Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0730345 (microalbuminuria)
 4,018 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Eplerenone is a new aldosterone receptor antagonist that will be used in the treatment of hypertension. Like spironolactone, it is a compound that can be associated with the development of hyperkalemia. Therefore, the same prescription considerations that are applied to spironolactone should be directed to its use. Unfortunately, the label for eplerenone will place more stringent restrictions on its use than is the case for spironolactone. The basis for the multiple contraindications to the use of eplerenone is primarily that of concern for the development of hyperkalemia. This may occur with eplerenone, as has been the case with spironolactone. The presumption in the prescribing information that certain patient subsets, such as diabetics with microalbuminuria and/or patients with mild renal failure, would be highly prone to developing clinically relevant hyperkalemia with eplerenone is not, however, grounded in fact. The favorable experience with spironolactone is important. It should provide us with the landmarks for advancing knowledge on the role of newer aldosterone receptor antagonists in disease state management and one would think, help in establishing criteria for the safe use of new compounds. New compounds in a drug class typically provide advantages over earlier entries into a drug class but not if regressive labeling has occurred. Time and additional clinical experience with eplerenone will establish its safety profile and determine if the original label for this compound was correct.
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PMID:Eplerenone: a new aldosterone receptor antagonist--are the FDAs restrictions appropriate? 1246 13

Eplerenone is a highly selective aldosterone blocker, which is under development for the treatment of hypertension and heart failure. To assess its usefulness in older patients with systolic hypertension and widened pulse pressure, we compared the effects of eplerenone with amlodipine, on clinic blood pressure (BP) and pulse pressure and in a subset of the patients, ambulatory BP, vascular compliance, and urinary albumin excretion. The study involved 269 patients > or =50 years of age who were randomly assigned to either eplerenone (50 to 200 mg daily) or amlodipine (2.5 to 10 mg daily) in a double-blind titration to effect design. After 24 weeks of therapy, reductions in clinic systolic BP were similar for both treatments (eplerenone, -20.5+/-1.1 mm Hg; amlodipine, -20.1+/-1.1 mm Hg). Reductions in clinic diastolic BP were modestly larger on amlodipine (-6.9+/-0.7 mm Hg) compared with eplerenone (-4.5+/-0.7 mm Hg) (P=0.014). Pulse pressure was also reduced similarly from baseline by the 2 treatment groups (eplerenone, -15.9 mm Hg versus amlodipine, -13.4 mm Hg, P=0.07). Changes from baseline in pulse wave velocity after 24 weeks of therapy were statistically similar for eplerenone and amlodipine. In patients with microalbuminuria at baseline (>30 mg albumin/g creatinine), eplerenone reduced the urinary albumin/creatinine ratio by 52% compared with a reduction of 10% by amlodipine (P=0.04). Thus, eplerenone was as effective as amlodipine in lowering systolic BP and pulse pressure as well as pulse wave velocity in older patients with widened pulse pressure hypertension. Furthermore, eplerenone reduced microalbuminuria to a greater extent than amlodipine in this older patient group.
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PMID:Effects of the selective aldosterone blocker eplerenone versus the calcium antagonist amlodipine in systolic hypertension. 1475 24

Eplerenone is a specific aldosterone receptor antagonist that has been shown to have antihypertensive efficacy and to reduce end-organ manifestations in experimental animal models. Studies in humans have confirmed the blood pressure-lowering efficacy of this agent, as well as providing evidence of benefit in congestive heart failure. The side-effect profile indicates that the specificity of eplerenone for the mineralocorticoid receptor is responsible for the lower incidence of sex hormone- related side-effects than have been seen with other mineralocorticoid receptor blockers. Hyperkalemia is most frequently observed with eplerenone among patients with severe impairment of renal function and in diabetics with microalbuminuria, especially in combination with angiotensin-converting enzyme inhibitors. This agent appears to be a promising and effective new addition for the treatment of hypertension and heart failure with few of the side-effects that have plagued earlier drugs of this class.
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PMID:Eplerenone: a new selective aldosterone receptor antagonist. 1534 28