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1 General aspects (0)   1.1 Epidemiology (3)   1.2 Population genetics (25)   1.3 Pathogenesis (13)   1.4 Quality of life (1)   1.5 Glaucomas as cause of blindness (3)   1.6 Prevention and screening (6) 2 Anatomical structures in glaucoma (0)   2.1 Conjunctiva (1)   2.2 Cornea (4)   2.3 Sclera (1)   2.4 Anterior chamber angle (1)   2.5 Meshwork (10)     2.5.1 Trabecular meshwork (0)     2.5.2 Schlemms canal (0)     2.5.3 Scleral outlet channels (0)   2.6 Aqueous humor dynamics (4)     2.6.1 Production (0)     2.6.2 Outflow (0)       2.6.2.1 Trabecular meshwork (0)       2.6.2.2 Uveoscleral (0)     2.6.3 Compostion (0)   2.7 Episcleral veins and venous pressure (0)   2.8 Iris (1)   2.9 Ciliary body (3)   2.10 Lens (0)   2.11 Vitreous body (0)   2.12 Choroid, peripapillary choroid, peripapillary atrophy (2)   2.13 Retina and retinal nerve fibre layer (18)   2.14 Optic disc (20)   2.15 Optic nerve (0)   2.16 Chiasma and retrochiasmal central nervous system (0)   2.17 Stem cells (0)   2.20 Other (0) 3 Laboratory methods (0)   3.1 Microscopy (1)   3.2 Electron microscopy (2)   3.3 Immunohistochemistry (3)   3.4 Molecular genetics (1)     3.4.1 Linkage studies (0)     3.4.2 Gene studies (0)   3.5 Molecular biology incl. SiRNA (0)   3.6 Cellular biology (0)   3.7 Biochemistry (0)   3.8 Pharmacology (0)   3.9 Pathophysiology (0)   3.10 Immunobiology (0)   3.11 Pharmacogenetics (0)   3.12 Proteomics (0)   3.13 In vivo imaging (0)     3.13.1 Laser Scanning (0)       3.13.1.1 Confocal Scanning Laser Ophthalmoscopy (0)       3.13.1.2 Confocal Scanning Laser Polarimetry (0)     3.13.2 Optical Coherence Tomography (0)       3.13.2.1 Anterior Segment (0)       3.13.2.2 Posterior Segment (0)     3.13.3 RGC Imaging (0)     3.13.4 Other (0)   3.20 Other (0) 4 Tissue culture of ocular cells (5) 5 Experimental glaucoma; animal models (15)   5.1 Rodent (0)   5.2 Primates (0)   5.3 Other (0) 6 Clinical examination methods (0)   6.1 Intraocular pressure measurement; factors affecting IOP (8)     6.1.1 Devices, techniques (0)     6.1.2 Fluctuation, circadian rhythms (0)     6.1.3 Factors affecting IOP (0)   6.2 Tonography, aqueous flow measurement (see also 2.6) (0)   6.3 Biomicroscopy (slitlamp) (0)     6.3.1 Anterior segment (0)     6.3.2 Posterior segment (0)   6.4 Gonioscopy (0)   6.5 Ophthalmoscopy (1)   6.6 Visual field examination and other visual function tests (2)     6.6.1 Conventional manual (0)     6.6.2 Automated (6)     6.6.3 Special methods (e.g. color, contrast, SWAP etc.) (14)   6.7 Electro-ophthalmodiagnosis (7)   6.8 Photography (0)     6.8.1 Anterior segment (0)     6.8.2 Posterior segment (11)   6.9 Computerized image analysis (0)     6.9.1 Laser scanning (15)       6.9.1.1 Confocal Scanning Laser Ophthalmoscopy (0)       6.9.1.2 Confocal Scanning Laser Polarimetry (0)     6.9.2 Optical coherence tomography (4)       6.9.2.1 Anterior (0)       6.9.2.2 Posterior (0)     6.9.5 Other (0)   6.10 Fluorescein (ICG) angiography (0)     6.10.1 Anterior segment (1)     6.10.2 Posterior segment (0)   6.11 Bloodflow measurements (13)   6.12 Ultrasonography and ultrasound biomicroscopy (7)   6.13 Provocative tests (1)   6.19 Telemedicine (0)   6.20 Progression (4)   6.30 Other (0) 8 Refractive errors in relation to glaucoma (0)   8.1 Myopia (3)   8.2 Hypermetropia (0)   8.3 Contact lenses (0)   8.4 Refractive surgical procedures (2)   8.5 Other (0) 9 Clinical forms of glaucomas (0)   9.1 Developmental glaucomas (0)     9.1.1 Congenital glaucoma, Buphthalmos (4)     9.1.2 Juvenile glaucoma (0)     9.1.3 Syndromes of Axenfeld, Rieger, Peters, aniridia (7)     9.1.4 Other (0)   9.2 Primary open angle glaucomas (0)     9.2.1 Ocular hypertension (1)     9.2.2 Other risk factors for glaucoma (7)     9.2.3 Open angle glaucoma with elevated IOP (0)     9.2.4 Normal pressure glaucoma (7)   9.3 Primary angle closure glaucomas (4)     9.3.1 Acute primary angle closure glaucoma (pupillary block) (7)     9.3.2 Chronic primary angle closure glaucoma (pupillary block) (2)     9.3.3 Plateau iris syndrome (1)     9.3.4 Primary angle closure