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词条 Nadolol
释义

  1. Medical uses

  2. Side effects

  3. Contraindications

  4. Mechanism of action

  5. Chemistry

  6. References

  7. External links

{{Drugbox
| Watchedfields = changed
| verifiedrevid = 470624569
| IUPAC_name =* rel-(2R,3S)-5[(2R)-3-(tert-butylamino)-2-hydroxypropyl]oxy1,2,3,4-tetrahydronaphthalene-2,3-diol
  • (2R,3S)-5[(2R)-3-(tert-butylamino)-2-hydroxypropyl]oxy1,2,3,4-tetrahydronaphthalene-2,3-diol

| image = Nadolol.svg
| tradename = Corgard, others
| Drugs.com = {{drugs.com|monograph|nadolol}}
| MedlinePlus = a682666
| pregnancy_AU =
| pregnancy_US = C
| pregnancy_category =
| legal_UK = POM
| legal_US = Rx-only
| legal_status =
| routes_of_administration = Oral
| bioavailability =
| protein_bound = 30%
| metabolism = Not metabolised
| elimination_half-life = 14-24 hours
| excretion = Renal and fecal (unchanged)
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 42200-33-9
| ATC_prefix = C07
| ATC_suffix = AA12
| PubChem = 39147
| IUPHAR_ligand = 554
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB01203
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 35815
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = FEN504330V
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D00432
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 649
| C=17 | H=27 | N=1 | O=4
| molecular_weight = 309.401 g/mol
| smiles = OC(CNC(C)(C)C)COc1cccc2c1C[C@H](O)[C@H](O)C2
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 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
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = VWPOSFSPZNDTMJ-UCWKZMIHSA-N
}}Nadolol, sold under the brand name Corgard among others, is a medication used to treat high blood pressure, heart pain, and atrial fibrillation.[1] It has also been used to prevent migraine headaches and complications of cirrhosis.[2][1] It is taken by mouth.[2]

Common side effects include dizziness, feeling tired, a slow heart rate, and Raynaud syndrome.[1] Serious side effects may include heart failure and bronchospasm.[1] Its use in pregnancy and breastfeeding is of unclear safety.[3] It is a non-selective beta blocker and works by blocking β1-adrenergic receptors in the heart and β2-adrenergic receptors in blood vessels.[4]

Nadolol was patented in 1970 and came into medical use in 1978.[5] It is avaliable as a generic medication.[4] A month supply in the United Kingdom costs the NHS about £6 as of 2019.[2] In the United States the wholesale cost of this amount is about $US 52 .[6] In 2016 it was the 283rd most prescribed medication in the United States with more than a million prescriptions.[7]

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.[8]

It is regularly used off-label[8] for control of heart rate in people with atrial fibrillation,[9] prevention of migraine headaches;[10] prevention of bleeding veins in people with portal hypertension caused by cirrhosis;[1] and to treat people with high levels of thyroid hormone.[11]

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 cardioselective beta-blockers like metoprolol and propanolol in the prevention of breakthrough cardiac events[12]. 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.[13] It has also been found to be useful (off-label) for several neurological disorders such as the prevention of migraine attacks,[14] attention deficit/hyperactivity disorder(ADHD)[15] and its use has been explored as a treatment for essential tremor[16] and Parkinson's disease[17] but neither is well established.[18][19][20]

Side effects

The most common side effects include dizziness and fatigue.[17]

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.[21]

Mechanism of action

{{Main|Beta-blocker}}

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|date=January 2017}}

Chemistry

Nadolol is a mixture of stereoisomers. It is polar and hydrophilic, with low lipid solubility.[22]

