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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2018/03/03 20:45:45」(JST)

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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.

Chemistry

Nadolol is a mixture of stereoisomers. It is polar and hydrophilic, with low lipid solubility.^[1]

Four stereoisomers of nadolol

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.^[2]

It is regularly used off-label^[2] for control of heart rate in people with atrial fibrillation,^[3] prevention of migraine headaches;^[4] prevention of bleeding veins in people with portal hypertension caused by cirrhosis;^[5] and to treat people with high levels of thyroid hormone.^[6]

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.^[7] Nadolol has the advantage of once daily dosing and thus improved patient compliance. For patients with decreased kidney function, nadolol may be dosed less often.^[8] It has also been found to be useful (off-label) for several neurological disorders such as the prevention of migraine attacks,^[9] attention deficit/hyperactivity disorder(ADHD)^[10] and its use has been explored as a treatment for essential tremor^[11] and Parkinson's disease^[12] but neither is well established.^[13]^[14]^[15]

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.^{[citation needed]}

Side effects

The most common side effects include dizziness and fatigue.^[12]

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.^[16]

References

^ Bragg W, Norton D, Shamsi SA (November 2008). "Optimized separation of beta-blockers with multiple chiral centers using capillary electrochromatography-mass spectrometry". J Chromatogr B. 875 (1): 304–16. doi:10.1016/j.jchromb.2008.06.028. PMC 2680439 . PMID 18619928.
^ ^a ^b Nadolol entry in AccessMedicine. McGraw-Hill Global Education Holdings, LLC. Accessed 8 November 2014
^ January CT, Wann LS, Alpert JS, Calkins H, Cigarroa JE, 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. 130: e199–267. doi:10.1161/CIR.0000000000000041. PMC 4676081 . PMID 24682347.
^ Silberstein SD, Holland S, Freitag F, Dodick DW, Argoff C, et al. (2012). "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. 78 (17): 1337–45. doi:10.1212/WNL.0b013e3182535d20. PMC 3335452 . PMID 22529202.
^ Giannelli V, Lattanzi B, Thalheimer U, Merli M. "Beta-blockers in liver cirrhosis". Ann Gastroenterol. 27 (1): 20–26. PMC 3959530 . PMID 24714633.
^ Bahn RS, Burch HB, Cooper DS, Garber JR, Greenlee MC, et al. (2011). "Hyperthyroidism and Other Causes of Thyrotoxicosis: Management Guidelines of the American Thyroid Association and American Association of Clinical Endocrinologists". Thyroid. 21 (6): 593–646. doi:10.1089/thy.2010.0417. PMID 21510801.
^ Chockalingam P, Crotti L, Girardengo G, Johnson JN, Harris KM, et al. (13 November 2012). "Not all beta-blockers are equal in the management of long QT syndrome types 1 and 2: higher recurrence of events under metoprolol". J Am Coll Cardiol. 60 (20): 2092–9. doi:10.1016/j.jacc.2012.07.046. PMC 3515779 . PMID 23083782.
^ "Corgard (nadolol) dosing, indications, interactions, adverse effects, and more". reference.medscape.com. Retrieved 27 May 2017.
^ "Nadolol - a beta-blocker - Corgard. High blood pressure drugs". patient.info. Retrieved 27 May 2017.
^ Barkley, Russell A.; Murphy, Kevin R. (27 May 2017). "Attention-deficit Hyperactivity Disorder: A Clinical Workbook". Guilford Press. Retrieved 27 May 2017 – via Google Books.
^ Zesiewicz TA, Elble RJ, Louis ED, Gronseth GS, Ondo WG, et al. (Nov 2011). "Evidence-based guideline update: treatment of essential tremor: report of the Quality Standards subcommittee of the American Academy of Neurology". Neurology. 77 (19): 1752–5. doi:10.1212/WNL.0b013e318236f0fd. PMC 3208950 . PMID 22013182.
^ ^a ^b U.S. National Library of Medicine Nadolol entry in Medline Plus
^ Foster NL, Newman RP, Lewitt PA, Gillespie MM, Larsen TA, et al. (October 1984). "Peripheral beta-adrenergic blockade treatment of parkinsonian tremor". Ann Neurol. 16: 505–508. doi:10.1002/ana.410160412.
^ "Nadolol: MedlinePlus Drug Information". www.nlm.nih.gov. Retrieved 27 May 2017.
^ "Nadolol Dosage Guide with Precautions - Drugs.com". drugs.com. Retrieved 27 May 2017.
^ "Corgard Label" (PDF). fda.gov. Retrieved 27 May 2017.

