[Stereospecificity of lowering intraocular pressure using a locally administered carbonic anhydrase inhibitor].
As MK-417, the S-enantiomer of the racemic compound MK-927, is the more active enantiomer in vitro, the potential differential ocular hypotensive activity was investigated in patients. The 1% concentration was chosen as the basis for comparison, as preliminary data indicated that the concentration would fall relatively steeply on the dose-response curve. This was a two-center crossover study of 1% MK-417, 1% MK-927, and placebo (common vehicle) in 27 patients with bilateral, relatively symmetric primary open-angle glaucoma or ocular hypertension. Following a washout period for ocular hypertensive therapy, IOP had to be greater than or equal to 23 mmHg at 10:00 o'clock with IOP difference between eyes less than or equal to 6 mmHg. Treatment days were separated by a 1-2 week washout period. IOP was measured at 9:30. At 10:00 patients received the test drug in one designated eye and placebo in the other eye. IOP was measured at 1, 2, 4, 6, and 8 h after the dose. IOP and the percentage of change in IOP from 30 min before the dose in the active drug-treated eye shows that MK-417 is slightly more potent than MK-927 in this patient model.
Diestelhorst
M
M
Universitäts-Augenklinik, Köln.
Bechetoille
A
A
Lippa
E
E
Brunner-Ferber
F
F
Krieglstein
G K
GK
D000328:Adult; D000368:Aged; D002257:Carbonic Anhydrase Inhibitors / Q000627:therapeutic use*; D005260:Female; D005902:Glaucoma, Open-Angle / Q000188:drug therapy*; D006801:Humans; D007429:Intraocular Pressure / Q000187:drug effects*; D008297:Male; D008875:Middle Aged; D009798:Ocular Hypertension / Q000188:drug therapy*; D009883:Ophthalmic Solutions; D019998:Racemases and Epimerases; D013449:Sulfonamides / Q000008:administration & dosage*; D013876:Thiophenes / Q000008:administration & dosage*
D002257:Carbonic Anhydrase Inhibitors; D009883:Ophthalmic Solutions; D013449:Sulfonamides; D013876:Thiophenes; D019998:Racemases and Epimerases; C057921:sezolamide
Zur Stereospezifität der Augendrucksenkung eines lokal applizierten Karboanhydrasehemmers.