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

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

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

Biệt dược thương mại : Pindolol 10 mg tablet

Giá bán buôn : USD >1.0

Đơn vị tính : tablet
Biệt dược thương mại : Visken 10 mg Tablet

Giá bán buôn : USD >1.05

Đơn vị tính : tablet
Biệt dược thương mại : Visken 15 mg Tablet

Giá bán buôn : USD >1.52

Đơn vị tính : tablet
Biệt dược thương mại : Apo-Pindol 5 mg Tablet

Giá bán buôn : USD >0.24

Đơn vị tính : tablet
Biệt dược thương mại : Gen-Pindolol 5 mg Tablet

Giá bán buôn : USD >0.24

Đơn vị tính : tablet
Biệt dược thương mại : Novo-Pindol 5 mg Tablet

Giá bán buôn : USD >0.24

Đơn vị tính : tablet
Biệt dược thương mại : Nu-Pindol 5 mg Tablet

Giá bán buôn : USD >0.24

Đơn vị tính : tablet
Biệt dược thương mại : Pms-Pindolol 5 mg Tablet

Giá bán buôn : USD >0.24

Đơn vị tính : tablet
Biệt dược thương mại : Sandoz Pindolol 5 mg Tablet

Giá bán buôn : USD >0.24

Đơn vị tính : tablet
Biệt dược thương mại : Apo-Pindol 10 mg Tablet

Giá bán buôn : USD >0.42

Đơn vị tính : tablet
Biệt dược thương mại : Gen-Pindolol 10 mg Tablet

Giá bán buôn : USD >0.42

Đơn vị tính : tablet
Biệt dược thương mại : Novo-Pindol 10 mg Tablet

Giá bán buôn : USD >0.42

Đơn vị tính : tablet
Biệt dược thương mại : Nu-Pindol 10 mg Tablet

Giá bán buôn : USD >0.42

Đơn vị tính : tablet
Biệt dược thương mại : Pms-Pindolol 10 mg Tablet

Giá bán buôn : USD >0.42

Đơn vị tính : tablet
Biệt dược thương mại : Sandoz Pindolol 10 mg Tablet

Giá bán buôn : USD >0.42

Đơn vị tính : tablet
Biệt dược thương mại : Apo-Pindol 15 mg Tablet

Giá bán buôn : USD >0.61

Đơn vị tính : tablet
Biệt dược thương mại : Gen-Pindolol 15 mg Tablet

Giá bán buôn : USD >0.61

Đơn vị tính : tablet
Biệt dược thương mại : Novo-Pindol 15 mg Tablet

Giá bán buôn : USD >0.61

Đơn vị tính : tablet
Biệt dược thương mại : Nu-Pindol 15 mg Tablet

Giá bán buôn : USD >0.61

Đơn vị tính : tablet
Biệt dược thương mại : Pms-Pindolol 15 mg Tablet

Giá bán buôn : USD >0.61

Đơn vị tính : tablet
Biệt dược thương mại : Sandoz Pindolol 15 mg Tablet

Giá bán buôn : USD >0.61

Đơn vị tính : tablet
Biệt dược thương mại : Visken 5 mg Tablet

Giá bán buôn : USD >0.61

Đơn vị tính : tablet
Biệt dược thương mại : Pindolol 5 mg tablet

Giá bán buôn : USD >0.73

Đơn vị tính : tablet

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

Công ty : Advanced Pharmaceutical Services Inc.
Công ty : Ivax Pharmaceuticals
Công ty : Major Pharmaceuticals

Website : http://www.majorpharmaceuticals.com
Công ty : Merckle GmbH

Website : http://www.merckle.de
Công ty : Murfreesboro Pharmaceutical Nursing Supply

Website : http://www.unitdosesupply.com
Công ty : Mylan

Website : http://www.mylan.com
Công ty : Novartis AG

Website : http://www.novartis.com
Công ty : Novopharm Ltd.
Công ty : Pharmaceutical Utilization Management Program VA Inc.
Công ty : Physicians Total Care Inc.

Website : http://www.physicianstotalcare.com
Công ty : Qualitest

Website : http://www.worldoftest.com
Công ty : Sandhills Packaging Inc.

Website : http://www.sandhillspackaging.com

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

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