Latanoprost treatment for glaucoma: effects of treating for 1 year and of switching from timolol

Camras, Carl B.; Wax, Martin B.; Ritch, Robert; Weinreb, Robert N.; Robin, Alan L.; Higginbotham, Eve J.; Lustgarten, Jacqueline S.; Stewart, William C.; Sherwood, Mark B.; Krupin, Theodore; Wilensky, Jacob T.; Cioffi, George A.; Katz, L. Jay; Schumer, Robert A.; Kaufman, Paul L.; Minckler, Don S.; Zimmerman, Thom J.; Stjernschantz, Johan

doi:10.1016/s0002-9394(98)00094-4

Cited by 61 publications

(26 citation statements)

References 30 publications

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“…PGF 2a -derivative ophthalmic solutions, including latanoprost solution, have been reported to cause an iris colour change and dark skin around the eye as side effects. [11][12][13][14][15][16][17][18][19][20] In cultured melanoma cells, a carboxylic acid of latanoprost has been reported to increase melanogenesis 31) and the results obtained in the present study confirm this report. However, the stimulatory effects on melanin content in cultured B16-F10 melanoma cells in our experiment did not correlate with the prostanoid FP-receptor agonistic activities of the 15,15-difluoro derivatives.…”

Section: Discussionsupporting

confidence: 90%

“…9,10) In addition, long-term application of PGF 2a derivatives causes chronic adverse effects, such as iris/skin pigmentation, eyelash growth, and so on. [10][11][12][13][14][15][16][17][18][19] The PGF 2a -derivative-induced eye colour change is most likely due to an increased amount of melanin within iris stroma melanocytes. [20][21][22] These adverse effects may be related to the stimulation of prostanoid FP receptors in the eye.…”

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confidence: 99%

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New Fluoroprostaglandin F2.ALPHA. Derivatives with Prostanoid FP-Receptor Agonistic Activity as Potent Ocular-Hypotensive Agents

Nakajima

Matsugi

Goto

et al. 2003

Biological & Pharmaceutical Bulletin

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An elevated intraocular pressure (IOP) is one of the risk factors for the development of glaucoma. Recent prospective epidermal studies in the United States indicate that if IOP is lowered below 12 mmHg, 1) or by more than 30% from the baseline IOP in patients with normal-tension glaucoma, 2) the progress of the visual field defect can be delayed. Prostaglandin (PG) derivatives exert ocular-hypotensive effects through stimulation of prostanoid receptors (FP, DP, IP etc.) and possibly by activation of signal-transduction systems such as intracellular Ca 2ϩ and cyclic AMP. [3][4][5][6] One of the most potent PGF 2a derivatives at reducing IOP is latanoprost, a selective prostanoid FP-receptor agonist, and this drug has been successfully developed as an anti-glaucoma agent. 7) Recently, another selective prostanoid FP-receptor agonist, travoprost, was launched in the United States and other countries.8) Because of their potent, long-lasting ocular-hypotensive effects, prostanoid FP-receptor agonists are widely used for the treatment of glaucoma.However, clinical use over several years has revealed the existence of patients who do not respond well to PGF 2a derivatives. 9,10) In addition, long-term application of PGF 2a derivatives causes chronic adverse effects, such as iris/skin pigmentation, eyelash growth, and so on. [10][11][12][13][14][15][16][17][18][19] The PGF 2a -derivative-induced eye colour change is most likely due to an increased amount of melanin within iris stroma melanocytes. [20][21][22] These adverse effects may be related to the stimulation of prostanoid FP receptors in the eye. 3)To judge from the accumulating findings relating to latanoprost and other PGF 2a derivatives, prostanoid FP-receptor agonists are among the most promising ocular-hypotensive agents. To try to find prostanoid FP-receptor agonists that might be more potent at inducing an IOP reduction while causing fewer or weaker side effects than latanoprost, we synthesized new PGF 2a derivatives and evaluated their prostanoid FP-receptor-mediated activities both in vitro and in vivo. We report here some interesting new compounds with fluorine(s) in the 15-position of the PGF 2a -derivative structure. MATERIALS AND METHODS Materials Prostarumon® F injection 1000 (1 mg/ml PGF 2a ) was obtained from Ono Pharmaceutical Co., Ltd. (Osaka, Japan), while cloprostenol was from Cayman Chemical Co. (Ann Arbor, MI, U.S.A.). Latanoprost free acid, latanoprost, and free acid and ester forms of various PGF 2a derivatives (Table 1) Constriction of the Isolated Iris Sphincter in CatsA functional prostanoid FP-receptor-affinity assay was performed using iris sphincter muscles isolated from cat eyes. 23)This tissue expresses predominantly prostanoid FP receptors. 24,25) Male European cats (Charles River Japan, Kanagawa, Japan) weighing from 2.5 to 5.0 kg were sacrificed by injection of intravenous sodium pentobarbital (Dainippon Pharmaceutical Co., Ltd., Osaka, Japan). The eyes were immediately enucleated and placed into modified Krebs-Henseleit sol...

