Version May 2024
Elevated intraocular pressure: Ophthalmic:
Open-angle glaucoma: 0.5%: Instill 1 to 2 drops into the affected eye(s) 3 times daily.
Angle-closure glaucoma (off-label use): 1%: Instill 1 drop into the affected eye as part of a 4-drug regimen; may repeat in 30 to 60 minutes if intraocular pressure (IOP) remains elevated (eg, >40 mm Hg). Note: Reserve medical management for emergency situations when an assessment by an ophthalmologist will be delayed by ≥1 hour (Ref).
Prevention and treatment of postsurgical IOP elevation: 1%: Instill 1 drop into the operative eye 1 hour prior to anterior segment laser surgery, second drop in same eye immediately upon completion of procedure.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling; monitor cardiovascular parameters closely. Use with caution in patients with chronic renal failure.
There are no dosage adjustments provided in the manufacturer's labeling; monitor cardiovascular parameters closely.
Refer to adult dosing.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
Frequency not always defined.
5% to 15%:
Gastrointestinal: Xerostomia (10%)
Ophthalmic: Eye discomfort, eye pruritus, ocular hyperemia
1% to 5%:
Cardiovascular: Cardiac arrhythmia (<3%), chest pain (<3%), facial edema (<3%), peripheral edema (<3%), localized blanching
Central nervous system: Altered sense of smell (<3%), ataxia (<3%), depression (<3%), dizziness (<3%), drowsiness (<3%), headache (<3%), insomnia (<3%), malaise (<3%), nervousness (<3%), paresthesia (<3%)
Dermatologic: Contact dermatitis (<3%), dermatitis (<3%)
Gastrointestinal: Constipation (<3%), dysgeusia (<3%), nausea (<3%)
Neuromuscular & skeletal: Myalgia (<3%), weakness (<3%)
Ophthalmic: Blurred vision, conjunctivitis, dry eye syndrome, eyelid edema, eye discharge, foreign body sensation of eye, lacrimation
Respiratory: Asthma (<3%), dry nose (<3%), dyspnea (<3%), pharyngitis (<3%), rhinitis (<3%)
<1%, postmarketing, and/or case reports: Blepharitis, blepharoconjunctivitis, bradycardia, conjunctival edema, corneal erosion, corneal infiltrates, corneal staining, crusting of eyelid, epithelial keratopathy, erythema of eyelid, eyelid disease, eyelid retraction, eye irritation, eye pain, follicular conjunctivitis, hypersensitivity reaction, keratitis, ocular edema, photophobia, scaling of eyelid, visual disturbance
Hypersensitivity to apraclonidine, clonidine, or any component of the formulation; concomitant use with MAO inhibitors.
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Canadian labeling: Additional contraindications (not in US labeling): Children and adolescents <18 years old.
Concerns related to adverse effects:
• CNS effects: May cause dizziness and somnolence, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
• Hypersensitivity reactions: Use may lead to allergic-like reactions, including hyperemia, pruritus, discomfort, tearing, foreign body sensation, and edema of the lid and conjunctiva; if these symptoms occur, discontinue use.
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with severe uncontrolled cardiovascular disease (eg, hypertension), coronary insufficiency, recent myocardial infarction, cerebrovascular disease, Raynaud disease, and thromboangiitis obliterans.
• Hepatic impairment: Close monitoring of cardiovascular parameters is recommended in patients with hepatic impairment; clonidine (structurally related to apraclonidine) administered systemically undergoes partial hepatic metabolism.
• Renal impairment: Close monitoring of cardiovascular parameters is recommended in patients with renal impairment; use with caution in patients with chronic renal failure. Topical apraclonidine has not been studied in patients with renal impairment; however, the half-life of clonidine (structurally related to apraclonidine) administered systemically is increased significantly in severe impairment.
• Vasovagal reactions: Potential for a vasovagal attack to occur; use with caution in patients with history of vasovagal reactions.
Special populations:
• Contact lens wearers: Some products contain benzalkonium chloride which may be absorbed by soft contact lenses; contact lenses should be removed during instillation; may be reinserted 15 minutes after instillation.
