Nadolol

Các tên gọi khác (1) :

Corgard

Thuốc Gốc

Small Molecule

CAS: 42200-33-9

ATC: C07AA12

ĐG : Apothecon , http://www.apothecon.nl

CTHH: C₁₇H₂₇NO₄

PTK: 309.4006

A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Nadolol is also used for migraine disorders and for tremor. [PubChem]

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₁₇H₂₇NO₄

Phân tử khối

309.4006

Monoisotopic mass

309.194008357

InChI

InChI=1S/C17H27NO4/c1-17(2,3)18-9-12(19)10-22-16-6-4-5-11-7-14(20)15(21)8-13(11)16/h4-6,12,14-15,18-21H,7-10H2,1-3H3/t12?,14-,15+/m1/s1

InChI Key

InChIKey=VWPOSFSPZNDTMJ-UCWKZMIHSA-N

IUPAC Name

(2R,3S)-5-[3-(tert-butylamino)-2-hydroxypropoxy]-1,2,3,4-tetrahydronaphthalene-2,3-diol

Traditional IUPAC Name

nadolol

SMILES

CC(C)(C)NCC(O)COC1=CC=CC2=C1C[C@H](O)[C@H](O)C2

Độ tan chảy

124-136 °C

Độ hòa tan

8330 mg/L (at 25 °C)

logP

0.81

logS

-2.1

pKa (strongest acidic)

13.59

pKa (Strongest Basic)

9.76

PSA

81.95 Å²

Refractivity

85.53 m³·mol^-1

Polarizability

34.63 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

-5.41

pKa

9.67

Dược Lực Học : Nadolol is a nonselective beta-adrenergic receptor antagonist with a long half-life, and is structurally similar to propranolol. Clinical pharmacology studies have demonstrated beta-blocking activity by showing (1) reduction in heart rate and cardiac output at rest and on exercise, (2) reduction of systolic and diastolic blood pressure at rest and on exercise, (3) inhibition of isoproterenol-induced tachycardia, and (4) reduction of reflex orthostatic tachycardia. Nadolol has no intrinsic sympathomimetic activity and, unlike some other beta-adrenergic blocking agents, nadolol has little direct myocardial depressant activity and does not have an anesthetic-like membrane-stabilizing action.

Cơ Chế Tác Dụng : A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Nadolol is also used for migraine disorders and for tremor. [PubChem] Like other beta-adrenergic antagonists, nadolol competes with adrenergic neurotransmitters such as catecholamines for binding at sympathetic receptor sites. Like propranolol and timolol, nadolol 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, nadolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production. Nadolol therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively.

Dược Động Học :

▧ Absorption :
Absorption of nadolol after oral dosing is variable, averaging about 30 percent.
▧ Protein binding :
30%
▧ Metabolism :
Not metabolized by the liver and excreted unchanged primarily by the kidneys.
▧ Route of Elimination :
Unlike many other beta-adrenergic blocking agents, nadolol is not metabolized by the liver and is excreted unchanged, principally by the kidneys. Nadolol is excreted predominantly in the urine.
▧ Half Life :
14-24 hours

Độc Tính : Oral, mouse: LD₅₀ = 4500mg/kg. 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 cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension.

Tương Tác Thuốc :

Acetohexamide The beta-blocker, nadolol, may decrease symptoms of hypoglycemia.
Aminophylline Antagonism of action and increased effect of theophylline
Chlorpropamide The beta-blocker, nadolol, may decrease symptoms of hypoglycemia.
Clonidine Increased hypertension when clonidine stopped
Dihydroergotamine Ischemia with risk of gangrene.
Disopyramide The beta-blocker, nadolol, 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, nadolol, may decrease symptoms of hypoglycemia.
Glipizide The beta-blocker, nadolol, may decrease symptoms of hypoglycemia.
Glisoxepide The beta-blocker, nadolol, may decrease symptoms of hypoglycemia.
Glyburide The beta-blocker, nadolol, may decrease symptoms of hypoglycemia.
Glycodiazine The beta-blocker, nadolol, may decrease symptoms of hypoglycemia.
Ibuprofen Risk of inhibition of renal prostaglandins
Indomethacin Risk of inhibition of renal prostaglandins
Insulin Glargine The beta-blocker, nadolol, may decrease symptoms of hypoglycemia.
Isoprenaline Antagonism
Lidocaine The beta-blocker, nadolol, may decrease symptoms of hypoglycemia.
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, nadolol, 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
Tolazamide The beta-blocker, nadolol, may decrease symptoms of hypoglycemia.
Tolbutamide The beta-blocker, nadolol, 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 : Naldol 80 mg tablet

