Development and validation of a liquid chromatography–tandem mass spectrometric assay for Eplerenone and its hydrolyzed metabolite in human plasma

Zhang, Ji Y.; Fast, Douglas M.; Breau, Alan P.

doi:10.1016/s1570-0232(02)00964-9

Cited by 25 publications

(19 citation statements)

References 11 publications

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“…The solubility of eplerenone in aqueous solutions is low and independent of pH (12,26). Under basic conditions, eplerenone is hydrolyzed to form the open lactone form, whereas under acidic conditions, it is converted back to the closed form (80). In eplerenone the 17á-thioacetyl group of spironolactone is replaced with a carbomethoxy group (Fig.…”

Section: Chemistrymentioning

confidence: 99%

Eplerenone: A Selective Aldosterone Blocker

Stier

2003

Cardiovascular Drug Reviews

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Recent studies suggest that aldosterone may play a larger role than once appreciated in normal physiologic function and cardiovascular disease. Some of the adverse cardiovascular effects that have been described include cardiac and vascular fibrosis, vascular necrosis and inflammation, impaired endothelial function, reduced fibrinolysis, hypertension, left ventricular hypertrophy (LVH), congestive heart failure, and cardiac arrhythmias. In light of these findings, the ability to block the actions of aldosterone has gained increased therapeutic importance. Eplerenone is a selective aldosterone receptor blocker that displays little interaction with androgen and progesterone receptors. Eplerenone has already been approved for the treatment of systemic hypertension and has been evaluated in numerous hypertension subgroups, including patients with low plasma renin activity; diabetes; LVH; uncontrolled blood pressure while receiving monotherapy with angiotensin-converting enzyme inhibitors, angiotensin-receptor blockers, calcium channel blockers, or beta-blockers; and in black patients. Results of these trials indicate that eplerenone lowers blood pressure and reduces end-organ damage. Further proof of the therapeutic importance of mineralocorticoid receptor blockade comes from the eplerenone post acute myocardial infarction survival and efficacy study (EPHESUS). In this large-scale clinical outcome trial, eplerenone was shown to reduce total mortality by 15% as well as the combined endpoint of cardiovascular mortality/cardiovascular hospitalization by 13% when administered at a mean of 7.3 days post myocardial infarction to patients with evidence of systolic left ventricular dysfunction and symptoms of heart failure. Eplerenone is well tolerated, with an adverse effect profile comparable to placebo. The advent of selective aldosterone blockers, such as eplerenone, should prove to be of great therapeutic value in hypertension control and prevention of cardiovascular disease and associated end-organ damage.

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Section: Chemistrymentioning

confidence: 99%

Eplerenone: A Selective Aldosterone Blocker

Stier

2003

Cardiovascular Drug Reviews

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“…Liquid chromatography with tandem mass spectrometry (LC-MS-MS) has been widely employed for the analysis of drug compounds in biological fluids because of its excellent specificity, speed, and sensitivity [5,6]. To our knowledge, LC-MS-MS method has not been applied for the determination of levodropropizine.…”

Section: Introductionmentioning

confidence: 99%

Rapid and sensitive liquid chromatography–tandem mass spectrometry method for the quantitation of levodropropizine in human plasma

Tang

Zhao

Wang

et al. 2005

Journal of Chromatography B

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“…exhibited a major product ion at m/z 163.5 as illustrated in Fig. 1B [11]. Therefore, the mass transitions chosen for quantification were m/z 433.4 → 373.3 for isoforskolin and m/z 415.3 → 163.5 for I.S., respectively.…”

Section: Mass Spectrometrymentioning

confidence: 99%