UpToDate Contents

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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. 本態性振戦の薬理学的治療 pharmacologic treatment of essential tremor
5. 慢性片頭痛 chronic migraine

English Journal

Effects of 18 pharmaceuticals on the physiological diversity of edaphic microorganisms.

Pino-Otín MR1, Muñiz S2, Val J3, Navarro E4.
The Science of the total environment.Sci Total Environ.2017 Oct 1;595:441-450. doi: 10.1016/j.scitotenv.2017.04.002. Epub 2017 Apr 7.
PMID 28395259

Determination of Some β-Blockers and β2-Agonists in Plasma and Urine Using Liquid Chromatography-tandem Mass Spectrometry and Solid Phase Extraction.

Salem AA1, Wasfi I2, Al-Nassib SS1, Allawy Mohsin M3, Al-Katheeri N2.
Journal of chromatographic science.J Chromatogr Sci.2017 Sep 1;55(8):846-856. doi: 10.1093/chromsci/bmx045.
PMID 28633284

β1 -Adrenoceptor, but not β2 -adrenoceptor, subtype regulates heart rate in type 2 diabetic rats in vivo.

Cook RF1, Bussey CT1, Mellor KM2, Cragg PA1, Lamberts RR1.
Experimental physiology.Exp Physiol.2017 Aug 1;102(8):911-923. doi: 10.1113/EP086293. Epub 2017 Jun 9.
PMID 28543947

Japanese Journal

βしゃ断剤の運動負荷時血行動態に及ぼす作用と血中濃度との関係　　ＮａｄｏｌｏｌとＰｒｏｐｒａｎｏｌｏｌとの比較:NadololとPropranololとの比較

臨床薬理 15(3), 407-416, 1984
NAID 130002047586

Related Pictures

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★リンクテーブル★

リンク元

「ナドロール」

Nadolol
Clinical data
Trade names	Corgard
AHFS/Drugs.com	Monograph
MedlinePlus	a682666
Pregnancy; category	US: C (Risk not ruled out); ;
Routes of; administration	Oral
ATC code	C07AA12 (WHO);
Legal status
Legal status	UK: POM (Prescription only); US: ℞-only;
Pharmacokinetic data
Protein binding	30%
Metabolism	Nil
Biological half-life	14-24 hours
Excretion	Renal and fecal (unchanged)
Identifiers
	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; ;
CAS Number	42200-33-9 ;
PubChem CID	39147;
IUPHAR/BPS	554;
DrugBank	DB01203 ;
ChemSpider	35815 ;
UNII	FEN504330V;
KEGG	D00432 ;
ChEMBL	CHEMBL649 ;
ECHA InfoCard	100.050.625
Chemical and physical data
Formula	C17H27NO4
Molar mass	309.401 g/mol
3D model (JSmol)	Interactive image;
	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 ;
(verify)

　　[★]

英: nadolol
商: Corgard。ナディック

[1] Bragg W, Norton D, Shamsi SA (November 2008). "Optimized separation of beta-blockers with multiple chiral centers using capillary electrochromatography-mass spectrometry". J Chromatogr B. 875 (1): 304–16. doi:10.1016/j.jchromb.2008.06.028. PMC 2680439 . PMID 18619928.

[AccessMedNadolol-2] Nadolol entry in AccessMedicine. McGraw-Hill Global Education Holdings, LLC. Accessed 8 November 2014

[3] January CT, Wann LS, Alpert JS, Calkins H, Cigarroa JE, 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. 130: e199–267. doi:10.1161/CIR.0000000000000041. PMC 4676081 . PMID 24682347.

[4] Silberstein SD, Holland S, Freitag F, Dodick DW, Argoff C, et al. (2012). "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. 78 (17): 1337–45. doi:10.1212/WNL.0b013e3182535d20. PMC 3335452 . PMID 22529202.

[5] Giannelli V, Lattanzi B, Thalheimer U, Merli M. "Beta-blockers in liver cirrhosis". Ann Gastroenterol. 27 (1): 20–26. PMC 3959530 . PMID 24714633.

[6] Bahn RS, Burch HB, Cooper DS, Garber JR, Greenlee MC, et al. (2011). "Hyperthyroidism and Other Causes of Thyrotoxicosis: Management Guidelines of the American Thyroid Association and American Association of Clinical Endocrinologists". Thyroid. 21 (6): 593–646. doi:10.1089/thy.2010.0417. PMID 21510801.

