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药品详细

Apraclonidine(安普乐)

化学结构式图
中文名
安普乐
英文名
Apraclonidine
分子式
C9H10Cl2N4
化学名
2,6-dichloro-1-N-(4,5-dihydro-1H-imidazol-2-yl)benzene-1,4-diamine
分子量
Average: 245.109
Monoisotopic: 244.028251754
CAS号
66711-21-5
ATC分类
S01E 抗青光眼制剂及缩瞳药
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Apraclonidine, also known as iopidine, is a sympathomimetic used in glaucoma therapy. It is an alpha2-adrenergic agonist.

生产厂家
  • Akorn inc
  • Alcon laboratories inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Chen PL, Chen JT, Lu DW, Chen YC, Hsiao CH: Comparing efficacies of 0.5% apraclonidine with 4% cocaine in the diagnosis of horner syndrome in pediatric patients. J Ocul Pharmacol Ther. 2006 Jun;22(3):182-7. Pubmed
  2. Aslanides M, Tsiklis NS, Ozkilic E, Coskunseven E, Pallikaris G, Jankov MR: The effect of topical apraclonidine on subconjunctival hemorrhage and flap adherence in LASIK patients. J Refract Surg. 2006 Jun;22(6):585-8. Pubmed
  3. Koc F, Kansu T, Kavuncu S, Firat E: Topical apraclonidine testing discloses pupillary sympathetic denervation in diabetic patients. J Neuroophthalmol. 2006 Mar;26(1):25-9. Pubmed
  4. Garibaldi DC, Hindman HB, Grant MP, Iliff NT, Merbs SL: Effect of 0.5% apraclonidine on ptosis in Horner syndrome. Ophthal Plast Reconstr Surg. 2006 Jan-Feb;22(1):53-5. Pubmed
  5. Onal S, Gozum N, Gucukoglu A: Effect of apraclonidine versus dorzolamide on intraocular pressure after phacoemulsification. Ophthalmic Surg Lasers Imaging. 2005 Nov-Dec;36(6):457-62. Pubmed
  6. Costa VP, Harris A, Stefansson E, Flammer J, Krieglstein GK, Orzalesi N, Heijl A, Renard JP, Serra LM: The effects of antiglaucoma and systemic medications on ocular blood flow. Prog Retin Eye Res. 2003 Nov;22(6):769-805. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Benzene and Derivatives
  • Halobenzenes
  • Anilines
Substructures
  • Imidazolines
  • Aliphatic and Aryl Amines
  • Benzene and Derivatives
  • Aryl Halides
  • Halobenzenes
  • Imidazoles
  • Heterocyclic compounds
  • Guanidines
  • Aromatic compounds
  • Carboxamidines
  • Anilines
适应症
药理
Indication For prevention or reduction of intraoperative and postoperative increases in intraocular pressure (IOP) before and after ocular laser surgery when used prophylactically. Also used as a short-term adjunctive therapy in patients with open-angle glaucoma who are on maximally tolerated medical therapy requiring additional IOP reduction.
Pharmacodynamics Apraclonidine significantly lowers intraocular pressure with minimal effects on cardiovascular and pulmonary parameters. It lowers intraocular pressure by reducing aqueous humor production and increasing uveoscleral outflow.
Mechanism of action Apraclonidine is a relatively selective alpha2 adrenergic receptor agonist that stimulates alpha1 receptors to a lesser extent. It has a peak ocular hypotensive effect occurring at two hours post-dosing. The exact mechanism of action is unknown, but fluorophotometric studies in animals and humans suggest that Apraclonidine has a dual mechanism of action by reducing aqueous humor production through the constriction of afferent ciliary process vessels, and increasing uveoscleral outflow.
Absorption Topical use of apraclonidine ophthalmic solution leads to systemic absorption. Studies of apraclonidine (0.5% ophthalmic solution) dosed one drop three times a day in both eyes for 10 days in normal volunteers yielded mean peak and trough concentrations of 0.9 ng/mL and 0.5 ng/mL, respectively.
Volume of distribution Not Available
Protein binding 98.7%
Metabolism
Not Available
Route of elimination Not Available
Half life 8 hours
Clearance Not Available
Toxicity Accidental or intentional ingestion of oral apraclonidine has been reported to cause apnea, arrhythmias, asthenia, bradycardia, conduction defects, diminished or absent reflexes, dryness of the mouth, hypotension, hypothermia, hypoventilation, irritability, lethargy, miosis, pallor, respiratory depression, sedation or coma, seizure, somnolence, transient hypertension, and vomiting.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
logP 1.4 Not Available
Predicted Properties
Property Value Source
water solubility 4.09e-01 g/l ALOGPS
logP 2.14 ALOGPS
logP 1.66 ChemAxon
logS -2.8 ALOGPS
pKa (strongest basic) 8.48 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 4 ChemAxon
hydrogen donor count 3 ChemAxon
polar surface area 62.44 ChemAxon
rotatable bond count 1 ChemAxon
refractivity 63.79 ChemAxon
polarizability 23.27 ChemAxon
药物相互作用
Drug Interaction
Tranylcypromine The MAO inhibitor, Tranylcypromine, may increase the vasopressor effect of the alpha2-agonist, Apraclonidine. Concomitant therapy is contraindicated.
Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
食物相互作用
Not Available

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