Atenolol: Difference between revisions

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Atenolol is excreted unchanged in the kidneys. Elimination is dependent on the [[glomerular filtration rate]]. Atenolol is ''not'' metabolized in the liver by [[cytochrome P-450]]  [http://www.ncbi.nlm.nih.gov/sites/entrez/?db=gene&cmd=Retrieve&dopt=summary&list_uids=1565 2D6] [[allele]].
Atenolol is excreted unchanged in the kidneys. Elimination is dependent on the [[glomerular filtration rate]]. Atenolol is ''not'' metabolized in the liver by [[cytochrome P-450]]  [http://www.ncbi.nlm.nih.gov/sites/entrez/?db=gene&cmd=Retrieve&dopt=summary&list_uids=1565 2D6] [[allele]].


With normal renal function, the serum [[half-life]] is about 8 hours. While it was originally thought<ref name="isbn0-683-04522-9">{{cite book |author=Kaplan, Norman M.; Lieberman, Ellin |authorlink= |editor= |others= |title=Clinical Hypertension|chapter=Treatment of Hypertension: Drug Therapy |edition=Fifth |language= |publisher=Williams & Wilkins |location=Baltimore |year=1990 |origyear= |pages=220 |quote=All beta-blockers act longer on the blood pressure than the pharmacokinetic data would imply. In moderate doses, most beta-blockers will likely keep the blood pressure down when given once daily. To ensure adequate control, early morning blodd presures should be measured before the daily dose is taken |isbn=0-683-04522-9 |oclc= |doi= |url= |accessdate=}}</ref> and promoted<ref name="isbn1-56363-703-0">{{cite book |author=Physicians Desk Reference |authorlink= |editor= |others= |title=Physicians' Desk Reference |edition=36th |language=English |publisher=Medical Economics |location=Oradell, NJ |year=1982|origyear= |pages=1884 |quote= |isbn=0874898501 |oclc= |doi= |url= |accessdate=}}</ref> that atenolol can be used once a day for isolated hypertension because the [[central nervous system]] pharmacodynamic effect persists longer, subsequent studies suggest atenolol should be dosed twice a day even for hypertension.<ref name="isbn0-683-04544-X">{{cite book |author=Kaplan, Norman M.; Lieberman, Ellin |authorlink= |editor= |others= |title=Clinical Hypertension |edition=Sixth|chapter=Treatment of Hypertension: Drug Therapy  |language= |publisher=Williams & Wilkins |location=Baltimore |year=1994 |origyear= |pages=225 |quote=In the usual doses prescribed, various beta blockers have equal antihypertensive efficacy. However, they many not all provide full 24-hour lowering of the BP which may be particularly critical in protecting against early morning cardiovascular catastrophes.  Metoprolol blunted this rise, but atenolol and pindolol did not (Raferty and Carrageta, 1985). Neutel et al, (1990) found a similar lack of 24-hour effect with once-daily atenolol but a sustained effect with acebutolol. Moreover, twice-daily doses of "cardioselective" agents may preserve this cardioselectivity better than once-daily large doses (Lipworth et al, 1991).|isbn=0-683-04544-X |oclc= |doi= |url= |accessdate=}}</ref><ref name="pmid18259123">{{cite journal |author=Sarafidis P, Bogojevic Z, Basta E, Kirstner E, Bakris GL |title=Comparative efficacy of two different beta-blockers on 24-hour blood pressure control |journal=J Clin Hypertens (Greenwich) |volume=10 |issue=2 |pages=112–8 |year=2008 |month=February |pmid=18259123 |doi=10.1111/j.1751-7176.2008.08021.x |url= |issn=}}</ref>
With normal renal function, the serum [[half-life]] is about 8 hours. While it was originally thought<ref name="isbn0-683-04522-9">{{cite book |author=Kaplan, Norman M.; Lieberman, Ellin |authorlink= |editor= |others= |title=Clinical Hypertension|chapter=Treatment of Hypertension: Drug Therapy |edition=5th|language= |publisher=Williams & Wilkins |location=Baltimore |year=1990 |origyear= |pages=220 |quote=All beta-blockers act longer on the blood pressure than the pharmacokinetic data would imply. In moderate doses, most beta-blockers will likely keep the blood pressure down when given once daily. To ensure adequate control, early morning blood pressures should be measured before the daily dose is taken |isbn=0-683-04522-9 |oclc= |doi= |url= |accessdate=}}</ref> and promoted<ref name="isbn1-56363-703-0">{{cite book |author=Physicians Desk Reference |authorlink= |editor= |others= |title=Physicians' Desk Reference |edition=36th |language=English |publisher=Medical Economics |location=Oradell, NJ |year=1982|origyear= |pages=1884 |quote= |isbn=0874898501 |oclc= |doi= |url= |accessdate=}}</ref> that atenolol can be used once a day for isolated hypertension because the [[central nervous system]] pharmacodynamic effect persists longer, subsequent studies suggest atenolol should be dosed twice a day even for hypertension.<ref name="isbn0-683-04544-X">{{cite book |author=Kaplan, Norman M.; Lieberman, Ellin |authorlink= |editor= |others= |title=Clinical Hypertension |edition=6th|chapter=Treatment of Hypertension: Drug Therapy  |language= |publisher=Williams & Wilkins |location=Baltimore |year=1994 |origyear= |pages=225 |quote=In the usual doses prescribed, various beta blockers have equal antihypertensive efficacy. However, they many not all provide full 24-hour lowering of the BP which may be particularly critical in protecting against early morning cardiovascular catastrophes.  Metoprolol blunted this rise, but atenolol and pindolol did not (Raferty and Carrageta, 1985). Neutel et al, (1990) found a similar lack of 24-hour effect with once-daily atenolol but a sustained effect with acebutolol. Moreover, twice-daily doses of "cardioselective" agents may preserve this cardioselectivity better than once-daily large doses (Lipworth et al, 1991).|isbn=0-683-04544-X |oclc= |doi= |url= |accessdate=}}</ref><ref name="pmid18259123">{{cite journal |author=Sarafidis P, Bogojevic Z, Basta E, Kirstner E, Bakris GL |title=Comparative efficacy of two different beta-blockers on 24-hour blood pressure control |journal=J Clin Hypertens (Greenwich) |volume=10 |issue=2 |pages=112–8 |year=2008 |month=February |pmid=18259123 |doi=10.1111/j.1751-7176.2008.08021.x |url= |issn=}}</ref>


