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Atenolol
Các tên gọi khác (4 ) :
  • 1-p-Carbamoylmethylphenoxy-3-isopropylamino-2-propanol
  • 2-(p-(2-Hydroxy-3-(isopropylamino)propoxy)phenyl)acetamide
  • 4-(2-Hydroxy-3-((1-methylethyl)amino)propoxy)benzeneacetamide
  • Atenololum
Thuốc tim mạch
Thuốc Gốc
Small Molecule
CAS: 29122-68-7
ATC: C07AB03, C07AB11
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C14H22N2O3
PTK: 266.3361
A cardioselective beta-adrenergic blocker possessing properties and potency similar to propranolol, but without a negative inotropic effect. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C14H22N2O3
Phân tử khối
266.3361
Monoisotopic mass
266.16304258
InChI
InChI=1S/C14H22N2O3/c1-10(2)16-8-12(17)9-19-13-5-3-11(4-6-13)7-14(15)18/h3-6,10,12,16-17H,7-9H2,1-2H3,(H2,15,18)
InChI Key
InChIKey=METKIMKYRPQLGS-UHFFFAOYSA-N
IUPAC Name
2-(4-{2-hydroxy-3-[(propan-2-yl)amino]propoxy}phenyl)acetamide
Traditional IUPAC Name
atenolol
SMILES
CC(C)NCC(O)COC1=CC=C(CC(N)=O)C=C1
Độ tan chảy
158-160
Độ hòa tan
1.33E+004 mg/L (at 25 °C)
logP
0.16
logS
-2.8
pKa (strongest acidic)
14.08
pKa (Strongest Basic)
9.67
PSA
84.58 Å2
Refractivity
73.51 m3·mol-1
Polarizability
29.98 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
4
H Bond Donor Count
3
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
caco2 Permeability
-6.44
pKa
9.6
Dược Lực Học : Atenolol, a competitive beta(1)-selective adrenergic antagonist, has the lowest lipid solubility of this drug class. Although it is similar to metoprolol, atenolol differs from pindolol and propranolol in that it does not have intrinsic sympathomimetic properties or membrane-stabilizing activity. Atenolol is used alone or with chlorthalidone in the management of hypertension and edema.
Cơ Chế Tác Dụng : A cardioselective beta-adrenergic blocker possessing properties and potency similar to propranolol, but without a negative inotropic effect. [PubChem] Like metoprolol, atenolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart and vascular smooth muscle, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension. Higher doses of atenolol also competitively block beta(2)-adrenergic responses in the bronchial and vascular smooth muscles.
Dược Động Học :
▧ Absorption :
Approximately 50% of an oral dose is absorbed from the gastrointestinal tract, the remainder being excreted unchanged in the feces.
▧ Protein binding :
Plasma protein binding is 6-16%
▧ Metabolism :
Hepatic (minimal)
▧ Route of Elimination :
Approximately 50% of an oral dose is absorbed from the gastrointestinal tract, the remainder being excreted unchanged in the feces. Unlike propranolol or metoprolol, but like nadolol, atenolol undergoes little or no metabolism by the liver, and the absorbed portion is eliminated primarily by renal excretion.
▧ Half Life :
6-7 hours
Độc Tính : LD50=2000-3000 mg/kg(orally in mice). Symptoms of an atenolol overdose include a slow heart beat, shortness of breath, fainting, dizziness, weakness, confusion, nausea, and vomiting.
Chỉ Định : For the management of hypertention and long-term management of patients with angina pectoris
Tương Tác Thuốc :
  • Acetohexamide The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
  • Ampicillin Ampicillin decreases bioavailability of atenolol
  • Chlorpropamide The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
  • Clonidine Increased hypertension when clonidine stopped
  • Dihydroergotamine Ischemia with risk of gangrene
  • Diltiazem Increased risk of bradycardia
  • Disopyramide The beta-blocker, atenolol, may increase the toxicity of disopyramide.
  • Epinephrine Hypertension, then bradycardia
  • Ergonovine Ischmeia with risk of gangrene
  • Ergotamine Ischemia with risk of gangrene
  • Fenoterol Antagonism
  • Formoterol Antagonism
  • Gliclazide The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
  • Glipizide The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
  • Glisoxepide The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
  • Glyburide The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
  • Glycodiazine The beta-blocker, atenolol, may decrease symptoms of 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, atenolol, may decrease symptoms of hypoglycemia.
  • Insulin Detemir The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
  • Insulin Glargine The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
  • Insulin Glulisine The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
  • Insulin Lispro The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
  • Isoprenaline Antagonism
  • Lidocaine The beta-blocker, atenolol, 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
  • Procaterol Antagonism
  • Repaglinide The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
  • Salbutamol Antagonism
  • Salmeterol Antagonism
  • Terazosin Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Terbutaline Antagonism
  • Tolazamide The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
  • Tolbutamide The beta-blocker, atenolol, 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 : Injection - Intravenous - 0.5 mg/ml
Tablet - Oral - 25 mg, 50 mg, 100 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Ivax
    Sản phẩm biệt dược : Myocord
  • Công ty : Teva
    Sản phẩm biệt dược : Normiten
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Tenormin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00335
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2249
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506915
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00235
ChemSpider
http://www.chemspider.com/Chemical-Structure.2162.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=25753
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/65862-168-01
PharmGKB
http://www.pharmgkb.org/drug/PA448499
Wikipedia
http://en.wikipedia.org/wiki/Atenolol
RxList
http://www.rxlist.com/cgi/generic/atenolol.htm
Drugs.com
http://www.drugs.com/atenolol.html
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