Aldosterone Receptor Antagonist: Difference between revisions

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== Introduction ==
== Introduction ==
[[File:Response to stress.jpeg|right|frameless]]
[[File:Response to stress.jpeg|right|frameless]]
Aldosterone is a hormone secreted by the adrenal gland (zona glomerulosa). Aldosterone was classified as a mineralocorticoid hormone as it was found to play a major role in sodium reabsorption and potassium excretion. '''The primary action of aldosterone''' 
Aldosterone receptor antagonists are a class of drugs which block the effects of aldosterone. Aldosterone is the main mineralocorticoid [[Hormones|hormone]] in the body and is produced in the adrenal cortex of the [[Adrenal Glands|adrenal gland]].  


# Sodium and water retention 
Aldosterone increases sodium reabsorption by the kidneys, salivary glands, sweat glands and colon. At the same time, it increases the excretion of hydrogen and potassium ions.
# Also promotes myocardial fibrosis and induce cardiac hypertrophy and remodeling.  
# Can directly alter endothelial function by reducing nitric oxide availability and stimulating a vascular inflammatory response.  


Aldosterone receptor antagonists (ARAs) are a type of [[Diuretics|diuretic]] used in patients with [[Heart Failure|CHF]]. They also have other properties that can prevent [[Congestive Heart Failure|heart failure]] from becoming worse, along with improving symptoms of [[Heart Failure|heart failure]]. Aldosterone receptor antagonists are proven to be beneficial in heart failure patients even if they are already on angiotensin-converting enzyme (ACE) inhibitors or angiotensin II receptor blockers (ARBs).  
Aldosterone receptor antagonists block the effects of aldosterone, preventing the the reabsorption of sodium, which encourages water loss. This leads to a decrease in blood pressure and a reduction in fluid around the heart.


* These medicines cause the kidneys to get rid of extra water and they help to retain potassium by inhibiting secretion of potassium into distal tubule of the nephron<ref>Nagarajan V, Chamsi-Pasha M, Tang WH. The role of aldosterone receptor antagonists in the management of heart failure: an update. [Review]. Cleveland Clinic Journal of Medicine. 2012;79(9):631-9.</ref>.
Aldosterone receptor antagonists may be used in the treatment of high blood pressure or heart failure. They also have a weak diuretic action.
Because of this, they are called potassium-sparing diuretics.<ref>University of Michigan [https://www.uofmhealth.org/health-library/tx4152 Aldosterone Receptor Antagonists: Diuretics for Heart Failure] Available from: https://www.uofmhealth.org/health-library/tx4152 (last accessed 18.6.2019)</ref>


Blocking the aldosterone receptor prevents an increase in aldosterone, ultimately preventing changes to the [[Cardiovascular System|cardiovascular]] system and allowing for increased water excretion.
Aldosterone receptor antagonists or MRAs have been shown to reduce heart failure-related hospitalisations, prolong life, and improve exercise tolerance and quality of life.<ref name=":1">Heart Failure Matters ALDOSTERONE RECEPTOR ANTAGONISTS OR MINERALOCORTICOID RECEPTOR ANTAGONIST (MRAS) Available:https://www.heartfailurematters.org/what-your-doctor-can-do/aldosterone-receptor-antagonists-or-mineralocorticoid-receptor-antagonist-mras/#animated-journey (accessed 7.4.2022)</ref>
 
== Polypharmacy ==
Aldosterone receptor antagonists are proven to be beneficial in heart failure patients even if they are already on angiotensin-converting enzyme (ACE) inhibitors or angiotensin II receptor blockers (ARBs).  


Most aldosterone receptor antagonists are used in conjunction with other medications, specifically [[Beta-Blockers|Beta Blockers]] and [[ACE Inhibitors in the Treatment of Congestive Heart  Failure|Ace Inhibitors.]]
Most aldosterone receptor antagonists are used in conjunction with other medications, specifically [[Beta-Blockers|Beta Blockers]] and [[ACE Inhibitors in the Treatment of Congestive Heart  Failure|Ace Inhibitors.]]
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== Adverse Effects ==
== Adverse Effects ==
Due to the prevention of potassium secretion into the distal tubule both these drugs are associated with an adverse effect of  
Due to the prevention of potassium secretion into the distal tubule both these drugs are associated with an adverse effect of:
* [[Hyperkalemia]] due to them being potassium sparing diuretics.
* [[Hyperkalemia]] due to them being potassium sparing diuretics.


* Gynecomastia and breast pain in men because it tends to bind to progesterone and androgen receptors<ref name=":0" />.  
* Gynecomastia and breast pain in men because it tends to bind to progesterone and androgen receptors<ref name=":0" />. The newer drugs don’t have this effect<ref name=":1" />.


== Physiotherapy - Implications ==
== Physiotherapy - Implications ==
This drug, while acting to relieve the body of excessive fluids, can inadvertently disrupt the [[Electrolytes|electrolyte]] and pH balance in the system. Because the main side effect is hyperkalemia, Hyperkalemia affects the cardiac conductive tissue and can cause serious arrhythmias ( eg ventricular fibrilllation, asystolic arrest).   
These drugs can sometimes affect kidney function and can also increase potassium levels (hyperkalemia). Hyperkalemia affects the cardiac conductive tissue and can cause serious arrhythmias ( eg ventricular fibrilllation, asystolic arrest).  It important to check for any irregular heartbeats if the patient begins complaining of chest pains or [[Dyspnoea|shortness of breath]]<ref>Sica DA. Diuretic-related side effects: development and treatment. J Clin Hypertens. 2004;6:532–540.</ref>. This is especially important for patients who also use ACE inhibitors or ARBs.   


