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PhXA34, a New Potent Ocular Hypotensive Drug: A Study on Dose-Response Relationship and on Aqueous Humor Dynamics in Healthy Volunteers

PhXA34, a New Potent Ocular Hypotensive Drug: A Study on Dose-Response Relationship and on... Abstract • The prostaglandin analogue PhXA34 was tested in two studies in normal human eyes; 1, 3, and 10 μg of PhXA34 reduced the intraocular pressure by about 2, 3, and 4 mm Hg, respectively, 6 to 10 hours after a single topical dose. The only side effect observed was a slight conjunctival hyperemia after 10 μg of PhXA34. In a second study we determined the effect of 10 μg of PhXA34 once daily for 7 days on intraocular pressure, outflow facility, aqueous flow, blood-aqueous barrier permeability, ocular discomfort, and hyperemia. The mean intraocular pressure was below 9 mm Hg 12 hours post dose. About one third of the intraocular pressure reduction could be explained by increased outflow facility. Aqueous flow was unaffected. Treatment caused a 21% increase in aqueous fluorescence 1 hour after an oral dose of fluorescein. Mild ocular discomfort and some hyperemia were initially observed in half of the subjects, but frequency and magnitude of these side effects declined during the study. References 1. Kerstetter JR, Brubaker RF, Wilson SE, Kullerstrand LJ. Prostaglandin F2α-1-isopropylester lowers intraocular pressure without decreasing aqueous humor flow . Am J Ophthalmol . 1988;105:30-34. 2. Villumsen J, Alm A. Prostaglandin F2α-isopropylester eye drops: effects in normal human eyes . Br J Ophthalmol . 1989;73:419-426.Crossref 3. Villumsen J, Alm A, Söderström M. Prostaglandin F2α-isopropylester eye drops . Br J Ophthlalmol . 1989;73:975-979.Crossref 4. Camras CB, Siebold EC, Lustgarten JS, et al. Maintained reduction of intraocular pressure by prostaglandin F2α-1-isopropyl ester applied in multiple doses in ocular hypertensives and glaucoma patients . Ophthalmology . 1989;96:1329-1337.Crossref 5. Villumsen J, Alm A. The effect of adding prostaglandin F2α-isopropylester to timolol in patients with open angle glaucoma . Arch Ophthalmol . 1990;108:1102-1105.Crossref 6. Villumsen J, Alm A. Ocular effects of two different prostaglandin F2α esters: a doublemasked cross-over study on normotensive eyes . Acta Ophthalmol . 1990;68:341-343.Crossref 7. Selén G, Karlsson M, Astin M, Stjernschantz J, Resul B. Effects of PhXA34 and PhDA100A, two phenyl substituted prostaglandin esters, on aqueous humor dynamics and microcirculation in the monkey eye . Invest Ophthalmol Vis Sci . 1991;32( (suppl) ):869. 8. Brubaker RF. Clinical evaluation of the circulation of aqueous humor . In: Duane TD, ed. Clinical Ophthalmology . Philadelphia, Pa: JB Lippincott; 1986;3:1-11. 9. Gibbens MV. The consensual ophthalmotonic reaction . Br J Ophthalmol . 1988;72:746-749.Crossref 10. Crawford C, Kaufman PL. Pilocarpine antagonizes prostaglandin F2α-induced ocular hypotension in monkeys: evidence for enhancement of uveoscleral outflow by prostaglandin F2α . Arch Ophthalmol . 1987;105:1112-1116.Crossref 11. Nilsson SFE, Samuelsson M, Bill A, Stjernschantz J. Increased uveoscleral outflow as a possible mechanism of ocular hypotension caused by prostaglandin F2α-1-isopropylester in the cynomolgus monkey . Exp Eye Res . 1989;48:707-716.Crossref 12. Lütjen-Drecoll E, Tamm E. Morphological study of the anterior segment of cynomolgus monkey eyes following treatment with prostaglandin F2α . Exp Eye Res . 1988;47:761-769.Crossref 13. Camras CB, Bito LZ, Eakins KE. Reduction of intraocular pressure by prostaglandins applied topically to the eyes of conscious rabbits . Invest Ophthalmol Vis Sci . 1977;16:1125-1134. 14. Bito LZ, Draga A, Blanco DJ, Camras CB. Long-term maintenance of reduced intraocular pressure by daily or twice daily topical applications of prostaglandins to cat or rhesus monkey eyes . Invest Ophthalmol Vis Sci . 1983;24:312-319. 15. Stern BA, Bito LZ. Comparison of the hypotensive and other ocular effects of prostaglandins E2α and F2α on cat and rhesus monkey eyes . Invest Ophthalmol Vis Sci . 1982;22:588-598. 16. Camras CB, Podos SM, Rosenthal JS, Lee PY, Severin CH. Multiple dosing of prostaglandin F2α or epinephrine on cynomolgus monkey eyes, II: slit-lamp biomicroscopy, aqueous humor analysis and fluorescein angiography . Invest Ophthalmol Vis Sci . 1987;28:463-469. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Archives of Ophthalmology American Medical Association

PhXA34, a New Potent Ocular Hypotensive Drug: A Study on Dose-Response Relationship and on Aqueous Humor Dynamics in Healthy Volunteers