[7] Chockalingam P, Crotti L, Girardengo G, Johnson JN, Harris KM, et al. (13 November 2012). "Not all beta-blockers are equal in the management of long QT syndrome types 1 and 2: higher recurrence of events under metoprolol". J Am Coll Cardiol. 60 (20): 2092–9. doi:10.1016/j.jacc.2012.07.046. PMC 3515779 . PMID 23083782.

[8] "Corgard (nadolol) dosing, indications, interactions, adverse effects, and more". reference.medscape.com. Retrieved 27 May 2017.

[9] "Nadolol - a beta-blocker - Corgard. High blood pressure drugs". patient.info. Retrieved 27 May 2017.

[10] Barkley, Russell A.; Murphy, Kevin R. (27 May 2017). "Attention-deficit Hyperactivity Disorder: A Clinical Workbook". Guilford Press. Retrieved 27 May 2017 – via Google Books.

[11] Zesiewicz TA, Elble RJ, Louis ED, Gronseth GS, Ondo WG, et al. (Nov 2011). "Evidence-based guideline update: treatment of essential tremor: report of the Quality Standards subcommittee of the American Academy of Neurology". Neurology. 77 (19): 1752–5. doi:10.1212/WNL.0b013e318236f0fd. PMC 3208950 . PMID 22013182.

[MedlinePlus-12] U.S. National Library of Medicine Nadolol entry in Medline Plus

[13] Foster NL, Newman RP, Lewitt PA, Gillespie MM, Larsen TA, et al. (October 1984). "Peripheral beta-adrenergic blockade treatment of parkinsonian tremor". Ann Neurol. 16: 505–508. doi:10.1002/ana.410160412.

[14] "Nadolol: MedlinePlus Drug Information". www.nlm.nih.gov. Retrieved 27 May 2017.

[15] "Nadolol Dosage Guide with Precautions - Drugs.com". drugs.com. Retrieved 27 May 2017.

[Label-16] "Corgard Label" (PDF). fda.gov. Retrieved 27 May 2017.

