uf-021 and Glaucoma

In the first part of the article the main information and recent research on the uveoscleral outflow pathway, including its morphology and physiology were presented. The structure of extracellular matrix of ciliary muscle and the changes of it, that are induced by prostaglandins, resulting in decreasing intraocular pressure were emphasized. In the second part biochemical characteristics of prostaglandin analogues, using nowadays were presented. Their efficacy in reducing intraocular pressure and safety profile were described.

Topics: Amides; Bimatoprost; Cloprostenol; Dinoprost; Glaucoma; Humans; Intraocular Pressure; Latanoprost; Lipids; Prostaglandins F; Prostaglandins F, Synthetic; Receptors, Prostaglandin; Travoprost; Treatment Outcome

Latanoprost, a prostaglandin F(2alpha) analog prodrug, and unoprostone, an analog of a prostaglandin metabolite, have been shown to be effective in decreasing intraocular pressure when used alone or in combination with other ocular hypotensive agents. The increase in the uveoscleral outflow and some of the side effects are probably FP-receptor mediated, which may account for some differences between the cited drugs. This article reviews the recent literature available on the clinical efficacy of these prostanoids, as well as the studies directly comparing these drugs.

Topics: Antihypertensive Agents; Dinoprost; Drug Therapy, Combination; Glaucoma; Humans; Intraocular Pressure; Latanoprost; Ocular Hypertension; Ophthalmic Solutions; Prostaglandins F, Synthetic

The characteristic loss of visual field due to glaucoma is directly associated with retinal ganglion cell (RGC) death. The process of RGC death is thought to be biphasic, starting with a primary injury, followed by a slow secondary degeneration. Retinal ischemia may establish the cellular conditions that create a fatal biochemical cascade; hypoxia, followed by high excitotoxic levels of glutamate cause pathologically elevated levels of intracellular calcium resulting in neuronal cell death via apoptosis or necrosis. Impaired ocular perfusion, primarily due to abnormal autoregulation and/or vasoconstriction caused by endothelin-1, probably contributes to the ischemic milieu. Neuroprotection, the preservation of neurons that were either not damaged or only slightly damaged during the primary insult, has become important for the clinician when considering treatment options. Unoprostone, the first synthetic docosanoid, has been demonstrated to exhibit neuroprotective properties. In an ischemic animal model, unoprostone protected RGCs in a dose-dependent manner. Unoprostone inhibits glutamate stimulation and opens maxi-K channels, which are potassium channels that reach an activation threshold only during depolarization and/or at high intracellular Ca2+ concentrations. The resultant large efflux of K+ hyperpolarizes the cell, thereby closing voltage-gated Ca2+ channels and limiting neuronal damage by decreasing influx of intracellular Ca2+. Unoprostone has also been shown to protect rat photoreceptors from constant light-induced damage. Lastly, unoprostone has vasorelaxant properties, evidenced by increased choroidal blood flow and inhibition of vasoconstrictors such as endothelin-1. These findings indicate that a substantial clinical benefit of unoprostone is neuroprotection of RGCs.

Topics: Animals; Dinoprost; Glaucoma; Humans; Neuroprotective Agents; Rats; Retina

Despite treatment, glaucoma patients may still suffer vision loss because of inadequate control of intraocular pressure or late presentation. This article reviews the latest evidence supporting a reappraisal of first-line treatment in the management of glaucoma, including a review of latanoprost, recently approved for first-line treatment of glaucoma and ocular hypertension.

Topics: Amides; Antihypertensive Agents; Bimatoprost; Brimonidine Tartrate; Cloprostenol; Dinoprost; Drug Therapy, Combination; Glaucoma; Humans; Latanoprost; Lipids; Prostaglandins; Prostaglandins F, Synthetic; Quinoxalines; Sulfonamides; Thiophenes; Travoprost

The prostaglandin analogs are new exciting drugs added to the therapeutic armamentarium for patients with glaucoma. Several studies have evaluated the ocular hypotensive properties and side effects of latanoprost in different forms of glaucoma. This drug, seems to be the most effective intraocular pressure (IOP)-reducing agent currently available, and has a low incidence of ocular and systemic side effects. Fewer data are available regarding unoprostone, but the IOP-reducing effect of this drug seems to be comparable or slightly inferior to that of timolol and it produces fewer side effects. When compared with unoprostone, latanoprost has been shown to effect a greater reduction in IOP. A major drawback to the use of prostaglandin analogues is the lack of long-term experience such as that currently available for other classes of agents.