Archives of Ophthalmology , Volume 109 (11) – Nov 1, 1991

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Publisher
American Medical Association
Copyright
Copyright © 1991 American Medical Association. All Rights Reserved.
ISSN
0003-9950
eISSN
1538-3687
DOI
10.1001/archopht.1991.01080110100045
Publisher site
See Article on Publisher Site

Abstract

Abstract • The prostaglandin analogue PhXA34 was tested in two studies in normal human eyes; 1, 3, and 10 μg of PhXA34 reduced the intraocular pressure by about 2, 3, and 4 mm Hg, respectively, 6 to 10 hours after a single topical dose. The only side effect observed was a slight conjunctival hyperemia after 10 μg of PhXA34. In a second study we determined the effect of 10 μg of PhXA34 once daily for 7 days on intraocular pressure, outflow facility, aqueous flow, blood-aqueous barrier permeability, ocular discomfort, and hyperemia. The mean intraocular pressure was below 9 mm Hg 12 hours post dose. About one third of the intraocular pressure reduction could be explained by increased outflow facility. Aqueous flow was unaffected. Treatment caused a 21% increase in aqueous fluorescence 1 hour after an oral dose of fluorescein. Mild ocular discomfort and some hyperemia were initially observed in half of the subjects, but frequency and magnitude of these side effects declined during the study. References 1. Kerstetter JR, Brubaker RF, Wilson SE, Kullerstrand LJ. Prostaglandin F2α-1-isopropylester lowers intraocular pressure without decreasing aqueous humor flow . Am J Ophthalmol . 1988;105:30-34. 2. Villumsen J, Alm A. Prostaglandin F2α-isopropylester eye drops: effects in normal human eyes . Br J Ophthalmol . 1989;73:419-426.Crossref 3. Villumsen J, Alm A, Söderström M. Prostaglandin F2α-isopropylester eye drops . Br J Ophthlalmol . 1989;73:975-979.Crossref 4. Camras CB, Siebold EC, Lustgarten JS, et al. Maintained reduction of intraocular pressure by prostaglandin F2α-1-isopropyl ester applied in multiple doses in ocular hypertensives and glaucoma patients . Ophthalmology . 1989;96:1329-1337.Crossref 5. Villumsen J, Alm A. The effect of adding prostaglandin F2α-isopropylester to timolol in patients with open angle glaucoma . Arch Ophthalmol . 1990;108:1102-1105.Crossref 6. Villumsen J, Alm A. Ocular effects of two different prostaglandin F2α esters: a doublemasked cross-over study on normotensive eyes . Acta Ophthalmol . 1990;68:341-343.Crossref 7. Selén G, Karlsson M, Astin M, Stjernschantz J, Resul B. Effects of PhXA34 and PhDA100A, two phenyl substituted prostaglandin esters, on aqueous humor dynamics and microcirculation in the monkey eye . Invest Ophthalmol Vis Sci . 1991;32( (suppl) ):869. 8. Brubaker RF. Clinical evaluation of the circulation of aqueous humor . In: Duane TD, ed. Clinical Ophthalmology . Philadelphia, Pa: JB Lippincott; 1986;3:1-11. 9. Gibbens MV. The consensual ophthalmotonic reaction . Br J Ophthalmol . 1988;72:746-749.Crossref 10. Crawford C, Kaufman PL. Pilocarpine antagonizes prostaglandin F2α-induced ocular hypotension in monkeys: evidence for enhancement of uveoscleral outflow by prostaglandin F2α . Arch Ophthalmol . 1987;105:1112-1116.Crossref 11. Nilsson SFE, Samuelsson M, Bill A, Stjernschantz J. Increased uveoscleral outflow as a possible mechanism of ocular hypotension caused by prostaglandin F2α-1-isopropylester in the cynomolgus monkey . Exp Eye Res . 1989;48:707-716.Crossref 12. Lütjen-Drecoll E, Tamm E. Morphological study of the anterior segment of cynomolgus monkey eyes following treatment with prostaglandin F2α . Exp Eye Res . 1988;47:761-769.Crossref 13. Camras CB, Bito LZ, Eakins KE. Reduction of intraocular pressure by prostaglandins applied topically to the eyes of conscious rabbits . Invest Ophthalmol Vis Sci . 1977;16:1125-1134. 14. Bito LZ, Draga A, Blanco DJ, Camras CB. Long-term maintenance of reduced intraocular pressure by daily or twice daily topical applications of prostaglandins to cat or rhesus monkey eyes . Invest Ophthalmol Vis Sci . 1983;24:312-319. 15. Stern BA, Bito LZ. Comparison of the hypotensive and other ocular effects of prostaglandins E2α and F2α on cat and rhesus monkey eyes . Invest Ophthalmol Vis Sci . 1982;22:588-598. 16. Camras CB, Podos SM, Rosenthal JS, Lee PY, Severin CH. Multiple dosing of prostaglandin F2α or epinephrine on cynomolgus monkey eyes, II: slit-lamp biomicroscopy, aqueous humor analysis and fluorescein angiography . Invest Ophthalmol Vis Sci . 1987;28:463-469.

Journal

Archives of OphthalmologyAmerican Medical Association

Published: Nov 1, 1991

References

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