Apraclonidine

Ophthalmic
Short-term adjunctive therapy of chronic glaucoma

Ophthalmic
Control or prevention of post-surgical intraocular pressure elevation

History of severe or unstable and uncontrolled CV disease including severe uncontrolled arterial HTN. Concomitant or w/in 14 days of MAOI use.

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.

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.

Ophth: C

Avoid contact w/ soft contact lenses. This drug may cause dizziness and somnolence, if affected, do not drive or operate machinery.

Closely monitor IOP (esp on patient who develop excessive reductions) and visual fields.

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.

May cause a potentiating effect w/ alcohol.

Description:
Mechanism of Action: 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).

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

Store between 2-25°C. Protect from light and freezing.

Antiglaucoma Preparations

S01EA03 - apraclonidine ; Belongs to the class of sympathomimetics used in the treatment of glaucoma.

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.