Disease relevance of C07668

• Apraclonidine may be of value as an additional therapy for open-angle glaucoma in selected patients [1].
• CONCLUSIONS: Apraclonidine effectively lowers IOP associated with open-angle glaucoma or ocular hypertension; these pilot results will need to be confirmed by a larger pivotal study [1].
• Of patients with chronic angle-closure glaucoma, IOP was similar to prelaser values in 11 (69%) of 16 eyes treated with 0.5% (P > 0.7) and 12 (80%) of 15 eyes treated with 1.0% apraclonidine (P > 0.3) [2].
• Ocular effects of apraclonidine in Horner syndrome [3].
• High incidence of topical allergic reactions to 1% apraclonidine [4].

High impact information on C07668

• Unoprostone appears to have a reproducible antiendothelin-1 effect, betaxolol may exert a calcium-channel blocker action, apraclonidine consistently leads to anterior segment vasoconstriction, and carbonic anhydrase inhibitors seem to accelerate the retinal circulation [5].
• RESULTS: A single instillation of apraclonidine 1.15%, two instillations of epinephrine 1.25%, two instillations of dipivefrin 0.1%, and two instillations and one instillation of dipivefrin 0.04% eye drops inhibited 98%, 96%, 87%, 73%, and 47% of PGE(2)-induced aqueous flare elevation, respectively [6].
• CONCLUSIONS: The alpha(2)-adrenoceptor agonists brimonidine, apraclonidine, and oxymetazoline are potent vasoconstrictors in the porcine ciliary artery [7].
• The structural modification to apraclonidine decreases corneal absorption and the drug's ability to cross the blood-brain barrier, minimising the risk of centrally mediated cardiovascular side effects [8].
• Apraclonidine (p-aminoclonidine) ophthalmic solution effectively reduces the rise in intraocular pressure (IOP) following anterior segment laser surgery [9].

Chemical compound and disease context of C07668

• PURPOSE: To compare the safety and efficacy of apraclonidine ophthalmic solution 0.25% and 0.5% (both given 3 times daily) to timolol maleate (0.5%) given twice daily, in primary open-angle glaucoma or ocular hypertension [1].
• OBJECTIVE: To identify the incidence and characteristics of allergic reactions associated with the long-term use of 1% apraclonidine hydrochloride [10].
• Only five patients (22.7%) previously allergic to apraclonidine developed an allergic reaction to brimonidine [11].
• The comparative ocular hypotensive effect of apraclonidine with timolol maleate in exfoliation versus primary open-angle glaucoma patients [12].
• Comparing efficacies of 0.5% apraclonidine with 4% cocaine in the diagnosis of horner syndrome in pediatric patients [13].

Biological context of C07668

• No significant change in pulse rate or blood pressure was seen during apraclonidine administration [14].
• There were no statistically significant changes in mean heart rate or blood pressure in either group except for a slight reduction in diastolic blood pressure at 1 hour (P = 0.005) in the brimonidine group (-5.2 +/- 7.4 mmHg) compared with the apraclonidine group (-0.2 +/- 6.4 mmHg) [15].
• When compared with baseline day only, aqueous flow in the apraclonidine-treated eyes decreased by 0.3 microliter/minute (P < 0.04), and episcleral venous pressure decreased by 1.0 mmHg (P < 0.001) [16].
• The acute administration of apraclonidine did not affect both mean blood pressure and OPP, but a worsening of the visual field was nevertheless recorded [17].
• In spite of pre- and post-laser treatment with topical apraclonidine (Iopidine) and normal IOP 1 hour postoperatively, the patient presented the next day with visual acuity of 20/300, corneal edema, pain, and IOP of 60 mm Hg [18].

Anatomical context of C07668

• INTERVENTION: Both groups received one drop of apraclonidine 1.0% 15 minutes before ALT to 180 degrees of previously untreated trabecular meshwork [19].
• Effect of apraclonidine on blood-aqueous barrier permeability to plasma protein in man [20].
• Effects of 0.5% apraclonidine on optic nerve head and peripapillary retinal blood flow [21].
• Mild blanching of the conjunctiva occurred in apraclonidine-treated eyes [22].
• Effect of topical apraclonidine on flow properties of central retinal and ophthalmic arteries [23].

Associations of C07668 with other chemical compounds

• After a unilateral single dose application of topical 1% apraclonidine hydrochloride, intraocular pressure (IOP), heart rate, and interpalpebral distance were measured [24].
• OBJECTIVE: To determine the incidence of intraocular pressure (IOP) rise of varying degrees after laser peripheral iridotomy (LPI) in patients with and without glaucoma treated perioperatively with pilocarpine and apraclonidine [25].
• PURPOSE: To compare the efficacy of 0.5% and 1.0% apraclonidine in preventing laser-induced intraocular pressure (IOP) elevation after trabeculoplasty, neodymium: YAG (Nd: YAG) iridotomy, and capsulotomy [2].
• The production of a reactive electrophilic intermediate of apraclonidine was demonstrated through the formation of two glutathione apraclonidine adducts from the horseradish peroxidase/H2O2-mediated oxidation of apraclonidine in the presence of glutathione [26].
• One eye in the apraclonidine group, two in the acetazolamide group, and five in the control group had IOPs greater than 30 mm Hg [27].

Gene context of C07668

• Patients with HS have denervation supersensitivity of the alpha1 receptors in the iris stroma of the affected eye, making the pupil dilator responsive to apraclonidine [28].

Analytical, diagnostic and therapeutic context of C07668

• CONCLUSION: Apraclonidine effectively decreased large IOP elevations in glaucomatous eyes undergoing trabeculectomy combined with extracapsular cataract surgery [29].
• Effect of topical apraclonidine on the frequency of intraocular pressure elevations after combined extracapsular cataract extraction and trabeculectomy [29].
• METHODS: A prospective, randomized, double-masked study compared topical 1% apraclonidine with placebo [29].
• One eye in the apraclonidine group and six in the control group had IOPs greater than 30 mm Hg [27].
• Preventing intraocular pressure increase after phacoemulsification and the role of perioperative apraclonidine [30].

References