Apraclonidine

Apraclonidine
Clinical data
Trade names Iopidine
AHFS/Drugs.com Monograph
MedlinePlus a608005
Routes of
administration
Topical (ophthalmic solution)
ATC code S01EA03 (WHO)
Legal status
Legal status
  • UK: POM (Prescription only)
  • US: ℞-only
  • ℞ (Prescription only)
Pharmacokinetic data
Protein binding 98.7%
Biological half-life 8 hours
Identifiers
CAS Number 66711-21-5 YesY
PubChem (CID) 2216
IUPHAR/BPS 7117
DrugBank DB00964 YesY
ChemSpider 2130 YesY
UNII 843CEN85DI YesY
KEGG D07461 YesY
ChEBI CHEBI:2788 YesY
ChEMBL CHEMBL647 YesY
Chemical and physical data
Formula C9H10Cl2N4
Molar mass 245.108 g/mol
3D model (Jmol) Interactive image
  (verify)

Apraclonidine (INN), also known under the brand name Iopidine, is a sympathomimetic used in glaucoma therapy. It is an α2 adrenergic receptor agonist and a weak α1 adrenergic receptor agonist.

Topical apraclonidine is administered at a concentration of 1% for the prevention and treatment of post-surgical intraocular pressure (IOP) elevation and 0.5% for short-term adjunctive therapy in patients on maximally tolerated medical therapy who require additional reduction of IOP. 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 glaucoma for patients on maximally tolerated medical therapy who require additional reduction of IOP. These patients, 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 α1 receptors. Apraclonidine is useful in this case due to its weak α1-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,[1] but without the cardiovascular side effects.

External links

References

  1. Toris, C. B.; Tafoya, M. E.; Camras, C. B.; Yablonski, M. E. (1995). "Effects of Apraclonidine on Aqueous Humor Dynamics in Human Eyes". Ophthalmology. 102 (3): 456. doi:10.1016/S0161-6420(95)31000-7.
This article is issued from Wikipedia - version of the 9/9/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.