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Pharmacological / Pharmacokinetic Properties of Beta-Adrenergic Blocking Agents (Beta-Blockers)

 

The table below shows the pharmacological and pharmacokinetic properties of beta-blockers.

 

Beta-Blockers Cardioselective / Beta-1 Selective ISA (Intrinsic Sympathomimetic Activity) / PAA (Partial Agonist Activity) Lipid Solubility Alpha Blockade Elimination Half Life (hours) Route of Elimination
Acebutolol Yes + Low - Moderate No 3-4 (Acebutolol), 8-13 (Diacetolol) Hepatic, Renal
Atenolol Yes - Low No 6-7 Renal
Bisoprolol Yes - Moderate No 10-12 Hepatic, Renal
Carvedilol No - High Yes 6-10 Hepatic
Celiprolol Yes + Low No 5-6 Renal
Metoprolol Yes - Moderate No 3-7 Hepatic
Nadolol No - Low No 20-24 Renal
Nebivolol Yes - High No 10 (in fast metabolisers, but 3-5 times longer in slow metabolisers) Hepatic
Oxprenolol No ++ Moderate No 1-2 Hepatic
Pindolol No +++ Moderate No 3-4 Hepatic, Renal
Propranolol No - High No 3-6 Hepatic
Sotalol No - Low No 10-20 Renal

 

 

References:

1. Accord Healthcare Ltd. Summary of Product Characteristics – Atenolol 100mg Tablets. Available at http://www.medicines.org.uk/emc/medicine/25739 [Accessed on 08/07/15].

2. Accord Healthcare Ltd. Summary of Product Characteristics – Bisoprolol 2.5mg/5mg/10mg Film Coated Tablet. Available at http://www.medicines.org.uk/emc/medicine/25983 [Accessed on 08/07/15].

3. Accord Healthcare Ltd. Summary of Product Characteristics – Propranolol 40 mg Film-Coated Tablets. Available at http://www.medicines.org.uk/emc/medicine/27274 [Accessed on 08/07/15].

4. Accord Healthcare Ltd. Summary of Product Characteristics – Sotalol Hydrochloride 160 mg Tablets. Available at http://www.medicines.org.uk/emc/medicine/25989 [Accessed on 08/07/15].

5. Amdipharm Mercury Company Ltd. Summary of Product Characteristics – Oxprenolol 40 mg Tablets. Available at http://www.medicines.org.uk/emc/medicine/27985 [Accessed on 08/07/15].

6. Amdipharm Mercury Company Ltd. Summary of Product Characteristics – Visken Tablets 5 mg. Available at http://www.medicines.org.uk/emc/medicine/16866 [Accessed on 08/07/15].

7. Aurobindo Pharma - Milpharm Ltd. Summary of Product Characteristics – Carvedilol 12.5 mg Film-Coated Tablets. Available at http://www.medicines.org.uk/emc/medicine/27714 [Accessed on 08/07/15].

8. Aurobindo Pharma - Milpharm Ltd. Summary of Product Characteristics – Metoprolol Tartrate 50 mg Film-Coated Tablets. Available at http://www.medicines.org.uk/emc/medicine/28460 [Accessed on 08/07/15].

9. Dery AS, Hamilton LA, Starr JA. Nebivolol for the Treatment of Heart Failure. Am J Health Syst Pharm. 2011;68(10):879-886.

10. Hawkins NM, Petrie MC, Macdonald MR, et al. Heart Failure and Chronic Obstructive Pulmonary Disease: The Quandary of Beta-Blockers and Beta-Agonists. J Am Coll Cardiol. 2011;57(21):2127-2138.

11. Lechat P. Clinical Pharmacology of Beta-Blockers in Cardiology: Trial Results and Clinical Applications. Hot Topics in Cardiology 2008;10:7-44.

12. Lopez-Sendon J, Swedberg K, McMurray J, et al. Expert consensus document on Beta-Adrenergic Receptor Blockers. Eur Heart Journal 2004;25:1341–1362.

13. Morrow DA and Boden WE. Stable Ischemic Heart Disease. In: Mann DL, Zipes DP, Libby P, Bonow RO, eds. Braunwald's Heart Disease: A Textbook of Cardiovascular Medicine. 10th ed. Philadelphia, PA: Elsevier Saunders; 2014:1196-1200.

14. Sandoz Ltd. Summary of Product Characteristics – Nebivolol 5 mg Tablets. Available at http://www.medicines.org.uk/emc/medicine/22624 [Accessed on 08/07/15].

15. Sanofi. Summary of Product Characteristics – Corgard Tablets 80mg. Available at http://www.medicines.org.uk/emc/medicine/12767 [Accessed on 08/07/15].

16. Sanofi. Summary of Product Characteristics – Sectral 100mg Capsule. Available at http://www.medicines.org.uk/emc/medicine/27926 [Accessed on 08/07/15].

17. Sweetman SC (ed). Martindale: The Complete Drug Reference. 37th edition. London: Pharmaceutical Press, 2011.

18. Zentiva. Summary of Product Characteristics – Celectol 200 Tablets. Available at http://www.medicines.org.uk/emc/medicine/15942 [Accessed on 08/07/15].

 

 

 

Prepared: 8th July 2015

 

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