Tìm theo
Carteolol
Các tên gọi khác (2) :
  • Carteolol
  • Carteololum
antihypertensive agents, sympatholytics, anti arrhythmia agents, adrenergic beta antagonists
Thuốc Gốc
Small Molecule
CAS: 51781-06-7
ATC: C07AA15, S01ED05
ĐG : Alcon Laboratories , http://www.alcon.com
CTHH: C16H24N2O3
PTK: 292.3734
A beta-adrenergic antagonist used as an anti-arrhythmia agent, an anti-angina agent, an antihypertensive agent, and an antiglaucoma agent. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H24N2O3
Phân tử khối
292.3734
Monoisotopic mass
292.178692644
InChI
InChI=1S/C16H24N2O3/c1-16(2,3)17-9-11(19)10-21-14-6-4-5-13-12(14)7-8-15(20)18-13/h4-6,11,17,19H,7-10H2,1-3H3,(H,18,20)
InChI Key
InChIKey=LWAFSWPYPHEXKX-UHFFFAOYSA-N
IUPAC Name
5-[3-(tert-butylamino)-2-hydroxypropoxy]-1,2,3,4-tetrahydroquinolin-2-one
Traditional IUPAC Name
carteolol
SMILES
CC(C)(C)NCC(O)COC1=CC=CC2=C1CCC(=O)N2
Độ hòa tan
4.21e-01 g/l
logP
1.1
logS
-2.8
pKa (strongest acidic)
13.41
pKa (Strongest Basic)
9.76
PSA
70.59 Å2
Refractivity
83.14 m3·mol-1
Polarizability
32.79 Å3
Rotatable Bond Count
6
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 : Carteolol is a beta1 and beta2 (non-selective) adrenergic receptor-blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity. Carteolol, when applied topically to the eye, has the action of reducing elevated, as well as normal, intraocular pressure, whether or not accompanied by glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss and optic nerve damage. Carteolol reduces intraocular pressure with little or no effect on pupil size or accommodation in contrast to the miosis which cholinergic agents are known to produce.
Cơ Chế Tác Dụng : A beta-adrenergic antagonist used as an anti-arrhythmia agent, an anti-angina agent, an antihypertensive agent, and an antiglaucoma agent. [PubChem] The primary mechanism of the ocular hypotensive action of carteolol in reducing intraocular pressure is most likely a decrease in aqueous humor production. This process is initiated by the non-selective beta1 and beta2 adrenergic receptor blockade.
Dược Động Học :

▧ Metabolism :
Hepatic.
Độc Tính : The most common effects expected with overdosage of a beta-adrenergic blocking agent are bradycardia, bronchospasm, congestive heart failure and hypotension.
Chỉ Định : For the treatment of intraocular hypertension and chronic open-angle glaucoma
Tương Tác Thuốc :
  • Acetohexamide The beta-blocker, carteolol, may decrease symptoms of hypoglycemia.
  • Aminophylline Antagonism of action and increased effect of theophylline
  • Chlorpropamide The beta-blocker, carteolol, may decrease symptoms of hypoglycemia.
  • Clonidine Increased hypertension when clonidine stopped
  • Dihydroergotamine Ischemia with risk of gangrene
  • Disopyramide The beta-blocker, carteolol, may increase the toxicity of disopyramide.
  • Epinephrine Hypertension, then bradycardia
  • Ergotamine Ischemia with risk of gangrene
  • Fenoterol Antagonism
  • Formoterol Antagonism
  • Gliclazide The beta-blocker, carteolol, may decrease symptoms of hypoglycemia.
  • Glyburide The beta-blocker, carteolol, may decrease symptoms of hypoglycemia.
  • Ibuprofen Risk of inhibition of renal prostaglandins
  • Indomethacin Risk of inhibition of renal prostaglandins
  • Insulin Glargine The beta-blocker, carteolol, may decrease symptoms of hypoglycemia.
  • Methyldopa Possible hypertensive crisis
  • Methysergide Ischemia with risk of gangrene
  • Orciprenaline Antagonism
  • Oxtriphylline Antagonism of action and increased effect of theophylline
  • Pipobroman Antagonism
  • Piroxicam Risk of inhibition of renal prostaglandins
  • Prazosin Risk of hypotension at the beginning of therapy
  • Repaglinide The beta-blocker, carteolol, may decrease symptoms of hypoglycemia.
  • Terazosin Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Terbutaline Antagonism
  • Theophylline Antagonism of action and increased effect of theophylline
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Liều Lượng & Cách Dùng : Solution - Ophthalmic
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Cartrol
  • Sản phẩm biệt dược : Endak
  • Công ty : Novartis
    Sản phẩm biệt dược : Ocupress
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00521
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2583
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507513
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06874
ChemSpider
http://www.chemspider.com/Chemical-Structure.2485.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/58768-001-01
PharmGKB
http://www.pharmgkb.org/drug/PA164768736
Wikipedia
http://en.wikipedia.org/wiki/Carteolol
RxList
http://www.rxlist.com/cgi/generic2/carteol.htm
Drugs.com
http://www.drugs.com/cdi/carteolol-drops.html
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