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Claims for Patent: 4,599,353

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Claims for Patent: 4,599,353

Title: Use of eicosanoids and their derivatives for treatment of ocular hypertension and glaucoma
Abstract:Ocular hypertension and glaucoma can be effectively controlled in primates through topical application of an effective amount of an eicosanoid or an eicosanoid derivative to the surface of an afflicted eye. Eicosanoids, particularly the prostaglandins PGE.sub.2 and PGF.sub.2.alpha., and derivatives thereof, have been found effective in quantities less than about 1000 .mu.g per eye. Ophthalmic compositions containing C.sub.1 to C.sub.5 alkyl esters of PGF.sub.2.alpha. are presently preferred for use in treating ocular hypertension and glaucoma in primates, including man.
Inventor(s): Bito; Laszlo Z. (New York, NY)
Assignee: The Trustees of Columbia University in the City of New York (New York, NY)
Application Number:06/374,165
Patent Claims: 1. A method for treating hypertension or glaucoma in a primate subject's eye comprising periodically contacting the surface of the eye with an amount of an eicosanoid or an eicosanoid derivative effective to reduce intraocular pressure in the eye without any substantial initial increase in said pressure and to maintain reduced intraocular pressure.

2. The method of claim 1 wherein the surface of the eye is contacted daily.

3. The method of claim 1 wherein the eicosanoid or eicosanoid derivative is a prostaglandin or a prostaglandin derivative.

4. The method of claim 3 wherein the prostaglandin or prostaglandin derivative is PGE.sub.2 or a PGE.sub.2 derivative.

5. The method of claim 3 wherein the prostaglandin or prostaglandin derivative is PGF.sub.2.alpha. or a PGF.sub.2.alpha. derivative.

6. The method of claim 5 wherein the PGF.sub.2.alpha. derivative is a C.sub.1 to C.sub.5 alkyl ester of PGF.sub.2.alpha..

7. The method of claim 6 wherein the PGF.sub.2.alpha. derivative is PGF.sub.2.alpha. methyl ester, PGF.sub.2.alpha. ethyl ester, PGF.sub.2.alpha. isopropyl ester, or PGF.sub.2.alpha. isobutyl ester.

8. The method of claim 5 wherein the PGF.sub.2.alpha. or PGF.sub.2.alpha. derivative is lipid soluble.

9. The method of claim 5 wherein the PGF.sub.2.alpha. or PGF.sub.2.alpha. derivative is in the form of a physiologically acceptable salt of PGF.sub.2.alpha..

10. The method of claim 9 wherein the PGF.sub.2.alpha. salt is PGF.sub.2.alpha. tromethamine.

11. The method of claim 3 wherein the amount of prostaglandin or prostaglandin derivative is in the range from about 0.01 .mu.g to about 1,000 .mu.g.

12. The method of claim 11 wherein the amount of prostaglandin or prostaglandin derivative is in the range from about 0.1 .mu.g to about 500 .mu.g.

13. A composition for topical treatment of glaucoma in the eye of a primate subject comprising an effective amount of PGF.sub.2.alpha. methyl ester, PGF.sub.2.alpha. ethyl ester, PGF.sub.2.alpha. isopropyl ester, or PGF.sub.2.alpha. isobutyl ester dissolved in an ophthalmically compatible carrier.

14. A composition for the topical treatment of glaucoma in a primate subject's eye comprising an effective amount of a lower alkyl ester of PGF.sub.2.alpha. dissolved in an ophthalmically compatible carrier.

15. A method for topically treating glaucoma in a primate subject's eye comprising contacting daily the surface of the eye with about 50 .mu.l of a composition of claim 14 which is a lower alkyl ester of PGF.sub.2.alpha..

16. A composition of claim 14, wherein the lower alkyl ester is C.sub.1 to C.sub.5.

17. A composition of claim 14, wherein the carrier is sterile anhydrous peanut oil.

18. A composition of claim 14, wherein the carrier is sterile mineral oil.

19. A composition of claim 14, wherein the effective amount is from about 0.01% to about 1.0% by weight.
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