Tìm theo
Pindolol
Các tên gọi khác (21 ) :
  • 1-(1H-indol-4-Yloxy)-3-(isopropylamino)propan-2-ol
  • 1-(1H-indol-4-Yloxy)-3-(propan-2-ylamino)-propan-2-ol
  • 1-(1H-indol-4-Yloxy)-3-[(1-methylethyl)amino]propan-2-ol
  • 4-(2-Hydroxy-3-isopropylaminopropoxy)-indole
  • Betapindol
  • Blockin L
  • Blocklin L
  • Blocklin-L
  • Calvisken
  • Cardilate
  • Carvisken
  • Decreten
  • Durapindol
  • Glauco-visken
  • Pectobloc
  • Pinbetol
  • Pindolol
  • Pindololum
  • Prinodolol
  • Pynastin
  • Visken
Thuốc Gốc
Small Molecule
CAS: 13523-86-9
ATC: C07AA03, C07AA14, C07AA17
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C14H20N2O2
PTK: 248.3208
A moderately lipophilic beta blocker (adrenergic beta-antagonists). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C14H20N2O2
Phân tử khối
248.3208
Monoisotopic mass
248.152477894
InChI
InChI=1S/C14H20N2O2/c1-10(2)16-8-11(17)9-18-14-5-3-4-13-12(14)6-7-15-13/h3-7,10-11,15-17H,8-9H2,1-2H3
InChI Key
InChIKey=JZQKKSLKJUAGIC-UHFFFAOYSA-N
IUPAC Name
[2-hydroxy-3-(1H-indol-4-yloxy)propyl](propan-2-yl)amine
Traditional IUPAC Name
pindolol
SMILES
CC(C)NCC(O)COC1=CC=CC2=C1C=CN2
Độ tan chảy
171 °C
Độ hòa tan
7880 mg/L
logP
1.75
logS
-2.5
pKa (strongest acidic)
14.09
pKa (Strongest Basic)
9.67
PSA
57.28 Å2
Refractivity
71.46 m3·mol-1
Polarizability
28.27 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
3
H Bond Donor Count
3
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
caco2 Permeability
-4.78
pKa
9.25
Dược Lực Học : Pindolol is a non-selective beta-adrenergic antagonist (beta-blocker) which possesses intrinsic sympathomimetic activity (ISA) in therapeutic dosage ranges but does not possess quinidine-like membrane stabilizing activity. Pindolol impairs AV node conduction and decreases sinus rate and may also increase plasma triglycerides and decrease HDL-cholesterol levels. Pindolol is nonpolar and hydrophobic, with low to moderate lipid solubility. Pindolol has little to no intrinsic sympathomimetic activity and, unlike some other beta-adrenergic blocking agents, pindolol has little direct myocardial depressant activity and does not have an anesthetic-like membrane-stabilizing action.
Cơ Chế Tác Dụng : A moderately lipophilic beta blocker (adrenergic beta-antagonists). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638) Pindolol non-selectively blocks beta-1 adrenergic receptors mainly in the heart, inhibiting the effects of epinephrine and norepinephrine resulting in a decrease in heart rate and blood pressure. By binding beta-2 receptors in the juxtaglomerular apparatus, Pindolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production and therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively.
Dược Động Học :
▧ Absorption :
Rapidly and reproducibly absorbed (bioavailability greater than 95%).
▧ Volume of Distribution :
* 2 L/kg
▧ Protein binding :
40%
▧ Metabolism :
Hepatic. In man, 35% to 40% is excreted unchanged in the urine and 60% to 65% is metabolized primarily to hydroxy-metabolites which are excreted as glucuronides and ethereal sulfates.
▧ Route of Elimination :
Pindolol undergoes extensive metabolism in animals and man. In man, 35% to 40% is excreted unchanged in the urine and 60% to 65% is metabolized primarily to hydroxy-metabolites which are excreted as glucuronides and ethereal sulfates. About 6% to 9% of an administered intravenous dose is excreted by the bile into the feces.
▧ Half Life :
3 to 4 hours
▧ Clearance :
* 50-300 mL/min [cirrhotic patients]
Độc Tính : LD50=263 mg/kg (orally in rats). Signs of overdose include excessive bradycardia, cardiac failure, hypotension, and bronchospasm.
Chỉ Định : For the management of hypertension, edema, ventricular tachycardias, and atrial fibrillation.
Tương Tác Thuốc :
  • Acetohexamide The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
  • Aminophylline Antagonism of action and increased effect of theophylline
  • Chlorpromazine Increased effect of both drugs
  • Chlorpropamide The beta-blocker, pindolol, 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, pindolol, may increase the toxicity of disopyramide.
  • Dyphylline Antagonism of action and increased effect of theophylline
  • Epinephrine Hypertension, then bradycardia
  • Ergonovine Ischemia with risk of gangrene
  • Ergotamine Ischemia with risk of gangrene
  • Fenoterol Antagonism
  • Formoterol Antagonism
  • Gliclazide The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
  • Glipizide The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
  • Glisoxepide The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
  • Glyburide The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
  • Glycodiazine The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
  • Ibuprofen Risk of inhibition of renal prostaglandins
  • Indomethacin Risk of inhibition of renal prostaglandins
  • Insulin Glargine The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
  • Isoprenaline Antagonism
  • Lidocaine The beta-blocker increases the effect and toxicity of lidocaine
  • Mesoridazine Increased risk of cardiotoxicity and arrhythmias
  • Methyldopa Possible hypertensive crisis
  • Methysergide Ischemia with risk of gangrene
  • Orciprenaline Antagonism
  • Oxtriphylline Antagonism of action and increased effect of theophylline
  • 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, pindolol, may decrease symptoms of hypoglycemia.
  • Salbutamol Antagonism
  • Salmeterol Antagonism
  • Terazosin Increased risk of hypotension. Initiate concomitant therapy cautiously.
  • Terbutaline Antagonism
  • Theophylline Antagonism of action and increased effect of theophylline
  • Thioridazine Increased risk of cardiotoxicity and arrhythmias
  • Tolazamide The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
  • Tolbutamide The beta-blocker, pindolol, 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
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Betapindol
  • Công ty :
    Sản phẩm biệt dược : Blockin L
  • Công ty :
    Sản phẩm biệt dược : Blocklin L
  • Công ty :
    Sản phẩm biệt dược : Calvisken
  • Công ty :
    Sản phẩm biệt dược : Decreten
  • Công ty :
    Sản phẩm biệt dược : Durapindol
  • Công ty :
    Sản phẩm biệt dược : Glauco-Visken
  • Công ty :
    Sản phẩm biệt dược : Pectobloc
  • Công ty :
    Sản phẩm biệt dược : Pinbetol
  • Công ty :
    Sản phẩm biệt dược : Prinodolol
  • Công ty :
    Sản phẩm biệt dược : Pynastin
  • Công ty :
    Sản phẩm biệt dược : Visken
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00960
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4828
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508362
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07445
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00513
ChemSpider
http://www.chemspider.com/Chemical-Structure.4662.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-0052-01
PharmGKB
http://www.pharmgkb.org/drug/PA450966
Wikipedia
http://en.wikipedia.org/wiki/Pindolol
RxList
http://www.rxlist.com/cgi/generic3/pindolol.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/pin1611.shtml
Drugs.com
http://www.drugs.com/cdi/pindolol.html
... loading
... loading