Topics: Antihypertensive Agents; Dinoprost; Glaucoma; Humans; Intraocular Pressure; Latanoprost; Ophthalmic Solutions; Prognosis; Prostaglandins; Prostaglandins F, Synthetic; Randomized Controlled Trials as Topic

This paper presents the classification of prostaglandins and their receptors. The ocular distribution of the receptors and the effects of their agonists are presented. The efficacy in lowering intraocular pressure of different prostaglandins and their derivatives, especially the PGF2a group, is discussed. The history of latanoprost development is also presented. Good therapeutic index characterises two antiglaucomatous PG-derivatives: latanoprost and unoprostone.

Topics: Animals; Blood-Aqueous Barrier; Dinoprost; Glaucoma; Humans; Intraocular Pressure; Latanoprost; Prostaglandins; Prostaglandins F, Synthetic

Prostaglandin (PG) analogues are a new class of ocular hypotensive drugs that have been developed for the treatment of open angle glaucoma. Two of these drugs, latanoprost and unoprostone, are presently commercially available. Latanoprost was introduced in 1996 in the US and Europe. Presently it enjoys the most widespread use and is the most well documented drug of this group. It reduces the intraocular pressure (IOP) by a mechanism of action different from other drugs; namely by increasing the uveoscleral outflow. The aqueous inflow is not affected. The optimal dose regimen is one drop of 50 microg/ml once daily, which reduces the IOP by approximately 30% in patients with glaucoma. A more pronounced ocular hypotensive effect is demonstrated when latanoprost is combined with other glaucoma therapies, including beta-blockers, adrenergic and cholinergic agonists or carbonic anhydrase inhibitors. Latanoprost is well tolerated. The drug reaches a plasma concentration below that needed for stimulation of the FP-receptor, which may explain its favourable systemic tolerability profile. The major ocular adverse effect is increased iris pigmentation, which is due to increased synthesis of melanin in the melanocytes of the iris stroma. It is most frequently seen in green-brown eyes and it is probably permanent. A low frequency of cystoid macular oedema has also been reported, predominantly in predisposed eyes. Unoprostone was launched in Japan in 1994, but there is little experience with this drug outside the Japanese market and the documentation is more limited. Its main mechanism of action is on outflow, but this is not yet fully elucidated. The recommended dosage regimen is 1 drop of 1.2 mg/ml twice daily. No comparative studies in humans between the 2 drugs have yet been published.

Topics: Animals; Dinoprost; Forecasting; Glaucoma; Humans; Latanoprost; Polypharmacy; Prostaglandins F, Synthetic; Prostaglandins, Synthetic

Prostaglandin (PG) analogs are some of the most recent additions to the list of ocular hypotensive medications. Two analogs of naturally occurring PGs are available commercially, isopropyl unoprostone (Rescula [Ciba Vision, Atlanta, GA]) and latanoprost (Xalatan [Pharmacia & Upjohn, Bridgewater, NJ]). Presently, latanoprost 0. 005% is the only PG analog commercially available in the United States. These agents have been shown to be the most effective topical medications for reducing intraocular pressure. They have a different mechanism of action than other ocular hypotensives, and act primarily by increasing uveoscleral outflow. Because of this, PGs have a substantial additive effect when used with agents that reduce aqueous production (eg, beta blockers or carbonic anhydrase inhibitors) or that increase trabecular outflow facility (eg, pilocarpine). Local side effects include mild conjunctival hyperemia and local irritation, darkening of iris color, increased growth of eyelashes, and a possible association with cystoid macular edema or iritis in some patients with other risk factors. No systemic side effects have been proven to be caused by latanoprost. Recommended dosing is once daily at bedtime.

