apraclonidine

Apraclonidine is a synthetic adrenergic agonist used primarily as an ophthalmic solution to lower intraocular pressure in patients with glaucoma or ocular hypertension. It belongs to the class of selective alpha‑2 adrenergic receptor agonists and is available in 0.5 % or 0.10 % aqueous solutions.

The drug decreases aqueous humor production by stimulating alpha‑2 receptors in the ciliary body and enhances uveoscleral outflow. Because of its partial alpha‑1 agonist activity, it can also cause mild mydriasis and redness, especially at higher concentrations.

Clinical indications include primary open‑angle glaucoma, secondary glaucoma, and ocular hypertension. Apraclonidine is typically administered one to four times daily, depending on the severity of the disease and the prescribed concentration. It is often used as an adjunct to other antiglaucoma agents and is compatible with many preservatives and eyelash eye drops.

Common adverse reactions are transient burning or stinging of the eye, mild conjunctival hyperaemia, blurred vision, and temporary mydriasis. Systemic absorption can lead to mild allergic reactions, flushing, or a transient rise in blood pressure in susceptible individuals. Rarely, it may cause photophobia or headache.

Contraindications include hypersensitivity to apraclonidine or any excipient, severe systemic hypertension, or known hypersensitivity to beta‑adrenergic blockers. Pregnant or lactating women should use it only if the potential benefit justifies the risk.

Apraclonidine was first synthesized in the 1970s; its ophthalmic formulation was approved by the U.S. Food and Drug Administration in 1982. It has since been included in several glaucoma treatment guidelines and is considered a second‑line agent when first‑line therapies are insufficient.