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1 General aspects (0)   1.1 Epidemiology (10)   1.2 Population genetics (7)   1.3 Pathogenesis (3)   1.4 Quality of life (3)   1.5 Glaucomas as cause of blindness (2)   1.6 Prevention and screening (5) 2 Anatomical structures in glaucoma (0)   2.1 Conjunctiva (0)   2.2 Cornea (1)   2.3 Sclera (0)   2.4 Anterior chamber angle (0)   2.5 Meshwork (3)     2.5.1 Trabecular meshwork (10)     2.5.2 Schlemms canal (0)     2.5.3 Scleral outlet channels (0)   2.6 Aqueous humor dynamics (0)     2.6.1 Production (0)     2.6.2 Outflow (1)       2.6.2.1 Trabecular meshwork (1)       2.6.2.2 Uveoscleral (0)     2.6.3 Compostion (3)   2.7 Episcleral veins and venous pressure (1)   2.8 Iris (4)   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 (20)   2.14 Optic disc (18)   2.15 Optic nerve (2)   2.16 Chiasma and retrochiasmal central nervous system (1)   2.17 Stem cells (0)   2.20 Other (0) 3 Laboratory methods (2)   3.1 Microscopy (3)   3.2 Electron microscopy (2)   3.3 Immunohistochemistry (8)   3.4 Molecular genetics (2)     3.4.1 Linkage studies (8)     3.4.2 Gene studies (3)   3.5 Molecular biology incl. SiRNA (9)   3.6 Cellular biology (6)   3.7 Biochemistry (3)   3.8 Pharmacology (5)   3.9 Pathophysiology (2)   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 (0) 5 Experimental glaucoma; animal models (20)   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 (11)     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) (1)   6.3 Biomicroscopy (slitlamp) (0)     6.3.1 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Refractive errors in relation to glaucoma (0)   8.1 Myopia (0)   8.2 Hypermetropia (0)   8.3 Contact lenses (1)   8.4 Refractive surgical procedures (0)   8.5 Other (0) 9 Clinical forms of glaucomas (0)   9.1 Developmental glaucomas (3)     9.1.1 Congenital glaucoma, Buphthalmos (0)     9.1.2 Juvenile glaucoma (0)     9.1.3 Syndromes of Axenfeld, Rieger, Peters, aniridia (4)     9.1.4 Other (0)   9.2 Primary open angle glaucomas (0)     9.2.1 Ocular hypertension (0)     9.2.2 Other risk factors for glaucoma (8)     9.2.3 Open angle glaucoma with elevated IOP (1)     9.2.4 Normal pressure glaucoma (6)   9.3 Primary angle closure glaucomas (1)     9.3.1 Acute primary angle closure glaucoma (pupillary block) (2)     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 (0)     9.4.2 Glaucomas associated with disorders of the cornea, conjunctiva, sclera (0)       9.4.2.1 Iridocorneal endothelial syndrome (ICE, incl. irisatrophy) (0)       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 (1)       9.4.3.1 Pigmentary glaucoma (6)       9.4.3.5 Other (0)     9.4.4 Glaucomas associated with disorders of the lens (0)       9.4.4.1 Exfoliation syndrome (2)       9.4.4.2 Glaucomas associated with cataracts (1)       9.4.4.3 Glaucomas associated with lens dislocation (0)       9.4.4.5 Other (0)     9.4.5 Glaucomas associated with disorders of the retina, choroid and vitreous (0)       9.4.5.1 Neovascular glaucoma (2)       9.4.5.5 Other (0)     9.4.6 Glaucomas associated with inflammation, uveitis (0)     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 (1)       9.4.11.3 Epithelial, fibrous, and endothelial proliferation (0)       9.4.11.4 Glaucomas associated with corneal surgery (3)       9.4.11.5 Glaucomas associated with vitreoretinal surgery (0)     9.4.15 Glaucoma in relation to systemic disease (4)     9.4.20 Other (0) 10 Differential diagnosis e.g. anterior and posterior ischemic optic neuropathy (4) 11 Medical treatment (0)   11.1 General management, indication (8)   11.2 Cholinergic drugs (4)   11.3 Adrenergic drugs (0)     11.3.1 Epinephrine (0)     11.3.2 Thymoxamine, dapiprazole (0)     11.3.3 Apraclonidine, brimonidine (4)     11.3.4 Betablocker (12)     11.3.5 Other (1)   11.4 Prostaglandins (31)   11.5 Carbonic anhydrase inhibitors (0)     11.5.1 Systemic (0)     11.5.2 Topical (7)   11.6 Osmotic treatment (1)   11.7 Treatment of bloodflow (1)   11.8 Neuroprotection (7)   11.9 Gene therapy (2)   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 (0)   11.16 Vehicles, delivery systems, pharmacokinetics, formulation (1)   11.17 Cooperation with medical therapy e.g. persistency, compliance, adherence (0)   11.20 Other (0) 12 Surgical treatment (0)   12.1 General management, indication (5)   12.2 Laser iridotomy (0)   12.3 Laser iridoplasty (0)   12.4 Laser trabeculoplasty and other laser treatment of the angle (1)   12.7 Surgical iridectomy (0)   12.8 Filtering surgery (1)     12.8.1 Without tube implant (4)     12.8.2 With tube implant or other drainage devices (11)     12.8.3 Non-perforating (13)     12.8.4 Using laser (0)     12.8.5 Other (0)     12.8.10 Woundhealing antifibrosis (10)     12.8.11 Complications, endophthalmitis (6)   12.9 Trabeculotomy, goniotomy (1)   12.10 Cyclodestruction (3)   12.11 Cyclodialysis (0)   12.12 Cataract extraction (0)     12.12.1 Intracapsular (0)     12.12.2 Extracapsular (1)     12.12.3 Phacoemulsification (2)   12.14 Combined cataract extraction and glaucoma surgery (0)     12.14.1 Intracapsular (0)     12.14.2 Extracapsular (0)     12.14.3 Phacoemulsification (6)   12.15 Capsulotomy (0)   12.16 Vitrectomy (0)   12.17 Anesthesia (0)   12.20 Other (2) 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 (5) 15 Miscellaneous (2)

