Iopidine®
Apraclonidine 0.5%, 1% · ophthalmic solution
Antiglaucoma
Approved uses
Post-surgical intraocular pressure spike after argon laser trabeculoplasty, argon laser iridotomy or Nd:YAG capsulotomy
1% solution: one drop in the operative eye one hour before the laser, and a second drop immediately after it is finished
The 1% strength exists only for this peri-laser use, given twice around the procedure rather than on a schedule
Short-term adjunctive pressure reduction in patients already on maximally tolerated therapy
0.5% solution: one to two drops in the affected eye(s) three times daily
Short-term by design: tachyphylaxis and allergic conjunctivitis limit how long it keeps working
OFF-LABELNot in the FDA label for this product
Horner syndrome, confirming an oculosympathetic palsy
One drop of the 0.5% solution in each eye, read at 45 to 60 minutes
n=85 eyes · reversal in all
This is the test that displaced cocaine. Denervation makes the dilator's alpha-1 receptors supersensitive, so apraclonidine dilates the affected pupil while very weakly constricting the normal one, and the anisocoria REVERSES. Across 31 eyes with oculosympathetic paresis and 54 control eyes, all confirmed against the cocaine test, apraclonidine dilated the affected pupils by a mean 2.04 mm and constricted the controls by 0.14 mm, reversed the anisocoria in every Horner case, and lifted the ptotic lid by a mean 1.75 mm. The authors concluded it has at least the sensitivity and specificity of the cocaine test. Two cautions the study does not cover: supersensitivity takes days to weeks to develop, so an acute Horner can test falsely negative, and apraclonidine is avoided in infants for the risk of central nervous system depression.
Contraindications
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).
Available FormsApraclonidine ophthalmic solution 0.5% in 5 mL and 10 mL bottles, and 1% in single-use containers.
Mechanism of ActionA relatively selective alpha-2-adrenergic agonist; when instilled in the eye it has the action of reducing elevated, as well as normal, intraocular pressure (IOP), whether or not accompanied by glaucoma. Its predominant mechanism of action is reduction of aqueous flow via stimulation of the alpha-adrenergic system.
Warnings & Precautions
- For topical ophthalmic use only; not for injection or oral ingestion.
- Topical apraclonidine has been reported to cause cardiovascular collapse requiring resuscitation; use with caution in severe cardiovascular disease, including hypertension.
- Use with caution in coronary insufficiency, recent myocardial infarction, cerebrovascular disease, chronic renal failure, Raynaud's disease or thromboangiitis obliterans.
- Discontinue if ocular allergic-like symptoms occur.
- The preservative may be absorbed by soft contact lenses; remove lenses before instillation and reinsert 15 minutes afterwards.
Common Side Effects
The following adverse reactions were reported in 5 to 15% of the patients: discomfort, hyperemia, and pruritus. Dry mouth occurred in approximately 10% of the patients.
Pregnancy & LactationPregnancy: Apraclonidine was embryocidal in rabbits at an oral dose 150 times the maximum recommended human ophthalmic dose; there are no adequate and well-controlled studies in pregnant women.
Lactation: Not stated on the FDA label.
Pediatric UseSafety and effectiveness in pediatric patients have not been established.