Topics: Animals; Antihypertensive Agents; Aqueous Humor; Dinoprost; Glaucoma; Humans; Intraocular Pressure; Latanoprost; Molecular Structure; Ophthalmic Solutions; Prostaglandins F, Synthetic

Low doses of naturally occurring prostaglandins reduce the intraocular pressure (IOP) in many species. Species differences do occur both in terms of efficiency and mechanism of action, and also among the different prostaglandins. Among the prostaglandins mainly PGF2 alpha has been tested in human eyes. Although it is an effective ocular hypotensive drug it is not clinically useful due to pronounced ocular side-effects, mainly conjunctival hyperemia and irritation, at doses that produce a maximal effect on IOP. Modification of the drug has resulted in two analogues that are now in clinical use, latanoprost and unoprostone. In long-term studies latanoprost, when applied as a once-daily dose of a 0.005% concentration, reduces IOP at least as effectively as adrenergic beta-receptor blockers. The reduction of IOP is due to increased outflow. This takes place mainly, or exclusively, through the uveoscleral routes, thus introducing a new pharmacological principle for the treatment of glaucoma. The drug reaches systemic concentrations that are below the level expected to stimulate FP-receptors outside the eye and it is rapidly eliminated with a half-life in plasma of 17 minutes, which explains why the clinical trials have not revealed any systemic side-effects with latanoprost. The most frequent side-effect observed with latanoprost is an increased pigmentation of the iris mainly in eyes with irides that are already partly brown. This effect is seen with several naturally occurring prostaglandins and is due to stimulation of melanin production in the melanocytes of the iridial stroma. No structural changes of the melanocytes have been observed in studies performed both in vivo and in vitro. The mechanism of action for unoprostone is the same as for latanoprost. No effect on iris colour has been reported for unoprostone but so far there is limited experience with the drug in eyes with a mixed iris colour.

Topics: Adrenergic Agonists; Adrenergic beta-Antagonists; Animals; Carbonic Anhydrase Inhibitors; Cholinergic Agonists; Dinoprost; Drug Therapy, Combination; Glaucoma; Humans; Intraocular Pressure; Latanoprost; Ocular Hypotension; Prostaglandins; Prostaglandins F, Synthetic

Topics: Animals; Clinical Trials as Topic; Dinoprost; Dose-Response Relationship, Drug; Drug Administration Schedule; Glaucoma; Humans; Intraocular Pressure; Latanoprost; Prostaglandins F, Synthetic; Structure-Activity Relationship

Recently, an epidemiological study was conducted in Japan by Shiose, et al, and the prevalence of open-angle glaucoma in Japanese aged 40 years or older was found to be 2.62% [primary open-angle glaucoma 0.58%, low-tension glaucoma (LTG) 2.04%]. Historically, treatment for glaucoma has been based on lowering intraocular pressure. It is also necessary to improve intraocular blood flow. In the beginning of the study, the effect of anti-glaucoma agents on choroidal blood flow was examined in rabbit eyes. An increase of choroidal blood flow was found following topical application of the prostaglandin-related compound isopropyl unoprostone (UF-021) and the adrenergic alpha-1 antagonist bunazosin hydrochloride (DE-070). Then, a new vasoconstrictor, endothelin, showed strong effects on intraocular pressure, intraocular circulation, and visual function in rabbit eyes. Endothelin-1 (ET-1) was found to be a marked vasoconstrictor with prolonged reduction of intraocular pressure and the blood flow in the choroid and optic nerve head. The effects were suppressed by Ca2+ channel blocker and adrenergic alpha-1 blocker. Plasma concentration of ET-1 was determined by radioimmunoassay in patients with glaucoma. A significantly high level of ET-1 concentration was seen in patients with LTG. Endothelin appears to be an important tool for studying the pathogenesis of LTG. Finally, a prospective clinical trial of the therapeutic effects of bunazosin hydrochloride was performed in patients with LTG for one year. Clinical usefulness was evaluated by changes in the mean deviation value of Humphrey perimetry. Satisfactory results were obtained in maintaining the visual field and in reducing intraocular pressure. In the light of our investigations, it is advisable to introduce an adrenergic alpha-1 blocker or prostaglandin-related compound for reduction of glaucomatous damages. We look forward to the development of the neuro-protective future glaucoma therapy.