Giá bán buôn : USD >1.03

Đơn vị tính : tablet
Biệt dược thương mại : Nadolol 40 mg tablet

Giá bán buôn : USD >1.07

Đơn vị tính : tablet
Biệt dược thương mại : Apo-Nadol 160 mg Tablet

Giá bán buôn : USD >1.26

Đơn vị tính : tablet
Biệt dược thương mại : Nadolol 80 mg tablet

Giá bán buôn : USD >1.45

Đơn vị tính : tablet
Biệt dược thương mại : Nadolol 160 mg tablet

Giá bán buôn : USD >2.25

Đơn vị tính : tablet
Biệt dược thương mại : Corgard 20 mg tablet

Giá bán buôn : USD >3.04

Đơn vị tính : tablet
Biệt dược thương mại : Corgard 40 mg tablet

Giá bán buôn : USD >3.11

Đơn vị tính : tablet
Biệt dược thương mại : Corgard 120 mg tablet

Giá bán buôn : USD >3.96

Đơn vị tính : tablet
Biệt dược thương mại : Corgard 80 mg tablet

Giá bán buôn : USD >4.33

Đơn vị tính : tablet
Biệt dược thương mại : Corgard 160 mg tablet

Giá bán buôn : USD >4.4

Đơn vị tính : tablet
Biệt dược thương mại : Nadolol powder

Giá bán buôn : USD >94.8

Đơn vị tính : g
Biệt dược thương mại : Apo-Nadol 40 mg Tablet

Giá bán buôn : USD >0.26

Đơn vị tính : tablet
Biệt dược thương mại : Novo-Nadolol 40 mg Tablet

Giá bán buôn : USD >0.26

Đơn vị tính : tablet
Biệt dược thương mại : Apo-Nadol 80 mg Tablet

Giá bán buôn : USD >0.37

Đơn vị tính : tablet
Biệt dược thương mại : Novo-Nadolol 80 mg Tablet

Giá bán buôn : USD >0.37

Đơn vị tính : tablet
Biệt dược thương mại : Nadolol 20 mg tablet

Giá bán buôn : USD >0.92

Đơn vị tính : tablet

Nhà Sản Xuất

Công ty :

Sản phẩm biệt dược : Anabet
Công ty :

Sản phẩm biệt dược : Corgard
Công ty :

Sản phẩm biệt dược : Solgol

Đóng gói

Công ty : Apothecon

Website : http://www.apothecon.nl
Công ty : Cardinal Health

Website : http://www.cardinal.com
Công ty : Dispensing Solutions

Website : http://www.drxdispensing.com
Công ty : Diversified Healthcare Services Inc.

Website : http://www.dhscorp.com
Công ty : E.R. Squibb and Sons LLC
Công ty : Emcure Pharmaceuticals Ltd.

Website : http://www.emcure.co.in
Công ty : Global Pharmaceuticals

Website : http://www.globalphar.com
Công ty : Impax Laboratories Inc.

Website : http://www.impaxlabs.com
Công ty : Ivax Pharmaceuticals
Công ty : King Pharmaceuticals Inc.

Website : http://www.kingpharm.com
Công ty : Major Pharmaceuticals

Website : http://www.majorpharmaceuticals.com
Công ty : Mead Johnson and Co.

Website : http://www.meadjohnson.com
Công ty : Murfreesboro Pharmaceutical Nursing Supply

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

Website : http://www.mylan.com
Công ty : Pharmaceutical Utilization Management Program VA Inc.
Công ty : Pharmedix

Website : http://www.pharmedixrx.com
Công ty : Physicians Total Care Inc.

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

Website : http://www.worldoftest.com
Công ty : Quality Care
Công ty : Resource Optimization and Innovation LLC
Công ty : Sandhills Packaging Inc.

Website : http://www.sandhillspackaging.com
Công ty : Sandoz

Website : http://www.sandoz.ca
Công ty : Teva Pharmaceutical Industries Ltd.

Website : http://www.tevapharm.com
Công ty : UDL Laboratories

Website : http://www.udllabs.com

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB01203

PubChem Compound

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=39147

PubChem Substance

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505509

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D00432

ChemSpider

http://www.chemspider.com/Chemical-Structure.35815.html

BindingDB

http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=25766

National Drug Code Directory

http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-0028-01

PharmGKB

http://www.pharmgkb.org/drug/PA450573

Wikipedia

http://en.wikipedia.org/wiki/Nadolol

RxList

http://www.rxlist.com/cgi/generic3/nadolol.htm

PDRhealth

http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/cor1102.shtml

Drugs.com

http://www.drugs.com/cdi/nadolol.html

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