Other warnings/precautions:
• Appropriate use: For topical ophthalmic use only; not for injection or oral administration.
• Tachyphylaxis: The IOP-lowering efficacy may decrease over time in some patients; most patients experience a benefit for less than one month; routinely monitor IOP.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Ophthalmic:
Iopidine: 1% (24 ea) [contains benzalkonium chloride]
Generic: 0.5% (5 mL, 10 mL)
Yes
Solution (Apraclonidine HCl Ophthalmic)
0.5% (per mL): $17.35
Solution (Iopidine Ophthalmic)
1% (per each): $33.27
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Ophthalmic:
Iopidine: 0.5% (5 mL); 1% (0.1 mL) [contains benzalkonium chloride]
Ophthalmic: For topical ophthalmic use only; not for injection or oral administration.
0.5% solution: Wait 5 minutes between instillation of other ophthalmic agents to avoid washout of previous dose. After topical instillation, finger pressure should be applied to lacrimal sac to decrease drainage into the nose and throat and minimize possible systemic absorption.
1% solution: Use a separate container for each single drop dose; discard container after each use. When treating acute angle-closure glaucoma, separate administration of other ophthalmic agents by ≥1 minute (Ref).
Elevated intraocular pressure:
0.5% solution: Short-term, adjunctive therapy in patients who require additional reduction of intraocular pressure (IOP)
1% solution: Prevention and treatment of postsurgical IOP elevation following argon laser trabeculoplasty, argon laser iridotomy or Nd:YAG posterior capsulotomy (manufacturer's labeling) or as part of a 4-drug medical management regimen in acute angle-closure glaucoma when the patient cannot be seen by an ophthalmologist for ≥1 hour (off-label use) (Krawitz 1990; Pokhrel 2007).
Iopidine may be confused with indapamide, iodine, Lodine
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Mianserin: May diminish the therapeutic effect of Alpha2-Agonists (Ophthalmic). Risk X: Avoid combination
Mirtazapine: May diminish the antihypertensive effect of Alpha2-Agonists. Management: Consider avoiding concurrent use. If the combination cannot be avoided, monitor for decreased effects of alpha2-agonists if mirtazapine is initiated/dose increased, or increased effects if mirtazapine is discontinued/dose decreased. Risk D: Consider therapy modification
Monoamine Oxidase Inhibitors: May enhance the adverse/toxic effect of Apraclonidine. Monoamine Oxidase Inhibitors may increase the serum concentration of Apraclonidine. Risk X: Avoid combination
Tricyclic Antidepressants: May diminish the therapeutic effect of Alpha2-Agonists (Ophthalmic). Risk C: Monitor therapy
Adverse events have been observed in animal reproduction studies. If ophthalmic agents are needed during pregnancy, the minimum effective dose should be used in combination with punctal occlusion to decrease potential exposure to the fetus (Samples 1988).
It is not known if apraclonidine is present in breast milk. The manufacturer recommends that caution be exercised when administering apraclonidine 0.5% to breastfeeding women and that breastfeeding be discontinued on the day apraclonidine 1% is administered.
Closely monitor patients who develop exaggerated reductions in intraocular pressure; visual fields (periodically for glaucoma patients on maximally tolerated medical therapy using 0.5% solution to delay surgery); tachyphylaxis; cardiovascular parameters in patients with renal and/or hepatic impairment; depression in depressed patients. Check intraocular pressure 30 to 60 minutes after administration for acute use of 1% solution for acute angle-closure glaucoma (Pokhrel 2007).
Apraclonidine is a potent alpha-adrenergic agent similar to clonidine; relatively selective for alpha2-receptors but does retain some binding to alpha1-receptors; appears to result in reduction of aqueous humor formation; its penetration through the blood-brain barrier is more polar than clonidine which reduces its penetration through the blood-brain barrier and suggests that its pharmacological profile is characterized by peripheral rather than central effects.
Onset of action: 1 hour
Peak effect: Decreased intraocular pressure: 3 to 5 hours
Half-life elimination, systemic: 0.5% solution: 8 hours
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