{{-}}

References

1. ^1 {{cite journal |last1=Giannelli |first1=V |last2=Lattanzi |first2=B |last3=Thalheimer |first3=U |last4=Merli |first4=M |title=Beta-blockers in liver cirrhosis. |journal=Annals of gastroenterology |date=2014 |volume=27 |issue=1 |pages=20-26 |pmid=24714633}}
2. ^1 2 {{cite book|title=British national formulary : BNF 76|date=2018|publisher=Pharmaceutical Press|isbn=9780857113382|pages=148|edition=76}}
3. ^{{cite web |title=Nadolol Pregnancy and Breastfeeding Warnings |url=https://www.drugs.com/pregnancy/nadolol.html |website=Drugs.com |accessdate=3 March 2019 |language=en}}
4. ^1 2 3 4 {{cite web |title=Nadolol Monograph for Professionals |url=https://www.drugs.com/monograph/nadolol.html |website=Drugs.com |publisher=American Society of Health-System Pharmacists |accessdate=3 March 2019 |language=en}}
5. ^{{cite book |last1=Fischer |first1=Jnos |last2=Ganellin |first2=C. Robin |title=Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=460 |url=https://books.google.ca/books?id=FjKfqkaKkAAC&pg=PA460 |language=en}}
6. ^{{cite web |title=NADAC as of 2019-02-27 |url=https://data.medicaid.gov/Drug-Pricing-and-Payment/NADAC-as-of-2019-02-27/s7c9-pfa6 |website=Centers for Medicare and Medicaid Services |accessdate=3 March 2019 |language=en}}
7. ^{{cite web |title=The Top 300 of 2019 |url=https://clincalc.com/DrugStats/Top300Drugs.aspx |website=clincalc.com |accessdate=22 December 2018}}
8. ^1 Nadolol entry in AccessMedicine. McGraw-Hill Global Education Holdings, LLC. Accessed 8 November 2014
9. ^{{cite journal | vauthors=January CT, Wann LS, Alpert JS, Calkins H, Cigarroa JE, Cleveland JC Jr, Conti JB, Ellinor PT, Ezekowitz MD, Field ME, Murray KT, Sacco RL, Stevenson WG, Tchou PJ, Tracy CM, Yancy CW | display-authors=5 | title=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 | journal=Circulation | volume=130 | pages=e199-267 | doi=10.1161/CIR.0000000000000041 | pmc=4676081 | pmid = 24682347}}
10. ^{{cite journal | vauthors=Silberstein SD, Holland S, Freitag F, Dodick DW, Argoff C, Ashman E |display-authors=5 | year=2012 | title=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 | journal=Neurology | volume=78 | issue=17 | pages=1337–45 | doi=10.1212/WNL.0b013e3182535d20 | pmc=3335452 | pmid = 22529202}}
11. ^{{cite journal | vauthors = Bahn RS, Burch HB, Cooper DS, Garber JR, Greenlee MC, Klein I, Laurberg P, McDougall IR, Montori VM, Rivkees SA, Ross DS, Sosa JA, Stan MN |display-authors=5 | year = 2011 | title = Hyperthyroidism and Other Causes of Thyrotoxicosis: Management Guidelines of the American Thyroid Association and American Association of Clinical Endocrinologists | journal = Thyroid | volume = 21 | issue = 6 | pages = 593–646 | doi=10.1089/thy.2010.0417 | pmid = 21510801}}
12. ^{{cite journal |vauthors= Mazzanti A, Maragna R, Vacanti G, Monteforte N, Bloise R, Marino M, Braghieri L, Gambelli P, Memmi M, Pagan E, Morini M, Malovini A, Ortiz M, Sacilotto L, Bellazzi R, Monserrat L, Napolitano C, Bagnardi V, Priori SG |display-authors=5 |date=15 April 2018 |title=Interplay Between Genetic Substrate, QTc Duration, and Arrhythmia Risk in Patients With Long QT Syndrome |journal=Journal of the American College of Cardiology |volume=71 |issue=15 |pages=1663-1671 |doi=10.1016/j.jacc.2018.01.078 | pmc= | pmid = }}
13. ^{{cite web|url=http://reference.medscape.com/drug/corgard-nadolol-342361|title=Corgard (nadolol) dosing, indications, interactions, adverse effects, and more|website=reference.medscape.com|accessdate=27 May 2017}}
14. ^{{cite web|url=http://patient.info/medicine/nadolol-a-beta-blocker-corgard|title=Nadolol - a beta-blocker - Corgard. High blood pressure drugs|website=patient.info|accessdate=27 May 2017}}
15. ^{{cite web|url=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+for+ADHD&f=false|title=Attention-deficit Hyperactivity Disorder: A Clinical Workbook|first1=Russell A.|last1=Barkley|first2=Kevin R.|last2=Murphy|date=27 May 2017|publisher=Guilford Press|accessdate=27 May 2017|via=Google Books}}
16. ^{{cite journal | vauthors = Zesiewicz TA, Elble RJ, Louis ED, Gronseth GS, Ondo WG, Dewey RB Jr, Okun MS, Sullivan KL, Weiner WJ |display-authors=5 | date = Nov 2011 | title = Evidence-based guideline update: treatment of essential tremor: report of the Quality Standards subcommittee of the American Academy of Neurology | journal = Neurology | volume = 77 | issue = 19 | pages = 1752–5 | doi = 10.1212/WNL.0b013e318236f0fd | pmc=3208950 | pmid = 22013182}}
17. ^1 U.S. National Library of Medicine [https://www.nlm.nih.gov/medlineplus/druginfo/meds/a682666.html Nadolol entry in Medline Plus]
18. ^{{cite journal | vauthors = Foster NL, Newman RP, Lewitt PA, Gillespie MM, Larsen TA, Chase TN |display-authors=5 |date=October 1984 | title = Peripheral beta-adrenergic blockade treatment of parkinsonian tremor | pages= 505–508 |journal=Ann Neurol |volume=16 | doi = 10.1002/ana.410160412}}
19. ^{{cite web|url=https://www.nlm.nih.gov/medlineplus/druginfo/meds/a682666.html|title=Nadolol: MedlinePlus Drug Information|website=www.nlm.nih.gov|accessdate=27 May 2017}}
20. ^{{cite web|url=https://www.drugs.com/dosage/nadolol.html|title=Nadolol Dosage Guide with Precautions - Drugs.com|website=drugs.com|accessdate=27 May 2017}}
21. ^{{cite web|url=http://www.accessdata.fda.gov/drugsatfda_docs/label/2008/018063s060lbl.pdf|title=Corgard Label|website=fda.gov|accessdate=27 May 2017}}
22. ^{{cite journal | vauthors = Bragg W, Norton D, Shamsi SA | date = November 2008 | title = Optimized separation of beta-blockers with multiple chiral centers using capillary electrochromatography-mass spectrometry | journal = J Chromatogr B | volume = 875 | issue = 1 | pages = 304–16 | doi = 10.1016/j.jchromb.2008.06.028 | pmc=2680439 | pmid = 18619928}}

External links

  • [https://druginfo.nlm.nih.gov/drugportal/name/nadolol Drug information by the NIH]
{{Endothelial antihypertensives}}{{Adrenergics}}

6 : Beta blockers|Phenol ethers|Alcohols|Tetralins|Peripherally selective drugs|RTT
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