WordNet

a beta-adrenergic blocking agent (trade name Corgard) that is used to treat hypertension and angina (同)Corgard

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/12/03 19:40:24」(JST)

wiki en

Nadolol (Corgard) is a non-selective beta blocker used in the treatment of high blood pressure and chest pain. Additionally, it is often prescribed in the treatment of atrial fibrillation, migraine headaches, and complications of cirrhosis.

Medical uses

Nadolol is used to treat hypertension and for long-term treatment of angina pectoris and is approved by the FDA for these purposes.^[1]

It is regularly used off-label^[1] for control of heart rate in people with atrial fibrillation,^[2] prevention of migraine headaches;^[3] prevention of bleeding veins in people with portal hypertension caused by cirrhosis;^[4] and to treat people with high levels of thyroid hormone.^[5]

Nadolol is one of the preferred beta-blockers in the management of patients with LQTS for shortening of the QT interval and prevention of ventricular arrhythmia. It is more efficacious than metoprolol in the prevention of breakthrough cardiac events while on therapy and is equivalent to propranolol.^[6] Nadolol has the advantage of once daily dosing and thus improved patient compliance. For patients with decreased renal function, nadolol may be dosed less often.^[7] It has also been found to be useful (off-label) for several neurological disorders such as the prevention of migraine attacks,^[8] attention deficit/hyperactivity disorder(ADHD)^[9]^[10]^[11] and its use has been explored as a treatment for essential tremor^[12] and Parkinson's disease^[13] but neither is well established.^[14]^[15]^[16]

Side effects

The most common side effects include dizziness and fatigue.^[13]

Contraindications

Nadolol and other beta blockers should be used with cautions in people with heart failure and its use should not be abruptly stopped. It is contraindicated for people with asthma, a slow heart rate and certain severe heart problems.^[17]

Mechanism of action

Nadolol is a non-selective beta blocker; that is, it non-selectively blocks both beta-1 and beta-2 receptors. It has a preference for beta-1 receptors, which are predominantly located in the heart, thereby inhibiting the effects of catecholamines and causing a decrease in heart rate and blood pressure. Its inhibition of beta-2 receptors, which are mainly located in the bronchial smooth muscle of the airways, leads to airway constriction similar to that seen in asthma. Inhibition of beta-1 receptors in the juxtaglomerular apparatus of the kidney inhibits the renin-angiotensin system, causing a decrease in vasoconstriction and a decrease in water retention. Nadolol's inhibition of beta-1 receptors in the heart and kidney leads to its effects on lowering blood pressure.

The drug impairs AV node conduction and decreases sinus rate.

Nadolol may also increase plasma triglycerides and decrease HDL-cholesterol levels.

Chemistry

Nadolol is a mixture of stereoisomers. It is polar and hydrophilic, with low lipid solubility.^[18]

Four stereoisomers of nadolol

References

^ ^a ^b Nadolol entry in AccessMedicine. McGraw-Hill Global Education Holdings, LLC. Accessed November 8, 2014
^ January CT, et al 2014 AHA/ACC/HRS Guideline for the Management of Patients With Atrial Fibrillation: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines and the Heart Rhythm Society. Circulation. 2014 Apr 10. PMID 24682347
^ Silberstein SD et al. Evidence-based guideline update: pharmacologic treatment for episodic migraine prevention in adults: report of the Quality Standards Subcommittee of the American Academy of Neurology and the American Headache Society. Neurology. 2012 Apr 24;78(17):1337-45. PMID 22529202 PMC 3335452
^ Giannelli V et al. Beta-blockers in liver cirrhosis. Ann Gastroenterol. 2014;27(1):20-26. PMID 24714633 PMC 3959530
^ Bahn RS et al, “Hyperthyroidism and Other Causes of Thyrotoxicosis: Management Guidelines of the American Thyroid Association and American Association of Clinical Endocrinologists,” Thyroid, 2011, 21(6):593-646. PMID 21510801
^ Chockalingam, P; Crotti, L; Girardengo, G; Johnson, JN; Harris, KM; van der Heijden, JF; Hauer, RN; Beckmann, BM; Spazzolini, C; Rordorf, R; Rydberg, A; Clur, SA; Fischer, M; van den Heuvel, F; Kääb, S; Blom, NA; Ackerman, MJ; Schwartz, PJ; Wilde, AA (Nov 13, 2012). "Not all beta-blockers are equal in the management of long QT syndrome types 1 and 2: higher recurrence of events under metoprolol". Journal of the American College of Cardiology 60 (20): 2092–9. doi:10.1016/j.jacc.2012.07.046. PMID 23083782.
^ http://reference.medscape.com/drug/corgard-nadolol-342361
^ http://patient.info/medicine/nadolol-a-beta-blocker-corgard
^ https://books.google.com/books?id=EkyTTvjNRZAC&pg=PA669&lpg=PA669&dq=Nadolol+for+ADHD&source=bl&ots=AHBVTAhCwv&sig=w0nW8Plyub3GN87J7itGz1fB11Y&hl=en&sa=X&ei=UAjRVMWkJoatyQSDzoDQCA&ved=0CFEQ6AEwBTgK#v=onepage&q=Nadolol%20for%20ADHD&f=false
^ http://psychcentral.com/disorders/sx1t.htm
^ http://www.doctorshangout.com/profiles/blogs/nadolol-nonselective-long-acting-beta-blocker
^ Zesiewicz TA et al. Evidence-based guideline update: treatment of essential tremor: report of the Quality Standards subcommittee of the American Academy of Neurology. Neurology. 2011 Nov 8;77(19):1752-5. PMID 22013182 PMC 3208950
^ ^a ^b U.S. National Library of Medicine Nadolol entry in Medline Plus
^ http://onlinelibrary.wiley.com/doi/10.1002/ana.410160412/abstract
^ http://www.nlm.nih.gov/medlineplus/druginfo/meds/a682666.html
^ http://www.drugs.com/dosage/nadolol.html
^ Corgard Label
^ Bragg W et al. Optimized separation of beta-blockers with multiple chiral centers using capillary electrochromatography-mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Nov 1;875(1):304-16. PMID 18619928 PMC 2680439

