,Chemistry, Medicinal
D002986 Clinical Trials as Topic Works about pre-planned studies of the safety, efficacy, or optimum dosage schedule (if appropriate) of one or more diagnostic, therapeutic, or prophylactic drugs, devices, or techniques selected according to predetermined criteria of eligibility and observed for predefined evidence of favorable and unfavorable effects. This concept includes clinical trials conducted both in the U.S. and in other countries. Clinical Trial as Topic
D005902 Glaucoma, Open-Angle Glaucoma in which the angle of the anterior chamber is open and the trabecular meshwork does not encroach on the base of the iris. Glaucoma Simplex,Glaucoma, Pigmentary,Glaucoma, Simple,Open-Angle Glaucoma,Chronic Primary Open Angle Glaucoma,Glaucoma, Compensated,Glaucoma, Compensative,Glaucoma, Open Angle,Glaucoma, Primary Open Angle,Glaucoma, Secondary Open Angle,Primary Open Angle Glaucoma,Secondary Open Angle Glaucoma,Compensated Glaucoma,Compensative Glaucoma,Open Angle Glaucoma,Open Angle Glaucomas,Open-Angle Glaucomas,Pigmentary Glaucoma,Simple Glaucoma,Simplex, Glaucoma,Simplices, Glaucoma
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000319 Adrenergic beta-Antagonists Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety. Adrenergic beta-Antagonist,Adrenergic beta-Receptor Blockader,Adrenergic beta-Receptor Blockaders,beta-Adrenergic Antagonist,beta-Adrenergic Blocker,beta-Adrenergic Blocking Agent,beta-Adrenergic Blocking Agents,beta-Adrenergic Receptor Blockader,beta-Adrenergic Receptor Blockaders,beta-Adrenoceptor Antagonist,beta-Blockers, Adrenergic,beta-Adrenergic Antagonists,beta-Adrenergic Blockers,beta-Adrenoceptor Antagonists,Adrenergic beta Antagonist,Adrenergic beta Antagonists,Adrenergic beta Receptor Blockader,Adrenergic beta Receptor Blockaders,Adrenergic beta-Blockers,Agent, beta-Adrenergic Blocking,Agents, beta-Adrenergic Blocking,Antagonist, beta-Adrenergic,Antagonist, beta-Adrenoceptor,Antagonists, beta-Adrenergic,Antagonists, beta-Adrenoceptor,Blockader, Adrenergic beta-Receptor,Blockader, beta-Adrenergic Receptor,Blockaders, Adrenergic beta-Receptor,Blockaders, beta-Adrenergic Receptor,Blocker, beta-Adrenergic,Blockers, beta-Adrenergic,Blocking Agent, beta-Adrenergic,Blocking Agents, beta-Adrenergic,Receptor Blockader, beta-Adrenergic,Receptor Blockaders, beta-Adrenergic,beta Adrenergic Antagonist,beta Adrenergic Antagonists,beta Adrenergic Blocker,beta Adrenergic Blockers,beta Adrenergic Blocking Agent,beta Adrenergic Blocking Agents,beta Adrenergic Receptor Blockader,beta Adrenergic Receptor Blockaders,beta Adrenoceptor Antagonist,beta Adrenoceptor Antagonists,beta Blockers, Adrenergic,beta-Antagonist, Adrenergic,beta-Antagonists, Adrenergic,beta-Receptor Blockader, Adrenergic,beta-Receptor Blockaders, Adrenergic
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013999 Timolol A beta-adrenergic antagonist that is similar in action to PROPRANOLOL; the levo-isomer is more active. Timolol has been proposed as an anti-hypertensive, anti-arrhythmic, anti-angina, and anti-glaucoma agent. It is also used in the treatment of MIGRAINE DISORDERS and tremor. (S)-1-((1,1-Dimethylethyl)amino)-3-((4-(4-morpholinyl)-1,2,5-thiadazol-3-yl)oxy)-2-propanol,2-Propanol, 1-((1,1-dimethylethyl)amino)-3-((4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl)oxy)-, (S)-,Blocadren,L-714,465,MK-950,Optimol,Timacar,Timolol Hemihydrate,Timolol Maleate,Timolol Maleate, (1:1) Salt,Timoptic,Timoptol,L 714,465,L714,465,MK 950,MK950

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