Tìm theo
Oxprenolol
Các tên gọi khác (2) :
  • Oxprenolol
  • Oxprenololum
Thuốc chống lo âu, hoảng sợ
Thuốc Gốc
Small Molecule
CAS: 6452-71-7
ATC: C07AA02
CTHH: C15H23NO3
PTK: 265.348
A beta-adrenergic antagonist used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H23NO3
Phân tử khối
265.348
Monoisotopic mass
265.167793607
InChI
InChI=1S/C15H23NO3/c1-4-9-18-14-7-5-6-8-15(14)19-11-13(17)10-16-12(2)3/h4-8,12-13,16-17H,1,9-11H2,2-3H3
InChI Key
InChIKey=CEMAWMOMDPGJMB-UHFFFAOYSA-N
IUPAC Name
{2-hydroxy-3-[2-(prop-2-en-1-yloxy)phenoxy]propyl}(propan-2-yl)amine
Traditional IUPAC Name
oxprenolol
SMILES
CC(C)NCC(O)COC1=CC=CC=C1OCC=C
Độ hòa tan
6.80e-01 g/l
logP
2.10
logS
-2.6
pKa (strongest acidic)
14.09
pKa (Strongest Basic)
9.67
PSA
50.72 Å2
Refractivity
76 m3·mol-1
Polarizability
30.31 Å3
Rotatable Bond Count
9
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
caco2 Permeability
-4.68
Dược Lực Học : Oxprenolol is a non-selective beta blocker with some intrinsic sympathomimetic activity. Oxprenolol is a lipophilic beta blocker which passes the blood-brain barrier more easily than water soluble beta blockers. As such, it is associated with a higher incidence of CNS-related side effects than hydrophilic ligands such as atenolol, sotalol and nadolol. Oxprenolol is an potent beta-blocker and should not be administered to asthmatics because it can cause irreversible airway failure and inflammation.
Cơ Chế Tác Dụng : A beta-adrenergic antagonist used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety. [PubChem] Like other beta-adrenergic antagonists, oxprenolol competes with adrenergic neurotransmitters such as catecholamines for binding at sympathetic receptor sites. Like propranolol and timolol, oxprenolol binds at beta(1)-adrenergic receptors in the heart and vascular smooth muscle, inhibiting the effects of the catecholamines epinephrine and norepinephrine and decreasing heart rate, cardiac output, and systolic and diastolic blood pressure. It also blocks beta-2 adrenergic receptors located in bronchiole smooth muscle, causing vasoconstriction. By binding beta-2 receptors in the juxtaglomerular apparatus, oxprenolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production. Oxprenolol therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively.
Dược Động Học :
▧ Absorption :
Oral bioavailability is 20-70%.
▧ Metabolism :
Hepatic.
▧ Half Life :
1-2 hours
Độc Tính : Symptoms of overdose include abdominal irritation, central nervous system depression, coma, extremely slow heartbeat, heart failure, lethargy, low blood pressure, and wheezing.
Chỉ Định : Used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety.
Tương Tác Thuốc :
  • Acetohexamide The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
  • Chlorpropamide The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
  • Clonidine Increased hypertension when clonidine stopped
  • Dihydroergotamine Ischemia with risk of gangrene
  • Disopyramide The beta-blocker, oxprenolol, may increase the toxicity of disopyramide.
  • Epinephrine Hypertension, then bradycardia
  • Ergonovine Ischemia with risk of gangrene
  • Ergotamine Ischemia with risk of gangrene
  • Fenoterol Antagonism
  • Formoterol Antagonism
  • Gliclazide The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
  • Glipizide The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
  • Glisoxepide The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
  • Glyburide The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
  • Glycodiazine The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
  • Ibuprofen Risk of inhibition of renal prostaglandins
  • Indomethacin Risk of inhibition of renal prostaglandins
  • Insulin Glargine The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
  • Isoprenaline Antagonism
  • Lidocaine The beta-blocker increases the effect and toxicity of lidocaine
  • Methyldopa Possible hypertensive crisis
  • Methysergide Ischemia with risk of gangrene
  • Orciprenaline Antagonism
  • Pipobroman Antagonism
  • Pirbuterol Antagonism
  • Piroxicam Risk of inhibition of renal prostaglandins
  • Practolol Antagonism
  • Prazosin Risk of hypotension at the beginning of therapy
  • Repaglinide The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
  • Salbutamol Antagonism
  • Salmeterol Antagonism
  • Terazosin Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Terbutaline Antagonism
  • Tolazamide The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
  • Tolbutamide The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Verapamil Increased effect of both drugs
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Trasacor
  • Công ty :
    Sản phẩm biệt dược : Trasicor
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01580
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4631
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508996
ChemSpider
http://www.chemspider.com/Chemical-Structure.4470.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50240370
PharmGKB
http://www.pharmgkb.org/drug/PA10284
Wikipedia
http://en.wikipedia.org/wiki/Oxprenolol
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