Literature DB >> 3058101

Local tolerance and activity of MK-927, a novel topical carbonic anhydrase inhibitor.

E A Lippa1, H A von Denffer, H M Hofmann, F L Brunner-Ferber.   

Abstract

A three-dose, randomized, double-masked, parallel, placebo-controlled ocular tolerance study was undertaken in 12 healthy, normal volunteers with the water-soluble, topical carbonic anhydrase inhibitor MK-927. To our knowledge, this constitutes the first administration of MK-927 to humans. Ten subjects received three drops of 2% MK-927 ophthalmic solution and two subjects received three drops of placebo (vehicle) in one randomly selected eye. Local tolerance of 2% MK-927 was acceptable and supports further clinical trials in patients. Significant intraocular pressure (IOP)-lowering activity was noted when comparing IOP four hours after first dose with that 20 hours predose in the treated eye of subjects receiving MK-927 (mean percent change in IOP, -29.7%; mean change in IOP, -4.6 mm Hg) as opposed to the same comparison for the contralateral, untreated eye (-7.2% and -1.3 mm Hg, respectively). In the two subjects treated with placebo, IOP-lowering activity was not seen in either the placebo-treated eye (-0.4%) or the contralateral, untreated eye (+3.1%).

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Year:  1988        PMID: 3058101     DOI: 10.1001/archopht.1988.01060140866029

Source DB:  PubMed          Journal:  Arch Ophthalmol        ISSN: 0003-9950


  6 in total

1.  A single dose of the topical carbonic anhydrase inhibitor MK-927 decreases IOP in patients.

Authors:  N Pfeiffer; R Hennekes; E A Lippa; F Grehn; H Garus; F L Brunner-Ferber
Journal:  Br J Ophthalmol       Date:  1990-07       Impact factor: 4.638

2.  L-662,583 is a topically effective ocular hypotensive carbonic anhydrase inhibitor in experimental animals.

Authors:  M F Sugrue; P Gautheron; P Mallorga; T E Nolan; S L Graham; H Schwam; K L Shepard; R L Smith
Journal:  Br J Pharmacol       Date:  1990-01       Impact factor: 8.739

3.  Comparative tolerability of topical carbonic anhydrase inhibitor MK-927 and its S-enantiomer MK-417.

Authors:  N Pfeiffer; J Gerling; E A Lippa; F L Brunner-Ferber; D Panebianco; F Grehn
Journal:  Graefes Arch Clin Exp Ophthalmol       Date:  1991       Impact factor: 3.117

Review 4.  Pharmacological advances in the treatment of glaucoma.

Authors:  J B Serle
Journal:  Drugs Aging       Date:  1994-09       Impact factor: 3.923

5.  Two topical carbonic anhydrase inhibitors sezolamide and dorzolamide in Gelrite vehicle: a multiple-dose efficacy study.

Authors:  F P Gunning; E L Greve; A M Bron; J M Bosc; J G Royer; J L George; P Lesure; D Sirbat
Journal:  Graefes Arch Clin Exp Ophthalmol       Date:  1993-07       Impact factor: 3.117

6.  Topical carbonic anhydrase inhibition increases ocular pulse amplitude in high tension primary open angle glaucoma.

Authors:  K G Schmidt; A von Rückmann; L E Pillunat
Journal:  Br J Ophthalmol       Date:  1998-07       Impact factor: 4.638

  6 in total

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