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 肝硬変患者における静脈瘤出血に対する一次予防および静脈瘤形成予防 primary and pre primary prophylaxis against variceal hemorrhage in patients with cirrhosis
2. β遮断剤の主な副作用 major side effects of beta blockers
3. 肝硬変患者における静脈瘤出血再発の防止 prevention of recurrent variceal hemorrhage in patients with cirrhosis
4. 成人における片頭痛の予防的治療 preventive treatment of migraine in adults
5. 本態性振戦の薬理学的治療 pharmacologic treatment of essential tremor

English Journal

Three column intermittent simulated moving bed chromatography: 3. Cascade operation for center-cut separations.

Jermann S1, Meijssen M1, Mazzotti M2.
Journal of chromatography. A.J Chromatogr A.2015 Jan 23;1378:37-49. doi: 10.1016/j.chroma.2014.12.011. Epub 2014 Dec 16.
A general design methodology for chromatographic three fraction separation by application of the three column intermittent simulated moving bed (3C-ISMB) cascade is proposed and experimentally validated by studying the purification of an intermediately retained stereoisomer of nadolol, from an equim
PMID 25560452

Nasal IgA secretion in a murine model of acute stress. The possible role of catecholamines.

Jarillo-Luna RA1, Rivera-Aguilar V2, Pacheco-Yépez J3, Godínez-Victoria M3, Oros-Pantoja R4, Miliar-García A3, Campos-Rodríguez R3.
Journal of neuroimmunology.J Neuroimmunol.2015 Jan 15;278C:223-231. doi: 10.1016/j.jneuroim.2014.11.009. Epub 2014 Nov 13.
Stress stimuli affect the immune system of the mucosa, and in particular IgA secretion. It is well documented that intense psychological and physical stress can increase susceptibility to infection by diverse pathogens in the upper respiratory tract. Our workgroup reported that chronic stress caused
PMID 25468772

Nadolol for the treatment of infantile hemangioma.

Villalba-Moreno AM1, Cotrina-Luque J2, Del Vayo-Benito CA2, Flores-Moreno S2, Bautista-Paloma FJ2.
American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists.Am J Health Syst Pharm.2015 Jan 1;72(1):44-6. doi: 10.2146/ajhp140097.
PURPOSE: The successful use of nadolol as an alternative to propranolol therapy in three cases of infantile hemangioma is reported.SUMMARY: Infantile hemangioma is a benign vascular neoplastic disorder that affects up to 10% of newborns and can lead to deformity or local complications in severe case
PMID 25511837

Japanese Journal

A placebo-contorolled clinical trial of Nadolol in the prophylaxis of growth of esophageal varices inchirrhosis

MERKRL C
Gastroenterology 127, 476-484, 2004
NAID 30022999057

Vasovagal syncope : a prospective, randomized, crossover evaluation of the effect of propranolol, nadolol and placebo on syncope recurrence and patients' well-being

