Nadolol

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
Legal status
Legal status
Pharmacokinetic data
Protein binding 30%
Metabolism Nil
Biological half-life 14-24 hours
Excretion Renal and fecal (unchanged)
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
ECHA InfoCard 100.050.625
Chemical and physical data
Formula C17H27NO4
Molar mass 309.401 g/mol
3D model (JSmol)
  (verify)

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.

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]

See also

References

  1. ↑ Bragg W, et al. (Nov 2008). "Optimized separation of beta-blockers with multiple chiral centers using capillary electrochromatography-mass spectrometry". J Chromatogr B Analyt Technol Biomed Life Sci. 875 (1): 304–16. PMC 2680439 Freely accessible. PMID 18619928. doi:10.1016/j.jchromb.2008.06.028.
  2. 1 2 Nadolol entry in AccessMedicine. McGraw-Hill Global Education Holdings, LLC. Accessed November 8, 2014
  3. ↑ 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. "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. PMC 4676081 Freely accessible. PMID 24682347. doi:10.1161/CIR.0000000000000041.
  4. ↑ Silberstein SD, Holland S, Freitag F, Dodick DW, Argoff C, Ashman E (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. PMC 3335452 Freely accessible. PMID 22529202. doi:10.1212/WNL.0b013e3182535d20.
  5. ↑ Giannelli V, Lattanzi B, Thalheimer U, Merli M. "Beta-blockers in liver cirrhosis". Ann Gastroenterol. 27 (1): 20–26. PMC 3959530 Freely accessible. PMID 24714633.
  6. ↑ Bahn RS, 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. PMID 21510801. doi:10.1089/thy.2010.0417.
  7. ↑ 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. PMC 3515779 Freely accessible. PMID 23083782. doi:10.1016/j.jacc.2012.07.046.
  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, 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. PMC 3208950 Freely accessible. PMID 22013182. doi:10.1212/WNL.0b013e318236f0fd.
  12. 1 2 U.S. National Library of Medicine Nadolol entry in Medline Plus
  13. ↑ "Peripheral beta-adrenergic blockade treatment of parkinsonian tremor". Ann Neurol. 16: 505–508. October 1984. 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.
  16. ↑ "Corgard Label" (PDF). fda.gov. Retrieved 27 May 2017.
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