apraclonidine

Action and Spectrum

Actions and Spectrum 

apraclonidine acts by stimulating alpha-adrenergic receptors in the eye, specifically the alpha-2 adrenergic receptors.  

It selectively activates these receptors, leading to a reduction in the production of fluid in the eye and an increase in its outflow.

Drug Interaction

Adverse Reaction

Frequency not defined  

Discomfort 

Blanching 

Edema 

Corneal erosion 

Conjunctivitis 

Abnormal vision 

Conjunctival 

Edema Irritation 

Keratitis 

Discharge 

Lid retraction 

Photophobia 

Pain 

Lid disorder 

Lid margin crusting 

Conjunctivitis 

Lid erythema 

Tearing 

Blurred vision 

Corneal infiltrate, Corneal staining 

Hyperemia 

Pruritus 

Arrhythmia 

Nervousness 

Peripheral edema 

Headache 

Insomnia 

Asthenia 

Paresthesia 

Parosmia 

Dizziness 

Dry nose 

Constipation 

Nausea 

Malaise 

Depression 

Facial edema 

Asthma 

Chest pain 

Dyspnea 

Abnormal coordination 

Black Box Warning

Black Box Warning 

None

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• apraclonidine is contraindicated in individuals who have a known hypersensitivity or allergy to apraclonidine or any of its components.  

Caution: 

• Exercise caution if you have ongoing cardiac disease, such as HTN, coronary insufficiency, a recent MI, cerebrovascular disease, chronic renal failure, Raynaud’s disease or a history of vasovagal episodes. 
• apraclonidine should be used with caution in patients with severe depression or other psychiatric disorders. 
• apraclonidine should be used cautiously in individuals with a history of cerebral or coronary insufficiency, as it may potentially exacerbate these conditions. 

Pregnancy / Lactation

Pregnancy consideration: 

Pregnancy category: C 

Lactation: Excretion into human milk is unknown  

Pregnancy Categories:         

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.  

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women. 

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 

Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology  

As a direct and agonist of alpha-2 adrenergic receptors, apraclonidine works. Norepinephrine, a neurotransmitter that controls several physiological functions, is prevented from being released by attaching to these receptors. 

Pharmacodynamics 

The pharmacodynamics of apraclonidine involves its interaction with alpha-adrenergic receptors and subsequent modulation of intraocular pressure (IOP).  

Pharmacokinetics 

Absorption   

When applied topically to the eye, it is absorbed through the cornea and conjunctiva.   

Distribution 

apraclonidine has a limited distribution within the body.  

Metabolism 

apraclonidine undergoes hepatic metabolism in the liver.  

Elimination and excretion 

The metabolites of apraclonidine are eliminated through the renal route.

Adminstartion

Administration 

apraclonidine is primarily administered as eye drops for ophthalmic use.

Patient Information Leaflet

Patient information leaflet 

Generic Name: apraclonidine  

Why do we use apraclonidine? 

apraclonidine is used in ophthalmology for specific indications related to the eye.   

apraclonidine can be used as an adjunctive therapy in the management of glaucoma.  

apraclonidine may use in cases of ocular hypertension to help lower IOP and reduce the risk of developing glaucoma.