==Dosage==
==Dosage==

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Atenolol.png
atenolol
IUPAC name: see chemistry section
Synonyms:
Formula: C14H22N2O3
 Uses: hypertention;angina pectoris
 Properties: hydrophilic
 Hazards: see side effects & drug interactions
Mass (g/mol): CAS #:
266.34 29122-68-7


In medicine, atenolol is a cardioselective adrenergic beta-antagonist that is "possessing properties and potency similar to propranolol, but without a negative inotropic effect."[1] Atenolol is hydrophilic[2]

History

Atenolol was developed by the Stuart Company which was a division of Imperial Chemical Industries (ICI). ICI was renamed Zeneca in 1992. Atenolol received approval in the United States August 19, 1981.[3] According to drugstore.com, 90 days of generic 50 mg pills costs $17.99 in January, 2009.

Generic atenolol was available in 1988.[4]

Chemistry

Atenolol may defined by IUPAC nomenclature:

  • 4-[2'-hydroxy-3'-[(1-methylethyl)amino]propoxy-benzeneacetamide
  • Benzeneacetamide, 4-[2'-hydroxy-3'-[(1-methylethyl) amino] propoxy]- (according to [1])

It is a hydrophilic drug, with solubility in water equal to 26.5 mg/mL at 37ºC, with chemical formula C14H22N2O3 andmolecular mass 266.34 gram/mole for the free base form. It is freely soluble in strongly acidic solutions.

Metabolism

Atenolol is excreted unchanged in the kidneys. Elimination is dependent on the glomerular filtration rate. Atenolol is not metabolized in the liver by cytochrome P-450 2D6 allele.

With normal renal function, the serum half-life is about 8 hours. While it was originally thought[5] and promoted[6] that atenolol can be used once a day for isolated hypertension because the central nervous system pharmacodynamic effect persists longer, subsequent studies suggest atenolol should be dosed twice a day even for hypertension.[7][8]

Dosage

For healthy adults, the starting dose recommended by the manufacturer is 50 mg orally once daily[6] and the maximum dose is 100 mg orally once daily. If the estimated creatinine clearance is less than 15 ml/min then the dose should be given every other day[6] or the dose should be 25 mg once per day[9].

However, atenolol may require twice daily dosing[8] The INVEST trial used atenolol twice a day if 50 mg once per day did not control pressure. In this study atenolol had similar outcomes to other antihypertensive agents.[10]

Efficacy

Coronary heart disease

Heart failure

Although atenolol has not received indication in the United States for the treatment of heart failure, two cohort studies suggest that the beta-blockers atenolol and carvedilol may be more effect than metoprolol for the treatment of heart failure.[11][12]

Randomized controlled trials by one research group also suggest atenolol might benefit.[13][14]

Hypertension

Atenolol may not reduce mortality as well as other antihypertensives according to a systematic review; however, this review did not compare atenolol against other adrenergic beta-antagonists and it is not clear whether all of the included trials allowed patients with active coronary heart disease who would have most benefitted from a adrenergic beta-antagonist.[15]

The INVEST trial used atenolol twice a day if 50 mg once per day did not control pressure. In this study atenolol had similar outcomes to other antihypertensive agents.[10]

External links

The most up-to-date information about Atenolol and other drugs can be found at the following sites.


