Apraclonidine

Molecular formula CgHioCl2N4 Molecular weigM 245.11 CAS Registry No 66711-21-5 Merck Index 13,756 

Sample preparation Inject a 50 xL aliquot of a solution in glutathione bicarbonated Ringer s solution (pH 7.4). 

Mobile phase MeCN water 20 80 to 60 40 ( ) containing 5 mM sodium heptanesulfonic acid at pH 3.5 Flowrate 1-1.5 Injection volume 50 Detector UV 254 

Gluchowski, C. Tang-Liu, D.D.-S. Comeal and conjunctival/scleralpenetration of p-aminoclonidine, AGN 190342, and clonidine in rabbit eyes, Current Eye Res., 1990,9,1051-1059. 

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C 3H,sCl2Ni02 41936-93-0) see Clenbuterol 7V-(4-amino-3,5-dichlorophenyl)trichloroacetamide (C (H5Cl5N20 S686/-4/-S) see Apraclonidine... 

G)H2Cl7N20 86567-35-0) see Apraclonidine (dichloromethylene)bisphosphonic acid tetrakis(l-methyl-ethyl) ester... 

Patients should be monitored for tachyphylaxis, especially with / -blockers or apraclonidine. Treatment can be temporarily discontinued to monitor its benefit. 

Instill 1 to 2 drops in the affected eye(s) 3 times daily. Because apraclonidine 0.5% will be used with other ocular glaucoma therapies, use an approximate 5-minute interval between instillation of each medication to prevent washout of the previous dose. Not for injection into the eye. 

Pharmacology Apraclonidine hydrochloride is a relatively selective -adrenergic agonist. When instilled into the eyes, apraclonidine reduces intraocular pressure (lOP) and has minimal effect on cardiovascular parameters. 

Pharmacokinetics Topical use of apraclonidine 0.5% leads to systemic absorption. The onset of action is usually within 1 hour and the maximum lOP reduction occurs 3 to 5 hours after application of a single dose. 

Renal/Hepatic function impairment Although the topical use of apraclonidine has not been studied in renal failure patients, structurally related clonidine undergoes a significant increase in half-life in patients with severe renal impairment. Close monitoring of cardiovascular parameters in patients with impaired renal function is advised if they are candidates for topical apraclonidine therapy. Close monitoring of cardiovascular parameters in patients with impaired liver function is also advised as... 

Lactation Consider discontinuing nursing for the day on which apraclonidine is used. Children Safety and efficacy for use in children have not been established. 

Monitoring Glaucoma patients on maximally tolerated medical therapy who are treated with 0.5% apraclonidine to delay surgery should have their visual fields monitored periodically. Discontinue treatment if lOP rises significantly. lOP reduction Because apraclonidine is a potent depressor of lOP, closely monitor patients who develop exaggerated reductions in lOP. 

Cardiovascular disease Acute administration of 2 drops of apraclonidine has had minimal effect on heart rate or blood pressure however, observe caution in treating patients with severe cardiovascular disease, including hypertension. 

Use 0.5% apraclonidine with caution in patients with coronary insufficiency, recent Ml, cerebrovascular disease, chronic renal failure, Raynaud disease, or thromboangiitis obliterans. 

Depression Use caution and monitor depressed patients because apraclonidine has been infrequently associated with depression. 

Acetazolamide (Diamox) Apraclonidine (lopidine) Betaxolol, Ophthalmic (Betoptic) Brimonidine (Alphagan P)... 

Contraindications Hypersensitivity to apraclonidine or clonidine or any component of the formulation. 

Apraclonidine and brimonidine Used in glaucoma to reduce intraocular pressure... 

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