Topics: Adrenergic alpha-Antagonists; Choroid; Dinoprost; Endothelins; Glaucoma; Humans; Intraocular Pressure; Ophthalmic Solutions; Quinazolines; Regional Blood Flow

To evaluate the effect of substituting latanoprost(LAT) 0.005% for unoprostone(UNO) 0.12% after a trial of unilateral treatment.. We treated 30 patients with primary open-angle glaucoma(n = 8), ocular hypertension (n = 1), or normal-tension glaucoma(n = 21) with UNO for 4 weeks in one eye and then substituted LAT for UNO. Four weeks later we measured the intraocular pressure(IOP) in the ipsilateral eye.. The mean baseline IOP level was 18.6 +/- 3.8(mean +/- standard deviation) mmHg. The mean IOP levels(reduction rates) after UNO and LAT therapy were 16.7 +/- 3.1 mmHg (16.6%) and 14.1 +/- 3.2 mmHg (28.9%), respectively(p < 0.001). All patients who responded to UNO also responded to LAT; however, 55% of those who did not respond to UNO responded to LAT.. If LAT is substituted for UNO, it can be predicted that 63.3% of the patients will respond.

Topics: Adult; Aged; Antihypertensive Agents; Dinoprost; Drug Therapy, Combination; Female; Glaucoma; Glaucoma, Open-Angle; Humans; Intraocular Pressure; Latanoprost; Male; Middle Aged; Ocular Hypertension; Ophthalmic Solutions; Prospective Studies; Prostaglandins F, Synthetic; Treatment Outcome

To compare incidence of iridial pigmentation prospectively induced by long term treatment with latanoprost and isopropyl unoprostone (hereafter, unoprostone) in Japanese patients with glaucoma.. Patients with glaucoma treated with prostaglandin (PG) related ophthalmic solutions were sequentially enrolled. Patients treated for more than 30 months with PG related ophthalmic solutions were subjected to analysis. The entry criteria were no history of intraocular surgery, laser iridotomy, and/or laser trabeculoplasty within 12 months before and after the enrolment; and no history of uveitis; no changes in antiglaucoma drugs within 6 months before and after the enrolment. Photographs of the irides were taken under the same conditions and three glaucoma specialists evaluated the iridial pigmentation with masking of patient information. The correlation of iridial pigmentation with the background factors and the reduction of intraocular pressure (IOP) before and after the treatment were investigated.. 48 eyes in 48 patients satisfied the enrolment criteria (25 eyes in the latanoprost group, 23 eyes in the unoprostone group). At the end of the follow up period, iridial pigmentation was present in 15 patients (60.0%) in the latanoprost group and seven patients (30.4%) in the unoprostone group. The correlation between development of iridial pigmentation and age, sex, concurrent use of other ophthalmic solutions, and IOP reduction was not significant.. The incidence of iridial pigmentation induced by latanoprost or unoprostone is high in the case of long term treatment. Iridial pigmentation did not affect PG related ophthalmic solution induced IOP reduction.

Topics: Adult; Aged; Aged, 80 and over; Antihypertensive Agents; Dinoprost; Eye Color; Female; Follow-Up Studies; Glaucoma; Humans; Iris Diseases; Latanoprost; Male; Middle Aged; Ophthalmic Solutions; Pigmentation Disorders; Prospective Studies; Prostaglandins F, Synthetic; Risk Factors

We administered UF-021 isopropyl unoprostone (Rescula) ophthalmic solution, a new prostaglandin-related compound developed as an anti-glaucoma agent, to 13 low tension glaucoma patients for 24 weeks, and clinically evaluated the effect of the intraocular pressure (IOP) reduction, visual field change, and side effects of the agent. Intraocular pressure was reduced in 11 out of 12 patients who were studied for statistical analysis. In these 12 patients, significant IOP reduction was recognized in the mean IOP for 24 weeks after the administration of UF-021. No side effects were detected in any of the 13 patients. From these results, UF-021 could be used as a new anti-glaucoma agent for low tension glaucoma, and also safer than many other anti-glaucoma agents.

