Apraclonidine


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : Ophth Short-term adjunctive therapy of chronic glaucoma As 0.5% soln: Instill 1-2 drops tid. Control or prevention of post-surgical IOP elevation As 1% soln: Instill 1 drop 1 hr before and immediately upon completion of surgery.
Dosage Details
Ophthalmic
Short-term adjunctive therapy of chronic glaucoma
Adult: As 0.5% soln: Instill 1-2 drops into the affected eye tid. Observe approx 5 min interval between installations of other ocular glaucoma therapy (to prevent washout of previous dose). Max recommended duration: 1 mth.

Ophthalmic
Control or prevention of post-surgical intraocular pressure elevation
Adult: As 1% soln: Instill 1 drop into the operative eye 1 hr before and 1 drop immediately upon completion of anterior segment laser surgery.
Contraindications
History of severe or unstable and uncontrolled CV disease including severe uncontrolled arterial HTN. Concomitant or w/in 14 days of MAOI use.
Special Precautions
Patient w/ history of vasovagal attacks, angina; severe coronary insufficiency, recent MI, overt cardiac failure, cerebrovascular disease, Reynaud’s disease, thromboangiitis obliterans, depression. Hepatic and renal (e.g. chronic renal failure) impairment. Pregnancy and lactation.
Adverse Reactions
Hyperaemia, ocular pruritus and discomfort, increased lachrymation, mydriasis, eyelid retraction and oedema, conjunctival blanching and oedema, conjunctivitis, blurred vision, foreign body sensation in the eye; dry mouth and nose, asthenia, headache, dysgeusia, drowsiness, rhinitis, dermatitis. Rarely, depression.
Patient Counseling Information
Avoid contact w/ soft contact lenses. This drug may cause dizziness and somnolence, if affected, do not drive or operate machinery.
MonitoringParameters
Closely monitor IOP (esp on patient who develop excessive reductions) and visual fields.
Drug Interactions
Decreased IOP-lowering effect w/ TCAs. May cause an additive effect w/ CNS depressants (e.g. barbiturates, opiates, sedatives, anaesthetics). May cause a systemic pressor response w/ topical sympathomimetics. May reduce pulse and blood pressure w/ β-blockers (ophth and systemic), antihypertensives, and cardiac glycosides.
Potentially Fatal: Increased serum concentration and enhanced AR w/ MAOIs.
Food Interaction
May cause a potentiating effect w/ alcohol.
Action
Description: Apraclonidine, a clonidine derivative, is a relatively selective α2-adrenergic agonist. It inhibits adenylate cyclase, thus inhibiting the production of cyclic adenosine monophosphate (cAMP). In ophthalmology, this leads to reduction of aqueous humour, thereby lowering intra-ocular pressure (IOP).
Onset: 1 hr.
Duration: ≥12 hr.
Pharmacokinetics:
Absorption: Systemic absorption is low.
Distribution: Crosses the ocular-blood barrier.
Excretion: Elimination half-life: 8 hr (as 0.5% soln).
Chemical Structure

Chemical Structure Image
Apraclonidine

Source: National Center for Biotechnology Information. PubChem Database. Apraclonidine, CID=2216, https://pubchem.ncbi.nlm.nih.gov/compound/Apraclonidine (accessed on Jan. 21, 2020)

Storage
Store between 2-25°C. Protect from light and freezing.
ATC Classification
S01EA03 - apraclonidine ; Belongs to the class of sympathomimetics used in the treatment of glaucoma.
References
Anon. Apraclonidine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/10/2016.

Apraclonidine Solution (Sandoz Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/10/2016.

Buckingham R (ed). Apraclonidine Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/10/2016.

Iopidine Solution/Drops (Alcon Laboratories, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/10/2016.

Joint Formulary Committee. Apraclonidine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/10/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Apraclonidine Hydrochloride (EENT). AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 03/10/2016.

Disclaimer: This information is independently developed by MIMS based on Apraclonidine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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