v t e Adrenergic receptor modulators
α₁	Agonists: 6-FNE Amidephrine Anisodine Buspirone Cirazoline Corbadrine Desglymidodrine Dexisometheptene Dipivefrine Dopamine Droxidopa (L-DOPS) Ephedrine Epinephrine Etilefrine Etilevodopa Ethylnorepinephrine Indanidine Isometheptene L-DOPA (levodopa) L-Phenylalanine L-Tyrosine Melevodopa Metaraminol Methoxamine Methyldopa Midodrine Naphazoline Norepinephrine Octopamine (drug) Oxymetazoline Phenylephrine Phenylpropanolamine Pseudoephedrine Synephrine Tetryzoline Tiamenidine XP21279 Xylometazoline Antagonists: Abanoquil Adimolol Ajmalicine Alfuzosin Amosulalol Anisodamine Arotinolol Atiprosin Atypical antipsychotics (e.g., brexpiprazole, clozapine, olanzapine, quetiapine, risperidone) Benoxathian Buflomedil Bunazosin Carvedilol Corynanthine Dapiprazole Domesticine Doxazosin Ergolines (e.g., ergotamine, dihydroergotamine, lisuride, terguride) Etoperidone Eugenodilol Fenspiride Hydroxyzine Indoramin Ketanserin L-765,314 Labetalol mCPP Mepiprazole Metazosin Monatepil Moxisylyte Naftopidil Nantenine Neldazosin Niaprazine Nicergoline Niguldipine Pardoprunox Pelanserin Perlapine Phendioxan Phenoxybenzamine Phentolamine Phenylpiperazine antidepressants (e.g., hydroxynefazodone, nefazodone, trazodone, triazoledione) Piperoxan Prazosin Quinazosin Quinidine Ritanserin Silodosin Spiperone Talipexole Tamsulosin Terazosin Tiodazosin Tolazoline Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin) Tricyclic antidepressants (e.g., amitriptyline, clomipramine, doxepin, imipramine, trimipramine) Trimazosin Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine) Urapidil WB-4101 Zolertine
α₂	Agonists: (R)-3-Nitrobiphenyline 4-NEMD 6-FNE Amitraz Apraclonidine Brimonidine Cannabivarin Clonidine Corbadrine Detomidine Dexmedetomidine Dihydroergotamine Dipivefrine Dopamine Droxidopa (L-DOPS) Etilevodopa Ephedrine Ergotamine Epinephrine Etilefrine Ethylnorepinephrine Guanabenz Guanfacine Guanoxabenz L-DOPA (levodopa) L-Phenylalanine L-Tyrosine Lofexidine Medetomidine Melevodopa Methyldopa Mivazerol Naphazoline Norepinephrine Oxymetazoline Phenylpropanolamine Piperoxan Pseudoephedrine Rezatomidine Rilmenidine Romifidine Talipexole Tasipimidine Tetrahydrozoline Tiamenidine Tizanidine Tolonidine Urapidil Vatinoxan XP21279 Xylazine Xylometazoline Antagonists: 1-PP Adimolol Amesergide Aptazapine Atipamezole Atypical antipsychotics (e.g., asenapine, brexpiprazole, clozapine, lurasidone, paliperidone, quetiapine, risperidone, zotepine) Azapirones (e.g., buspirone, gepirone, ipsapirone, tandospirone) BRL-44408 Buflomedil Cirazoline Efaroxan Esmirtazapine Fenmetozole Fluparoxan Idazoxan mCPP Mianserin Mirtazapine NAN-190 Olanzapine Pardoprunox Phentolamine Phenoxybenzamine Piperoxan Piribedil Rauwolscine Rotigotine SB-269970 Setiptiline Spiroxatrine Sunepitron Tolazoline Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine) Yohimbine
β	Agonists: Abediterol Alifedrine Amibegron Arbutamine Arformoterol Arotinolol BAAM Bambuterol Befunolol Bitolterol Broxaterol Buphenine Carbuterol Carmoterol Cimaterol Clenbuterol Colterol Corbadrine Denopamine Dipivefrine Dobutamine Dopamine Dopexamine Droxidopa (L-DOPS) Ephedrine Epinephrine Etafedrine Etilefrine Etilevodopa Ethylnorepinephrine Fenoterol Formoterol Hexoprenaline Higenamine Indacaterol Isoetarine Isoprenaline Isoxsuprine L-DOPA (levodopa) L-Phenylalanine L-Tyrosine Levosalbutamol Mabuterol Melevodopa Methoxyphenamine Methyldopa Mirabegron Norepinephrine Orciprenaline Oxyfedrine PF-610355 Phenylpropanolamine Pirbuterol Prenalterol Ractopamine Procaterol Pseudoephedrine Reproterol Rimiterol Ritodrine Salbutamol Salmeterol Solabegron Terbutaline Tretoquinol Tulobuterol Vilanterol Xamoterol XP21279 Zilpaterol Zinterol Antagonists: Acebutolol Adaprolol Adimolol Afurolol Alprenolol Alprenoxime Amosulalol Ancarolol Arnolol Arotinolol Atenolol Befunolol Betaxolol Bevantolol Bisoprolol Bopindolol Bornaprolol Brefonalol Bucindolol Bucumolol Bufetolol Bufuralol Bunitrolol Bunolol Bupranolol Butaxamine Butidrine Butofilolol Capsinolol Carazolol Carpindolol Carteolol Carvedilol Celiprolol Cetamolol Cicloprolol Cinamolol Cloranolol Cyanopindolol Dalbraminol Dexpropranolol Diacetolol Dichloroisoprenaline Dihydroalprenolol Dilevalol Diprafenone Draquinolol Ecastolol Epanolol Ericolol Ersentilide Esatenolol Esprolol Eugenodilol Exaprolol Falintolol Flestolol Flusoxolol Hydroxycarteolol Hydroxytertatolol ICI-118,551 Idropranolol Indenolol Indopanolol Iodocyanopindolol Iprocrolol Isoxaprolol Isamoltane Labetalol Landiolol Levobetaxolol Levobunolol Levomoprolol Medroxalol Mepindolol Metipranolol Metoprolol Moprolol Nadolol Nadoxolol Nebivolol Nifenalol Nipradilol Oxprenolol Pacrinolol Pafenolol Pamatolol Pargolol Penbutolol Pindolol Practolol Primidolol Procinolol Pronethalol Propafenone Propranolol Ridazolol Ronactolol Soquinolol Sotalol Spirendolol SR 59230A Sulfinalol Talinolol Tazolol Tertatolol Tienoxolol Tilisolol Timolol Tiprenolol Tolamolol Toliprolol Xibenolol Xipranolol

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案内

Corgard