Topics: Adult; Aged; Dinoprost; Female; Glaucoma; Humans; Intraocular Pressure; Male; Middle Aged; Ophthalmic Solutions

UF-021 ophthalmic solution, a novel prostaglandin-related therapeutic agent for glaucoma, was additionally applied to the eyes in intractable cases of primary open angle glaucoma (14 cases, 21 eyes) and ocular hypertension (1 case, 2 eyes) in which intraocular pressure (IOP) had not been kept under satisfactory control even with combined drug therapy by conventional, existing anti-glaucoma agents including sympathetic beta-blockers. Decrease of IOP by UF-021 ophthalmic solution (0.12%) in the treated eyes was observed from not less than one month after the initial application by 3 mmHg and more in about 85%, and by 5 mmHg and more in about 76% of the enrolled patients, respectively. The IOP reduction induced by the additional application of UF-021 was sustained for more than 6 months, resulting in successful avoidance of surgical operations in many patients. When UF-021 ophthalmic solution was applied concurrently with various anti-glaucoma agents including carbonic anhydrase inhibitors, it caused no controversial side-effects and yielded therapeutic efficacy for a prolonged period. These findings suggest that UF-021 can yield IOP-reducing activity through a novel pharmacological mechanism different from other existing drugs. In conclusion, UF-021 ophthalmic solution is extremely useful for the treatment of glaucoma.

Topics: Dinoprost; Female; Glaucoma; Glaucoma, Open-Angle; Humans; Intraocular Pressure; Male; Ophthalmic Solutions

The purpose of this study was to evaluate both the intraocular pressure (IOP)-decreasing and neuroprotective effects of Rescula (0.12% unoprostone isopropyl) as an alternative therapy to betablockers with a long-term drift effect in patients with glaucoma. Twenty-eight patients with unilateral or bilateral glaucoma were treated with Rescula instead of the original beta-blocker therapy. IOP was measured using a Goldmann applanation tonometer, and visual field defects were evaluated quantitatively by Humphrey automatic perimetry central 30-2 threshold test. The mean follow-up time was at least 1 year. Rescula achieved a significant (p = 0.00001) and long-lasting reduction in IOP (from 20.78 +/- 2.71 to 17.14 +/- 2.70 mmHg) in patients with open-angle glaucoma after 12 months of follow-up. It also demonstrated a significant (p = 0.02) IOP-reducing effect (from 20.67 +/- 3.60 to 16.36 +/- 3.67 mmHg) in patients with angle-closure glaucoma 12 months later. The mean deviation of visual field defects changed from -13.27 dB baseline to -10.64 dB at 12 months as evaluated by Humphrey field analyzer II central 30-2 threshold test after Rescula; however, there was no statistical difference (p = 0.098). Our results showed that Rescula has a significant IOP-reducing effect as an alternative therapy to beta-blockers with long-term drift effect in patients with open-angle and angle-closure glaucoma. However, a neuroprotective effect to prevent further progression of the visual field defect in patients with glaucoma was not demonstrated in this study.

Topics: Adrenergic beta-Antagonists; Adult; Aged; Antihypertensive Agents; Dinoprost; Female; Glaucoma; Humans; Intraocular Pressure; Male; Middle Aged; Neuroprotective Agents; Prospective Studies; Visual Fields

We retrospectively investigated the long-term effects of isopropyl unoprostone monotherapy on intraocular pressure and visual field for normal-tension glaucoma and primary open-angle glaucoma patients. Among 80 eyes of 49 subjects receiving isopropyl unoprostone monotherapy for 2 years or more, 32 eyes of 32 subjects were analyzed because of the good reliability of their visual acuity and visual field (age, 68.1 +/- 10.1 yrs, follow-up period 47.8 +/- 14.7 months). The mean values of intraocular pressure and visual field indices were compared with baseline data before medication. The visual field changes were also analyzed using the Kaplan-Meier life-table method. The mean intraocular pressure decreased for 4 years from 14.7 +/- 4.3 mmHg (mean +/- SD) at baseline, to 12.7 +/- 4.4mmHg at 4 years. The global index of visual field (mean defect, loss variance) did not change significantly during the 4 years. The accumulative probability of survival was 80.7 +/- 8.0% after 4 years when the endpoint was defined as 3dB progression in mean defect. Isopropyl unoprostone might have the possibility of stabilizing the visual field for a long period of time.

