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Apraclonidine

  • Antiglaucoma agentsAntiglaucoma agents

An alpha-2 agonist eye drop for short-term extra pressure lowering in glaucoma, for example around laser surgery. Its effect fades with time.

Updated

Quick facts

Group
Antiglaucoma agents
Target
α2 adrenergic receptors of the ciliary body
Used for
Short-term add-on therapy
Key effects
Red · Dry mouth · Blanching of the conjunctiva
Monitor
Intraocular pressure · Pulse and blood pressure
ATC
S01EA03

No doses: the clinician sets them by the current guideline.

Mechanism of action

Apraclonidine is a relatively selective α2 agonist related to clonidine. Stimulating α2 receptors in the eye reduces aqueous humour flow, so intraocular pressure falls. It is also a vasoconstrictor, which causes eyelid and conjunctival blanching. In many patients the effect wanes over weeks (tachyphylaxis).

  1. Apraclonidine stimulates α2 receptors in the eye
  2. Aqueous humour flow falls
  3. Intraocular pressure drops; effect may fade (tachyphylaxis)

Indications

  • Short-term add-on therapy in glaucoma on maximal medical treatment that needs more pressure lowering Open-angle glaucoma →

Adverse effects

Common

  • Red, itchy, uncomfortable eye
  • Dry mouth
  • Blanching of the conjunctiva, eyelid swelling
  • Tiredness and drowsiness

Contraindications

  • Use of monoamine oxidase (MAO) inhibitors
  • Hypersensitivity to apraclonidine or to clonidine

Key interactions

MAO inhibitors
Contraindicated
CNS depressants (alcohol, opioids, sedatives, anaesthetics)
Possible additive sedation
Beta-blockers, antihypertensives, cardiac glycosides
Lower pulse and blood pressure; both are checked
Tricyclic antidepressants
May blunt the effect, as they do with clonidine

What is monitored

  • Intraocular pressure, closely, because of tachyphylaxis
  • Visual fields when used to delay surgery
  • Pulse and blood pressure with cardiovascular drugs

Administration and safety

  • For eye use only; not for injection or swallowing.
  • Contact lenses come out before the drop and go back in about 15 minutes later.
  • Look-alike names: apraclonidine, clonidine and brimonidine are different products.

Pregnancy and breastfeeding

There are no adequate human studies; it is used only if the benefit justifies the risk.

Nursing care

  • Check for MAO inhibitor use before the first dose.
  • Warn about drowsiness and dizziness before driving or hazardous work.
  • Teach to stop and report red, itchy, swollen eyes.
  • Check mood in patients with a history of depression.

Pharmacokinetics

Absorption
Topical use leads to systemic absorption
Onset and duration
Effect usually within an hour, maximal at about three hours

Test yourself

Think of the answer, then tap the question to see it.

Why is apraclonidine used only short term?

Its pressure-lowering effect fades over time (tachyphylaxis) and allergic-like eye reactions are common.

Which drug class is contraindicated with it?

Monoamine oxidase inhibitors.

What receptor does it stimulate?

The α2 adrenergic receptor.

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More Pharmacology questions →

Connections

← Back to the class: Antiglaucoma agents

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: DailyMed - APRACLONIDINE solution (DailyMed (U.S. National Library of Medicine), 2024); Apraclonidine Ophthalmic: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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