Tìm theo
Apraclonidine
Các tên gọi khác (3) :
  • 4-Aminoclonidine
  • Apraclonidina
  • Apraclonidinum
adrenergic alpha 2 receptor agonists, anti glaucoma agents, eent preparations, ophthalmics
Thuốc Gốc
Small Molecule
CAS: 66711-21-5
ĐG : Akorn Inc. , http://www.akorn.com
CTHH: C9H10Cl2N4
PTK: 245.109
Apraclonidine, also known as iopidine, is a sympathomimetic used in glaucoma therapy. It is an alpha2-adrenergic agonist.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C9H10Cl2N4
Phân tử khối
245.109
Monoisotopic mass
244.028251754
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)
InChI Key
InChIKey=IEJXVRYNEISIKR-UHFFFAOYSA-N
IUPAC Name
2,6-dichloro-1-N-(4,5-dihydro-1H-imidazol-2-yl)benzene-1,4-diamine
Traditional IUPAC Name
apraclonidine
SMILES
NC1=CC(Cl)=C(NC2=NCCN2)C(Cl)=C1
Độ hòa tan
4.09e-01 g/l
logP
1.4
logS
-2.8
pKa (Strongest Basic)
8.48
PSA
62.44 Å2
Refractivity
63.79 m3·mol-1
Polarizability
23.27 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
4
H Bond Donor Count
3
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : Apraclonidine, also known as iopidine, is a sympathomimetic used in glaucoma therapy. It is an alpha2-adrenergic agonist. 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.
Dược Động Học :
▧ 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.
▧ Protein binding :
98.7%
▧ Half Life :
8 hours
Độc Tính : 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.
Chỉ Định : 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.
Tương Tác Thuốc :
  • 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.
Liều Lượng & Cách Dùng : Liquid - Ophthalmic
Solution / drops - Ophthalmic
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Iopidine
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00964
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2216
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505614
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07668
ChemSpider
http://www.chemspider.com/Chemical-Structure.2130.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50021812
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0065-0665-05
PharmGKB
http://www.pharmgkb.org/drug/PA164748866
Wikipedia
http://en.wikipedia.org/wiki/Apraclonidine
RxList
http://www.rxlist.com/cgi/generic2/apraclonidine.htm
Drugs.com
http://www.drugs.com/cdi/apraclonidine-drops.html
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