Topics: Aged; Dinoprost; Female; Glaucoma; Glaucoma, Open-Angle; Humans; Intraocular Pressure; Male; Retrospective Studies; Visual Fields

Topics: Amides; Antihypertensive Agents; Bimatoprost; Cloprostenol; Dinoprost; Evidence-Based Medicine; Fluorescein Angiography; Glaucoma; Humans; Latanoprost; Lipids; Prostaglandins F, Synthetic; Trabeculectomy; Travoprost

Topics: Amides; Bimatoprost; Cloprostenol; Dinoprost; Glaucoma; Humans; Intraocular Pressure; Laser Therapy; Latanoprost; Lipids; Practice Guidelines as Topic; Prostaglandins F, Synthetic; Travoprost; United States

To report angiographically documented cystoid macula edema associated with the use of each of the three newly available ocular hypotensive lipids: unoprostone, travaprost, and bimatoprost.. Observational case series.. Retrospective review of three patients in a clinical practice who had uncontrolled glaucoma on maximal tolerable therapy except for an ocular hypotensive lipids. All three patients also had previous cataract and filtration surgery, and all had an absent or open posterior lens capsule. The patients were informed of the potential risks of cystoid macula edema associated with the use of an ocular hypotensive lipids versus the risks of repeat filtration surgery.. An ocular hypotensive lipids was started in the affected eye in each patient, and the patient was instructed to check visual acuity everyday and report back any change in vision occurred.. Decreased vision of at least two lines caused by angiographically confirmed cystoid macula edema was noted in each of three patients started, respectively, on unoprostone, travaprost, and bimatoprost. The visual acuity returned to baseline, and the cystoid macula edema was angiographically resolved after discontinuation of the ocular hypotensive lipids and the initiation of a topical steroid and non-steroidal anti-inflammatory eyedrops. Until a causal relationship between cystoid macula edema and ocular hypotensive lipids is proved or disproved, caution in their use in high-risk eyes would be prudent.

Topics: Aged; Aged, 80 and over; Amides; Antihypertensive Agents; Bimatoprost; Cloprostenol; Dinoprost; Female; Fluorescein Angiography; Glaucoma; Humans; Intraocular Pressure; Lens Implantation, Intraocular; Lipids; Macular Edema; Male; Phacoemulsification; Retrospective Studies; Trabeculectomy; Travoprost; Visual Acuity

Rescula (0.12% unoprostone isopropyl) is the first docosanoid compound approved for treatment of glaucoma in humans. It is commercially available in Japan, and is undergoing clinical testing elsewhere. The aim of this study was to evaluate the effect of Rescula on intraocular pressure (IOP) in normotensive dogs. After establishing a baseline diurnal IOP curve, six dogs were unilaterally treated with Rescula while the contralateral eye was treated with a placebo. Applanation tonometry was performed in both eyes, and pupil size was evaluated, 30 min after treatment, and at 1-hr intervals for the next 9 hr. Rescula caused a significant (p=0.014) and long-lasting decrease in IOP, from 20.49+/-2.02 mm Hg in control eyes to 15.49+/-0.69 mm Hg in treated eyes. These results suggest that Rescula is potentially efficacious in treatment of canine glaucoma.