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Section: Discussionsupporting

confidence: 90%

mentioning

confidence: 99%

New Fluoroprostaglandin F2.ALPHA. Derivatives with Prostanoid FP-Receptor Agonistic Activity as Potent Ocular-Hypotensive Agents

Nakajima

Matsugi

Goto

et al. 2003

Biological & Pharmaceutical Bulletin

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“…In smooth muscle, PGF 2a and CCh promote changes in contractility, and in addition PGF 2a functions as smooth muscle mitogen. In the eye, PGF 2a and its analog PhXA41 (latanoprost) mediate, through PGF 2a receptors, a broad range of biological effects including smooth muscle contraction (Abdel-Latif, 1995) and reduction of IOP in glaucoma patients (Bito and Stjernschantz, 1989;Camras et al, 1998). While the hypotensive effects of PGF 2a and latanoprost are mediated through an increase in uveoscleral out¯ow of aqueous humor (Crawford and Kaufman, 1987;Stjernschantz et al, 1995), the molecular mechanism underlying this effect is not known.…”

Section: Discussionmentioning

confidence: 99%

“…The physiological and pathophysiological functions of PGs in the eye are of great interest in ophthalmology because AA metabolites have been implicated in a number of ocular disorders including uveitis, surgical trauma, cystoid macular edema, transient monocular blindness, retrolental ®broplasia and diabetic retinopathy (for reviews, see Bito and Stjernschantz, 1989). In addition, certain PGs, such as the PGF 2a analog latanoprost, are routinely employed to lower intraocular pressure (IOP) in glaucoma patients (for a recent review see Camras et al, 1998). While there is mounting experimental evidence which indicates that the IOP-lowering effects of PGF 2a and its analog latanoprost occurs through an increased uveoscleral out¯ow of aqueous humor the molecular mechanisms underlying these effects remain to be determined.…”

Section: Introductionmentioning

confidence: 99%

Effects of Prostaglandin F2αand Carbachol on MAP Kinases, Cytosolic Phospholipase A2and Arachidonic Acid Release in Cat Iris Sphincter Smooth Muscle Cells

Husain

Abdel‐Latif

2001

Experimental Eye Research

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“…Copyright © 2003 S. Karger AG, Basel Latanoprost (LP), a prostaglandin (PG) F 2· analogue, has a strong intraocular pressure-lowering effect and has become an important drug in the treatment of glaucoma. A number of clinical trials have shown the efficacy and safety of the drug [1][2][3][4][5]. However, recently there have been a number of reports about the development of cystoid macular edema (CME) associated with LP use [6][7][8][9][10][11][12][13].…”

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confidence: 99%

Effects of Latanoprost on Blood-Retinal Barrier Permeability in Rabbits

et al. 2003

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Purpose: To investigate the effect of latanoprost (LP) on the inward and outward permeability (P_in and P_out) of the blood-retinal barrier (BRB). Methods: Four New Zealand white rabbits received topical LP (0.005%) once daily for 3 weeks in one eye and phosphate-buffered saline (PBS) in the fellow eye (topical group). Five New Zealand white rabbits were injected intravitreously with LP (0.1 ml, 0.005%) in one eye and PBS (0.1 ml) in the fellow eye (injection group). In the injection group, vitreous fluorophotometry (VFP) to estimate the P_in and differential vitreous fluorophotometry (DVF) to estimate the P_out were performed 60 min after LP was injected. After the baseline measurements, VFP and DVF were performed 60 and 180 min after intravenous injection of sodium fluorescein, respectively. Fluorescein (F) and fluorescein monoglucuronide (FG) concentrations were obtained by DVF, and the F/FG ratio was calculated as an index of the P_out. Results: In the topical group, there were no significant differences in the P_in or F/FG ratio between the LP- and the PBS-treated eyes. In the injection group, the P_in in the LP-treated eyes was significantly higher than in PBS-treated eyes (p < 0.05). There was no significant difference in the F/FG ratio between the two groups. Conclusion: Although we cannot exclude the effect of differences in species, the physiologic effect of LP, which increased the P_in, was seen in experimental studies. Because antiglaucoma drugs are generally used over an extended period, further clinical studies of the effect of LP on the BRB should be performed in patients who have BRB breakdown, such as in uveitis, and in patients who are pseudophakic and aphakic.

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Latanoprost treatment for glaucoma: effects of treating for 1 year and of switching from timolol

Abstract: Latanoprost is a well-tolerated ocular hypotensive agent that appears to be more effective than timolol in reducing intraocular pressure. The increase in iris pigmentation appears to be harmless but requires further investigation.

Cited by 61 publications

References 30 publications

New Fluoroprostaglandin F2.ALPHA. Derivatives with Prostanoid FP-Receptor Agonistic Activity as Potent Ocular-Hypotensive Agents

New Fluoroprostaglandin F2.ALPHA. Derivatives with Prostanoid FP-Receptor Agonistic Activity as Potent Ocular-Hypotensive Agents

Effects of Prostaglandin F2αand Carbachol on MAP Kinases, Cytosolic Phospholipase A2and Arachidonic Acid Release in Cat Iris Sphincter Smooth Muscle Cells

Effects of Latanoprost on Blood-Retinal Barrier Permeability in Rabbits

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