Apraclonidine

Apraclonidine

Systematic (IUPAC) name
2,6-dichloro-N- (4,5-dihydro-1H-imidazol-2-yl) benzene-1,4-diamine
Clinical data
Trade names	Iopidine
AHFS/Drugs.com	monograph
MedlinePlus	a608005
Legal status	UK: POM (Prescription only) ℞ (Prescription only)
Routes of administration	Ophthalmic solution
Pharmacokinetic data
Protein binding	98.7%
Biological half-life	8 hours
Identifiers
CAS Number	66711-21-5 Y
ATC code	S01EA03 (WHO)
PubChem	CID: 2216
IUPHAR/BPS	7117
DrugBank	DB00964 Y
ChemSpider	2130 Y
UNII	843CEN85DI Y
KEGG	D07461 Y
ChEBI	CHEBI:2788 Y
ChEMBL	CHEMBL647 Y
Chemical data
Formula	C9H10Cl2N4
Molecular mass	245.108 g/mol
SMILES Clc1c(c(Cl)cc(N)c1)N/C2=N/CCN2
InChI InChI=1S/C9H10Cl2N4/c10-6-3-5(12)4-7(11)8(6)15-9-13-1-2-14-9/h3-4H,1-2,12H2,(H2,13,14,15) Y Key:IEJXVRYNEISIKR-UHFFFAOYSA-N Y
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Apraclonidine (INN), also known as Iopidine, is a sympathomimetic used in glaucoma therapy. It is an α₂-adrenergic agonist and a weak alpha-1 adrenergic receptor agonist.

Topical apraclonidine is administered at a concentration of 1% for the prevention and treatment of postsurgical intraocular pressure elevation and 0.5% for short-term adjunctive therapy in patients on maximally tolerated medical therapy who require additional redirection of intraocular pressure. One drop is usually added one hour prior to laser eye surgery and another drop is given after the procedure is complete.

Clinical uses

Apraclonidine is indicated for the short-term adjunctive treatment of patients on maximally tolerated medical therapy who require additional reduction. Patients on maximally tolerated medical therapy who are treated with apraclonidine to delay surgery should have frequent follow-up examinations and treatment should be discontinued if the intraocular pressure rises significantly.

Apraclonidine may be useful in the diagnosis of Horner's syndrome. In Horner's syndrome, the sympathetic innervation to the pupillary dilator muscle is lost. The affected pupil is thus miotic and the pupillary dilator responds to denervation by increasing alpha-1 receptors. Apraclonidine is useful in this case due to its weak alpha-1 adrenergic properties. When applied to the denervated (and thus hyper-sensitive) pupillary dilator muscle, a super-normal dilatory response is generated in which the pupil dilates to a degree greater than that which would be seen in a non-denervated muscle. This causes the reversal of anisocoria that is characteristic of Horner's.

Topical apraclonidine can also decrease IOP in glaucoma patients by increasing trabecular outflow, in a similar way to clonidine, but without the cardiovascular side effects.

External links

• Iopidine prescribing information (from the FDA website)
• Simple information on Apraclonidine