Topics: Animals; Dinoprost; Dog Diseases; Dogs; Fatty Acids; Glaucoma; Intraocular Pressure; Ophthalmic Solutions; Random Allocation; Tonometry, Ocular

Topics: Administration, Topical; Adult; Ciliary Body; Corneal Edema; Dinoprost; Female; Glaucoma; Humans; Intraocular Pressure; Laser Therapy; Latanoprost; Ocular Hypertension; Prostaglandins F, Synthetic; Retinitis Pigmentosa

Corneal epithelial disorders due to isopropyl unoprostone (unoprostone) eye drops, a prostaglandin F2alpha-related substance and antiglaucoma agent, have been reported since the agent became commercially available. The in vitro study was performed to clarify the mechanism of cell injury due to unoprostone. After Chang's human conjunctival cells were cultured and exposed for 2, 4 and 8 min to 0.03, 0.06, and 0.12% unoprostone and its vehicle containing 1% polysorbate 80, a cell growth assay and DNA histogram analysis using a flow cytometer and scanning electron microscopy were performed. The number of living cells was reduced, and the floating cell number increased immediately after exposure to 0.12% unoprostone for 8 min. When the cells were cultured for another 48 hr after exposure to unoprostone, the cell number was reduced dose and time dependently. Exposure for 2 min to 0.12% unoprostone showed no effect on the cell cycle. However, exposure for 2 min to 0.12% unoprostone caused alteration of the cell surface, such as reduction of microvilli and filopodia. The vehicle did not affect the cell surface or cell growth. These results suggest that clinically instilled eye drops ofunoprostone can affect cell structure, inhibit cell growth, and gradually cause corneal epithelial disorders.

Topics: Cell Division; Cell Survival; Cells, Cultured; Conjunctiva; Dinoprost; DNA; Dose-Response Relationship, Drug; Flow Cytometry; Glaucoma; Humans; Microscopy, Electron, Scanning; Ophthalmic Solutions; Time Factors

To present a case in which iris pigmentation developed after treatment with isopropyl unoprostone, an analogue of a prostaglandin metabolite.. Case report.. A Japanese man with dark brown irises, treated unilaterally with isopropyl unoprostone, developed iris-color change in the treated eye after a 20-month treatment.. Isopropyl unoprostone can induce iris pigmentation as does latanoprost.

Topics: Administration, Topical; Dinoprost; Eye Color; Follow-Up Studies; Glaucoma; Humans; Iris; Iris Diseases; Male; Middle Aged; Ophthalmic Solutions

Unoprostone (isopropyl unoprostone) is a docosanoid compound which is related to a metabolite of prostaglandin (PG)F2 alpha. Unoprostone has oculo-hypotensive effects. The drug is thought to lower intraocular pressure (IOP) by increasing aqueous humour outflow. Aqueous humour production remains unaffected. Marked reductions in IOP have been demonstrated in healthy volunteers and patients with glaucoma or ocular hypertension after instillation of unoprostone 0.12%. Unoprostone 0.12% appears to have similar efficacy to timolol 0.5% in patients with primary open-angle glaucoma or ocular hypertension. In phase II and III clinical studies, adverse events observed with unoprostone were predominantly local; systemic effects occurred less frequently.

Topics: Animals; Clinical Trials as Topic; Dinoprost; Glaucoma; Humans

Topics: Animals; Dinoprost; Glaucoma; Haplorhini; Humans; Intraocular Pressure; Latanoprost; Prostaglandins F, Synthetic; Prostaglandins, Synthetic; Rabbits

The ophthalmic solution of UF-021, a novel prostaglandin (PG) related compound, was investigated for its intraocular pressure (IOP) reducing activity and local ocular side effects in different species of animals. UF-021 ophthalmic solution (0.03 to 0.24%), when topically applied to the eyes of rabbits, caused dose-dependent IOP reduction (2.8 to 5.2 mmHg), without transient IOP rise. Both in cats and monkeys, UF-021 ophthalmic solution (0.12%) elicited rapid, significant IOP reduction (ca. 9 mmHg and 2 mmHg, respectively), without any controversial, local ocular side effects being revealed. On the other hand, PGE2, PGF2 alpha-isopropyl ester all brought about marked increases in IOP prior to development of their IOP reducing activities. In addition, these primary PGs showed intense local ocular irritation, which presented a striking contrast with UF-021. Enhancement of IOP reducing activity, coupled with freedom from any significant ocular side effects, as described above, suggests that UF-021 ophthalmic solution could be promising as a new anti-glaucoma agent.

Topics: Animals; Cats; Dinoprost; Dinoprostone; Female; Glaucoma; Intraocular Pressure; Macaca; Male; Rabbits