Tìm theo
Acebutolol
Các tên gọi khác (9 ) :
  • (+-)-Acebutolol
  • (±)-acebutolol
  • 3'-acetyl-4'-(2-hydroxy-3-(isopropylamino)propoxy)butyranilide
  • 5'-butyramido-2'-(2-hydroxy-3-isopropylaminopropoxy)acetophenone
  • Acebutolol
  • Acebutololum
  • Acetobutolol
  • N-(3-Acetyl-4-[2-hydroxy-3-(isopropylamino)propoxy]phenyl)butanamide
  • N-[3-Acetyl-4-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]phenyl]butanamide
Thuốc tim mạch
Thuốc Gốc
Small Molecule
CAS: 37517-30-9
ATC: C07AB04
ĐG : Alphapharm Party Ltd. , http://www.alphapharm.com.au
CTHH: C18H28N2O4
PTK: 336.4259
A cardioselective beta-adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm as well as weak inherent sympathomimetic action. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H28N2O4
Phân tử khối
336.4259
Monoisotopic mass
336.204907394
InChI
InChI=1S/C18H28N2O4/c1-5-6-18(23)20-14-7-8-17(16(9-14)13(4)21)24-11-15(22)10-19-12(2)3/h7-9,12,15,19,22H,5-6,10-11H2,1-4H3,(H,20,23)
InChI Key
InChIKey=GOEMGAFJFRBGGG-UHFFFAOYSA-N
IUPAC Name
N-(3-acetyl-4-{2-hydroxy-3-[(propan-2-yl)amino]propoxy}phenyl)butanamide
Traditional IUPAC Name
acebutolol
SMILES
CCCC(=O)NC1=CC(C(C)=O)=C(OCC(O)CNC(C)C)C=C1
Độ tan chảy
136-138
Độ hòa tan
259 mg/L
logP
1.71
logS
-3.3
pKa (strongest acidic)
13.91
pKa (Strongest Basic)
9.57
PSA
87.66 Å2
Refractivity
94.87 m3·mol-1
Polarizability
38.51 Å3
Rotatable Bond Count
10
H Bond Acceptor Count
5
H Bond Donor Count
3
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
caco2 Permeability
-5.83
Dược Lực Học : Acebutolol is a cardioselective, beta-adrenoreceptor blocking agent, which possesses mild intrinsic sympathomimetic activity (ISA) in its therapeutically effective dose range. In general, beta-blockers reduce the work the heart has to do and allow it to beat more regularly. Acebutolol has less antagonistic effects on peripheral vascular ß2-receptors at rest and after epinephrine stimulation than nonselective beta-antagonists. Low doses of acebutolol produce less evidence of bronchoconstriction than nonselective agents like propranolol but more than atenolol.
Cơ Chế Tác Dụng : A cardioselective beta-adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm as well as weak inherent sympathomimetic action. [PubChem] Acebutolol is a selective β1-receptor antagonist. Activation of β1-receptors by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Acebutolol blocks these receptors, lowering the heart rate and blood pressure. This drug then has the reverse effect of epinephrine. In addition, beta blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels.
Dược Động Học :
▧ Absorption :
Well absorbed from the Gl tract with an absolute bioavailability of approximately 40% for the parent compound. In
▧ Protein binding :
26%
▧ Metabolism :
Subject to extensive first-pass hepatic biotransformation (primarily to diacetolol).
▧ Route of Elimination :
Elimination via renal excretion is approximately 30% to 40% and by non-renal mechanisms 50% to 60%, which includes excretion into the bile and direct passage through the intestinal wall.
▧ Half Life :
The plasma elimination half-life is approximately 3 to 4 hours. The half-life of its metabolite, diacetolol, is 8 to 13 hours.
Độc Tính : Symptoms of overdose include extreme bradycardia, advanced atrioventricular block, intraventricular conduction defects, hypotension, severe congestive heart failure, seizures, and in susceptible patients, bronchospasm, and hypoglycemia.
Chỉ Định : For the management of hypertension and ventricular premature beats in adults.
Tương Tác Thuốc :
  • Acetohexamide Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
  • Chlorpropamide Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
  • Clonidine Increased hypertension when clonidine stopped
  • Dihydroergotamine Ischemia with risk of gangrene
  • Disopyramide Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
  • Epinephrine Hypertension, then bradycardia
  • Ergonovine Ischemia with risk of gangrene
  • Ergotamine Ischemia with risk of gangrene
  • Fenoterol Antagonism
  • Formoterol Antagonism
  • Gliclazide Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
  • Glipizide Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
  • Glisoxepide The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
  • Glyburide Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
  • Ibuprofen Risk of inhibition of renal prostaglandins
  • Indacaterol Beta-adrenergic antagonists, especially those that are not cardioselective, may interfere with the effect of indacaterol when administered concurrently. Beta-blockers may exacerbate bronchospasms in patients with COPD.
  • Indomethacin Risk of inhibition of renal prostaglandins
  • Insulin Aspart The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
  • Insulin Detemir The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
  • Insulin Glargine The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
  • Insulin Glulisine The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
  • Insulin Lispro The beta-blocker, acebutolol, may decrease symptoms of hypoglycemia.
  • Isoprenaline Antagonism
  • Lidocaine The beta-blocker, acebutolol, may increase the effect and toxicity of lidocaine.
  • Methysergide Ischemia with risk of gangrene
  • Orciprenaline Antagonism
  • Pipobroman Antagonism
  • Pirbuterol Antagonism
  • Piroxicam Risk of inhibition of renal prostaglandins
  • Prazosin Risk of hypotension at the beginning of therapy
  • Repaglinide Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
  • Salmeterol Antagonism
  • Terazosin Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Terbutaline Antagonism
  • Tolazamide Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for hypoglycemia.
  • Tolbutamide Acebutolol may decrease symptoms of hypoglycemia and increase the time required for the body to compensate for 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
Giá thị trường
Nhà Sản Xuất
  • Công ty : Bayer
    Sản phẩm biệt dược : Prent
  • Công ty : Wyeth
    Sản phẩm biệt dược : Sectral
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01193
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=1978
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509113
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06803
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02338
ChemSpider
http://www.chemspider.com/Chemical-Structure.1901.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=25755
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-1200-01
PharmGKB
http://www.pharmgkb.org/drug/PA448011
Wikipedia
http://en.wikipedia.org/wiki/Acebutolol
RxList
http://www.rxlist.com/cgi/generic2/ace.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/sec1396.shtml
Drugs.com
http://www.drugs.com/cdi/acebutolol.html
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