* It important to check for any irregular heartbeats if the patient begins complaining of chest pains or [[Dyspnoea|shortness of breath]]<ref>Sica DA. Diuretic-related side effects: development and treatment. J Clin Hypertens. 2004;6:532–540.</ref>.
In addition to monitoring the patient’s [[Vital Signs|vitals]] before, during and after treatment, patients should be educated on lifestyle changes to help decrease their mortality.
* In addition to monitoring the patient’s [[Vital Signs|vitals]] before, during and after treatment, patients should be educated on lifestyle changes to help decrease their mortality.


== References ==
== References ==

Revision as of 02:25, 7 April 2022

Original Editor - Lauren Pulliam Southern Top Contributors - Lucinda hampton, Kim Jackson, Lauren Pulliam Southern and Beau Lawrence

Introduction[edit | edit source]

Response to stress.jpeg

Aldosterone receptor antagonists are a class of drugs which block the effects of aldosterone. Aldosterone is the main mineralocorticoid hormone in the body and is produced in the adrenal cortex of the adrenal gland.

Aldosterone increases sodium reabsorption by the kidneys, salivary glands, sweat glands and colon. At the same time, it increases the excretion of hydrogen and potassium ions.

Aldosterone receptor antagonists block the effects of aldosterone, preventing the the reabsorption of sodium, which encourages water loss. This leads to a decrease in blood pressure and a reduction in fluid around the heart.

Aldosterone receptor antagonists may be used in the treatment of high blood pressure or heart failure. They also have a weak diuretic action.

Aldosterone receptor antagonists or MRAs have been shown to reduce heart failure-related hospitalisations, prolong life, and improve exercise tolerance and quality of life.[1]

Polypharmacy[edit | edit source]

Aldosterone receptor antagonists are proven to be beneficial in heart failure patients even if they are already on angiotensin-converting enzyme (ACE) inhibitors or angiotensin II receptor blockers (ARBs).  

Most aldosterone receptor antagonists are used in conjunction with other medications, specifically Beta Blockers and Ace Inhibitors.

[2]

Common ARAs[edit | edit source]

Two common aldosterone receptor antagonists are[3]

  • Spironolactone: taken orally with doses of 12.5-25 mg per day and has a long half-life of 13-17 hours[4].
  • Eplerenone is also taken orally with doses of 50 mg twice daily with a half-life of 4 hours[5] and both are excreted by via the liver and kidneys[6].

Adverse Effects[edit | edit source]

Due to the prevention of potassium secretion into the distal tubule both these drugs are associated with an adverse effect of:

  • Gynecomastia and breast pain in men because it tends to bind to progesterone and androgen receptors[3]. The newer drugs don’t have this effect[1].

Physiotherapy - Implications[edit | edit source]

These drugs can sometimes affect kidney function and can also increase potassium levels (hyperkalemia). Hyperkalemia affects the cardiac conductive tissue and can cause serious arrhythmias ( eg ventricular fibrilllation, asystolic arrest). It important to check for any irregular heartbeats if the patient begins complaining of chest pains or shortness of breath[7]. This is especially important for patients who also use ACE inhibitors or ARBs.

In addition to monitoring the patient’s vitals before, during and after treatment, patients should be educated on lifestyle changes to help decrease their mortality.

References[edit | edit source]

  1. ↑ 1.0 1.1 Heart Failure Matters ALDOSTERONE RECEPTOR ANTAGONISTS OR MINERALOCORTICOID RECEPTOR ANTAGONIST (MRAS) Available:https://www.heartfailurematters.org/what-your-doctor-can-do/aldosterone-receptor-antagonists-or-mineralocorticoid-receptor-antagonist-mras/#animated-journey (accessed 7.4.2022)
  2. ↑ Study Rx Aldosterone Receptor Antagonist - Spironolactone Available from: https://www.youtube.com/watch?v=XrOcp5FFvbI (last accessed 18.6.2019)
  3. ↑ 3.0 3.1 Lainscak M, Pelliccia F, Rosano G, Vitale C, Schiariti M, Greco C, Speziale G, Gaudio C (2015). Safety profile of mineralocorticoid receptor antagonists: Spironolactone and eplerenone. Int J Cardiol. 200, 25-9
  4. ↑ U.S. Food and Drug Administration (FDA). Aldactone spironolactone tablets, USP. Available online at: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/012151s062lbl.pdf. Last accessed 11/29/18.
  5. ↑ U.S. Food and Drug Administration (FDA). INSPRA eplerenone tablets. Available online at: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21437lbl.pdf. Last accessed 11/29/18.
  6. ↑ Nappi JM, Sieg A (2011). Aldosterone and aldosterone receptor antagonists in patients with chronic heart failure. Vasc Health Risk Manag. 7, 353-63.
  7. ↑ Sica DA. Diuretic-related side effects: development and treatment. J Clin Hypertens. 2004;6:532–540.
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