suspect (0)     9.3.5 Primary angle closure (0)     9.3.10 Other (1)   9.4 Glaucomas associated with other ocular and systemic disorders (0)     9.4.1 Steroid-induced glaucoma (1)     9.4.2 Glaucomas associated with disorders of the cornea, conjunctiva, sclera (0)       9.4.2.1 Iridocorneal endothelial syndrome (ICE, incl. irisatrophy) (1)       9.4.2.2 Posterior polymorphous dystrophy (0)       9.4.2.3 Fuchs' endothelial dystrophy (0)       9.4.2.5 Other (0)     9.4.3 Glaucomas associated with disorders of the iris and ciliary body (0)       9.4.3.1 Pigmentary glaucoma (3)       9.4.3.5 Other (1)     9.4.4 Glaucomas associated with disorders of the lens (0)       9.4.4.1 Exfoliation syndrome (6)       9.4.4.2 Glaucomas associated with cataracts (1)       9.4.4.3 Glaucomas associated with lens dislocation (0)       9.4.4.5 Other (1)     9.4.5 Glaucomas associated with disorders of the retina, choroid and vitreous (1)       9.4.5.1 Neovascular glaucoma (4)       9.4.5.5 Other (0)     9.4.6 Glaucomas associated with inflammation, uveitis (4)     9.4.7 Glaucomas associated with ocular trauma (0)     9.4.8 Glaucomas associated with intraocular tumors (0)     9.4.9 Glaucomas associated with elevated episcleral venous pressure (1)       9.4.10 Glaucomas associated with hemorrhage (0)     9.4.11 Glaucomas following intraocular surgery (0)       9.4.11.1 Ciliary block (malignant) glaucoma (0)       9.4.11.2 Glaucomas in aphakia and pseudophakia (0)       9.4.11.3 Epithelial, fibrous, and endothelial proliferation (0)       9.4.11.4 Glaucomas associated with corneal surgery (2)       9.4.11.5 Glaucomas associated with vitreoretinal surgery (1)     9.4.15 Glaucoma in relation to systemic disease (3)     9.4.20 Other (0) 10 Differential diagnosis e.g. anterior and posterior ischemic optic neuropathy (9) 11 Medical treatment (0)   11.1 General management, indication (3)   11.2 Cholinergic drugs (4)   11.3 Adrenergic drugs (0)     11.3.1 Epinephrine (1)     11.3.2 Thymoxamine, dapiprazole (0)     11.3.3 Apraclonidine, brimonidine (9)     11.3.4 Betablocker (9)     11.3.5 Other (0)   11.4 Prostaglandins (24)   11.5 Carbonic anhydrase inhibitors (0)     11.5.1 Systemic (2)     11.5.2 Topical (10)   11.6 Osmotic treatment (0)   11.7 Treatment of bloodflow (3)   11.8 Neuroprotection (8)   11.9 Gene therapy (0)   11.13 Combination therapy (0)     11.13.1 Betablocker and pilocarpine (0)     11.13.2 Betablocker and carbon anhydrase inhibitor (0)     11.13.3 Betablocker and brimonidine (0)     11.13.4 Betablocker and prostaglandin (0)     11.13.5 Other (0)   11.14 Investigational drugs; pharmacological experiments (7)   11.15 Other drugs in relation to glaucoma (3)   11.16 Vehicles, delivery systems, pharmacokinetics, formulation (0)   11.17 Cooperation with medical therapy e.g. persistency, compliance, adherence (0)   11.20 Other (1) 12 Surgical treatment (0)   12.1 General management, indication (6)   12.2 Laser iridotomy (4)   12.3 Laser iridoplasty (2)   12.4 Laser trabeculoplasty and other laser treatment of the angle (5)   12.7 Surgical iridectomy (0)   12.8 Filtering surgery (0)     12.8.1 Without tube implant (8)     12.8.2 With tube implant or other drainage devices (5)     12.8.3 Non-perforating (5)     12.8.4 Using laser (2)     12.8.5 Other (0)     12.8.10 Woundhealing antifibrosis (15)     12.8.11 Complications, endophthalmitis (7)   12.9 Trabeculotomy, goniotomy (3)   12.10 Cyclodestruction (1)   12.11 Cyclodialysis (1)   12.12 Cataract extraction (5)     12.12.1 Intracapsular (0)     12.12.2 Extracapsular (1)     12.12.3 Phacoemulsification (5)   12.14 Combined cataract extraction and glaucoma surgery (1)     12.14.1 Intracapsular (0)     12.14.2 Extracapsular (1)     12.14.3 Phacoemulsification (6)   12.15 Capsulotomy (1)   12.16 Vitrectomy (0)   12.17 Anesthesia (0)   12.20 Other (1) 13 Therapeutic prognosis and outcome (0)   13.1 Prognostic factors (0)   13.2 Outcome (0)     13.2.1 IOP (0)     13.2.2 Visual field (0)       13.2.2.1 Progression (0)       13.2.2.2 Improvement (0)     13.2.3 Other (0) 14 Costing studies; pharmacoeconomics (1) 15 Miscellaneous (4)

