Tuesday, June 3, 2014

Staying alive with Edema and a heart condition

This is just an introduction to an article I wrote and compiled in February when I tried to switch to Eplerenone from Spironolactone successfully. Both these drugs prevent morbidity (unwanted deaths) from having edema while having Congestive Heart Failure symptoms at the same time. These two drugs prevent strokes and heart attacks from the stress of the water buildup specifically in your legs to your heart. Spironolactone is a miracle drug. However, if you are a man you won't be able to have sex while taking a full dose of this drug. However, I found that I can take 1/2 tablet of spironolactone which gets rid of most edema symptoms while taking the drug and still have a sexual relationship with my wife. However, you need to see how this will work out for you as well and likely consult your doctor. I couldn't take Eplerenone I found because I was in pain and felt terrible. Also, Eplerenone is much more expensive than Spironolactone. I have also discovered that certain vitamins and exercise will lengthen your lives a lot beyond the normal around 5 years you have left sometimes when diagnosed with Congestive Heart failure. Also, they are beginning to inject stem cells into heart patients and the hearts are beginning to heal themselves with strong heart cells. This might save your life and mine during the next few years. Cedars Sinai I believe in Los Angeles is one of the Hospitals doing this kind of research.

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Tuesday, February 4, 2014

Eplerenone as an alternative to Spironolactone for Edema

I have written before about taking Spironolactone for Edema related to Heart problems at my present age of 65. However, what Spironolactone also does is reduce your libido considerably. So, if you are a man for example, you might walk or drive by a very pretty woman and you might say to yourself, "Oh. She's pretty" but not have any feelings much other than that as a man. Doctors prescribe spironolactone because you might only pay about 20 to 30 dollars for 30 pills. However, if you take Eplerenone instead (which does not suppress your libido) your feelings might be more normal from before regarding your libido if you are a man. However, here in the U.S. Eplerenone might cost 90 dollars or more for 30 tablets. So, this is something to consider as well.

My thoughts after I started taking spironolactone were that I felt so much better and my quality of life improved so much and I immediately lost at least 15 pounds in water weight while taking spironolactone that my life became immediately of a higher quality and I didn't feel strained all the time while awake like often happened before going on Spironolactone for edema. So, both eplerenone basically are supposed to completely eliminate edema swelling symptoms in legs and feet while you are taking them and the same is supposed to be true of eplerenone. I haven't tried eplerenone yet but might in the next week or so instead of spironolactone. Eplerenone appears to be a more recent designer drug of the last 10 to 15 years whereas spironolactone apparently has been around much longer.

 

Eplerenone

From Wikipedia, the free encyclopedia
Eplerenone
Systematic (IUPAC) name
pregn-4-ene-7,21-dicarboxylic acid, 9,11-epoxy-17-hydroxy-3-oxo, γ-lactone, methyl ester (7α, 11α, 17α)
Clinical data
Trade names Inspra
AHFS/Drugs.com monograph
MedlinePlus a603004
Pregnancy cat. B3 (Aust)
Legal status Schedule 4 (Aust), Rx only (US)
Routes oral
Pharmacokinetic data
Bioavailability 69%
Metabolism hepatic (CYP3A4)
Half-life 6-8 hours
Excretion 67% renal
32% biliary
Identifiers
CAS number 107724-20-9 Yes
ATC code C03DA04
PubChem CID 5282131
IUPHAR ligand 2876
DrugBank DB00700
ChemSpider 10203511 Yes
UNII 6995V82D0B Yes
KEGG D01115 Yes
ChEBI CHEBI:31547 Yes
ChEMBL CHEMBL1095097 Yes
Chemical data
Formula C24H30O6 
Mol. mass 414.49
 Yes (what is this?)  (verify)
Eplerenone (INN) /ɛpˈlɛrənn/ is an aldosterone antagonist used as an adjunct in the management of chronic heart failure. It is similar to the diuretic spironolactone, though it is much more selective for the mineralocorticoid receptor in comparison (i.e., does not possess any antiandrogen, progestogen, or estrogenic effects), and is specifically marketed for reducing cardiovascular risk in patients following myocardial infarction. It is marketed by Pfizer under the trade name Inspra. Eplerenone is a potassium-sparing diuretic, meaning that it helps the body get rid of water but still keep potassium.

Medical use

Eplerenone is specifically indicated for the reduction of risk of cardiovascular death in people with heart failure and left ventricular dysfunction within 3–14 days of an acute myocardial infarction, in combination with standard therapies and as treatment against hypertension. It appears equivalent to spironolactone but is much more expensive.[1]

Adverse effects

Common adverse drug reactions (ADRs) associated with the use of eplerenone include: hyperkalaemia, hypotension, dizziness, altered renal function, and increased creatinine concentration.[2] Eplerenone may have a lower incidence of sexual side effects such as feminization, gynecomastia, impotence, low sex drive and reduction of size of male genitalia.[3] Due to the high risk of elevated potassium levels in individuals taking eplerenone, the United States FDA suggests routine checks on the individual's potassium level to screen for hyperkalemia.

Contraindications

Eplerenone is contraindicated in patients with hyperkalaemia, severe renal impairment (creatinine Cl less than 30 ml/min), or severe hepatic impairment (Child-Pugh score C). The manufacturer of eplerenone also contraindicates ( relative C.I. ) concomitant treatment with ketoconazole, itraconazole or other potassium-sparing diuretics (though the manufacturer still considers taking these drugs to be absolute C.I.) Potential benefits should be weighted against possible risks.

Drug interactions

Eplerenone is primarily metabolised by the cytochrome P450 enzyme CYP3A4. Thus the potential exists for adverse drug interactions with other drugs that induce or inhibit CYP3A4. Specifically, the concomitant use of the CYP3A4 potent inhibitors ketoconazole and itraconazole is contraindicated. Other CYP3A4 inhibitors including erythromycin, saquinavir, and verapamil should be used with caution. Other drugs that increase potassium concentrations may increase the risk of hyperkalaemia associated with eplerenone therapy, including salt substitutes,[4] potassium supplements and other potassium-sparing diuretics.

Lab Synthesis

Eplerenone synth.png
Steroidal, Aldosterone Antagonists: Increased selectivity of 9α,11-epoxy derivatives. doi:10.1002/hlca.19970800220.

end quote from:
eplerenone,   from wikipedia. 


Later:  April 1st 2014. I found out I had just too much pain and other bad reactions to be able to benefit from Eplerenone. I was very discouraged by this. I first reduced my dose of eplerenone to 1/2 tablet. This still didn't help so I went back on 1/2 tablet of spironolactone. Though there is a tiny amount of swelling of edema with 1/2 tablet of spironolactone I found that my pain left when I stopped taking eplerenone and I found 1/2 table of spironolactone does not take away a man's sexual desire (at least in my case) and this makes my wife very happy. So, maybe this is an alternative. I haven't really told my doctor what I have done yet but I consulted with my son who is a trained Nurse with a Bachelor of Science in Nursing. He said it is important not to suddenly go off either of these drugs because it is too hard on your body. They really change the way one's body operates and one has to be careful of both of them in this sense. Both Spironolactone and Eplerenone reduce morbidity (deaths)  in patients who have Edema. So, the main reason people take either Spironolactone or Eplerenone is so they don't suddenly have a heart attack, heart failure or stroke or other complication that kills them because of the stress on one's heart if you have a heart problem and edema at the same time. Both these medications completely relieve the body of all symptoms of Edema if either of these medications can be tolerated by the person taking one of them. The easiest to be able to take by most people in Spironolactone but it will take away all of your sexual feelings completely if you take a full dose if you are a man. But staying alive is nice too.


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