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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/12/09 20:25:14」(JST)

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Apraclonidine (INN), also known as Iopidine, is a sympatholytic 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, ^[1] but without the cardiovascular side effects.

External links

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

References

^ 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. edit

Chen P, Chen J, Lu D, Chen Y, Hsiao C (2006). "Comparing efficacies of 0.5% apraclonidine with 4% cocaine in the diagnosis of horner syndrome in pediatric patients". J Ocul Pharmacol Ther 22 (3): 182–7. doi:10.1089/jop.2006.22.182. PMID 16808679.
Aslanides l, Tsiklis N, Ozkilic E, Coskunseven E, Pallikaris l, Jankov M (2006). "The effect of topical apraclonidine on subconjunctival hemorrhage and flap adherence in LASIK patients". J Refract Surg 22 (6): 585–8. PMID 16805122.
Koc F, Kansu T, Kavuncu S, Firat E (2006). "Topical apraclonidine testing discloses pupillary sympathetic denervation in diabetic patients". J Neuroophthalmol 26 (1): 25–9. doi:10.1097/01.wno.0000204648.79744.71. PMID 16518162.
Garibaldi D, Hindman H, Grant M, Iliff N, Merbs S (2006). "Effect of 0.5% apraclonidine on ptosis in Horner syndrome". Ophthal Plast Reconstr Surg 22 (1): 53–5. doi:10.1097/01.iop.0000196322.05586.6a. PMID 16418668.
Onal S, Gozum N, Gucukoglu A (2005). "Effect of apraclonidine versus dorzolamide on intraocular pressure after phacoemulsification". Ophthalmic Surg Lasers Imaging 36 (6): 457–62. PMID 16355950.

UpToDate Contents

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1. ホルネル症候群 horner syndrome
2. 眼瞼下垂症の概要 overview of ptosis
3. 原発性乳児緑内障 primary infantile glaucoma
4. 瞳孔不同患者へのアプローチ approach to the patient with anisocoria
5. 閉塞隅角緑内障 angle closure glaucoma

English Journal

[Incomplete Horner's syndrome as a presenting sign of fourth ventricle ependymoma].

Escrivá E, Martínez-Costa L.Author information Servicio de Oftalmología, Hospital Dr. Peset, Valencia, España. estherescrivapastor@yahoo.esAbstractCASE REPORT: The case of 44 year old male patient with palpebral ptosis and trigeminal neuralgia as presenting sign of fourth ventricle ependymoma is reported. After surgical treatment, the patient developed a residual paresis of the sixth cranial nerve.
Archivos de la Sociedad Española de Oftalmología.Arch Soc Esp Oftalmol.2013 Sep;88(9):359-61. doi: 10.1016/j.oftal.2012.05.006. Epub 2012 Jul 24.
CASE REPORT: The case of 44 year old male patient with palpebral ptosis and trigeminal neuralgia as presenting sign of fourth ventricle ependymoma is reported. After surgical treatment, the patient developed a residual paresis of the sixth cranial nerve.DISCUSSION: Horner's syndrome occurs due to an
PMID 23988043

But it's not all there.

Peterson JD, Bilyk JR, Sergott RC.Author information Wills Eye Institute, Philadelphia, PA 19107, USA.AbstractA 44-year-old man presented with acute onset headache and isolated anisocoria. Dilation lag was noted in the smaller pupil and Horner syndrome was suspected despite the lack of eyelid ptosis. Cocaine testing confirmed the clinical diagnosis, and urgent neuroimaging found an internal carotid artery dissection. The patient was managed with systemic anticoagulation with a good final outcome. Horner syndrome should be suspected in any patient with aniscoria and dilation lag, despite the absence of eyelid ptosis or other associated findings.
Survey of ophthalmology.Surv Ophthalmol.2013 Sep-Oct;58(5):492-9. doi: 10.1016/j.survophthal.2012.02.009. Epub 2012 Jul 10.
A 44-year-old man presented with acute onset headache and isolated anisocoria. Dilation lag was noted in the smaller pupil and Horner syndrome was suspected despite the lack of eyelid ptosis. Cocaine testing confirmed the clinical diagnosis, and urgent neuroimaging found an internal carotid artery d
PMID 22784676

Autonomic Function in Migraine Patients: Ictal and Interictal Pupillometry.

Cambron M, Maertens H, Paemeleire K, Crevits L.Author information Faculty of Medicine and Health Sciences, Ghent University, Ghent, Belgium; Department of Neurology, Universitair Ziekenhuis Brussel, Jette, Belgium.AbstractOBJECTIVE AND BACKGROUND: Pupillometric investigations into migraine have suggested that an autonomic disturbance is part of the pathogenesis of that condition. This observation is controversial, however, which may reflect that the putative sympathetic hypofunction is either subtle or transient. In this study, we assessed the sympathetic function of migraine patients and controls during both a symptom-free phase and a migraine attack, and challenged patients with apraclonidine to reveal small changes in autonomic function.
Headache.Headache.2013 Jun 28. doi: 10.1111/head.12139. [Epub ahead of print]
OBJECTIVE AND BACKGROUND: Pupillometric investigations into migraine have suggested that an autonomic disturbance is part of the pathogenesis of that condition. This observation is controversial, however, which may reflect that the putative sympathetic hypofunction is either subtle or transient. In
PMID 23808550

Japanese Journal

臨床研究小切開水晶体再建術後の眼圧上昇要因およびアプラクロニジンの効果の検討

江口亮,高木智恵子,石川暢子 [他]
日本眼科学会雑誌 118(9), 768-772, 2014-09
NAID 40020205802

Comparing Brimonidine 0.2% to Apraclonidine 1.0% in the Prevention of Intraocular Pressure Elevation and Their Pupillary Effects Following Laser Peripheral Iridotomy

Yuen Nancy S. Y.,Cheung Peggy,Hui Sui Ping
Japanese journal of ophthalmology 49(2), 89-92, 2005-03-01
NAID 10016484662

末梢性ホルネル症侯群における塩酸アプラクロニジン点眼試験の有用性

渡邊敏夫,内海隆,樋上泰成,小嶌祥太,澤田達,奥英弘,菅澤淳,中島正之,池田恒彦
神経眼科 = Neuro-ophthalmology Japan 20(3), 321-325, 2003-09-25
NAID 10012678360

Related Pictures

★リンクテーブル★

リンク元	「アプラクロニジン」
拡張検索	「apraclonidine hydrochloride」

「アプラクロニジン」

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	Rx only;
Routes	Ophthalmic solution
Pharmacokinetic data
Protein binding	98.7%
Half-life	8 hours
Identifiers
CAS number	66711-21-5
ATC code	S01EA03
PubChem	CID 2216
DrugBank	DB00964
ChemSpider	2130
UNII	843CEN85DI
KEGG	D07461
ChEBI	CHEBI:2788
ChEMBL	CHEMBL647
Chemical data
Formula	C9H10Cl2N4
Mol. 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) ; Key:IEJXVRYNEISIKR-UHFFFAOYSA-N ;
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