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Abstract #8983 Published in IGR 5-2

Pharmacological characterization of a novel antiglaucoma agent, Bimatoprost (AGN 192024)

Woodward DF; Krauss AH; Chen J; Liang Y; Li C; Protzman CE; Bogardus A; Chen R; Kedzie K; Krauss HA
Journal of Pharmacology and Experimental Therapeutics 2003; 305: 772-785

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Replacement of the carboxylic acid group of prostaglandin (PG) F_2ALP with a nonacidic moiety, such as hydroxyl, methoxy, or amido, results in compounds with unique pharmacology. Bimatoprost (AGN 192024) is also a pharmacologically novel PGF_2ALP analogue, where the carboxylic acid is replaced by a neutral ethylamide substituent. Bimatoprost potently contracted the feline lung parenchymal preparation (EC₅₀ value of 35-55 nm), but exhibited no meaningful activity in a variety of PG-sensitive tissue and cell preparations. Its activity seemed unrelated to FP receptor stimulation according to the following evidence: 1. Bimatoprost exhibited no meaningful activity in tissues and cells containing functional FP receptors. 2. Bimatoprost activity in the cat lung parenchyma is not species-specific because its potent activity in this preparation could not be reproduced in cells stably expressing the feline FP receptor. 3. Radioligand binding studies using feline and human recombinant FP receptors exhibited minimal competition versus (³H)17-phenyl PGF_2a for bimatoprost. 4. Bimatoprost pretreatment did not attenuate PGF_2ALP-induced Ca²⁺ signals in Swiss 3T3 cells. 5. Regional differences were apparent for bimatoprost but not FP agonist effects in the cat lung. Bimatoprost reduced intraocular pressure (IOP) in ocular normotensive and hypertensive monkeys over a 0.001-0.1% dose range. A single-dose and multiple-dose ocular distribution/metabolism studies using (³H)bimatoprost (0.1%) were performed. Within the globe, bimatoprost concentrations were ten to 100-fold higher in anterior segment tissues compared with the aqueous humor. Bimatoprost was overwhelmingly the predominant molecular species identified at all time points in ocular tissues, indicating that the intact molecule reduces IOP.

Dr. D.F. Woodward, Department of Biological Sciences, Allergan, Inc., 2525 Dupont Drive, Irvine, CA 92612, USA. woodward_david@allergan.com

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Classification:

11.4 Prostaglandins (Part of: 11 Medical treatment)

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