FLEVARI P
J Am Coll Cardiol 40, 499-504, 2002
NAID 30008089091

Related Pictures

★リンクテーブル★

リンク元

「ナドロール」

Nadolol
Systematic (IUPAC) name
	* rel-(2R,3S)-5-{[(2R)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-1,2,3,4-tetrahydronaphthalene-2,3-diol (2R,3S)-5-{[(2R*)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-1,2,3,4-tetrahydronaphthalene-2,3-diol;
Clinical data
Trade names	Corgard
AHFS/Drugs.com	monograph
MedlinePlus	a682666
Pregnancy; category	US: C (Risk not ruled out); ;
Legal status	UK: POM (Prescription only); US: ℞-only;
Routes of; administration	Oral
Pharmacokinetic data
Protein binding	30%
Metabolism	Nil
Biological half-life	14-24 hours
Excretion	Renal and fecal (unchanged)
Identifiers
CAS Number	42200-33-9
ATC code	C07AA12
PubChem	CID: 39147
IUPHAR/BPS	554
DrugBank	DB01203
ChemSpider	35815
UNII	FEN504330V
KEGG	D00432
ChEMBL	CHEMBL649
Chemical data
Formula	C17H27NO4
Molecular mass	309.401 g/mol
	SMILES OC(CNC(C)(C)C)COc1cccc2c1C[C@H](O)[C@H](O)C2 ;
	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 ; Key:VWPOSFSPZNDTMJ-UCWKZMIHSA-N ;
(what is this?) (verify)

　　[★]

英: nadolol
商: Corgard。ナディック

[AccessMedNadolol-1] Nadolol entry in AccessMedicine. McGraw-Hill Global Education Holdings, LLC. Accessed November 8, 2014

[2] January CT, et al 2014 AHA/ACC/HRS Guideline for the Management of Patients With Atrial Fibrillation: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines and the Heart Rhythm Society. Circulation. 2014 Apr 10. PMID 24682347

[3] Silberstein SD et al. Evidence-based guideline update: pharmacologic treatment for episodic migraine prevention in adults: report of the Quality Standards Subcommittee of the American Academy of Neurology and the American Headache Society. Neurology. 2012 Apr 24;78(17):1337-45. PMID 22529202 PMC 3335452

[4] Giannelli V et al. Beta-blockers in liver cirrhosis. Ann Gastroenterol. 2014;27(1):20-26. PMID 24714633 PMC 3959530

[5] Bahn RS et al, “Hyperthyroidism and Other Causes of Thyrotoxicosis: Management Guidelines of the American Thyroid Association and American Association of Clinical Endocrinologists,” Thyroid, 2011, 21(6):593-646. PMID 21510801

[6] Chockalingam, P; Crotti, L; Girardengo, G; Johnson, JN; Harris, KM; van der Heijden, JF; Hauer, RN; Beckmann, BM; Spazzolini, C; Rordorf, R; Rydberg, A; Clur, SA; Fischer, M; van den Heuvel, F; Kääb, S; Blom, NA; Ackerman, MJ; Schwartz, PJ; Wilde, AA (Nov 13, 2012). "Not all beta-blockers are equal in the management of long QT syndrome types 1 and 2: higher recurrence of events under metoprolol". Journal of the American College of Cardiology 60 (20): 2092–9. doi:10.1016/j.jacc.2012.07.046. PMID 23083782.

[7] ttp://reference.medscape.com/drug/corgard-nadolol-342361

[8] ttp://patient.info/medicine/nadolol-a-beta-blocker-corgard

[9] ttps://books.google.com/books?id=EkyTTvjNRZAC&pg=PA669&lpg=PA669&dq=Nadolol+for+ADHD&source=bl&ots=AHBVTAhCwv&sig=w0nW8Plyub3GN87J7itGz1fB11Y&hl=en&sa=X&ei=UAjRVMWkJoatyQSDzoDQCA&ved=0CFEQ6AEwBTgK#v=onepage&q=Nadolol%20for%20ADHD&f=false

[10] ttp://psychcentral.com/disorders/sx1t.htm

[11] ttp://www.doctorshangout.com/profiles/blogs/nadolol-nonselective-long-acting-beta-blocker

[12] Zesiewicz TA et al. Evidence-based guideline update: treatment of essential tremor: report of the Quality Standards subcommittee of the American Academy of Neurology. Neurology. 2011 Nov 8;77(19):1752-5. PMID 22013182 PMC 3208950

[MedlinePlus-13] U.S. National Library of Medicine Nadolol entry in Medline Plus

[14] ttp://onlinelibrary.wiley.com/doi/10.1002/ana.410160412/abstract

[15] ttp://www.nlm.nih.gov/medlineplus/druginfo/meds/a682666.html

[16] ttp://www.drugs.com/dosage/nadolol.html

[Label-17] Corgard Label

[18] Bragg W et al. Optimized separation of beta-blockers with multiple chiral centers using capillary electrochromatography-mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Nov 1;875(1):304-16. PMID 18619928 PMC 2680439

匿名

検索

案内

案内

nadolol