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Abstract #6202 Published in IGR 2-2

Pharmacological profiles of the potent carbonic anhydrase inhibitor dorzolamide hydrochloride, a topical antiglaucoma agent

Kobayashi M; Naito K
Nippon yakurigaku zasshi 2000; 115: 323-328

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Carbonic anhydrase (CA) plays an important role in the secretion of aqueous humor. The orally administered CA inhibitor acetazolamide lowers the intraocular pressure (IOP) of patients with glaucoma. However, approximately 50% of patients stop treatment with acetazolamide as a consequence of intolerable side-effects due to the extraocular inhibition of the enzyme. This prompted attempts to develop a topically active CA inhibitor. Merck Research Laboratories focused on developing a water- and solvent-soluble compound to penetrate the cornea. Dorzolamide hydrochloride is a potent inhibitor of human CA isoenzyme II, with an IC value of 0.18 nM in vitro. In contrast, its inhibitory activity against human CA isozyme I is much weaker (IC value of 600 nM). Topically administered dorzolamide penetrated the ciliary body, inhibited its CA actiVity and had a hypotensive effect in rabbits; in contrast, topical administration of acetazolamide or methazolamide did not decrease IOP. In clinical trials, dorzolamide administered three times daily was effective in lowering IOP in patients with open-angle glaucoma or ocular hypertension. The hypotensive effect of dorzolamide 0.5% was similar to that of oral CA inhibitors or timolol (0.25%) twice daily. Dorzolamide did not induce the severe systemic adverse events associated with oral CA inhibitors. Dorzolamide was as effective as pilocarpine or dipivefrine as an adjunctive therapy in patients receiving beta-adrenergic antagonists. Dorzolamide also reduced IOP and accelerated retinal arteriovenous passage time in addition to improving visual function in patients with normal-tension glaucoma. LA: Japanese

Dr. M. Kobayashi, Tsukuba Research Institute, Pharmacology, Banyu Pharmaceutical Co., Ltd., Tsukuba 300-2611, Japan

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Classification:

11.5.2 Topical (Part of: 11 Medical treatment > 11.5 Carbonic anhydrase inhibitors)

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