References

  1. ↑ Anonymous (2024), Atenolol (English). Medical Subject Headings. U.S. National Library of Medicine.
  2. ↑ Tuininga YS, Crijns HJ, Brouwer J, et al (December 1995). "Evaluation of importance of central effects of atenolol and metoprolol measured by heart rate variability during mental performance tasks, physical exercise, and daily life in stable postinfarct patients". Circulation 92 (12): 3415–23. PMID 8521562. [e]
  3. ↑ Drugs@FDA. U S Food and Drug Administration
  4. ↑ Drugs@FDA. U S Food and Drug Administration
  5. ↑ Kaplan, Norman M.; Lieberman, Ellin (1990). “Treatment of Hypertension: Drug Therapy”, Clinical Hypertension, 5th. Baltimore: Williams & Wilkins, 220. ISBN 0-683-04522-9. “All beta-blockers act longer on the blood pressure than the pharmacokinetic data would imply. In moderate doses, most beta-blockers will likely keep the blood pressure down when given once daily. To ensure adequate control, early morning blood pressures should be measured before the daily dose is taken” 
  6. ↑ 6.0 6.1 6.2 Physicians Desk Reference (1982). Physicians' Desk Reference (in English), 36th. Oradell, NJ: Medical Economics, 1884. ISBN 0874898501. 
  7. ↑ Kaplan, Norman M.; Lieberman, Ellin (1994). “Treatment of Hypertension: Drug Therapy”, Clinical Hypertension, 6th. Baltimore: Williams & Wilkins, 225. ISBN 0-683-04544-X. “In the usual doses prescribed, various beta blockers have equal antihypertensive efficacy. However, they many not all provide full 24-hour lowering of the BP which may be particularly critical in protecting against early morning cardiovascular catastrophes. Metoprolol blunted this rise, but atenolol and pindolol did not (Raferty and Carrageta, 1985). Neutel et al, (1990) found a similar lack of 24-hour effect with once-daily atenolol but a sustained effect with acebutolol. Moreover, twice-daily doses of "cardioselective" agents may preserve this cardioselectivity better than once-daily large doses (Lipworth et al, 1991).” 
  8. ↑ 8.0 8.1 Sarafidis P, Bogojevic Z, Basta E, Kirstner E, Bakris GL (February 2008). "Comparative efficacy of two different beta-blockers on 24-hour blood pressure control". J Clin Hypertens (Greenwich) 10 (2): 112–8. DOI:10.1111/j.1751-7176.2008.08021.x. PMID 18259123. Research Blogging.
  9. ↑ Atenolol - FDA approved drug information (drug label) from DailyMed (U.S. National Library of Medicine).
  10. ↑ 10.0 10.1 Pepine CJ, Handberg EM, Cooper-DeHoff RM, et al. (December 2003). "A calcium antagonist vs a non-calcium antagonist hypertension treatment strategy for patients with coronary artery disease. The International Verapamil-Trandolapril Study (INVEST): a randomized controlled trial". JAMA 290 (21): 2805–16. DOI:10.1001/jama.290.21.2805. PMID 14657064. Research Blogging.
  11. ↑ Kramer JM, Curtis LH, Dupree CS, et al (December 2008). "Comparative effectiveness of beta-blockers in elderly patients with heart failure". Arch. Intern. Med. 168 (22): 2422–8; discussion 2428–32. DOI:10.1001/archinternmed.2008.511. PMID 19064824. Research Blogging.
  12. ↑ Go AS, Yang J, Gurwitz JH, Hsu J, Lane K, Platt R (December 2008). "Comparative effectiveness of different beta-adrenergic antagonists on mortality among adults with heart failure in clinical practice". Arch. Intern. Med. 168 (22): 2415–21. DOI:10.1001/archinternmed.2008.506. PMID 19064823. Research Blogging.
  13. ↑ Sturm B, Pacher R, Strametz-Juranek J, Berger R, Frey B, Stanek B (December 2000). "Effect of beta 1 blockade with atenolol on progression of heart failure in patients pretreated with high-dose enalapril". Eur. J. Heart Fail. 2 (4): 407–12. PMID 11113718. [e]
  14. ↑ Hülsmann M, Sturm B, Pacher R, et al (November 2001). "Long-term effect of atenolol on ejection fraction, symptoms, and exercise variables in patients with advanced left ventricular dysfunction". J. Heart Lung Transplant. 20 (11): 1174–80. PMID 11704477. [e]
  15. ↑ Carlberg B, Samuelsson O, Lindholm LH (2004). "Atenolol in hypertension: is it a wise choice?". Lancet 364 (9446): 1684–9. DOI:10.1016/S0140-6736(04)17355-8. PMID 15530629. Research Blogging.
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