Medically reviewed on Nov 15, 2018
(a pra KLOE ni deen)
- Apraclonidine HCl
- Apraclonidine Hydrochloride
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Iopidine: 0.5% (5 mL, 10 mL); 1% (1 ea) [contains benzalkonium chloride]
Generic: 0.5% (5 mL, 10 mL)
Brand Names: U.S.
- Alpha2 Agonist, Ophthalmic
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
Systemic: 0.5% solution: 8 hours
Use: Labeled Indications
Intraocular pressure reduction:
0.5% solution: Short-term, adjunctive therapy in patients who require additional reduction of IOP
1% solution: Prevention and treatment of postsurgical intraocular pressure (IOP) elevation following argon laser trabeculoplasty, argon laser iridotomy or Nd:YAG posterior capsulotomy
Hypersensitivity to apraclonidine, clonidine, or any component of the formulation; concomitant use with MAO inhibitors.
Canadian labeling: Additional contraindications (not in US labeling): Children and adolescents <18 years old.
Intraocular pressure reduction: Ophthalmic:
0.5%: Instill 1 to 2 drops in the affected eye(s) 3 times daily.
1%: Instill 1 drop in operative eye 1 hour prior to anterior segment laser surgery, second drop in same eye immediately upon completion of procedure.
Refer to adult dosing.
Dosing: Renal Impairment
There are no dosage adjustments provided in the manufacturer's labeling; monitor cardiovascular parameters closely. Use with caution in patients with chronic renal failure.
Dosing: Hepatic Impairment
There are no dosage adjustments provided in the manufacturer's labeling; monitor cardiovascular parameters closely.
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.
Iopidine 0.5%: Store between 2°C to 27°C (36°F to 80°F); protect from freezing and light.
Iopidine 1%: Store between 2°C to 25°C (36°F to 77°F); protect from light.
Mianserin: May diminish the therapeutic effect of Alpha2-Agonists (Ophthalmic). 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. Consider therapy modification
Monoamine Oxidase Inhibitors: May enhance the adverse/toxic effect of Apraclonidine. Monoamine Oxidase Inhibitors may increase the serum concentration of Apraclonidine. Avoid combination
Tricyclic Antidepressants: May diminish the therapeutic effect of Alpha2-Agonists (Ophthalmic). Monitor therapy
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
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.
• 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.
• Depression: Use with caution in depressed patients and monitor signs/symptoms of depression; therapy is associated infrequently with depression.
• 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.
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
• 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.
• 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.
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.
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 punctual occlusion to decrease potential exposure to the fetus (Samples 1988).
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience blurred vision, dry eyes, increased tears, or dry mouth. Have patient report immediately to prescriber vision changes, eye pain, severe eye irritation, eyelid edema, eye discharge, or foreign body sensation in eye (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.
More about apraclonidine ophthalmic
- Apraclonidine ophthalmic Side Effects
- During Pregnancy or Breastfeeding
- Dosage Information
- Drug Interactions
- Pricing & Coupons
- En Español
- Drug class: ophthalmic glaucoma agents
Other brands: Iopidine