Name: Apraclonidine

How is this medicine (Apraclonidine) best taken?

Use apraclonidine as ordered by your doctor. Read all information given to you. Follow all instructions closely.

  • For the eye only.
  • Take out contact lenses before using this medicine. Lenses may be put back in 15 minutes after apraclonidine is given. Do not put contacts back in if your eyes are irritated or infected.
  • Do not touch the container tip to the eye, lid, or other skin.
  • Tilt your head back and drop drug into the eye.
  • After use, keep your eyes closed. Put pressure on the inside corner of the eye. Do this for 1 to 2 minutes. This keeps the drug in your eye.
  • If more than 1 drug is being used in the same eye, use each drug at least 5 minutes apart.

What do I do if I miss a dose?

  • Use a missed dose as soon as you think about it.
  • If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
  • Do not use 2 doses at the same time or extra doses.

What are some side effects that I need to call my doctor about right away?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

  • Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
  • Change in eyesight, eye pain, or very bad eye irritation.
  • Eyelid swelling.
  • Eye discharge.
  • Feeling that something is in the eye.

Indications and usage

Apraclonidine 0.5% Ophthalmic Solution is indicated for short-term adjunctive therapy in patients on maximally tolerated medical therapy who require additional IOP reduction. Patients on maximally tolerated medical therapy who are treated with Apraclonidine Ophthalmic Solution to delay surgery should have frequent follow-up examinations and treatment should be discontinued if the intraocular pressure rises significantly.

The addition of Apraclonidine Ophthalmic Solution to patients already using two aqueous suppressing drugs (i.e., beta-blocker plus carbonic anhydrase inhibitor) as part of their maximally tolerated medical therapy may not provide additional benefit. This is because Apraclonidine Ophthalmic Solution is an aqueous suppressing drug and the addition of a third aqueous suppressant may not significantly reduce IOP.

The IOP lowering efficacy of Apraclonidine Ophthalmic Solution diminishes over time in some patients. This loss of effect, or tachyphylaxis, appears to be an individual occurrence with a variable time of onset and should be closely monitored. The benefit for most patients is less than one month.


Apraclonidine Ophthalmic Solution is contraindicated in patients with hypersensitivity to Apraclonidine or any other component of this medication, as well as systemic clonidine. It is also contraindicated in patients receiving monoamine oxidase inhibitors (MAO inhibitors).

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Ophthalmic:

Iopidine: 0.5% (5 mL, 10 mL); 1% (1 ea) [contains benzalkonium chloride]

Generic: 0.5% (5 mL, 10 mL)

Adverse Reactions

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% (Limited to important or life-threatening): 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.

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.

• 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.

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.